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依据流体动力学平衡体系制备了一种包含尼莫地平固体分散体的新型胃内漂浮缓释系统,提高难溶性药物尼莫地平溶出速率的同时控制其释放,以达到既高效又长效的目的。尼莫地平固体分散体以poloxamer188为载体溶剂──熔融法制备。缓释漂浮片由尼莫地平固体分散体、羟丙甲纤维素、碳酸镁、十六醇等组成,均匀设计法优化处方。较优处方于体内外均显示了较好的漂浮状态。体内同位素示踪研究表明该系统可明显延长体内的滞留时间,而非漂浮片则很快通过吸收部位。饮食对该系统的体内转运有明显的影响,空腹服用将大大缩短该系统的体内滞留时间。统计矩分析表明该系统的相对生物利用度为普通尼莫地平片的四倍,体内平均滞留时间为其二倍。
According to the hydrodynamic equilibrium system, a novel gastric floating and sustained release system containing solid dispersion of nimodipine is prepared to improve the dissolution rate of the poorly soluble drug nimodipine while controlling its release so as to achieve both high efficiency and long-term efficacy . Nimodipine solid dispersion poloxamer188 as carrier solvent ─ ─ melt preparation. Sustained-release floating tablets from nimodipine solid dispersion, hypromellose, magnesium carbonate, cetyl alcohol and other components, uniform design optimization prescription. The superior prescription showed better floating status both in vitro and in vivo. In vivo isotope tracing studies have shown that this system can significantly prolong the residence time in the body, whereas non-floating tablets pass through the absorption site quickly. Diet has a significant effect on the in vivo transport of the system, and fasting will greatly reduce the in vivo residence time of the system. Statistical moment analysis showed that the relative bioavailability of this system was four times of that of nimodipine, and the average residence time in vivo was twice.