ABSTRACT

Diabetes Mellitus is a chronic metabolic disorder caused by the deficiency of the pancreatic hormone insulin (Type 1 DM) or due to the resistance of the peripheral cells to the insulin secreted by pancreatic β cells(Type 2 DM). It is characterized by chronic hyperglycaemia. The patients are associated with symptoms like polyuria, polydipsia and polyphagia.Type I Diabetes is normally controlled by diet restriction, exercise and insulin therapy. Type II Diabetes is treated with various oral hypoglycaemic agents in addition to dietary restriction and exercise. In severe cases exogenous supply of insulin is also used for therapy. Periodontitis is considered to be the 6th complication of diabetes mellitus. It is a group of inflammatory diseases affecting the supporting structures that surround the tooth. It causes inflammation of gum, loss of alveolar bone and destruction of periodontal ligament. Maintaining oral hygiene is the first step in controlling periodontitis. Chlorhexidine or listerine mouthwash is used commonly. The antibiotic of choice for the treatment is Doxycycline. Diabetes promotes periodontal infection and causes periodontitis. The proinflammatory cytokines produced in response to periodontal infection increase the insulin resistance and aggravate Diabetes. Thus diabetes and periodontitis share a bidirectional relationship. The severity of periodontitis is related to the glycaemic control of the patient and not to the duration of diabetes. Control of blood glucose level and maintenance of oral heath are really important in diabetes mellitus. This article reviews the relation between diabetes mellitus and periodontal health.

Keywords: Diabetes mellitus, periodontitis, hyperglycaemia, AGE, cytokines, bidirectional relationship

ABSTRACT

The Microsponge Delivery System (MDS) is a unique technology used for controlled release and prolonged topical administration. Due to the difficulty that arouse in the release of the active ingredient over an extended period of time the fundamental need for the Microsponge technology arouse. The MDS consists of macroporous beads typically 10 – 25 microns in diameter loaded with the active pharmaceutical ingredient. When applied to the skin the MDS releases its active ingredient on a time mode and also in response to different stimuli like rubbing, temperature, pH etc. This technology is currently being used in sunscreens, skin care, cosmetics and prescription products.  It offers entrapment of ingredients and is believed to contribute towards reduced side effects, improved stability, increased elegance and enhanced formulation flexibility. Innumerable studies have confirmed that microsponge systems are non irritating, non mutagenic, non allergic and non toxic. Microsponges are used mostly for topical drug delivery and have been recently used for oral administration and tissue engineering.

Keywords: Microsponge, Controlled release, Topical drug delivery.

ABSTRACT

In vitro-invivo correlation plays a key role in pharmaceutical development of dosage form, optimization of formulation. This articles describes about the regulatory criteria and the factors associated with developing an In-vitro and in-vivo correlation. This factors plays an important role in optimizing the design and protocol required fort development of any dosage form and to identify the bioavailability pattern of the dosage forms. This article provide information on the various guidelines, factors in developing the correlations, bio pharmaceutical classification system,and other applications.

Keywords: In Vitro In Vivo correlation, Food and Drug Administrations Factors, Bio pharmaceutical classification system.

ABSTRACT

Liver harm is most vital health issues or so a lot of than 900 medicines involved in case of liver injury. World health organization estimate that eightieth of total population used herbal drugs for some characteristic of primary health care while not any facet effects. Herbal medicine has emerged as a skilled approach with sensible values in handling various diseases, developing an affordable phytotherapy to treat severe liver diseases needs economical exploration of properties like antiviral action, antihepatotoxicity, stimulation of liver regeneration besides choleretic activity. The search used keywords such as herbal drugs, hepatoprotective effects, every crossed with the term drug elicited liver harm, with explicit stress on experimental models,  effective dose and hepatoprotective effects of those herbal preparations. The scientific basis for the statement that plants and their active constituents play a crucial role within the bar malady is endlessly advancing. The search result unconcealed twelve of the major herbs  active constituents having hepatoprotective  properties that area unit organic compound, flavonoids, glycoside, lignan, organ sulphur compounds, phenylethanoid organic compound, phenolic resin acids, polyprenols, poly phenols, quinine, resins and triterpenoid. The current review is aimed toward collecting information on promising active phytoconstituents from medicinal plants that are tested in hepatotoxicity models exploitation fashionable scientific system.

Keywords: Antioxidant, Biotransformation, Hepatotoxic, Hepatoprotective, Leads, Medicinal plants, Phytoconstituents

ABSTRACT

Ayurveda pharmacopeia is based upon herbal, mineral and herbo-mineral natural products but herbs takes first rank in pharmaceutics.  Herbal medicines have been widely used all over the world since ancient times and have been recognized by physicians and patients for their better therapeutic value as they have fewer adverse effects as compared with modern medicines. Unlike the existing allopathic system, the herbal remedies have hundreds and thousands of constituents that all work together against the diseases. Mostly, the conventional pharmaceuticals or pharmacognostical products in the market are rooted from natural products and their derivatives with herbal products playing pivotal role. All over the world, the research on these herbal remedies has been carried out in the different fields’ for instance pharmaceutical chemistry, pharmacognosy, pharmacology and clinical therapeutics.  ‘Nanotechnology’ is the new emerging technology in the drug discovery and it has the property of self targeting in the sense that without the attachment of a specific legend, these can be used for targeting, due to their distinctively small size, at the infected pathological areas. Some of such formulations are already present in the market and many more are expected to come by 2020 after their success in ongoing clinical trials. Drug delivery research is clearly moving from the micro- to the nanosize scale. Nanotechnology is therefore emerging as a field in medicine that is expected to elicit significant therapeutic benefit. Nanoparticles are able to adsorb and/or encapsulate a drug, thus protecting it against chemical and enzymatic degradation. A nanocarrier is nanomaterial being used as a transport module for another substance, such as a drug. Nanocarriers are currently used in drug delivery and their unique characteristics demonstrate potential use in chemotherapy. Herbal remedies may be selected as feasible drug candidate for delivery through a nano delivery system. It is being assumed that the “herbal remedy” with the nanocarriers will increase its potential for the treatment of various chronic diseases and health benefits. In this review, author has made an effort to explore this new approach is escalating the interest of number of scientists to improve and to accelerate the joint drug discovery and development of novel nano delivery systems for ayurveda herbal remedies.

Keywords: Natural products, Herbal remedies, Nanotechnology, Nanoparticles, Novel Drug Delivery  System

ABSTRACT

In present times, the pelletization technologies are giving much attention as they represent an efficient pathway for manufacture of new drug delivery system .It has good advantage over the conventional dosage form. Pelletization technique help in the formation of spherical beads or pellets having a diameter 0.5 -1.5 mm which can be eventually coated for preparation of modified release dosage form . It leads to an improvement in flow ability, appearance and mixing properties thus avoiding for generation of excessive dust and reduces segregation and remove the undesirable properties and improve the physical and chemical properties of fine powder. The aim of this study is to provide detailed and different techniques of pelletization such as powder layering, suspension /solution layering, extrusion and spheronization, cryopelletization, etc. It also gives a brief idea about the evaluation of pellets and application of pelletization technique.

Keywords : Pelletization, Extrusion, Spheronization, Cryopelletization

ABSTRACT

The controlled processes that provide functional integration between cells and organs are impaired in the elderly persons. As a result, there occur failures to maintain homeostasis under physiological stress conditions. In the advancing age, the important pharmacokinetic as well as pharmacodynamics properties are tremendously changed. In elderly patients failure to maintain the pharmacokinetic changes include decreased absorption of number of drugs, increase in volume of distribution of drugs, decrease hepatic and renal clearances where as pharmacodynamic changes involve usually altered sensivity to number of classes of drugs such as cardiovascular, anticoagulants and psychotropic drugs. The inappropriate medication use is a major health care issue for the elderly population. Beers criteria were developed in 1991 to define inappropriate medication use of elderly. By developing these new criteria, a clear picture emerged for a list of medications with questionable benefit and/or significant risk that should be avoided in older adults.

Keywords: Geriatrics, Pharmacokinetic, Pharmacodynamic Factors, Beers Criteria. 

ABSTRACT

The eye presents unique opportunities and challenges for the delivery of pharmaceutical dosage forms. Ocular inserts of Moxifloxacin HCl were prepared with the objective of reducing frequency of administration, controlled release and greater therapeutic effect. Moxifloxacin HCl a broad spectrum fourth generation fluroquinolone used in the treatment of conjunctivitis, keratitis, kerato-conjunctivitis etc. In the present wok reservoir type of ocular inserts formulated by sandwiching poly vinyl alcohol containing Moxifloxacin HCl in between two rate controlling membranes of ethyl cellulose and PVP-K30. The reservoir types of ocular inserts containing Moxifloxacin HCl were formulated by film casting technique using PVA as drug reservoir polymer and EC: PVP-K30 as a rate controlling material. In vitro drug release revealed that the optimized (FM₆) formulation showed a controlled release. In vivo studies showed a release of 97.67% over a period of 5 days with high correlation coefficient  of  In vitro-In vivo release studies. In the present study the ocular inserts of Moxifloxacin HCl (FM₆) provided desired drug release for 5 days and remained stable.

Keywords: Moxifloxacin HCL, Ocular inserts, In vitro drug release, Microbiological studies, Draize test, In vivo studies.

ABSTRACT

The aim and objective of the study was to formulate the matrix system of Loxoprofen sodium that has a very short plasma half-life of 1.15 hours. Natural hydrophilic polymers (Xanthan gum and Pectin) were used to formulate matrix system. These polymers were used to sustain the drug in the matrix system that allowed the slow release of the drug. Different concentration of Xanthan gum and Pectin were used, individually as well as polymeric blends. Wet granulation method was selected for the compression of granules into tablets of 350mg each. Both pre-compressional and post-compressional parameters showed good results. Dissolution studies carried out in distilled water and 0.1 N HCl for 12 hours.  Matrix system of Xanthan gum showed comparatively good sustained effects in both media with suitable drug released concentration. Kinetics of drug release was studies by different kinetics models and it was observed that Higuchi was the best fit model for F6 that released minimum drug from the matrix. Values of similarity index showed that F5 resembled with the reference formulation (F6). All the tablets showed good swellability upon hydration that was greatly related to polymers concentration.

Keywords: Loxoprofen sodium, Xanthan gum, Pectin, Matrix system.

ABSTRACT

Simple and precise UV- spectrophotometric methods, first order derivative and area under curve [AUC], have been developed and validated for the estimation of azelnidipine in bulk drug and its tablet formulation. The standard and sample solutions of azelnidipine were prepared in methanol. Azelnidipine was estimated at 242.6 nm for the first order derivative UV-spectrophotometric method (A) while in area under curve (AUC) method (B) the zero order spectrum of azelnidipine was measured in between 250.5 nm to 258.8 nm. Beer’s law was obeyed in the concentration range of 1 to 20 μg / ml with coefficient of correlation value 0.9993 for first order derivative method. Similarly in AUC method, Beer’s law was obeyed in the concentration range of 1 to 20 μg / ml with coefficient of correlation value 0.9991. These methods were tested and validated for various parameters according to ICH guidelines. The precision expressed as relative standard deviation, which was within the range of 0.1157 to 0.9995 % for the above two methods. The proposed methods were successfully applied for the determination of azelnidipine in pharmaceutical formulation. Results of the analysis were validated statistically and were found to be satisfactory. The proposed methods are simple, easy to apply, low-cost and require relatively inexpensive instruments.

