2005Zhōnghuá yàoxué zázhìRequires access

Pharmacokinetics of 9-nitrocamptothecin after single oral administrations in rats

Chunyan Zhang

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Abstract

OBJECTIVE To develop a reversed phase high performance liquid chromatographic method for the determination of 9-nitro-camptothecin in plasma and to investigate the pharmacokinetics of 9-nitroeamptotheein at three doses in rats. METHODS Venous blood was collected from eyehole after a single oral administration of 9-nitrocamptothecin. The plasma concentrations of 9-nitroeamptothecin were measured using HPLC, pharmacokinetic parameters were calculated by DAS( 1.0) .RESULTS The main pharmacokinetic parameters were: cmax 653.02ng·mL-1(2mg·kg-1), 832.9 ng·mL-1(3 mg·kg-1 ) and 2 731.15 ng·mL-1 (5 mg·kg-1); tmax0.32 h (2 mg·kg-1) , 0.45 h (3 mg·kg-1) and0.3h(5mg·kg-1); AUC0-∞ 856.49 μg·h·L-1(2 mg·kg-1), 1 485.69 μg·h·L-1(3 mg·kg-1) and 3 995.39 μg·h·L-1(5 mg·kg-1) .CONCLUSION The parent compound was metahlised or eliminated quickly. The plasma concentration-time curve of 9-nitrocamptothecin was fitted with an one-compartment open pharmacokinetic model and appeared to be a linear pharmacokinetic characteristics.

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OBJECTIVE To develop a reversed phase high performance liquid chromatographic method for the determination of 9-nitro-camptothecin in plasma and to investigate the pharmacokinetics of 9-nitroeamptotheein at three doses in rats. METHODS Venous blood was collected from eyehole after a single oral administration of 9-nitrocamptothecin. The plasma concentrations of 9-nitroeamptothecin were measured using HPLC, pharmacokinetic parameters were calculated by DAS( 1.0) .RESULTS The main pharmacokinetic parameters were: cmax 653.02ng·mL-1(2mg·kg-1), 832.9 ng·mL-1(3 mg·kg-1 ) and 2 731.15 ng·mL-1 (5 mg·kg-1); tmax0.32 h (2 mg·kg-1) , 0.45 h (3 mg·kg-1) and0.3h(5mg·kg-1); AUC0-∞ 856.49 μg·h·L-1(2 mg·kg-1), 1 485.69 μg·h·L-1(3 mg·kg-1) and 3 995.39 μg·h·L-1(5 mg·kg-1) .CONCLUSION The parent compound was metahlised or eliminated quickly. The plasma concentration-time curve of 9-nitrocamptothecin was fitted with an one-compartment open pharmacokinetic model and appeared to be a linear pharmacokinetic characteristics.

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Available abstract

OBJECTIVE To develop a reversed phase high performance liquid chromatographic method for the determination of 9-nitro-camptothecin in plasma and to investigate the pharmacokinetics of 9-nitroeamptotheein at three doses in rats. METHODS Venous blood was collected from eyehole after a single oral administration of 9-nitrocamptothecin. The plasma concentrations of 9-nitroeamptothecin were measured using HPLC, pharmacokinetic parameters were calculated by DAS( 1.0) .RESULTS The main pharmacokinetic parameters were: cmax 653.02ng·mL-1(2mg·kg-1), 832.9 ng·mL-1(3 mg·kg-1 ) and 2 731.15 ng·mL-1 (5 mg·kg-1); tmax0.32 h (2 mg·kg-1) , 0.45 h (3 mg·kg-1) and0.3h(5mg·kg-1); AUC0-∞ 856.49 μg·h·L-1(2 mg·kg-1), 1 485.69 μg·h·L-1(3 mg·kg-1) and 3 995.39 μg·h·L-1(5 mg·kg-1) .CONCLUSION The parent compound was metahlised or eliminated quickly. The plasma concentration-time curve of 9-nitrocamptothecin was fitted with an one-compartment open pharmacokinetic model and appeared to be a linear pharmacokinetic characteristics.

Key concepts: Pharmacokinetics, Cmax, Chemistry, Camptothecin, High-performance liquid chromatography, Chromatography, Pharmacology, Plasma concentration

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