2012•Zhongguo yaolixue tongbaoRequires access

A study of pharmacokinetics and the absolute bioavailability of PSD-007 in rabbits

Hongli Chen

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Abstract

Aim To investigate the pharmacokinetic characteristics and the absolute bioavailability of PSD-007 in rabbits.Methods The blood of rabbits was collected from the blink of the ears after ip/iv administration of PSD-007,and the plasma drug concentrations at different times were determined by ultraviolet visible spectrophotometer.The best compartment model and the pharmacokinetic parameters were calculated by the software of 3P97.Results The elimination process of PSD-007 fitted one-compartment model after ip administration of 10 mg·kg-1 of PSD-007,but fitted three-compartment open model after iv administration,the eliminate rate of which was faster.The principal pharmacokinetic parameters were T12Ke=11.6 h,Cmax=2.312 mg·L-1,AUC=43.177 mg·L-1·h,CL=0.232 L·kg-1·h-1,V/F(c)=3.888 L·kg-1;Vc=0.75 L·kg-1,T12α=2.824 h,T12β=40.632 h,AUC=65.161 mg·L-1·h,CL(s)=0.153 L·kg-1·h-1.The absolute bioavailability was 66.2%.Conclusions PSD-007 has fast absorption,quick effect and elimination,without accumulation phenomenon,and pharmacokinetic characteristics were different based on different ways of giving medicine.

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Aim To investigate the pharmacokinetic characteristics and the absolute bioavailability of PSD-007 in rabbits.Methods The blood of rabbits was collected from the blink of the ears after ip/iv administration of PSD-007,and the plasma drug concentrations at different times were determined by ultraviolet visible spectrophotometer.The best compartment model and the pharmacokinetic parameters were calculated by the software of 3P97.Results The elimination process of PSD-007 fitted one-compartment model after ip administration of 10 mg·kg-1 of PSD-007,but fitted three-compartment open model after iv administration,the eliminate rate of which was faster.The principal pharmacokinetic parameters were T12Ke=11.6 h,Cmax=2.312 mg·L-1,AUC=43.177 mg·L-1·h,CL=0.232 L·kg-1·h-1,V/F(c)=3.888 L·kg-1;Vc=0.75 L·kg-1,T12α=2.824 h,T12β=40.632 h,AUC=65.161 mg·L-1·h,CL(s)=0.153 L·kg-1·h-1.The absolute bioavailability was 66.2%.Conclusions PSD-007 has fast absorption,quick effect and elimination,without accumulation phenomenon,and pharmacokinetic characteristics were different based on different ways of giving medicine.

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Available abstract

Aim To investigate the pharmacokinetic characteristics and the absolute bioavailability of PSD-007 in rabbits.Methods The blood of rabbits was collected from the blink of the ears after ip/iv administration of PSD-007,and the plasma drug concentrations at different times were determined by ultraviolet visible spectrophotometer.The best compartment model and the pharmacokinetic parameters were calculated by the software of 3P97.Results The elimination process of PSD-007 fitted one-compartment model after ip administration of 10 mg·kg-1 of PSD-007,but fitted three-compartment open model after iv administration,the eliminate rate of which was faster.The principal pharmacokinetic parameters were T12Ke=11.6 h,Cmax=2.312 mg·L-1,AUC=43.177 mg·L-1·h,CL=0.232 L·kg-1·h-1,V/F(c)=3.888 L·kg-1;Vc=0.75 L·kg-1,T12α=2.824 h,T12β=40.632 h,AUC=65.161 mg·L-1·h,CL(s)=0.153 L·kg-1·h-1.The absolute bioavailability was 66.2%.Conclusions PSD-007 has fast absorption,quick effect and elimination,without accumulation phenomenon,and pharmacokinetic characteristics were different based on different ways of giving medicine.

Key concepts: Pharmacokinetics, Bioavailability, Cmax, Absorption (acoustics), Pharmacology, Chemistry, Compartment (ship), Medicine

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