Ramchandra Vishnu Keny

Buccal mucosa is a potential site for the delivery of drugs to the systemic circulation in a sustained manner; avoiding the first-pass metabolism. The goal of present investigation was to design and evaluate mucoadhesive buccal films of Repaglinide in order to avoid first-pass effect and release the drug for extended period of time. The Buccal films were formulated using polymers, Carbopol-971P and HPMC K4M, by solvent casting method; using PEG 400 as plasticizer. In this study, an attempt has been made to prepare Repaglinide inclusion complex; to enhance its solubility and was incorporated into the mucoadhesive buccal films in order to improve the bioavailability. A comparative study has been done between; uncomplexed Repaglinide loaded buccal films and inclusion complex loaded buccal films. The films prepared were evaluated for various physicochemical parameters and in vitro drug release. It was observed that inclusion complex loaded buccoadhesive films showed higher cumulative percentage of drug release at the end of 8 hours. The release data obtained was analyzed using various mathematical models. The Repaglinide loaded films followed zero order kinetics with principle mechanism of drug release being fickian diffusion. Whereas the inclusion complex loaded films followed zero order kinetics and exhibited non-fickian diffusion mechanism. HCC1 formulation having acceptable physicochemical parameters and with highest cumulative percentage of drug release (95.18%) at the end of 8 hours was chosen as optimum formulation and its short term stability studies revealed adequate stability of the formulation.

The aim of the present study was to design a buoyant in-situ gel of Alfuzosin HCl for use in management of Benign Prostrate Hyperplasia (BPH). The attempt was made to provide sustain drug release as well as prolong gastric retention thus improving bioavailability of the drug along with the added advantage of liquid oral dosage forms. The devised phase transition systems are to be administered in liquid form and gels in-situ on coming in contact with gastric fluid. Such liquid formulations are devised taking into consideration the geriatric patients who mostly founds difficult to swallow the solid oral dosage forms. Different prototypes were formulated, using Gellan gum, Sodium alginate and combination of both in-situ gelling polymers. HPMC K100M was incorporated as release retarding agent also used as strength forming polymer. Calcium Carbonate imparts buoyancy and also acts as cross-linking agent. Sodium citrate is used for liquefying solution, which act as sequestering agent by forming a complex with calcium carbonate (Ca+2) and thus delays the gelation until the preparation reaches the  acidic environment of stomach. The evaluation was carried out for In Vitro parameters and the results substantiated that the optimized formulation (S4A) revealed excellent floating characteristics and gastric retention. The results of dissolution studies was fitted into five different mathematical models and subjected to regression analysis. The drug release from all formulations was found to follow Zero order kinetics and shows to best fit Peppa’s equations exhibiting fickian diffusion release mechanism.