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温敏型黏膜黏附性眼前房原位凝胶:聚合物组合设计与优化。

Thermoreversible mucoadhesive ophthalmic in situ hydrogel: Design and optimization using a combination of polymers.

机构信息

Department of Pharmaceutics, K. B. Institute of Pharmaceutical Education and Research, Gandhinagar, Gujarat-382023, India.

出版信息

Acta Pharm. 2010 Sep;60(3):349-60. doi: 10.2478/v10007-010-0029-4.

Abstract

The purpose of the study was to develop an optimized thermoreversible in situ gelling ophthalmic drug delivery system based on Pluronic F 127, containing moxifloxacin hydrochloride as a model drug. A 3(2) full factorial design was employed with two polymers: Pluronic F 68 and Gelrite as independent variables used in combination with Pluronic F 127. Gelation temperature, gel strength, bioadhesion force, viscosity and in vitro drug release after 1 and 10 h were selected as dependent variables. Pluronic F 68 loading with Pluronic F 127 was found to have a significant effect on gelation temperature of the formulation and to be of importance for gel formation at temperatures 33-36 °C. Gelrite loading showed a positive effect on bioadhesion force and gel strength and was also found helpful in controling the release rate of the drug. The quadratic mathematical model developed is applicable to predicting formulations with desired gelation temperature, gel strength, bioadhesion force and drug release properties.

摘要

本研究旨在开发一种基于泊洛沙姆 F127 的优化的温敏原位凝胶眼用给药系统,其中包含盐酸莫西沙星作为模型药物。采用 3(2) 完全析因设计,以两种聚合物(泊洛沙姆 F68 和明胶)作为独立变量,与泊洛沙姆 F127 联合使用。凝胶温度、凝胶强度、生物黏附力、黏度和 1 小时及 10 小时后的体外药物释放率被选为因变量。结果表明,泊洛沙姆 F68 与泊洛沙姆 F127 的负载对制剂的凝胶温度有显著影响,对于 33-36°C 温度下的凝胶形成非常重要。明胶负载对生物黏附力和凝胶强度有积极影响,并且有助于控制药物的释放速率。所建立的二次数学模型适用于预测具有所需凝胶温度、凝胶强度、生物黏附力和药物释放特性的制剂。

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