Keywords:  Azelnidipine, Derivative spectroscopy, Area under curve method.

ABSTRACT

A simple accurate, precise and reproducible spectrophotometric method has been developed and validated for the simultaneous estimation of Paracetamol and Dicyclomine hydrochloride in combined tablet dosage form by Q-Absorbance ratio method. Q-Absorbance ratio method involves two wavelengths the iso-absorptive point and  λ_max of paracetmol i.e. 231.5 nm and 257 nm respectively in 6 : 4 ratio methanol: 0.1 N NaOH mixture.  The linearity was detected in the range of 2-12 µg/ml (R² = 0.9997) for Paracetamol and 10-35 µg/ml (R² = 0.9989) for Dicyclomine Hydrochloride. The accuracy existed between 98-102% and the %RSD was less than 2%. The developed method was validated for linearity, accuracy and precision as per ICH guidelines.

Keywords: Paracetamol, Dicyclomine hydrochloride, Q-Absorbance ratio method.

ABSTRACT

Hypochaeris radicata, an edible perennial herb is native of Europe has many medicinal uses which include antimicrobial, antioxidant, antiinflammatory and anticancer activities. The study was aimed at to investigate the phytochemical constituents present in the leaf and root extracts of H. radicata by thin layer chromatography. The results of the study revealed the presence of phytochemical constituents such as alkaloids, flavonoids, saponins, terpenoids and glycosides in the leaf and root extracts of this species. Further, the thin layer chromatographic profiles may serve as characteristic fingerprint for leaf and root extracts of H. radicata. It could be concluded that as the species, H. radicata contained rich variety of phytochemicals, it can be used for drug preparations in pharmaceutical industries.

Keywords: Hypochaeris radicata, Asteraceae, TLC, secondary metabolites.

ABSTRACT

The main objective of the study is to measure the appropriateness of antibiotic prescription for urinary tract infections in several general hospitals and to evaluate the quality of antibiotic prescription among these services. For this study a cross-sectional study was carried out in the various hospitals from different hospitals of north India. The patients were analyzed between the age group of 15-45 years. The main variables of the study were: type of urinary infection, hospital admission, antibiotic prescription, either the presence of one or more disorders and urine culture request. A panel of experts, established first-choice, second-choice and inappropriate antibiotic treatments for each type of urinary tract infection, based on the available scientific evidence. A total of 8500 patients were analyzed from acute urinary tract infected. Out of which 81-83% were lower urinary tract infected patients. The most commonly used antibiotics in hospitals were ciprofloxacin and Amoxicillin clavulinate. The percentages of first-choice, alternative-choice and inappropriate antibiotic prescriptions were: 43%, 44% and 14% respectively. This paper describes the first choice of drugs prescribed by the doctors. We observed a significant variability in appropriateness of antibiotic prescriptions among the participating centers (p < 0.001).

Keywords: Urinary tract infection, Antibiotic prescription, Ciprofloxacin and Amoxicillin clavulinate. 

ABSTRACT

To evaluate the anti-inflammatory and antioxidant potential of methanol extract of flowers of Salvia officinalis Linn. (MESO). Antioxidant activity and free radical scavenging activity of MESO has been evaluated by employing various in vitro models including reducing power, Total antioxidant activity, DPPH radical, ABTS  radical, superoxide radical (O₂^{• –}), nitric oxide, hydrogen peroxide, hydroxyl radical scavenging activity and metal chelating activity. Anti-inflammatory activity has been evaluated by carrageenan induced rat paw edema animal model. The plant extract (MESO) revealed significant antioxidant activity with lower IC₅₀ values. Metal chelating activity was found poor. In inflammation model, MESO demonstrated significant anti-inflammatory activity with maximum oedema inhibition at 3 rd hour post carrageenan injection. The results indicated that the plant could be a potential source of antioxidant and could find a use in the herbal therapy of inflammation also.

Keywords: Antioxidant, free radical, anti-inflammatory, Salvia

ABSTRACT

In the present research work nifedipine transdermal patch were prepared and optimized by using D-optimal mixture design. The prepared transdermal patches were evaluated for various parameters like drug excipients compatibility study, physicochemical evaluation, mechanical properties, In vitro drug release and In vitro permeation study. The result of evaluation parameters demonstrated a successful development of transdermal patch with poly vinyl pyrrolidone (PVP) and ethyl cellulose (EC) as rate controlling polymer.

Keywords: Transdermal, D-Optimal, Permeation

ABSTRACT

The objective of the present research was to develop and characterize an olive oil based oral microemulsion systems for famotidine, is a BCS class III drugs which are known to have high solubility but low permeability. An olive oil based microemulsion formulation with Tween-80 as surfactant, and PEG-400 as co-surfactant, was developed for oral delivery of famotidine. Pseudoternary phase diagram was constructed to determine the microemulsion existing zone. Optimized microemulsion was evaluated for its transparency, droplet size, polydispersity index, zeta potential, viscosity, conductivity, DSC studies, SANS studies. The results showed that maximum oil was incorporated in microemulsion system that was contained surfactant to co-surfactant ratio (Km) of 2:1. The optimized microemulsion formulation containing olive oil (7.14%), Tween-80 & PEG-400 [Smix=64.29% (2:1 ratio)], and distilled water (28.57%), had a droplet size (10 times diluted) and zeta potential (10 times diluted) of 170.1 nm and -6.58 mV respectively. Particle size characterization of the resulting microemulsion is essential in ensuring stability and efficient dosage. FTIR and DSC studies revealed the compatibility among the famotidine and microemulsion components. The experimental SANS data of optimized formulation fit well by spherical micelles interacting with hard sphere potential. These results demonstrate microemulsion formulation may be used as an effective and alternative drug delivery system for the antiulcer oral therapy with famotidine.

Keywords: Famotidine; BCS class III drugs; Olive oil; Pseudoternary phase diagram; Microemulsion

ABSTRACT

A novel buccal film can be applied to the oral mucosal surface which can be retained there for few hours, even where it is challenged with fluids. Polymers play an important role in designing such buccal films so as to increase the residence time of the active agent at the desired location. Hence the objective of our study was to optimize a suitable formula which comprises a best combination of polymers in suitable ratio to produce buccal film with desirable physical and mechanical properties. The study was carried out in chitosan film with three other different combination of polymers such as PVPK 30 (polyvinyl pyrolodine 30) PVPK 90 (polyvinyl pyrolodine 90) and HPMC (Hydroxy propyl methyl cellulose) at various concentrations. The effect of each concentration of the particular polymer in combination with the other polymers in making buccal film by solvent casting method was evaluated through twelve different batches of buccal film like F1,F2,F3,F4,F5,F6,F7,F8,F9,F10,F11,andF12.The physical and mechanical properties of formulated films were studied in terms of its appearance, texture, average weight, thickness, folding endurance, swelling index, surface pH, tensile strength, percentage elongation and bioadhesive strength. Overall results of our investigation reveals that the combination of PVPK30 at a concentration of 0.6%w/v with 1% concentration of chitosan is found to be effective in producing film with better bioadhesiveness and further addition of 0.2% of HPMC with 0.4% PVPK90 to this combination could enhances its elastic properties without having any added effect on its bioadhesive strength. 

Keywords: Buccal film, effect of polymers, evaluation of mechanical and physical property. 

ABSTRACT

The present study was made an attempt to optimize the growth parameters of the halobacteria for the mass scale production of carotenoids. The results suggested that, the pigmented KP2 showed maximum carotenoids production at 40ºC, 20% NaCl, pH 7, 1.5% sucrose, 1% beef extract, 1.5% manganese chloride and 1.5% proline. The KT2 showed maximum carotenoids production at 30ºC, 20% NaCl, pH 7, 0.5% glucose, 1.5% beef extract, 0.5% manganese chloride and 1% proline. Moreover, the KT3 showed maximum carotenoids production at 20ºC, 20% NaCl, pH 7, 1.5% sucrose, 0.5% beef extract, 1.5% copper sulphate and 0.5% proline. The identification of individual carotenoids was done by using thin layer chromatography through standard R_f value and the results suggested that, all the pigmented halobacteria contains three different carotenoids viz., bacterioruberin, mono-anhydrobacterioruberin and squalene. It is concluded from the present study that, the optimization of the microbial growth parameters of the halobacteria isolated from the saltpan of Kanyakumari district could be used for the mass scale production of pigmented carotenoids. 

Keywords: Carotenoids, Halobacteria, Optimization, Pigments, Saltpan

ABSTRACT

A simple UV-Visible spectrophotometric method is developed for the simultaneous determination of Ebastine and Phenylephrine hydrochloride in pharmaceutical dosage form using  the  first order derivative spectrophotometric method. The determination of both the drugs is based on the respective zero crossing point (ZCP) of their first order derivative spectra obtained in methanol. The first order derivative spectra were obtained using methanol as a solvent and the determinations were made at 241.0 nm (ZCP of Phenylephrine HCl) for Ebastine and 232.0 nm (ZCP of Ebastine) for Phenylephrine hydrochloride. The linearity was obtained in the concentration range of 4-24 μg/ml for both drugs and correlation coefficient (r²) were found to be 0.9994 and 0.9991 for Ebastine and Phenylephrine hydrochloride respectively. The percentage purity of drugs in combined tablet dosage form was found to be 100.02 % for Ebastine and 99.89 % for Phenylephrine hydrochloride. The % recoveries were found to be 99.88% for Ebastine and 99.24% for Phenylephrine hydrochloride.  The method was found to be simple, accurate and precise and was applicable for the simultaneous determination of Ebastine and Phenylephrine in tablet dosage form.

Keywords: Ebastine (EBS), Phenylephrine hydrochloride (PHE), recovery, first order derivative spectrophotometric method, validation.

ABSTRACT

More than 90 countries have given the artificial sweetener aspartame the green light to be used in thousands of food and beverage products. The artificial dipeptide sweetener aspartame [APM; L- aspartyl-L- phenylalanine methyl ester] is present in many products especially unsweetened and sugar products. These products are frequently utilized by people trying to lose weight or patients with diabetes. Concern relating to the possible adverse effect has been raised due to aspartame^s metabolic components. Aspartame is rapidly and completely metabolized in humans and experimental animals to aspartic acid (40%), phenylalanine (50%) and methanol (10%). Methanol, a toxic metabolite is primarily metabolized by oxidation to formaldehyde and then to formate these processes are accompanied by the formation of superoxide anion and hydrogen peroxide. This study focus is to understand whether the oral administration of aspartame (40 mg/kg b.w.) for 90 days, have any effect on membrane bound ATPase’s, antioxidant status and immune response (cell and humoral) of rats. To mimic human methanol metabolism, folate deficient rats were used. After 90 days of aspartame administration, shows free radical production by a significant increase in LPO and nitric oxide (NO) level and decrease in both enzymatic and nonenzymatic antioxidant level which alters the immune response. This study concludes that oral administration of aspartame (40mg/kg b.w) for longer duration may cause oxidative stress on immune organs and altered the immune response (cell and humoral) in wistar albino rats.

