ABSTRACT

It was already reported that increasing population is a matter of concern in India. In an order to control the population, Indian government promotes the family planning with several means of contraceptives. These contraceptives include oral contraceptive pills (OCP’s), intra uterine devices (IUCD’s), condom, barrier methods and irreversible surgical methods. They are available in market with several reported adverse effects. Thus, search for an effective, safe and user-friendly contraceptive is remains a challenge. In this article an approach was made to explore the Unani contraceptives measures. The validated studies on Unani contraceptives were also described in the present review.

Key words: Unani contraceptives, Mane’y hamal, Mudir-e-haiz, Musqit-e-janeen.

ABSTRACT

Natural products from medicinal plants, either as pure compounds or as standardized extracts, provide unlimited opportunities for new drug leads. Due to an increasing demand for seeking therapeutic drugs from natural products there is a need to develop analytical methodologies for different purposes which include the extraction, isolation and characterization of active ingredients in botanicals and herbal preparations. Various analytical methods available for the isolation, characterization and quantification of active ingredients from plant extracts which include various spectrometric and chromatographic methods along with some hyphenated techniques are discussed. The present review helps to design a method for the isolation, characterization and quantitative determination of major constituents from plants.

Keywords: Natural products, isolation, characterization, quantification, analytical techniques.

ABSTRACT

The natural product curcumin is a polyphenolic compound extracted from the rhizome of Curcuma longa L. Curcumin is the principle curcuminoid present in turmeric, responsible for its bright yellow color. Curcumin is a nature’s gift to mankind which has broad range of therapeutic, diagnostic and prophylactic potential. In addition to its use as a spice, flavoring and coloring agent in food, turmeric has been used in India for medicinal values for centuries. In Ayurveda, use of curcumin is well documented for the treatment of various ailments. But the applications of curcumin are curtailed by its low solubility, stability, bioavailability, rapid metabolism and short half life. This weapon can be sharpened and re explored as new age one key answer to many ailments and disorders by using it in the form of liposomal, nanoparticulate, microparticulate drug delivery and also by complexing it with metal ions, polymers, cyclodextrine and other carriers. Curcumin has ability to bind with various transition and earth metal ions to form stable complex. Complexation of curcumin with transition metals is one of the useful ways to overcome the problem related to solubility, stability and bioavailability. From several recent studies, it was observed that curcumin metallocomplexes shows greater therapeutic effects than curcumin alone.

Keywords: Curcumin, curcumin metal complex, stability, bioavailability.

ABSTRACT

Tuberculosis remains a significant public health issue worldwide especially in developing countries. India leads the world in its burden of tuberculosis (TB) due to its neglect as a public health problem, and mismanagement of TB patients in both public and private sectors. The original National Tuberculosis Programme (NTP), launched in 1962, failed because of several reasons. To overcome its shortcomings, the DOTS strategy was introduced in 1992 as an initiative under the Revised National Tuberculosis Control Program (RNTCP). Though the latter has been better funded and better managed, it is yet to address several key issues like lack of adequate and updated infrastructure, unregulation of the private practice sector and the emergence and increase in number of drug-resistant tuberculosis in India.

Keywords: Tuberculosis, DOTS, RNTCP, mismanagement.

ABSTRACT

Insulin remains indispensable in the management of diabetes mellitus since its discovery in 1921. Relatively, a large percentage of world population is affected by diabetes mellitus. In today's era; insulin delivery by alternative route is an area of current interest in the design of drug delivery system. Most of the global pharmaceutical companies are showing encouraging progress in their attempts to develop alternative insulin delivery technologies. For most patients with type 1 diabetes, the tedious part of the treatment is to tolerate needle after needle, both for glucose measurement and to deliver insulin. The introduction of insulin therapy years ago has saved the lives of millions of patients with diabetes. It is growing increase in the percentage of population having diabetes mellitus due to hereditary and environmental factor.  Needle-free insulin delivery appeared to be astonishing approach and its allure rested in being comfortable and safe. The document present here encompass, in brief, the emerging technologies and discoveries that are in pipeline, including insulin inhalers, implantable insulin pumps, insulin spray, smart cells, insulin pill, insulin complement, islet cell transplant, insulin nano pump and the other promising advances in safe and comfortable insulin delivery. Therefore it will be a tripartite task for the researcher, health authorities and community pharmacist to foster the long term safety profile and to provide comfortable insulin delivery.

Keywords: Insulin, Diabetes Future trends, Novel drug delivery system, Implantable insulin pump.

ABSTRACT

Kleptomania is the inability to refrain from the urge to steal items and is done for reasons other than personal financial gain. It is a type of impulsive control disorder. Impulse control disorders (ICDs) are common psychiatric conditions in which affected individuals typically report significant impairment in social and occupational functioning, and may incur legal and financial difficulties as well. Kleptomania is characterized by repetitive uncontrollable theft of items that are of little use to the afflicted person. It is commonly associated with other anxiety and eating disorders, alcohol abuse, substance abuse and various mood disorders. Amygdala and nucleus accumbens are the major structures of brain involved in kleptomania. Serotonin and dopamine neuro transmitters and opioids are thought to be involved in the pathophysiology of kleptomania. Decreased serotonin and increased dopamine levels can lead to kleptomania. It can be effectively treated with behavioral or psychotherapy and pharmacological therapies. Selective serotonin inhibitors (SSRIs), tricyclic anti depressants (TCAs) and opioid antagonists are commonly used to treat kleptomania. Behavioral therapy involves Psychotherapy, Covert sensitization, aversion therapy, coping and support, self education, treatment of other mood disorders. This review summarizes the current information, associated disorders, and underlying pathophysiology regarding kleptomania, its treatment and prevention.

Keywords: kleptomania, impulsive compulsive disorder, amygdala, nucleus accumbens, dopamine, serotonin. 

ABSTRACT

Nigella sativa (Black seed) is a plant which has been used for centuries for medicinal and culinary purposes and reported to possess a number of pharmacological properties that include anti-parasitic, antibacterial, antifungal, antiviral, antioxidant and anti-inflammatory activities. Its oil is used as condiment, carminative, food preservative, analgesic and to treat many ailments in different parts of world. It has been extensively used in Unani system of medicine as a natural remedy for a number of diseases such as asthma, inflammation, cough, eczema, fever and gastrointestinal disturbances. It also has galactagogue, abortifacient, emmenagogue and uterotonic activity which makes it useful in amenorrhoea, dysmenorrhoea, puerperal sepsis and to improve lactation. Many active principles have been isolated from Nigella sativa seed including thymoquinone, nigellone, and fixed oils. This review is an attempt to highlight the therapeutic uses of Nigella sativain Unani medicine and pharmacological properties.

Keywords: Unani, medicine, pharmacological, phytochemical.

ABSTRACT

Horse gram (Macrotyloma uniflorum Lam.) is a popular pulse, locally known as Kollu belongs to the family Fabaceae that still remain an under exploited legume crop. Horse gram seeds are rich in protein and consumed in majority by poorest section of the society.  It is rich in protein, iron, calcium and polyphenols. Different part of the plants are used for the treatment of heart disease, asthma, bronchitis , urinary discharges and for treatment of kidney stones. The present paper is an overview on its phytochemical and pharmacological properties reported in the literature.

Keywords: Macrotyloma uniflorum,phytochemical and pharmacological activity.

ABSTRACT

Graphene is one of the crystalline forms of carbon, along with diamond, graphite, carbon nanotubes and fullerenes where in carbon atoms are arranged in a regular hexagonal pattern. Graphene can be described as a one-atom thick layer of the layered mineral graphite. High-quality graphene is very strong, light, nearly transparent, and excellent conductor of heat and electricity. Its interaction with other materials and with light, and its inherently two-dimensional nature, produce unique properties Owing to its interesting electrical, optical, mechanical and chemical properties, graphene has found potential applications in a wide range of areas, including biomedicine. Graphene has a number of properties which make it potentially promising for bioapplications. Its large surface area, chemical purity and the possibility of easy functionalization provide opportunities for drug delivery. Its unique mechanical properties suggest its application in tissue- engineering and regenerative medicine. Its combination of ultimate thinness, conductivity and strength make it an ideal support for imaging biomolecules in transmission electron microscopy. Also, chemically functionalized graphene might lead to fast and ultrasensitive measurement devices, capable of detecting a range of biological molecules including glucose, cholesterol, hemoglobin and DNA. This review summarize the latest progress of using graphene for various biomedical applications, including drug delivery, cancer therapies and biosensing, and discuss the opportunities and challenges in this emerging field.

