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用于皮肤应用的灰黄霉素水凝胶的制备。

Preparation of hydrogels of griseofulvin for dermal application.

作者信息

Aggarwal N

机构信息

University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India.

出版信息

Int J Pharm. 2006 Dec 1;326(1-2):20-4. doi: 10.1016/j.ijpharm.2006.07.001. Epub 2006 Jul 8.

Abstract

In an attempt to prepare topical formulations of griseofulvin that can deliver the drug locally in effective concentration, various hydrogel formulations were prepared using carbomer (940 NF) as base; essential oils, propylene glycol (PG), N-methyl-2-pyrrolidone (NMP) as penetration enhancers. The in vitro skin permeation studies through Laca mouse skin were performed using vertical type cells. PG in the hydrogel formulation was found to influence drug release rate by increasing its solubility and partitioning. Further combinations of PG with varying amounts of NMP in the hydrogel formulations exhibited a significantly greater increase in the flux on comparison with the control and formulation containing PG alone. The diffusion samples obtained by in vitro permeation studies through mouse skin when subjected to microbioassay using Microsporum gypseum as tester microorganism exhibited antifungal activity. This indicates that the drug permeated through the mouse skin possess sufficient antifungal activity in vitro against the tested microorganism. The prepared hydrogels did not show any skin sensitization and histological studies were carried out to check the safety of permeation enhancers used. Further these formulations were found to be stable at three different temperatures 4, 25 and 40 degrees C with respect to percent drug content, release characteristics, pH, transparency, feel and viscosity.

摘要

为了制备能以有效浓度局部递送灰黄霉素的局部用制剂,使用卡波姆(940 NF)作为基质制备了各种水凝胶制剂;使用精油、丙二醇(PG)、N-甲基-2-吡咯烷酮(NMP)作为渗透促进剂。通过垂直型细胞进行了经Laca小鼠皮肤的体外皮肤渗透研究。发现水凝胶制剂中的PG通过增加其溶解度和分配来影响药物释放速率。与对照和仅含PG的制剂相比,水凝胶制剂中PG与不同量NMP的进一步组合显示通量显著增加。通过体外渗透研究经小鼠皮肤获得的扩散样品,当使用石膏样小孢子菌作为测试微生物进行微生物测定时表现出抗真菌活性。这表明透过小鼠皮肤渗透的药物在体外对测试微生物具有足够的抗真菌活性。所制备的水凝胶未显示任何皮肤致敏作用,并进行了组织学研究以检查所用渗透促进剂的安全性。此外,发现这些制剂在4、25和40摄氏度这三个不同温度下,在药物含量百分比、释放特性、pH值、透明度、触感和粘度方面是稳定的。

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