Keywords: Aspartame, LMI, FPT, immunization antioxidant, immune organs.

ABSTRACT

To evaluate phytochemical constituents and antioxidant potential of methanol aerial parts (leaf and stem) extract of Mentha arvensis L from Kashmiri Himalaya region. The extract shows the presence of flavonoids, saponins, alkaloids, steroids, carbohydrates, proteins, tannins and phenolics. The antioxidant activity of methanol aerial extract of Mentha arvensis L was evaluated by using 1,1-diphenyl, 2-picrylhydrazyl (DPPH) scavenging and reducing power assays. The total phenolic and total flavonoid content (mg/g) was found to be 672.11 and 283.1 respectively. The percentage inhibition of DPPH scavenging was found to be 81.33% at concentration of 0.5mg/ml. The reducing power was found to be 0.76 at 0.1mg/ml and increased to 2.42 at 0.5mg/ml. The results obtained revealed that methanol extract from aerial parts of Mentha arvensis L can be promising candidates for natural sources of antioxidants with high activity. 

Keywords: Mentha arvensis; DPPH; antioxidant potential; reducing power; phenolics; flavanoids.

ABSTRACT

This study was performed to evaluate the In vitro antimicrobial activity of entire parts of aqueous and methanolic extracts of Sphaeranthus amaranthoides Burm. The antimicrobial activities of medicinal plant extracts used for the treatment of parasitic diseases were examined with four bacteria – two from Gram positive group (Bacillus subtilis and Staphylococcus aureus) and rest two from Gram-negative group (Escherichia coli and Salmonella typhi) following disc diffusion method. The methanolic extract revealed antibacterial activity more than the aqueous extract. Both the extracts showed less activity against Bacillus subtilis and where as Salmonella typhi no inhibition (NI). It showed more activity on Escherichia coli compared to standard. Both the extracts showed minimum inhibitory concentration (MIC) of 25mg/ml on Bacillus subtilis and 12.5mg/ml on Staphylococcus aureus. Totally the methanolic and aqueous extracts of Sphaeranthus amaranthoids showed good anti bacterial activity. Phytochemical screening revealed the presence of steroids, alkaloids, sugars, phenolics, flavonoids, saponins, tannins and amino acids with mottled degree

Keywords: Anti bacterial, Phytochemical screening, Methanolic, Sphaeranthus amaranthoides Burm, Disc diffusion

ABSTRACT

The present study was undertaken for the development of physicochemical and phytochemical parameters of the roots of Paederiafoetida [Linn] Belonging to the family, Rubiaceae. The plant commonly known as skunk vine is a perennial climber, in Sanskrit as Prasarni, in Marathi  as Hiranvel, in Hindi as Gandha Prasarini, in English as Chinese flower plant. The physicochemical and phytochemical investigation confirms the purity and authenticity of Paederiafoetidaroots by using standard methods. The physicochemical studies revealed the presence of moisture content as 6% w/w, total ash as 8.75 %w/w, acid insoluble ash as 1.1%w/w, water soluble ash as 1.8%w/w, alcohol soluble extractive as 9.8%w/w, water soluble extractive as 9.2%w/w, ether soluble extractive as 2.4% w/w, foaming index as less than 100 and swelling index as 1.7cm. The fluorescence analysis in short wavelength, long wavelength and day light is also reported, which is a tool to determine the chemical nature of crude drug. Preliminary phytochemical screening of the ethanolic extract of the roots revealed the presence of alkaloids, glycosides, carbohydrates, triterpinoids, steroids, tannins and resins. All these methods will help in setting down pharmacopoeial standards in determining the quality and purity of the Paederiafoetida roots.

Keywords: Paederiafoetida, Rubiaceae, Fluorescence, Physicochemical, Phytochemical.

ABSTRACT

An isocratic, reversed phase-HPLC method was developed and validated for the quantitative determination of Ofloxacin and Ketorolac Tromethamine in combined-dosage form. A thermo hypersil BDS C18 (250mmx4.6mm, particle size 5µm) column with mobile phase containing water (p^H - 2.8 adjusted with ortho phosphoric acid) and methanol in the ratio of 60: 40, v/v was used. The flow rate was 1.0 mL/min, column temperature was 30°C and effluents were monitored at 241 nm. The retention times of ofloxacin and ketorolac tromethamine were 4.671min and 5.751 min respectively. The correlation co-efficient values for both the ofloxacin and Ketorolac tromethamine were found to be 1. The proposed method was validated with respect to linearity, accuracy, precision, specificity, and robustness. Recovery of ofloxacin and Ketorolac tromethamine in formulations was found to be 100% confirms the non-interferences of the excipients in the formulation. Due to its simplicity, rapidness and high precision, the method can be successfully applied to the estimation of Ofloxacin and Ketorolac tromethamine in combined dosage form.

Keywords: RP-HPLC, Ofloxacin and Ketorolac Tromethamine.

ABSTRACT

Developments in the recent past on teaching the students by using audio visual aids such as power point presentation, over head projector and virtual teaching have improved learning process. However, still a few teachers follow the traditional method of teaching with chalk and board. The present survey is an attempt to know the opinion of the 132 medical students (3^rd semester) about the use of chalk and board while teaching. A questionnaire was given to students seeking their view on the utility of lecture, voice modulation, eye contact of the teacher and use of chalk and board. It was observed from survey results that 65.15% of students expressed satisfaction with regard to understanding of subject. Surprisingly 60.6% of students preferred the traditional method of teaching of chalk and board while only 34.4% of students preferred power point presentation. The participants also felt that while using chalk and board the eye contact and classroom management were effective. It is concluded that the traditional chalk and board method of teaching is still accepted by the students.

Keywords: chalk and board, teaching, power point presentation, medical students.

ABSTRACT

Phenylene-1, 4-oxy-bis-hydantoins have been synthesized from 5-bromohydantoin and substituted quinol (1,4-dihydroxybenzene) in the presence of K₂CO₃ in dioxane. The structures of newly synthesized compounds have been established on the basis of IR, NMR and Mass spectral data. These compounds were screened for their antibacterial activity against gram +ve and gram – ve bacteria. This phenylene-1, 4-oxy-bis-hydantoins are so far not reported in literature.

Keywords: Hydantoin, bis-hydantoin, quinol, anticonvulsant

ABSTRACT

A simple, economic, selective, precise, and accurate High Performance liquid Chromatographic method for the analysis of Furazolidone in bulk drug and pharmaceutical formulations was developed and validated in the present study. The mobile phase consists of a mixture of potassium dihydrogen phosphate and acetonitrile 80:20. And Adjust pH 6.50±0.1 with dilute potassium hydroxide solution. This was found to give a sharp peak of Furazolidone at a retention time of 4.245 min. HPLC analysis of Furazolidone was carried out at a wavelength of 354 nm with a flow rate of 1.0 mL/min. The linear regression analysis data for the calibration curve showed a good linear relationship with a regression coefficient (r²) of 1 in the concentration range of 25 to 150 µg ml^-1. The linear regression equation was y =46002x+40407. The developed method was employed with a high degree of precision and accuracy for the analysis of Furazolidone. The developed method was validated for accuracy, precision, robustness, detection and quantification limits as per the ICH guidelines.  The wide linearity range, accuracy, sensitivity, short retention time and composition of the mobile phase indicated that this method is better for the quantification of Furazolidone.

Keywords: Furazolidone, HPLC, Validation.

ABSTRACT

Strobilanthes barbatuscommonly known as Suruli mammuni belonging to the family acanthaceae is found in the hills in tropical Asia of which 150 speciesof this familyare distributed in the Indian subcontinent.The important characteristic feature of members in this family is that they show a phenomenon called MASTINGie.synchronous production of seed at long intervals by a population of plants. Strict masting only occurs in species that are monocarpic in which individuals of the species only reproduce once during their life time, and then die. The extraction was carried out by cold extraction using two solvents such as petroleum-etherand hydro alcohol according to the increasing order of polarity. The qualitative phyto-chemical screening showed the presence of Phytosterols,triterpenoids and saponinsin petroleum-ether extract andSaponinsand tanninsin hydro alcoholic extract. Antioxidant study was performed byDPPH methodand Nitric Oxide scavenging method in the above two extracts and comparative study was also done. The study was performed by taking various concentrations of the two extracts ranging from 12.5, 25, 50,100,200µg/ml.The results showed a positive response as compared with the standard ascorbic acid. The comparative study of antioxidant activity in the two extracts shows that petroleum–ether extract shows better antioxidant activity than hydro alcoholic extract.

Keywords: Strobilanthes barbatus, acanthaceae, masting, Petroleum-ether, Hydro alcohol, DPPH method, Nitric oxide scavenging activity.

ABSTRACT

The novel compounds containing two phenyl rings at 3, 5 position of 1, 2-pyrazoline sulphonamide derivatives synthesized. N-((3-(4-aminophenyl)-5-(3,4-disubstitutedphenyl)-4,5-dihydropyrazol-1-yl)methyl)benzenamine screened  for Angiotensin II receptor antagonistic activity  in  1K-1C goldblatt hypertensive rats using tail cuff method. N-((3-(4-aminophenyl)-5-(3,4-dichlorophenyl)-4,5-dihydropyrazol-1-yl)methyl)benzenamine sulphonamide exhibited potent antihypertensive activity.

Keywords: 1,2-pyrazoline, sulfonamide, angiotensin II, antihypertensive

ABSTRACT

A simple, precise and sensitive reverse-phase high performance liquid chromatographic method was developed and validated for the simultaneous estimation of Ofloxacin and Flavoxate Hcl in pharmaceutical formulations. Chromatographic separation was performed on a High performance liquid chromatography equipped with auto sampler and UV detector. Good sensitivity for all analyte was observed with UV detection at wavelength of 301 nm, Separation was performed on a BDS Hypersil C18 (250 X 4.6mm) 5µm,using a mixture of 0.1% Triethyl Amine buffer pH 4 and Acetonitrile in the ratio of (40:60, v/v). The method results in excellent separation with good resolution between the two analytes. The within day variation between Ofloxacin and Flavoxate Hcl 1.72 and 1.97 % . The recovery was greater than 95 % with RSD less than 1.95 %. The method was validated according to ICH guidelines by performing linearity, accuracy, precision, limits of quantitation and selectivity. The results show the method is suitable for its intended use.

Keywords: Ofloxacin (OX), Flavoxate HCl (FX), HPLC, Simultaneous determination.

ABSTRACT

Para hydroxyacetophenones react with different aldehydes of Para nitro benzaldehyde (Ia) ,Ortho nitro  benzaldehyde (Ib),4 hydroxy 3methoxy benzaldehyde (Ic) , 3, 4 dimethoxybenzaldehyde (Id)  in the presence of aqueous solution of potassium hydroxide and ethanol at room temperature to form 1,3 Diaryl-2-propane-1-ones or chalcones. The synthesized compounds were characterized by means of their IR spectral data. All the compounds were tested for their antibacterial activities by the cup plate method on E.coli ,Pseudomonasaeurgenosa, staphylococcus aeureous .Screening results shows that Id compound shows better antimicrobial activity against E.coli

Keywords : Anti microbial agent, chalcone, synthesis.

