Objective: To study the pharmacokinetic, distribution and elimination properties of rhTα 1 after intravenous(i.v.) and subcutaneous(s.c.)injection in mice and rats. Methods: Competition ELISA was used for testing dru...Objective: To study the pharmacokinetic, distribution and elimination properties of rhTα 1 after intravenous(i.v.) and subcutaneous(s.c.)injection in mice and rats. Methods: Competition ELISA was used for testing drug concentration in serum, urine, bile and tissue after administration of rhTα 1 in mice(0.16, 0.5, 2.5 mg/kg) and rats(0.32, 1, 5 mg/kg). Pharmacokinetic parameters were calculated by Win Nolin software. Results: Absorption of rh Tαl is rapid in both mice and rats after s.c. administration. The pharmacokinetics in mice are characterized by linear, T_(1/2) showed a prolongation with increasing dose, 1.10, 1.35, and 1.50 h corresponding to 0.32, 1 and 5 mg/kg respectively, but in rats T_(1/2) showed no difference among doses. AUC0-∞ showed a clear increase with increasing doses in mice(904.18, 2998.83, and 19001.82 h*ng/m L) and in rats(1327.56 ±237.00,2924.53 ±685.14, and 35286.26 ±5999.58 h*ng/m L). After i.v. administration of 1 mg/kg rhTα 1 in mice, the drug is seen distributed in most organs, the thymus/serum exposure ratio was higher than others at the 1 and 2 h, the accumulative urinary excretion of primary drug was 32.97% ±15.85% within 6 h. Conclusion: The results indicate that rapid absorption, extensive distribution and quick renal excretion were the basic kinetic characteristics of rh Tαl after s.c. and i.v. administration.展开更多
基金Natural Science Foundation of Gansu Provincegrant number:1506RJZA278
文摘Objective: To study the pharmacokinetic, distribution and elimination properties of rhTα 1 after intravenous(i.v.) and subcutaneous(s.c.)injection in mice and rats. Methods: Competition ELISA was used for testing drug concentration in serum, urine, bile and tissue after administration of rhTα 1 in mice(0.16, 0.5, 2.5 mg/kg) and rats(0.32, 1, 5 mg/kg). Pharmacokinetic parameters were calculated by Win Nolin software. Results: Absorption of rh Tαl is rapid in both mice and rats after s.c. administration. The pharmacokinetics in mice are characterized by linear, T_(1/2) showed a prolongation with increasing dose, 1.10, 1.35, and 1.50 h corresponding to 0.32, 1 and 5 mg/kg respectively, but in rats T_(1/2) showed no difference among doses. AUC0-∞ showed a clear increase with increasing doses in mice(904.18, 2998.83, and 19001.82 h*ng/m L) and in rats(1327.56 ±237.00,2924.53 ±685.14, and 35286.26 ±5999.58 h*ng/m L). After i.v. administration of 1 mg/kg rhTα 1 in mice, the drug is seen distributed in most organs, the thymus/serum exposure ratio was higher than others at the 1 and 2 h, the accumulative urinary excretion of primary drug was 32.97% ±15.85% within 6 h. Conclusion: The results indicate that rapid absorption, extensive distribution and quick renal excretion were the basic kinetic characteristics of rh Tαl after s.c. and i.v. administration.
