EXPERIMENTAL AND CLINICAL STUDIES ON TA-058 IN URINARY TRACT INFECTIONS

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TA-058, a new semisynthetic penicillin antibiotic agent, was studied both fundamentally and clinically. Results obtained were as follows; 1) TA-058 was highly active against gram-positive bacteria and P. mirabilis. 2) Urinary recovery rate within 2 hours after intravenous bolus injection of, 1g of TA-058 in healthy volunteers was over 50 %. About 80 % of the dose was excreted in the urine within 12 hours. A peak urinary concentration of over 5, 000μg/ml was achieved after 2 hours. 3) Amoxicillin, a metabolite of TA-058 was detected in the urine of healthy volunteers by bioautogram and high performance liquid chromatography. Amount of, amoxicillin in the urine was 2 to 4 % of TA-058. 4) Eight patients with chronic complicated urinary tract infections were treated with 1g of TA-058 twice a day for 5 days by intravenous bolus injection. The overall clinical efficacy of the treatment was moderate in 2 and poor in 6 patients. 5) Neither subjective side effects nor aggravations in laboratory test results related to the TA-058 treatment were observed.
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