吗替麦考酚酯纳米混悬剂的制备及其兔眼内生物学性质研究  

Preparation of Mycophenolate Mofetil Nanosuspensions and Ocular Biological Characters in Rabbits

作　　者：李伟[1] 辛萌[1] 杨丽娜[1] 吴祥根[1] 

机构地区：[1]山东省眼科研究所青岛眼科医院,山东青岛266071

出　　处：《中国药师》2010年第8期1072-1076,共5页China Pharmacist

摘　　要：目的:研究吗替麦考酚酯纳米混悬剂在兔眼角膜黏附性、泪液和房水药物动力学特性。方法:以薄膜分散-高压乳匀法制备纳米混悬剂,测定其理化性质。HPLC法检测角膜黏附、泪液和房水中的吗替麦考酚酯和麦考酚酸的含量。结果:混悬剂滴眼液呈米黄色乳液状,纳米混悬剂药物粒子呈圆球状,粒径均一,纳米混悬剂平均粒径592 nm,多分散系数Pdl为0.114,Zeta电位为-29.6 mV。与普通混悬剂滴眼液相比,纳米混悬剂的角膜黏附性、泪液和房水中药物浓度明显提高。结论:纳米混悬剂可以促进和提高吗替麦考酚酯眼局部给药后角膜黏附和药物吸收。Objective： To investigate the rabbits＇ corneal mucoadhesion, and the pharmacokinetic characters of mycophenolate mofetil nanosuspensions in lacrimal fluid and aqueous humor. Method： Mycophenolate mofetil nanosuspensions were prepared by thin- film method and high pressure homogenization, and their physico-chemical properties were also evaluated. The concentrations of mycophenolate mofetil and mycophenolic acid in corneal muscoadhesive samples,lacrimal fluid and aqueous humor samples were determined by HPLC. Result： Nanosuspension was ecru and the drug particles were discrete and spherical with smooth surfaces. The mean diameter of nanosuspension was 592 nm, the Pdl was 0. 114 and Zeta potential was - 29. 6 inV. The nanosuspension had a higher drug concentration in corneal museoadhesive samples, lacrimal fluid and aqueous humor samples than ordinary myeophenolate mofetil suspensuion. Conclusion： The nanosuspension can increase the corneal museoadhesive and drug absorption obviously.

关 键 词：吗替麦考酚酯 麦考酚酸 纳米混悬剂 

分 类 号：R945[医药卫生—微生物与生化药学]