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用于鼻内给药的奥氮平纳米乳剂的制备与表征

Formulation and characterization of nanoemulsion of olanzapine for intranasal delivery.

作者信息

Kumar Mukesh, Misra Ambikanandan, Pathak Kamla

机构信息

Rajiv Academy for Pharmacy, NH #2, Mathura-281001, Uttar Pradesh, India.

出版信息

PDA J Pharm Sci Technol. 2009 Nov-Dec;63(6):501-11.

Abstract

The objective was to formulate an olanzapine nanoemulsion that could potentially deliver the drug directly to the brain following intranasal administration. The nanoemulsions were prepared using the water titration method. The mucoadhesive character was imparted by the addition of 0.5%w/w chitosan and 0.5%w/w polycarbophil and was characterized for drug content, pH, percentage transmittance, globule size, zeta potential, and PDI. The composition (%w/w) of the optimized olanzapine nanoemulsion was capmul MCM, tween 80, and a mixture of 1:1 ratio of polyethylene glycol 400 and ethanol, and aqueous phase in a ratio of 15:35:17.5:32.5. The optimized olanzapine nanoemulsion exhibited a high diffusion coefficient and no nasal cilio-toxicity. The drug release followed the Higuchi model. The optimized nanoemulsions were found to be stable for 3 months.

摘要

目的是制备一种奥氮平纳米乳剂,使其在鼻内给药后有可能将药物直接递送至大脑。采用水相滴定法制备纳米乳剂。通过添加0.5%w/w的壳聚糖和0.5%w/w的聚卡波非赋予其粘膜粘附特性,并对药物含量、pH值、透光率百分比、球粒大小、zeta电位和多分散指数进行了表征。优化后的奥氮平纳米乳剂的组成(%w/w)为辛酸癸酸甘油三酯、吐温80以及聚乙二醇400与乙醇按1:1比例混合的混合物,与水相的比例为15:35:17.5:32.5。优化后的奥氮平纳米乳剂表现出高扩散系数且无鼻纤毛毒性。药物释放遵循 Higuchi 模型。发现优化后的纳米乳剂在3个月内稳定。

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