论文部分内容阅读
目的:研制盐酸青藤碱胃滞留型择时释药片,考察处方和工艺因素对其体外释药的影响,解析其释放机制。方法:以盐酸青藤碱为模型药物采用压制包衣法制得胃滞留型择时释药片;以膨胀率和释药时滞为指标,筛选片芯用崩解剂;通过体外药物释放试验,考察影响择时释药片漂浮性能和释药时滞的包衣处方和工艺因素;通过溶蚀试验探讨其释药机制。结果:体外释放时,盐酸青藤碱胃滞留型择时释药片经一定时滞后药物均呈脉冲释放。片芯选用羧甲基淀粉钠作为崩解剂;随包衣处方中羟丙甲纤维素与卡拉胶的比例和凝胶材料用量增加,释药时滞延长;包衣压片压力和衣膜材料制备工艺对时滞无显著影响;释药机制为衣膜溶蚀和片芯溶胀协同作用。结论:盐酸青藤碱胃滞留型择时释药片经一定时滞后药物呈脉冲释放,调节其包衣处方可获得具有适当时滞的择时给药系统,满足时辰治疗要求。
OBJECTIVE: To develop a sustained-release tablet for gastric retention of sinomenine hydrochloride, study the effects of prescription and technical factors on its release in vitro, and analyze the release mechanism. METHODS: Gastroretentive tablets were prepared by sinomenine hydrochloride as a model drug. The swelling rate and drug release time lag were used as indices to select the disintegrating agent for tablet cores. The in vitro drug release test was conducted. The coating formulation and process factors affecting the buoyancy performance and time lag of release of the tablets at the time of release were investigated; the dissolution mechanism was explored through the dissolution test. RESULTS: When released in vitro, sinomenine hydrochloride gastro-retentive selective release tablets showed pulsed release after a certain time lag. The tablet core used sodium carboxymethyl starch as a disintegrant; with the increase in the proportion of hypromellose and carrageenan in the coating formulation and the amount of gel material used, the time lag of drug release was prolonged; the tablet compression pressure and film material The preparation process has no significant effect on the time lag; the drug release mechanism is the synergistic effect of film erosion and core swelling. Conclusion: The sinomenine hydrochloride gastroretentive selective release tablets are pulsed release after a certain time lag, and the adjustment of the coating prescription can obtain a timely delivery system with a time lag, satisfying the time treatment requirements.