Keywords:  Graphenes , Biomedical Application, drug delivery, Biosensing

ABSTRACT

From very beginning, human is very curious about health and its prevention. In every era of world memoirs of life, different definitions and thoughts came under consideration about health. Every civilization, like Babylonians, Egyptians, Greeks and Mesopotamians etc has tried to suggest the best ways for the human achievements of well beingness. Greek physicians in BC century have paved great attention towards this important task in ratiocinative way. They elaborated the concept of health and factors which are essential for its maintenance. Among them, Riyazat (exercise) is the very basic and useful tool for maintenance of health. As well as, other recommendations of exercise have also described by Greek physicians. Unani physicians provided cognitions regarding timing, modes, and benefits of Riyazat. In this review paper, it will be attempted to provide the benefitting 15owledge to the humanity to save the health and promote the cognitive values.

Key words: Riyazat; Greek physicians; Health; Humor; Mizaj, Exercise

ABSTRACT

The synthesis of Nitrogen containing heterocycles particularly substituted pyrrolidines constitutes very important moieties of many biologically active molecules¹ including natural and non-natural substances. The synthesis of functionalized pyrrolidines continues to attract interest, both for their synthetic challenges,² and also their value in synthetic chemistry³ and their diverse biological properties.⁴ The present work includes the synthesis of substituted pyrrolidines from alkyl dihalide and primary amines by simple and efficient cyclocondensation process. This methodology gives varies of substitution pattern on 2,3-position of the pyrrolidines⁵ Scheme 1. This strategy improved greener synthetic methodology and worked out as a simple and straightforward one-pot approach for the synthesis nitrogen containing heterocycle as pyrrolidines.

Keywords: Pyrrolidine, Heterocyclic compound, Dihalide.

ABSTRACT

This research is directed towards Synthesis and quantitation of process-related impurity in Felodipine bulk and formulation. The synthesis of 1,4-Dihydro-2,6-Dimethyl-4-(m- chloro phenyl) pyridine-3,5 Dicarboxylate was identified, characterized, developed and validate by using various analytical techniques such as UV, IR, NMR  for the assessment of impurities in the bulk and formulation in Felodipine. The synthesis of of 1,4-Dihydro-2,6-Dimethyl-4-(m- chloro phenyl) pyridine-3,5 Dicarboxylate was performed by Hantzch pyridine synthesis, by using m-chlorobenzaldehyde, ethylacetoacetate, in presence of ammonia and methanol as a catalyst. The percentage yield was observed to be 80.29%. The preliminary evaluation was performed via melting point, elemental analysis and thin layer chromatography (TLC). Melting point of obtained synthesised compound was noticed to be 134-137⁰C, whereas Rate of flow ( Rf) value was estimated and found to be 0.70. The TLC of impurity was performed by using Benzene and Methanol (6:1). The structure confirmation of obtained synthesized impurity by using sophisticated analytical instrument viz, Fourier transform infra red( FT-IR), nuclear magnetic resonance (NMR) and ultra violet (UV) spectroscopy. The method was validated as per ICH guidelines and was found to be linear, precise, robust, accurate, rugged.

Keywords: Impurity, Felodipine, UV, Validation.

ABSTRACT

In present study, Brevicin produced from Brevibacillus borstelensis AG1 isolated from Marcha - a natural herbal cake of North East India was used to enhance the shelf life and microbial safety of orange juice. Food borne pathogens viz. Listeria monocytogenes MTCC 839, Bacillus subtilis CRI and Clostridium perfringens MTCC 1739were inoculated at the amount of 8.16, 8.13 and 8.18 log CFU/ml, respectively in orange juice to study the preservative effect of bacteriocin against them as compared to chemical preservative – sodium benzoate and commercial biopreservative i.e. nisin. Viable cells were counted periodically and a consistent reduction in number of viable cells of each tested pathogen was observed. Brevicin when tested was found antagonistic to most challengeable and serious food borne pathogens to control in processed fruit/vegetables products. Brevicin was found active over a wide pH range i.e. 3.0 to 11.0 and thermostable upto 100^oC. It showed better preservative potential by reducing the pathogenic load of indicators in orange juiceas compared to control having maximum spoilage proving its potential as a natural preservative to enhance microbial safety and shelf life of different food items.

Keywords: Biopreservation, bacteriocin, application, Brevibacillus borstelensis AG1, orange juice

ABSTRACT

A simple, accurate and precise UV spectrophotometric method has been developed for the quantitative estimation of Efavirenz in bulk and tablet dosage form. The λmax was found to be 239 nm. Beer’s law was obeyed in the concentration range of 10-20μg/ml. The regression equation was Y=0.052x-0.113 with value of R² as 0.996. The method showed good linearity, accuracy and reproducibility. Accuracy as expressed mean percent recovery ± standard deviation was found to be 95.29% ± 0.0429. Percent relative standard deviation values for the intra-day and inter-day precision studies were found to be 0.23 and 0.31, respectively. The limit of detection and limit of quantitation values were found to be 1.39 and 4.22, respectively. Assay of Efavirenz in tablet formulation was performed and percent purity of tablet was found to be 98.65% ± 0.0078.

Keywords: Efavirenz, UV spectrophotometry, Validation.

ABSTRACT

Schleicheraoleosa is (Lour.) Oken belonging to the family Sapindaceae. An ethanolic extract of Schleicheraoleosa bark was investigated for its Anti-nociceptic and anti-inflammatory activities in rats and mice. Anti-nociceptic  activity was evaluated  by using the tail immersion, tail flick and hot plate latency assay while the anti-inflammatory test were carried out using the carrageenan induced paw oedema model in rats. Pentazocin was used for analgesic activity and Indomethacin was used for anti-inflammatory activities as standard drugs. The in tail immersion, tail flick and the hot plate latency times were increased with the increase in  doses of 200, 400 & 600 mg/kg significantly. . Similarly, for the carrageenan induced paw oedema model the result show that the extracts at the doses of 200, 400 & 600 mg/kg significantly (P < 0.001) inhibited the paw oedema in a dose dependent manner. The present study proved that the ethanolic extract of S. oleosa has analgesic and anti-inflammatory activities property.

Keywords: Anti nociceptic activity, Anti-inflammatory activity, Scheilcheraoleosa.

ABSTRACT

The present study was undertaken to investigate the Diuretic and antiurolithiatic activities of Ethanolic leaf extract of Sida Acuta in Albino rats. Ethanolic leaf extract was administered to experimental rats orally at doses of 200mg/kg and 400mg/kg (each p.o). Furosemide (5mg/kg) was used as a standard. The diuretic effect of the extract was evaluated by measuring the urine volume and determining sodium, potassium, chloride and bicarbonate contents. In In vitro antiurolithiatic activity Calcium oxalate crystallization was induced by the addition of 0.01M sodium oxalate solutions in synthetic urine. The effect of extract (100, 300 and 500μg/ml) was studied by time course measurement of absorbance. In-vivo Urolithiasis was induced in male rats by administering ethylene glycol (0.75%) in drinking water to groups II-V except normal control (Group I) for 28 days. Groups I, II and III served as normal control, positive control (hyperurolithiatic), and standard (cystone 750mg/kg), respectively, Groups IV and V served as curative regimen. Oxalate, calcium, phosphate were monitored in urine. Serum calcium, creatinine and uric acid were also recorded. The extract of Sida acuta was safe and exhibited no gross behavioral changes in the rats. A significant diuretic effect was observed from the experimental animals treated with extract of Sida acuta individually compared to the control. The results obtained suggest potential usefulness of extract of Sida acuta leaf as an antiurolithiatic agent.

Keywords: Sida acuta, Medicinal plants, Diuretic and Urolithiatic activity.

ABSTRACT

A simple, sensitive, rapid, accurate and precise spectrophotometric method has been developed for estimation of Glimepiride in bulk and tablet dosage forms. The zero order spectra shows maximum absorbance at 249 nm. Calibration graph was found to be linear over the concentration range of 5-30 μg/ml. Results of analysis were validated for precision, range, linearity, interference study and recovery studies, The method can be adopted in its routine analysis.

