Optimization and pharmacodynamic evaluation of solid dispersion of gliclazide for dissolution rate enhancement

The present study utilizes approach of solid dispersions (SDs) to improve dissolution rate of Gliclazide (GLZ); a poorly water soluble anti-diabetic drug. Formulations were prepared by solvent evaporation and melt dispersion techniques using poloxamer as hydrophilic carriers. SDs and physical mixtures (PM) were characterized by thin layer chomatography, FTIR spectroscopy, X-Ray Diffractometry, and Differential Scanning Calorimetry. TLC was used to identify any possibility of degradation during preparation and optimize melting temperature for melt dispersion batches, which was supported by FTIR and DSC, showing absence of chemical interaction between the drug and carrier. XRD showed that GLZ was converted to amorphous form. Enhancement in dissolution was found more prominent with melt dispersions compared to solvent evaporation and physical mixtures. In vivo pharmacodynamic bioavailability study was performed for 28 days on alloxan induced diabetic wistar rats. Blood glucose levels were evidently lowered and controlled by SD compared to GLZ alone.Colegio de Farmacéuticos de la Provincia de Buenos Aire

SPECTROPHOTOMETRIC DETERMINATION OF DASATINIB IN PHARMACEUTICAL FORMULATIONS

Objective: A new, simple, sensitive, precise and reproducible bioanalytical method was developed for the determination of Dasatinib in pharmaceutical formulations with Chloranilic acid. Methods: The method is based on formation of violet colored complex. The UV spectrum of Dasatinib in methanol showed λ max at 521 nm. Beer’s law is valid in the concentration range of 10-60 μg/ml. This method was validated for linearity, accuracy, precision, ruggedness and robustness. Results: The method has demonstrated excellent linearity over the range of 10-60 μg/ml with regression equation y = 0.021x-0.083 and regression correlation coefficient r2= 0.997. Moreover, the method was found to be highly sensitive with LOD (2.96μg/ml) and LOQ (8.98μg/ml). Conclusion: Based on results the proposed method can be successfully applied for the assay of Dasatinib in various pharmaceutical dosageforms

VISIBLE SPECTROPHOTOMETRIC METHOD DEVELOPMENT AND VALIDATION OF IMATINIB IN BULK AND FORMULATION

Objective: A new, simple, sensitive, precise and reproducible UV visible spectrophotometric method was developed for the determination of Imatinib in pharmaceutical formulations with alizarin. Methods: The method is based on formation of yellow-colored complex. The UV spectrum of Imatinib in methanol showed λ max at 431 nm. Beer’s law is valid in the concentration range of 10-70 μg/ml. This method was validated for linearity, accuracy, precision, ruggedness and robustness. Results: The method has demonstrated excellent linearity over the range of 10-70 μg/ml with regression equation y =0.013x-0.017 and regression correlation coefficient r2= 0.997. Moreover, the method was found to be highly sensitive with LOD (4.3μg/ml) and LOQ (13.07μg/ml). Conclusion: Based on results the proposed method can be successfully applied for the assay of Imatinib in various pharmaceutical dosage forms

FORMULATION AND EVALUATION OF MICROEMULSION CONTAINING NEEM SEED OIL

Objective: The objective of the present study was to formulate Microemulsion containing seed oil. Neem seed (Azadirachtaindica) oil was extracted from its seeds by the soxhlet apparatus. Acetone is used as a solvent. PEG 400 and Carbopol 940p was select as surfactant, co-surfactant and hydrogel thickening agent. Microemulsions were characterized for pH, viscosity, spreadability, in vitro drug transport study and in vivo antibacterial activity and shows satisfactory results. Antibacterial activity of formulation against E. coli Shows at a concentration of 3%. The neem seed oil microemulsion has the potential for antibacterial activity. Methods: A ratio of surfactant and cosurfactant i.e, S/CoSchoosen and corresponding mixture was made. The mixture was mixed with oil. Each mixture was mixed thoroughly using magnetic stirrer until homogenous dispersion/solution was obtained. Double distilled water was used in this formulations as to prevent the incorporation of surface active impurities. The mixture was titrated with water and ambient temperature with constant stirring at the endpoint where the mixture become clouded, the quantity of aquous phase added. The percentage of three different pseudo-phases incorporated were calculated.  Results: Solubility studies in various solvents reveals that the oil is insoluble in distilled water and ethanol. Soluble in methanol. Conclusion: It was observed that the microemulsion having multilamellar nature. Batches with carbopol shows better homogenous distribution. The stability of microemulsion prepared with carbopol 71 was gretter than with xanthan gum. The in vitro study of microemulsion was performed and Batch (F7) is optimized batch which shows highest drug release

