Detail of "63358-49-6"

Reference

Pharmacokinetics of TA-058 in experimental animals

Pharmacokinetics of TA-058 in experimental animals. Yamaguchi, Toutaro; Maezawa, Isao; Yoshida, Hirotsugu; Tani, Kato; Sakuma, Yoshimitsu; Onta, Tokio; Ishii, Nobuo; Ohshima, Satoshi; Nitta, Shuji (Microbiol. Res. Lab., Tanabe Seiyaku Co., Ltd., Saitama 335, Japan). Chemotherapy (Tokyo), 32(Suppl. 2), 119-32 (Japanese) 1984. CODEN: NKRZAZ. ISSN: 0369-4682. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) In exptl. animals, the distribution and excretion of TA-058 (I) [63358-49-6] were compared with those of ref. penicillins. TA-058 was administered i.v. or i.m. to mice, rats, rabbits, and dogs in single doses of 20-100 mg/kg. The serum levels of I were higher than those of carbenicillin, ampicillin, and piperacillin and persisted much longer than those of the ref. penicillins. The biol. half-lives of I were 0.59, 0.96 and 0.99 h for rats (i.v.), dogs (i. v.) and dogs (drip i.v.), resp., at doses of 20 mg/kg. In mice, I was distributed in high concns. in various tissues in the decreasing order of the liver, kidneys, and lungs. In rats, the following order of tissue distribution was obsd.: kidneys > liver > lungs. TA-058 was excreted mainly in the urine of the rat, rabbit and dog within 5-24 h after its administration. The biliary excretion of I was 18.8 and 13.6% of the dose in 24 h for rats and rabbits, resp. These rates were lower than those of piperacillin. TA-058 was stable in body fluids and tissues in a cold or frozen state and no active metabolite of I was obsd. in these samples.

Disposition of 3H- or 14C-TA-058 in mice and rats

Disposition of 3H- or 14C-TA-058 in mice and rats. Takahashi, Tadao; Nakamura, Susumu; Honda, Shoichi; Harigaya, Shoichi; Yoshida, Hirotsugu; Sakuma, Yoshimitsu (Pharmacol. Res. Lab., Tanabe Seiyaku Co., Ltd., Saitama 335, Japan). Chemotherapy (Tokyo), 32(Suppl. 2), 133-51 (Japanese) 1984. CODEN: NKRZAZ. ISSN: 0369-4682. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The disposition and metab. of TA-058 (I) [63358-49-6], a new semisynthetic penicillin, were studied in mice and rats. The plasma half-lives of radioactivity in mice and rats after i.m. injection of [3H]I (20 mg/kg) were 17 and 18 min, resp. The tissue levels in both animals were highest at about 15 min after the injection. The kidneys, liver, lungs, and plasma showed high concns. of radioactivity, while the brain had the lowest level. When [14C]I (20 mg/kg) was injected i.v., the tissue levels in rats were similar to those obtained after i.m. injection. In the whole-body autoradiograms of mice and rats after i.v. injection of [14C]I (20 mg/kg), considerable radioactivity was obsd. in the kidneys, liver, lungs, s.c. connective tissue, and oral and nasal mucosa.