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

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 pharmacodynami...

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Main Authors: Junzuan Xi, Dawei Qian, Jinao Duan, Pei Liu, Zhenhua Zhu, Jianming Guo, Yang Zhang, Ying Pan
Format: Article
Language:English
Published: MDPI AG 2015-06-01
Series:Molecules
Subjects:
Online Access:http://www.mdpi.com/1420-3049/20/6/10705
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author Junzuan Xi
Dawei Qian
Jinao Duan
Pei Liu
Zhenhua Zhu
Jianming Guo
Yang Zhang
Ying Pan
author_facet Junzuan Xi
Dawei Qian
Jinao Duan
Pei Liu
Zhenhua Zhu
Jianming Guo
Yang Zhang
Ying Pan
author_sort Junzuan Xi
collection DOAJ
description 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.
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spelling doaj.art-e14f9c195c31487a917b3f031ce7edd22022-12-22T01:33:40ZengMDPI AGMolecules1420-30492015-06-01206107051072010.3390/molecules200610705molecules200610705Preparation, Characterization and Pharmacokinetic Study of Xiangfu Siwu Decoction Essential Oil/β-Cyclodextrin Inclusion ComplexJunzuan Xi0Dawei Qian1Jinao Duan2Pei Liu3Zhenhua Zhu4Jianming Guo5Yang Zhang6Ying Pan7Jiangsu Key Laboratory for High Technology Research of Traditional Chinese Medicine Formulae, Nanjing University of Chinese Medicine, Nanjing 210023, ChinaJiangsu Key Laboratory for High Technology Research of Traditional Chinese Medicine Formulae, Nanjing University of Chinese Medicine, Nanjing 210023, ChinaJiangsu Key Laboratory for High Technology Research of Traditional Chinese Medicine Formulae, Nanjing University of Chinese Medicine, Nanjing 210023, ChinaJiangsu Key Laboratory for High Technology Research of Traditional Chinese Medicine Formulae, Nanjing University of Chinese Medicine, Nanjing 210023, ChinaJiangsu Key Laboratory for High Technology Research of Traditional Chinese Medicine Formulae, Nanjing University of Chinese Medicine, Nanjing 210023, ChinaJiangsu Key Laboratory for High Technology Research of Traditional Chinese Medicine Formulae, Nanjing University of Chinese Medicine, Nanjing 210023, ChinaJiangsu Key Laboratory for High Technology Research of Traditional Chinese Medicine Formulae, Nanjing University of Chinese Medicine, Nanjing 210023, ChinaJiangsu Key Laboratory for High Technology Research of Traditional Chinese Medicine Formulae, Nanjing University of Chinese Medicine, Nanjing 210023, ChinaXiang-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.http://www.mdpi.com/1420-3049/20/6/10705Xiangfu Siwu decoctionessential oilβ-cyclodextrininclusion complexpharmacokinetics
spellingShingle Junzuan Xi
Dawei Qian
Jinao Duan
Pei Liu
Zhenhua Zhu
Jianming Guo
Yang Zhang
Ying Pan
Preparation, Characterization and Pharmacokinetic Study of Xiangfu Siwu Decoction Essential Oil/β-Cyclodextrin Inclusion Complex
Molecules
Xiangfu Siwu decoction
essential oil
β-cyclodextrin
inclusion complex
pharmacokinetics
title Preparation, Characterization and Pharmacokinetic Study of Xiangfu Siwu Decoction Essential Oil/β-Cyclodextrin Inclusion Complex
title_full Preparation, Characterization and Pharmacokinetic Study of Xiangfu Siwu Decoction Essential Oil/β-Cyclodextrin Inclusion Complex
title_fullStr Preparation, Characterization and Pharmacokinetic Study of Xiangfu Siwu Decoction Essential Oil/β-Cyclodextrin Inclusion Complex
title_full_unstemmed Preparation, Characterization and Pharmacokinetic Study of Xiangfu Siwu Decoction Essential Oil/β-Cyclodextrin Inclusion Complex
title_short Preparation, Characterization and Pharmacokinetic Study of Xiangfu Siwu Decoction Essential Oil/β-Cyclodextrin Inclusion Complex
title_sort preparation characterization and pharmacokinetic study of xiangfu siwu decoction essential oil β cyclodextrin inclusion complex
topic Xiangfu Siwu decoction
essential oil
β-cyclodextrin
inclusion complex
pharmacokinetics
url http://www.mdpi.com/1420-3049/20/6/10705
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