Effect of external factors on the curcumin/2-hydroxypropyl-尾-cyclodextrin: in vitro and in vivo study
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- 作者：Hui-Zi Ouyang (13)
Ling Fang (1)
Lin Zhu (3)
Lei Zhang (2)
Xiao-Liang Ren (1)
Jun He (3)
Ai-Di Qi (1) qiaidi_tcm@163.com - 关键词：Cyclodextrin – ; Curcumin – ; Phase solubility – ; Stability – ; Pharmacokinetics
- 刊名：Journal of Inclusion Phenomena and Macrocyclic Chemistry
- 出版时间：August 2012
- 出版年：2012
- 期刊代码：19_09230750
- 类别：soc
- 卷：73
- 期：1-4
- 页码：423-433
- 数据来源：sp
摘要
The effect of 2-hydroxypropyl-β-cyclodextrin (HPβCD) on solubility, stability and oral bioavailability of curcumin by external factors adjustment, was investigated with an aim of a simple, stable and effective formulation. The phase solubility studies showed the solubility of curcumin increased slightly with increasing pH. However, the apparent stability constant (K S) were found to decrease with increasing pH from 1.29 脳 104 M−1 at pH 3.0 to 5.22 脳 103 M−1 at pH 7.0. The thermodynamic parameters were calculated for inclusion complex formation in aqueous solution. Interestingly, it could be concluded that the degrees of curcumin stability improved by HPβCD grew with increasing drug–cyclodextrin binding ability. Furthermore, in vivo study not only revealed that the bioavailability of curcumin after oral administration to rats was significantly improved by curcumin/HPβCD inclusion complex, but also showed more dramatic changes in the plasma concentration–time curve (1752.76–866.70 ng mL−1 h) and the peak plasma concentration (370.10–178.11 ng mL−1) of drug by formation of complexes in pH 3–7 solution.