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目的:利用壳聚糖胶囊作为载体将缓释微丸导向结肠,研究药物在大鼠体内的药动学过程和结肠靶向性规律。方法:制备大豆异黄酮缓释微丸,将其装入壳聚糖胶囊中,再以HPMCP包裹胶囊,分别给大鼠口服大豆异黄酮结肠靶向缓释胶囊(受试制剂)和市售大豆异黄酮普通胶囊(参比制剂),测定经时血药浓度和结肠组织中分布量,计算药动学参数。结果:大豆异黄酮结肠靶向缓释胶囊(受试制剂)和市售大豆异黄酮普通胶囊(参比制剂)比较,前者的t1/2和MRT(平均滞留时间)均明显延长,而且前者在结肠组织中生物利用度是后者的2.42倍,前者在血浆中生物利用度是后者的3.02倍。结论:大豆异黄酮结肠靶向缓释胶囊较市售大豆异黄酮普通胶囊具有更好的结肠定位释药作用,同时可以有效地提高大豆异黄酮的生物利用度,值得进一步开发研究。
OBJECTIVE: To study the pharmacokinetics and colon targeting of drugs in rats by using chitosan capsule as a carrier to guide the sustained-release pellets to the colon. Methods: Soybean isoflavone sustained-release pellets were prepared, loaded into chitosan capsules, and then encapsulated by HPMCP. Rats were orally administered with soy isoflavone colon-targeted sustained-release capsules (test preparation) and commercial soybean Isoflavones normal capsules (reference preparation), the determination of serum concentration over time and colon tissue distribution, calculation of pharmacokinetic parameters. Results: Compared with the conventional commercial soy isoflavones capsules (reference preparation), the t1 / 2 and MRT (average retention time) of the soy isoflavone colon targeted sustained release capsules (test preparation) were significantly prolonged, and the former was The bioavailability in colon tissue was 2.42 times that of the latter, while the former bioavailability in plasma was 3.02 times that of the latter. CONCLUSION: The soy isoflavone colon targeted slow-release capsules have better colon-specific release properties than common soy isoflavones capsules, and can effectively increase the bioavailability of soy isoflavones, which deserves further research.