Characterization and Pharmacokinetic Study of Aprepitant Solid Dispersions with Soluplus®

Molecules

Jinwen Liu²  Meijuan Zou²  Hongyu Piao²  Yi Liu²  Bo Tang²  Ying Gao²  Ning Ma²  Gang Cheng¹  Thomas Rades²  Holger Grohganz² 

[1] Department of Pharmacy, Shenyang Pharmaceutical University, No. 103 Wenhua Road, Shenyang 110016, China;

关键词: aprepitant;    Soluplus^®;    solid dispersions;   

DOI  :  10.3390/molecules200611345

来源: mdpi

【 摘 要 】

Solid dispersions are a useful approach to improve the dissolution rate and bioavailability of poorly water-soluble active pharmaceutical ingredients (APIs). The aim of this study was to improve the physicochemical properties and bioavailability of a poorly water-soluble aprepitant by preparation of solid dispersions. The solid dispersions were characterized by dissolution, FTIR, XRPD, DSC, SEM and pharmacokinetic studies in rats. The dissolution rate of the aprepitant was significantly increased by solid dispersions, and XRD, DSC, and SEM analysis indicated that the aprepitant existed in an amorphous form within the solid dispersions. The result of dissolution study showed that the dissolution rate of SDs was nearly five-fold faster than aprepitant. FTIR spectrometry suggested the presence of intermolecular hydrogen bonds between the aprepitant and polymer. Pharmacokinetic studies in rats indicated that the degree drug absorption was comparable with that of Emend^®. Aprepitant exists in an amorphous state in solid dispersions and the solid dispersions can markedly improve the dissolution and oral bioavailability of the aprepitant. The AUC_0–t of the SDs was 2.4-fold that of the aprepitant. In addition, the method and its associated techniques are very easy to carry out.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.