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柠檬草油作为渗透促进剂的洛索洛芬氨丁三醇凝胶剂的制备及评价。

Formulation and Characterization of Emulgel Lornoxicam Containing Lemon Grass Oil as Penetration Enhancer.

机构信息

Institute of Pharmaceutical Research, GLA University, Uttar Pradesh, Mathura, 281406, India.

出版信息

Antiinflamm Antiallergy Agents Med Chem. 2024;23(3):164-173. doi: 10.2174/0118715230289163240703075629.

Abstract

INTRODUCTION

Emulgel dosage form is an advanced form of transdermal drug delivery. It is a combination of emulsion and gel in a definite ratio. Emulsions are incorporated into the gel with proper mixing. The emulsion present in emulgel can be either oil/water or water/oil, which is thickened by mixing it with a gelling agent.

MATERIALS AND METHODS

On the basis of the solubility of lornoxicam in various oils, a surfactant and a co-surfactant were selected for further research. For the preparation of emulgel, the emulsion was prepared with Smix (surfactant and co-surfactant) in a ratio of 1:2. The prepared emulsion was incorporated into different concentrations of carbapol 934 in a 1:1 ratio to make a homogenous emulgel.

RESULTS

The emulgel was inspected visually to see if it had any phase behaviour, spreadability, or grittiness by applying it to a slide. All formulations were evaluated for pH, physical properties, drug content, spreadability, extrudability, swelling index, viscosity, and centrifugation. Franz diffusion cell was used to perform release of formulation with the help of egg membrane. Among all formulations, F3 showed 83% release after 6 hours and showed acceptable physical properties like homogeneity, colour, consistency, pH value, spreadability, extrudability, and drug content.

DISCUSSION

Thus, emulgel can be regarded as a more feasible drug delivery system for hydrophobic drugs (lornoxicam) than the currently marketed formulation. Optimized emulgel formulation consists of a microemulsion of lornoxicam, 1% of carbopol 934, propylene glycol, sodium benzoate, lemon grass oil, glycerin, and distilled water. In the release studies, pH 7.4 phosphate buffer emulgel formulation (F3) showed 83% after 6 hours. Emulgel was found to be stable under stable conditions.

CONCLUSION

The emulgel of the poorly water-soluble drug (lornoxicam) was formulated. The components and their optimum ratio for the formulation of microemulsion were obtained by solubility studies and droplet size analysis. Thus, microemulsion can be regarded as a more feasible dose delivery system for lornoxicam than the currently marketed tablet, capsule, and injection formulations. Optimized microemulsion of lornoxicam was incorporated into the gel base. Therefore, it may be concluded that emulgel of lornoxicam can be used as a controlledrelease dosage form of the drug for local application in rheumatoid arthritis.

摘要

简介

乳凝胶剂型是一种先进的透皮药物传递形式。它是乳液和凝胶以一定比例的组合。通过适当的混合将乳液掺入凝胶中。乳凝胶中的乳液可以是油/水或水/油,通过与成胶剂混合将其增稠。

材料和方法

根据氯诺昔康在各种油中的溶解度,选择表面活性剂和助表面活性剂进行进一步研究。为了制备乳凝胶,用 Smix(表面活性剂和助表面活性剂)以 1:2 的比例制备乳液。将制备的乳液以 1:1 的比例掺入不同浓度的卡波姆 934 中,制成均匀的乳凝胶。

结果

通过将其涂在载玻片上,目视检查乳凝胶是否具有任何相行为、铺展性或沙砾感。所有配方均评估 pH 值、物理性质、药物含量、铺展性、挤出性、溶胀指数、粘度和离心。使用 Franz 扩散池在鸡蛋膜的帮助下进行制剂释放。在所有配方中,F3 在 6 小时后释放了 83%,并表现出可接受的物理性质,如均匀性、颜色、一致性、pH 值、铺展性、挤出性和药物含量。

讨论

因此,乳凝胶可以被认为是一种比目前市售制剂更适合疏水性药物(氯诺昔康)的药物传递系统。优化的乳凝胶配方由氯诺昔康的微乳、1%卡波姆 934、丙二醇、苯甲酸钠、柠檬草油、甘油和蒸馏水组成。在释放研究中,pH7.4 磷酸盐缓冲乳凝胶配方(F3)在 6 小时后释放了 83%。乳凝胶在稳定条件下稳定。

结论

对疏水性药物(氯诺昔康)的乳凝胶进行了配方。通过溶解度研究和液滴尺寸分析获得了微乳配方的成分及其最佳比例。因此,微乳可以被认为是比目前市售的片剂、胶囊和注射剂更适合氯诺昔康的剂量传递系统。优化的氯诺昔康微乳被掺入凝胶基质中。因此,可以得出结论,氯诺昔康乳凝胶可用作局部应用于类风湿关节炎的药物控释剂型。

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