Co-carrier-based solid dispersion of celecoxib improves dissolution rate and oral bioavailability in rats

溶解 生物利用度 化学 有机化学 医学 药理学
作者
Phuong Tran,Thu Nhan Nguyen,Jeong‐Sook Park
出处
期刊:Journal of Drug Delivery Science and Technology [Elsevier BV]
卷期号:79: 104073-104073 被引量:6
标识
DOI:10.1016/j.jddst.2022.104073
摘要

This study aimed to prepare a co-carrier-based solid dispersion (SD) of celecoxib (CXB) to improve its dissolution and oral bioavailability. The CXB-loaded SD formulation was prepared using CXB, pol407, Aerosil 200, and Eudragit L100 at a weight ratio of 1:3:1.5:1. PXRD, DSC, and FTIR analyses were conducted to evaluate the structural behavior and interactions between the drug and carrier. The dissolution profile was studied to demonstrate superior CXB dissolution capacity of CXB-SD than that of the physical mixture and raw CXB, and the results showed that the dissolution efficiency (%) of optimized CXB-SD significantly (P < 0.05) increased compared to that of raw CXB. The mean dissolution times of CXB-SD at pH 1.2 and 6.8 were reduced by 2.4-fold and 2.5-fold, respectively, compared to that of raw CXB. The dissolution of CXB-SD fitted well with the zero-order model. The preparation of the CXB-SD formulation improved the bioavailability of CXB, as demonstrated by the increased AUClast (1.88-fold) and Cmax (2.24-fold) of CXB-SD compared to that of raw CXB. In conclusion, these results indicate that SDs can enhance the dissolution and oral bioavailability of poorly water-soluble CXB.

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