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Study on the Ophthalmic Drug Delivery System for Aspartic Levofloxacin

Author: GaoZuo
Tutor: WangDongKai
School: Shenyang Pharmaceutical University
Course: Pharmacy
Keywords: Ocular administration Chitosan nanoparticles Ionic crosslinking method Thermal -type gel Poloxamer Elimination kinetics Tissue distribution
CLC: R94
Type: Master's thesis
Year: 2005
Downloads: 52
Quote: 0
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Abstract


Most of the treatment of eye diseases topical drugs into the eye cavity and organizations. The traditional ophthalmic preparations often due to the special eye physiological barriers and protection mechanisms to the extremely low bioavailability. Aspartate levofloxacin as a model drug, from research lipophilic start, first of all try to be prepared chitosan nanoparticles, chitosan nanoparticles suspension and poloxamer thermal gel combined with the preparation of the compound administered system, the last of this the two formulations ordinary eye drops a the rabbit tear in the elimination of dynamics and intraocular tissue distribution comparison. Using ultraviolet spectrophotometry drug dissociation constants: pK 1 = 5.63 ± 0.03, the pK 2 = 8.52 ± 0.05; measured on the basis of the pH of the drug the value dependent apparent oil-water partition coefficient, and drugs in vitro corneal permeability visit. Results show that the oil-water distribution coefficient, corneal permeability is preferably in the vicinity of the isoelectric point, the drug apparent. Try ionic crosslinking SYSTEM prepared contained a water-soluble drug chitosan nanoparticles. By single factor and orthogonal experiment to optimize the prescription process, prepared nanoparticles of average particle size of 357nm, the zeta potential of 35mv, encapsulation efficiency was 14.01%. Encapsulation efficiency and levofloxacin show that the multi-anion complex, reducing the extent of the drug positively charged cationic drugs is one possible way to improve the encapsulation efficiency of these drugs. Prepared poloxamer thermal gel, chitosan nanoparticles added to the solution viscosity and gelling temperature rise, chitosan and poloxamer PEO block hydrogen bonding complexation hinder micelle entangling may be the cause. To the membrane dissolution model study in vitro release that simple poloxamer gel system in drug release with zero order kinetics process, the compound administered drug release system is a slight delay. Preparation in rabbits tear elimination kinetics and intraocular tissue distribution studies. Area under the curve (AUC) composite drug delivery system for drugs - 1.8 times the ordinary preparations; chitosan nanoparticles suspension was slightly higher than the ordinary preparations, but there was no significant difference (P> 0.05), with nanoparticles package seal low. Tissue distribution within the eye that can significantly affect the intraocular tissue concentration of drug in the length of the ocular surface residence time.

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