HPMC对单层及双层缓释骨架制剂体外释放的研究[1]资料.docVIP

HPMC对单层及双层缓释骨架制剂体外释放影响因素研究 杨亚鹏, 王梦圆，郭旻彤 通讯作者：郭旻彤，男，教授，硕士生导师，研究方向：缓控释制剂及产业化研究。E-mail： 通讯作者：郭旻彤，男，教授，硕士生导师，研究方向：缓控释制剂及产业化研究。E-mail：guo5566@zzu.edu.cn （郑州大学药学院，河南 郑州 450001） 摘要：目的 考察HPMC作为亲水凝胶骨架材料和调控层材料对骨架型缓释制剂片剂体外释放的影响。 方法 以盐酸地尔硫卓为水溶性模型药物，HPMC 为亲水凝胶骨架材料，分别制备盐酸地尔硫卓缓释片和具有调控层的双层骨架片，考察HPMC作为凝胶骨架材料和调控层材料对水溶性药物缓释制剂体外释放的影响。 结果 增加HPMC的黏度及用量可以减慢药物释放，但具有一定的限度；选用乳糖或微晶纤维素为稀释剂时也会影响药物的释放；在一定的范围内，硬度对水溶性药物的体外释放影响较小；联合应用CMC-Na为骨架材可以显著减慢药物释放，达到24小时持续释放；当以HPMC和EC 为调控层辅料制备双层骨架片时，增加调控层的重量质量及HPMC 的比例，能减慢药物释放，尤其减少了前期突释现象；但当增大到一定程度时，药物释放的速率变化较小。 结论 HPMC 的黏度、用量、与稀释剂的配伍及与骨架材料的联合应用等对药物的释放影响较大；在缓释片的基础上加上一层不含药物的调控层制备双层骨架片，可以有效控制缓释药物前期释放过快，改变药物释放规律。。 关键词：羟丙基甲基纤维素；缓释片；双层片 Effect of the release of hydroxypropylmethyl cellulose on sustained-release tablets and bilayer tablets Mintong Guo*，Yapeng Yang （School of Pharmacy，Zhengzhou University，Zhengzhou 450001） ABSTRACT: Objective TO study the influence of vitro release of HPMC as hydrophilic matrix materials on sustained-release tablets and bilayer tablets. Methods Diltiazem Hydrochloride as water-solube model drug, HPMC as basic matrix materials, to prepare the diltiazem sustained-release tablets and bilayer tablets, examine the behavior of the drug release . Resulets The diluents and the viscosity and amount of HPMC can influence the release of drug to some degree, the pressure had a few effects on drug release . The significant effect was observed when the application of HPMC together with CMC-Na, so as up to 24 hours continuous release; When HPMC as control layer material to prepare the bilayer tablet, increase the quality of control layer and the proportion of HPMC can decrease the drug release , especially in reducing the initial burst release. Conclusion The viscosity 、amount of HPMC ,the interaction with diluents, and the combination with other matrix material has a big impact on the drug release; Prepare the bilayer tablet with a control layer on the basis of the sustained-release tablet , can effectively control the drug release.