Wang Jin-Feng, Wang Fang, Zhao Nan, Yang Cui-Yan, Wang Guo-Yu, Wei Ying, Zhang Wen-Ya
208th Hospital of People's Liberation Army, Changchun 130062, China.
Zhongguo Zhong Yao Za Zhi. 2017 Jan;42(2):298-302. doi: 10.19540/j.cnki.cjcmm.20161222.030.
To investigate the preparation technology and release mechanism of tectorigenin intragastric floating sustained-release tablets. The tablet was produced by wet granulation compression method, with hydroxypropyl methyl cellulose (HPMCK15M), cross-linked polyvinyl pyrrolidone (PVPP), octadecanol and sodium bicarbonate as excipient. The prescriptions were screened and optimized by orthogonal experimental design with in vitro floating capacity and drug release characteristics as the evaluation indexes. The optimization results were as follows: tectorigenin 33.3%, HPMCK15M 16.7%, PVPP 20.0%, octadecanol 13.3%, sodium bicarbonate 5%, and starch gel 10.7%. The prepared tablet can be floated within 10 s in the artificial gastric juice, lasting for 12 h in vitro, with a cumulative release rate of 70% in 10 h. The analysis of Rritger-Peppas equation showed that the sustained-release tablet had two advantages of both drug diffusion and skeleton dissolution. The tablet had good appearance and compressibility, as well as favorable floating capacity and drug release characteristics.
考察鸢尾苷元胃内漂浮型缓释片的制备工艺及释药机制。采用湿法制粒压片法制备片剂，以羟丙基甲基纤维素（HPMCK15M）、交联聚乙烯吡咯烷酮（PVPP）、十八醇和碳酸氢钠为辅料。以体外漂浮能力和药物释放特性为评价指标，通过正交试验设计筛选并优化处方。优化结果如下：鸢尾苷元33.3%、HPMCK15M 16.7%、PVPP 20.0%、十八醇13.3%、碳酸氢钠5%、淀粉浆10.7%。制备的片剂在人工胃液中10 s内可漂浮，体外持续12 h，10 h累积释放率为70%。Rritger-Peppas方程分析表明，该缓释片具有药物扩散和骨架溶蚀双重优势。该片剂外观良好，可压性好，具有良好的漂浮能力和药物释放特性。
