PREPARATION AND RELEASE CHARACTERISTICS OF SR SUPPOSITORIES COMPOSED OF INDOMETHACIN MICROSPHERES

摘要

EC microspheres of indomethacin, an anti-inflammatory agent, were prepared using solvent evaporation technique. Influence of drug:polymer ratio and stirring rate on the formation of microspheres, drug loading capacity, and particle size were investigated. Microspheres were formed under all conditions employed. The highest drug loading capacity was achieved with the drug-polymer ratio of 1:1. Stirring rate didn't have any significant effect on drug loading capacity and in vitro drug release whereas increase in stirring rate led to decrease in particle size. Subsequently, sustained release (SR) suppositories were prepared with IND microspheres having the highest loading capacity. Melting method was employed using different bases PEG mixtures (400:1500:4000) and Witepsol H_(15)). Content uniformity for IND, weight variations, hardness, and melting time were determined. In vitro dissolution profile of SR suppositories were investigated. A delayed release time of 480 min was achieved. The in vitro release profile of the SR suppositories followed the (Bt)~a kinetics. Thus, SR-suppositories of IND microspheres can be used as an alternative way of rectal inpatient therapy with reduced dosage frequency and improved patient compliance.