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基于纤维素聚合物的新型米康唑硝酸盐三元混合物口腔给药凝胶的研制。

Development of cellulosic polymer based gel of novel ternary mixture of miconazole nitrate for buccal delivery.

机构信息

Herbal Medicinal Products Department, CSIR-Central Institute of Medicinal and Aromatic Plants (CSIR-CIMAP), P.O. CIMAP, Lucknow, U.P. 226015, India.

Herbal Medicinal Products Department, CSIR-Central Institute of Medicinal and Aromatic Plants (CSIR-CIMAP), P.O. CIMAP, Lucknow, U.P. 226015, India.

出版信息

Carbohydr Polym. 2014 Mar 15;103:126-33. doi: 10.1016/j.carbpol.2013.12.019. Epub 2013 Dec 14.

Abstract

Aim of the present investigation was to develop cellulosic polymer based mucoadhesive antifungal gel comprising novel ternary mixture of miconazole nitrate (MN) for buccal delivery. Crosslinking of gel was made by adjusting pH with triethanolamine (TEA) and gel formulation was optimized on the basis of flux of MN (0.562-1.751 mg/cm(2)/h) calculated from ex vivo permeation study. Based on statistically validated polynomial equation and plotted response surfaces, B17 was found to be the optimum batch. Texture profile in terms of adhesiveness (3.24 ± 0.012 g), firmness (10.83 ± 0.067 g), spreadability (3.63 ± 0.033 mJ) and extrudability (35.6 ± 0.1 mJ) of B17 was evaluated using a novel instrumental approach. The texture parameters were found to be consistent over 90 days. Ternary mixture containing gel showed broader zone of growth inhibition (32.67-47.33 mm) in comparison to marketed formulation containing pure MN (17.50-40.33 mm) against selected strains of fungi. In conclusion, consistent and effective mucoadhesive antifungal gel of MN with extended residence time in oral mucosa was developed.

摘要

本研究旨在开发一种基于纤维素聚合物的、具有黏附性的新型抗真菌口腔凝胶,其中包含硝酸咪康唑(MN)的三元混合物。通过用三乙醇胺(TEA)调节凝胶的 pH 值来实现交联,并且根据体外渗透研究中计算出的 MN 通量(0.562-1.751 mg/cm(2)/h)来优化凝胶配方。基于统计学验证的多项式方程和绘制的响应曲面,发现 B17 是最佳批次。使用新的仪器方法评估了 B17 的粘性(3.24 ± 0.012 g)、硬度(10.83 ± 0.067 g)、延展性(3.63 ± 0.033 mJ)和可挤出性(35.6 ± 0.1 mJ)的纹理参数。结果表明,B17 的纹理参数在 90 天内保持一致。与含有纯 MN 的市售制剂(17.50-40.33 mm)相比,含有凝胶的三元混合物对选定的真菌菌株显示出更宽的抑菌区(32.67-47.33 mm)。结论是,成功开发了具有黏附性且可延长在口腔黏膜中停留时间的 MN 抗真菌口腔凝胶。

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