氢氯噻嗪HPMC骨架片释药机制影响因素研究

Influencing Factors of Release Mechanism of Hydrochlorothiazide HPMC Matrix Tablets

关键词:  HPMC  释药机制

Key words:  HPMC  release mechanism

摘要:

目的 研究影响HPMC骨架释药机制的因素。方法 以氢氯噻嗪为模型药物，HPMC为骨架材料，制备缓释片，测定释放度并描述其释放机制。考察各处方因素和释放条件对释放机制的影响。结果 HPMC用量越大、难溶性填充剂，释放机制越趋向于零级释放。较低的HPMC用量、水溶性填充剂，释放机制趋向于Higuchi和Peppas方程，释药行为以溶蚀和扩散相结合。结论 HPMC型号、片剂的硬度、制备方法、溶出度测定方法、转速对释放机制影响不大。HPMC用量、填充剂的性质、溶出介质的离子强度影响释放机制。

Abstract:

OBJECTIVE To study the influencing factors of release mechanism of HPMC matix. METHODS Hydrochlorothiazide was selected as a model drug and HPMC as matrix to prepare sustained release tablets, and its release mechanism was described by testing dissolution rate and investigated by the factors of formula and release conditions. RESULTS The release mechanism had the tendency to fit the zero order equation when more HPMC was used and insolubility additives were chosen. When using less HPMC and water-solubility additives, the release mechanism had the tendency to fit Higuchi equation and Ritger-Peppas equation, the release form was the synergistic action of the matrix degradation and drug diffusion. CONCLUSION The types of HPMC used in matrix, the tabletting force, the preparation methods, the assay method of dissolution and rotation speed showed no significant effects on the release mechanism. The content of HPMC, the solubility of additives and the ionic strength of dissolution medium were associated with the release mechanism of hydrochlorothiazide.