外用微海绵基克霉唑凝胶的制备及评价

Jitendra Shinde, Rakesh Patel, Shweta Shriwas
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引用次数: 0

摘要

该研究的首要目标是开发一种基于含有克霉唑的微海绵凝胶的新型药物递送方法。克霉唑不易被胃肠道吸收,半衰期很短,只有2小时。被肝脏代谢成惰性分子。因此,必须修改氯霉唑的给药方法,使其适合外用。微海绵给药是一种新的药物缓释途径。采用准乳状溶剂扩散技术,以二氯甲烷(DCM)和乙醇(1:1)为原料,制备了微海绵。许多指标,包括产量,包封效率,粒度测量和体外药物释放研究,用于每个微海绵配方。外用时,将优化后的微海绵制剂F6转化为凝胶制剂。根据物理因素,如pH值、粘度、铺展性、药物含量和体外扩散研究,将制备的凝胶与市售配方进行比较。结果表明,准乳液溶剂扩散法制备微海绵是一种很有前途的制备方法。克霉唑在微海绵凝胶制剂MGI (F6)中稳定释放12小时。因此,微海绵形式的药物可以减少不良反应的风险,并通过避免皮肤接触来提高患者的依从性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Formulation and Evaluation of Topical Microsponge Based Gel of Clotrimazole
The study's overarching goal is to develop a novel medication delivery method based on microsponge gel containing clotrimazole. Clotrimazole is poorly absorbed from the gastrointestinal tract (GIT), has a short half-life of only 2 h, & is metabolized into inert molecules by the liver. Therefore, clotrimazole's drug delivery method must be modified for topical application. Microsponge delivery is a novel approach to sustained drug release. Microsponges were made with a polymer solution of Eudragit RS 100 in dichloromethane (DCM) and ethanol (1:1) using a quasi-emulsion solvent diffusion technique. A number of metrics, including production yield, entrapment efficiency, particle size measurement, and in vitro drug release studies, were used to each microsponge formulation. For topical administration, the optimized microsponge formulation F6 was transformed into a gel formulation. Prepared gel was compared to a commercially available formulation based on physical factors such as pH, viscosity, spreadability, drug content, and an in vitro diffusion investigation. Most of the formulations were discrete and spherical in shape, indicating a satisfactory production yield, suggesting quasi-emulsion solvent diffusion method is a promising methodology for the fabrication of microsponge. Clotrimazole was released steadily over the course of 12 hours from the microsponge gel formulation MGI (F6). Therefore, the medicine in the form of a microsponge can reduce the risk of adverse effects and increase patient compliance by avoiding skin contact.
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