Objective: The study was conducted with an objective to achieve a potential sustained release oral drug delivery system of an antihypertensive drug, perindopril which is a angiotensin converting enzyme inhibitor having half-life of 2 hrs. Perindopril is water-soluble drug, so we can control or delay the release rate of drug using release retarding polymers. This may also decrease the toxic side effects by preventing the high initial concentration in the blood.Methods: Microcapsules were prepared by solvent evaporation technique using Eudragit L100 and ethyl cellulose as a retarding agent to control the release rate and magnesium stearate as an inert dispersing carrier to decrease the interfacial tension between lipophilic and hydrophilic phase.Results: Prepared microcapsules were evaluated for the particle size, percentage yield, drug entrapment efficiency, flow property, and in vitro drug release for 12 hrs. Results indicated that the percentage yield, mean particle size, drug entrapment efficiency, and the micrometric properties of the microcapsules were influenced by various drug:polymer ratio. The release rate of microcapsules could be controlled as desired by adjusting the combination ratio of dispersing agents to retarding agents.
Conclusion:Perindopril microcapsules can be successfully designed to develop sustained drug delivery that reduces the dosing frequency and their by one can increase the patient compliance.
Amoebiasis is an infection of the large intestine caused by Entamoeba histolytica. Tinidazole is the preferred drug used in the treatment of intestinal amoebiasis. The conventional tablet dosage form provides minimal amount of drug in the colon with undesirable adverse effect due to variation in the transit time. Hence, to target the drug directly to the site of action in the colon, there is need to develop colon targeted drug delivery systems that will enhance the therapeutic drug level, increases the bioavailability of active medicament and reduce the dose of drug. The fast disintegrating core tablet of Tinidazole was prepared by direct compression method. The core tablet was evaluated for hardness, thickness, Friability, weight variation, drug content, in vitro disintegration time and in vitro drug release studies. Using the optimized formulation (C3), different formulations (F1-F6) of coated tablet was prepared by using different polymers like chitosan and xanthan gum. The formulated coated tablet were evaluated for various parameters like for hardness, thickness, Friability, weight variation, drug content, swelling study and in vitro dissolution study. The optimized formulation F3 shows 6.24% drug release in Stomach and Small Intestine and maximum drug release up to 96.53% in the colon. The kinetic data analysis of formulations indicated that it fits to Korsmeyer -Peppas Model and follows zero order release kinetics. The mechanism of drug release from the tablet followed non-Fickian (super case-11) transport. The stability studies of the optimized formulation were investigated as per ICH guidelines. There were no significant changes in thickness, hardness, weight variation, friability, drug content and in vitro drug release. These findings suggest that compression coated tablet using polysaccharide carriers provide more site specific delivery, reduced degradation and release of drug in stomach and small intestine.
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