Abstract
The results of laboratory and clinical experiments for ophthalmic use ofminocycline were summarized as follows.
(1) The minimum growth inhibitory concentration of minocycline was somewhat superior to tetracycline, being 0.25 mcg/ml for KOCH-WEEKS bacillus, 0.1-0.25mcg/ml for MORAX-AXENFELD diplobacillus, 0.1-1mcg/ml for Pneumococcus, 0.5mcg/ml for Corynebacterium diphtheriae. 0.1mcg/ml for Neisseria gonorrhoea, 0.1-5mcg/ml for Streptococcus, 0.2-1mcg/ml for Staphylococcus and 50mcg/ml for Pseudomonas aeruginosa.
(2) The distribution of the sensitivity for 93 strains of Staph. aureus isolatedfrom eye patients was in the range of ≤0.1-2.5mcg/ml. All of the tetracycline resistant strains showedhigh sensitivity to minocycline.
(3) The blood concentration was determined with 3 healthy adults after single oral administration of 200mg minocycline. The average values of 3 cases produced peak level, 1.89 mcg/ml, after 2 hours, and measurable amounts,0.55mcg/ml, were present in serum after 24 hours.
(4) In rabbits, aqueous levels by the oral administration of 100mg minocycline attained to the peak after 2 hours and maintained still after 24 hours. By the instillation or the subconjunctival injection, more favourable aqueous level were obtained than the oral administration.
(5) The concentration of the ocular tissue was examined at peak time of aqueous level. The concentration by the instillation was higher than the oral administration in the outer parts of the eye, especially in the cornea. The highest tissue concentration was observed by the subconjunctival injection, especially in the outer parts of the eye and the retina with choroid.
(6) The oral application of minocycline revealed excellent effects in 10 cases of hordeolum, a case of acute dacryocystitis, 2 cases of chronic dacryocystitis, a case of corneal infiltration, 3 cases of preventive application against postremoval of foreign body on the cornea, 2 cases of perforating injury and a case of orbital abscess.
(7) Side effect: In one of 20 cases, experienced anorexia, but no other severe side effects were noticed.