Accelerated Release Testing Method and Preparation of Docetaxel Capsule Tension Ring / 中国药学杂志

ABSTRACT

OBJECTIVE: To develop the accelerated release test method of docetaxel capsule tension ring and optimize its formulation. METHODS: The effects of ethanol concentration in the medium (0%, 5%, 10%) and temperature (37 and 45 ℃) on the release rate of docetaxel capsule tension ring were investigated, and the correlation regression equation between the accelerated release rate and the long-term release was established. Then, the best prescription was screened out with the accelerated release test method. RESULTS: The drug release rate of these preparations could be increased by four times under the accelerated conditions, i.e., using pH 7.4 phosphate buffer solution containing 5% ethanol as the release medium and operating at (45±0.5)℃. The accelerated release and long-term release were fitted the best using binomial model (y=0.004 6x2+0.437 4x+9.683 7, r2=0.998 4). The preparation using PLGA5050 (60K-100K=1:1, W/W) with drug-loading of 30% released drug stably and sustainedly for 30 d, and its release behavior was consistent with Peppas equation drug release model. CONCLUSION: Accelerated release testing can be employed as a rapid screening test to facilitate the formulation optimization of docetaxel capsule tension ring. This preparation has been proven to have sustained-release characteristics, suggesting a good clinical application prospect.