【作者】 刘志东； 李佳玮； 聂淑芳； 潘卫三；

【Author】 Zhidong Liu, Jiawei Li, Shufang Nie, Weisan Pan

【机构】 沈阳药科大学药学院；

【摘要】 目的:研究Transcutol P(Trans)对五种药物的离体角膜透过率的影响,探讨其存眼用制剂中的应用。方法:采用体外扩散实验考察不同浓度的Trans对利巴韦林、依诺沙星、加替沙星,盐酸左氧氟沙星和奥沙普秦兔角膜透过率的影响。结果:Trans使盐酸左氧氟沙星和依诺沙星的表观渗透系数分别增加了3．0和3．3倍(P<0．01);0．005％和0．02％的Trans分别使利巴书林和加替沙星的表观渗透系数增加了1．5倍(P>0．05);Trans不能增大奥沙普秦的表观渗透系数．0．03％(v／v)Trans将其表观系数由7．819×10-6cm／s降低到2．787×10-6cm／s。结论:Trans能够增加水溶性药物的角膜透过量。更多还原

【Abstract】 PURPOSE: To explore the use of Transcutol P (Trans) in an ocular drug delivery system. METHODS: The effects of Trans on the corneal permeability of drugs were investigated in vitro, using isolated rabbit corneas. RESULTS: In the presence of Trans at a concentration between 0.005% and 0.03%, the maximum increase in the apparent permeability coefficient (Papp) was 1.5-, 1.5-, 3.0- and 3.3-fold for ribavirin, gatifloxacin, levofloxacin hydrochloride and enoxacin, respectively. However, the Papp value of oxaprozin was reduced in the presence of Trans. The maximum reduction was found to be 2.8-fold at a concentration of 0.03% Trans. CONCLUSION: Trans may have potential clinical benefits in improving the ocular drug delivery of hydrophilic compounds.更多还原