Keywords: Glimepiride, Tablets, Ultraviolet Method, Spectrometric method.

ABSTRACT

Oxalis corniculata Linn. (Oxalidaceae) is one of the important medicinal plants used traditionally for the treatment of fever, pain and inflammation. The present study was aimed to screen antipyretic activity of petroleum ether, chloroform, ethyl acetate, methanol extracts and β-sitosterol isolated from petroleum ether extract of Oxalis corniculata Linn. The leaves of Oxalis corniculata Linn. was used for successive extraction with increasing polarity solvents. Petroleum ether extract was selected for activity-guided fractionation to isolate β-sitosterol due to its better efficacy than other extracts. Antipyretic activity was done by yeast induced pyrexia method. All the extracts were screened at the dose of 100 mg/kg, i.p. and isolated β-sitosterol was screened at the dose of 10 and 20 mg/kg. The result showed that after five hour of petroleum ether extract (100 mg/kg) administration significant inhibition of pyrexia up to 89.5% was observed. Isolated β-sitosterol 10 and 20 mg/kg, i.p. showed promising antipyretic activity with inhibition of pyrexia by 91.23 and 94.41% respectively. Results are compared with standard drug paracetamol (50 mg/kg i.p.). Thus the present pharmacological screening provides support for the folklore claim of antipyretic activity of Oxalis corniculata Linn.

Keywords: Oxalis corniculata Linn., Brewer’s yeast, Pyrexia, β-sitosterol.

ABSTRACT

A simple, sensitive and reproducible stability indicating RP-HPLC method for the simultaneous determination of Phenylephrine and Ebastinein bulk and Pharmaceutical dosage formhas been developed and validated. Chromatographic separation was carried out on kromasil C₁₈ (250×4.6mm, 5mparticle size) column using a mobile phase composed of Phosphate buffer (adjusted to pH 5.0 with dilute OPA): acetonitrile: methanol in the ratio of 30:45:25 %v/v/vat a flow rate of 0.8 ml/min. The analyte was monitored using PDA detector wavelength at 211 nm. The retention time was found to be 2.295 min and 4.225 min for Phenylephrine and Ebastine respectively. The proposed method was found to be having linearity in the concentration range of 25-150µg/ml for both Phenylephrine(r²0.99996)and Ebastine(r²0.99987)respectively. The developed method has been statistically validated according to ICH guidelines. Stress testing which covered acid, alkali, peroxide, photolytic and thermal degradation was performed on under test to prove the specificity of the method and the degradation was achieved. The proposed method can be successfully applied for the stability indicating RP-HPLC simultaneous determination of Phenylephrine and Ebastine in bulk and combined tablet dosage form and in routine quality control analysis.

Keywords: Phenylephrine, Ebastine, RP-HPLC, Forced degradation, Method validation.

ABSTRACT

Plants are very useful to mankind. Many of them are used exclusively for medicinal purposes. According to the World Health Organization (WHO), “a medicinal plant is a plant which, in one or more of its organs, contains substances that can be used for therapeutic purposes, or which are precursors for chemo-pharmaceutical semi-synthesis.” Such plants are in great demand by pharmaceutical companies for their active ingredients. The present study deals with the in-house formulation of herbal antidiabetic tablet Glucomap. Various evaluation parameters of tablets were evaluated and were compared with standard drug glucomap.

Keywords: Herbal antidiabetic tablet, Glucomap, In-house formulation.

ABSTRACT

A simple, accurate and sensitive RP-HPLC method was developed and validated for the determination of candesartan cilexetil and hydrochlorothiazide in tablet dosage form. The separation of the two drugs was achieved on a Reprospher 100 –C l 8 column (250 x 4.6 mm, 5 µm particle size) with UV detection at 260 nm. The mobile phase consists of two solution, solution (1) orthophosphoric acid (pH 2.2) and the solution (2) which is acetonitrile and purified water in the ratio 55: 45 v/v, respectively. The method was validated in terms of linearity, accuracy, precision, specificity, limit of detection, limit of quantitation and robustness. Linearity was observed in the concentration range 10-70µg/ml for hydrochlorothiazide and 12.8 -89.6µg/ml for candesartan cilexetil. The limit of quantitation was found to be 8.58 and 4.6 µg/ml for hydrochlorothiazide and candesartan cilexetil, respectively whereas the limit of detection, was found to be 2.8 and 1.5 µg /ml for hydrochlorothiazide and candesartan cilexetil, respectively. The % recovery range of candesartan cilexetil was 97.84-101.62% and 100.9-101.53% for hydrochlorothiazide. Variation in HPLC conditions (flow rate, column temperature, mobile phase composition, and wavelength) were used to evaluate the robustness of the method. The method proved to be robust and still produces good results.

Keywords: Candesartan cilexetil, hydrochlorothiazide, Method Development, Validation, RP-HPLC.

ABSTRACT

Present study was carried out to study compatibility of Atorvstatin Calcium (ATR) and Telmisartan (TEL) with selected generally regarded as safe (GRAS) excipients and to prepare bilayer tablet. Isothermal stress testing was performed in binary mixtures which was subjected to 50°C for 4 weeks. Isothermal stressed samples were evaluated with RP-HPLC method and FTIR analysis. A trial was conducted with single disintegrant and diluent with direct compression technique and in-vitro dissolution was carried out. To improve the release profile of ATR layer, multiple disintegrants were used namely croscarmellose sodium (CCS), sodium starch glycolate (SSG)  and crosprovidone (CP). These disintegrants were taken as variable in Box-behnken design (BBD) in Minitab 16.2.3.0. The tablets were prepared from obtained design formulations by direct compression. Similarly, Telmisartan layer was prepared by wet granulation technique. TEL was treated with alkalizing agent, sodium hydroxide in stoichiometrical proportion. Croscarmellose sodium, sodium starch glycolate and crosprovidone were taken as variable and subjected to BBD. Intra and extra granulation was done with mixtures of disintegrants. Optimized formulation as per response surface optimizer in Minitab 16 contains be 10.0 mg of SSG, 7.36 mg of CP and 10.0 mg of CCS per tablet for ATR layer. Similarly in case of TEL tablet, it was found that as concentration of SSG, CP and CCS increases, the release of drug also increases. When multiple disintegrants were used in the combination, better release was obtained. Optimize formulation as per response surface optimizer in Minitab 16  contains 22.03 mg of SSG, 15 mg of CP and 15 mg of CCS per tablet for Telmisartan layer. Bilayer tablet was prepared with this optimized formulation in 10 station compression machine. The prepared bilayer tablet was further evaluated and in-vitro dissolution were compared with market products. Thus, the conversion of salt form, optimized combination of disintegrants, use of polyvinyl pyrrolidone K-30 as carrier, intra and extra granulation was observed to be effective in release of TEL from the dosage form where as only the optimized combination of disintegrants was  sufficient for release of ATR from the dosage form.

Keywords: Compatibility, Isothermal stress testing, Atorvastatin Calcium, Telmisartan, Bilayer tablet.

ABSTRACT

Nature has been source of medicinal plants from thousands of years. In traditional medicine practice, the leaf of Dolicus lablab, commonly known as ‘hyacinth bean’ is said to have a significant medicinal value. In Ancient Arab medical practice the leaf of Dolicus lablab were said to be used in treatment of infections. Hence our present study aimed to test both anti bacterial and antifungal activities of methanol, ethanol, aqueous extracts of Dolicus lablab against three strains of fungi (Trichophyton rubrum, Trichophyton mentagrophytes, Candida albicans.) and four strains of bacteria (Escherichia coli, Pseudomonas aeruginosa, Bacillus subtilis, Staphylococcus  epidermidis) using agar well diffusion method. Among the three extracts, methanolic extract showed very potential antifungal and antibacterial activity ,with a highest zone of inhibition against fungi, T. mentagrophytes (30mm) and two Gram(-) bacteria, E. coli, P. aureginosa, with a Zone of inhibition at a range 15-19mm and 8-11mm.

Keywords: Dolicus lablab leaf, Antibacterial activity, Antifungal activity, Zone of inhibition.

