大豆异黄酮结肠靶向缓释胶囊的结肠定位释药与吸收研究.docVIP

大豆异黄酮结肠靶向缓释胶囊的结肠定位释药与吸收研究 任彦荣1,2，胡宗利1，陈国平1* （1.重庆大学生物工程学院，重庆 400044；2.重庆教育学院生化系，重庆 400067） 摘要 目的：缓释：缓释：大豆异黄酮结肠靶向缓释胶囊1/2和MRT均明显延长，而且前者在结肠组织中生物利用度较后者的2.42倍，前者在血浆中生物利用度较是后者的3.02倍。 结论：大豆异黄酮结肠靶向缓释胶囊Study on the colon site-specific delivery and absorption of soybean isoflavone colon targeting sustained-release pellet capsules REN Yan-rong1,2 , Hu Zong-li1 , CHEN Guo-ping1* （1 College of Bioengineering, Chongqing University, Chongqing 400044, 2 Chongqing Education College, Chongqing 400067, China）the absorption and distribution of chitosan capsule filled with soybean isoflavone sustained-release pellets in rats.Methods:The soybean isoflavone sustained-release pellets were filled into the chitosan capsules coated with HPMCP. The capsules as well as the other soybean isoflavone capsules were administered orally. Blood and colon tissue were collected periodically, the concentrationof soybean isoflavone was measured by HPLC,and used to calculate pharmacokinetic parameters.Results: After oral administration,the t1/2 and MRT of soybean isoflavone colon targeting sustained-release pellet capsules were significantly prolonged,and the bioavailability of the former is the latter 2.42 times in colon, the bioavailability of the former is the latter 3.02 times in plasma. Conclusion: Soybean isoflavone colon targeting sustained-release pellet capsules may be more better in colon location release drug effect than conventional capsule.Hence,it is worth studying further. Key words：soybean isoflavone；sustained release capsules;colon site-specific delivery 大豆异黄酮（soybean isoflavone）是异黄酮类混合物，其母核结构为3-苯并呋喃酮，是存在于大豆等豆科植物中一类重要的生物活性物质。但其口服生物利用度仅为10%～40%，药理研究发现结肠是决定大豆异黄酮生物利用率的主要部位[]。我们将大豆异黄酮制备成混合型骨架型的缓释制剂，装入具有胶囊中，体外研究发现具有一定的缓释作用。仪器、材料和动物 Agilent1100 Series高效液相色谱仪（Agilent公司，USA）；CP225D电子天平（北京赛多利斯科学仪器有限公司）；LDZ5-2离心机 (北京医用离心机厂)XW-80A漩涡混合仪 (上海医科大学仪器厂)染料木苷元对照品(sigma公司，编号：G-6055)其他试剂均为分析纯色谱条件ZOBAX SB-C18（5μm，250mm×4.6mm）；流动相：-0.1%H3PO4水溶液(4：)；检测波长：262nm；柱温：35℃；流速：1.0mL/min；进样量20μl。染料木苷元染料木苷元空白血浆、染料木苷元、受