Pharmacophore an International Research Journal
The purpose of this research work was to develop a novel gastro retentive floating microsphere of Amlodi-pine Besylate. Amlodipine besylate has maximum solubility in acidic pH and thus most suitable to prolong release of drug in stomach so an attempt has been made to sustain the drug release by incorporation oh hy-drophilic swellable polymers such as HPMC and ethylcellulose and present it in the form of gastro retentive floating microspheres which after oral administration are designed to provide the desired controlled and complete release of drug for prolonged period of time in the treatment of hypertension. Floating micro-sphere of Amlodipine Besylate were formulate using various material HPMC, ethylcellulose, ethanol, di-chloromethane, SLS. The concentration of these agents was also optimized to get desired controlled release of drug. The floating microsphere were evaluated for physical characterization, size of microsphere, en-trapment efficiency, swelling index, buoyancy studies and in vitro release studies. The result indicated that the optimized intragastric floating microsphere (F8) composed of 1g Amlodipine Besylate, 4g ethylcellulose, 0.3g HPMC exhibited 97% release in 8 hrs, while the buoyancy lag time was 20 sec and the intragastric floating microsphere remain buoyant for 20 hrs. In vitro drug release kinetics evaluated using the linear regression methods was using found to follow the Zero order kinetics. Optimized intragastric floating microsphere showed no significant change in physical appearance, drug content, total buoyancy time or in vitro dissolution pattern after storage at 40oC/75% relative humidity for 1 month.
