中药有效部位hpmc骨架片释药模型及其机理的分析-release model and mechanism analysis of hpmc matrix tablets as effective parts of traditional chinese medicine.docxVIP

中文摘要 羟丙基甲基纤维素(HPMC)是目前使用最为广泛的缓释骨架材料之一，大量运 用于现代缓释制剂的研究中。HPMC骨架片的化药研究已经比较成熟，相比而言， 中药有效部位HPMC骨架片的研究比较落后，而对其释药行为，包括释药数学模型 及释药机理探讨的系统研究极少。因此，对 其在中药有效部位应用中的释药行为 研究，具有较为重要的现实意义。 本课题以黄芪中活性成分黄芪皂苷为水溶性模型药物，研究黄芪皂苷在亲水 性凝胶HPMC基质中的释药行为；以葛根中活性成分葛根总黄酮为水难溶性模型药 物，研究不同性质有效部位在亲水性凝胶HPMC基质中的释药行为测定药物释放量 及HPMC的溶蚀量与时间的关系，通过计算处方组分的等价重均分子量(Meq)，导 出定量化数学模型。进而探讨 研究HPMC骨架片的体外释药行为，考察HPMC骨架 片释药影响因素，建立中药有效部位HPMC骨架片释药的数学模型，探讨HPMC应用 于中药有效部位的释药机理，及预测药物释放。 结果显示黄芪总皂苷及葛根总黄酮释放均符合HPMC骨架溶蚀控释机理。用 HPMCK15M系列实验结果导出黄芪皂苷从HPMC骨架中释放的数学模型: M P ( t)/MP (8) = (100.1969Ln(t ) - 0.6281)M eq-(-0.0768Ln(t ) + 0.3839) 葛根总黄酮从HPMC骨架中释放的数学模型: M P ( t)/MP (8) = (100.4829Ln(t ) - 0.7001)M eq-(-0.0038t 2 + 0.0766t + 0.2399) 用以上数学模型预测HPMCK4M组分处方中HPMC溶蚀与葛根总黄酮释放，理论值与 实验实测值有较好的吻合度。结果表明该种数学模型适用于HPMC中以骨架溶蚀机 理为主的中药有效部位的释放行为的定量描述及预测。 关键词:羟丙基甲基纤维素（ HPMC）；缓释；骨架片；释放；模型；黄芪总皂苷； 葛根总黄酮 investigation on the release model and mechanism of Chinese medicine effective position in HPMC matrix tablets Abstract：Hydroxypropyl methycellulose（HPMC）is one of the most widely used sustained-release matrix material,applied to a large number of Sustained currently Preparations of modern research. the drug research of HPMC matrix tablets is relatively mature.Relatively speaking，the research of the chinese medicine effective position in HPMC matrix tablets is backward，and the release behaviors include the system research on mathematical release model and the releasing mechanism are very little in current.So, preliminary Study to the release behaviors is of great realistic significance. Taking Astragloside as model of soluble drug, the total puerariae flavones as model of insoluble drug,investigate the the release acts of the effective part with different nature in the hydrophilic matrix gel of HPMC.Research the relation of drug release with the time and the dissolution of HPMC, by calculating the prescription component equivalent molecular weight (Meq), derived quantitative mathematical Model. Further explore and study the release behavi