Cephradineの眼科的応用のための基礎的ならびに臨床的検討

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  • OPHTHALMIC USE OF CEPHRADINE
  • Cephradine ガンカテキ オウヨウ ノ タメ ノ キソテキ ナラビニ

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Laboratory and clinical experiments were performed on cephradine (CED) in ophthalmological field, and the results obtained were as follows.<BR>1. Antimicrobial activity of CED against various organisms was 50 μg/ml for Koch-Weeks bacillus, 0.2 μg/ml for Morax-Axenfeld diplobacillus, 1. 56-.6.25 μg/ml for Pneuntococcus, 0.39 pg/ml for C. diphtheriae, 0.2 μg/ml for Gonococcus, 0.39 μg/ml for Strept. hentolyticus, 50-100 μg/ml for Strept. viridans, 0.78-4.56 μg/ml for Staph. aureus and > 100 μg/ml for Ps. aeruginosa.<BR>2. The distribution of the sensitivity for 40 strains of Staph. aureus was in the range of 1.56-12.5 μg/ml, and most of them (25 strains, 62.5%) were in 3.13 μg/ml.<BR>3. The peak of serum level was attained 1 hour after oral administration of 500 mg CED, then decreased relatively quickly until 6 hours (0.1 μg/ml), and not recognized after 8 hours.<BR>4. After oral administration of 50 mg/kg in rabbit, the peak level of aqueous humor was obtained at 2 hours (1.6 μg/ml). Aqueous/serum ratio was 26.02%.<BR>The ocular tissue concentrations at 2 hours after oral application of 50 mg/kg were high in both outer and inner parts of the eye. After 4 hours, the tissue levels were scarcely recognized except lid, sclera and vitreous body.<BR>5. Clinical results<BR>1) CED capsule<BR>Oral administration of 250-500 mg CED 4 times daily revealed good effects in 22 of 28 cases, such as ulcerative blepharitis, external hordeolum, internal hordeolum, chronic dacryocystitis, marginal corneal ulcer and corneal ulcer.<BR>2) CED dry syrupBy oral application of 25-50 mg/kg/day divided 4 times, the good clinical effects were obtained in 15 of 18 cases, such as acute conjunctivitis, ulcerative blepharitis, external hordeolum, chronic dacryocystitis, marginal corneal ulcer, corneal infiltration and iridocyclitis purulenta. <BR>6. Side effects<BR>Three cases of anorexia were experienced, by cephradine capsule, and each one case of diarrhoea and soft tool by dry syrup, but no other severe side effects were noticed.

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