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Preparation of Thermosensitive Gel Loaded by Chloramphenicol Solid Lipid Nanoparticles for Ophthalmic Use

Author: KongZhiFeng
Tutor: ZhangDianRui
School: Shandong University
Course: Pharmacy
Keywords: Chloromycetin Solid Lipid Nanoparticles Ophthalmic thermosensitive hydrogel
CLC: R94
Type: Master's thesis
Year: 2011
Downloads: 92
Quote: 0
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Abstract


Most of the treatment of eye diseases need administered topically, the drug into the eye cavity and tissues. The eyes of the highly sensitive and effective protection mechanism to limit the many pharmacy means, brought great difficulties for the design of the dosage form. In this study, the introduction of temperature-sensitive polymer materials poloxamer ocular drug delivery systems, ophthalmic preparations were free-flowing liquid at room temperature, after administration of a semi-solid gel. Can effectively overcome the shortcomings of conventional ophthalmic preparations, and to achieve the administration purposes. The papers to chloramphenicol as a model drug, with the trial design software Design Expert (version7.1.3, beta), using the Box-Behnken experimental design, inspect oil phase dosage, F188 dosage drugs accounted for the proportion of the oil phase three factors. the impact of solid lipid nanoparticles, turbidity (NTU), encapsulation efficiency (EE%) and drug loading amount (DL%) indicators, using multiple regression equation to fit between the factors and response functions relationship, multivariate statistical and mathematical methods to solve the optimization design of chloramphenicol - solid lipid nanoparticles prescription. Research was optimized prescription chloramphenicol solid lipid nanoparticles oil phase (glycerol monostearate) the amount of 10% F188 amount of 8%, the chloramphenicol and oil phase mass ratio to 13.55%, the resulting The product in sustained action. Use poloxamer 407 and poloxamer 188 as the main matrix, using the cold solution prepared gel solution, stir Determination gelling temperature, effects of the concentration of the poloxamer 407 and poloxamer 188 and the phase transition temperature the relationship between the optimal choice 25? 07/6? 88 as temperature-sensitive gel matrix. Chloramphenicol - solid lipid nanoparticles with blank temperature-sensitive gel matrix according to the proportion of research and evenly Synthesis of eye gel with temperature-sensitive. By high performance liquid chromatography prepared chloramphenicol standard curve, recovery test, determination of chloramphenicol, thermosensitive hydrogel chloramphenicol, P407 content, in vitro dissolution kinetics study and investigate the drug release mechanism. The results show that the temperature-sensitive gel dissolution conform Hixon-Crowell model, HPLC method for the determination of temperature-sensitive gel chloramphenicol content is simple, fast, and reliable measurement results. Establish a high-performance liquid chromatography eye method for the determination of the temperature-sensitive gel chloramphenicol, and temperature-sensitive gels prepared in vitro release test and the in vitro rabbit corneal penetration test, while the effects of temperature-sensitive gel home rabbit eye irritation. Pharmacokinetic experiments using rabbits as experimental animals, rabbit aqueous humor concentration of the CAP in different time using High Performance Liquid Chromatography with DAS pharmacokinetic dynamics software processing to calculate the pharmacokinetic parameters. Prove the ophthalmic thermosensitive hydrogel extended CAP in eye retention time, eye irritation small, well tolerated and no significant ocular toxicity in vitro and in vivo experiments, can significantly extend the drug residence time in the eye, enhancing drug bioavailability, with a high clinical value, is expected to become a new type of drug delivery system for the treatment of eye diseases, eye to show a good application prospect.

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CLC: > Medicine, health > Pharmacy > Pharmacy
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