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基于羟丙甲纤维素的载缬沙坦喷雾干燥乳液的口服吸收。

Oral absorption of a valsartan-loaded spray-dried emulsion based on hydroxypropylmethyl cellulose.

机构信息

College of Pharmacy, Kyungsung University, Daeyeon-dong, Nam-gu, Busan 608-736, Republic of Korea.

College of Pharmacy, Chungnam National University, 220 Gung-dong, Yuseong-gu, Daejeon 305-764, Republic of Korea.

出版信息

Int J Biol Macromol. 2014 Aug;69:222-8. doi: 10.1016/j.ijbiomac.2014.05.059. Epub 2014 May 28.

Abstract

The aim of this study was to develop a novel valsartan-loaded spray-dried emulsion based on hydroxypropylmethyl cellulose (HPMC) with enhanced oral absorption. The valsartan-loaded redispersible dry emulsion was prepared by using a high-pressure homogenization and spray-drying process with water, Capryol 90, HPMC, and different surfactants, based on the results of the solubility study. The spray-dried emulsions formed small and homogeneous emulsions with a mean droplet emulsion size ranging from 133.5 to 152.5nm at the dispersion state in water. The valsartan-loaded redispersible dry emulsion with HPMC/poloxamer 407 showed enhanced pH-independent valsartan release, resulting in a dramatically enhanced oral bioavailability of valsartan compared to the raw material and commercial product. Therefore, a formulation strategy using the redispersible dry emulsion with HPMC/poloxamer 407 is very effective for the development of a new dosage form containing valsartan.

摘要

本研究旨在开发一种基于羟丙甲纤维素(HPMC)的新型缬沙坦载喷雾干燥乳液,以增强口服吸收。根据溶解度研究的结果,使用高压匀化和喷雾干燥工艺,以水、Capryol 90、HPMC 和不同的表面活性剂制备缬沙坦载可再分散干乳液。喷雾干燥乳液在水中的分散状态下形成小而均匀的乳液,平均乳液粒径为 133.5-152.5nm。含有 HPMC/泊洛沙姆 407 的缬沙坦载可再分散干乳液表现出增强的 pH 独立缬沙坦释放,与原料药和市售产品相比,显著提高了缬沙坦的口服生物利用度。因此,使用 HPMC/泊洛沙姆 407 的可再分散干乳液的配方策略对于开发含有缬沙坦的新剂型非常有效。

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