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醋氯芬酸-芦荟透皮凝胶剂的制剂与表征

Formulation and Characterization of Aceclofenac -Aloe vera Transemulgel.

作者信息

Raju Y Prasanna, Haritha K, Satyanarayana Rao P, Vandana K R, Bindu D Thushara, Vinesha V, Chowdary V Harini

机构信息

Sri Padmavathi School of Pharmacy, Tiruchanur, Tirupati, IN517103, India.

出版信息

Curr Drug Deliv. 2015;12(6):703-8. doi: 10.2174/156720181206151228113209.

DOI:10.2174/156720181206151228113209
PMID:25751659
Abstract

The present research was aimed to formulate aceclofenac transemulgel using Aloe vera as gel base. The prepared formulations were subjected to physical characterization, in-vitro and in-vivo assessment. Aceclofenac, a hydrophobic potential non steroidal anti inflammatory drug, causes ulceration upon chronic oral administration, could be formulated into transemulgel to enhance therapeutic efficacy and to lower the unwanted side effects. The transemulgel was prepared from aqueous Aloe vera gel and aceclofenac emulsion. The prepared transemulgel was evaluated for its pH, viscosity, drug content, skin irritation, in-vitro diffusion and accelerated stability studies. The prepared aceclofenac-Aloe vera tranemulgel and commercial aceclofenac gel were subjected to pharmacodynamic studies in albino rats of Wistar strain employing carrageenan induced left hind paw edema method to assess the anti-inflammatory effect. The transemulgel showed a pH of 6.78 and viscosity of 18 cps. In-vitro diffusion data revealed better permeation characteristics. Topical application of formulation found no skin irritation. Stability study has proved the integrity of the formulation. The prepared aceclofenac Aloe vera transemulgel showed better in-vitro drug release when compared with the commercial aceclofenac gel formulation. Anti-inflammatory activity in treated rats showed the significant paw volume reduction at p<0.05 compared with that of control. Thus, it is concluded that aceclofenac, a potential non steroidal anti inflammatory drug, showed high therapeutic efficiency when formulated into transemulgel using aqueous Aloe vera as gel base.

摘要

本研究旨在以芦荟为凝胶基质制备醋氯芬酸透皮凝胶。对所制备的制剂进行了物理表征、体外和体内评估。醋氯芬酸是一种具有疏水性的非甾体抗炎药,长期口服会导致溃疡,可制成透皮凝胶以提高治疗效果并降低不良反应。透皮凝胶由芦荟水凝胶和醋氯芬酸乳剂制备而成。对所制备的透皮凝胶进行了pH值、粘度、药物含量、皮肤刺激性、体外扩散和加速稳定性研究。采用角叉菜胶诱导Wistar品系白化大鼠左后爪水肿法,对所制备的醋氯芬酸-芦荟透皮凝胶和市售醋氯芬酸凝胶进行药效学研究,以评估其抗炎效果。该透皮凝胶的pH值为6.78,粘度为18厘泊。体外扩散数据显示其具有更好的渗透特性。制剂的局部应用未发现皮肤刺激性。稳定性研究证明了制剂的完整性。与市售醋氯芬酸凝胶制剂相比,所制备的醋氯芬酸芦荟透皮凝胶显示出更好的体外药物释放。在治疗的大鼠中进行的抗炎活性研究表明,与对照组相比,在p<0.05时爪体积显著减小。因此,得出结论:醋氯芬酸作为一种潜在的非甾体抗炎药,以芦荟水凝胶为凝胶基质制成透皮凝胶时显示出较高的治疗效率。

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