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成人から新生児にいたるオフロキサシン(OFLX)1回点眼後の血中移行について検討した。成人では,34名95サンプル中1サンプルのみに15.1ng/mlの血清中OFLX濃度を検出した。乳幼児〜小児では,26名26サンプル中1サンプルに5.7ng/mlの血清中濃度を検出した。
未熟児および新生児では,25名39サンプル中20サンプルに5.0〜20.3ng/gのOFLX濃度を検出した。この他1名は血清移行につき検討し,10.5ng/mlの血清中OFLXを認めた。
点眼によって吸収されたOFLXの血中濃度は,OFLXの毒性に対して最も敏感な反応を示す幼若犬での実験結果に比較してもはるかに低く,未熟児や新生児においても副作用を起こす危険性はないことが示唆された。
We quantitated the concentration of ofloxacin inthe circulating blood after a single instillation ofofloxacin ophthalmic solution into the cul-de-sac.Out of 95 samples from 34 adults, only one sampleshowed serum concentration of 15.1 ng/ml. Oflox-acin could not be detected in the other 94 samples.Out of 26 samples from 26 persons aged between 2months and 14 years, serum concentration of 5.7ng/ml was detected in one sample from a 4-year-boy. Ofloxacin could not be detected in the other25 samples. Out of 39 samples from 25 prematureand 1 newborn babies, ofloxacin was detected in thecirculating blood at various levels from 5.0 to 20.3ng/ml in 20 samples. Ofloxacin could not be detect-ed in the other 19 samples. One serum sample fromthe newborn showed 10.5 ng/ml of ofloxacin. Thefindings show that the serum and blood concentra-tion of ofloxacin is remarkably low after a singletopical instillation. Ophthalmic solution of oflox-acin would also be innocuous when used in pre-mature babies.
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