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恩诺沙星的体外经皮吸收:LMOG有机凝胶与戊聚糖乳膏的比较。

Ex-Vivo percutaneous absorption of enrofloxacin: Comparison of LMOG organogel vs. pentravan cream.

作者信息

Kirilov Plamen, Tran Van Hung, Ducrotté-Tassel Alban, Salvi Jean-Paul, Perrot Sébastien, Haftek Marek, Boulieu Roselyne, Pirot Fabrice

机构信息

Université Claude Bernard Lyon 1, EA 4169 "Aspects fondamentaux, cliniques et thérapeutique de la fonction barrière cutanée", SFR Lyon-Est Santé, INSERM US 7, CNRS UMS 3453, ISPB, 8 avenue Rockefeller, 69373 Lyon Cedex 08, France.

Université Claude Bernard Lyon 1, EA 4169 "Aspects fondamentaux, cliniques et thérapeutique de la fonction barrière cutanée", SFR Lyon-Est Santé, INSERM US 7, CNRS UMS 3453, ISPB, 8 avenue Rockefeller, 69373 Lyon Cedex 08, France.

出版信息

Int J Pharm. 2016 Feb 10;498(1-2):170-7. doi: 10.1016/j.ijpharm.2015.12.018. Epub 2015 Dec 11.

Abstract

The objective of this study was to investigate the percutaneous absorption of enrofloxacin from two base formulations, Pentravan cream and LMOG organogel. Ex-vivo experiments were carried out on pig ear skin. The percutaneous permeation through pig skin of two formulations containing 5 wt% of enrofloxacin was measured and compared using Franz diffusion cells. At appropriate intervals up to 120 h, diffusion samples were taken and analyzed using HPLC assays. Permeation profiles were established and the parameters Tlag and flux values were calculated. In this ex-vivo study, the flux values were 0.35 μgcm(-2)h(-1) for Pentravan and 1.22 μgcm(-2)h(-1) for LMOG organogel, corresponding respectively to 7.9 % and 29.3 % of enrofloxacin absorbed after 120 h by these formulations. The lag time (T lag) of Pentravan and organogel were 6.32 and 0.015 h respectively. The absorption time to reach the antibiotic concentration of enrofloxacin (2 μgmL(-1)) in the receptor was 60 h with Pentravan and 30 h with the organogel, suggesting more effective treatment by the latter. Enrofloxacin contained in organogel could be absorbed through pig ear skin 3.7 times greater than that in Pentravan (commercial formulation). This study demonstrates the perspective of organogel formulations as potential drug delivery systems.

摘要

本研究的目的是调查恩诺沙星从两种基质制剂(Pentravan乳膏和LMOG有机凝胶)中的经皮吸收情况。在猪耳皮肤上进行了体外实验。使用Franz扩散池测量并比较了两种含5 wt%恩诺沙星制剂透过猪皮的经皮渗透情况。在长达120小时的适当时间间隔内,采集扩散样品并使用HPLC分析方法进行分析。建立了渗透曲线,并计算了参数滞后时间(Tlag)和通量值。在这项体外研究中,Pentravan的通量值为0.35 μgcm(-2)h(-1),LMOG有机凝胶的通量值为1.22 μgcm(-2)h(-1),分别对应于这些制剂在120小时后吸收的恩诺沙星的7.9%和29.3%。Pentravan和有机凝胶的滞后时间(T lag)分别为6.32小时和0.015小时。达到受体中恩诺沙星抗生素浓度(2 μgmL(-1))的吸收时间,Pentravan为60小时,有机凝胶为30小时,这表明后者的治疗效果更佳。有机凝胶中含有的恩诺沙星透过猪耳皮肤的吸收量比Pentravan(市售制剂)高3.7倍。本研究证明了有机凝胶制剂作为潜在药物递送系统的前景。

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