ABSTRACT

The aim of the study was to assess Pharmacognestic study of crude plant extract of Rivea hypocrateriformis and was carried out to characterize the chemical composition of some constituents by GC-MS analysis. Different solvent extracts (aqueous, methanolic, chloroform, ethyl acetate and DMSO) of plant R. hypocrateriformis leaves were assessed for in vitro antimicrobial activity assay by disc diffusion method furthermore antioxidant assay was carried out DPPH free radical scavenging activity, Phytochemical screening was carried out by ‘guide to modern techniques of plant analysis” and GC-MS analyses were performed to identify the constituents present in the plant that stand behind such activities. Due to higher polarity, DMSO extract show revealed presence of maximum phytochemical composition susceptibility as well as methanol and chloroform shows average amount of phytoconstituents. The antibacterial screening is the major of the inhibition hollow observed in inhibition zone. The highest inhibition zone was observed in DMSO extract against each bacterial strain. Where E. coli shows mid active zone inhibition and S. aureus show less, IC₅₀ value of the sample was found to be moderate as compared to standard and the eight compounds were identified in R. hypocrateriformis leaf extract by GCMS analysis. R. hypocrateriformis plant had considerable major chemical composition present in crude extract. Due to presence of major chemical components make it seems to be important for medical purposes and plant contains Potential antibacterial components that may be useful for evolution of pharmaceutical for the therapy of ailments. Also plant extracts can be used for the treatment of infections caused by the strains of the test bacterial organisms.

Keywords: Antimicrobial, DPPH, GC-MS.

ABSRACT

The aim of this study was to prepare a solid dosage form able to release theophylline after a maximum delayed time and at a maximum cumulative amount in 12 hours. To achieve this goal a blend of two polymers with different properties was used along with talc powder and utilizing D-expert statistical software package. The polymer blend consists of Eudragit NE 30D and Eudragit RL 30D-55. Solid precipitates composed from polymer blend and talc powder and containing a fixed amount of theophylline were prepared using spray dryer. The prepared solid precipitates were compressed into tablets and the dissolution profile of each formulation was investigated. Delayed time was observed in term of time required to release 10 % of the labeled theophylline. Delay time was ranged from 2.14 to 4.1 hour while, percent of theophylline released in 12 hours ranged from 84.06 to 97.94 %. After that optimization was performed to prepare a dosage form with a desired properties in term of maximum delayed time and maximum percent theophylline released in 12 hours. The optimized solid precipitates as generated from the statistical software package was formulated and investigated. The optimized formulation was able to delay the time of theophylline release to 3.24 hour and release 93.64 % of the incorporated theophylline in 12 hours. Solid dispersion technique in conjunction with statistical design was shown to be very efficient for the optimization of both the delayed time and cumulative amount of drug released in 12 hours.

Keywords: D-Optimal experimental design, optimization, Theophylline, Delayed release

ABSTRACT

Concomitant therapy of anti inflammatory agent and disease modifying drug in pulsatile pattern proves the best treatment for pain relief and in remission of disease. In the current work, combination therapy of aceclofenac and leflunomide was studies for rheumatoid arthritis. Tab in tab formulation was developed with inner leflunomide and outer aceclofenac fraction. Outer fraction provides instant relief from symptomatic pain and inner part provides disease remission. pH sensitive polymers were investigated for coating and coating parameters were optimized. Considering the pH solubility of Eudragit S 100 and Eudragit L 100 in different ratio, final composition was derived. With final composition, desired lag phase observed in the drug release study. Further, X-ray studies and Pharmacokinetic study with final formulation also proves the efficacy of the final formulation w.r.t. desired lag phase and drug plasma concentration in-vivo. Final formulation found stable in 3 months stability study w.r.t. physical and chemical parameters. Optimized novel pulse release combination therapy developed to provide the relief to arthritis patient. 

Keywords: Arthritis, chronobiological, pH sensitive polymer, pulsatile, combination therapy.

ABSTRACT

Oral fast disintegrating films (OFDF) is an emerging technology brings out “formulations taken without water” with quick onset of action and improved patient compliance. The present aim of study is to enhance the dissolution rate of the dosage form by using the different superdisintegrants and co-processed superdisintegrants. The films were prepared by solvent casting method using hydrophilic polymers that rapidly dissolves on the tongue or buccal cavity, delivering the drug to the systemic circulation. The polymer was used  HPMC E15, PEG 6000 as plasticizer, citric acid as the saliva stimulating agent, sucrose as the sweetening agents and sodium starch glycolate, crosscarmelose sodium and crospovidone as the superdisintegrants and tween 80 as surfactant . The FTIR reports suggest that drug and excipients were compatible. These oral disintegrating films were evaluated for various evaluation parameters. The in-vitro dissolution studies were conducted as per USP II with sinker. There were three ODFs prepared by using different types of the superdisintegrants, two were prepared by using the co-processed superdisintegrants and one was without any superdisintegrants. Among all formulation, the F6 shown the better in-vitro drug release profile which was prepared by using co-procesed superdisintegrants. It can be concluded that the co-processed superdisintegrants enhances the dissolution rate by comparing with other formulation.

Keywords: HPMC E15, PEG 6000, SSG, CCS, Crospovidone, co-processed superdisintegrants, Tramadol hydrochloride.

ABSTRACT

Metformin HCl is an oral anti-diabetic drug used in the treatment of type-2 diabetes but has been linked with gastrointestinal disturbances and lactic acidosis. The aim of this study is to improve the efficacy and achieve dose reduction of metformin HCl by entrapping the drug in solid lipid nanoparticles (SLN). Solid lipid nanoparticles of metformin were prepared by hot homogenization method at different stearic acid and polysorbate 20 ratios. The formulated particles were characterized by particle size, time-dependent pH, differential scanning calorimetry, drug entrapment efficiency (EE) and loading capacity, and in vivo hypoglycaemic activity in mice. P-values less than 0.05 were considered statistically significant. Formulations prepared with lipid-surfactant ratios of 1:5 and 1:2 formed nanoparticles with sizes of 474 and 617 nm, respectively, with moderate entrapment efficiencies and loading capacities, while time-resolved pH showed dependence on surfactant proportion. The size and entrapment efficiency-optimized metformin HCl nanoparticles (1:2 lipid-surfactant ratio) showed faster, higher and sustained reduction of blood glucose in mice than pure metformin HCl powder. Metformin SLN improved the delivery of metformin and may reduce the occurrence of side effects associated with metformin. Solid lipid nanoparticles of metformin HCl may therefore be recommended for effective management of type-2 diabetes mellitus.

Keywords: Diabetes; entrapment; Hypoglycaemic activity.

ABSTRACT

A new, rapid, precise, selective and sensitive validative forced degradative UV spectroscopy method was developed for estimation of Montelukast sodium in bulk and pharmaceutical formulation in the developed method, the absorbance was measured at  272.19nm.the drugs obeyed the Beer’s law in the  concentration range of 30-150μg/mL. Accuracy studies of the method were determined by recovery studies and were found to be 99.9 for Montelukast sodium. It can be used for routine analysis of drug in bulk and in pharmaceutical formulation.

Keywords: forced degradation studies, Montelukast sodium,validation.

ABSTRACT

Published reports of comparison of erythrocyte parameters for newly enrolled urban and rural junior secondary school students in different geographical zone in Nigeria are relatively scanty. To determine and compare erythrocyte parameters of newly enrolled urban and rural junior secondary school students in south-south and south-east, Nigeria. The study population was a total of 240 subjects (60 male and 60 female subjects for each urban and rural area) of JSS1 students. 5mls of blood sample were collected from ante cubital vein with minimum stasis and the values of Red blood cell count, Haemoglobin, Mean cell volume, Mean cell haemoglobin, Mean cell haemoglobin concentration, Red cell distribution coefficient volume, Red cell distribution standard deviation and Haematocrit, was determined by MAXCOM MC- 6200 fully automated haematology analyzer, while the data were analyzed using Z-test; p value less than 0.05 were considered statistically significant. There were significant gender variations in the values of these parameters in both urban and rural newly enrolled students. The mean values of Haemoglobin, Mean cell volume, Mean cell haemoglobin, Red cell distribution width standard deviation and Haematocrit were significantly higher in rural males and females compared to urban males and females (p˂0.05). No significant differences were found in mean values of red blood cell count and Coefficient variation of red cell distribution width when compared both rural and urban males and females. From the above study, there is variation in the gender, age and some erythrocyte parameters amongst newly enrolled urban and rural junior secondary school students under investigation.