ABSTRACT

An efficient synthesis of N-glucosylated 1, 2, 4-dithiazolidines from 1-arylidene-4-arylthiosemicarbazides and N-tetra-O-acetyl-β-D-glucopyranosylimino chloromethane sulphenyl chloride has been worked out. 1-Arylidene-4-arylthiosemicarbazides were synthesized by reacting different aryl/hetero aryl aldehydes/ketones with 4-arylthiosemicarbazides. The identities of new glucosylated heterocycles have been established on the basis of usual chemical transformation, IR, NMR and mass spectral studies. The final compounds were screened for biological activity against different bacterial strains.

Keywords: N-glucosylated 1,2,4-dithiazolidines, 1-arylidene-4-arylthiosemicarbazides, 4-arylthiosemicarbazides

ABSTRACT

The present study investigated the hepatoprotective activity of methanolic rhizome extract of Curculigo orchioides (MECO) in CCl₄-induced hepatotoxicity model in rats. The hepatoprotective activity of methanolic rhizome extract of Curculigo orchioides were evaluated against CCl₄-induced hepatic damage in rats. The three doses of MECO (100, 200 and 400 mg/kg) were administered orally once daily for seven days. Serum glutamate oxaloacetate transaminase (AST), serum glutamate pyruvate transaminase (ALT), serum alkaline phosphatase (ALP) and total bilirubin were estimated along with the estimation of superoxide dismutase (SOD) and malondialdehyde (MDA) levels in liver tissues. Further histopathological examination of the liver sections was carried out to support the induction of hepatotoxicity and hepatoprotective efficacy. The extract revealed significant activities and substantially elevated serum enzymatic levels of AST, ALT, ALP and total bilirubin were found to be normalized significantly by the MECO in a dose dependent manner with maximum hepatoprotection observed at 400 mg/kg dose level. The histopathological observations also indicated the biochemical evidences of hepatoprotection. Elevated level of superoxide dismutase (SOD) and decreased level of malondialdehyde (MDA) further affirmed the hepatoprotective observations. The results of the present study demonstrated that MECO have potent hepatoprotective activity against CCl₄-induced hepatic damage in experimental animals.

Keywords: hepatoprotective, antioxidant, carbon tetrachloride, Curculigo orchioides, Silymarin

ABSTRACT

More than 90 countries have given the artificial sweetener aspartame the green light to be used in thousands of food and beverage products. The artificial dipeptide sweetener aspartame [APM; L- aspartyl-L- phenylalanine methyl ester] is present in many products especially unsweetened and sugar products. These products are frequently utilized by people trying to lose weight or patients with diabetes. Concern relating to the possible adverse effect has been raised due to aspartame^s metabolic components. Aspartame is rapidly and completely metabolized in humans and experimental animals to aspartic acid (40%), phenylalanine (50%) and methanol (10%). Methanol, a toxic metabolite is primarily metabolized by oxidation to formaldehyde and then to formate these processes are accompanied by the formation of superoxide anion and hydrogen peroxide. This study focus is to understand whether the oral administration of aspartame (40 mg/kg b.w.) for 90 days, have any effect on membrane bound ATPase’s, antioxidant status and immune response (cell and humoral) of rats. To mimic human methanol metabolism, folate deficient rats were used. After 90 days of aspartame administration, shows free radical production by a significant increase in LPO and nitric oxide (NO) level and decrease in both enzymatic and nonenzymatic antioxidant level which alters the immune response. This study concludes that oral administration of aspartame (40mg/kg b.w) for longer duration may cause oxidative stress on immune organs and altered the immune response (cell and humoral) in wistar albino rats.

Keywords: Aspartame, LMI, FPT, immunization, antioxidant, immune organs.

ABSTRACT

Obesity and its comorbidities represent major concern worldwide, so the aim of the current study is to investigate the prevalence of obesity and the use of weight loss medication in Saudi populations. A community-based, cross-sectional survey, conducted in Jeddah, Saudi Arabia from September to November 2013. Enrolled participant was asked to complete a self-administered questionnaire; the questionnaires were distributed to friends, relatives, and governmental sector hospitals. Body mass index (BMI) was used as an obesity indicator. A total of 312 participants were enrolled, 262 participants were included. The prevalence rate of overweight and obesity in the present study were 26% and 16.1%, respectively. Overweight and obesity prevalence were showed in age (36-45years) (34.6% and 42.2%), respectively. Surprisingly, 47.2 % of bachelor carriers did not know their IBW and 66.6% of participants with above bachelor degree were wrong about their IBW. 48.8% of the participants had no family history of obesity. Additionally, the current study showed that 22.5% had chronic diseases, 5% of them had diabetes. Regarding the use of weight loss managements, only 10% of the participants used pharmacological treatments, 25% used herbs and only 1.5% underwent a bariatric surgery. The current study revealed an increase in the prevalence of overweight and obesity among study participants that indicates the necessity of more population's education and governmental cooperation to increase the community awareness for the importance of doing physical activity and cut off dietary risk factors.

Keywords: obesity, weight loss medications, questionnaire, body mass index, Saudi Arabia

ABSTRACT

This research manuscript describes simple, sensitive, accurate, precise and repeatable reverse phase high performance liquid chromatography method for the estimation of Chlorhexidine gluconate in mouthwash. The sample was analyzed by reverse phase ACE 5 C18 column (150 mm × 4.6 mm i.d, 5 μm particle size) as stationary phase; acetonitrile : methanol : triethyl Amine (0.1 %) PH 3.0 (22: 49: 29, v/v/v) as a mobile phase at a flow rate of 0.8 ml/min. Quantification was achieved with Photo Diode Array detector at 258 nm. The retention time for chlorhexidine gluconate was found to be 2.477 min. The linearity was obtained in the concentration range of 10 -80 µg/ml for chlorhexidine gluconate. The method was successfully applied to mouthwash because no chromatographic interferences from formulation excipients were found. The method retained its accuracy and precision when the standard addition technique was applied.

Keywords: Chlorhexidine gluconate, RP-HPLC, Method validation.

ABSTRACT

Andrographolide is a diterpene lactone present in aerial parts of Andrographis paniculata especially in the leaves. It was reported to possess a wide variety of bioactivities. In the present research immunomodulatory effects of pure andrographolide have been studied on chicken spleenocytes in vitro. The immunological intervention of andrographolide was assayed using Nitro Blue Tetrazolium dye reduction assay, Inducible Nitric Oxide Synthase assay and Macrophage function test. Cytotoxic effects of andrographolide  on spleenocytes were tested using MTT assay. Andrographolide suppressed Nitro Blue Tetrazolium dye reduction assay response at all experimental concentrations. 45% reduction in immune response was observed when spleenocytes were treated with andrographolide at a concentration of 40µg/ml. The overall Inducible Nitric Oxide Synthase assay response of spleenocytes get decreased with incorporation of andrographolide in media. It was observed that when spleenocytes were mitogenically stimulated in presence of Covcanavalin A and Phytohaemagglutinin ,the suppression of Inducible Nitric Oxide Synthase assay response was observed. Andrographolide was found to enhance the phagocytic ability of spleenocytes upto 10 folds. It was found to be nontoxic at the concentration of 40µg/ml and 96% of spleenocytes remained viable as estimated by Trypan blue dye exclusion method. It was found to have immunosuppressive properties and it can be used to treat inflammatory disorders such as allergies, rheumatoid arthritis etc.

Keywords: Andrographolide, Cytotoxicity, Spleenocytes, Mitogens, Immunosuppression.

ABSTRACT

Rapid, accurate, precise and economical UV-Visible spectrophotometric methods were developed for the determination of Oxalamine phosphate (OMP) in bulk and pharmaceutical formulations. These methods (Method-A and Method-B) were based on the formation of colored complexes with Iron (III), o-Phenonthroline (M-A) and Cobalt thiocyanate (M-B). The absorbance concentration of plots were linear over the concentration range 10-60µg/ml (Method-A) and 4-24 µg/ml (Method-B) respectively for both methods with a minimum detection limit (LOD) of 2.059 µg/ml (Method-A) and 0.106 µg/ml (Method-B), limit of quantification (LOQ) of 6.240 µg/ml (Method-A) and 3.240 µg/ml (Method-B) respectively. The absorbance was measured at 482 and 620 nm with use of the cited reagents, respectively. The reactions were extremely rapid at room temperature and absorbance values remain unchanged up to 18hrs. Recoveries were 97.90-102.06%. Interferences of the other ingredients and excipients were not observed. The proposed methods are simple and sensitive and this is the first reported complexometric methods for the determination of Oxalamine phosphate (OMP) in commercial tablets.

Keywords: UV-Visible Spectrophotometry; Oxalamine phosphate; o-Phenonthroline; Cobalt thiocyanate

ABSTRACT

A clean and efficient route was established to synthesize sulfonamido-thiocarbamides via one-pot reactions in aqueous medium without use of a catalyst and/or organic solvent. The reaction with stoichiometric molar portion could be carried out in an open atmosphere to offer sulfonamido-thocarbamides in good to excellent yields and purities. The novel and clean methodology offers the advantages including short reaction time, excellent yields, operational simplicity, less leaks and environmentally benign path. The identity of newly synthesized compounds is based on elemental and spectral data. They have been further screened for their microbiological activities.

Keywords: Thiocarbamide, Antibacterial and anti-fungal activity, sulfonamido-thiocarbamides.

ABSTRACT

Asokarishtam, prepared using the bark of Asoka (Saraca asoka (Roxb.) de.wilde) is widely used in the management of uterine diseases. The scarcity of genuine Asoka bark is a problem facing by the ayurvedic industries and alternative to it without affecting the efficacy has become an urgent requirement. The present study explores whether leaf of Saraca asoka (Roxb.) de.wilde is an appropriate alternate for the bark of Saraca asoka (Roxb.) de.wilde. The physicochemical and phytochemical analysis were performed using standard procedures. The total phenolic content was determined using Folin-ciocalteu’s method, tannin content by Folin-Denis Method, flavonoids by Aluminium chloride colorimetric method and radical scavenging activity by 2’2-diphenyl-1-picryl hydrazine method. Thin layer chromatographic profiling was also performed on precoated silica gel aluminium plate. The physicochemical and phytochemical analysis of Asokarishtam with leaf  and Asokarishtam with bark  do not show any significant variation. The total phenolic content (6.47 %, 7.33 %), tannin content (6.02 %, 5.79 %), flavonoid content (0.775 %, 0.786 %) and radical scavenging activity (20 µg/ml, 18 µg/ml)    of both Asokarishtam with leaf and bark are comparable. Thin layer chromatographic profiling shows similar Rf in Asokarishtam with leaf and bark. From this study it is concluded that there is a probability of substituting leaf of Saraca asoka (Roxb.) de.wilde for its bark. Activity evaluations including In-Vivo and Toxicological studies are proposed before confirming the usage of leaves for the bark in the preparation of Asokarishtam.

Keywords: Saraca asoka (Roxb.) de.wilde, Asokarishtam, bark, leaf

ABSTRACT

The Idea of Study is to check the effectiveness and impact of lacquer coating quality after post fabrication and printing process. The porosity test is used to check the uniformity of lacquer in collapsible tube, after internal lacquering there are various methods left to make final printed tube (ref flow chart 1). During these processes the collapsible tube may get minor damage that may damage the uniformity of internal lacquer coating. Since uniform lacquer coating is very important for product compatibility and quality for long term study and use. Hence this study has done on printed and unprinted lacquered tube to see the porosity uniformity of lacquer. After observation, data study (Nos. of dark spot deposition) we can not found any major difference in dark spot generation (porosity test) for both type of tube. Also we kept one drug product in both printed and unprinted tube after two month study there is no significance difference observed during stability.

