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用于治疗甲癣的盐酸特比萘芬指甲油:制剂、表征及体外评价

Terbinafine hydrochloride nail lacquer for the management of onychomycosis: formulation, characterization and in vitro evaluation.

作者信息

Thatai Purva, Sapra Bharti

机构信息

Department of Pharmaceutical Sciences, Pharmaceutics Division, Punjabi University, Patiala, 147002, India.

出版信息

Ther Deliv. 2018 Feb;9(2):99-119. doi: 10.4155/tde-2017-0069.

Abstract

AIM

The present investigation's intention was to develop an optimized nail lacquer (NL) for the management of onychomycosis.

MATERIALS & METHODS: The NL was optimized statistically adopting 3 full factorial design having different polymer ratios and solvent ratios. The formulations were assessed for drug permeation drying time and peak adhesive strength of the film. Characterization was done using techniques including attenuated total reflectance-Fourier transform infrared spectroscopy (ATR-FTIR), scanning electron microscopy (SEM), differential scanning calorimetry (DSC), x-ray diffraction (XRD), etc.

RESULTS & CONCLUSION: The formulation that had 1:1 polymer ratio and 80:20 solvent ratio was chosen as the optimized formulation. In vitro permeation studies showed better penetration (∼3.25-fold) as well as retention (∼11-fold) of the optimized NL formulation in the animal hoof as compared with the commercial formulation. The findings of in vitro and ex vivo studies elucidated the potential of the optimized formulation. [Formula: see text].

摘要

目的

本研究旨在开发一种用于治疗甲癣的优化指甲油(NL)。

材料与方法

采用具有不同聚合物比例和溶剂比例的3因素全因子设计对NL进行统计学优化。对制剂进行药物渗透、干燥时间和膜的峰值粘附强度评估。使用衰减全反射傅里叶变换红外光谱(ATR-FTIR)、扫描电子显微镜(SEM)、差示扫描量热法(DSC)、X射线衍射(XRD)等技术进行表征。

结果与结论

选择聚合物比例为1:1、溶剂比例为80:20的制剂作为优化制剂。体外渗透研究表明,与市售制剂相比,优化后的NL制剂在动物蹄中的渗透性更好(约3.25倍)以及滞留性更好(约11倍)。体外和离体研究结果阐明了优化制剂的潜力。[公式:见正文]

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