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| 1 | Effect of age on the pharmacokinetics of polymorphic nimodipine in rats after oral administration显示文摘The previous investigation has proved that their existed pharmacokinetic difference between the different crystal forms of the polymorphic drugs after oral administration.However,no systemic investigations have been made on the change of this pharmacokinetic difference,resulted either from the physiological or from the pathological factors.In this paper,we used polymorphic nimodipine(Nim) as a model drug and investigated the effect of age difference(2- and 9-month old) on the pharmacokinetics after oral delivery in rats.As the results shown,for L-form of Nim(L-Nim),the AUC0–24 hin 2-month-old rats was 343.68747.15 ng h/m L,which is 23.36% higher than that in 9-month-old rats.For H-form of Nim(H-Nim),the AUC0–24 hin 2-monthold rats was 140.91719.47 ng h/m L,which is 54.64% higher than that in 9-month-old rats.The AUC0–24 h ratio between H-Nim and L-Nim was 2.44 in 2-month-old rats and 3.06 in 9-month-old rats.Since age difference could result in unparallelled change of the absorption and bioavailability of the polymorphic drugs,the results in this experiment are of value for further investigation of crystal form selection in clinical trials and rational clinical application of the polymorphic drugs. | Wenli Liu Xiaona Wang Ruilian Chen Kaixuan Zhang Yao Li Yi Li Duanyun Si Junbo Gong Dianshu Yin Yongli Wang Zhenping Wei Mingshi Yang | 2016 | Acta Pharmaceutica Sinica B2016，6，5： | 3 |
| 2 | LC/MS/MS and radioisotope method combined for recognizing the affinity between catalpol and OCT2 transporter显示文摘越来越草药的药被发现是药 transporters 的底层。在这份报纸,与放射性同位素方法相结合的层析 / 双人脚踏车团 spectrometry (LC/MS/MS ) 被用于 catalpol 的 quantification,繁体中文药,学习在草药的药和 transporters 之间的亲密关系关系。Catalpol 举起实验被使用几 transporters (OAT1, OCT2, OAT3, OATP1B1 和 OATP2B1 ) 执行。并且样品与甲醇被猛抛并且与 LC/MS/MS 确定了。结果证明 catalpol 与 OCT2-transfected S2 房间有一种好亲密关系。在学习在 catalpol 和 14C-tetraethylammonium (茶) 之间的药药相互作用以后,我们发现 catalpol 能便于茶运输由 OCT2 调停了,建议那 catalpol 能可能是 OCT2 的一个新倡导者。 | Zhiyu ZHANG Changxiao LIU Duanyun SI Rong LU Xiulin YI | 2012 | Frontiers of Chemical Science and Engineering2012，6，4： | 1 |
| 3 | Quantitation of catal pol in rat plasma by liquid chromatography/electrospray ioni zation tandem mass spectrometry and its pharmacokinetic study显示文摘 | Lu Rong Gu Yuan Si DuanYun | 2009 | J Chromatogr B Analyt Technol Biomed Life Sci2009，877，29： | 1 |
| 4 | Absolute bioavailability,dose proportionality,and tissue distribution of rotundic acid in rats based on validated LC-QqQ-MS/MS method显示文摘Rotundic acid(RA),an ursane-type pentacyclic triterpene acid isolated from the dried barks of Ilex rotunda Thunb.(Aquifoliaceae),possesses diverse bioactivities.To further study its pharmacokinetics,a simple and sensitive liquid chromatography with triple quadrupole mass spectrometry(LC-QqQ-MS/MS)method was developed and validated to quantify RA concentration in rat plasma and tissue using etofesalamide as an internal standard(IS).Plasma and tissue samples were subjected to one-step protein precipitation.Chromatographic separation was achieved on a ZORBAX Eclipse XDB-C_(18) column(4.6mm×50mm,5μm)under gradient conditions with eluents of methanol:acetonitrile(1:1,V/V)and 5mM ammonium formate:methanol(9:1,V/V)at 0.5mL/min.Multiple reaction monitoring transitions were performed at m/z 487.30→437.30 for RA and m/z 256.10→227.10 for IS in the negative mode.The developed LC-QqQ-MS/MS method exhibited good linearity(2-500 ng/mL)and was fully validated in accordance with U.S.Food and Drug Administration bioanalytical guidelines.Dose proportionality and bioavailability in rats were determined by comparing pharmacokinetic data after single oral(10,20,and 40mg/kg)and intravenous(10mg/kg)administration of RA.Tissue distribution was studied following oral administration at 20mg/kg.The results showed that the absolute bioavailability of RA after administration at different doses ranged from 16.1%to 19.4%.RA showed good dose proportionality over a dose range of 10-40 mg/kg.RA was rapidly absorbed in a dose-dependent manner and highly distributed in the liver.In conclusion,this study is the first to systematically elucidate the absorption and distribution characteristics of RA in rats,which can provide additional information for further development and evaluation of RA in drug metabolism and pharmacokinetic studies. | Haihua Shang Xiaohan Dai Mi Li Yueyi Kai Zerong Liu Min Wang Quansheng Li Yuan Gu Changxiao Liu Duanyun Si | 2022 | Journal of Pharmaceutical Analysis2022，12，2： | 0 |
| 5 | Development of an LC–MS/MS method for the quantitation of deoxyglycychloxazol in rat plasma and its application in pharmacokinetic study显示文摘Deoxyglycychloxazol(TY501) is a glycyrrhetinic acid derivative which exhibits high anti-inflammatory activity and reduced pseudoaldosteronism compared to glycyrrhetinic acid.In this study,a sensitive and rapid liquid chromatography–tandem mass spectrometry(LC–MS/MS) method was established for the quantitation of TY501 in rat plasma.Plasma samples were treated by precipitating protein with methanol and supernatants were separated by a Symmetry C_8 column with the mobile phase consisting of methanol and 10 m M ammonium formate(containing 0.1% of formic acid)(90:10,v/v).The selected reaction monitoring(SRM) transitions were performed at m/z 647.4-191.2 for TY501 and m/z 473.3-143.3 for astragaloside aglycone(IS) in the positive ion mode with atmospheric pressure chemical ionization(APCI) source.Calibration curve was linear over the concentration range of 5–5000 ng/m L.The lower limit of quantification was 5 ng/m L.The mean recovery was over 88%.The intra- and inter-day precisions were lower than 6.0% and 12.8%,respectively,and the accuracy was within 7 1.3%.TY501 was stable under usual storage conditions and handling procedure.The validated method has been successfully applied to a pharmacokinetic study after oral administration of TY501 to rats at a dosage of 10 mg/kg. | Rongshan Li Ruixue Ran Quansheng Li Yurong Huang Yuan Gu Duanyun Si | 2016 | Journal of Pharmaceutical Analysis2016，6，3： | 0 |
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