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目的:考察眼用复方阿奇霉素温度敏感型原位凝胶兔眼局部单次应用后角膜及房水中的药动学特征。方法:日本大耳白兔39只,随机分为13个时间组,双眼分别给予眼用复方阿奇霉素温度敏感型原位凝胶50μl,分别于给药后5,15,30 min,1,6,12,24,48,96,144,192,240 h后抽取房水,处死,剖取角膜组织,以HPLC-MS/MS法检测角膜及房水中的药物浓度,评价阿奇霉素在兔眼角膜及房水中药动学特征。结果:房水中的达峰浓度(Cmax)为(0.050 1±0.015)μg·ml-1(1 h),角膜中的达峰浓度为(45.2±14.3)μg·g-1(15 min);房水中和角膜中阿奇霉素的半衰期(t1/2)分别为85.0h和84.4 h;房水中和角膜中的AUC(0-240)分别为1.230 7μg·ml-1·h-1和1 969.8μg·g-1·h-1。结论:眼用复方阿奇霉素温度敏感型原位凝胶兔眼给药后,角膜中迅速的达到较高的药物浓度,并持续较长时间,有很好的临床应用前景。
OBJECTIVE: To investigate the pharmacokinetics of cornea and aqueous humor after local single application of ophthalmone azithromycin temperature-sensitive in situ gel rabbit eye. Methods: Thirty-nine Japanese white rabbits were randomly divided into 13 time groups. The eyes were given 50μl of azithromycin in situ temperature-sensitive gels, respectively, at 5, 15, 30 min, After 12,24,48,96,144,192,240 h, aqueous humor was extracted and sacrificed. Corneal tissue was dissected. The concentration of drug in cornea and aqueous humor was detected by HPLC-MS / MS, and the pharmacokinetics of azithromycin in cornea and aqueous humor were evaluated. Results: The peak concentration in aqueous humor was (0.050 1 ± 0.015) μg · ml-1 (1 h) and the peak concentration in cornea was (45.2 ± 14.3) μg · g-1 (15 min) The half-lives (t1 / 2) of azithromycin in aqueous humor and cornea were 85.0 h and 84.4 h, respectively; AUC (0-240) in aqueous humor and cornea were 1.230 7 μg · ml-1 · h-1 and 1 969.8 μg · g-1 · h-1. Conclusion: The ophthalmic compound azithromycin temperature-sensitive in situ gel rabbit eye after administration, the cornea rapidly reached a higher drug concentration, and continued for a long time, there is a good clinical application.