Keywords: Collapsible tube, Lacquer coating, Impact extrusion process, porosity test, Electrolytic Deposition, Cupper deposition.

ABSTRACT

A novel stability indicating RP-HPLC method was developed for simultaneous estimation of Ethylhexyl triazone and Bemotrizinol in sun care formulations. Separation of Ethylhexyl triazone, Bemotrizinol and their degradation products was achieved on Waters symmetry C18 (150 × 3.9 mm, 5µ) as stationary phase and mixture of pH 4.50 ammonium formate buffer and 1,4-dioxane (20:80, v/v) as mobile phase. Both analytes were simultaneously measured at UV detection of 311 nm. Method was validated for specificity, method precision (Intra-day and inter-day), linearity, accuracy and robustness as per ICH guideline. Ethylhexyl triazone and Bemotrizinol were linear in the concentration range of 0.10-225 µg/mL and 0.12-225 µg/mL respectively with correlation coefficient of > 0.999. This method can be utilized in cosmetic industries to monitor both analytes in sun care formulations to assure the quality of the products.

Keywords: Ethylhexyl triazone, Bemotrizinol, Stability indicating

ABSTRACT

Carbamazepine; an antiepileptic drug, exists in various polymorphic forms out of which Form III is extensively studied as a model  form for  cocrystallization. The main focus of the present study was to cocrystallize Carbamazepine form III with Itaconic acid as a coformer by solvent evaporation technique using Acetone (Class III) as the solvent medium for drug and coformer interaction at molecular level. The obtained Carbamazepine cocrystals were evaluated for parameters like Visual morphology, differential scanning calorimetry, infrared spectroscopy, x-ray diffractometry, contact angle, drug content uniformity, flow properties and in vitro drug release testing. A comparison of the cocrystal characteristics was made with a physical mixture of Carbamazepine with itaconic acid inorder to confirm an interaction at a molecular level between the drug and coformer. The obtained carbamazepine cocrystals showed distinct difference in its morphological characteristics as compared to plain drug. Additionally, the cocrystals showed presence of additional peaks in differential scanning calorimetry thermograph as well as bandshifts in the infrared spectrum. The X-Ray diffractogram of cocrystals was found to show a shift towards left thus confirming a change in the crystal lattice. In vitro drug release testing of cocrystals showed an increase in drug release when compared to drug release from physical mixture and plain drug when tested in 1% Sodium lauryl sulphate. Hence Solvent evaporation technique was found to be successful in producing cocrystals of Carbamazepine polymorph III with Itaconic acid as a coformer.

Keywords: Carbamazepine, Itaconic acid, solvent evaporation, coformer, cocrystal, polymorph

ABSTRACT

Breast cancer comprises a diverse collection of diseases rather than a single homogeneous disease. Both preclinical and clinical research now commonly target specific subgroups of breast cancer with the aim of identifying biological markers or genetic phenotypes, and to reveal subgroup-specific therapeutic targets or indicators of prognosis. Since genetics is believed to account for only 10% of the reported cases, the environmental factors including diet are thought to play a significant role in predisposing breast cancer. The present study was aimed to evaluate the chemotherapeutic potential of taurine in 7, 12-dimethyl Benz (a) anthracene (DMBA) induced mammary carcinoma in rats. Oral treatment of taurine (100 mg/kg BW) to breast tumor bearing rats daily for ten to fifteen weeks was found to be effective against DMBA induced mammary gland carcinogenesis in female Sprague Dawley rats. The increased activities of 5′-ND, GGT and LDH in tissue of control and experimental breast cancer rats were significantly (p < 0.05) decreased to near normal levels. Thus, the results of the present study clearly indicate that taurine significantly suppresses DMBA induced breast cancer in rats.

Keywords:  Breast cancer, 5’ND, GGT, LDH, Taurine. 

ABSTRACT

The present study was carried out with an objective to formulate modified dosage form of Clopidogrel bisulfate. Clopidogrel bisulfate is available in the form of oral immediate release tablets. It is modified into both pharmaceutical aqueous injection and oral solid floating tablet formulations.  In-vitro and in- vivo evaluation of both the formulations were evaluated. The aqueous injection comprises solubilizer and aqueous solvent. Floating tablet were formulated in different ratio’s of natural based swelling polymer Swelstar MX-I. The floating tablets were based on effervescent approach using sodium bicarbonate as gas generating agent. The effect of polymers concentration on drug release profile was evaluated. The formulations containing sodium bicarbonate 34 mg per tablet provided desired buoyancy (floating lag time of about 2 minutes and total floating time of >24 hours). The in –vivo study on rabbits to see the effect of bleeding time, clotting time, platelet count and partial thromboplastin time were investigated. The results indicates that the bleeding time of clopidogrel floating tablets exhibited effect upto 12 hrs and the effect was maintained for 24 hours compared to reference product. The IV bolus solution showed maximum bleeding time in 1 hr and than decreased significantly as compared to normal control. No significant change in mean platelt count was observed. The clotting time of treated groups significantly increased in test formulation group as compared to normal group upto12 hours but regains to baseline in 24 hours.

Keywords: Aqueous injection, Floating tablet, Swelstar MX-I, Bleeding time

ABSTRACT

Pyrolysis has shown that the polymetallic chelates of naphthazarin with Co(II), Ni(II) and Cu(II) assumed compositionally defined structures as [(C₁₀H₆O₄)(M)₂xH₂O]yH₂O where M stands for Co(II)/Ni(II)/Cu(II), x = 04, 04, 00, (coordinated water), y = 3, 1_1/2, and 4, (lattice water) respectively satisfying the metal ligancy. Each crystal of polymetal chelate assumed cubic symmetry with forbidden number 7, 15, 23 etc being absent. The inter planer spacing d (A⁰), a A⁰ (cell unit), of ρ g/cc and molecular weights of the polymetal chelates have been determined and reported. The calculated formula weight showed correspondence to the found molecule weight of each of the polymetal chelate.

Keywords; Pyrolysis, Naphthazarin, Cubic, Crystallographics, X-ray

ABSTRACT

Two sensitive, precise and cost-effective UV-spectrophotometric methods are described for the determination of flunarazine dihydrchloride (FNH) in bulk drug and tablets. The proposed methods are based on the measurement of the absorbance of FNH either in 0.1 M HCl (method A) or in acetonitrile (method B) at 253 nm. As per the International Conference on Harmonization (ICH) guidelines, the methods were validated for linearity, accuracy, precision, limits of detection (LOD) and quantification (LOQ) and robustness and ruggedness. Beer’s law is obeyed over the concentration ranges of 2.5-30.0 µg mL^-1 in method A and 1.0-20.0 µg mL^-1 in method B. The calculated molar absorptivity values are 2.12×10⁴ and 2.47×10⁴ L mol^-1 cm^-1 for method A and method B, respectively. The proposed methods were applied successfully to the determination of FNH in tablets with good accuracy and precision without any detectable interference from common excipients. The accuracy of the proposed methods was further assessed by the recovery studies via a standard addition method. In addition, forced degradation of FNH was conducted in accordance with the ICH guidelines. Acidic and basic hydrolysis, thermal stress, peroxide and photolytic degradation were used to assess the degradation behavior of the drug. Substantial degradation was observed during oxidative degradation and no degradation was observed under other stress conditions.

Keywords: Flunarazine dihydrchloride, degradation studies, spectrophotometry, pharmaceuticals.

ABSTRACT

Staphylococcus aureus is associate with variety of clinical infections in various communities and healthcare institutions both in developed and developing countries. It produces extracellular enzymes like lipase, protease and lecithinase that degrade lipid, proteins present in the skin environment. Study was conducted to associated virulence factors in clinical isolates of S. aureus and to evaluate the incidence of β lactamase production. It comprised 271 clinical samples (pus from surgical, burn, ulcer, abscess and sputum from hospitals of Allahabad. S. aureus was isolated and identified by conventional culture followed by biochemical tests including coagulase test. β-lactamase test and antibiotic susceptibility tests were performed for all isolates.

Among 59 isolates of S. aureus, coagulase, carotenoid pigment, haemolysis, lipase, lecithinase and protease activity was examined to be in 59 (100%), 55(93.22%), 51 (86.44%), 23 (39.98%), 25 (42.37%) and 19 (32.2%) respectively. Secretion of lipase, protease and lecithinase were insignificantly related to each other as well as bacterial isolates from different sample type.  Regarding 43 (72.89%) penicillin resistant isolates, 31(72.09%) were β-lactamase producers and of 20 (33.89%) methicillin resistant S. aureus (MRSA), 14 (70%) were β-lactamase producer. β-lactamase production was analyzed to be statistically significant for penicillin but not quite significant for methicillin resistant S. aureus (χ2=24.30, P>0.05 for penicillin and χ2=3.7, P=0.054 for methicillin). Positive correlation occurs between β-lactamase production and resistance to other antibiotics included in the study (R=0.97).It seems no variation in the liberation of virulence detecting enzymes among S. aureus. Even if penicillin resistance majorly results due to β-lactamase, methicillin resistance shares some other mechanism of resistance.

Keywords: S. aureus, virulence factors, β-lactamase, penicillin and methicillin

ABSTRACT

A new simple, rapid, precise, accurate and specific stability indicating method has been developed for the simultaneous estimation of Niacin (NIA) and Lovastatin (LOVA) in tablet dosage form. A chromatographic column used for separation was (250*4.6mm i.d., 5 mm) C₁₈ (Hyperchrome ODS-BP).The mobile phase was 0.02M Disodium hydrogen Phosphate buffer:Acetonitrile (75:25, pH-5) and UV detection of effluent at 237nm.The flow rate was 1ml/min. The retention times of Niacin and Lovastatin were 3.29 min and 4.75 min, respectively. The range of Linearity for Niacin and Lovastatin were 125-325μg/ml and 5-25 μg/ml respectively. The recoveries of Niacin and Lovastatin were found to be in the range of 99.91-100.42 % and 100.03-100.41% respectively. The optimized RP-HPLC method proved to be specific, accurate and robust for the estimation of Niacin and Lovastatin in tablet dosage form. Stability testing study includes the acid hydrolysis, base hydrolysis, oxidation, thermal degradation, and photolysis.

Keywords: Niacin, Lovastatin, RP-HPLC Method

ABSTRACT

A well developed and validated RP – HPLC method by UV- detection was used for the determination of Gatifloxacin in human plasma with metronidazole as internal standard. Solid phase extraction was involved in the process. The drug and the internal standard were eluted under isocratic mode using a 150 X 4.6 mm i.d, 5 µm Phenomenex ODS 2 C18 column. The mobile phase composed of a mixture of 5:95 % v/v methanol and 20mM mixed phosphate buffer (pH 3.5± 0.05) at a flow rate of 1.4 mL/Minute. The detection wave length of the detector was 268 nm. A volume of  50 µL was injected and the runtime of the method was 9 minutes. The method showed good linearity in the range of  50.1 to 7000.9 ng/mL. The recovery of gatifloxacin was 92.42 % with a standard deviation of 1.533 and recovery of internal standard was 87.6 %. The LOD of Gatifloxacin was 50.1 ng/mL. Matrix effects were not observed.

