PHASE I STUDY OF L-105
The phase I study of L-105, a new cephem antibiotic injection, was performed in 37 healthy adult male volunteers to observe the safety, pharmacokinetics, and changes in dominant bacterial species of Enterobacteriaceae. Each subject was administered L-105 in the following dose: 0.25, 0.5, 1.0 and 2.0...
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| Published in: | CHEMOTHERAPY Vol. 34; no. Supplement3; pp. 133 - 148 |
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| Main Authors: | , , , , , , |
| Format: | Journal Article |
| Language: | English Japanese |
| Published: |
Japanese Society of Chemotherapy
1986
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| Online Access: | Get full text |
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| Summary: | The phase I study of L-105, a new cephem antibiotic injection, was performed in 37 healthy adult male volunteers to observe the safety, pharmacokinetics, and changes in dominant bacterial species of Enterobacteriaceae. Each subject was administered L-105 in the following dose: 0.25, 0.5, 1.0 and 2.0 g single i.v. bolus injection, 2.0g single i. v. drip infusion over 1 hour, and 1.0 g i. v. injections 9 times at intervals of 12 hours; also 0.25 and 0.5 g single i. m. injection, and 0.25 g i. m. injections 6 times at intervals of 6 hours. The results were as follows: 1. No abnormalities were observed in subjective and objective symptoms, physical examination, hematology, blood chemistry, and urinalysis. 2. When single i. v. injection of 0. 25, 0.5, 1.0, and 2.0 g were administered, L-105 maximum concentrations (Cmax) in serum were 28. 9, 73. 2, 112 and 243μg/ml, respectively, showing a dose dependent, and with a single drip i. v. infusion of 2.0 g the Cmax 90.1μg/ml. The Cmax with a single i. m. injection of 0.25 and 0.5 g were 9.8 and 16.9μg/ml, respectively. 3. The half-life time of serum concentration with single i. v. or single i.m. was about 1.0 hour (0.92-1.31). No accumulation of L-105 in the serum was observed in the multiple administration. 4. The urinary recovery rates after single i. v. injection and i. m. injection were about 50 to 70 % within 6 hours and the fecal recovery rates after single i. v. injection were 8.3 to 15.1%. 5. No changes in dominant bacterial species of Enterobacteriaceae in stool were found after multiple i. v. injections. |
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| ISSN: | 0009-3165 1884-5894 |
| DOI: | 10.11250/chemotherapy1953.34.Supplement3_133 |