Pharmacokinetics of C-1027 in mice as determined by TCA-RA method

• Published in: World journal of gastroenterology : WJG 2005-02, Vol.11 (5), p.717-720
• Main Authors: Liu, You-Ping, Li, Quan-Sheng, Huang, Yu-Rong, Zhou, Mao-Jin, Liu, Chang-Xiao
• Format: Article
• Language: English
• Subjects: Aminoglycosides - pharmacokinetics; Animals; Antibiotics, Antineoplastic - pharmacokinetics; Brief Reports; C-1027; Chemical Precipitation; Enediynes; Female; HPLC; Injections, Intravenous; Iodine Radioisotopes - pharmacokinetics; Male; Mice; Mice, Inbred Strains; Radioimmunoassay - methods; Radioimmunoassay - standards; Reproducibility of Results; TCA-RA方法; Trichloroacetic Acid; 三氯乙酸; 灵敏性; 药物动力学
• ISSN: 1007-9327; 2219-2840
• DOI: 10.3748/wjg.v11.i5.717

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 Iodogen 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 100μg/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 0.33L/kg; the biological half-lives (T1/2) were 3.10, 3.40 and 3.90h; the areas under curve (AUC) were 18.41, 103.69 and 202.74ng/h/mL; the elimination rate constants (K) were 1.04, 1.26 and 0.58/h; and the total body clearance (Cl) were 0.54, 0.48 and 0.49L/kg/h, respectively.CONCLUSION: TCA-RA is a sensitive, reliable and suitable method for the determination of ^125I-C-1027 in mouse serum.