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首页> 外文期刊>World Journal of Gastroenterology >Pharmacokinetics of C-1027 in mice as determined by TCA-RA method.
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Pharmacokinetics of C-1027 in mice as determined by TCA-RA method.

机译：通过TCA-RA方法测定的C-1027在小鼠体内的药代动力学。

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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: (125)I-C-1027 was prepared by the Iodogen method and separated by HPLC. The radioactivity assay was established and used to determine (125)I-C-1027 in mice at doses of 10, 50 and 100 microg/kg after precipitation with 20% trichloroacetic acid (TCA-RA method). Several pharmacokinetic parameters were determined after intravenous injection of (125)I-C-1027 to mice. RESULTS: After intravenous injection of (125)I-C-1027 to mice, at doses of 10, 50 and 100 microg/kg; the apparent distribution volumes (V(d)) were 0.26, 0.31 and 0.33 L/kg; the biological half-lives (T(1/2)) 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 (K) 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 (125)I-C-1027 in mouse serum.
机译：目的：为了验证放射性测定，TCA-RA方法，用于测量血清中的C-1027并评估其在确定C-1027在小鼠体内药代动力学中的应用。方法：用碘法制备（125）I-C-1027，并用HPLC分离。建立了放射性测定法，并用于在小鼠中用20％三氯乙酸沉淀后以10、50和100微克/千克的剂量测定（125）I-C-1027（TCA-RA方法）。在向小鼠静脉内注射（125）I-C-1027后，确定了几个药代动力学参数。结果：以10、50和100 microg / kg的剂量向小鼠静脉内注射（125）I-C-1027。表观分布体积（V（d））为0.26、0.31和0.33 L / kg;生物学半衰期（T（1/2））为3.10、3.40和3.90小时；曲线下面积（AUC）为18.41、103.69和202.74 ng / h / mL;消除速率常数（K）为1.04、1.26和0.58 / h；总身体清除率（Cl）分别为0.54、0.48和0.49 L / kg / h。结论：TCA-RA是一种灵敏，可靠，适合的方法，用于测定小鼠血清中的（125）I-C-1027。

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