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木葡聚糖微球干粉吸入剂的制备、表征及肺部药代动力学研究。

Preparation, characterization and pulmonary pharmacokinetics of xyloglucan microspheres as dry powder inhalation.

机构信息

R.C. Patel Institute of Pharmaceutical Education and Research Shirpur, Dist Dhule, India.

R.C. Patel Institute of Pharmaceutical Education and Research Shirpur, Dist Dhule, India.

出版信息

Carbohydr Polym. 2014 Feb 15;102:529-36. doi: 10.1016/j.carbpol.2013.11.036. Epub 2013 Dec 4.

Abstract

The purpose of the present investigation was to prepare microspheres using xyloglucan as the polymer and to evaluate them for pulmonary delivery of Montelucast. Xyloglucan microspheres were prepared using spray-drying technique employing lactose monohydrate as carrier for dry powder inhalation. The formulation of microspheres was optimized using response surface methodology. Multiple response surface simultaneous optimizations using desirability approach were use to find optimal formulation. In vitro characterization of optimized microsphere formulation demonstrates its suitability as dry powder inhalation. It found to provide high and prolonged drug concentration within lungs after pulmonary administration in animal model.

摘要

本研究旨在制备以木葡聚糖为聚合物的微球,并评估其在孟鲁司特肺部给药中的应用。采用喷雾干燥技术,以乳糖一水合物为载体,制备木葡聚糖微球,用于干粉吸入。采用响应面法优化微球的配方。采用理想性方法对多响应面进行同步优化,以找到最佳配方。优化后的微球配方的体外特性表明其适合作为干粉吸入剂。在动物模型中,肺部给药后发现其能在肺部提供高且持久的药物浓度。

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