EXPERIMENTAL AND CLINICAL STUDIES FOR OPHTHALMIC USE OF TA-058

Abstract

Experimental and clinical studies for ophthalmic use of TA-058, a new penicillin, were performed.
1) Rabbits were used for the experimental studies. After subconjunctival injection of TA-058 (300 mg/eye), the peak levels were 109.6 μg/ml at 30 minutes in serum level and 76.3 μg/ml at 15 minutes in aqueous humor. After intramuscular injection (100 mg/kg), the peak levels were 5.6 μg/ml at 1 hour in aqueous humor and 107.5 μg/ml at 30 minutes in serum. The peak level in aqueous humor after intravenous injection (100 mg/kg) was 8.4 μg/ml at 1 hour. When this drug was given by subconjunctival injection, relatively high level was observed in aqueous humor, and the aqueous humor/serum ratio at 15 minutes was 86.7 %.
The concentration of TA-058 in ocular tissues reached to the relatively high level by any route of the administration.
2) 4 patients with corneal abscess were treated with TA-058 to evaluate its clinical efficacy. In 3 cases, TA-058 was effective, while no improvement was found in 1 case with α-hemolytic streptococcus infection.
No side effect was observed with administration of TA-058.