Enhanced oral bioavailability of dexibuprofen by a novel solid Self-emulsifying drug delivery system (SEDDS)
Enhanced oral bioavailability of dexibuprofen by a novel solid Self-emulsifying drug delivery system (SEDDS)
复制标题
DOI：
10.1016/j.ejpb.2009.03.001
复制
发表时间：
2009-08-01
影响因子：
4.9
通讯作者：
Choi, Han-Gon
中科院分区：
文献类型：
--
作者：
Balakrishnan, Prabagar;Lee, Beom-Jin;Choi, Han-Gon
本研究的主要目的是通过喷雾干燥液体SEDDS和全惰性固体载体Aerosil 200来制备固体形式的脂质自乳化药物递送系统(SEDDS)，以提高难溶性药物右布洛芬的口服生物利用度。液体SEDDS是由右布洛芬、Labrasol、Capryol 90和Labrafil M 1944 CS组成的系统。粒度分析显示液体和固体 SEDDS 重构乳液的 z 平均粒径没有差异。通过 SEK DSC 和 XRD 研究对固体 SEDDS 进行了表征。固体SEDDS和右布洛芬粉末在10 mg/kg剂量下的大鼠体内结果显示，固体SEDDS中药物的初始血浆浓度显着高于右布洛芬粉末（P < 0.05）。固体 SEDDS 的 AUC 和 Cmax 显着高于右布洛芬粉末 (P < 0.05)。特别地，固体SEDDS的AUC比右布洛芬粉末的AUC高约两倍。我们的结果表明，这种固体SEDDS可以用作所有有效的口服固体剂型，以提高难溶性药物右布洛芬的生物利用度。 (C) 2009 Elsevier B.V. 保留所有权利。
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.