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比较不同制剂技术对梓葛复方制剂口服后葛根素、梓醇吸收及入脑的影响,为开发梓葛口服新制剂奠定实验基础。制备载药的纳米晶、自微乳[分别用聚氧乙烯脱水山梨醇单油酸酯(吐温-80)和Cremophor RH-40为乳化剂]和羟丙基-β-环糊精包合物,小鼠灌胃给药后,HPLC-MS/MS同时测定血浆、脑组织中葛根素和梓醇的含量,计算药动学参数,比较葛根素、梓醇在血浆和脑组织中的药动学参数和脑靶向指数。各制剂技术对葛根素、梓醇的口服吸收和入脑有不同影响:自微乳(吐温-80)较其余各组更能促进葛根素的口服吸收(P<0.05),包合物较纳米晶能显著增加梓醇的口服吸收(P<0.01);包合物组葛根素的脑靶向指数显著高于其余各组(P<0.05),而梓醇则是包合物、自微乳均较纳米晶有更高的脑靶向指数(P<0.05);就脑组织AUC而言,葛根素以自微乳(吐温-80)组最大,显著高于其余各组(P<0.01),梓醇以包合物组最大,但与自微乳组无显著性差异。自微乳(吐温-80)技术能提高葛根素、梓醇的口服入脑量,有望用于开发梓葛复方口服新制剂。
The effects of different preparation techniques on the absorption of puerarin and catalpol into the brain after oral administration of Zi Ge Compound Preparations were compared, which laid the experimental foundation for the development of new oral preparation of Zi Ge. Preparation of drug loaded nanocrystals, self-microemulsion [polyoxyethylene sorbitan monooleate (Tween-80) and Cremophor RH-40 as emulsifier] and hydroxypropyl-β-cyclodextrin inclusion Pharmacokinetic parameters of puerarin and catalpol in plasma and brain tissue were determined by HPLC-MS / MS simultaneously after gavage administration. The pharmacokinetics of puerarin and catalpol in plasma and brain tissue were compared Kinetic parameters and brain targeting index. Each preparation technique had different effects on the oral absorption of puerarin and catalpol, and on the brain. Self-microemulsion (Tween-80) promoted the oral absorption of puerarin more significantly than the other groups (P <0.05) Nanocrystals could significantly increase the oral absorption of catalpol (P <0.01). The brain-targeting index of puerarin in the inclusion complex was significantly higher than that of the other groups (P <0.05) (P <0.05). Compared with nanocrystals, puerarin had the highest brain targeting index (P <0.05), and the highest puerarin (Tween-80) group was significantly higher than the other groups in terms of AUC 0.01), catalpol was the largest inclusion compound group, but no significant difference with self-microemulsion group. Self-microemulsion (Tween -80) technology can improve the oral intake of puerarin, catalpol, is expected to be used for the development of Zi Ge compound oral preparation.