Irbesartan drug formulated as nanocomposite particles for the enhancement of the dissolution rate  

作　　者：Zhiliang Zhang Yuan Le Jiexin wang Hong Zhao Jianfeng Chen 

机构地区：[1]State Key Laboratory of Organic-Inorganic Composites,Beijing University of Chemical Technology,Beijing 100029.China [2]Research Center of the Ministry of Education for High Gravity Engineering and Technology,Beijing University of Chemical Technology,Beijing 100029,China

出　　处：《Particuology》2012年第4期462-467,共6页颗粒学报（英文版）

基　　金：supported by the National Natural Science Foundation of China (nos. 20821004, 20806004 and 21006002);the National "863" Program of China (no.2009AA033301)

摘　　要：Irbesartan （IBS）, an angiotensin II receptor antagonist, is a poorly water-soluble drug. To enhance the dis- solution rate, IBS nanocomposite particles were produced via an anti-solvent precipitation combined with a spray drying process. Four pharmaceutically acceptable excipients, including three different polymers and one charged surfactant, were evaluated as stabilizers to control the particle size and to prevent the agglomeration of particles. The experiment results indicated that polyvinylpyrrolidone （PVP） combined with sodium dodecyl sulfate （SDS） significantly decreased the particle size and enhanced the stability of drug nanoparticles. As a result, we finally obtained stable IBS nanoparticles with an average size of approx- imately 55 nm. In the dissolution test, the IBS nanocomposite particles showed a significantly enhanced dissolution rate and 100% of the drug dissolved within 20 rain. In contrast, the physical mixture with the same recipe as the IBS nanocomposite particles and the raw 1BS reached only 8% and 40% of drug dissolved in 20 rain, respectively, and both of them did not dissolve completely, even after 120 rain.Irbesartan （IBS）, an angiotensin II receptor antagonist, is a poorly water-soluble drug. To enhance the dis- solution rate, IBS nanocomposite particles were produced via an anti-solvent precipitation combined with a spray drying process. Four pharmaceutically acceptable excipients, including three different polymers and one charged surfactant, were evaluated as stabilizers to control the particle size and to prevent the agglomeration of particles. The experiment results indicated that polyvinylpyrrolidone （PVP） combined with sodium dodecyl sulfate （SDS） significantly decreased the particle size and enhanced the stability of drug nanoparticles. As a result, we finally obtained stable IBS nanoparticles with an average size of approx- imately 55 nm. In the dissolution test, the IBS nanocomposite particles showed a significantly enhanced dissolution rate and 100% of the drug dissolved within 20 rain. In contrast, the physical mixture with the same recipe as the IBS nanocomposite particles and the raw 1BS reached only 8% and 40% of drug dissolved in 20 rain, respectively, and both of them did not dissolve completely, even after 120 rain.

关 键 词：lrbesartanComposite particlesStabilizerDissolution rate 

分 类 号：TQ460.4[化学工程—制药化工] O643.361[理学—物理化学]