Keywords: Erythrocyte, newly enrolled, parameters

ABSTRACT

The purpose of present work was for formulation and characterization of Clopidrogrel floating tablets to improve bioavailability and to minimize the side effects of the drug. FTIR studies were conducted for drug polymer compatibility. The Clopidrogrel sustained release floating tablets were formulated by wet granulation method.  Tablets were subjected to pre and post compressional evaluation studies. The different concentrations of HPMC K4M, HPMC K15M, xanthan gum, guargum, and sodium bi carbonate 25% w/w is used as gas generating agent and micro cellulose crystalline MCC are used in different concentrations (75%, 50%, 25%) as diluent. The tablets were tested for thickness, weight variation, hardness, friability, drug content; In vitro floating parameters and drug release studies were also conducted. Compatibility studies revealed that there is no interaction between drug and polymers in the formulations. The flow properties were within the limits and the granular bed exhibited uniform flow and ease for compression. Clopidogrel floating tablets showed uniform post compressional properties with minimum standard deviation. The formulations showed minimum floating lag time and prolonged duration of floating. In vitro drug release of clopidogrel was sustained up to 12 h. Clopidrogrel release followed zero order, first order, Higuchi drug release kinetics for drug release. The peppas diffusion coefficient ranged from 0.455 - 0.895 indicating drug release by non fickian diffusion followed by erosion. The F4 floating tablet was optimized formulation which showed 100% release sustained for 12 h. The stability studies indicated stability of drug in the optimized formulation against temperature and humidity.

Keywords: Clopidrogrel, Floating tablets, HPMC K15M, Xanthan gum, guar gum, Release kinetics, Stability studies.

ABSTRACT

Isosorbide Dinitrate (ISD) is a moderate to long acting oral organic nitrate which acts as a vasodilator profoundly used in the treatment of angina pectoris, a condition which occurs when the oxygen supply to the myocardium is insufficient for its needs. It is slightly soluble in water and propanol, sparingly soluble in ethanol and freely soluble in methanol. The most economical solvent Distilled water was choosen as a solvent. The drug has absorption maximum (method A) at 304nm, Area under curve (method B) at 300-310 and first order derivative method (method C) at 287nm. Linearity for all three methods was found in the range of 5-25 μg/ml with Correlation coefficient is 0.999, Standard error is 0.001. The drug sample was analyzed by UV spectroscopy using distilled water as solvent and the average content of drug present in the formulation was found to be 99.7%. The % recovery of accuracy studies was found to be 99.1 % for method A, 101.5 % for method B, 100.6 % for method C. The %RSD of precision was found to be 1.11% for intraday, 1.22 % for inter day. The force degradation studies of Isosorbide Dinitrate was done on Stress degradation by hydrolysis under alkaline condition by using 0.1N NaOH was found to be 10.09% for 24hrs, 13.3% for 3days, 14.2% for 5days .Stress degradation by hydrolysis under acidic condition by using 0.1N HCl and degradation was found to be  2.68% for 24hrs, 9.7% for 3days, 11.9% for 5days.  Oxidative degradation was done by using hydrogen peroxide (3%v/v) and degradation was found to be 3.22% for 24hrs, 5.06% for 3days, and 8.29% for 5days. The proposed methods can be successfully employed for quality control during manufacture and for assessment of the stability of Isosorbide Dinitrate in bulk samples and its tablet dosage forms.

Keywords: Isosorbide Dinitrate, Forced Degradation studies, Tablet dosage forms, UV Spectroscopy, Validation

ABSTRACT

The objective of the present study was to enhance the dissolution profile, absorption efficiency of water insoluble drugs like Telmisartan. A novel “Powder Solution Technology” involves absorption and adsorption efficiency, which makes use of liquid medications admixed with suitable carriers and coating materials and formulated into a free flowing, dry looking, non adherent and compressible powder forms. Based upon a new mathematical model expression improved flow characteristics and hardness of the formulation has been achieved by changing the proportion of carrier and coating material ratio from 15:1 to 5:1. Avicel ^® PH 102 was showing acceptable flow properties compared with Avicel ^®PH 200. Higher dissolution rates were observed in optimized liquisolid formulation containing Poly ethylene glycol 400 and Avicel ^®PH 102 compared with marketed product (SARTAN^® 20mg tablets). Poly ethylene glycol 400 was showing highest solubility compared with poly ethylene glycol 200, propylene glycol and glycerin.The crystalline state of telmisartan drug state was changed to amorphous state due to liquisolid formation and was confirmed by both X-ray diffraction and Fourier transform infrared spectroscopy results, this transition occur as the drug is in solution form. Additionally, increasing the wetting properties and subsequent surface area of the drug available for dissolution.

Keywords: Liquisolid tablets, Telmisartan, Polyethylene glycol, Dissolution, Powder solution Technology.

ABSTRACT

A series of 1-(2, 6-difluorobenzyl)-1H-1, 2, 3-triazole (5a-d and 7a-d) were synthesized and evaluated for CNS depressant  and anticonvulsant activities by photoactometer, rotarod and pentylene tetrazole induced convulsion method respectively in Swiss albino mice. Diazepam was used as a standard drug. Out of the 8 compounds tested, compounds (5b, 7a and 7b) were showed the CNS depressant activity comparable to that of diazepam at a dose of 5 mg/kg. The active members of the series (5b, 7a and 7b) were selected for anticonvulsant activity study.

Keywords: 1, 2, 3-triazole, CNS depressant, Pentylenetetrazole, Clonic convulsions.

ABSTRACT

Antibiotic Prophylaxis should be appropriate to reduce the risk of postoperative surgical infections. Surgical Site Infections (SSIs) are responsible for Increased Mortality and Morbidity rate during surgical operations which lead to major complications. The inappropriate and overuse of antibiotics effects the cost and efficacy of drugs which leads to the resistant bacteria. To assess the pattern of antibiotic usage in surgical in-patients and for Postoperative wound infections. The present study is a prospective observational study done for a period of six months in Basaweshwara Medical College and Research Centre, Chitradurga in surgical ward. A Total of 162 patients were enrolled into the study. Among them, Surgical Site Infection (SSIs) was found in 37 (22.8%) patients and patients without SSIs are 125 (77.2%). The patients with age group 25-60 years were 104 (64.2%) in which SSIs are more (23).According to the study male patients underwent more surgeries (107 (66%)) in which 21 (56.8%) are with SSIs. Infection rate were more in males when compare to females in the study. A total of 265 antibiotics were used among 162 patients in which third generation cephalosporins are more preferred. The study concludes that there is a proper need to control the use of antibiotics appropriately. The inappropriate use leads to economic burden and resistance. SSIs may decrease the quality of life of the patients. Hence minimization of SSI is also very important in the developing countries by maintaining infection control plans by suitable organizations which makes an impact on the infections

Keywords: Antibiotics, Surgical Site Infections (SSIs), Prophylaxis.

ABSTRACT

A Novel series of 1-phenyl-5-(1H-pyrrol-1yl)-1H-pyrazole-4-carboxilic acid hydrazide derivatives were prepared by a 4 step course of action starting with Phenyl Hydrazine and 2-(1-ethoxyethylidine)malononitrile, with good yields and simple reaction condition. Synthesized compounds were test for their antibacterial activities. The structures were confirmed by ES-MS, NMR analysis.

