title: Comparative pharmacokinetic profiles of five poorly soluble pulchinenosides in different formulations from Pulsatilla chinensis saponins extracts for enhanced bioavailability.
abstract: Pulsatilla chinensis, a traditional Chinese medicine (TCM), has been used for treating amoebic diseases, vaginal trichomoniasis and bacterial infections over a long history. Now growing attention has been attracted to its antitumor activities. The purpose of this work was to compare the pharmacokinetic profiles of pulchinenosides in different formulations and to improve their oral bioavailability. Extracts of P. chinensis saponins were prepared for PRS-Na (salt forming), PRS-HPβCD (hydroxypropyl-β-cyclodextrin inclusion complex), PRS-O/W (oil-in-water emulsion) and PRS-silica (micronization), respectively. A simpler and more durable LC-MS/MS method was developed in this study for quantitative analysis of pulsatilla sapoin D, B7, B10, B11 and sapoin PD simultaneously. The four formulations enhanced saponins oral bioavailability to varying degrees, as PRS-HPβCD > PRS-silica > PRS-O/W > PRS-Na, which indicated that water-soluble preparations can obviously improve the solubility of saponins, and are helpful to increase bioavailability. In particular, hydroxypropyl-β-cyclodextrin inclusion complex was the most effective way to promote absorption of saponins, raising the F values (bioavailability) >20 times. Therefore, P. chinensis saponin molecules can be slowly released by emulsion and micronization, which can avoid the enormous Cmax appearing in HPβCD, considering the pharmacokinetics profiles. However, appropriate pharmacokinetic parameters were observed in PRS-Na, although the F value was minimum among the four preparations.
authors.affiliation: Jiangxi University of Traditional Chinese Medicine, 56 Yangming Road, Nanchang, 330006, People's Republic of China.|The People's Hospital of Shangrao, Shuyuan Road, Shangrao, Jiangxi, 334000, People's Republic of China.
authors.forename: Jun
authors.initials: J
authors.lastname: Huang
authors.affiliation: Jiangxi University of Traditional Chinese Medicine, 56 Yangming Road, Nanchang, 330006, People's Republic of China.
authors.forename: Yali
authors.initials: Y
authors.lastname: Liu
authors.affiliation: Jiangxi University of Traditional Chinese Medicine, 56 Yangming Road, Nanchang, 330006, People's Republic of China.|The National Pharmaceutical Engineering Center for Solid Preparation in Chinese Herbal Medicine, 56 Yangming Road, Nanchang, Jiangxi, 330006, People's Republic of China.
authors.forename: Xiang
authors.initials: X
authors.lastname: Li
authors.affiliation: Jiangxi University of Traditional Chinese Medicine, 56 Yangming Road, Nanchang, 330006, People's Republic of China.|The National Pharmaceutical Engineering Center for Solid Preparation in Chinese Herbal Medicine, 56 Yangming Road, Nanchang, Jiangxi, 330006, People's Republic of China.
authors.forename: Yonggui
authors.initials: Y
authors.lastname: Song
authors.affiliation: Jiangxi University of Traditional Chinese Medicine, 56 Yangming Road, Nanchang, 330006, People's Republic of China.
authors.forename: Wei
authors.initials: W
authors.lastname: Li
authors.affiliation: Jiangxi University of Traditional Chinese Medicine, 56 Yangming Road, Nanchang, 330006, People's Republic of China.
authors.forename: Kuangyi
authors.initials: K
authors.lastname: Liu
authors.affiliation: Jiangxi University of Traditional Chinese Medicine, 56 Yangming Road, Nanchang, 330006, People's Republic of China.|The National Pharmaceutical Engineering Center for Solid Preparation in Chinese Herbal Medicine, 56 Yangming Road, Nanchang, Jiangxi, 330006, People's Republic of China.
authors.forename: Dan
authors.initials: D
authors.lastname: Su
authors.affiliation: Jiangxi University of Traditional Chinese Medicine, 56 Yangming Road, Nanchang, 330006, People's Republic of China.|The National Pharmaceutical Engineering Center for Solid Preparation in Chinese Herbal Medicine, 56 Yangming Road, Nanchang, Jiangxi, 330006, People's Republic of China.
authors.forename: Yulin
authors.initials: Y
authors.lastname: Feng
authors.affiliation: Jiangxi University of Traditional Chinese Medicine, 56 Yangming Road, Nanchang, 330006, People's Republic of China.|The National Pharmaceutical Engineering Center for Solid Preparation in Chinese Herbal Medicine, 56 Yangming Road, Nanchang, Jiangxi, 330006, People's Republic of China.
authors.forename: Shilin
authors.initials: S
authors.lastname: Yang
mesh_terms: D000818:Animals; D001682:Biological Availability; D002853:Chromatography, Liquid; D004355:Drug Stability; D004365:Drugs, Chinese Herbal / Q000008:administration & dosage; D057230:Limit of Detection; D016014:Linear Models; D018517:Plant Roots / Q000737:chemistry; D031946:Pulsatilla / Q000737:chemistry*; D051381:Rats; D017208:Rats, Wistar; D015203:Reproducibility of Results; D012503:Saponins / Q000097:blood* / Q000737:chemistry / Q000493:pharmacokinetics*; D012995:Solubility
chemical_list: D004365:Drugs, Chinese Herbal; D012503:Saponins
keywords: Pulsatilla chinensis saponins; bioavailability; pharmacokinetics; water-soluble formulations