Study on the Ocular Pharmacokinetics of Ion-Activated In Situ Gelling Ophthalmic Delivery System for Gatifloxacin by Microdialysis |
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| Authors: | Zhidong Liu Xing-Gang Yang Xiang Li Weisan Pan Jiawei Li |
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| Affiliation: | 1. Department of Pharmaceutical, Shenyang Pharmaceutical University, Shenyang, P. R. China;2. Research Center of Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, P. R. China;3. Department of Experimental Department, Tianjin University of Traditional Chinese Medicine, Tianjin, P. R. China |
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| Abstract: | The poor bioavailability and therapeutic response exhibited by conventional ophthalmic solutions due to rapid precorneal elimination of the drug may be overcome by the use of gel system. The present work was conducted to evaluate the relative bioavailability of ion-activated in situ ophthalmic gel of gatifloxacin by microdialysis. The conventional ophthalmic solution of gatifloxacin was used as reference. The AUC of test group is 3.8-fold vs. the reference group (1.4316 ± 0.1327 μg·mL?1·h vs. 0.3756 ± 0.0380 μg·mL?1·hr) (P < 0.05), and the Cmax of test group vs. the control group is 3.0-fold (0.3363 ± 0.0634 μg·mL?1 vs. 0.1112 ± 0.0151 μg·mL?1) (P < 0.05). The Tmax of test group is longer than that of reference group (2.0 ± 0.67 hr vs. 0.667 ± 0.17 hr) (P < 0.1), and Ke of test group is lower than that of reference group. The developed formulation has a higher bioavailability and longer residence time in aqueous humor than conventional ophthalmic solutions. The developed system is a viable alternative to conventional eye drops. |
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| Keywords: | gatifloxacin ion-activated in situ gelling ophthalmic delivery system pharmacokinetics microdialysis |
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