FORMULATION AND EVALUATION OF LIPOSOMAL GEL CONTAINING EXTRACT OF PIPRINE

Objective: The objective of present research work is to develop Liposomes as a carrier system for 70% Hydroalcoholic extract, its incorporation in to gel formulations and to characterize the prepared and develop Liposomal gel formulation. There are many reports revealing the pharmacological potential of Piper Nigrum. Methods: Cholestrol in various weight ratios were dissolved in 10 ml of Methanol: Chloroform (1:1) ratio used as a solvent. The extract solution was taken in a 500 ml round bottom flask. The flask was rotated in rotary flash evaporator at 40 rpm for 20 min in the thermostatically controlled water bath at 40 °C under vacuum 240 mmHg. The solvent was slowly removed by this process, and a very thin film of dry lipids was formed on the flask. The dry lipid film was slowly hydrated with 10 ml of Saline Phosphate Buffer pH 7.4 containing Insulin Drug. The flask was once again rotated at the same speed as before and at room temperature for 2 hr. The liposomal was left to overnight at 4°C, full lipid hydration. Results: This study was done for herbal formulations used for topical delivery of therapeutic agents at the time of injury to accelerate skin repair in the shortest time possible, with minimal pain. Plant Piper Nigrum. Family Piperaceac is extensively used. Conclusion: The present study revealed liposomal gel as an efficient carrier for herbal extract. Keywords: Piperine, Gel, Herbal extract, Liposomes, Liposomal gel

TREATMENT OF MOUTH ULCER BY CURCUMIN LOADED THERMOREVERSIBLE MUCOADHESIVE GEL: A TECHNICAL NOTE

Objective: Mouth ulcer is one of the commonest disorders caused due to a variety of etiological factors. Although many formulations like solution, suspension and ointments are commercially available, no therapy can be said completely useful for the treatment of mouth ulcers. The efficacy of the therapy can be improved by the approach of bio adhesion. The phenomenon of sol to gel conversion can be useful due to its ease of administration compared to gel formulations. Curcumin is known to have wound healing, anti-carcinogenic and anti-bacterial activities can be effective in treatment of mouth ulcers.Methods: Hence, the present study was aimed to formulate Thermo reversible Mucoadhesive Gel (TMG) containing Curcumin for treatment of mouth ulcer. Formulations were prepared by using Pluronic F68 and Pluronic F127 as thermo reversible agent along with carbomers and Xanthan gum as bioadhesive polymers. The formulations were characterized for gelation temperature, pH, gel strength, spreadability, in vitro muco adhesion and in vitro drug release.Results: Increase in the concentration of mucoadhesive agent enhanced the mucoadhesive force significantly. All batches were found to be satisfactory results for gelation temperature, Gel strength, Muco adhesion studies, Spreadability, gelling capacity, In-vitro drug release etc. The formulations delivered drug for about 4 h.Conclusion: The obtained results show that the residence time as well as the contact area of curcumin at the ulcer can be enhanced along with a sustained release. It can be concluded that TMG of Curcumin can be ideal candidate for mouth ulcer.Â

FORMULATION AND EVALUATION OF CRACK CREAM FROM PLANT EXTRACTS

Objective: The main aim of our research was to develop an anti-cracked heels cream formulation consisting of Hedychium Spicatum, Aloe barbadensis, Azadirachta indica for the treatment of cracked heels. Methods: An anti-cracked heels cream formulation consisting of Hedychium Spicatum, Aloe barbadensis, Azadirachta indica extracts was prepared. Microbiological studies were performed the safety of materials used in the formulation. Results: The developed cream consisting of Hedychium Spicatum, Aloe barbadensis, Azadirachta indica was found to be safe and effective for the treatment of cracked heels. Conclusion: It can be concluded that herbal creams without side effects having anti-inflammatory property can be used as the provision of a barrier to protect the skin

A REVIEW ON ADVANCES IN PHARMACEUTICAL CO-CRYSTAL PREPARATION ROUTES, INTELLECTUAL PROPERTY PERSPECTIVE AND REGULATORY ASPECTS

As in recent years, due to the pervasiveness of poorly soluble APIs that demonstrates poor and erratic bioavailability, pharmaceutical cocrystal’s applicability to tailor the physicochemical properties has gained attention. Pharmaceutical cocrystal has been an exciting field of interest to researchers as this encouraged several regulatory bodies to create regulatory standards, which led to the approval of these crystals for marketing in various nations. With the upsurge in the growth of pharmaceutical cocrystals, the major concern is over the intellectual property perspective and regulatory status of cocrystals. With the new guidelines from the United States Food and Drug Administration (USFDA) and European Medicines Agency (EMA), the manufacturing and characterization of cocrystal have become less complicated. In this article, various preparation routes are mentioned along with this intellectual property perspective and regulatory perspective, including regulatory guidelines, which give an idea of whether cocrystals meet the criteria for patent eligibility and how they would change the current state of the pharmaceutical industry. Here, we also reviewed some recently approved patients on pharmaceutical crystals, which provided benefits over poor physicochemical property of drug substances and also enhanced the therapeutic effectiveness of that drugs

Preparation and in vitro and in vivo evaluation of glipizide mucoadhesive microspheres using factorial design

The purpose of the research was to prepare controlled release glipizide mucoadhesive microspheres with a coat consisting of sodium alginate and a mucoadhesive polymer Carbopol 971P. Orificeionic gelation method by using 32 factorial design were investigated with a view to develop mucoadhesive microspheres of controlled release. The resulting microspheres were discrete, free flowing, spherical and multinucleate monolithic type. Microencapsulation efficiency was in the range of 56-88%. Microspheres exhibit good mucoadhesive property in the falling film test. Glipizide release from the mucoadhesive microspheres was slow and extended over long period of time. Drug release was non-Fickian type. The concentration of carbopol 971P and sodium alginate had a more significant effect on different variables. In-vivo testing demonstrated a significant hypoglycemic effect of glipizideColegio de Farmacéuticos de la Provincia de Buenos Aire