ABSTRACT

Depression is commonly found as a co-morbid condition in diabetes. The relationship between the diabetes and depression is bidirectional. Coexistence of diabetes and depression is associated with poor symptom control, increased suffering, health care expenditure, disability, decreased quality of life and greater risk of death. Depression in diabetes is under diagnosed and undertreated. Depression adversely effect on both psychological well being and diabetic outcomes. Management of depression in diabetes should be directed toward improving psychological and medical outcomes, and quality of life. Pharmacologic and psychotherapeutic interventions shown to be effective in the management of depression in diabetes, which improve the glycaemic control and reduce the risk of short term complications. Selective serotonin reuptake inhibitors(SSRI), Serotonin norepinephrine reuptake inhibitors, and atypical antidepressants (eg. Buproprion) are preferred pharmacologic interventions for patients with diabetes and depression.

Keywords: Diabetes, Depression, Glycaemic control, Anti depressants.

ABSTRACT

Even today the most preferred delivery of drugs is still through oral route but because of some inherited limitations with this route, various other routes have been explored including transdermal. Delivery and complete absorption of the drugs is the major concern these days due to various reasons including poor solubility and incomplete bioavailability, this could be due to incomplete presystemic absorption or presystemic degradation. Transdermal drug delivery system is the method by which the drug absorption occurs through the skin primarily for its systemic effect. It provides better therapeutic efficacy and safety for the administration of insulin. Most of the oral anti-diabetic drug exhibit low bioavailability and hence a poor patient compliance. Hence, it can be used as better site for delivery of numerous drugs including proteins and peptides such as insulin.

Keywords: Insulin; transdermal delivery; antidiabetic drugs; bioavailability

ABSTRACT

Metabolic syndrome is a constellation of interrelated cardio-metabolic risk factors that include Central Obesity, Hyperglycemia, Hypertension and Dyslipidemia. It has been estimated that about 1 in 5 (20.4%) adults in the U.S. have high blood pressure, it is very crucial to evaluate the serious health problems, level of awareness and knowledge about conditions relevant to metabolic disorders. Metabolic syndrome is caused not by genetic defects alone; in most cases, genetic factors predispose a person to a disease, while lifestyle factors determine whether (and when) the disease will develop. Several studies have demonstrated clearly the importance of dietary factors and physical activity level in the development of the metabolic syndrome. Given the same dietary and lifestyle factors, some individuals may be more prone to type 2 diabetes than others because of different genetic backgrounds. At a public health level, more attention must be given to modification of lifestyles of the general public to reduce risk of obesity and T2DM and to increase physical activity. At a clinical level, individual patients with increased metabolic risk need to be identified so that their multiple risk factors can be reduced. Considering the long asymptomatic period often preceding the manifestation of T2DM and CVD, early diagnosis could enable earlier targeted interventions such as implementation of healthy lifestyle changes in nutritional behavior and exercise or pharmacotherapy, thus reducing disease development. A deeper understanding of the underlying gene- interactions  In terms of both public health  and for individuals and genetic subgroups is therefor needed.

Keywords: Metabolic Syndrome(MetS) ,Type II Diabetes Mellitus (T2DM),Impaired Fasting Glucose(Ifg), Maturity Onset Diabetes Of the Young(MODY)

ABSTRACT

Buccal administration of drugs provides a convenient route of administration for both systemic and local drug actions. However, the preferred site for retentive oral transmucosal delivery systems and for sustained- and controlled-release delivery devices is the buccal mucosa, mainly because of the differences in permeability characteristics between the two regions and the buccal mucosa’s expanse of smooth and relatively immobile mucosa. The buccal mucosa offers excellent possibilities for the (long-term) delivery of suitable drugs, especially for metabolically unstable drugs, such as peptides. In the development of these buccal drug delivery systems, mucoadhesion of the device is a key element. Mucoadhesive polymers have been utilized in many different dosage forms in efforts to achieve systemic delivery of drugs through the buccal mucosa. Buccoadhesive drug delivery is relatively new drug delivery strategy; in this traditional polymers are replaced by novel bioadhesive polymers such as thiomers & lectins etc. to overcome limitation of traditional polymer.

Keywords: Buccal Drug Delivery, Oral mucosa, Buccal absorption, Mucoadhesion, Buccoadhesive Polymer, Buccoadhesive Dosage Form

ABSTRACT

Microsponge is unique drug delivery technique used for topical controlled drug delivery system as well as oral controlled drug delivery system. Microsponges are highly porous surface polymeric microspheres.  A well typical Microsponges (25 µm) can have up to 250000 pores approximately, due to  they also  give prolonged  release of active ingredients with continuously and reduce side effect, enhanced the stability of active ingredients. Mostly liquid – liquid suspension polymerization and quasi-emulsion diffusion methods are used for preparation of microsponges with different polymer such as Ethyl cellulose, Eudragit RS- 100, Eudragit S-100 and Eudragit E-100, Eudragit L-100, acrylic polymer etc used as formulation. Various therapeutics agents are loaded into Microsponges and then consolidate into different formulation like as gel, cream, and tablets. Drug is released from microsponges by different trigging system such as pressure system, solubility system, temperature change and pH triggered system. Various process parameters like concentration of drug and polymer, concentration of surfactants, volume of internal and external phase etc. affect the particles size, production yield, encapsulation efficiency and release of drug. In market different Microsponges based product are available such as NeoBenz®Micro, Neo®MicroSD, NeoBenz®Microwash,  Retin A Micro,  Retinol 15 Night cream, EpiQuin Micro and Retinol cream etc.

Keywords: Controlled release, drug delivery, healthcare systems and Microsponges.

ABSTRACT

Buccal drug delivery is the most innovative delivery system which releases the drug to buccal mucosa by avoiding first-pass metabolism in the liver and pre-systemic elimination in the gastrointestinal tract. Buccal route is an attractive route of administration for systemic drug delivery. Buccal bioadhesive films, releasing topical drugs in the oral cavity at a slow and predetermined rate, The mucosa of the buccal cavity is the most easily accessible transmuocosal site. Buccal transmucosal delivery helps to bypass first- pass metabolism by allowing direct access to the systemic circulation through the internal jugular vein.

Keywords: First-pass metabolism, Buccal route

ABSTRACT

Nanotoxicology is an emerging new multidisciplinary field of science. This new technology deals with measures, manipulates, and manufactures at the atomic, molecular, and supramolecular levels, aimed at creating materials, devices, and systems with fundamentally new molecular organizations, properties, and functions associated with greater strength, stability, chemical and biological activity. They are used in rapidly increasing nanoproducts, nanodevices, electronics, diagnostics and drug delivery systems. They are present in a variety of consumer products such as foods, drugs, cosmetics, food colour additives, food containers, paints and surface coatings. Because of their extremely small size they are capable of entering the human body by inhalation, ingestion, skin penetration, intravenous injections and medical devices, and have the potential to interact with intracellular macromolecules. Because of their greater stability they are anticipated to remain in the body and in the environment for long periods of time. However, information on their potential adverse health effects is very limited at the present time. It is not known at what concentration or size they can exhibit toxicity. Therefore, there are obvious public safety concerns. This has led to the initiation of a new research discipline commonly known as Nanotoxicology. The current review article reveals the concept of Nanotoxicology from nanomedicine and non-medical nanoparticles.

Keywords: Nanotechnology, nanoparticles, nanomaterials, nanomedicine, nanotoxicity.

ABSTRACT

Hydrogels are cross-linked polymers with the capacity to swell in a fluid medium. Crosslinking in hydrogels happens by synthetic or physical means relying upon the polymer properties and exploratory conditions. Attributable to a vast assortment in concoction structure and crosslinking strategies, different hydrogels have been set up for different applications in pharmaceutical and biomedical fields. This part starts with brief presentation, preferences, detriments, order, sorts of hydrogel are talked about likewise. They are insoluble because of the nearness of compound (tie-focuses, intersections) and/or physical crosslinks, for example, ensnarement’s and crystallites. These materials can be blended to react to various physiological boosts present in the body, for example, pH, ionic quality and temperature. At last, the part finishes up with known hydrogel applications in the pharmaceutical area.¹

Keywords: Hydrogels; Applications in drug delivery; Drug release; Polymer network structure, Water; Pores

ABSTRACT

The Mouth Dissolving Drug Delivery Systems was an advancement that came into existence in the early 1970’s and combats over the use of the conventional tablets, syrups, capsules which are the other oral drug delivery systems. Orally disintegrating dosage forms can address the pharmaceutical needs of the paediatric and geriatric patient group having difficulties in swallowing the conventional solid oral dosage forms. Orally disintegrating dosage forms also have the advantage of self medication, pain avoidance hence better patient compliance. Taste masking of bitter drugs is an important parameter. Orally disintegrating dosage forms may have an added advantage of bypassing first pass metabolism. Acyclovir is an antiviral drug used for the treatment of herpes simplex virus (HSV), mainly HSV-1 and HSV-2 and varicella zoster virus. It is a BCS class III drug. Hence an orally disintegrating tablet formulation of acyclovir was prepared by direct compression techniques after incorporating superdisintegrants croscarmellose sodium , sodium starch glycolate and Crossprovidone . Eight formulations were prepared. Tablet containing sodium starch glycolate and croscarmellose sodium showed excellent in vitro dispersion time and drug release as compared to other formulation. After   study of eight formulations F8 showed short dispersion time with maximum drug release in 25 min. It is concluded that fast disintegrating acyclovir tablets could be prepared by direct compression using superdisintegrants.

