甲硝唑HPMC骨架缓释片的制备和药物释放研究.pdfVIP

甲硝唑HPMC 骨架缓释片的制备与药物释放研究 周泽乾1 1 1 2 ∗ 王康 范江洋 张力明 何志敏 1 2 （天津大学化学工程研究所）（天津丹泰制药有限公司） 摘要：本文利用湿法造粒，制备了甲硝唑羟丙基甲基纤维素（HPMC ）骨架缓释片。实验结果表明，提高HPMC 含量与使用高粘度HPMC 可有效降低释药速率，但粘度4000mPa.s 以上HPMC 释药速率的降低不明显；含有 粒径较大的甲硝唑原药的片剂，由于药物较强的致孔作用，药物释放速率较高；由于表面积较小的键形片上， HPMC 水化凝胶层面积相对较小，甲硝唑从键形片的释放快于表面积较大的圆形片的释放。HPMC 粘度、药 物颗粒粒径与片形对释药速率的影响都与药物的溶解度有关。机制分析表明，药物曲线的释放符合 Higuchi 方程。 关键词：甲硝唑 羟丙基甲基纤维素 缓释 甲硝唑颗粒大小 片剂形状 骨架片 中图分类号：O636 Preparation of matrix tablet of metronidazole and evaluation of controlled-release Zhou Zeqian, Wang Kang, Fan Jiangyang, Zhang Liming and He Zhimin (Chemical Engineering Research Center, Tianjin University,Tianjin 30072, China) Abstract ： In this paper, the hydroxypropyl methylcellulose (HPMC) hydrophilic matrix tablets were prepared by wet granulation method. The experimental results indicated that the drug release rate was decreased using high amount of HPMC or high viscosity of HPMC. However, it was no obvious differences among the release rate for system containing HPMC above 4000 mPa.s. The drug release from tablets with larger particle size of metronidazole was high due to appearing the big release hole during the process of drug release. It was found that the drug release from oval tablets is faster than that from round tablets. The reason was the amount of HPMC in the surface of oval tablets was relatively low. The effect of the viscosity of HPMC, the particle size of drug and the figure of tablet on drug release was depended on the solubility of drug. It was demonstrated that the release rate of metronidazole represented a favorable compliance with Higuchi equation. Keywords: metronidazole, hydroxypropyl methylcellulose, sustained rel