1. Shandong B&L Freda Pharm. Co.��Ltd.��Jinan 250014��China��2.Drug Safety Evaluation Center of Shandong Institute of Pharmaceutical Industry��Jinan 250033��China
Abstract��
OBJECTIVE To compare the pharmacokinetics and bioavailability of gatifloxacin ophthalmic gel with gatifloxacin eye drops by topical application.METHODS New Zealand rabbits' left eyes were topically applied 60 ��L of gatifloxacin ophthalmic gel,the right eyes were topically applied 60 ��L of gatifloxacin eye drops.Tears,aqueous humors and corneas were sampled at different intervals after drug instillation,and the drug levels were assayed by liquid chromatograph/mass spectrometer(LC-MS).RESULTS The half-lives of elimination in the tears were 195.3 and 80.7 min,and the AUC0��480 of the drug levels in the tears were 62 385 and 33 280 ��g��min��g-1 for the test group and the reference group respectively.The peak levels of drug in aqueous humors were 1.05 and 0.62 mg��L-1,and the AUC0��360 of the drug levels in the aqueous humors were 111.7 and 66.1 mg��min��L-1 respectively.The AUC0��480 of the drug levels in the corneas were 3 435.5 and 1 688.4 ��g��min��g-1 respectively.CONCLUSION The bioavailability of gatifloxacin ophthalmic gel was increased significantly,and its action time was obviously increased compared with gatifloxacin eye drops.
2007, Vol. 42 
