Pharmacokinetics and Tissue Distribution of Spinosin after Intravenous Administration in Rats
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概要
- 論文の詳細を見る
Spinosin is the major effective single constituent in the traditional Chinese herb Semen Ziziphi Spinosae, which is used for sedation and hypnosis. For the further use of spinosin in treating insomnia, the pharmacokinetics and tissue distribution of spinosin after intravenous administration to rats was investigated. An HPLC method with an ODS column (250mm×4.6mm, i.d.) and a mobile phase of acetonitrile-water-acetic acid (23:77:1) was used for the determination of spinosin in the plasma and tissues of rats. Vanillin was used as an internal standard, and spinosin was detected at 334nm. The calibration curve of spinosin in plasma showed good linearity over the concentration range of 1-300μg/ml, and the quantitation of limit of plasma was 1μg/ml. The linear range of concentrations of spinosin in the heart, spleen, stomach, lung, testis, brain, and intestine was 0.1-40μg/ml and the quantitation limit was 0.1μg/ml. The linear range of concentrations of spinosin in the liver and kidney was 1-150μg/ml, and the quantitation limit was 1μg/ml. The correlation coefficients of all calibration curves were between 0.9939 and 0.9980. The intra and interrun precision for all samples was less than ⩽11.0%. The time-concentration curve of spinosin after the intravenous administration of a single dose of 20mg/kg to rats corresponded to the two-compartment model. The main pharmacokinetic parameters T_<0.5α>, T_<0.5β>, CLs, AUC_<0-T>, and V_c were 6.66min, 51.5min, 1.42l・min^<-1>, 2.83mg・min・ml^<-1>, and 14.0l・kg^<-1>, respectively. At 20min, a concentration peak occurred in liver and brain tissues. The highest level of spinosin occurred in the liver, followed by the spleen and kidney. The lowest level of spinosin appeared in the testis, followed by the brain. Spinosin was not detected in smooth and skeletal muscle. After intravenous administration, the drug was distributed extensively and transferred quickly in rats in vivo.
- 公益社団法人日本薬学会の論文
- 2007-08-01
著者
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Deng Yu-lin
School Of Life Science And Technology Beijing Institute Of Technology
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Li Yan
School Of Public Health Kunming Medical College
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Yu Ye-ling
School Of Pharmacy Shenyang Pharmaceutical University
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Dai Yue-han
School Of Life Science And Technology Beijing Institute Of Technology
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Li Yu-juan
School Of Life Science And Technology Beijing Institute Of Technology
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Li Yan
School Of Chemistry & Chemical Engineering Jinan University
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