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用于局部应用的倍他米松 17-戊酸去氧胆酸水凝胶:体外和体内评价。

Deoxycholate hydrogels of betamethasone-17-valerate intended for topical use: In vitro and in vivo evaluation.

机构信息

Ege University, Department of Pharmaceutical Technology, 35100 Bornova, Izmir, Turkey.

出版信息

Int J Pharm. 2011 Jan 17;403(1-2):123-9. doi: 10.1016/j.ijpharm.2010.10.036. Epub 2010 Nov 1.

Abstract

The aim of this study was to evaluate the suitability of sodium-deoxycholate (Na-DOC) gels containing betamethasone-17-valerate (BMV) for topical application. The gels were characterized for rheological and textural properties. The in vitro flux of BMV from Na-DOC gels across rat skin was 2.5 (0.05% gel) and 8.5 times (0.1% gel) higher compared to the commercial cream (0.1%), respectively. The pharmacodynamic responses after in vivo topical application in rats were also determined. A significant correlation between anti-inflammatory activity and in vitro permeation of BMV was observed. Na-DOC gels produced significantly higher edema inhibition compared to commercial cream at all time intervals. Finally, according to the results of histology studies, Na-DOC gel has no irritant effect on the skin. In conclusion, Na-DOC gel formulation could be suggested as a promising alternative system for the topical application of BMV.

摘要

本研究旨在评估含有倍他米松 17-戊酸酯(BMV)的脱氧胆酸钠(Na-DOC)凝胶用于局部应用的适宜性。对凝胶的流变学和质构特性进行了表征。与商业乳膏(0.1%)相比,Na-DOC 凝胶中 BMV 的体外通量分别高出 2.5 倍(0.05%凝胶)和 8.5 倍(0.1%凝胶)。还测定了大鼠体内局部应用后的药效学反应。观察到抗炎活性与 BMV 的体外渗透之间存在显著相关性。Na-DOC 凝胶在所有时间间隔的水肿抑制作用均明显高于商业乳膏。最后,根据组织学研究的结果,Na-DOC 凝胶对皮肤没有刺激性作用。总之,Na-DOC 凝胶制剂可作为局部应用 BMV 的有前途的替代系统。

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