Enhancement of solubility, dissolution and Bioavailability of ibuprofen in solid dispersion systems

被引:57
作者
Newa, Madhuri [1 ]
Bhandari, Krishna Hari [1 ]
Kim, Jong Oh [1 ]
Im, Jong Seob [1 ]
Kim, Jung Ae [1 ]
Yoo, Bong Kyu [1 ]
Woo, Jong Soo [1 ]
Choi, Han Gon [1 ]
Yong, Chul Soon [1 ]
机构
[1] Yeungnam Univ, Coll Pharm, Kyongsan 712749, South Korea
关键词
ibuprofen; solid dispersion; polyethylene glycol 8000; solubility; dissolution; bioavailability;
D O I
10.1248/cpb.56.569
中图分类号
R914 [药物化学];
学科分类号
100701 [药物化学];
摘要
To improve its solubility, dissolution, and bioavailability; Ibuprofen-polyethylene glycol 8000 (PEG 8000) solid dispersions (SDs) with different drug loadings were prepared, characterized by scanning electron microscopy (SEM) and differential scanning calorimetry(DSC), and evaluated for solubility, in-vitro release, and oral bioavailability of ibuprofen in rats. Loss of individual surface properties during melting and solidification as revealed by SENT micrographs indicated the formation of effective SDs. Absence or shifting towards the lower melting temperature of the drug peak in SDs and physical mixtures in DSC study indicated the possibilities of drug-polymer interactions. Quicker release of ibuprofen from SDs in rat intestine resulted in a significant increase in AUC and C-max, and a significant decrease in T-max over pure ibuprofen. Preliminary results of this study suggested that the preparation of ibuprofen SDs using PEG 8000 as a meltable hydrophilic polymer carrier could be a promising approach to improve solubility, dissolution and bioavailability of ibuprofen.
引用
收藏
页码:569 / 574
页数:6
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