Irbesartan drug formulated as nanocomposite particles for the enhancement of the dissolution rate--颗粒学报PARTICUOLOGY

Zhang, Z., Le, Y., Wang, J., Zhao, H., & Chen, J. (2012). Irbesartan drug formulated as nanocomposite particles for the enhancement of the dissolution rate. Particuology, 10(4), 462–467. https://doi.org/10.1016/j.partic.2012.01.002

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

Zhiliang Zhang ^a, Yuan Le ^a, Jiexin Wang ^a, Hong Zhao ^a, Jianfeng Chen ^{a b *}

a State Key Laboratory of Organic–Inorganic Composites, Beijing University of Chemical Technology, Beijing 100029, China
b Research Center of the Ministry of Education for High Gravity Engineering and Technology, Beijing University of Chemical Technology, Beijing 100029, China

10.1016/j.partic.2012.01.002

Volume 10, Issue 4, August 2012, Pages 462-467

Received 21 July 2011, Revised 9 October 2011, Accepted 20 January 2012, Available online 18 April 2012.

E-mail: chenjf@mail.buct.edu.cn

Highlights

► IBS composite nanoparticles were prepared by using PVP/SDS as the stabilizer.

► PVP/SDS could significantly decrease the particle size to 55 nm.

► The stability of drug nanoparticles is greatly enhanced by PVP/SDS.

► The composite nanoparticles showed a significant enhancement in dissolution rate.

Abstract

Irbesartan (IBS), an angiotensin II receptor antagonist, is a poorly water-soluble drug. To enhance the dissolution 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 approximately 55 nm. In the dissolution test, the IBS nanocomposite particles showed a significantly enhanced dissolution rate and 100% of the drug dissolved within 20 min. In contrast, the physical mixture with the same recipe as the IBS nanocomposite particles and the raw IBS reached only 8% and 40% of drug dissolved in 20 min, respectively, and both of them did not dissolve completely, even after 120 min.

Graphical abstract

Keywords

Irbesartan; Composite particles; Stabilizer; Dissolution rate

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