卡波姆71G和羟丙基甲基纤维素在氢氯噻嗪骨架缓释片中的应用

目的:以氢氯噻嗪为模型药物,卡波姆71G和羟丙基甲基纤维素(HPMCSH4000)为骨架材料制备氢氯噻嗪缓释片,并对影响其释放的因素进行考察.方法:以HPMCSH4000和卡波姆71G为亲水性骨架材料,湿颗粒法压片制备氢氯噻嗪缓释片,采用中华人民共和国药典2000年版二部收载的溶出度测定方法II(桨法),测定药物的体外释放度,以一级方程的相关系数(r),t30,t50和t75为指标进行处方筛选,并考察影响氢氯噻嗪释放的因素.结果:最优处方的r,t30,t50和t75符合实验要求,制备的缓释片释放曲线符合一级释放方程,卡波姆71G和HPMCSH4000的用量、压片压力、释放介质的pH值、桨法转速对药物的体外释放均有一定影响.结论:以卡波姆71G和HPMCSH4000为骨架材料,可以制备出具有理想释药的氢氯噻嗪骨架缓释片.

Evaluation of carbopol 71G and HPMC as matrix materials in a sustained release formulation

Objective:To evaluate the factors affecting the sustained release in vitro of hydrochlorothiazide matrix tablets. Methods:Hydrochlorothiazide was mixed with the matrix materials hydrophilic polymers hydroxypropyl methylcellulose (HPMC_ SH4000 ) and carbopol 71G followed by the wet granule compression of the materials into the tablets. The dissolution of hydrochlorothiazide matrix tablets was measured using the paddle method described in the China Pharmacopoeia (2000) Dissolution Apparatus II. The formulation of hydrochlorothiazide matrix tablets was optimized based on the values of correlation coefficients r, t_ 30 , t _ 50 and t _ 75 derived by a first-order equation. The factors affecting the drug release behavior were assessed by measuring the drug cumulative released percent. Results:Hydrochlorothiazide was released from the optimal tablets by the first-order equation. The factors affecting the drug release behaviors from the matrix tablets included the quantity of HPMC and carbopol 71G,tablet hardness, pH environment of the dissolution media and pad rotating speed.Conclusion:HPMC and Carbopol 71G offered better advantages as matrix materials in the preparation of the sustained released matrix tablets.