含有抗炎药固体分散体的外用凝胶的配制与评估

Sethu Lekshmi, Therase Jose, Manju Maria Mathews, B. R
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摘要

从溶解性差的药物中配制和开发出最有效的产品是制药业最具挑战性的任务之一。固体分散体是克服溶解性问题的一种有效的溶解性增强方法。本研究旨在配制含有醋氯芬酸固体分散体的外用凝胶,以提高其在皮肤中的渗透性。使用合适的亲水性载体制备了醋氯芬酸固体分散体,以增加其水溶性。本研究采用溶剂蒸发和共同研磨的方法,用聚乙烯吡咯烷酮(PVPk-30)和 HPMC E15 LV 这两种不同的亲水性载体制备了醋氯芬酸的固体分散体。药物与载体的比例分别为 1:1、1:2 和 1:3。制剂优化的评估参数包括药物含量、实际产量百分比、DSC、体外溶解度研究和傅立叶变换红外光谱。使用 Carbopol 934 和 HPMC K100M 这两种胶凝剂将优化后的 SD(F3)固体分散体加入到不同浓度的局部凝胶中。体外溶解研究结果表明,与其他制剂和纯药物相比,含有 PVP k30(药物和 PVP k30 的比例为 1:3)的制剂 F3 的溶解速率更高。使用两种不同浓度的胶凝剂,将优化后的固体分散体加入到制备的局部凝胶中。从获得的稳定性数据来看,物理外观、粘度、pH 值和药物含量均无明显变化。可以认为,本研究工作成功地生产出了含有醋氯芬酸固体分散体的外用凝胶。预计水溶性将得到改善,从而提高皮肤渗透性。
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 gels incorporated with solid dispersions of an antiinflammatory drug
Formulation and development of a most effective product from poorly soluble drugs is one of the most challenging tasks in pharmaceutical industries. Solid dispersion is an efficient solubility enhancement method to overcome the solubility problem. The aim of this study was to formulate topical gels incorporated with solid dispersion of Aceclofenac to enhance permeability through the skin. Aceclofenac solid dispersions were prepared using suitable hydrophilic carriers to increase its aqueous solubility. In this study, solid dispersions of Aceclofenac were prepared by solvent evaporation and co-grinding method with two different hydrophilic carriers such as polyvinyl pyrrolidone (PVPk-30), and HPMC E15 LV. These were used in the ratio of (drug: carrier) 1: 1, 1:2 & 1:3 respectively. Evaluation parameters for formulation optimization were drug content, percentage practical yield, DSC, , in-vitro dissolution studies & FTIR. The optimized SD (F3) solid dispersion is incorporated in topical gels of different concentrations prepared by using two gelling agents such as Carbopol 934 and HPMC K100M. From the results of in-vitro dissolution studies it was found that formulation F3 containing PVP k30 (1 : 3 ratio of drug: PVP k30) shows a higher dissolution rate compared with other formulations and pure drug. Optimized solid dispersion was incorporated into topical gels prepared by using two gelling agents in different concentrations. From the stability data obtained, no significant changes in physical appearance, viscosity, pH, and drug contents were seen. The present research work could be concluded as a successful production of topical gels incorporated with Aceclofenac solid dispersion. Improvement in aqueous solubility and thereby greater skin permeation is expected
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