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A Fujino

Publications and source records attributed to A Fujino.

72 records · Page 4Linked to original sources

[Absorption, distribution, metabolism and excretion of netilmicin in rats (II). Accumulation study of netilmicin after repeated administration].

Repeated administration of netilmicin (NTL), a new aminoglycoside antibiotic, to rats at daily intramuscular dose of 10 or 20 mg/kg for 22 days did not affect the plasma level and the plasma half-life of the drug. The concentrations of NTL in the kidney increased markedly after repeated administration, and reached peak level after 8 and 15 doses for 10 and 20 mg/kg, respectively. Cumulative effect of NTL after repeated dose was also observed in the liver, spleen and lung, although the peak concentrations of NTL in these organs were below 1/50 of that in the kidney. Blood and tissue levels of NTL in rats were determined after a single intramuscular administration of 14C-NTL at a dose of 20 mg/kg following 21 repeated intramuscular administrations of NTL at daily dose of 20 mg/kg. The repeated dose of NTL had no effect on the blood level-time curve of radioactivity. The concentration of NTL in the kidney determined by radioassay was about 1/3 of that determined by bioassay, whereas the half-lives in the tissue levels determined by these two assays were nearly identical with each other. The half-life in the lung determined by bioassay was almost identical to that determined by radioassay, whereas the former was rather shorter than the latter in the liver and spleen.

Animals↗

[Absorption, distribution, metabolism and excretion of netilmicin in rats (III). Metabolic fate of 14C-netilmicin after intramuscular administration (author's transl)].

The metabolic fate of 14C-netilmicin (14C-NTL) was studied in rats after intramuscular administration (20 mg/kg). 1. Binding ratio of 14C-NTL to rat plasma protein, determined by the ultracentrifugal method, was 15 approximately 20% during the first 1 hour after intramuscular administration. 2. Binding ratio of 14C-NTL to HSA, determined by the equilibrium dialysis method, was 15 approximately 23%. Binding constant (K) and maximum binding number (n) were calculated as 1.48 X 10(4) and 3.3 mole/mole, respectively. Half of 14C-NTL bound to HSA was dissociated from HSA by gel-filtration. 3. The radioactivity in tail vein blood reached peak level at 10 minutes after intramuscular administration and declined rapidly. 4. Since the distribution rate of 14C-NTL into the blood cells was low during the first 2 hours, the plasma level at that time was about 1.5 times higher than whole blood level. 5. The recovery of radioactivity in the bile (0 approximately 24 hours) was only 0.13% of the dose administered. An average concentration during 2 hours after intramuscular injection was 2.5 mcg/ml. 6. Within 2 hours after administration, approximately 40% of the dose was recovered in the urine. Within 24 hours, 87.8% of the dose was excreted in the urine, 2.6% in the feces, 0.3% in the cage washing and 8.8% in the carcass. Total recovery ratio was 99.5% of the dose. 7. The radioactivity was widely distributed in the tissues, especially high in the kidney and bone, low in the brain. A high concentration of radioactivity was found in the renal cortex at 24 hours after administration. 8. Netilmicin was excreted into the urine unchanged and no metabolites were detected by TLC at all.

Animals↗

[Absorption, distribution, metabolism and excretion of netilmicin in rats (IV). Distribution in kidney and transmigration to fetus or suckling (author's transl)].

Distribution in kidney and transmigration to fetus or suckling in rats were studied in male, pregnant or lactating rats after intramuscular administration of 14C-netilmicin (20 mg/kg). 1. After administration to male rats, the radioactivity in the kidney declined slowly with a half-life of approximately 6 days. 2. The radioactivity in the kidney was distributed in the renal cortex. The distribution pattern was further investigated by means of microautoradiography. The radioactivity was specifically observed in lysosomal granules of the proximal tubules at 6 hours after administration and reached maximum at 24 hours after administration, then declined gradually. On the other hand, the radioactivity in the distal tubules was lower than that of the proximal tubules. The highest radioactivity in the distal tubules was detected later than 24 hours after administration. 3. In pregnant rats (20th day of gestation), the distribution of radioactivity in the tissues were almost the same as those in the male rat. The small amount of radioactivity was detected in the fetal kidney and bone. 4. In mother rats (14 days after parturition), the radioactivity in the milk was 3 approximately 4 mcg equivalent of netilmicin/ml during 24 hours after administration. The small amount of radioactivity (0.13% of dose) was observed in the gastrointestinal contents of a suckling with 6 hours after administration.

Animals↗

[Clinical evaluation of cefotiam in internal medicine, with special reference to infectious disease associated with hematological disorders (author's transl)].

Clinical evaluation of cefotiam (panspolin), a new cephem antibiotics, was performed in the infectious disease associated with hematological disorders and in the respiratory system. In hematological dis orders, 40% of good and 25% of fair results were obtained in clinical effects. In respiratory infections, however, 92% of good results were obtained. Opportunistic infection due to Gram-negative bacilli are often experienced in patients with leukemia. Since cefotiam has sufficient bacteriocidal effects in broad spectrum, it would be a good therapeutic agent against infectious diseases associated with hematological disorders.

Adolescent↗