AIM: To validate a radioactivity assay, the TCA-RA method, for the measurement of C-1027 in serum and to evaluate its application in determination of pharmacokinetics of C-1027 in mice. METHODS: 125I-C-1027 was prepar...AIM: To validate a radioactivity assay, the TCA-RA method, for the measurement of C-1027 in serum and to evaluate its application in determination of pharmacokinetics of C-1027 in mice. METHODS: 125I-C-1027 was prepared by the lodogen method and separated by HPLC. The radioactivity assay was established and used to determine 125I-C-1027 in mice at doses of 10, 50 and 100 μg/kg after precipitation with 20% trichloroacetic acid (TCA-RA method). Several pharmacokinetic parameters were determined after intravenous injection of 125I-C-1027 to mice. RESULTS: After intravenous injection of 125I-C-1027 to mice, at doses of 10, 50 and 100μg/kg; the apparent distribution volumes (Vd) were 0.26, 0.31 and 0.33 L/kg; the biological half-lives (T1/2) were 3.10, 3.40 and 3.90 h; the areas under curve (AUC) were 18.41, 103.69 and 202.74 ng/h/mL; the elimination rate constants (A) were 1.04, 1.26 and 0.58/h; and the total body clearance (Cl) were 0.54, 0.48 and 0.49 L/kg/h, respectively. CONCLUSION: TCA-RA is a sensitive, reliable and suitable method for the determination of 125I-C-1027 in mouse serum.展开更多
基金Supported by the National "863" Project of China, No. 2003AA2Z347D
文摘AIM: To validate a radioactivity assay, the TCA-RA method, for the measurement of C-1027 in serum and to evaluate its application in determination of pharmacokinetics of C-1027 in mice. METHODS: 125I-C-1027 was prepared by the lodogen method and separated by HPLC. The radioactivity assay was established and used to determine 125I-C-1027 in mice at doses of 10, 50 and 100 μg/kg after precipitation with 20% trichloroacetic acid (TCA-RA method). Several pharmacokinetic parameters were determined after intravenous injection of 125I-C-1027 to mice. RESULTS: After intravenous injection of 125I-C-1027 to mice, at doses of 10, 50 and 100μg/kg; the apparent distribution volumes (Vd) were 0.26, 0.31 and 0.33 L/kg; the biological half-lives (T1/2) were 3.10, 3.40 and 3.90 h; the areas under curve (AUC) were 18.41, 103.69 and 202.74 ng/h/mL; the elimination rate constants (A) were 1.04, 1.26 and 0.58/h; and the total body clearance (Cl) were 0.54, 0.48 and 0.49 L/kg/h, respectively. CONCLUSION: TCA-RA is a sensitive, reliable and suitable method for the determination of 125I-C-1027 in mouse serum.
