Formulation and Evaluation of Matrix Microspheres for Simultaneous Delivery of Candesartan Cilexetil and Captopril for Treatment of Nephritic Syndrome

The objective of the present study was to prepare and evaluate matrix microspheres system for simultaneous and sustained release of candesartan cilexetil and captopril for the management of nephritic syndrome, Ethyl cellulose was used as a retardant polymer and IR study showed better compatibility of it with both the drugs, the matrix microspheres were prepared by emulsion solvent evaporation method and the prepared microspheres were characterized for morphology, drug loading and micromeretical properties. The drug release was performed in pH-6.8. The prepared microspheres were spherical in shape and free flowing in nature, the drug loading capacity ranges from 62-86%, the matrix microspheres show extended release up to 6-8 h, thus, the matrix microspheres have a potential for the prolongation and simultaneous release of candesartan cilexetil and captopril for mitigation of nephritic syndrome. INTRODUCTION: In the present scenario, the diabetes becomes a very common disease and longstanding diabeties mellitus leads in nephritic syndrome which result in the chronic kidney failure or death. The combination of the ACE inhibitors and angiotensin receptor blockers (ARBs), used to treat nephritic syndrome because the combination of the both results in the complete suppression of the Renin Angiotensin System therefore candesartan cilexetil and captopril selected for the treatment of nephritic syndrome. The sustained effect of both the drugs achieved by matrix microspheres in which the ethyl cellulose used as a rate determining constituent 1, . Thus, the objective of the present study includes; a) Development of sustained release matrix microsphere system containing Candesartan cilexetil and captopril using ethyl cellulose as the retardant polymer which will sustain the release of drugs for a longer period of time to increase the patient compliance. b) To study the effect of drugs to polymer and solvent ratio on in vitro drug release. c) To fit the drug release data to various drug release models. MATERIAL AND METHOD: Captopril was procure from the Lupin Pharmaceutical Ltd., India and candesartan cilexetil was obtained as a gift sample fromVijayshree Chemicals Pvt. Ltd. Ethyl cellulose obtained as a Gift sample from Colorcon Asia Pvt. Ltd., Goa. All other chemicals and reagents used were of the analytical grade. Method of preparation: The microspheres were prepared by emulsion solvent evaporation method using the formulation as shown in table 1. In this method ethyl cellulose was dissolved in acetone and a given amount of the drugs were dispersed in it to make different drugs to polymer ratio of 1:1, 1:2, 1:3 and stirred it for about 15 minutes, then polymer-drugs dispersion poured in to 50 ml of liquid paraffin (light)