首页> 外文期刊>Regulatory peptides. >Pharmacokinetics of (125)I-GST-TatdMt, a recombinant fusion protein possessing potent anti-obesity activity, after intravenous, nasal, oral, and subcutaneous administration.
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Pharmacokinetics of (125)I-GST-TatdMt, a recombinant fusion protein possessing potent anti-obesity activity, after intravenous, nasal, oral, and subcutaneous administration.

机译:(125)I-GST-TatdMt,一种在静脉,鼻,口服和皮下给药后均具有有效的抗肥胖活性的重组融合蛋白的药代动力学。

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This study first reports the absorption kinetics of GST-TatdMt, a recombinant Tat protein possessing potent anti-obesity activity, in rats after nasal, s.c., and p.o. administration. GST-TatdMt was over-expressed in E. coli, purified, and radioiodinated using the IODO-GEN method. The radioiodinated (125)I-GST-TatdMt was administered to rats by nasal, s.c., and oral routes at doses of 7.3 mug (420.7 nCi), 146.5 mug (8413.8 nCi), and 146.5 mug (8413.8 nCi), respectively. For the determination of absolute bioavailability, (125)I-GST-TatdMt was also given to rats by i.v. injection (73.2 mug, 4206.9 nCi). Following administration by extravascular routes, the systemic absorption of radioactivity was prolonged, with C(max) being attained within 4.2-8.0 h. The absolute bioavailability calculated as dose-normalized AUC(extravascular)/AUC(i.v.) was 98.0, 75.8, and 87.1% after nasal, s.c., and oral administration, respectively. The majority of administered radioactivity was excreted in urine (57.5-64.7%), with fecal excretion being less (2.5-12.7%). The distribution of (125)I-GST-TatdMt to various tissues was also determined at 4 and 72 h after s.c. injection. The findings of this study suggest that this protein may be absorbed into the systemic circulation when given by extravascular administration.
机译:这项研究首先报道了在鼻,皮下和大便后大鼠中具有强大的抗肥胖活性的重组Tat蛋白GST-TatdMt的吸收动力学。行政。使用IODO-GEN方法在大肠杆菌中过表达GST-TatdMt,对其进行纯化和放射性碘标记。通过鼻腔,皮下和口腔途径分别以7.3马克(420.7 nCi),146.5马克(8413.8 nCi)和146.5马克(8413.8 nCi)的剂量将放射性碘(125)I-GST-TatdMt通过鼻,皮下和口服途径给予大鼠。为了确定绝对生物利用度,还通过静脉内注射将(125)I-GST-TatdMt给予大鼠。注射(73.2杯,4206.9 nCi)。通过血管外途径给药后,放射性的全身吸收被延长,在4.2-8.0小时内达到C(max)。经鼻,皮下和口服给药后,以剂量标准化的AUC(血管外)/ AUC(静脉内)计算的绝对生物利用度分别为98.0%,75.8%和87.1%。所给予的放射性大部分通过尿液排泄(57.5-64.7%),而粪便排泄较少(2.5-12.7%)。在皮下注射后第4和72小时也测定了(125)I-GST-TatdMt在各种组织中的分布。注射。这项研究的发现表明,当通过血管外给药时,该蛋白可能被吸收到体循环中。

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