Development of novel ibuprofen-loaded solid dispersion with improved bioavailability using aqueous solution

被引:28
作者
Park, Young-Joon [2 ]
Kwon, Ram [1 ]
Quan, Qi Zhe [3 ]
Oh, Dong Hoon [1 ]
Kim, Jong Oh [1 ]
Hwang, Ma Ro [1 ]
Koo, Yoon Bon [2 ]
Woo, Jong Soo [1 ]
Yong, Chul Soon [2 ]
Choi, Han-Gon [1 ]
机构
[1] Yeungnam Univ, Coll Pharm, Kyongsan 712749, South Korea
[2] Samil Pharmaceut Co Ltd, Res Ctr, Ansan 425852, South Korea
[3] Beijing Union Univ, Biochem Engn Coll, Beijing 100023, Peoples R China
关键词
Solid dispersion; Ibuprofen; Solubility; Pharmacokinetics; ENHANCEMENT; DISSOLUTION; FORMULATION; AGGLOMERATION; POLOXAMER-188; SOLUBILITY; RELEASE; COMPLEX; RATS;
D O I
10.1007/s12272-009-1516-3
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
To develop a novel ibuprofen-loaded solid dispersion with enhanced bioavailability, various ibuprofen-loaded solid dispersions were prepared with water, HPMC and poloxamer. The effect of HPMC and poloxamer on aqueous solubility of ibuprofen was investigated. The dissolution and bioavailability of solid dispersion in rats were then evaluated compared to ibuprofen powder. When the amount of carrier increased with a decreased in HPMC/poloxamer ratio, the aqueous solubility of ibuprofen was elevated. The solid dispersion composed of ibuprofen/HPMC/poloxamer at the weight ratio of 10:3:2 improved the drug solubility approximately 4 fold. It gave significantly higher initial plasma concentration, AUC and Cmax of drug than did ibuprofen powder in rats. The solid dispersion improved the bioavailability of drug about 4-fold compared to ibuprofen powder. Thus, this ibuprofen-loaded solid dispersion with water, HPMC and poloxamer was a more effective oral dosage form for improving the bioavailability of poor water-soluble ibuprofen.
引用
收藏
页码:767 / 772
页数:6
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