Keywords : Gatifloxacin, Antibacterial, Internal standard, RP – HPLC, Human plasma

ABSTRACT

The present research paper focuses on designing not only the sustained release tablets of acyclovir to ensure time-dependent, sustained release formulation but also studying the effect of sodium alginate, Xanthan gum and HPMCV K15 on the in vitro release profile of the tablet. The initial release of drug from these matrices occurs by the drug dissolution in the water penetrated into the matrix. The overall drug release from these matrices is governed by hydration, gel layer formation and drug diffusion into the gel layer and to the dissolution media. The formulations ACL1 to ACL5 are containing 200mg of drug with a combination of different excepients. The drug release showed in ACL1 was 95.78%, for only 10hrs and ACL2 showed 90.66% within 11hrs because there was less presence of Xanthan Gum. The Acyclovir tablets of ACL3 showed 91.35% in 12hrs, ACL4 and ACL5 showed drug release of 95.33% for 8hrs and 95.85% for 9hrs. In further formulations the dose of Acyclovir was increased to 400mg ACL6 to ACL10 that are containing combination of excipients. The drug release for the formulations ACL6 showed a drug release of 97.44% for 10hrs and ACL7 showed a drug release 92.4% for 11hrs. From these twelve formulations it was concluded that increase in concentration of Xanthan Gum and Sodium alginate overrun the effect of HPMC K15. The dissolution characteristics allowed for drug to be released in a controlled manner, highlighting the importance for the correct selection of polymers according to their physical, mechanical and pharmacokinetic properties.

Keywords: sodium alginate, Xanthan gum, HPMCV K15, dissolution characteristics, sustained release

ABSTRACT

Plants are widely used by people in traditional and modern medicine all over the world. In fact, all of their remedies can be used safely and without the side effects of drugs. Phytochemical analysis of medicinal plants has revealed that numerous bioactive compounds in plants traditionally used for medicinal purposes have many therapeutically properties. Hence in the present study, a general chemical identification of a Lebanese medicinal plant Urtica dioica was carried out. The results obtained validate the traditional uses of nettle, and showed that this plant possesses an important pharmaceutical value and leads to the isolation and characterization of three compounds from hexane extract. Structures of these compounds were elucidated by spectral methods [FTIR, GC-MS, ¹H NMR] after column chromatography on silica gel.

Keywords: Urtica dioica, phytochemical screening, bioactive compounds, FTIR, GC-MS, ¹H NMR.

ABSTRACT

The present study was aimed to scientifically validate the use of Trichosanthes dioica fruits in prevention of diabetes by evaluating their antihyperglycemic and antilipidemic potential. The effect was observed on fasting blood glucose (FBG) levels of STZ-nicotinamide (45, 110 mg/kg BW, respectively, i.p) induced diabetic rats after seven days daily administration of chloroform extract rich in moderately polar components (250 mg/Kg BW, p.o). FBG was significantly reduced (p < 0.05 %), when estimated on seventh day of treatment with fruit extract compared to diabetic control. Pre-treatment with fruit extract for seven days also normalized the blood glucose to basal level by the third hour of oral glucose challenge (2g/Kg BW, p.o) in diabetic rats. Moreover, the treatment with fruit extract resulted in significant reduction in the levels of total cholesterol and triglycerides comparable to metformin. Results of the present study showed that chloroform extract of T. dioica possesses antihyperglycemic properties and beneficial effects on diabetic hyperlipidemia. All these effects could be due to the bioactive components revealed in the T. dioica fruits such as cucurbitacins, which could justify their ethnomedical use.

Keywords: Diabetes, Trichosanthes dioica, STZ-nicotinamide, cucurbitacins, metformin

ABSTRACT

The chronic type-2 diabetes mellitus leads to diabetic nephropathy, which is one of the major microvascular complication of end stage renal disease worldwide and causes premature death in diabetic patients. The objective of the present investigation was to evaluate the antidiabetic activity and protective effect on diabetic induced nephropathy of combinations of ethanolic root extract of Asparagus racemosus (REAR) and seed extract of Eugenia jambolana(SEEJ) by using in-vivo model. The in-vivo antidiabetic activity and the effect on diabetic nephropathy was evaluated on streptozotocin- nicotinamide induced type-2 diabetes mellitus in male albino Wistar rats. The in-vivo study showed that blood glucose level was significantly reduced in dose dependent manner when compared to the diabetic control group. In addition, it significantly restored the body weight loss, increased kidney weight, glycosylated haemoglobin, blood urea, blood uric acid, blood urea nitrogen, blood creatinine, urine volume and urine microalbumin levels when compared to diabetic control groups. The report of histopathological study of rat kidney tissues strongly supported the protective effect of combinations of REAR and SEEJ in diabetic nephropathy. The findings of this investigation concluded that combinations of REAR and SEEJ has significant antidiabetic activity and potential protective effect in diabetic nephropathy.

Keywords: Type-2 diabetes mellitus, Diabetic nephropathy, Streptozotocin, Nicotinamide, Eugenia jambolana, Asparagus racemosus.

ABSTRACT

In this study, the crude methanol extract of whole plant of Vernonia cinerea Less. has been investigated for anti-diarrheal, anxiolytic, antimicrobial and membrane stabilizing activities. Test for anti-diarrheal activity was carried out by castor oil-induced diarrhea in mice. The anxiolytic activity was examined in mice by using the hole-cross test and open field-tests (OFT). The preliminary antimicrobial activity was determined at 500 μg/disc by the disc diffusion method against a number of Gram positive and Gram negative bacteria and fungi. RBC membrane stabilization method was used for the evaluation of in-vitro anti-inflammatory activity. The crude methanol extract of V. cinerea showed significant and dose-dependent anti-diarrheal activity in castor oil-induced diarrhea in mice. The results showed that the crude extract significantly increased the number of hole crossing as compared to control in hole cross tests. In open field test, the extract showed significant increase in number of square crossed. The efficacy of the extract (200-400 mg/kg b.w.) was compared with standard anxiolytic drug diazepam (1 mg/kg). Furthermore, the plant extract, at 500 µg/disc exhibited moderate antimicrobial activity against Blastomyces dermatitidis (zone of inhibition = 17.7 mm) and Shigella dysenteriae (zone of inhibition = 14.0 mm). In red blood cell stability test,  the sample at 0.5 and 1 mg/ml  inhibited the heat-induced haemolysis of RBCs by 15.45% and 27.73%, respectively whereas standard acetyl salicylic acid (ASA) demonstrated 71.36% inhibition of haemolysis. The obtained results provide supports for the use of this plant in traditional medicine but further pharmacologic studies are required to isolate and identify the bioactive molecules.

Keywords: Vernonia cinerea, Anti-diarrheal, Anxiolytic, Antimicrobial, Membrane Stabilization

ABSTRACT

This paper deals with the development and validation of stability indicating an isocratic high performance liquid chromatographic method for the quantitative determination of memantine hydrochloride. The method is simple, highly sensitive, selective and is capable of quantitative determination of memantine hydrochloride. The chromatographic separation is achieved by injecting 20µL standard solution of memantine hydrochloride into HPLC system with refractive index detector using a YMC ODS-AQ, 5µm (150 x4.6)mm column. The mobile phase consists of 10 mL Triethylamine in 1L water(pH 5.5 adjusted with glacial acetic acid):MeOH in the ratio of  40:60 v/v. The flow rate was set at 0.9 ml/min with column and cell temperatures at 40˚C and 50 ˚C respectively and runtime was optimized to 10 min. Forced degradation studies were performed on bulk sample of memantine hydrochloride using acid (5.0Nhydrochloric acid) ,alkali (1.0N sodium hydroxide),oxidation (30% hydrogen peroxide),thermal(105 ˚C),photolytic and humidity conditions. The peak purity was checked with LC-MS and LC-MS/MS. The developed LC method was validated with respect to specificity, precision, linearity, ruggedness, stability of analytical solution and robustness.

Keywords: Memantine hydrochloride, HPLC,LC-MS,  Assay

ABSTRACT

A simple, accurate, precise and sensitive RP- HPLC method has been developed for the determination of Gatifloxacin and Flurbiprofen Sodium in their pharmaceutical formulation. Chromatographic separation  was carried out on InertsilODS – 3 column (250 mm ×4.6 mm, 5µm ) as stationary phase by using mobile phase consisting of 0.02 M Phosphate buffer (pH 3.5 adjusted with orthophosphoric acid ) : Methanol (80 : 20 v/v). The flow rate was 1.5 ml/min with UV-detection at 245 nm. The retention time was found to be 2.59 min for Gatifloxacin and 5.41min for Flurbiprofen Sodium. The method was validated for various parameters according to ICH guideline. The linear regression analysis data for the calibration plots showed good linear relationship in the concentration range of 30 – 90 µg/ml and 3 – 9 µg/ml and correlation coefficient was found to be 0.9988 and 0.9992 for Gatifloxacin and Flurbiprofen Sodium respectively. The Limit of Detection for Gatifloxacin and Flurbiprofen Sodium were 1.45 and 0.028 respectively. The Limit of Quantification for Gatifloxacin and Flurbiprofen Sodium were 4.39 and 0.28 respectively.

Keywords : Gatifloxacin, Flurbiprofen Sodium, RP- HPLC, Validation, Ophthalmic Formulation.

ABSTRACT

The objective of the current study was to find out the consumer attitude and concern about cosmetic safety and their knowledge about the cosmetic label symbols. The survey was distributed to N =100 in Rasalkhaimah , UAE to a  population with varied characteristics for demography, gender, education, professions and age. From the result of the study it can be seen that people no doubt concerned about the safety of cosmetics but have a low level of understanding of cosmetic label symbols. There is significant correlation between the three variable i.e, age, gender and qualification and consumer concern about safety, their knowledge of cosmetic label symbols and attitude toward knowing the details of these symbols. Furthermore , those consumer who use cosmetics on daily basis have more tendency to believe that the cosmetics are adequately regulated and are safe to use.

Keyword : cosmetics ,symbols, variables , label.

ABSTRACT

This paper describes a strategy for the systematic development and validation of stability-indicating method of the determination of degradation impurities present in Naftopidil Orally dispersible tablets.  Efficient separation is achieved in 75mm length x 2.1mm ID, Octadecyl column with 3µ particle size. Using pH 3.2 phosphate buffer and acetonitrile as mobile phase in gradient pump mode. Flow rate was selected 0.4mL.min^-1with a detection wavelength of 210nm. Validation parameters such as specificity, linearity, precision, accuracy, determination of LOD,  LOQ and robustness were evaluated as per ICH guidelines. The validated Reverse phase –Ultra Performance liquid chromatography (RP-UPLC) method was successfully applied to the quantitative determination of impurities of Naftopidil in Naftopidil Orally Dispersible tablet dosage forms, helping to improve quality control and to assure therapeutic efficacy at reduced run time of minutes.