Keywords: Acyclovir, ODT, Superdisintegrants

ABSTRACT

A simple, precise and accurate stability indicating RP-HPLC method has been developed and subsequently validated for the simultaneous estimation of Sildenafil citrate and Estradiol valerate in bulk and pharmaceutical formulation. The separation was carried out using C₁₈ column (150mm x 4.6mm, 5μm), mixture of acetonitrile and water 80:20 % v/v as a mobile phase with a flow rate of 1 ml/min and the effluent was monitored at 290 nm using PDA detector. The retention time of Sildenafil citrate and Estradiol valerate were 2.55 min and 5.56 min respectively. The method is linear over the range of 125 - 750 μg/ml and 5 - 30 μg/ml for Sildenafil citrate and Estradiol valerate respectively. The method was found to be precise, accurate and specific during the study. The percentage assay was found to be 100.68 % and 99.58 % for Sildenafil citrate and Estradiol valerate respectively from the tablet formulation. Sildenafil citrate and Estradiol valerate were subjected to stress condition to check the degradation behaviour of them. The drugs undergo degradation under acidic, basic, oxidative and thermal condition. The proposed method enables rapid quantification and simultaneous analysis of both drugs from commercial formulations without any interference of excipients. So, the method can be used for routine analysis of Sildenafil citrate and Estradiol valerate in combined tablet formulation.

Keywords: Sildenafil citrate, Estradiol valerate, RP-HPLC, Simultaneous estimation, Stability indicating

ABSTRACT

corn silk tea on patients having kidney Stones  and its relationship with kidney stone elimination within 3 days  at Al -Najaf City. A quasi-experimental study design. Sociodemographic data were obtained on one hundred (100) patients having kidney stones (males and females) at kidney lithotrity Najaf center over two years period. Statistical methodology comprised Pearson X²  test, Likelihood Ratio, Correlation coefficient  and logistic regression analysis. A significant inverse relation was observed between patient's age (43-53) years and daily activity. Causes correlation among all the studied  items of patients with kidney stones were significantly correlated with (0.01) level (2-tailed) Pearson Correlation among patient's complain; patient's psychological data and patient's diagnosis. Causes correlation ship between patient's desired and response to share the herbal treatment and their knowledge  were high significant difference (HS), X^2=200,  c.c. (0.707), P value (0.00001) HS. These data have shown that aged patients (males and females) a correlate of kidney stones is associated with old age (43-53) years and daily activity. This association seems to be largely explained by patient's (complain, psychological data and patient's diagnosis). The association between patient's desired and response to share the herbal treatment and their knowledge were high significant. Kidney stones has long been viewed as both an indicator of renal failure and as a stressful situation associated with high morbidity and mortality risks. Further analysis suggests to apply on kidney stone's patients in different communities and large population using the chicken's gizzard membrane and corn silk drink to be largely explained.

Keywords: Chicken gizzard membrane, Corn Silk, tea, patient, kidney stones, elimination.

ABSTRACT

Malnutrition is defined to be the condition resulting from relative or absolute deficiency of one or more essential nutrients. The school age period is nutritionally the prime time to build up the body stores of nutrients in preparation for rapid growth in adolescents. The nutritional state is therefore critical to the development and wellbeing of the nation. The physical growth of the child is thus reflected by different Anthropometric measurements especially height and weight. This study was done to evaluate the level of malnutrition in government (govt.) higher primary school in Bengaluru. Cross sectional descriptive survey was done using a structured questionnaire, the dependent variables for this study were the anthropometric measurable like height for age and independent variables for the study were occupation of parents, family income, maternal education, gender and type of residence (kacha or pucca). A total of 404 children were included from the govt. primary school in the study. It was seen that maximum children belongs to the 13+ age group most of them being boys. Their family monthly income being in the range of Rs.5000 to 6000. Most of their family members are daily laborer’s and housewives by profession. Therefore it can be concluded that the Mother’s Education is directly proportional to the child health. Hence development in fields on family employment, mother’s education will result in improved child health.

Keywords: Malnutrition, Nutritional State, Physical State, Income, Anthropometric Measurements.

ABSTRACT

The present study deals with docking of Hematoporphrin with various anticancer drugs targeting enzymes. The targets used were PDB-ID 2Y3I, PDB-ID 3OZZ, PDB-ID 3UEN and PDB-ID 4O33. Hematoporphyrin docked with these enzymes and interactions between the enzyme and compound were measured and compared with standard Paclitaxel. The study concluded that, the compound (Hematoporphyrin) isolated from plant were high interactions with PDB-ID 4O33 when compared to standard.

Keywords: Docking, Hematoporphyrin, Paclitaxel, Protein Data Bank, Interactions.

ABSTRACT

Over the last decade, diabetes mellitus has emerged as an important clinical and public health problem throughout the world. The aim of the study is   perceive the Potentiality of a newer oral Antihyperglycemic combination therapy over conventional therapy in type 2 diabetes. The prospective study was conducted over a period of six months in the department of Medicine, Guntur City Hospital. The prevalence of type2 diabetes was high in male 65.79 % than female 34.21%. Majority of the patients  (23.68 %) belonged to age group of 51–55 years. Majority of patients (55.26%) having a family history of Diabetes. Majority of patients receiving Combination of Glibenclamide + Metformin (60.53%), evaluated for effect on FPG for both combinations. The mean changes in FPG were noted. In the same way effect on HbA₁c also noted. Mean changes in for every month HbA₁c will be noted. Our study reveals that Combination therapy with Metformin plus Glimepiride is more effective than Glibenclamide plus Metformin; in improving glycemic control in type 2 diabetes, while also allowing a reduction of the dosage of each drug.

Keywords: Diabetes Mellitus, ADA, HbA₁c, FPG, Glibenclamide, Metformin, Glimepiride.

ABSTRACT

Transfersomes loaded with lornoxicam, a potent non-steroidal anti-inflammatory drug, were developed by thin film hydration method for transdermal delivery of lornoxicam. The composition of phospholipid (soya lecithin), edge activator (span 80) and the drug (lornoxicam) was optimized based on vesicle size and entrapment efficiency. The optimized formulation was compared with lornoxicam loaded vesicles without the edge activator. The developed transfersomes of lornoxicam and lornoxicam loaded vesicles without edge activator were compared for in vitro permeation of lornoxicam through dialysis membrane and for ex vivo permeation through porcine ear skin. The average vesicle diameter of the optimized formulation was 678 nm with average drug entrapment efficiency of 65.3%. The in vitro flux obtained for the optimized formulation was 79.1µg/cm²/h while that for formulation without edge activator was found to be 70.2µg/cm²/hr. The ex vivo flux of lornoxicam through porcine ear skin obtained for optimized formulation of lornoxicam loaded transfersomes was 13.2µg/cm²/h while that for formulation without edge activator was 7.5µg/cm²/h. The developed transfersomal formulation was stable on storage for 30 days at 4 ± 1^o C with respect to drug content and vesicle size.

Keywords: Deformable vesicles, non-steroidal anti-inflammatory, edge activator, vesicle size, entrapment efficiency, in vitro and ex vivo permeation

ABSTRACT

Diabetic mellitus goes with metabolic disorders involving hyperglycaemia and lipid disorders. The study investigated the activity of aqueous ginger extract on the glucose level and lipid profile of cholesterol-fed diabetic rats.  The rats were randomly distributed into four groups of 5 rats per group. Group A (control) were placed on normal rat feed. Diabetes was induced in groups B, C, and D by intraperitoneal administration of one dose of alloxan monohydrate (150mg/kg/bwt) and fed diet mixed with 1% cholesterol. The rats in groups C and D were orally administered with 250 and 500mg/kg/bwt of ginger extract respectively for 14 days. Biochemical parameters were analysed by standard methods. A significant decrease (P<0.05) in the blood glucose concentration in the ginger administered groups (C and D) was observed compared to diabetic cholesterol-fed rats (group B). After 14 days of aqueous ginger extract administration (250 and 500mg/kg/bwt), the serum total cholesterol level reduced in the test groups (C and D) relative to the test control group (group B) (P>0.05). There was a statistical increase in the serum triacylglycerol level in group B compared to group A (P<0.05) but the extract administration at 500mg/kg/bwt significantly led to a reduction of triacylglycerol compared to group B (P<0.05). It can be concluded that the extract possess hypoglycaemic and hypolipidaemic properties and confirms its use in the traditional medicine. This result should be taken with caution as the extract did not restore the serum levels of these parameters to the same levels as the non-diabetic control groups.

Key words: alloxan, Ginger, glucose, lipid profile.

ABSTRACT

There are folkloric claims that Aloe vera has many pharmacological properties which have not been conclusively investigated. The aim of the study is to investigate the protective/toxic effects of chronic administration of Aloe vera gel extract on the haemostasis, haematology and renal handling of electrolytes, urea and creatinine in Wistar rats. The experimental animals were grouped into four: group 1(control) received vehicle and the test groups (2,3,4) received different doses of the extract (200, 300, and 500mg bwt/day ) respectively for 21 days. The bleeding time significantly decreased as the concentration of the extract increased while the clotting time increased relative to the control (P<0.05). The packed cell volume was only significantly decreased in group four (P<0.05) while the control group had a higher white blood cell count compared to the test groups (P>0.05). The serum electrolytes, urea and creatinine were not altered significantly (P>0.05). From the results of this study, it can be concluded that the chronic administration of Aloe vera gel did not disrupt the renal function of the wistar rats. 

