乙酰氯芬酸透皮贴剂的研制与评价

Rakesh Patel, G. Patel, A. Baria
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引用次数: 125

摘要

本研究的目的是通过溶剂蒸发技术,以邻苯二甲酸二丁酯为增塑剂,以聚合物重量的15% w/w加入不同比例的亲水性(羟丙基纤维素)和疏水性(乙基纤维素)聚合物体系,开发一种含有药物乙酰氯芬酸的基质型透皮治疗体系。研究了不同浓度的油酸和肉豆蔻酸异丙酯对乙酰氯芬酸透皮渗透的影响。用差示扫描量热法和红外光谱法对药物与聚合物的理化相容性进行了研究,结果表明药物与聚合物不存在不相容性。对配制的透皮膜的厚度、重量变化、药物含量、平整度、拉伸强度、折叠耐久性、含水率和水蒸气透射率进行物理评价。所制备的制剂均具有良好的物理稳定性。采用Franz扩散池对制剂进行体外渗透研究。与所有其他配方相比,含有渗透增强剂的亲水性聚合物制备的配方通过大鼠皮肤(Wistar白化大鼠)的体外皮肤渗透效果最好。结果表明,在不同处方条件下,乙酰氯芬酸的释放曲线符合零级和一级混合动力学。然而,优化处方F9的释放曲线(对Higuchi的r2 = 0.9935)表明,药物在贴片中的渗透受扩散机制控制。配方F9在所有配方中通量最高,药物渗透增强1.369倍。结果表明,油酸含量为15%,肉豆蔻酸异丙酯含量为10%时,乙酰氯芬酸在大鼠皮肤中的渗透性较好。关键词:醋氯芬酸,透皮膜,渗透促进剂,体外渗透研究
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 transdermal patch of Aceclofenac
The purpose of this research was to develop a matrix-type transdermal therapeutic system containing drug Aceclofenac with different ratios of hydrophilic (hydroxyl propyl cellulose) and hydrophobic (ethyl cellulose) polymeric systems by the solvent evaporation technique by using 15 % w/w of dibutyl phthalate to the polymer weight, incorporated as plasticizer. Different concentrations of oleic acid and isopropyl myristate were used to enhance the transdermal permeation of Aceclofenac. The physicochemical compatibility of the drug and the polymers studied by differential scanning calorimetry and infrared spectroscopy suggested absence of any incompatibility. Formulated transdermal films were physically evaluated with regard to thickness, weight variation, drug content, flatness, tensile strength, folding endurance, percentage of moisture content and water vapour transmission rate. All prepared formulations indicated good physical stability. In-vitro permeation studies of formulations were performed by using Franz diffusion cells. Formulation prepared with hydrophilic polymer containing permeation enhancer showed best in-vitro skin permeation through rat skin (Wistar albino rat) as compared to all other formulations. The results followed the release profile of Aceclofenac followed mixed zero-order and first-order kinetics in different formulation. However, the release profile of the optimized formulation F9 (r2 = 0.9935 for Higuchi) indicated that the permeation of the drug from the patches was governed by a diffusion mechanism. Formulation F9 showed highest flux among all the formulations and 1.369 fold enhancements in drug permeation. These results indicate that the formulation containing 15 % of oleic acid with 10 % Isopropyl myristate give better penetration of Aceclofenac through rat skin. Keywords: Aceclofenac, Transdermal Film, Permeation enhancer, In-vitro permeation study.
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