Keywords: phenyl hydrazine, pyrazole-4-carboxilic acid, Clauson-Kass procedure, hydrazide, antibacterial activity

ABSTRACT

Gastro retentive systems can remain in the gastric region for several hours and hence prolongs the gastric residence time of drugs and improve the bioavailability. The aim of this project was to develop sustained release floating matrix tablet for hydroalcoholic extract of neem leaves using psyllium husk as release controlling polymer along with synthetic polymer HPMC K100 M and sodium bicarbonate as gas generating agent. The tablets were prepared by direct compression method. Seven different formulations A1 to A7 were prepared by varying the concentration of psyllium husk, HPMC K100 M and sodium bicarbonate. Tablets were evaluated for pre and post compression parameters like tablet thickness, hardness, weight variation, drug content, friability, floating lag time and in vitro drug release. Results for angle repose, swelling index, weight variation, drug content, thickness, hardness, % friability for all the formulations were found to be in acceptable limit. In vitro drug release was observed for 12 hours and all the tablet formulations followed zero-order kinetics and/ or Korsemeyer-Peppas model in drug release. The formulations were optimized on the basis of buoyancy time and in vitro drug release. The optimized formulation was found to be A4 with 98.77% in vitro drug release in 12 h and 212 seconds buoyancy time. The BaSO₄ tagged formulation, similar to formulation A4 was tested in in vivo gastric retention study in rabbits. It was observed that formulation kept floating in the stomach region till 10 hours. Formulations containing combination of psyllium husk and HPMC K100M with sodium bicarbonate as gas generating agent can be a promising way for formulating gastroretentive drug delivery systems.

Keywords: Neem extract, psyllium husk, floating drug delivery, buoyancy.

ABSTRACT

Anthocyanins are multifunctional bioactive compounds implicated with beneficial health effects due to their strong antioxidant activity for scavenging free radicals that are involved in cell damage and tumour promotion. Evidence has accumulated to suggest that flavonoids potently suppress tumour cell proliferation and may effectively work as chemopreventive agents against carcinogenesis in humans. In the study, we detected the antiproliferative effects of anthocyanin on human epithelial cells and the Breast cancer cells by MTT assay. The HEp-2 and MCF-7 cells were seeded in 96-well culture plates in different concentrations of cassava leaf stalk extracts of Indian Cassava (Manihot esculenta, Crantz ) to determine their anticancer effects using the MTT assay. Anthocyanin extracted from cassava leaf stalk extracts have 79% inhibition on HEp-2cells at 1000 μg/ml (Table1). The anthocyanin extracted from cassava leaf extracts was tested against MCF-7 cell lines shows 78% inhibition at 1000 μg/ml (Table 2). So we confirm that, the anthocyanin compounds present in cassava leaf extracts are inhibiting the proliferation of the cancer cells.

Keywords: Cassava (Manihot esculenta), Anthocyanin, Hep 2, MCF 7, Antiproliferative.

ABSTRACT

To appraise the nephroprotective and antioxidant activity of hydroalcoholicCissampelospareira (C.pareira) whole plant extract using cisplatin induced nephrotoxic rats. C.pareirais a well know medicinal plant of Menispermaceae family which is widely used for ayurvedic medicine to treat various kidney complications. In the present study C.pareirawas observedfor its acute toxicity studies by using OECD guidelines no.425. The nephroprotective activity was evaluated by using cisplatin induced nephrotoxic rats. In-vivo antioxidant activity was evaluated by using glutathione and lipid peroxidation estimation in cisplatin induced rats. One way ANOVA followed by Dunnett’s test using Graph pad prism software. Statistical significance was set at P ≤ 0.05. From the acute toxicity study two doses were selected as 200 and 400 mg/kg p.o. body weight for the present study. C.pareira extract significantly increases the body weights, decrease the elevated urinary glucose levels in the urine, decrease the urea and creatinine levels in blood and increase the urinary creatinine levels in cisplatin induced nephrotoxic rats. In the in-vivo antioxidant study there was a dose dependent decreasing and increasing of lipid peroxidation, glutathione levels in hydroalcoholic extract treated groups respectively. The histopathological investigation was also supported nephroprotective activity of C.pareira. All the results were shown that the plants C.pareirahydroalcoholic extract has significant nephroprotective activity.

Keywords: Nephrotoxicity, Cisplatin, Antioxidant.

ABSTRACT

Plants produce a diverse range of bioactive molecules, making them a rich source of different types of medicines. A regular and widespread use of herbs throughout the world has increased serious concern over their quality, safety and efficacy. Thus, a proper scientific evidence or assessment has become the criteria for acceptance of herbal health claims. In the present study, we examined the antioxidant effects of Terminalia Catappa plant extract. Dried and powered of T. Catappa was extracted with hexane, chloroform, methanol, ethanol and water. Total phenolic and flavonoid contents of different solvent extracts were determined. Of the different solvent extracts, methanol extract had the highest phenol and flavonoid content of 121.9±3.1mg/g and 59.6±1.5mg/g respectively. Antioxidant assays were carried out by using different in vitro models such as total reducing power, total antioxidant activity, lipid peroxidation inhibitory activity, DPPH radical scavenging activity and superoxide radical scavenging activity. methanol extract showed the highest total antioxidant activity of 41.4±0.45 µM Fe(II)/g. The EC₅₀ values of ethanol extract for lipid peroxidation inhibitory activity and DPPH radical scavenging activity was found to be 0.1 and 0.5 mg/ml respectively. The anti-oxidant activities of other solvent extracts were poor when compared to the ethanol extract. These results suggest that, the active antioxidant compounds are better extracted in ethanol and there is a direct correlation between the total polyphenols extracted and its anti-oxidant activity. The invitro anti-oxidant activity of T. Catappa justifies the ethno medical use of this plant.

Keywords: Medicinal plant; Terminalia Catappa; solvent extracts; anti-oxidant activity.

ABSTRACT

The aim of the present study is to enhance solubility of simvastatin by solid dispersion technique. Solid dispersions were prepared by fusion method by using various polymers. Formulation is optimized on the basis of acceptable solid dispersion properties and in-vitro release. In order to obtained best optimized product, 5 different formulations were developed. Different polymers like PEG 6000, HPMC 6000,HPC 1000 were taken as variables. Angle of repose, carr’s index, particle size, drug content and dissolution study were studied as response variables. The different physical properties showed best comparable results with drug. But higher percentage of drug release was observed when the formulation contained PEG6000 in 1:1.5 ratio (f5) compared to other formulations. Form this study it concluded that formulation (f5) which contained PEG (1:1.5) as polymer showed best dissolution profile compared to the drug. The formulation contained PEG 6000 was selected as optimized product.

Keywords: Simvastatin, PEG 6000, HPME 6000, HPC 1000.

ABSTRACT

Abutilon indicum Linn. (Malvaceae) commonly called Country Mallow is abundantly found as weed in sub-Himalayan tract and in hotter parts of India. The present study attempts to summarize the pharmacognostical profile of Abutilon indicum Linn. The study comprises of preliminary phytochemical screening, morphology, and histology.

Keywords: Abutilon indicum Linn., Country Mallow, Kangi, Malvaceae, Pharmacognostic.

ABSTRACT

The aim of the present study is to prepare Tinidazole microspheres by using different polymers. Microspheres were prepared by solvent evaporation method by using various polymers. Formulation is optimized on the basis of acceptable microspheres properties and in-vitro release. In order to obtain best optimized product, 6 different formulations were developed. Different polymers like Eudragit S100, HPMC 6000 and HPC 1000 were taken as variables. Particle size analysis, Shape and Surface Morphology, Flow properties, Degree of swelling, Drug entrapment efficacy, Invitro drug release study were studied as response variables. The different physical properties showed best comparable results with drug. But higher percentage of drug release was observed when the formulation contained Eudragit S 1000 in 1:1 ratio(f3) compared to other formulations. The formulation contained Eudragit was selected as optimized product.

Keywords: Tinidazole, HPMC, HPC, Eudragit.

ABSTRACT

The aim of this study to assess Rabbit Syndrome (RS) in case of Olanzapine treatment patients with Bipolar affective disorder. Rabbit syndrome (RS) is an antipsychotic-induced rhythmic motion of the mouth/lips resembling the chewing movements of a rabbit. The movement consists of a vertical-only motion, with no involvement of the tongue. Long-term exposure to typical antipsychotics has clearly been associated with RS, but little is known of the risk of RS due to exposure to newer atypical antipsychotics. There have been isolated reports of RS in patients treated with the atypical agents Olanzapine, Risperidone, Aripiprazole and Clozapine. We have observed two cases of Rabbits syndrome in a 45 year old female diagnosed with bipolar affective disorder and 35 year old male patient diagnosed with generalized anxiety and depression treated with Olanzapine.