Keywords: Aloe vera, haematology, haemostasis, electrolyte.

ABSTRACT

Present  study  describes  the  spectrophotometric  method  development  and  subsequent  validation  of  dolutegravir  with  greater  precision  and  accuracy.  AIDS  is  the  most  dreadful  disease  in  the  society;  this  has  a  very  high  mortal  rate  among  the  countries,  as  results  loosing  many  beneficial  personalities.  There  are  many  antiviral  and  antiretroviral  drugs,  brought  forward  by  many  efficient  scientists. A  simple,  accurate,  novel,  safe,  and  precise  method  could  be  developed  for  the  estimation  of  Dolutegravir.  Spectrophotometric  measurements  were  carried  out  using  Schimadzu    double  beam(UV-1800  model)  Ultra  violet  visible  spectrophotometer  with  10mm  matched  quartz  cells  and  water  as  solvent. Linearity  for  the  method  was  found  in  the  range  of  2-14μg/ml  (r²=0.997).  Tablet  formulation  was  analyzed  and  %  assay  for  the  absorption  maxima  was  found  to  be  95.6%. The proposed method was validated as  per  ICH  guidelines.  Validated  studies  demonstrated  that  proposed  method  is  simple,  accurate,  precise,  specific,  rapid,  reliable,  and  reproducible.

Keywords:  Dolutegravir, spectroscopy, dosage form, validation.  

ABSTRACT

The present study was to evaluate preliminary phytochemical analysis and in vitro cytotoxic activity on root extracts and fractions of Jatropha gossipiifolia (family Euphorbiaceae). The Chloroform and ethanol extract was obtained by hot continuous percolation by soxhlet apparatus. The phytochemical analysis of both the extracts shows the presence of flavonoids, alkaloids, tannins, phenolic compounds and steroids. Both the extracts subjected to in vitro cytotoxic activity against breast cancer cell line (MCF–7) cell line by MTT assay. The active extract (ethanol) was then subjected to fractionation by column chromatography by gradient elution from n hexane – ethanol. The fractions (chloroform 100%, chloroform: ethyl acetate, ethyl acetate: ethanol, ethanol 100%) The fractions were then subjected to in vitro cytotoxic activity against MCF– 7 cell line by MTT assay. The ethanol extract shows good anticancer activity. The percentage growth of MCF-7 cells in chloroform and ethanol extract treated against MCF-7 cell line was found to be 49.59 and 28.46 respectively. The EC50 value of chloroform and ethanol extract was found to be 0.00018 & 0.00055mg/ml respectively. The ethanol 100% shows good anticancer activity compared to other fractions against MCF-7 cell line with the percentage growth of 14.650 and EC₅₀ value was found to be 0.00087mg/ml.

Keywords: Jatropha Gossypiifolia, MTT assay, MCF–7 cell line, Column chromatography

ABSTRACT

The main objective of present investigation is to formulate fast dissolving tablets of Diclofenac sodium and to evaluate flow, mechanical and release properties of diclofenac sodium tablets formulated by using two different super disintegrating agents namely sodium starch glycolate and microcrystalline cellulose. Two batches of formulations were prepared. F₁ to F₄ are formulated by using SSG with varying concentrations of 10 mg, 20 mg, 30 mg & 40 mg. similarly next four formulations (F₅ to F₈) were formulated by taking MCC as superdisintegrant with varying concentrations of 10 mg, 20 mg, 30 mg & 40 mg. All the eight formulations are having good flow properties and are prepared by direct compression technique.  Compatibility studies were conducted by using FTIR and all the excipients used in the formulation were compatible with the drug.  All the eight formulations shows first order release. The dissolution kinetics was presented in Table 5. The dissolution rate followed first-order kinetics as the graphs drawn between log % drug unreleased vs time were found to be linear. The dissolution rate of diclofenac sodium was found to be effected by the concentration of the superdisintegrant (sodium starch glycolate) used in the preparation of tablets. Based on the dissolution rate, the order of drug release from the four formulations was F₄> F₃> F₂> F₁. The formulation prepared with 40 mg of sodium starch glycolate (F₄) was offered relatively rapid release of diclofenac sodium when compared with other concentrations employed in this investigation.

Keywords: Diclofenac sodium, SSG, MCC, Direct compression method.

ABSTRACT

To establish an HPLC method for the determination of sulfasalazine in human plasma and to study the pharmacokinetics in Indian healthy volunteers following oral administration of sulfasalazine enteric-coated tablets.  In the study, 08 volunteers were administered with single oral dose of 500mg of sulfasalazine enteric-coated tablets with marketed reference product. The plasma concentrations of sulfasalazine were determined by HPLC-UV method. Chromatography was carried out on C-18 column with mobile phase comprising methanol and ammonium acetate buffer (pH 7.0) in the ratio of 48:52 pumped at a flow rate of 0.8 ml min−¹. The retention time for sulfasalazine were 12.2±0.05 min, the pharmacokinetic parameters were calculated with aid of the software DAS2.1.1. The calibration curve of sulfasalazine was linear in the range from 1.00 to 10.00μg/ml (r²=0.998). The main pharmacokinetic parameters of sulfasalazine enteric coated tablets with marketed reference product were as follows: half life were (7.51±0.54) and (7.32±0.72) h, C_max were (7.7125±1.0125) and (7.6±0.30)μg/ml, T_max were (6.38±0.62) and 6.38±0.62)h, AUC(0~t) were (84.92±20.25) and (79.39±19.45)μg·h/ml, respectively.

Keywords: Sulfasalazine, methanol, ammonium acetate buffer, HPLC-UV method, t_1/2, C_max, T_max, and AUC (0~t).

ABSTRACT

The aim of the proposed work was to develop stable mucoadhesive in situ (Phenylepherine HCL) thermo-reversible nasal gel by cold technique and evaluated its efficacy against congestion due to allergic rhinitis. By means of hit and trial methodology screened formulations were prepare via numerous thermo-sensitive hydro-Gel (Pluronic F-127, Poloxamer 407) and muco-adhesives (Carbopol 934-P, Polyvinylpyrrolidone K-30, Hydroxy propyl methyl cellulose (HPMC), Sodium alginate and methylcellulose) and characterized. Out of 15 formulations; T1, T5, T7, T12 & T14 formulation compositions were selected on the basis of drug released (in-vitro or ex-vivo release found approx. up-to 97.8%) behavior, gelation and mucoadhesive strength. Resulted, drug transformed (crystalline to amorphous) form in gel state was indicated better drug absorption due to its improved physicochemical parameters. Additionally, optimized formulation (T1) histopathology and stability studied has been demonstrated none nasal mucosa damage and stable at storage conditions according to the ICH guidelines respectively. Therefore, the developed optimized thermo-reversible in-situ nasal (T1) gel was showed tremendous local safety action which can be considered to use for allergic nasal congestion and explore, further.

Keywords: Phenylephrine HCL, Mucoadhesive; Allergic Rhinitis; Decongestant; Permeation enhancers

ABSTRACT

The present study was undertaken to determine the forced degradation of Pyrazinamide, performed by various conditions such as acid, alkali, oxidation, thermal and photolytic. The study includes both Pyrazinamide in bulk and tablet formulation. The study based on available guidelines and main reference .Pyrazinamide has a Pyrazine nucleus. It is easily hydrolyzed by acid and alkali. The assay value of degraded products measured by intraday (30mins, 60mins, 90mins) and interday (1^st, 3rd, 5^th day) by UHPLC. Extensive degradation was observed in alkali hydrolysis method, and the degraded products were analysed by using UHPLC. At 90mins of intraday study using 0.1M NaOH, the degradation assay value of bulk and formulation were found to be 84.50% and 83.40% respectively. Intraday study, the degradation of bulk and formulation was observed on 1^st day with the assay value of 23.62% and 25.42% respectively. However complete degradation of Pyrazinamide was observed on 3^rd day and 5^thday. It was determined that Pyrazinamide was found to be extremely unstable under alkali condition.

Keywords: Pyrazinamide, Kromasil C₁₈ Column, Buffer, Acetonitrile UHPLC determination

ABSTRACT

Glaucoma is an optic neuropathy associated with retinal ganglion cell death that results in visual field loss. Elevated intraocular pressure (IOP) is a primary risk factor for the disease. Glaucoma is the second leading cause of blindness worldwide. Primary open angle glaucoma alone accounts for about 75% of all primary glaucoma. Timolol maleate (non selective β adrenergic antagonist) and Latanoprost (prostaglandin analogue) are commonly used drugs. Our aim of study is to compare the ocular hypotensive effect and safety of topical Timolol maleate (0.5%) and Latanoprost (0.005%) in patients of primary open angle glaucoma. A total of 60 patients with primary open angle glaucoma were included and studied for 6 months. One group of patients were given 0.5% timolol maleate eye drops twelve hourly and other group were given 0.005% latanoprost eye drops once a day. In our study both drugs were significantly effective in lowering the intraocular pressure. The mean fall in IOP in Timolol group was 6.69mmHg (26.10%) and in Latanoprost group was 7.20mmHg (28.5%) from pretreatment values. The difference between the values of mean of reduction in IOP from baseline IOP of the two groups was 0.512 mmHg that was statistically insignificant. The systemic and ocular side effects observed in two groups were comparable and both groups were well tolerated. Timolol maleate and Latanoprost both drugs are effective significantly in lowering the IOP, well tolerated and safe with negligible systemic side effects and comparable ocular side effects.

