利用天然油脂开发和评估塞来昔布凝胶

Aarti Rajput, Rishabh Gaur, Mayank Kulshreshtha, Sumedha Singh Jadaun, Vibha Kumari
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引用次数: 0

摘要

背景介绍乳胶凝胶(Emulgel)结合了乳液和凝胶的特性。要制成不含或含水或不含水凝胶,必须先配制乳液,然后将乳液与胶凝剂结合,从而实现药物释放的双重控制。塞来昔布具有镇痛、解热和消炎活性,可用于治疗骨关节炎、剧烈疼痛、类风湿性关节炎和其他病症:方法:通过使用不同浓度的天然油和 carbopol-940 作为胶凝剂,开发并评估了塞来昔布凝胶。为了确定溶解度,对各种油、助表面活性剂和表面活性剂进行了筛选。精油(桉树油和松节油)被用作渗透改性剂。对与聚合物的相容性进行了研究,结果表明聚合物与药物物质之间不存在物理或化学作用。在制备乳胶凝胶时,使用 Smix(共表面活性剂和表面活性剂)比例(1:1、2:1 和 3:1)制备了各种乳液。在选择胶凝剂时,将选定的 1:1 的乳液体系比例与聚合物 carbapol 940、carbapol 934 和 HPMC(0:1:0、0:0.5:1、0:0:3、0.5:0:1、1:0:0)的凝胶基质组合在一起,制成均匀的乳胶:将凝胶薄层涂在载玻片上,目测凝胶是否有任何相态、手感、延展性和脆性。然后,用选定的胶凝剂制备了所有六种配方的乳凝胶。对所有乳凝胶的 pH 值、物理性质(稠度、均匀性、颜色、质地)、药物含量、铺展性、挤出性、膨胀指数、粘度、稳定性和离心力进行了评估。采用弗朗兹扩散池和鸡蛋膜进行体外药物释放:在所有制备的制剂中,EG1 的释放效果更好,粘度更高,药物含量更高,膨胀指数也高于其他制剂。制剂 EG1 在 8 小时内的药物释放率较高(91.25%)。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Development and Evaluation of Celecoxib Emulgel by Using Natural Oil.

Background: Emulgel combines the qualities of an emulsion with those of a gel. In order to create an emulgel w/o or o/w, emulsions have to be formulated, which are then combined with a gelling agent, resulting in a dual-control drug release. Celecoxib exhibits analgesic, antipyretic and anti-inflammatory activities and is used to treat osteoarthritis, severe pain, rheumatoid arthritis, and other medical conditions.

Methods: Celecoxib Emulgel was developed and evaluated by using natural oil and carbopol- 940 as a gelling agent in different concentrations. The screening of various oils, co-surfactants and surfactants was performed to determine the solubility. The essential oils (eucalyptus oil and turpentine oil) were used as penetration modifiers. Studies on compatibility with polymers have been conducted, and the results indicate that there should be no physical or chemical interactions between the polymers and the drug substance. For the preparation of emulgel, various emulsions were prepared with Smix (cosurfactant and surfactant) ratios (1:1, 2:1 and 3:1). The selection of a gelling agent was done by incorporating the selected emulsion system ratio of 1:1 with the combinations of polymers carbapol 940, carbapol 934, and HPMC (0:1:0, 0:0.5:1, 0:0:3, 0.5:0:1, 1:0:0) gel base to make a homogenous emulgel.

Results: The emulgel was examined visually to see if it had any phase behaviour, feel, spreadability, and grittiness by applying its thin layer to a slide. Then, all six formulations of emulgel were prepared with the selected gelling agent. All emulgels were evaluated for pH, physical properties (consistency, homogeneity, colour, texture), drug content, spreadability, extrudability, swelling index, viscosity, stability and centrifugation. A Franz diffusion cell and an egg membrane were used to perform in-vitro drug release.

Conclusion: Among all prepared formulations, EG1 had a better release, higher viscosity, higher drug content, and a higher swelling index than the others. The formulation EG1 showed higher drug release (91.25%) within 8 hours.

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