Keywords: Olanzapine, Rabbit Syndrome.

ABSTRACT

The purpose of this study was to develop chitosan based anastrozole nanoparticles for treatment of breast cancer. An ionic gelation method was used to prepare anastrozole controlled-release nanoparticles. A 3² full factorial design was employed. Experimental variables such as concentration of CS and cross-linking agent sodium TPP were varied to study their effect on drug entrapment efficiency and release rates of drug from nanoparticles. Fourier transform infrared spectroscopic (FTIR) analysis and differential scanning calorimetry (DSC) were employed to determine any interactions between drug and polymer. The FTIR studies revealed no chemical interaction between the drug and the polymer. Entrapment efficiency of nanoparticles ranged between 51.51 ± 0.81 % to 84.35 ± 1.06 %.In-vitro release studies were performed in phosphate buffer saline of pH 7.4. A slow release of anastrozole up to 72 h was observed. Mean particle size of nanoparticles ranged between 1635 nm to 72.30 nm with mean particle size of 273.6 nm, while zeta potential 0.52 mV. DSC results indicated that the anastrozole entrapped in the nanoparticles existed in an amorphous or disordered-crystalline status in the polymer matrix. Scanning electron microscopy was done to study the surface morphology. Results revealed that more spherical shaped particles with possible aggregation. The highest correlation coefficients were obtained for the Higuchi model, suggesting a diffusion mechanism for the drug release. The results demonstrated that anastrozole nanoparticles with chitosan could be an alternative delivery method for the long-term treatment of breast cancer.

Keywords: Anastrozole; Nanoparticles; Factorial design; Ionic gelation; Controlled release.

ABSTRACT

A rapid, specific, sensitive Ultra-performance liquid chromatographic method has been developed for determination of Losartan Potassium, Amlodipine and Hydrochlorothiazide impurities and its degradation products in pharmaceuticals preparation. 16 impurities including degradation as well as process related impurities have been well separated. UPLC was performed on a C18 column with “mobile phase A” consisting of 90:10:0.1 v/v/v of water, Acetonitrile and TFA; while “mobile phase B” consisted of 10:90:0.1v/v/v of water, Acetonitrile and TFA. The mobile phase was pumped in a gradient manner at the flow-rate of 0.35 mL min⁻¹. Ultraviolet detection was performed at 238 nm. Losartan Potassium, Amlodipine and Hydrochlorothiazide and its degradation products along with process impurities were chromatographed with a total run time of 20 minutes. Calibration showed that response of impurities was a linear function of concentration over the range LOQ to 150% of the target concentration (r ²≥0.999) and the method was validated over this range for precision, accuracy, linearity and specificity. For precision study, percentage relative standard deviation of each impurity was <15% (n=6). The method was found to be precise, accurate, linear and specific. The method was successfully employed for estimation of Losartan Potassium, Amlodipine and Hydrochlorothiazide impurities and its degradation products in finished product Tablets formulation.

Keywords: UPLC–Losartan Potassium, Amlodipine and Hydrochlorothiazide, Impurities and Method validation 

ABSTRACT

The present work was aimed to develop a 24 hour modified release dosage form of model drug propranolol HCl using different waxes by hot melt granulation technique. Three waxes: stearic acid, cetostearyl alcohol and glyceryl behenate were used at 5%, 10%, 15% 20% and 30% concentration in matrix systems. Prepared formulations showed good tabletting characteristics. The effect of various waxes and their concentrations were studied on the release of the drug. The drug release profile from the wax matrices were tired to match with targeted dissolution profile (TDP). Matrix systems containing 30% stearic acid showed dissolution profile similar to TDP for initial hours and later the release was slower than TDP. In case of matrix system containing 30% cetostearyl alcohol, the drug release was within the TDP and with systems containing glyceryl behenate, propranolol HCl release was within TDP with 10%, 15% and 20% concentration. The release of drug was slower than TDP for matrix system containing 30% glyceryl behenate. The matrix system showing drug release within TDP followed non- Fickian diffusion.

Keywords: Matrix, stearic acid, cetostearyl alcohol, glyceryl behenate, targeted dissolution profile

ABSTRACT

Imidazoles are nitrogen containing heterocyclic compounds, widely present in nature. The imidazole ring is a part of several important natural products, including purine, histamine, histidine and nucleic acid. Highly substituted imidazoles derivatives belong to a crucial structural motif that is seen in many pharmaceutically and biologically interesting molecules. They have been intensively used in medicinal chemistry as drugs such as antihistaminic¹, antiulcerative,² antihelmentic,³ and antipsychotic.⁴ Several benzimidazoles have been reported as antiviral,⁷ anticoagulant,⁸ antiinflammatory,⁹ antibacterial¹⁰ and anticancer agents.¹¹ The present work deals with the derivatization of 2-(1H-benzo[d]imidazol-2-yl)-3-oxobutanenitrile with thiazolidin-4-one, oxazolidin-4-one and azetidin-2-one and characterization. All the compounds were tested for biological activity against E. coli, S. typhi, S. aureus while streptomycin was used as standard.

Keywords: Imidazoles, Benzimidazole, Heterocyclic compound. 

ABSTRACT

Generic forms of chemically- synthesized drugs must exhibit chemical identity and be bioequivalent in healthy human subjects. Biologic products are 100- to 1,000-fold larger than chemically synthesized drugs, with sophisticated three-dimensional structures, and can be mixtures of isoforms rather than pure homogeneous entities. Therefore, the development process for biosimilars is more complex than for a true generic and the demonstration of approvability for biosimilars differs from the standard generics approach as it is based on a comparability exercise rather than on demonstration of bioequivalence. This study examines the case of a Low-molecular-weight heparins (LMWHs): enoxaparin which is among smallest biological molecules. Different chemical tests such as Nuclear Magnetic Resonance (NMR), Size exclusion Chromatography, Specific absorbance, stability tests and biological assay (anti-factor Xa activity and anti-factor II a activity) were used for a comparability exercise focusing on quality and structural aspects of enoxaparin biosimilar product compared to the reference product. All tests and comparative studies showed no significant difference. in fact the data observed suggests comparable results even under accelerated conditions of stability study. This study suggests that there is no significant difference in the profile structure and overall studied quality aspects of the reference product compared to the similar biological medicinal product. however specific analytical methods as well as additional biological and pharmacological tests may be used to address their interchangeability.

Keywords: Biologic, Biosimilar, comparability, Low-molecular-weight heparins, enoxaparin, Size exclusion Chromatography, Nuclear Magnetic Resonance, Specific absorbance, biological assay.

ABSTRACT

A modified liquid- liquid extraction based reverse phase high performance liquid chromatographic method has been developed and validated for the determination of Furosemide in human plasma. The chromatographic separation was achieved with Pinnacle C18 column (250 x 4.60 mm, 5μm i.d.) and a mobile phase comprising of a mixture of Methanol: Water: Triethylamine (70:30:0.1v/v/v), pH adjusted to 3.2 with orthophosphoric acid was used with UV detection at 274nm. The internal standard spironolactone structurally related to Furosemide was used. The retention time for Furosemide and spironolactone was found to be 3.75min and 8.12min respectively.  A calibration curve was linear in the concentration range of 200-2200ng/ml for Furosemide in blank human plasma. The % recovery from human plasma was found to be in the range of 89.41 to 93.91 for Furosemide. The lower limit of quantitaion was found to be 200ng/ml and no interference was found from endogenous compound. The specificity, linearity, accuracy, precision and stability of the method were evaluated from spiked human plasma sample as per EMA (European Medicine Agency) guideline. The method can be used for supporting therapeutic drug monitoring and pharmacokinetic studies.

Keywords: Furosemide, Spironolactone, High Performance Liquid Chromatography, Human plasma.

ABSTRACT

Aim of present study was to develop self emulsifying drug delivery system (SEDDS) for enhancement of solubility, dissolution rate and oral bioavailability of model drug Rilpivirine. Fifteen formulations were prepared using different oils, surfactants and co-surfactants. A pseudo ternary phase diagram was constructed to identify the self-micro emulsification region. Further, the resultant formulations were investigated for clarity, phase separation, drug content, % transmittance, globule size, freeze-thaw stability and in vitro dissolution studies. On the basis of dissolution profile and other above mentioned studies, F5 was found to be the best formulation of Rilpivirine SEDDS which contains Captex 355(Oil), Kolliphor RH 40 (Surfactant) and PG (Co-surfactant). In vivo studies revealed that the oral bioavailability of Rilpivirine from SEDDS was 2.2-fold higher compared to that of pure Rilpivirine suspension in rats, suggesting a significant increase (p<0.05) in oral bioavailability of Rilpivirine from SEDDS formulation.