Keywords: Timolol maleate, Latanoprost, Safety, Efficacy

ABSTRACT

A simple, rapid, accurate, precise and economical reverse phase high performance liquid chromatographic method was developed for simultaneous quantification of two anti-hypertensive drugs Olmesartan and Chlorthalidone. The separation of both the drugs was achieved on BDS C18 250mm x 4.6 mm, 5m using a mobile phase of 10 mM orthophosphoric acid buffer and acetonitrile (45:55v/v) at a flow rate of 1.0 mL min^-1 and detection was performed at 212 nm using photodiode array (PDA) detector. The drug was subjected to various ICH prescribed stress conditions including hydrolysis (neutral, acid and alkaline), oxidation, photolysis and thermal degradation. The proposed method was validated with respect to specificity, linearity, accuracy, and precision, limit of detection (LOD), limit of quantitation (LOQ), stability and robustness as per ICH guidelines. The proposed analytical method could effectively separate the drug from its degradation products employed as stability indicating studies.

Keywords: Stability Indicating, Validation, Reversed phase, Liquid Chromatography, Forced Degradation, Olmesartan and Chlorthalidone.

ABSTRACT

This survey was designed to investigate the evaluation of synergic anticancer activity of Punica grantum L and Ziziphus mauritiana extracts by using invitro cytotoxicity assay, invitro and invivo antioxidant estimation. The invitro antioxidant activity of ethanol, aqueous and chloroform extracts of  Punica grantum L and Ziziphus mauritiana and combination of them was estimated by reducing power, diphenyl picryl hydrazyl scavenging and hydrogen peroxide scavenging assays using standard procedure, the invivo antioxidant activity was  also performed  by estimation of  Catalase and Glutathione in liver homogenate. The extracts were screened for their invitro cytotoxicity by trypan blue exclusion assay and Allium cepa root tips. The results displayed the 100µg/ml of both ethanol and aqueous extracts i.e. Punica grantum L and it’s combination with Ziziphus mauritiana having the maximum invitro antioxidant activity. Ethanol and aqueous extract of combination of Punica grantum L and Ziziphus and ethanol extract of Punica grantum L has produced the significant increase in the glutathione and catalase levels. The cytotoxic effect of ethanol extracts of Punica grantum L and Ziziphus mauritiana significantly increased in Ehrlich ascites tumour cells with an increase in concentration by trypan blue cytotoxic assay and also significant root growth inhibition in Allium cepa after 48h. The percentage decrease in mitotic index was found to be 27.28 % in 800 μg/ml of ethanol extracts of Punica grantum L and Ziziphus mauritiana. Accordingly, the synergic anticancer activity of illustrated extracts was evinced.

Key words: Antioxidant, cytotoxic assay, Punica grantum L, Zizipus mauritiana

ABSTRACT

A new Mannich base, N-(Piperidinomethyl)phthalimide (L), formed by the condensation of piperidine, formaldehyde and phthalimide, and its Cu(II) complexes have been synthesized. Their structures have been elucidated on the basis of elemental analysis, molar conductance, IR, UV-visible, mass, ¹H NMR and ¹³C NMR, EPR, magnetic and thermal studies. All the complexes exhibit octahedral geometry. Infrared spectral data show that the organic ligand is bidentate, binding through one of the two carbonyl oxygen atoms of the phthalimide moiety and the piperidine ring nitrogen and also the existence of coordinated water molecules. The X band EPR spectra of Cu(II) complexes in DMSO at room temperature were recorded and their salient features are reported. Thermal data of some of the compounds show that the thermal decompositions take place mostly in two steps to produce metal oxides as final residues. Antimicrobial activities of the newly synthesized compounds were also investigated.

Keywords: Mannich base, thermal analysis, electrochemical behaviour, biological studies.

ABSTRACT

The aim of the present study is to compare the pharmacokinetics of nicardipine liquisolid tablets with its conventional tablets. 8 rats were taken, all the rats were having body weight approximately 200-260gr. Randomized Balanced Incomplete Block Design (BIBD) method was selected to determine pharmacokinetics of nicardipine liquisolid compact tablets. Blood samples were taken at predefined sampling points 0–24h after medication, and the plasma concentrations of nicardipine liquid solid compact tablets, conventional tablets were determined by high-performance liquid chromatography. The liquisolid compact tablets increased in C_max and AUC were observed, t_max occurred at 1.844 and 2.219 h with liquid solid compact tablets and conventional tablets. The area under the plasma concentration-time curve extrapolated to infinity AUC (0−∞) of liquisolid compact tablets was shown more than its conventional tablets. This research showed that formulation of nicardipine liquisolid compact tablets shown increase of bioavailability.

Keywords: nicardipine, pharmaco kinetics, rats, liquisolid compact tablets, study design, bio availability.

ABSTRACT

The rapid spread of multidrug-resistance against conventional antibiotics is a global threat that necessitates the search for alternative therapies from natural sources. In this investigation, the antibacterial potentials of ethanol extracts of moth beam (Vigna aconitifolia)  extracts were evaluated against Bacillus subtilis, Staphylococcus aureus, Staphylococcus werneri, Pseudomonas aeruginosa and Escherichia coli, Proteus mirabilis, Kleibsella pneumonia, Pseudomonas putida, using Agar cup-plate method. The extract showed  antimicrobial  activities  against  all  the  tested  gram positive and  gram negative  bacteria. Ethanol extracts in general exhibited greater antibacterial activity and results were comparable to the standard. Our finding identifies the potential use of moth bean as a natural source of antibacterial agent. Further studies are warranted to elucidate the mechanism of action of the extracts and to identify the active components responsible for the antibacterial activity.

Keywords: Vigna aconitifolia, Antimicrobial activity, Agar cup plate method.

ABSTRACT

The aim of the present study was an attempt to formulate and evaluate Levofloxacin loaded chitosan nanoparticles (CS-NP) by Emulsion solvent diffusion method using poloxamer 188 as surfactant; about eight different formulations (F1-F8) were prepared by changing the ratios of drug and excipients . Among all the formulations F3 was selected as optimized formulations  based on the physico chemical parameters and drug release studies and  it was incorporated in to 1% W/W of Carbopol gel (GF3) to obtained ophthalmic gel ,further, it was evaluated for antimicrobial activity against S. aureus and Bacillus subtilis. Compatibility studies by FT-IR showed no significant interactions between drug and excipients. The prepared Chitosan nanoparticle were characterized for different parameters like particle size analysis, zeta measurement, SEM, % drug content, entrapment efficiency, FT-IR, DSC, In-vitro release. The Gel containing chitosan nanoparticles (GF3)  were evaluated for different parameters like physical examination, pH, spread ability, viscosity, reological property, % drug content and  In-vitro release. The in vitro dug release and antimicrobial efficacy of GF3 formulation was compared with marketed product. From the results it was observed that the formulation controlled the drug release over a period of 24 hrs following Higuchi model and nonfickian diffusion mechanism with better antimicrobial action than the marketed product. The ocular irritancy study confirmed that ther is no irritation to the eye. From the above study we can conclude that the Levofloxacin loaded CS-NP were successfully prepared by emulsion solvent diffusion method and it is found to be  suitable for sustained ocular drug delivery having improved antibacterial action.

Keywords: Levofloxacin, Chitosan nanoparticles (CS-NP), DSC, FT-IR and Antimicrobial studies. 

ABSTRACT

Establishment of pharmacognostic profile of the flowers of Tecoma stans will assist in standardization for quality, purity and sample identification. Evaluation of the fresh, powdered and anatomical sections of Tecoma stans flowers were carried out to determine macromorphological, micromorphological, physiochemical and phytochemical profiles. Pharmacognostical studies involve the anatomical sections and powder analysis of flower, physiochemical studies such as loss on drying, extractive values, ash values etc. were done. In phytochemical studies the flowers are extracted with different solvents and qualitative chemical tests for each extracts were performed only alkaloids are isolated and characterized in the other parts of this plant. From phytochemical screening of flower parts we can find out various other secondary metabolites and also characterization.

Keywords: Tecoma Stans, Pharmacognostical, physiochemical and phytochemical studies.

ABSTRACT

A simple, precise and accurate RP-HPLC method was developed for the separation and quantification of  Ilaprazole and Levosulpiride in pharmaceutical dosage form. The quantification was carried out using Hypersil BDS C₈ column ( 150x 4.6mm,5µm) and mobile phase comprised of methanol and phosphate buffer(pH 7.5 adjusted with 0.01 M NaOH) in proportion of ratio 70:30 degassed under ultra- sonication. The flow rate was adjusted to 1 ml/min and the effluent was monitored at 242nm using PDA detector. The method was validated in terms of linearity, precision, accuracy and specificity, limit of detection and limit of quantization. Linearity of Ilaprazole and Levosulpiride were in range of 10-60 µg/ml and 75-450 µg/ml respectively. The retention time of Ilaprazole and Levosulpiride were 6.52 and 2.02 respectively. The percentage recoveries of both drugs were found to be 100.03%  and 100.18% for Ilaprazole and Levosulpiride respectively from the capsule formulation. The method was found to be precise, accurate and specific during the study. The proposed method enables rapid quantification and simultaneous analysis of both drugs from commercial formulations without any excipients interference. The method can be used for routine analysis of marketed product of Ilaprazole and Levosulpiride in combined capsule formulation.