Keywords: Naftopidil, Forced Degradation, RP-UPLC and Stability Indicating

ABSTRACT

This research manuscript describes simple, sensitive, accurate, precise and repeatable reverse phase high performance liquid chromatography method for the estimation of Ketoconazole in tablet dosage form. The sample was analyzed by reverse phase ACE 5 C18 column (150 mm × 4.6 mm i.d, 5 μm particle size) as stationary phase; methanol: acidic water  [91:9, v/v] pH 3.0 as a mobile phase at a flow rate of 0.85 ml/min. Quantification was achieved with Photo Diode Array detector at 243 nm. The retention time for Ketoconazole was found to be 2.764 min. The linearity was obtained in the concentration range of 5-40 µg/ml for Ketoconazole. The method was successfully applied to tablet because no chromatographic interferences from formulation excipients were found. The method retained its accuracy and precision when the standard addition technique was applied.

Keywords: Ketoconazole, RP-HPLC, Method validation.

ABSTRACT

In the last two decades, antibiotic resistance has become a severe problem worldwide. This has lead to the search for new, safe and effective antimicrobial agents from alternative natural resources like plant products. Different parts of Lawsonia inermis L. (Family: Lythraceae) like roots, bark, leaves, flowers and seeds are traditionally used for the treatment of various ailments.  Alkaloids, tannin, phenolics, saponin and anthraquinone are present in both types of extracts of leaves of Lawsonia inermis. Glycosides are present in ethanolic extract of leaves and seeds. Terpenoids and flavonoids are not found in leaves but present in seeds. The disc diffusion assay showed that the leaves and seeds of Henna plant have different degrees of bacterial and fungal growth inhibition, depending on the strains.  The aqueous extracts showed broadest antimicrobial activity by inhibiting more or less most of the microbial strains involved. Aqueous extract was more effective than their ethanolic extracts. Klebsiella pneumonie and Serratia  marcescens were the most resistant strains tested. It could be concluded that seeds and leaves of Lawsonia inermis have potential antimicrobial efficacy. All extracts (aqueous or ethanolic) have shown better antimicrobial efficacy against Staphylococcus aureus, Escherichia coli and Aspergillus niger. Differential antimicrobial activity of plant parts against different bacteria might be due to concentration of different active phyto-compounds in different parts. Among those antimicrobial compounds, phenolic compounds, terpenoids, and alkaloids are very important compounds in antimicrobial or antioxidant action.

Keywords: Henna, Lawsonia inermis,  Antimicrobial,  Phytochemical

ABSTRACT

A new gradient reverse phase Ultra Performance Liquid Chromatography (UPLC) method was developed for the analysis of Dissolution profile samples of Paricalcitol in Paricalcitol Soft Gelatin capsules. The aim of the new method was to achieve proper accuracy and precision for the highly potent low dose drug product formulations. The normal injection loop allows upto 10µL of the sample in normal condition in UPLC systems.  For the current method the loop was modified to handle 50µL of injection volume in order to achieve quantifiable area counts. Efficient separation is achieved on Acquity UPLC HSS T3 (100 mm length × 2.1 mm ID with, 1.8 m particle size. Validation parameters such as specificity, linearity, precision, accuracy, and robustness were evaluated as per ICH guidelines. The validated RP-UPLC method was successfully applied to the Dissolution of Paricalcitol Soft Gelatin Capsules dosage forms.

Keywords: Paricalcitol, Soft Gelatin Capsules, Validation, Acquity UPLC, 50µL injector loop, dissolution profile tests

ABSTRACT

This research aimed to evaluate a new approach for preparation of in situ gel and to design innovative peroral delivery systems for Ranitidine Hydrochloride (RHCl) able to enhance the control release. The present study was carried out to optimize and evaluate an oral in-situ gel containing ranitidine HCl with Pluronic F-127 and hydrophilic HPMC E50 by the simple mixing method. The compatibility of the polymers was proved by FTIR. The prepared in-situ gel formulations were tested for their physicochemical characteristics such as clarity, gel strength, gelation temperature, drug content, sol-gel transition time and in vitro release studies of ranitidine HCl-loaded in-situ gel formulation in phosphate buffer (pH 1.2 and 7.4. ) were performed using a modified diffusion cell across dialysis membrane. The prepared formulations were clear and Gel strength ranges from 31±1.6 to 33±1.2. The drug content for the prepared formulations was 97.23% to 99.02%.Then the Drug release at 12 h is 98.25 and thus shown controlled release.

Keywords: Oral in- situ gel, Ranitidine HCL; Pluronic F-127; HPMC E50.

ABSTRACT

There is an increasing incidence of cancer not just in our country but worldwide. The aim of this study is to evaluate socio-demographic data, knowledge, awareness, practice level in cancer patients through assessment of their respective attendants. A self-administered, structured, open ended and pretested questionnaire covering the general characteristics, KAP about cancer, screening and treatments was used to collect responses of cancer patient attendants in KIMS a Teaching Hospital at Hyderabad. Their age group was between 18-79years. The educational preparations of the attendants are as follows: 50 attendants are grouped as “CONTROL”, 50 are grouped as “TEST”. The information thus collected was entered and analyzed in SPSS and Microsoft Excel software. Responses from 100 attendants were recorded and analyzed. The results of both groups i.e. TEST and CONTROL pre-post interventions were tabulated and compared between the groups, educational intervention was given to only test group thus paired t-test results obtained at level of significance 0.005, shown that only test group attendants shown significant difference in aspects of knowledge and practice when compared to that of the control group who received information only at the end of the study. Our study has shown that educational interventional study give high scope in comparative studies where pre-post interventions were in use.

Keywords :Oncology, Chemotherapy, Health knowledge and practices.

ABSTRACT

To evaluate the anti-convulsion activity of Crocus sativus linn. aqueous extract  in electrical induced epilepsy models. To compare the anti convulsant activity of crocus sativus linn. with phenytion .After obtaining Institutional Ethical Committee approval, Wistar albino rats (150-200g) of either sex were randomly divided into 5 groups of 6 animals each. Dried powder of crocus sativus linn. was boiled with distilled water, cooled, filtered, placed on hotplate for complete evaporation, finally weighed and stored. The control group, test group and standard drugs group received saline, crocus sativus linn. extract (200,400 & 800 mg/kg), phenytoin (25 mg/kg) respectively by oral feeding. The anti-convulsent effect was assessed by maximal electrical shock (MES) in rats. In electrical induced epilepsy models It implies that saffron 400mg/kg (groupIV) and 800mg/kg(groupV) significantly (p<0.001) delays the onset and significantly (p<0.001) decreased the duration of tonic hind limb extension of MES induced convulsions compared to that of control. The current study demonstrates statistically significant anti-convulsant activity of crocus sativus linn.

Keywords: Crocus sativus Linn., anti-convulsant, MES.

ABSTRACT

Management of Diabetes mellitus type 2 with hypertension is very complex process as it is very difficult to find which therapy gives better action in diabetic and hypertensive patients  The patients with Diabetes Mellitus and Hypertension were identified and they are enrolled based on inclusion and exclusion criteria. Data was collected through standard data documentation form. A prospective study was carried out and cost effective analysis of those drugs was done. The scores obtained are evaluated & analyzed using statistical tools and Microsoft Excel software This study has shown that oral hypoglycemic drugs which are cheap i.e.  Is 1.0 rs, per day, per week it costs 7rs, per fifteen days it costs 15 rs, per month it costs 30.5 rs and per year it costs 365 rs. for diabetes and  for hypertension  Beta blockers were low priced  10.17 rs per day ,per week  it costs 71.19rs, per fifteen days it costs 152.55rs,  per month it is 315.27 rs,  per  year   it is  3712 rs, categorized  medication and at the same time it gives better therapeutic action in terms of  treatment  outcomes. Over all study has shown that combination therapy will attribute to the better treatment outcomes. Use of generic drugs should be encouraged than prescribing brand drugs because of same therapeutic out come and it cause more economic burden to patient and more complications. There is a need of educating patients to motivate them in order to make them realize the risk involved if untreated.

Keywords: Prescribing pattern, Cost Effective Analysis, Diabetes Mellitus, Hypertension.

ABSTRACT

There is highly co-incidence between hypertension and insulin resistance which is the important causative factor to develop diabetes mellitus (DM). Our study was prospective study in effect of beta-blockers, angiotensin-converting enzyme inhibitor (ACEI) and calcium channel blocker (CCB) on blood glucose level in patients newly diagnosed with hypertension and without diabetes in MVJ hospital, Bangalore. Fasting blood glucose and post prandial blood glucose measured for patients prescribed antihypertensive for four months. In a nutshell, we observed that Beta blockers worsen the glycemic condition and it increased blood glucose level, beside that it increased incident of impaired glucose tolerance. In case of calcium channel blocker and ACEIs, blood glucose level slightly increased and decreased respectively after two months.    

Keywords: Antihypertensive, Fasting blood glucose, Post prandial blood glucose, Impaired glucose tolerance

ABSTRACT

For patients suffering with different types of cardiovascular diseases, the need to understand the pattern of occurrence of the disease in a population is very essential. The goal of the present study was to understand the pattern of occurrence of the various cardiovascular diseases and bring awareness about the rational use of drugs. Total 100 patients suffering with different types of cardiovascular diseases were included in present study within a time period of 6months. It was a prospective randomized study. The tools which were used throughout the study were patient information sheets (case sheets) and questionnaire. As per the data collected from the case sheets of 100 patients it can be concluded that average prevalence of cardiovascular diseases were found to be more in males than in females. Among the various CVD high prevalence was found to be of hypertension. Common age group of CVD is observed as 40 to 60 years. We have concluded that the drugs used for the treatment of cardiac disease are almost found to be rational. Rational use of drugs minimizes poly-pharmacy, drug interactions and in turn it minimizes the hospital stay. The drugs prescribed are from national list of essential medicines. The prescribing habits, route of administration, dosage forms are found to be appropriate.

Keywords: Cardiovascular disease, Drug utilization evaluation.

ABSTRACT

Recently, fast dissolving films are gaining interest as an alternative of fast dissolving tablets. The present study aimed at preparing fast dissolving oral films of Naratriptan hydrochloride as a model drug which is used for the migraine treatment. Fast dissolving dosage forms have acquired great importance in pharmaceutical industry because of their unique properties like dissolve upon contact with a wet surface, such as the tongue, within a few seconds, meaning the consumer can take the product without need for additional liquid. This convenience provides both a marketing advantage and increased patient compliance. In the present investigation various trials were carried out using two grades of HPMC (E3 and E6), Propylene glycol, PEG-400 and other polymers by solvent casting method.  The prepared films were evaluated for film thickness, folding endurance, surface pH, morphological properties, %drug content and content uniformity, tensile strength, percent elongation, in vitro disintegration time and in vitro dissolution studies. The optimized formulation S11 prepared using HPMC E6 showed minimum disintegration time (10 sec), highest dissolution rate i.e. 98.23% of drug within 6 min and satisfactory physicochemical properties. Results of DSC and FTIR data of optimized formulation (S11) revealed that there was no incompatibility observed between the drug and excipients used in the formulation. These findings suggest that the fast dissolving oral film containing Naratriptan hydrochloride is considered to be potentially useful for the treatment of migraine where quick onset of action is desirable when compared with reference standard Naratrax conventional tablet.

Keywords: Naratriptan hydrochloride, fast dissolving films, solvent casting method, HPMC.

