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目的考察多西他赛囊袋张力环加速释放度试验条件,并优化多西他赛囊袋张力环的处方工艺。方法通过考察释放介质中乙醇含量(0%、5%、10%)和不同温度(37和45℃)对多西他赛囊袋张力环释药速度的影响,建立制剂体外加速释放度试验条件。利用加速释放度试验方法考察多西他赛囊袋张力环的体外释放度,筛选最优处方。结果在介质为含5%乙醇pH 7.4磷酸盐缓冲溶液、温度为(45±0.5)℃的加速释放条件下,药物释放速度提高了4倍,加速释放度与长期释放度用二项式拟合最好(y=0.004 6x~2+0.437 4x+9.683 7,r~2=0.998 4);载药量为30%,载体为PLGA5050(60K-100K=1∶1,W/W)的处方释药平稳,可持续释药30 d,符合Peppas equation释药模型。结论多西他赛囊袋张力环的释药特性可用加速释放度试验快速考察,该制剂体外释药平稳缓慢,具有临床应用前景。
OBJECTIVE To investigate the experimental conditions for the accelerated release of tension ring of docetaxel pouch and to optimize the formulation of docetaxel pouch tension ring. Methods The effects of ethanol content (0%, 5%, 10%) and different temperature (37 and 45 ℃) on the release rate of docetaxel in the capsular bag were investigated to establish the in vitro accelerated release test conditions . Accelerated release test was used to investigate the in vitro release of docetaxel pouch tension ring and the optimal formulation was screened. Results The drug release rate increased 4-fold under the accelerated release condition of 5% ethanol pH7.4 phosphate buffer solution at the temperature of (45 ± 0.5) ℃. The accelerated release rate and long-term release degree were fitted by binomial (Y = 0.004 6x ~ 2 + 0.437 4x + 9.683 7, r ~ 2 = 0.998 4), and the prescription of PLGA5050 (60K-100K = 1: 1, W / W) The drug was stable and sustained for 30 days, which was consistent with Peppas equation release model. Conclusion The release characteristics of the tension ring of docetaxel pouch can be rapidly investigated with the accelerated release test. The in vitro release of the formulation is stable and slow, and has the clinical application prospect.