Keywords: Ilaprazole, Levosulpiride, reverse-phase HPLC

ABSTRACT

A simple and precise reversed-phase high performance liquid chromatography (HPLC) method for the determination of meloxicam in human plasma was developed and validated. Using piroxicam as an internal standard (IS), separation was achieved on Symmetry shield RP-18 column. 0.5 ml plasma samples were prepared by protein precipitation using trifluoroacetic acid and acetonitrile. The mobile phase consisted of 0.025 M dibasic potassium phosphate (pH=6.0, adjusted with phosphoric acid), methanol, and acetonitrile (73:5:22, v:v:v) and was delivered at a flow rate of 1.5 ml/min. Eluents were measured using photodiode array detector set at 355 nm. Under these conditions, no interference in blank plasma or of commonly used drugs was observed. The relationship between the concentration of meloxicam in plasma and peak height ratio of meloxicam to the IS was linear over the range of 0.05-2.0 μg/ml. Intra-day and inter-day coefficient of variations (CV) and biases were ≤ 6.0% and ≤ 8.6%, and ±5.9% and ±5.3%, respectively. Extraction recovery of meloxicam and the IS from plasma was ≥80% and 98%, respectively. The method was applied to assess the stability of meloxicam under various clinical laboratory conditions. In processed samples, meloxicam was stable for at least 24 hours at room temperature (≥ 82%) and 48 hours at -20C (≥ 95%). In unprocessed sample it was stable for at least 24 hours at RT (≥ 82%), 16 weeks at -20ºC (≥ 87%), and after three freeze-thaw cycles (≥ 90%). The method is suitable for clinical and bioavailability investigation involving meloxicam concentration in the therapeutic range.

Keywords: Meloxicam, Piroxicam, Human plasma, HPLC

ABSTRACT

Carica papaya, a member of the family Caricaceae, is commonly known for its food and nutritional value throughout the world. During last few decades considerable progress has been achieved regarding the biological activity and medicinal application of papaya and now it is considered as valuable neutraceutical fruit plant. The present study was designed to determine the antimutagenic and anticytotoxic activities of different fractions (Aqueous, Chloroform, Ethanol and Ethyl acetate extracts) of Carica papaya leaves. Antimutagenic activity was determined by the Allium cepa root chromosomal assay using Cyclophosphamide monohydrate as the mutagenic agent and anticytotoxic activity of the extracts was evaluated by determination of mitotic index. All the four fractions displayed significant antimutagenic and anticytotoxic activities against cyclophosphamide-induced chromosomal aberrations and alltogether, the results of our study lend pharmacological credence to the anti-cancerous and ethnomedical use of this plant in traditional system of medicine and these results could be used to develop antimutagenic compounds for cancer therapy.

Keywords: Carica papaya, antimutagenicity, anticytotoxicity, ethyl acetate, aqueous, ethanol, chloroform fractions.

ABSTRACT

Solubility is an important physicochemical factor affecting absorption of drug and its therapeutic effectiveness. Drugs having poor aqueous solubility present one of the major confronts better absorption for good bioavailability of such drugs. The purpose of this study was to prepare and characterize solid dispersions of the poorly water soluble antihypertensive agent valsartan with water soluble carriers such as Kolliphor P 407, Kolliphor P 188, Kolliwax GMS II, Kolliphor HS15, HPMC AS and Soluplus in proportions viz. 1:1, 1:3, 1:5 (Drug: Carrier) with addition of 2% SLS to improve its aqueous solubility and rate of dissolution by solvent evaporation technique. All the formulations showed marked improvement in the solubility behavior and improved drug release. From all the formulations  SD6 was found to be optimized formulation  using soluplus as carrier based on the solubility and dissolution studies. The results obtained showed that the aqueous solubility and rate of dissolution was significantly improved when formulated in solid dispersion as compare to pure drug.

Keywords: Valsartan, solid dispersions, soluplus, aqueous solubility

ABSTRACT

The antiulcer effect of cow urine extract of Piper betel (family Piperaceae) was evaluated in pyloric ligation induced ulceration model in Wistar rats. The antiulcer activity was evaluated by measuring ulcer index and percentage of ulcer healing. The extract (500mg/kg b.w) showed significant antiulcer activity as evidenced from the data obtained. Histopathological findings also confirm the antiulcer activity of Cow urine Piper betel extract.

Keywords: Piper betel, antiulcer activity, pylorus ligation.

ABSTRACT

Geometry optimization calculations for (5z,5ˉz)-2,2ˉ- methylene bis (3-(5-mercapto-1,3,4-Thiadazole-2-yal)-2-(methyl -2,3-dihydro-1,3-oxazepine-4,7-dione), B, is carried out to establish a direct correspondence between experimental and theoretical by using density functional theory (DFT) with B3LYP/6-31G. The theoretical IR and ¹H-NMR for the same molecule are performed at the same level of theory. These data suggest that the spectra of the thiadazole are consistent with the thiadazole architecture proposed by Abbas and co-workers. The investigation of HOMO and LUMO approved that this molecule is very suitable to be a semiconductor material because it's have a very low energy band gap equal to 0.13628 ev.

Keyword: Density Functional Theory Calculations, Thiadazole-derivative, computational chemistry, Theoretical IR, ¹H-NMR spectrum , B3LYP functional

ABSTRACT

The present study was designed to investigate the antioxidant and gastro-protective potential of Cow urine betel vine extract. Antioxidant and gastro-protective activity was evaluated by using ethanol induced ulcer model; the animals were fed with Cow urine betel vine extract at the dose of 250 and 500mg/kg b.w orally for a period of 14 days. The pretreated extract reduced the gastric ulcers in a dose dependent manner which was determined by measuring the ulcer index and with marked attenuation in the levels of oxidative stress enzymes like SOD, LPO and CAT. Also Cow urine betel vine  increased the gastric mucous content in the selected ulcer model.

Keywords: Antioxidant activity, antiulcer activity and ethanol induced ulcer, Cow urine betel vine extract. 

ABSTRACT

Nanoparticles  act  as  a  promising  system  for  targeted  delivery  of  drugs  and  as  an  effective  route  of  drug  administration.  In  this  study,  polysorbate  80  coated  nanoparticles  of  serratiopeptidase  were  formulated  and  aimed for  the  treatment  of  blood  clots  in  brain.  Serratiopeptidase exerts effective activity against blood clotting and has ability to dissolve non-living tissues,   blood clots, cysts, atherosclerotic clots. Different  nanoparticle  formulations  of  serratiopeptidase  were  prepared  with  different  concentrations  of  chitosan  and  tripolyphosphate  using  ionic  gelation  method.  The  nanoparticles were coated using polysorbate 80 and were characterized  and  evaluated  for  different  parameters  such  as  particle  size,  entrapment  efficiency,  zeta  potential and  transmission  electron  microscopy.  The  in  vitro  drug  release  of  prepared  nanoparticles  was  studied  in  phosphate  buffer  (pH 7.4).  The  results  indicated  that  the  developed  nanoparticle  formulation  could  be  established  as  a  promising carrier  for  active  targeting  into  brain  to  dissolve  blood  clots.

Keywords:  Serratiopeptidase, chitosan, tripolyphosphate, nanoparticles, polysorbate 80, ionic gelation  method.

ABSTRACT

Most of the patients in current scenario are treated with more than one anti-hypertensives and most often with fixed dose combinations. Hence the use and efficacy of fixed dose combination are controversial and is the most debated issue in Indian perspective  The aim of this randomized pilot study was to evaluate the rationality and side effect profile of fixed dose anti-hypertensive combinations used in our hospital. A total of 25 hypertensive patients prescribed with anti-hypertensive FDCs were randomly selected and their outpatient record were monitored and recorded for a period of 2 weeks. The data was then suitably analyzed. Out of the 13 FDCs, only one FDC (7.69%) have its APIs present in both EML of WHO and NLEM of India. There was no established evidence in terms of therapeutic efficacy and safety for the 3 combinations (23.07%).76.92% of FDCs were cost effective when compared with their individual components. 11 FDCs (84.61%) provide published literature on the reduction of either dose of individual drugs or their adverse effects. Only one FDC was found to be irrational in this study. Giddiness (33.33%) was the most frequently seen side effect among the prescribed FDCs. During this limited study period with only 13 anti-hypertensive FDCs, we were able to find an irrational FDC, which clearly show an urgent need to conduct further studies on evaluating the rationality of FDCs as a whole. As a clinical pharmacist, our immense role in evaluating the rationality of FDCs could enable the DCGI to withdraw irrational FDCs from the market.   

Keywords: Hypertension, Fixed dose combination, Rationality, Side effects, Clinical pharmacist.

