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Molecules 2015, 20(6), 10705-10720; doi:10.3390/molecules200610705

Preparation, Characterization and Pharmacokinetic Study of Xiangfu Siwu Decoction Essential Oil/β-Cyclodextrin Inclusion Complex

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Jiangsu Key Laboratory for High Technology Research of Traditional Chinese Medicine Formulae, Nanjing University of Chinese Medicine, Nanjing 210023, China
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Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources Industrialization, Nanjing University of Chinese Medicine, Nanjing 210023, China
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Authors to whom correspondence should be addressed.
Academic Editor: Maria Emília Sousa
Received: 12 May 2015 / Revised: 5 June 2015 / Accepted: 5 June 2015 / Published: 10 June 2015
(This article belongs to the Section Natural Products)
View Full-Text   |   Download PDF [1752 KB, uploaded 10 June 2015]   |  

Abstract

Xiang-Fu-Si-Wu Decoction (XFSWD), a famous Chinese herbal formula, is considered an effective prescription for treating primary dysmenorrhea. The essential oil is a significant effective ingredient of XFSWD. However, its volatility, instability and poor water-solubility influence its pharmacodynamic effects. β-Cyclodextrin (β-CD) has the intrinsic ability to form specific inclusion complexes with such drugs to enhance their stability, solubility and bioavailability. The aim of this study was thus to compare the pharmacokinetic characteristics and the oral bioavailability of XFSWD essential oil (XEO) and its β-CD inclusion complex after oral administration to rats. A simple, rapid, and sensitive ultra-high performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) method was developed for the simultaneous quantification of five active components of XEO in rat plasma. The in vivo data showed that XEO/β-CD inclusion complex displayed higher maximum plasma concentration (Cmax), longer half-time (T1/2) and bigger area under the concentration-time curve (AUC0–24 h). These results demonstrated that the formation of β-CD inclusion complex has significantly increased the oral bioavailability of the drugs in rats than free oil. View Full-Text
Keywords: Xiangfu Siwu decoction; essential oil; β-cyclodextrin; inclusion complex; pharmacokinetics Xiangfu Siwu decoction; essential oil; β-cyclodextrin; inclusion complex; pharmacokinetics
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Xi, J.; Qian, D.; Duan, J.; Liu, P.; Zhu, Z.; Guo, J.; Zhang, Y.; Pan, Y. Preparation, Characterization and Pharmacokinetic Study of Xiangfu Siwu Decoction Essential Oil/β-Cyclodextrin Inclusion Complex. Molecules 2015, 20, 10705-10720.

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