Basic and clinical experiments were performed on intravenous cephradine (CED) in ophthalmological field. The results are summarized as follows.
1. Serum concentration: After intravenous- injection of 1.0g CED, in a single dose, to a healthy adult, the peak of serum level (34.0 μg/ml) was attained at 15 minutes, then decreased quickly to 2.3 μg/ml by 6 hours.
2. Ocular penetration in rabbit eye:
(1) Aqueous humor concentrations: The peak level of aqueous humor (13.45 μg/ml) was obtained at 30 minutes after intravenous injection of 50mg/kg, in a single dose. Aqueous/Serum ratio was 38.07%. After instillation of 5mg/ml solution of CED, 5 times every 5 minutes, the aqueous level was recognized 30 minutes and 1 hour, and no detectable 4 hours. After 50mg/0.5ml CED subconjunctival injection, in a single dose, the high aqueous levels were observed at 30 minutes and 1 hour, and still detectable 4 hours later.
(2) Ocular tissue concentrations: The ocular tissue concentrations at 30 minutes after intravenous injection of 50mg/kg CED were high in both outer and inner parts of the eye. After 4 hours, the tissue levels remained relatively high concentrations.
(3) Clinical results: Intravenous administration of 0.5, 1.0 or 2.0g CED 1 or 2 times daily revealed excellent or good effects in 8 of 12 cases, such as external hordeolum, internal hordeolum, lid abscess, chronic dacryocystitis, orbital abscess and corneal ulcer.
(4) Side effects: Three cases out of 12 complained burning sensation by intravenous injection of CED, but in neither case was it found necessary to withdraw the drugs. No severe side effects such as allergic reactions were observed. No abnormal findings in hepatic and renal function tests were observed.
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