ABSTRACT

Topical drug delivery systems have been utilized for centuries for the treatment of local skin disorders. One side the topical applications of the drug provides the potential advantages of delivering drug straightly to the site of action and delivering drug for extended period of time at the effected site that mainly acts at the related regions. On the other hand, topical delivery system elevates the contact time and mean resident time of drug. The aim of the work is to develop & characterize adapalene emulgel formulation. Adapalene emulgel formulations were prepared by dispersing Carbopol 934 in distilled water with constant stirring at a moderate speed, then the pH was adjusted to 6 - 6.5 using Triethanolamine. Evaluation of the adapalene emulgel was carried out for Physical appearance, Rheological study, pH values, Spreadability, Drug content determination, In vitro release study, Accelerated stability studies. It was noticed that all formulations were liquefied and diluted at the end of the experiments, indicating water diffusion through the membrane. The accelerated stability studies were performed according to ICH guidelines for three months & emulgels were found to be stable in differing temperature. The results demonstrate that the release of the drug is dependent on viscosity of the polymer used.

Keywords: Emulsion, Emulgel, Adapalene, Transdermal gel, water-in-oil system. 

ABSTRACT

Endophytic fungi are potential sources of bioactive secondary metabolites that can be exploited for therapeutic purposes. Our study was aimed to identify bioactive secondary metabolites from crude extracts of endophytic fungi of three popular medicinal plants (Alstonia boonei- Ahun, Enantia chlorantha- Awopa and Kigelia africana- Pandoro) that have ethnobotanical history in Nigeria. The endophytic fungi were isolated from the stem barks of the plants using standard procedures. They were later fermented in broth culture, and the extract from the cell free broth of each of the fungi was subjected to Gas-Chromatography Mass-Spectrophotometry (GCMS). The results showed that, twenty-one different compounds were characterised from Aspergillus niger, Macrophomina sp, Trichoderma sp. and Penicillium species. The bioactive compounds include; Griseofulvin, Cinnamic acids, Penicillin, Coumarin, Cubenol, Erythritol among others. The presence of these compounds may contribute to the therapeutic properties of the plants.

Keywords: Endophytic fungi, bioactive secondary metabolites, medicinal plant, GC/MS

ABSTRACT

The present study scrutinizes the antidiabetic and the antidiarrhoeal effects of ethanolic extracts of  Ficus racemosa L. stem barks (EEFB) in Wistar rats. Oral glucose tolerance test (OGTT) model and alloxan induced diabetic model (AIDM) were performed to assess antidiabetic activity of EEFB at doses of 750mg/kg, 500 mg/kg and 250 mg/kg, and 2g/ kg respectively. For antidiarrhoeal effects of EEFB, castor oil-induced diarrhoeal (COID) model and gastrointestinal motility test with barium sulphate milk (BSM) model were also assessed at doses of 750 mg/kg and 500 mg/kg, and 250mg/kg respectively. Administration of EEFB resulted low blood glucose levels in OGTT model at doses 750 mg/kg and 500 mg/kg significantly (P<0.01). However, dose at 250 mg/kg also showed positive result (P<0.05) of the mentioned same antidiabetic model. In AIDM, Wistar rats showed worthy result at 2g/kg dose (P<0.001). After administration of EEFB at doses 750 mg/kg and 500 mg/kg inhibited significantly positive in COID model at P<0.01and P<0.05 respectively. However, at the dose of 250 mg/kg illustrated positive but not significant result in BSM model.

Keywords: Ficus racemosa, bark extract, antidiabetic, antidiarrhoea and Wistar rats

ABSTRACT

The purpose of present research was to formulate and develop the patient friendly pantoprazole sodium fast dissolving tablets using sublimation method to achieve rapid dissolution. In this study, an attempt was made to fasten the drug release from the oral tablets by incorporating the superdisintegrants and camphor/ammonium bicarbonate as subliming agents. The prepared fast dissolving tablets were subjected to pre-compression analysis and evaluated for hardness, weight variation, friability, wetting time, water absorption ratio and disintegration time. From the results of in vitro drug release studies, the formulation F9 exhibited fast release profile of about 95.21% in 14 min and disintegration time 90 sec when compared with other formulations. For the optimized formulation F9, the initial dissolution rate was 38.82% / 2 min. Fourier transform infrared spectroscopy studies revealed that there was no possibility of interactions between drug and excipients. The present study demonstrated potential for rapid absorption, improved bioavailability, effective therapy and patient compliance.

Keywords: Fast dissolving tablet, pantoprazole sodium, subliming agent, superdisintegrant, proton pump inhibitor.

ABSTRACT

Efficient Helicobacter pylori elimination requires delivery of the antibiotic locally in the stomach. High dose of metronidazole (250 to 750 mg) is difficult to incorporate in floating tablets but can simply be given in liquid dosage form.  By keeping the above observation in mind, we made an attempt to build up a new raft forming oral in situ gelling system of metronidazole with improved residence time using sodium alginate as gelling polymer to eliminate H. pylori.  Methods: oral in situ gelling formulations were prepared using sodium alginate, xanthan gum, calcium carbonate, and sodium bicarbonate. Prepared formulations were evaluated for density, viscosity, floating lag time, floating duration, swelling index and in vitro drug release. Results. All formulations (F1–F12) showed floating within 180 s and had floating duration  of more than 24 h. every formulations showed excellent pourability. It was observed that concentration of sodium alginate and xanthan gum had major influence on floating lag time, cumulative percentage drug release and other evaluation parameters. The batch F11 was optimized since it have good pourability with extended release of 10 hrs. Conclusion: oral in situ gelling system of metronidazole  can be formulated by  use of sodium alginate as a gelling polymer and xanthan gum as release retardant to control  the drug release for more than  10 hrs.

Keywords: H. pylori , oral in situ, metronidazole,   xanthan gum  raft forming system. 

ABSTRACT

Psoriasis is a prolonged, immune-mediated inflammatory skin disease. It is characterized by sharply demarcated, red, scaly, coin-sized skin lesions most often on the elbows, hands, knees, scalp and feet. Around 10% of individuals with psoriasis develop arthritis, which may affect the hands, feet, wrists, ankles, neck and lower back. In some cases joints become deformed, causing significant disability. The worldwide prevalence of psoriasis is around 2%, but studies in developed countries have reported higher incidence rates of on average about 4.6%.  In India the prevalence of psoriasis fluctuates from 0.44 to 2.8%, it is two times more common in males compared to females, and most of the patients are in their third or fourth decade at the time of presentation. Nearly two thirds of people with psoriasis have a mild form of the disease, Therefore in most of the cases first line treatment approach is topical. Betamethsone dipropionate (BD) loaded in omega-3- fatty acid fish oil nanoemulsion for the healthier absorption of BD in deeper layer of the skin to stop further progression of inflammatory cycle. For the preparation of nanoemulsion different types of preformulation studies require to perform because every drug has its specific intrinsic chemical and physical property which has been consider before development of pharmaceutical formulation. This property provides the framework for drug's combination with pharmaceutical ingredients in the fabrication of dosage form.

Keywords: Preformulation, Betamethasone dipropionate, Nanoemulsion, Psoriasis, HLB surfactants, Salmon fish oil.

ABSTRACT

Interactions of (2E)-1-(4-chlorophenyl)-3-(3,4 dimethoxyphenyl)prop-2-en-1-one with various substituted thioureas such as thiourea, N-phenylthiourea, 2-chlorophenylthiourea, 3-chlorophenylthiourea and 4-chlorophenylthiourea in presence of isopropanol as a medium. The products isolated in these reactions were characterized on the basis of conventional elemental analysis, chemical characteristics and spectral data. All the synthesized compounds screened against various microorganisms such as gram positive Staphylococcus aureus, gram-negative Escherichia coli. Ciprofloxacin was used as a standard drug for the antimicrobial screening.

Keywords: (2E)-1-(4-chlorophenyl)-3-(3,4 dimethoxyphenyl)prop-2-en-1-one, substituted thioureas, isopropanol, antibacterial, ciprofloxin etc.

ABSTRACT

Constipation is a common problem in all types of ages. Cassia angustifolia (Senna) extracts contain anthranoids that are commonly used for constipation and are well known for their laxative properties. Senna leaves or pods are highly rich with Sennosides content A, B, C & D. These Sennosides are hydroxyanthracene glycosides, which work miraculously as a laxative. In the present study, Senna extract from different vendors with variable strengths of sennosides A&B were procured and the relation between residue on ignition (ROI) with that of metals and sennosides A&B was studied.  The optimized concentration of senna extracts containing different sennosides A&B content were analyzed on HPTLC to determine the ratios of sennosides  A&B  from the total sennosides as well as its relation with residue on ignition (ROI).  Residue on ignition (ROI) was analysed gravimetrically while content of Calcium was calculated by Complexometric method. Iron content was carried out spectrophotometrically and Sennosides A&B content was carried out using HPTLC. The process control of extraction can be monitored on the basis of ROI. Specified Sennosides and ROI value together can be used in quality specification. Batch to batch variation with respect to efficacy can be avoided by determining the fixed quality norms for content of Sennosides, ratio of sennosides A&B, ROI value and content of Calcium.

