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[通过微透析分析诺氟沙星和洛美沙星在房水中的药代动力学]

[Pharmacokinetics of norfloxacin and lomefloxacin in aqueous humour analysed by microdialysis].

作者信息

Sato H, Fukuda S, Inatomi M, Koide R, Uchida N, Kanda Y, Kiuchi Y, Oguchi K

机构信息

Department of Ophthalmology, Showa University School of Medicine, Tokyo, Japan.

出版信息

Nippon Ganka Gakkai Zasshi. 1996 Jul;100(7):513-9.

PMID:8741334
Abstract

The pharmacokinetics of norfloxacin (NFLX) and lomefloxacin (LFLX) in rabbit aqueous humour after instillation of 0.3% solution (20 microliters) and oral administration (20 mg/kg) were investigated by microdialysis. We also measured plasma concentration of fluoroquinolones after oral administration. After instillation, the maximum concentration (Cmax) of NFLX and LFLX in the aqueous humour was 0.80 and 1.20 micrograms/ml, and elimination half time (t1/2) was 130 and 96 min, respectively. After oral administration, the Cmax in plasma of NFLX and LFLX was 2.06 and 1.89 micrograms/ml, and the Cmax in aqueous humour was 0.16 and 0.62 microgram/ml, respectively. t1/2 of NFLX in aqueous humour and plasma was 225 and 295 min, and t1/2 of LFLX was 188 and 175 min, respectively. The ratio of aqueous humour/serum concentration of NFLX and LFLX was 7.8 and 35.3% 4 hrs after oral administration. These results suggest that, after instillation, LFLX penetrated better into the aqueous humour, and was eliminated faster, than NFLX, and that after oral administration, NFLX could not panetrate well into the aqueous humor from the blood.

摘要

采用微透析法研究了0.3%溶液(20微升)滴眼及口服给药(20毫克/千克)后,诺氟沙星(NFLX)和洛美沙星(LFLX)在兔眼房水中的药代动力学。我们还测定了口服给药后氟喹诺酮类药物的血浆浓度。滴眼后,NFLX和LFLX在房水中的最大浓度(Cmax)分别为0.80和1.20微克/毫升,消除半衰期(t1/2)分别为130和96分钟。口服给药后,NFLX和LFLX在血浆中的Cmax分别为2.06和1.89微克/毫升,在房水中的Cmax分别为0.16和0.62微克/毫升。NFLX在房水和血浆中的t1/2分别为225和295分钟,LFLX的t1/2分别为188和175分钟。口服给药4小时后,NFLX和LFLX的房水/血清浓度比分别为7.8%和35.3%。这些结果表明,滴眼后,LFLX比NFLX更易穿透进入房水,且消除更快;口服给药后,NFLX从血液中穿透进入房水的能力较差。

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