Amoxycillinの眼科的応用のための基礎的および臨床的実験成績

抄録

The laboratory and clinical experiments were performed on amoxycillin (abbr.AMPC) to apply the drug in ophthalmological field, and the results were obtained as follows.
1) The minimum inhibitory concentration of AMPC was 1.56 mcg/ml against Koch-Weeks bacillus, 0.005 mcg/ml against Morax-Axenfeld bacillus, 0.01-0.78 mcg/ml against D.pneumoniae, 0.04-0.39 mcg/ml against C.diphtheriae, 0.01 mcg/ml against N.gonorrhoeae, 0.005-0.01 mcg/ml against Strept.hemolyticus, 1.56-3.13 mcg/ml against Strept.viridans, >100 mcg/ml against Ps.aeruginosa and 0.02 mcg/ml against Staph.aureus 209 P.These values mean that the antibacterial activity of AMPC is nearly equal to that of ABPC or PC G.
2) The AMPC sensitivity was examined on 40 strains of Staph.aureus isolated from the patients of eye infection, and it distributed with 3 peaks, ≤0.1 mcg/ml, 3.13-6.25 mcg/ml and 50 mcg/ml, distribution curve being quite similar to that of ABPC or PC G.
A clear relationship was observed on the cross resistance between AMPC and ABPC or PC G.
3) AMPC was administered orally at a dose of 250 mg or 500 mg to healthy adults, and the blood concentration reached the peak after 2 hours.
In the group administered 250 mg AMPC, the transferred amounts were 3.31 mcg/ml after 1 hour, 7.6 mcg/ml after 2 hours, 1.91 mcg/ml after 4 hours and O.30 mcg/ml after 6 hours, whereas, in the group of 500 mg, 4.7 mcg/ml after 1 hour, 16.3 mcg/ml after 2 hours, 4.9 mcg/ml after 4 hours, 1.58 mcg/ml after 6 hours and 0.48 mcg/ml after 8 hours.These amounts at a peak was 2.7 times higher than those with ABPC.
4) Ocular penetration was examined.AMPC was administered orally at a dose of 50 mg/kg to mature white rabbits, and the amounts transferred in aqueous humor were 3.46 mcg/ml after 1 hour, 2.02 mcg/ml after 2 hours, 0.96 mcg/ml after 4 hours and 0.32 mcg/ml after 6 hours.The ratio of aqueous humor to serum was 20.6%-60.
One hour after the administration of AMPC, corresponding to the peak of aqueous humor level, the ocular tissue concentrations were excellent both in outer parts and inner parts of the eyes, proving 2-3 times higher than those with ABPC.
5) The clinical results were investigated with AMPC on 10 cases of external hordeolum, 4 cases of internal hordeolum, 1 case of eyelid abscess, 2 cases of acute dacryocystitis, 2 cases of corneal infiltration, 3 cases of corneal ulcer and 2 cases of orbital phlegmon.
The dose was 500 mg-2g daily for 3-8 days, the total being 1.5-14 g.The results obtained were remarkably effective in 6 cases, effective in 15 cases, slightly effective in 1 case and ineffective in 2 cases.The effective cases (remarkably effective plus effective) counted thus 21 (87.5%).
6) As to the side effect with AMPC, there observed 1 case of diarrhoea, 1 case of dyspepsia and 1 case of anorexia.
The ratio of side effect was 12.5%.