Keywords: Rilpivirine, SEDDS, Captex 355, Solubility, Bioavailability studies.

ABSTRACT

Cyclophosphamide is well known anticancer drug used for the treatment of several types of cancers. In combination with other drugs cyclophosphamide is prescribed to treat breast cancer, leukemia and ovarian cancer. But cyclophosphamide reduces the production of blood cells from the bone marrow. In the present investigation to combat the toxicity of cyclophosphamide, aqueous extract of immunomodulator plant like Ashwagandha was studied against toxicity of cyclophosphamide. After administration of cyclophosphamide @ 250 mg/kg b.w. (tablet) orally by gastric intubation method to rats, marked reduction in total count of WBC, ALC and Platelets were observed and slightly reduction in RBC was observed on day 4^th. When Ashwagandha (300mg/kg b.w.) administered five days prior to cyclophosphamide administration and continued for ten days then significant increase in total count of WBC, ALC and Platelets were observed after treatment but there is no significant statistical difference in the RBC count was seen in all groups during the period of the study. Thus findings of present investigation showed that therapeutic potency of Ashwagandha ameliorate the toxicity produced during cancer chemotherapy by mitigating the bone marrow depression.

Keywords: Cyclophosphamide, Ashwagandha, Rats, Red Blood Cell, White Blood Cell, Platelets and Absolute Lymphocyte Count.

ABSTRACT

In the present paper, the authors described a novel Liquid chromatography–tandem mass spectrometry (LC–MS/MS) method for the determination of montelukast in human plasma using montelukast d6 as internal standard (IS). After solid phase extraction (SPE), the analyte and the IS were chromatographed on a C18 columns using a isocratic mobile phase composed of acetonitrile–5mM ammonium acetate (80:20, v/v) pumped at a flow rate of 0.8mL/min. The proposed method was validated in the range of 5.01–599.91 ng/mL as per the US FDA guidelines. Precision and accuracy results were calculated using five successful calibration curves. Analyte stability in true samples and in plasma samples under different conditions were established and results met the acceptance criteria. The chromatographic run time was set at 3 min, which makes the proposed method is high through put. The method was successfully applied to a pharmacokinetic study in healthy South Indian male subjects under fasting condition.

Keywords: Montelukast, Solid–phase extraction (SPE), LC–MS/MS, Method validation, Pharmacokinetics.

ABSTRACT

A simple, selective and rapid reverse phase high performance liquid chromatographic (RP-HPLC) method for the analysis of Gliclazide in bulk and in tablet dosage form has been developed and validated. Sample was analysed on a Enable C18 (250mm X 4.6 mm i.d, particle size 5μm) column. The mobile phase consist of Methanol: Water (pH 3.5) in the ratio of 85:15v/v which was sonicated to degased and delivered at a flow rate of 1ml/min at ambient temperature. The retention time of Gliclazidewas 3.7+0.02 minutes. Studies were performed using an HPLC system equipped with a UV detector; the response was monitored at 230 nm.The calibration curve was linear over the concentration range of 20-70 μg/ml (r²=0.999). The limit of detection for Gliclazide was found to be 0.2438 μg/ml and the limit of quantification limit was about 0.7388 μg/ml. The accuracy of the method was established based on the recovery studies. The proposed method can be applied to the routine analysis of Gliclazide in bulk and in tablet dosage form.

Keywords: Gliclazide, ICH, RP-HPLC, Validation.

ABSTRACT

The growth profile of preschool children living in some rural areas of Bayelsa state was studied. The number of children studied was three hundred (300) out of which 158 were males and 142 were females. The result from the analysis of the anthropometric data obtained showed 93.5% of the children to be normal, 6.5% have mild PEM while non of the children had moderate nor severe PEM. The standard used for this study was the NCHS/WHO (1977) anthropometric data. The overall mean (x) weight for-age-for the male children was 17.5kg while that for the female children was 17.0kg.on the other hand, the overall mean (x) height for-age-for both male and female children is 1.11m. The mean height for-age-for female children aged 2, 3.5 and 5 years was higher than that of the male children by 0.3, 0.1 and 0.11m. the mean weight for-age-for male children and 2,3, 3.5 and 5 years is higher than that of the female children by 0.7kg , 0.3kg, 0.7kg and 1.11kg respectively. The occupational level of the parent is reflected on the growth profile of the children, for instance parent whose occupation were carpenters and unemployed contributed immensely to the 6.5% of children having mild PEM. The result showed that the children are well nourished. This is contrary to what is popularly believed of children in the childworld countries.

Key word: Protein Energy Malnutrition, World Health Organisation, National Center For Health Statistic, Anthropometry

ABSTRACT

Practically water insoluble Simvastatin has been accused for being poorly absorbed from gastro intestinal tract. With an aim to improve the solubility and dissolution characteristics of the drug, solid dispersion and surface solid dispersion were prepared by using different water soluble and insoluble carrier at different ratio. Dispersions were made by solvent evaporation technique and undergo drug content test, compatibility by FT-IR, DSC thermal study and in vitro drug release study. FT-IR and DSC thermographs showed the compatibility of the drug and carrier in the incorporated ratio. All the preparations were found to improve the dissolution behavior of Simvastatin significantly compare to the binary physical mixtures and the pure drug. The suitability of solid dispersion and surface solid dispersion technique was evaluated. Also the efficacy of the carriers to improve the dissolution behavior was compared. Tablets were formulated by incorporating dispersions and were subjected to various physical tests including thickness, diameter, hardness, average weight and disintegration time. Their release pattern was compared with compressed matrix of drug and two brand products available in Bangladesh market. Their drug release pattern was further characterized with mean dissolution time (MDT), fractional dissolution time (T_50% and T_80%) and percent dissolution efficiency. Tablets made of dispersion with HPMC, sodium starch glycolate and croscarmellose sodium were found to have better release rate and extent than the drug and the brand products.

Keywords: Phase homogenization; Release exponent; Mean dissolution time; Dissolution efficiency; Surfactant. 

ABSTRACT

The main objective of the present investigation was to formulate and evaluate chronomodulated pulsatile drug delivery system of Trimetazidine Hydrochloride which was aimed to release the drug after lag time (6 hrs) in order to mimic circardian rhythm of Angina Pectoris.Preformulation studies and compatibility studies were carried out for drug and excipients. Core tablet was prepared by direct compression using sodium starch glycolate as superdisintegrant and press coated with different polymer & varying its ratio. Further prepared tablets were optimized using 32 full factorial design. Nine batches were prepared varying the amount of polymer and ratio of polumer (HPMC K4M: EC) and they were evaluated for precompressional and postcompressional tests. Optimized batch was derived statistically using desirability function (Minitab 17).The Model was validated by formulating the check point batch. Accerelated stabilitiy study was carried out of optimized batch. Preformulation and compatibility studies was carried out using FTIR , DSC which shows satisfactory results, no interaction was found between drug and excipients. Press coating of core tablet with the combination of HPMC K4M and EC was found to be providing the desired release. Results of precompressional and postcompressional was found to be within the limits. Varying  the amount of coating and ratio of polymer have significant effect on lag time(Y1) as well as on time required for 90% drug release (Y2).Optimized batch shows lag time of 6 hrs followed by complete release within 1 hrs which is desiered in case of pulsatile delivery. No significant bias was found between predicted and observed value of check point batch.The data of stability study revealed that the optimized formulation is stable. Pulsatile drug delivery system of Trimetazidine Hydrochloride for chronomodulated therapy can be prepared by press coating technique using 200 mg of coating and HPMC K4M:EC(10:90) ratio of polymer which will provide lag time of 6hrs and complete release within 1 hrs.

Keywords: Chronomodulated, Pulsatile release, Lag time, Trimetazidine Hydrochloride, HPMC K4M , EC, Press Coated tablet