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一种新型固体分散体系统提高姜黄素的口服生物利用度

Enhancement of Oral Bioavailability of Curcumin by a Novel Solid Dispersion System.

作者信息

Hu Liandong, Shi Yanjing, Li Jian Heng, Gao Na, Ji Jing, Niu Feng, Chen Queting, Yang Xiaoning, Wang Shaocheng

机构信息

School of Pharmaceutical Sciences, Hebei University, No. 180, WuSi Road, Baoding, 071002, People's Republic of China.

Key Laboratory of Pharmaceutical Quality Control of Hebei Province, Hebei University, Baoding, People's Republic of China.

出版信息

AAPS PharmSciTech. 2015 Dec;16(6):1327-34. doi: 10.1208/s12249-014-0254-0. Epub 2015 Mar 25.

Abstract

The objective of this study was to improve the solubility and bioavailability of curcumin by a new curcumin dripping pills (Cur-DPs) formulation using melt mixing methods. The optimal formulation consisted of Polyethoxylated 40 hydrogenated castor oil (Cremophor RH40), Poloxamer 188, and Polyethylene glycol 4000 (PEG 4000). Differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and Fourier-transform infrared spectroscopy (FT-IR) were used to verify the forming of Cur-DPs. All the physical characterization information proved the formation of Cur-DPs, and the results demonstrated the superiority of the dripping pills in dissolution rates. The pharmacokinetic study of Cur-DPs was performed in rats compared to the pure curcumin suspension. The oral bioavailability of poorly water-soluble curcumin was successfully improved by CUR-DPs. And the stability of prepared Cur-DP was also in a good state in 3 months. These results identified the Cur-DPs was an effective new approach for pharmaceutical application.

摘要

本研究的目的是通过使用熔融混合方法的新型姜黄素滴丸(Cur-DPs)制剂来提高姜黄素的溶解度和生物利用度。最佳配方由聚乙氧基化氢化蓖麻油40(Cremophor RH40)、泊洛沙姆188和聚乙二醇4000(PEG 4000)组成。采用差示扫描量热法(DSC)、粉末X射线衍射法(PXRD)和傅里叶变换红外光谱法(FT-IR)来验证Cur-DPs的形成。所有物理表征信息都证明了Cur-DPs的形成,结果表明滴丸在溶出速率方面具有优越性。与纯姜黄素悬浮液相比,在大鼠中进行了Cur-DPs的药代动力学研究。水溶性差的姜黄素的口服生物利用度通过CUR-DPs成功提高。并且制备的Cur-DP在3个月内的稳定性也良好。这些结果表明Cur-DPs是一种有效的药物应用新方法。

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