Keywords: High Performance Thin Layer Chromatography (HPTLC), Senna extract, Residue on Ignition (ROI), Calcium, Iron, Sennosides A & B

ABSTRACT

Clobazam is an antiepileptic drug. There have been very less number of analytical methods developed for estimation of Clobazam in pure bulk form and in dosage form. In the present research a simple, accurate, precise and cost effective High performance liquid chromatographic method for the estimation of Clobazam, in bulk and pharmaceutical dosage form was carried out. HPLC method was developed on a Symmetry C-8 (4.6×150mm), 3.5µm particle, reversed-phase column. The mobile phase was acetonitrile: phosphate buffer (0.05M, pH- 4.5), 60:40 (v/v) at a flow rate of 0.8ml/min. The eluate was monitored at 231 nm. The method was validated reaching satisfactory results for selectivity, precision and accuracy. The retention time of the drug was found to be 3.38min in the mobile phase, acetonitrile: 0.05M potassium dihydrogen orthophosphate buffer (pH-4.5) 40: 60 (v/v). A linear response was observed in the range of 20-60µg/ml with a regression coefficient of 0.999. Validation parameters were carried out as per the guidelines of International Conference for Harmonization (ICH). This method can be used in the industries for determination of Clobazam to analyze the quality of formulation without interference of the excipients.

Keywords: Clobazam, Anti-epileptic, High performance liquid chromatography, ICH.

ABSTRACT

Tolterodine is indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency. Tolterodine tartrate having side effects mainly  dry mouth and other side effects like constipation ,headache ,stomach pain hence controlled release formulation  is prefer for tolterodine tartrate and this controlled release formulation is also reduced the frequency of dosing. In market control release capsules dosage form is available, we have planned, new controlled release tablet dosage form which is prepared by using multi unit particulate drug delivery system. Tolterodine Tartrate controlled release MUPS tablets were formulated by using insoluble inert starting seed or core which was prepared by using extrusion spheronization technique. use of water soluble material combined with tolterodine create greater amount of osmotic pressure causing the controlled release pellets burst and dump the drug. Hence water insoluble core pellets were used in this formulation the controlled release formulation comprised of a) water insoluble insert core b) Drug loading layer comprising of tolterodine c) Controlled release coating surrounding drug layer d) pellets mixed with conventional tablet excipients compressed into tablets. The aim of this study focused on the introduction of new alternative core for formulation of control release MUPS tablets and also studied the effect of protective plasticizer coating layer on extended release pellets prior to compression into MUPS tablets.

Keywords: Tolterodine tartrate, overactive bladder, Extrusion and speronization, FBP, Insoluble core, MUPS, Protective plasticized layer.

ABSTRACT

Chemical, fatty acid, amino acid composition and antioxidant activity of dehydrated Momordica tuberosa Roxb. (Adavi Kakara ) was investigated. The dehydrated M. tuberosa  possessed 21.76% protein and 33.96% fibre. The total lipid of seed was rich in oleic (22.05%), linoleic (25.09%) and linolenic (6.17%) acids. Major amino acids of the seeds are glutamic acid, arginine, leucine, aspartic acid and alanine. The ratio of essential to nonessential amino acids was 0.57 and in which, essential amino acids contributed to an extent of  36.36 g/100 g seed proteins. Inhibition of 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical at 50% was higher with pulp (6 mg) than whole fruit (14 mg) and seeds (20 mg). The ABTS radical inhibition assay was found to be high in whole fruit (98.4%) and followed by pulp (50.76%) and seed (16.14%) at 2 mg. Marginal differences in ferric ion reducing power were observed in all the samples at 10 mg level.

Keywords: Momordica  tuberosa, Chemical Composition, Fatty Acid, Amino Acid, Antioxidant Activity

ABSTRACT

The aim of the present study is to minimize the local gastrointestinal irritation which is one of the major side effects of Piroxicam (PR) by the formulation  oral  stomach specific in situ gelling emulsion ingestion by kinetic control of drug release. Material and method: In situ emulgel were prepared by using castor oil as oil phase ,tween 80 and span 80 as emulsifiers, sodium alginate was used as gelling agent,  xanthan gum was used as release retardant ,calcium carbonate was used as cross linking agent, pH triggered ionic gelation is the mechanism involved in the present study. Various evaluation tests were done for all formulations Results: Formulation F9 containing 2.5% of sodium alginate, 2 % of CaCO3, 1 % of sodium bicarbonate and 0.8% of Xanthan gum was selected as optimized batch based on  Q10 86.02±0.17 %, floating time 122.15±2.47 sec and drug content 91.86±1.02 %. The release pattern of drug was found to follow Korsemeyer and Highuchi model. The DSC study exposed that there was no incompatibility. Pharmacodynamic study on Wistar rats were showed significant anti inflammatory and anti arthritic activity of the optimized formulation. Further, in vivo toxicity studies carried out in wistar rats revealed no signs of gastric ulceration upon prolonged dosing. Conclusion: It was concluded that the oral stomach specific In situ gelling emulsion of piroxicam could be an effective dosage form which minimize the gastric irritation by coating drug with castor oil and remains buoyant and control the drug release for 24hrs.

Keywords: In situ gelling emulsion, Piroxicam, Castor oil, Gastric retention, In vitro release, Gastric irritations.

ABSTRACT

This study was performed to evaluate the antimicrobial activity of Hibiscus vitifolius. The ethyl acetate fraction of Hibiscus vitifolius were shown to possess an antimicrobial activity against bacteria and fungi, viz. Six bacterial strains were S. typhi, E. coli, E. faecalis, B. cereus, B.Substilis, Lacto bacillus and two fungal strains C.lunata, C.albicans  by using disc diffusion method. The anti bacterial activity of ethyl acetate fraction is almost comparable with standard solvent control Chloramphenicol. The anti fungal activity of ethyl acetate fraction extract is almost comparable with standard solvent control Fluconazole. Further studies are highly needed for future drug development.

Keywords: Hibiscus vitifolius, antimicrobial activity

ABSTRACT

1, 4-diazabicyclo [2.2.2] octane (DABCO) as an efficient organocatalyst were used for synthesis of annulated uracil derivatives via one-pot three component condensation reactions of substituted aromatic aldehydes, malononitrile and barbituric acid in aqueous ethanol carried at NTP. This is rapid, efficient synthetic route with several advantages viz; operational simplicity, mild reaction conditions, high yields of the biological active products, uses less toxic solvents and cheap catalyst. The synthesized products were screened for antimicrobial activity. Therefore annulated uracil derivatives   are excellent antimicrobial agents for globally alarming drug resistance issues in clinically used therapeutics.

Keywords:   Multi-component,   Pyrano [2, 3-d] pyrimidine, DABCO, Antimicrobial activity

ABSTRACT

A simple, sensitive, rapid and selective isocratic reversed phase High Performance Liquid Chromatographic (HPLC) method has been developed for  Zopiclone from bulk drug using a mobile phase consisting mixture of Acetonitrile : Buffer (pH 2.8) (80:20v/v)  Composition of buffer: (0.272gm in 200ml HPLC water  and pH adjusted to 2.8 using  ortho Phosphoric acid)  at the flow rate of 1.0 mL/min. A Cosmosil C₁₈ (250 cm x 4.6 mm, 5 μm) column was used as stationary phase. The retention time of Zopiclone found to be 2.19 min. The eluent were detected at 303 nm. Linearity was observed in the concentration range of 50-250 ppm for Zopiclone. Percent recoveries obtained for Zopiclone were 98.66%. The correlation coefficient for Zopiclone was found to be 0.998. After performing analysis by different analysts, it was found that the RP-HPLC method for the determination of Zopiclone was found to be Rugged. Percent RSD for robustness was well within the acceptable USP limits, ensuring that the proposed method was robust. The LOD were 0.22 µg/ml Zopiclone,. For Zopiclone, the LOQ were found to be 0.86 µg/ml. This demonstrated that the developed RP-HPLC method was simple, linear, precise, accurate, robust, and Rugged, could be conveniently adopted for the routine quality control analysis of Zopiclone.

Keywords: Zopiclone,  HPLC Method, Mobile phase.

ABSTRACT

A simple, precise, and rapid high performance liquid chromatography (HPLC) method for the determination of acetaminophen level in human plasma using caffeine as an internal standard (IS) was developed and validated. 0.5 ml plasma samples containing acetaminophen were mixed with 50 µg of the IS. After adding 30 µl of 50% perchloric acid, the mixture was vortexed for one minute and then centrifuged for 5 minutes at 13200 rpm. The clear supernatant was transferred into an auto-sampler vial and 100 µl was injected into the HPLC system with a run time of 7.0 min. The compounds of interest were efficiently separated on Symmetry C18 (4.6 x 150 mm, 5-µm) column, and were detected with a photodiode array detector set at 245 nm. The mobile phase consisted of water, methanol, and acetonitrile (80:10:10, v:v:v) and was delivered at a flow rate of 0.9 ml/min. No interference in blank plasma or by commonly used drugs was observed; and the detection limit of acetaminophen was 0.05 µg/ml. The relationship between acetaminophen concentration in plasma and peak area ratio of acetaminophen /IS was linear (r² ≥ 0.9991) in the range of 0.1– 40 µg/ml. Intra- and inter-day coefficient of variations (CV) and biases were ≤11.6%  and  ≤10.8%, and ≤≤14.0 and ≤12.8, respectively. Extraction recovery of acetaminophen and the IS from the plasma samples was ≥99% and 86%, respectively. Using the method, acetaminophen was found to be stable under conditions generally encountered in the clinical laboratory (≥99% and 91% in processed and unprocessed samples, respectively). Further, the method was successfully used to measure acetaminophen level in plasma samples from a healthy volunteer.

