Analytical Method Development and Validation for Simulataneous Determination of Amoxicillin, Omeprazole and Rifabutin in Bulk and in a Synthetic Mixture by UV Spectroscopy

Today Helicobacter pylori (H. pylori) infection is one of the very common bacterial infections worldwide. Upper gastro intestinal tract is primarily affected with this bacterial infection. H. pylori are primarily responsible for dyspepsia, gastric and duodenal ulcers and gastric carcinogenesis and obliteration of the infection has become an important treatment goal in clinical practice. Analysis of multi component formulations by any single analytical method is a very challenging task. A new, simple, precise, accurate, reproducible, and efficient UV spectrophotometric method is developed and validated for the simultaneous estimation of ternary mixture of amoxicillin (AMX), omeprazole (OMP) and rifabutin (RFB) in bulk and in a synthetic mixture which is recently approved by FDA in 2019 to be used for treatment of H. pylori by Vierordt’s method or simultaneous equation method. The solutions of standard and sample were prepared in 0.1 N HCl. Th

ENHANCEMENT OF SOLUBILITY AND BIOAVAILABILITY OF BCS CLASS-II AMBRISENTAN: IN VITRO, IN VIVO AND EX VIVO ANALYSIS

Objective: The aim of this investigation was to enhance the solubility and bioavailability of the BCS class II poorly water-soluble drug ambrisentan by solid dispersion (SD) techniques using Gelucire 50/13 as a hydrophilic carrier. Methods: Solid dispersion of ambrisentan was prepared by kneading method using different dug: carrier ratios. Prepared SD was characterized for solubility, drug content, percentage yield, in vitro dissolution, ex vivo permeation and bioavailability. Solid-state characterization was performed by differential scanning calorimetry (DSC), X-ray diffraction (XRD) and scanning electron microscopy (SEM). Results: All the SDs formulations showed increase in drug solubility and dissolution when compared with its pure form. Aqueous solubility of the drug was found to be increased 8.23 fold in SD. DSC study showed that endothermic peak of the drug was disappeared in spectra of SD, confirming its amorphous conversion, XRD study revealed the reduction to almost absence of specific high-intensity peaks of drug which confirmed the reduction of crysatallinity of ambrisentan in SD. SEM of optimized SD formulation demonstrates the complete encapsulation and solubilization drug. In vitro dissolution study showed that optimized SD formulation (ASD4) gives the faster drug release of 101.5% in 60 min, as compare to its pure form and other SD formulations. Conclusion: Solid dispersion ASD4 prepared with 1:4 drug to carrier ratio showed the highest drug solubility and in vitro dissolution. The ex vivo and in vivo studies performed on optimized formulation ASD4 showed enhancement in drug permeability and bioavailability in Gelucire 50/13 based SD formulation

Formulation Development and Evaluation of Floating Microsphere of Acyclovir

The guanine derivative antiviral drug acyclovir (ACV) is one of the oldest molecules laying successful market until date, being commercially available in various dosage forms for oral, topical and parenteral administrations. Clinical application of this drug is superior to new antiviral agents due to its potential values such as suppression of recurrence, safety profile, minimal drug interactions and being inexpensive. ACV is slightly water soluble, less permeable and poorly bioavailable, yet more potential antiviral molecule. The present study involves preparation and evaluation of floating microspheres using ACV as a model drug for improving the drug bioavailability by prolongation of gastric retention time.  Ethyl cellulose, hydroxyl propyl methyl cellulose microspheres loaded with ACV were prepared by solvent diffusion evaporation method. The microspheres had smooth surfaces with free-flowing and good-packing properties. The yield of the microspheres (F1-F6) was range from 62.23±0.85 to73.32±0.65% and ethyl cellulose microspheres entrapped the maximum amount of the drug. Scanning electron microscopy confirmed their hollow structures with sizes in 198.3 nm. The prepared microspheres (F3) exhibited prolonged drug release and percentage buoyancy was found to 76.65±0.52. The formulated batches were evaluated for percentage yield, particle size measurement, flow properties, percent entrapment efficiency, swelling studies. The formulations were subjected to stability studies and In-vitro release and release kinetics data was subjected to different dissolution models. It was concluded that developed floating microspheres of ACV offers a suitable and practical approach for prolonged release of drug over an extended period of time and thus oral bioavailability, efficacy and patient compliance is improved. Keywords: Acyclovir, Solvent diffusion evaporation method, Ethyl cellulose, Hydroxyl propyl methyl cellulos

