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        랫드에서 fluoroquinolone 항균제 DW-116 의 단회 경구투여에 의한 태반통과와 약물동태연구

        김종춘(Jong Chun Kim),윤효인(Hyo In Yun),신호철(Ho Chul Shin),허정두(Jeong Du Hur),이종화(Jong Hwa Lee),정문구(Moon Koo Chung) 한국응용약물학회 2002 Biomolecules & Therapeutics(구 응용약물학회지) Vol.10 No.1

        N/A The present study was conducted to investigate the placental transfer and pharmacokinetics of the fluoroquinolone antibacterial DW-116 in pregnant rats. The placental transfer and pharmacokinetics of DW-116 were examined after a single oral dose of 500 ㎎ [^14C]DW-116/㎏ on gestational day 18. Maternal and fetal tissues were collected at 0.17.0.5, 1, 2, 4, 8, and 24 h after dosing. Maximum radioactivity was detected in maternal plasma, placenta, and whole fetus at 1 h, and in amniotic plasma at 4 h after dosing. Thereafter, radioactivity gradually disappeared from these tissues and was 16∼28% of maximum levels at 24 h after dosing. Radioactivity in whole fetus were higher than those in the maternal plasma and placenta. The T_(1/2,abs), T_(1/2,β), AUC, T_max, and C_max in the maternal plasma were approximately 6 min, 13.3 h, 1620 ug^*hr/ml, 0.5 h, and 136 ug/ml, respectively. Those in the placenta were approximately 20 min, 12.3 h, 2150 ug^*h/ml, 1.0 h, and 172 ug/ml, respectively. Those in the whole fetus were 13 min, 12.8 h, 2549 ug^*h/ml, 1 h, and 191 ug/ml, respectively. In the amniotic fluid of maternal uterus, the T_(1/2,abs), T_(1/2,β), AUC, T_max, and C_max were approximately 1.3 h, 9.3 h, 2508 ug^*h/ml, 4.4 h, and 135 ug/ml, respectively. While DW-116 disappeared biphasically from maternal plasma, whole fetus and placenta, it was eliminated monophasically from amniotic fluid. In conclusion, this study demonstrated that the absorption and distribution of DW- 116 in maternal plasma and placenta were extensively rapid, and that the test chemical well passed the blood-placenta barrier and was transferred to the fetus.

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