ABSTRACT

The purpose of the present study was to develop an optimized gastric floating once-daily matrix tablet of ofloxacin (FERMTs) using  hydrophilic polymers such as HPMC K4M, HPMC 100M, isapagulha husk and sodium bicarbonate as buoyancy contributer. The formulation of FERMTs were designed by 2³full factorial design taking amount of HPMC K4M, HPMC 100M and sodium bicarbonate as formulation variables and prepared by wet granulation method. The FERMTs were then evaluated for hardness, friability, weight variation, content uniformity, in vitro drug release and floating capacity. Finally, the floating lag time (FLT) and cumulative % drug release at 4h, 8h, 12h and 16h were taken as response variables and the FERMT formulation was numerically optimized by 2³full factorial design using Design-Expert software (version 8.1). The optimized formula showed excellent floating efficiency over a 16 h period with FLT of 2.80 mins and drug release over a period of 16 hour. Analysis of dissolution data showed that the kinetic of drug release followed Korsemeyer-peppas model.

Keywords:  Floating tablet; Extended-release; Factorial design; Ofloxacin

ABSTRACT

Itraconazole is a potent triazole antifungal drug which has low solubility at physiological pH conditions. It is active in vitro against a wide variety of fungi with a spectrum of activity which qualitatively resembles that of ketoconazole, the first oral azole to gain widespread acceptance. Itraconazole binds more avidly to fungal cytochrome P-450 than does ketoconazole and unlike ketoconazole, has little effect on mammalian cytochrome P-450 enzyme systems.The purpose of present work was to explore the feasibility and preparation of the Itraconazole Hydrochloride salt to improve the solubility and dissolution rate of poorly soluble drug Itraconazole. Itraconazole Hydrochloride was synthesized by using addition reaction with hydrochloric acid. Then it was incorporated into a new derivative of cyclodextrins Sulfobutyl ether β-Cyclodextrin (CAPTISOL) and 2-Hydroxypropyl β-Cyclodextrin by using physical mixing, kneading and co-evaporation techniques. The solubility of prepared salt was found multifold than the solubility of itraconazole. The dissolution studies of itraconazole complexes exhibited high percentage drug dissolution than that of the pure drug which can be attributed to the increase in drug solubility provoked by the complexation technique. The results indicated Itraconazole HCL-Captisol (1:2 molar ratio) prepared by kneading method shows better characteristics when compared with pure drug and other formulations.

Keywords: Itraconazole; Itraconazole hydrochloride; Sulfobutyl ether₇ β-Cyclodextrin; 2-Hydroxypropyl β-Cyclodextrin; dissolution enhancement.

ABSTRACT

A simple, sensitive, precise, accurate and economic Q-absorption ratio method for the quantitative determination of betamethasone sodium phosphate and ofloxacin in bulk and combined dosage form has been developed and validated. Q absorption ratio method uses the ratio of absorbances at two selected wavelengths, one which is iso-absorptive point and other being the λ-max of one of the two components. Betamethasone sodium phosphate and ofloxacin shows an iso-absorptive point at 247nm in methanol, the second wavelength used was 289nm, which is λ-max of ofloxacin. The linearity was obtained in the concentration range of 2-12 ug/ml for both the drugs in distilled water. The proposed method is recommended for routine analysis. The results of analysis have been validated statistically and by recovery studies.

Keywords: Betamethasone sodium phosphate, Ofloxacin, Q-absorption ratio method, Validation.

ABSTRACT

L-asparaginase is an anticancer agent, especially for acute lymphoblastic leukemia. Nine E.coli strains were screened forits ability to produce an extracellular L-asparaginase enzyme. The optimum culture conditions for L-asparaginase production was found at pH 8.0, Incubation time 48 h, and 37^oC temperature. Highest yields of L-asparaginase(140.5 and 96.4 IU/ml) by E.coli strains using glucose and beef extract as sole carbon and nitrogen sources respectively. 0.6 fold of higher L-asparaginase activity (168.4 IU/ml) was recorded using pUC18 UV60 than the parent strain. 0.54 fold increased L-asparaginase activity (220.6 IU/ml)was observed using pUC18 NTG90.The molecular mass of L-asparaginase was determined by SDS-PAGE and it was found to be 29KDa.   

Keyword: L-asparaginase, E.coli, UV, NTG and SDS-PAGE

ABSTRACT

The present study was designed to investigate te antioxidant activity oof methanolic extract of Morinda Tinctoria Roxb against (MEMT) fruits in the cerebral ischemia induced animal model system.  Global cerebral ischemia was induced by temporary bilateral common carotid  artery occlusion for 15 min followed by reperfusion in Sprague Dawley Rats  and the animals were pre-treated with MEMT (200 and 400 mg kg-¹) for 1 week before induction. After induction of ischemia by BCCAO animals were again treated with MEMT for 1 week and the animals were sacrificed. Homogenized content of brain were estimated in control, sham and treatment groups. The MEMT showed the significance of p<0.01 done by ANOVA and Dunetts in the levels of antioxidants such as superoxide dismutase, glutathione peroxidase, glutathione reductase, lipid peroxidation, catalase, protein levels, vitamin C levels. At the 1 week after ischemia a maximum of 85% protection of neurons in CA1 region showed in treatment group at the dose 400 mg kg-¹. The results showed neuroprotective nature of MEMT and protection may be due to reduction of oxidative stress which occurs by alteration in levels of antioxidants and MEMT has the potential to use in treatment of global ischemia.

Keywords: Morinda tinctoria, bilateral common carotid artery occlusion, antioxidants, CA1

ABSTRACT

Terbinafine hydrochloride (TFH), is a potent antifungal agent of the allylamine class with broad spectrum activity against yeasts, dimorphic fungi, molds, and dermatophytes. A new, simple, rapid, selective, precise, accurate, and stability indicating high performance liquid chromatographic method has been developed for the determination of terbinafine hydrochloride (TFH) in pharmaceuticals. The assay was performed using an Zorbax Eclips XDB C-18 (3.5 µm, 4.6 × 150 mm i.d.,) column at 30ºC temperature with UV-detection at 222 nm. A mobile phase consisting of buffer (1000 mL water, 2 mL triethylamine, pH 3.4 adjusted with trifluoroacetic acid.), isopropyl alcohol and methanol (40:12:48, v/v/v), was used in the assay at a flow rate of 1 mL min^-1. The method was validated and system suitability parameters were investigated. An excellent linearity was obtained over the concentration range 1 - 80 μg mL^-1 TFH with limits of detection (LOD) and quantification (LOQ) values of 0.3 and 1.0 mg mL^-1, respectively. The proposed method were applied successfully to the determination of TFH in tablets. The results obtained were in good agreement with those obtained by a reference method, with high precision and without any detectable interference from tablets excipients. The validity and reliability of the proposed methods were further assessed by the recovery studies via a standard addition method. In addition, forced degradation of TFH was conducted in accordance with the ICH guidelines. Acidic, basic water hydrolysis, thermal stress, peroxide and photolytic degradation were used to assess the stability indicating power of the method. Slight degradation was observed during oxidative degradation and no degradation was observed under other stress conditions.

Keywords: Terbinafine Hydrochloride, High performance liquid chromatography, Stability indicating, Pharmaceuticals.

ABSTRACT

The concept of "Quality by Design" (QbD) is getting popularized in pharmaceutical manufacturing industry to understand the product and process to identify the risks involved during manufacturing.  One of the perpetual quality attribute is to have robust analytical method that can provide consistent results though out the life cycle of the product. General considerations during analytical method validation is to perform robustness studies by deliberate changes made in pH of the buffer in mobile phase, change in organic ratio, change in column oven temperature, change in buffer strength and using different column lot numbers etc. However to improve the analytical quality standard, a novel method concept under QbD was introduced which uses single mobile phase for three drug components and estimates using different column chemistries used in pharmaceutical industry viz., C18, C8, phenyl and Cyano column. The validated RP-LC method was successfully applied to the quantitative determination of Chlorpheniramine, Ibuprofen and Pseudoephedrine in tablet dosage form, helping to improve quality control and to assure therapeutic efficacy using all column chemistries.

Keywords: Quality by Design (QbD), Validation, RP-LC, Stability Indicating, Fixed-dose combination and robust

ABSTRACT

The study aims at developing novel extended release pellets of venlafaxine. The main objective of the work was to develop robust extended release formulations of Venlafaxine (test formulation) for regulated markets having comparable in-vitro dissolution profile with Innovator product - Effexor® XR (Reference Product). Venlafaxine spheroids were made using extrusion spheronization technique. The release of the drug from the spheroids was controlled by applying a coating comprising ethyl cellulose as rate controlling polymer. The coated pellets were then encapsulated in the hard gelatin capsules. The in-vitro dissolution studies were conducted to evaluate the release of the drug venlafaxine from the coated spheroids contained in capsule at pH 6.8 using phosphate buffer. The in-vitro dissolution profile of the test compositions was compared with Reference Product Effexor XR. The results obtained showed that the test formulations had higher percentage release of venlafaxine in initial time period. Therefore, a better control on the release was desired. During the manufacturing of spheroids, it was observed that more fines were generated during the extrusion spheronization, which is not suitable for large scale production of the formulation. Accordingly batches were optimized using different types of binder and coating composition. Effect of the binder and percentage coating was studied. The drug release of venlafaxine using Povidone K30 as binder, Ethyl cellulose and Acryl-EZE MP 93018508 white as release control polymers was compared with innovator’s drug release and was found to be equivalent. From the results, it was concluded that use Povidone K30 as binder during extrusion spheronization process results on generation of less fines, thus increases the yield of the product. Also, the formulation containing dual coating of Ethyl cellulose and Acryl-EZE MP 93018508 on the spheroids containing Povidone K30 as binder showed the dissolution profile similar to that of the Reference Product Effexor XR.

Keywords: Venlafaxine, Ethyl Cellulose, Povidone K30, Acryl-EZE, USP-I Apparatus.

ABSTRACT

Cefixime has bioavailability of 40-50%, which could be attributed to its low solubility in GI tract. The objective of this pilot study was to compare the efficacy and safety of improved formulation of cefixime 200 mg tablet (CEFOLAC) versus conventional marketed cefixime 200 mg tablet in patients with typhoid fever (TF). Patients with clinical diagnosis of TF were randomized to receive either treatment twice daily for 10 days. Primary efficacy end point was reduction of clinical symptoms score on day 5 and number of patients with absence of clinical symptoms. Secondary endpoints include microbiological cure and clinical relapse on day 10 and 21. Total 22 patients completed study successfully and were subjected to analysis. Percentage improvement in total clinical symptoms score from baseline to day 5 was greater in improved formulation of cefixime (70 %) than conventional cefixime 200 mg tablet (58 %). On day 5, numbers of patients with complete cure of clinical symptoms were greater in group A as compared to group B. All patients in both the groups were cured based on clinical symptoms and microbiological evaluation on day 10 and day 21. No case of clinical relapse was observed. Both the formulations of cefixime were well tolerated by patients. Improved formulation of cefixime offers faster and greater improvement in clinical symptoms than conventional cefixime tablet in patients with TF. Improved formulation of cefixime is a better option for the treatment of patients with TF than conventional cefixime tablet.

Keyword: Typhoid fever, Cefixime, Bioavailability, Solubility