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含有利福平的复乳剂

Multiple emulsions containing rifampicin.

作者信息

Khopade A J, Jain N K

机构信息

Department of Pharmaceutical Sciences, Dr. Harisingh Gour University, Sagar, India.

出版信息

Pharmazie. 1999 Dec;54(12):915-9.

Abstract

A stable multiple emulsion containing rifampicin in the internal aqueous phase was prepared by the incorporation of additives in both aqueous and oily phases. The formulation and process variables were optimized for primary and secondary emulsification. Drug release studies were performed on selected multiple emulsions to observe the effect of dilution. The release data were fitted to the Higuchi equation for slab and spherical geometry and effective diffusion coefficients were calculated. Stability studies for three months revealed good stability of the multiple emulsions with respect to creaming, phase separation, viscosity change, drug leakage, change in droplet size upon storage and exposure to osmotic and shear stress. The in vivo studies performed with stable multiple emulsions administered orally in human volunteers showed prolonged plasma drug levels. The multiple emulsions were found suitable for an improved tuberculosis therapy.

摘要

通过在水相和油相中加入添加剂,制备了一种内部水相中含有利福平的稳定多重乳液。对一级和二级乳化的配方和工艺变量进行了优化。对选定的多重乳液进行了药物释放研究,以观察稀释的影响。将释放数据拟合到平板和球形几何形状的Higuchi方程,并计算有效扩散系数。为期三个月的稳定性研究表明,多重乳液在乳析、相分离、粘度变化、药物泄漏、储存时液滴大小变化以及暴露于渗透压和剪切应力方面具有良好的稳定性。在人类志愿者中口服稳定多重乳液进行的体内研究显示血浆药物水平延长。发现多重乳液适用于改进的结核病治疗。

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