Pharmacokinetics of m-nifedipine in rabbits after intravenous injection
Abstract
AIM:
To study the dose effects on pharmacokinetics of m-Nif.
METHODS:
Fifteen rabbits were divided into 3 groups receiving i.v. m-Nif 0.5, 1, and 2 mg.kg-1. Plasma levels of m-Nif were determined with HPLC method.
RESULTS:
The concentration-time data were fitted with 2-compartment model. After i.v. 1 mg.kg-1, the parameters were: Vd = 0.37 +/- 0.10 L.kg-1, T1/2 alpha = 6.4 +/- 2.9 min, T1/2 beta = 84 +/- 22 min, AUC = 94 +/- 16 mg.min.L-1, Cl = 0.65 +/- 0.13 L.kg-1.h-1. No statistically significant difference was found in Cl and T1/2 beta between 3 dose groups. AUC (standardized to body weight) was correlated with doses.
CONCLUSIONS:
m-Nif was distributed widely and eliminated at a fairly rapid rate in the rabbits. No dose-dependent pharmacokinetics was found after i.v. m-Nif 0.5-2 mg.kg-1. m-Nifedipine, 2, 6-dimethyl-3, 5-dicarbomethoxy-4-(3'-nitrophenyl)-1, 4-dihydropyridine (m-Nif) is a new calcium channel blocker. Dihydropyridine calcium channel antagonists are mainly used for the treatment of hypertension and angina[1]. Nifedipine is susceptible to photodegradation, but m-Nif is stable when exposed to light. The 2 drugs have the same antihypertensive effect[2]. So far, no report has been found on pharmacokinetics of m-Nif. Using a high performance liquid chromatographic (HPLC) method, we studied the dose effects on the pharmacokinetics of i.v. m-Nif 0.5, 1, and 2 mg.kg-1 in conscious rabbits.
Keywords:
To study the dose effects on pharmacokinetics of m-Nif.
METHODS:
Fifteen rabbits were divided into 3 groups receiving i.v. m-Nif 0.5, 1, and 2 mg.kg-1. Plasma levels of m-Nif were determined with HPLC method.
RESULTS:
The concentration-time data were fitted with 2-compartment model. After i.v. 1 mg.kg-1, the parameters were: Vd = 0.37 +/- 0.10 L.kg-1, T1/2 alpha = 6.4 +/- 2.9 min, T1/2 beta = 84 +/- 22 min, AUC = 94 +/- 16 mg.min.L-1, Cl = 0.65 +/- 0.13 L.kg-1.h-1. No statistically significant difference was found in Cl and T1/2 beta between 3 dose groups. AUC (standardized to body weight) was correlated with doses.
CONCLUSIONS:
m-Nif was distributed widely and eliminated at a fairly rapid rate in the rabbits. No dose-dependent pharmacokinetics was found after i.v. m-Nif 0.5-2 mg.kg-1. m-Nifedipine, 2, 6-dimethyl-3, 5-dicarbomethoxy-4-(3'-nitrophenyl)-1, 4-dihydropyridine (m-Nif) is a new calcium channel blocker. Dihydropyridine calcium channel antagonists are mainly used for the treatment of hypertension and angina[1]. Nifedipine is susceptible to photodegradation, but m-Nif is stable when exposed to light. The 2 drugs have the same antihypertensive effect[2]. So far, no report has been found on pharmacokinetics of m-Nif. Using a high performance liquid chromatographic (HPLC) method, we studied the dose effects on the pharmacokinetics of i.v. m-Nif 0.5, 1, and 2 mg.kg-1 in conscious rabbits.