卡维地洛脉冲释放片的制备及体外释药特征

目的：制备卡维地洛脉冲释放片并考察其体外释药特征。方法：采用压制包衣法制备卡维地洛定时脉冲释放片，紫外分光光度法测定卡维地洛药物含量，以体外释放度为主要评价指标，考察崩解剂、包衣材料等对脉冲片释药性能的影响，并对处方进行优化。结果：处方中片芯含药量为10%，以63%的CMS-Na为崩解剂，27%的MCC为填充剂压制片芯；以35%的HPMC、62.5%的卡拉胶和1%的PEG 6000为衣膜材料，2.5%的滑石粉为润滑剂，粉末直接压片包衣。以pH4.0醋酸缓冲液为释放介质，包衣脉冲片时滞8 h后，累积释放度达80%以上。结论：卡维地洛压制包衣片能实现定时脉冲释药效果。

Preparation and release characteristics in vitro of carvedilol pulsed-release tablets

OBJECTIVE To prepare carvedilol pulsed-release tablets and investigate their release characteristics in vitro.METHODS Carvedilol pulsed-release tablets were prepared by compression-coated, the content of carvedilol was determined by UV-spectrophotometry, the influence of disintegrating agent and coating material on carvedilol release was investigated based on in vitro release and the formulation was optimized.RESULTS The formulation of tablet core consisted of 10% carvedilol, with 63% CMS-Na as disintegrating agent, 27% MCC as diluting agent. With 35% HPMC, 62.5% carrageenan and 1% PEG 6000 as coating materials, 2.5% talcum powder as lubricant, pulsed-release coated tablets were prepared by powder-pressed technique. With pH 4 acetic acid buffer as releasing medium, the cumulative release rate of drug from pulsed-release coated tablets was more than 80% after a delay of 8 h.CONCLUSION Carvedilol compression coated tablets can achieve the effect of time-controlled pulsatile drug delivery.