A new solid self-microemulsifying formulation prepared by spray-drying to improve the oral bioavailability of poorly water soluble drugs

Tao Yi, Jiangling Wan, Huibi Xu, Xiangliang Yang

研究成果: Article同行評審

192 引文 斯高帕斯(Scopus)

摘要

The objectives of the present work were, first, to develop a new solid self-microemulsifying drug delivery system (SMEDDS) for oral poorly water-soluble drugs such as nimodipine; and second, to evaluate its oral bioavailability in healthy rabbits. The liquid SMEDDS consisted of ethyl oleate, Labrasol®, Cremophor® RH 40 and nimodipine. The solid SMEDDS was prepared by spray-drying the liquid SMEDDS in a laboratory spray dryer, using dextran as solid carrier. The imaging of TEM and photo correlation spectroscopy revealed no difference in the droplet size of reconstituted microemulsion between both SMEDDS. Solid state characterization of the solid SMEDDS was performed by SEM, DSC, and X-ray powder diffraction. The same dose of nimodipine in the solid SMEDDS and in the liquid SMEDDS resulted in similar AUC and Cmax values, but the maximum absorption was retarded by the solid SMEDDS. AUC and Cmax after oral administration of the solid SMEDDS were 2.6- and 6.6-fold higher, respectively, compared with those of the conventional tablet. These results demonstrate that the solid SMEDDS may preserve an improved bioavailability with releasing microemulsion lipid droplets from the formulation in vivo. Thus, this solid self-microemulsifying system may provide a useful solid dosage form for oral poorly water-soluble drugs.

原文English
頁(從 - 到)439-444
頁數6
期刊European Journal of Pharmaceutics and Biopharmaceutics
70
發行號2
DOIs
出版狀態Published - 10月 2008
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