Bacterial and clinical experiments for ophthalmic use of
clindamycin-2-phosphate (CLDM-2-P) were performed and the results were summarized as follows. 1. The distribution of sensitivity for 100 strains of Staphylococcus aureus isolated in 1975 was in the range of less than or equal to 0.19 approximately greater than or equal to 100 mug/ml, and majority of them (96.0%) were in less than or equal to 0.39 mug/ml. 2. The serum concentration by
intramuscular injection of 300 mg and 600 mg CLDM-2-P in a single dose respecitvely reached the peak level after 2 hours and decreased gradually until 12 hours in both of them. 3. Ocular penetrations were examined in rabbit eyes. (1) After instillation of 1% CLDM-2-P
solution, the aqueous level reached the highest after 1 hour and measurable after 6 hours. (2) After subconjunctival injection of 5 mg/0.5 ml CLDM-2-P, the aqueous level reached the highest after 2 hours and decreased until 6 hours. (3) After
intramuscular injection of 100 mg/kg, the aqueous concentration was recognized from 1 to 8 hours, and peak was reached after 1 hour. 1 to 8 hours, and peak was reached after 1 hour. Aqueous-serum ratio in 1 hour was 37.13%. The ocular tissue concentrations at 2 hours showed relatively high levels in both of outer and inner parts of the eye. 4. The
intramuscular injection of CLDM-2-P, 300 approximately 1800 mg daily, against suppurative
ocular infections revealed excellent effects on cases of external
hordeolum, acute
chalazion, lid
abscess, orbital phlegmone, corneal infiltration,
corneal ulcer, and
iridocyclitis purulenta. 5. Side effects: Two cases out of 22 cases complained of diarrhoea and bitter taste after injection, and able to be treated continuously by the
drug. No abnormal findings in hepatic and renal tests were observed and no servere side effects like
allergic reactions were recognized.