Formulation Development and Evaluation of Floating Microsphere of Acyclovir

The guanine derivative antiviral drug acyclovir (ACV) is one of the oldest molecules laying successful market until date, being commercially available in various dosage forms for oral, topical and parenteral administrations. Clinical application of this drug is superior to new antiviral agents due to its potential values such as suppression of recurrence, safety profile, minimal drug interactions and being inexpensive. ACV is slightly water soluble, less permeable and poorly bioavailable, yet more potential antiviral molecule. The present study involves preparation and evaluation of floating microspheres using ACV as a model drug for improving the drug bioavailability by prolongation of gastric retention time.  Ethyl cellulose, hydroxyl propyl methyl cellulose microspheres loaded with ACV were prepared by solvent diffusion evaporation method. The microspheres had smooth surfaces with free-flowing and good-packing properties. The yield of the microspheres (F1-F6) was range from 62.23±0.85 to73.32±0.65% and ethyl cellulose microspheres entrapped the maximum amount of the drug. Scanning electron microscopy confirmed their hollow structures with sizes in 198.3 nm. The prepared microspheres (F3) exhibited prolonged drug release and percentage buoyancy was found to 76.65±0.52. The formulated batches were evaluated for percentage yield, particle size measurement, flow properties, percent entrapment efficiency, swelling studies. The formulations were subjected to stability studies and In-vitro release and release kinetics data was subjected to different dissolution models. It was concluded that developed floating microspheres of ACV offers a suitable and practical approach for prolonged release of drug over an extended period of time and thus oral bioavailability, efficacy and patient compliance is improved. Keywords: Acyclovir, Solvent diffusion evaporation method, Ethyl cellulose, Hydroxyl propyl methyl cellulos

Pharmacoepidemiological study of potential drug interactions in heart and neurological outpatients

Background: Drug-drug interaction (DDI) is a potential cause of adverse drug reactions. This study estimates the rate and factors associated with potential DDI in cardiac and neurological prescriptions from the out-patient department of various hospitals.Methods: A cross-sectional study was conducted from February to April, 2014 in various outpatients department of different hospitals in Indore. Total 60 prescriptions of cardiac and 60 prescriptions of neuro patients were collected from different hospitals. All the prescriptions were analyzes by various pharmaceutical and medical books, drug interaction checker software, and journals, etc.Results: Prescriptions having moderate drug interactions are more than that of severe and minor interactions and severity of the interaction found moderate in both type of prescriptions. Among cardiac patients 75% are male and 25% are females including all age groups, and in neuro patients, 58.33% are male, and 41.66% are females including all age groups. Types of drug interaction found in prescriptions are as follow, severe interaction (13% in cardiac, 8% in neuro), and moderate interaction (45% in cardiac, 37% in neuro), minor interaction (17% in cardiac, 25% in neuro), interaction not found (25% in cardiac, 30% in neuro patients).Conclusion: The hazards of prescribing many drugs, including side-effects, DDI and difficulties of compliance have long been recognized as particular problems when prescribing. Proper emphasis should be given to drug information center and training of clinical pharmacy across the country, which can play an important role in minimizing DDIs

Antiestrogenic Activity of Boerhaavia Diffusa Root Extract in Female Albino Rats

Abstract Disturbance of the natural steroid hormone balance can successfully disorganize the co-ordinate events involved in ovulation, ovum transport and implantation. Thus, compounds possessing estrogenic, progestation and anti-estrogenic, anti-progestational or anti-implantation activity may also exhibit anti-fertility activity. The present study was conducted to investigate the antiimplantation and antiestrogenic activity of Boerhaavia diffusa root extract in female rats. Female albino rats were taken and divided into three groups. Group I served as control, group II received methanolic extract at dose of 200 mg/kg body weight and group III received methanolic extract at dose of 400 mg/kg body weight. The root extract of Boerhaavia diffusa evaluated for anti-implantation activity, The methanolic extract at a dose of 200 mg/kg body weight inhibited pregnancy with mean number of implants 5.58 ± 0.34 [P<0.001]. The same extract at a dose of 400mg/kg body weight significantly inhibited pregnancy with mean number of implants 4.47 ± 0.23 [P<0.001]. The oral administration of the Boerhaavia diffusa methanolic root extract (BDME) at dose of 200 mg/kg and 400 mg/kg body weight caused a significant increase in the uterine weight in immature rats when compared to control, [P<0.001]. These results indicate that the methanolic root extract of Boerhaavia diffusa contain bioactive compounds which may cause antiestrogenic activity. We can conclude that the methanolic extract of Boerhaavia diffusa root showed significant antifertility activity by means of potent antiestrogenic and anti-implantation, in a dose-dependent manner

Development of sustained release formulation of glipizide using natural polymer from Tamrindus indica for better patient compliance

