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奈韦拉平口服纳米混悬剂的制备与表征

Preparation and characterisation of nevirapine oral nanosuspensions.

作者信息

Raju Anju, Reddy A Jagdeesh, Satheesh J, Jithan A V

机构信息

Department of Pharmaceutics, Mother Teresa College of Pharmacy, NFC Nagar, RR Dist-501 301, India.

New Drug Discovery Department, Hetero Drugs Limited (R and D), Balanagar, Hyderabad-500 018, India.

出版信息

Indian J Pharm Sci. 2014 Jan;76(1):62-71.

Abstract

The objective of this study was to prepare and characterise nevirapine nanosuspensions so as to improve the dissolution rate of nevirapine. Nevirapine is a nonnucleoside reverse transcriptase inhibitor of immunodeficiency virus type-1 and it is poorly water-soluble antiretroviral drug. The low solubility of nevirapine can lead to decreased and variable oral bioavailability. Nanosuspension can overcome the oral bioavailability problem of nevirapine. Nevirapine nanosuspensions were prepared using nanoedge method. The suspensions were stabilised using surfactants Lutrol F 127 or Poloxamer 407 and hydroxypropyl methyl cellulose. The nanosuspension was characterised for particle size, polydispersibility index, crystalline state, particle morphology, in vitro drug release and pharmacokinetics in rats after oral administration. The results support the claim for the preparation of nanosuspensions with enhanced solubility and bioavailability.

摘要

本研究的目的是制备奈韦拉平纳米混悬液并对其进行表征,以提高奈韦拉平的溶解速率。奈韦拉平是一种1型免疫缺陷病毒的非核苷类逆转录酶抑制剂,是一种水溶性较差的抗逆转录病毒药物。奈韦拉平的低溶解度会导致口服生物利用度降低且不稳定。纳米混悬液可以克服奈韦拉平的口服生物利用度问题。采用纳米边缘法制备奈韦拉平纳米混悬液。使用表面活性剂聚氧乙烯氢化蓖麻油F 127或泊洛沙姆407以及羟丙基甲基纤维素来稳定混悬液。对纳米混悬液的粒径、多分散指数、晶态、颗粒形态、体外药物释放以及大鼠口服给药后的药代动力学进行了表征。结果支持了制备具有更高溶解度和生物利用度的纳米混悬液这一说法。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/118c/4007257/df167a9d2317/IJPhS-76-62-g003.jpg

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