Enhanced oral bioavailability of dexibuprofen by a novel solid Self-emulsifying drug delivery system (SEDDS)

被引:307
作者
Balakrishnan, Prabagar [1 ]
Lee, Beom-Jin [2 ]
Oh, Dong Hoon [1 ]
Kim, Jong Oh [1 ]
Hong, Myung Ja [1 ]
Jee, Jun-Pil [3 ]
Kim, Jung Ae [1 ]
Yoo, Bong Kyu [1 ]
Woo, Jong Soo [1 ]
Yong, Chul Soon [1 ]
Choi, Han-Gon [1 ]
机构
[1] Yeungnam Univ, Coll Pharm, Kyongsan 712749, South Korea
[2] Kangwon Natl Univ, Coll Pharm, Chunchon, South Korea
[3] Seoul Natl Univ, Coll Pharm, Seoul, South Korea
关键词
Poorly water-soluble drugs; Self-emulsifying systems; Spray drying; Solid dosage form; Bioavailability; MICROEMULSIFYING FORMULATION; ABSORPTION ENHANCEMENT; INTESTINAL-ABSORPTION; DOSAGE FORM; IBUPROFEN; MECHANISMS; S(+)-IBUPROFEN; RELEASE;
D O I
10.1016/j.ejpb.2009.03.001
中图分类号
R9 [药学];
学科分类号
100702 [药剂学];
摘要
The main objective of this study was to prepare a solid form of lipid-based self-emulsifying drug delivery system (SEDDS) by spray drying liquid SEDDS with all inert solid carrier Aerosil 200 to improve the oral bioavailability of poorly water-soluble drug dexibuprofen. The liquid SEDDS was a system that consisted of dexibuprofen, Labrasol, Capryol 90 and Labrafil M 1944 CS. The particle size analysis revealed no difference in the z-average particle diameter of the reconstituted emulsion between liquid and solid SEDDS. The solid SEDDS was characterized by SEK DSC and XRD studies. In vivo results of solid SEDDS and dexibuprofen powder in rats at the dose of 10 mg/kg showed that the initial plasma concentrations of drug in solid SEDDS were significantly higher than those of dexibuprofen powder (P < 0.05). The solid SEDDS gave significantly higher AUC and Cmax than did dexibuprofen powder (P < 0.05). Ill Particular, the AUC of solid SEDDS was about twofold higher than that of dexibuprofen powder. Our results Suggested that this solid SEDDS Could be used as all effective oral solid dosage form to improve the bioavailability of poorly water-soluble drug dexibuprofen. (C) 2009 Elsevier B.V. All rights reserved.
引用
收藏
页码:539 / 545
页数:7
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