The study was to design a drug product to reduce the frequency of dosing, increase therapeutic effectiveness and improvement in patient compliance, by developing sustained release matrix tablet of Glimepiride using tamrind gum as a release modifier. In current study tamrind gum is used as a polymer which is investigated for sustained release carrier. The pre-formulation studies of drug excipient mixtures were performed. The tablets formulated were evaluated by physicochemical studies, in- vitro drug release, kinetic studies and stability studies. Drug and polymers has no interaction as observed by FTIR and UV studies. All the physicochemical parameters of tablets were found in the limits. Glimepiride is used in the treatment type II diabetes mellitus and is a first third generation sulphonyl urea agent. The drug release pattern was studied for extended period of 12 hrs for the optimized formulations. The release of drug under kinetic studies showed that it follows first order models. The different tablet formulations were put to stability studies and it was observed that there were no significant changes in release pattern, physicochemical parameters and drug content. The present study result indicates the suitability of the tamrind gum polymer in the preparation of sustained release formulations of glimepiride. Keywords: Sustained Release, Glipizide , Natural Polymer, Tamrindus Indic

Anti-hyperglycemic & Anti-hyperlipidemic Activity of Leaves of Centella asiatica Linn. in Diabetic Rats

Aim- The main aim of the study is to evaluate the Antidiabetic and antihyperlipidemic activity of Centella asiatica in diabetic animals. Material & Methods- Different extracts were prepared by successive solvent extraction methods. Diabetes was induced by single injection of STZ in normal animals and diabetes was confirmed by glucose oxidation methods. The treatments of different extracts were given from third day to 21st day and at the end of 22nd day, blood sample was withdrawn and different lipid level was determined.  Result- Among all the extracts, dichloromethane extracts showed significantly activity in reducing blood glucose level and decreased the VLDL, LDL, TC, Triglycerides and significantly increased the HDL-C level. Conclusion- The results obtained in this study have shown that dichloromethane extract shown significant Antidiabetic and antihyperlipidemic activity. Further detailed studies are required to isolate the active phytoconstituents by bioactivity guided isolation techniques responsible for anti-diabetic and hypolipidemic activity. The present findings are significant for the development of alternative, inexpensive and safer therapy for the treatment of diabetes mellitus and hyperlipidemic. Keywords: Hyperlipidemia, STZ induced diabetes, Centella asiatica, VLDL-C, LDL-

Anti-arthritic Evaluation of Different Extracts of Boerhaavia diffusa Linn. in FCA Induced Arthritis In Rats

The main aim of study is to evaluate the anti-arthritic effect of different extracts of Boerhaavia diffusa in arthritic rats. Different extracts were prepared by successive solvent extraction methods by using the various polar and non polar solvents and their % yields were calculated. Arthritis was induced by FCA induced arthritis model in rats and paw volume was measured on different days. Body weights of all animals were also measured simultaneously and at the end of experiment some haematological parameters were measured. On preliminary phytochemical studies extracts showed the presence of alkaloids, fatty acids, terpenoids, flavonoids and phenolic compounds. Among all extracts, methanolic extract significantly decreased the paw volume in all treated groups. Methanolic extracts also restored the body weight significantly. The results of our study revealed that all the extracts treated group’s causes significant alterations in the hematological parameters and maximal effects were observed at 400 mg/kg. Since methanolic extract showed best activity in arthritic model and its phytochemical study showed presence of flavonoids and phenolic compounds, so it may be possible that anti-arthritic activity of root extracts may be due to presence flavonoids.  Keywords: Arthritis, FCA induced arthritis, Boerhaavia diffusa, haematological parameters, and Body weigh

In-vitro anti-inflammatory activity of different extracts of flowers of Tridex procumbens

AIM- The main of study is to evaluate the In-vitro anti-inflammatory activity of different extracts of flowers of Tridex procumbens. Material & Methods-Successive solvent extraction method was followed for extraction by using different solvents i.e. petroleum ether, chloroform, methanol, butanol and water. Preliminary phytochemical screening method was performed for the presence of different phytoconstituents. For the evaluation of anti-inflammatory activity, protein denaturation and proteinase inhibitory method were performed. Diclofenac sodium was used as standard. Result- Among all the extracts, methanolic extract of Tridex procumbens showed 80.23% inhibition. The petroleum ether, chloroform, n-butanolic and water extract had shown the 12.23, 23.33, 20.45 and 36.20% inhibition respectively at 500 µg/ml concentration. The Diclofenac sodium showed 83.28 % inhibition against denaturation of protein. The different extracts were evaluated by using this method. Methanolic extract of Tridex procumbens showed 74.50% inhibition at 500 µg/ml. The petroleum ether, chloroform, n-butanolic and water extracts had shown the 30.16%, 41.22%, 43.28% and 31.97% inhibition respectively at 500 µg/ml. The Diclofenac sodium showed 79.21% inhibition against proteinase inhibitory activity at 100 µg/ml. Conclusion- Besides from the obvious therapeutic importance, methanolic extract would be useful in understanding the mechanism of diseases with higher levels of cellular and molecular level. These components could serve as lead molecules for development of prospective anti-arthritic agents. Further detailed studies are required to isolate the active phytoconstituents from methanolic extract which is responsible for anti-arthritic activity. Keywords: Protein denaturation model, proteinase inhibitory method, methanolic extract, anti-inflammatory activity, Tridex procumben