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脂质纳米乳剂作为包衣剂的新应用,可实现片剂中亲水性药物的零级释放。

A new application of lipid nanoemulsions as coating agent, providing zero-order hydrophilic drug release from tablets.

作者信息

Anton Nicolas, de Crevoisier Astrid, Schmitt Sabrina, Vandamme Thierry

机构信息

Faculty of Pharmacy, University of Strasbourg, 74 route du Rhin, BP 60024, 67401 Illkirch Cedex, France.

出版信息

J Drug Deliv. 2012;2012:271319. doi: 10.1155/2012/271319. Epub 2012 Jan 9.

Abstract

The objective of the present investigation was to evaluate potential of nanoemulsions as a coating material for the tablets. The nanoemulsion of size less than 100 nm was prepared using a simple and low-energy spontaneous emulsification method. Conventional tablets containing theophylline as a model hydrophilic drug were prepared. The theophylline tablets were coated with the nanoemulsion using a fluid bed coater. The effect of different levels of the nanoemulsion coating on the theophylline release was evaluated. The theophylline tablets containing different levels of the nanoemulsion coating could be successfully prepared. Interestingly, the coating of tablet with the nanoemulsion resulted in zero-order release of theophylline from the tablets. The noncoated theophylline tablets release the entire drug in less than 2 minutes, whereas nanoemulsion coating delayed the release of theophylline from tablets. This investigation establishes the proof of concept for the potential of nanoemulsions as a coating material for tablets.

摘要

本研究的目的是评估纳米乳剂作为片剂包衣材料的潜力。采用简单的低能量自发乳化法制备了粒径小于100nm的纳米乳剂。制备了含有茶碱作为模型亲水药物的常规片剂。使用流化床包衣机用纳米乳剂对茶碱片剂进行包衣。评估了不同水平的纳米乳剂包衣对茶碱释放的影响。成功制备了含有不同水平纳米乳剂包衣的茶碱片剂。有趣的是,用纳米乳剂包衣片剂导致茶碱从片剂中呈零级释放。未包衣的茶碱片剂在不到2分钟内释放出全部药物,而纳米乳剂包衣延迟了茶碱从片剂中的释放。本研究为纳米乳剂作为片剂包衣材料的潜力建立了概念验证。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ed9f/3261482/bd3bff15b096/JDD2012-271319.004.jpg

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