阿司匹林胃漂浮胶囊制备及其体外释药特征的研究

Study of preparation of Asp-HBS by HPMC and Carbopol and drug release characteristic

目的采用HPMC和Carbopol制备胃漂浮胶囊。方法以阿司匹林为模型药物，以不同黏度和不同用量的HPMC和Carbopol为主要辅料制成胃内漂浮型胶囊，采用桨法测定了Asp漂浮胶囊的释放度。结果当HPMCK4M和HPMCK15M的最佳配比为3：1，阿司匹林胃漂浮胶囊在0～10h内体外释药符合表观零级动力学过程，体外释放速度常数Kr=10．3％·h^-1。经Peppas方程拟合后得出释放参数n=0．6173。从0．45〈n〈0．89表明，体外释药特征属于骨架溶蚀与药物扩散协同作用。结论HPMC用量、粘度为影响阿司匹林胃漂浮胶囊释放速率的主要因素。

Objective： To develop a gastric floating sustained release capsule by the use of HPMC and Carbopol as matrix material. Methods： Aspirin was as a model drug, the gastric floating capsule containing different viscosity HPMC and various dosage Carbopol as main exeipients, and paddle method was adopted to determine Asp-HBS release rates in vitro. Results： When the ratio between HPMCK4M and HPMCK15M （3 ： 1） was the best proportion, aspirin gastric floating in vitro release accorded with zero-order kinetics, and the constant of in vitro release was Kr=10. 3%· h^-1. Via Peppas equation simulation, the drug release character was marix erode and drug diffuse. Conclusion： The amount and viscosity of HPMC significantly influence aspirin release from the gastric floating capsule;