Keywords: Acetaminophen, Caffeine, Human plasma, HPLC

ABSTRACT

Red pigment of Bacillus prodigiosus, now known as Serratia marcescens, were first time investigated and named in 1902. The major component was first isolated in pure form in 1929 and in next 5 years investigators elucidated the main structural features of Prodigiosin and culminated in the assignment of structure. In the present study, potent pigment producing bacteria were used which were previously isolated from soil samples collected from different regions of Baramati, Maharashtra, India. The large scale production of Prodigiosin was achieved by using optimized parameters (time of incubation, temperature of incubation, pH of the medium, speed of Agitation, carbon and nitrogen source used etc.). The effect of red pigment on normal cells was assessed by toxicity studies using trypan blue assay. It shows that pigment having very less or no toxic effect on normal cells at various concentrations (5, 10, 15, 20, 25, 30, 35, 40, 45, 50 µg/ml). The effect of various concentrations (7.8, 15.6, 31.25, 62.5, 125, 250 µg/ml) of pigment on human cancerous cells (Lymphocytes) was also determined by using flow cytometry. Apoptosis was quantified by a reduction in cell forward scatter and increase in cell side scatter in flow cytometric analysis. Study revealed that the produced red pigment may be used for production of effective anticancer drug in future.

Keywords: Prodigiosin, Serratia marcescens,ccytotoxic activity, Anticancer activity, FACS.

ABSTRACT

A novel, simple and rapid reversed-phase liquid chromatography mass spectrometric method (LC-MS) was developed and subsequently used for the characterization of Drotaverine hydrochloride (DRH) and its impurities. The separation was achieved in 22 minutes on Merck Purosphere STAR RP-18e (250 x 4.6) mm, 5 µm column in gradient mode with flow rate 1.5 mL/min. 0.05 M ammonium acetate buffer pH 3.0 and a mixture of acetonitrile and methanol 85:15 v/v  was used as mobile phase A and mobile phase B, respectively. Detection was carried out at the optimum wavelength of 280 nm using a photodiode array/triple quadrupole mass detectors. The retention time of Drotaverine was found about 7 minutes. Specificity of the method was established by blank solution and the extreme degraded sample was used for the detection of impurity masses. The impurities detected under mass detector were further ionized for their daughter ions.

Keywords: Drotaverine Hydrochloride (DRH), Impurities, LC-MS, Daughter Ions, Characterization,

ABSTRACT

In the present work Tadalafil fast disintegrating tablets were prepared with poloxamer as carrier to enhance the solubility of Tadalafil and in order to disperse at faster rate in the mouth. Chemically Tadalafil is (6R,12aR)-6-(1,3-Benzodioxol-yl) 2,3,6,7,12,12a hexahydro-2-methylpyrazino[10,20:1,6] pyrido [3,4-b]indole-1,4-dione used in erectile dysfunction. In this current work Tadalafil fast disintegrating tablets were formulated from F1-F12 by direct compression method by taking 1:1, 1:2 and 1:3 ratio of poloxamer as a water soluble polymer and super disintegrating agents such as crospovidine, croscarmellose sodium, sodium starch glycolate and kryon. There after FT-IR studies were performed and it was observed that there were no incompatible reactions found between the Tadalafil and excipients used in formulations. Then all the formulations of Tadalafil fast disintegrating tablets F1-F12 were evaluated for pre and post compressional parameters including in-vitro dissolution studies. In which formulation F-12, containing (1:3) ratio of drug-poloxamer and kryon as super disintegrating agent was shown significant changes in wetting time (13±2.09sec), dispersion time (36±3.605sec) and fastest percentage drug release of 99.27±2.78 within 30 minutes was observed.

Keywords: Tadalafil, Poloxamer 407, Crospovidone, Croscarmellose sodium, Sodium starch gycolate, Kryon T314

ABSTRACT

About 1,685,210 new cancer cases are expected to be diagnosed in 2016. Superoxide dismutase protect against oxygen free radicals by catalyzing the removal of superoxide radicals  hydrogen peroxide mediated LPO. B(a)P induces the oxidation of mitochondrial NADPH.  An increase in the NADP⁺/NADPH ratio, the low availability of substrate NADPH may be responsible for the decrease in the activity of GR. Reduced glutathione, vitamin C and α-tocopherol comprise the non-enzymatic antioxidant components which protects the cells against the deleterious effects of the free radicals. Phase I & II metabolizing enzymes plays an important role in the detoxification of electrophilic toxicants and their induction protects against carcinogenesis and mutagenesis.

Keywords : Benzo(a)Pyrene, Nobiletin, Detoxification, Antioxidants

ABSTRACT

Formamidines, Thiazoles, dithiazolidines, thiadiazines and other ring system derivatives have a long history of applications in pharmaceutical and agrochemical industries. Our interest in the chemistry of the formamidine  nucleus and its derivatives prompted us to explore the synthesis of 1-hepta-O-acetyl- β-D-lactopyranosyl-3-H/Aryl formamidines, N-hepta-O-acetyl- β-D-lactopyranosyl-N’-benzothiozolyl formamidines and N-hepta-O-acetyl-β-D–lactopyranosyl formimidic acid alkyl esters by reductive desulphurization of 1-hepta-O-acetyl- β-D–lactopyranosyl–H / aryl thiocarbamides, 1-hepta-O-acetyl-β-D-lactopyranosyl-3-[2-N-substituted benzothiazolyl] thiocarbamides and 1-hepta-O-acetyl-β-D–lactopyranosyl-O-alkyl thiocarbamates respectively using Raney Nickel. The identities of these newly synthesized derivatives have been established on the basis of chemical transformations and IR, ¹H NMR and Mass spectral studies. The title compounds have been assayed for their biological activity against gram-positive as well as gram negative microorganisms. These compounds show most promising activity towards these micro-organisms.

Keywords: Synthesis, Lactosylated formamidines and its derivatives, Antimicrobial activity.

ABSTRACT

Echinops echinatus Family: Asteraceae is used as medicinal plant used in urinary disorder, liver disorder, heart diseases, etc. The seeds are sweet and aphrodisiac (Aurveda). The methanolic extract of leaves was obtained by Soxhelt extractor followed by concentration in rotary evaporator. Separation of bioactive chemicals was carried out by column chromatography while analysis by GC-MS which shows presence of following chemicals compositions. Phenol, 2,4bis(1,1dimethylethyl), Pentanoic acid, 5hydroxy,2,4ditbutylphenyl esters, 7,9Ditertbutyl1oxaspiro(4,5)deca6,9diene2,8dione, Benzo[b]dihydropyran, Propanoic acid, 2methyl,(dodecahydro 6hydroxy9methyl3methylene2,9dioxoazuleno[4,5b] furan6yl) methyl ester, Hexadecanoic acid,2hydroxy1(hydroxymethyl) ethyl ester, Glycerol 1palmitate, Octadecanoic acid, 2,3dihydroxypropyl ester, Octadecanoic acid,2hydroxy1(hydroxymethyl)ethyl ester, DISTEARIN, 13Docosenamide,(Z), Bis(cis13docosenamido) methane, Stigmasterol, 28,33 Dinorgorgost5en24one,3hydroxy, 3Dodecene,

Keywords: Column chromatography, GC-MS Analysis

ABSTRACT

To investigate the phytoconstituents of ethanolic extract of Amorphophallus campanulatus decne tuber using GC-MS. GC-MS analysis of Amorphophallus campanulatus decne tuber was performed by using Agilent 6890 GC with 59739N MSD and GC -MS equipped with Elite–I fused with silica capillary column(Cpsil 8cb:30mm×25mm×0.25mm).The result of GC-MS analysis confirmed the presence of 10 compounds. The most prevailing compounds are heaxadecanoic acid, 9, 17-octadecadienal, Octadecanoic acid, heptacosane, 1-cholro, nosacosone, ergost-5-ene, stigmassterol, etc. the presence of phytoconstitutents reveals the presence of medicinal value.

Keywords:  Amorphophallus campanulatus decne tuber, GC-MS analysis.

ABSTRACT

Efflux inhibition is proven bacterial machinery responsible for removal of bacterial wastage including antibiotics. Recently, efflux inhibitors (EI) have been tested with encouraging results as an adjuvant therapy for treatment of various bacterial invasions especially methicilline-resistant Staphylococcus aureus (MRSA). Although, EI have emerged as innovative approach of treatment for several multi drug resistant bacterial infections including tuberculosis, toxicity profile limits their wider use. To address this issue, we have attempted synthesizing hybrid molecules those results by combining known EI and triazole. This synthesis was aimed to arrive at structure that possesses pharmacophore from known EI. Synthesized molecules were evaluated as growth inhibitors (GI) and Efflux inhibitor of S. aureus. Pharmacologically active compounds were then tested for their cytotoxicity to further narrow down search. Most active compounds 177, 178, 187 and 196 were then tested for their GEI action against MRSA. We arrived at compound 145 as most potent dual inhibitor.

Keywords: MRSA, triazole, resistance, PDST178, dual inhibition.