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利用环麦芽糊精研制新型载布洛芬固体分散体以提高生物利用度。

Development of novel ibuprofen-loaded solid dispersion with enhanced bioavailability using cycloamylose.

机构信息

Department of Food Engineering, Dankook University, Cheonan, 330-714, Korea.

出版信息

Arch Pharm Res. 2012 Mar;35(4):683-9. doi: 10.1007/s12272-012-0412-4. Epub 2012 May 3.

Abstract

To develop a novel ibuprofen-loaded solid dispersion with enhanced bioavailability using cycloamylose, it was prepared using spray-drying techniques with cycloamylose at a weight ratio of 1:1. The effect of cycloamylose on aqueous solubility of ibuprofen was investigated. The physicochemical properties of solid dispersions were investigated using scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and X-ray diffraction. The dissolution and bioavailability in rats were evaluated compared with ibuprofen powder. This ibuprofen-loaded solid dispersion improved about 14-fold drug solubility. Ibuprofen was present in an unchanged crystalline state, and cycloamylose played the simple role of a solubilizing agent in this solid dispersion. Moreover, the dispersion gave 2-fold higher AUC (area under the drug concentration-time curve) value compared with a ibuprofen powder, indicating that it improved the oral bioavailability of ibuprofen in rats. Thus, the solid dispersion may be useful to deliver ibuprofen with enhanced bioavailability without crystalline change.

摘要

为了开发一种新型的布洛芬固体分散体,以提高生物利用度,使用环麦芽七糖,通过喷雾干燥技术,以 1:1 的重量比制备。考察了环麦芽七糖对布洛芬水溶性的影响。采用扫描电子显微镜(SEM)、差示扫描量热法(DSC)和 X 射线衍射法研究了固体分散体的物理化学性质。与布洛芬粉末相比,评价了其在大鼠体内的溶解和生物利用度。这种布洛芬负载的固体分散体提高了约 14 倍的药物溶解度。布洛芬以未改变的晶态存在,而环麦芽七糖在该固体分散体中仅起到增溶作用。此外,与布洛芬粉末相比,该分散体的 AUC(药物浓度-时间曲线下面积)值提高了 2 倍,表明其提高了布洛芬在大鼠体内的口服生物利用度。因此,该固体分散体可能有助于提供具有增强生物利用度的布洛芬,而不会发生晶体变化。

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