利巴韦林原位胶化滴眼液在泪液中消除动力学的研究
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孙海燕 丁婉萍 唐 星
(沈阳药科大学 药学院，辽宁 沈阳 110016)
摘要：目的 比较利巴韦林滴眼液及其原位胶化滴眼液在兔泪液中的药代动力学。方法 两种制剂滴眼后，用反相高效液相色谱法测定不同时间兔眼结膜囊内泪液中利巴韦林的浓度，药物动力学参数用3P87进行处理，用SPSS统计软件对实验组和对照组AUC和tMRT进行t检验。结果 原位胶化滴眼液的泪液药物浓度-时间曲线下面积(AUC)和平均滞留时间(tMRT)明显大于对照组。结论 利巴韦林原位胶化滴眼液可明显延长药物在眼部的滞留时间，提高药物的生物利用度。
关键词： 药剂学；原位胶化滴眼液；反相高效液相色谱法；利巴韦林；药物动力学；生物利用度
中图分类号：R978.5 文献标识码：A
Pharmacokinetics of topical application in situ gels of ribavirin in rabbit eyes
SUN Hai-yan，DING Wan-ping，TANG Xing
(School of Pharmacy， Shenyang Pharmaceutical University， Shenyang 110016， China)
Abstravt： Objective To study the pharmcokinetics of ribavirin (RBVR) in the tears of New Zealand white rabbits following topical application in situ gels of ribavirin (ISG-RBVR 1 g·L-1) and RBVR eye drops (1 g·L-1) to rabbit eyes. Methods The rabbit tears were obtained and quantified at different times after topically applying single dose of ISG-RBVR and RBVR eye drops to the rabbit eyes.The drug level was assayed by RP-HPLC with UV dector.The pharmacokinetic parameters were calculated with 3P87 and SPSS. Results The area under concentration (AUC)-time curve and mean retention time after applying ISG-RBVR were found to be sigificantly higher compared with those of RBVR eye drops respectively. Conclusion The ISG-RBVR，which upon exposure to physiological conditions will shift the gel phase， can significantly extend RBVR release and increase the precorneal residence time of the drug， thus enhance ocular bioavailability compared with RBVR eye drops.
Key words： pharmaceutics； in-situ-gels eye drops； RP-HPLC；ribavirin；pharmacokinetics； bioavailability
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