纳米粒化:一种针对难溶性化合物的制剂方法。

Nanosizing: a formulation approach for poorly-water-soluble compounds.

作者信息

Merisko-Liversidge Elaine, Liversidge Gary G, Cooper Eugene R

机构信息

Elan Drug Delivery, 3500 Horizon Dr, King of Prussia, PA 19406, USA.

出版信息

Eur J Pharm Sci. 2003 Feb;18(2):113-20. doi: 10.1016/s0928-0987(02)00251-8.

Abstract

Poorly-water-soluble compounds are difficult to develop as drug products using conventional formulation techniques and are frequently abandoned early in discovery. The use of media milling technology to formulate poorly-water-soluble drugs as nanocrystalline particles offers the opportunity to address many of the deficiencies associated with this class of molecules. NanoCrystal Technology is an attrition process wherein large micron size drug crystals are media milled in a water-based stabilizer solution. The process generates physically stable dispersions consisting of nanometer-sized drug crystals. Nanocrystalline particles are a suitable delivery system for all commonly used routes of administration, i.e. oral, injectable (IV, SC, and IM) and topical applications. In addition, aqueous dispersions of nanoparticles can be post-processed into tablets, capsules, fast-melts and lyophilized for sterile product applications. The technology has been successfully incorporated into all phases of the drug development cycle from identification of new chemical entities to refurbishing marketed products for improving their performance and value.

摘要

难溶性化合物很难使用传统制剂技术开发成药品,并且在发现早期经常被放弃。使用介质研磨技术将难溶性药物制成纳米晶体颗粒为解决与这类分子相关的许多缺陷提供了机会。纳米晶体技术是一种研磨过程,其中大微米尺寸的药物晶体在水基稳定剂溶液中进行介质研磨。该过程产生由纳米尺寸药物晶体组成的物理稳定分散体。纳米晶体颗粒是适用于所有常用给药途径的给药系统,即口服、注射(静脉内、皮下和肌肉内)和局部应用。此外,纳米颗粒的水分散体可以后处理成片剂、胶囊、速溶片并冻干以用于无菌产品应用。该技术已成功应用于药物开发周期的所有阶段,从新化学实体的鉴定到翻新上市产品以提高其性能和价值。

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