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Biomedical subjects

T Kobari

Publications and source records attributed to T Kobari.

32 records · Page 2Linked to original sources
PubMed1985

Absorption, distribution and excretion of sultopride in man and several animal species.

Single oral and intramuscular doses of 14C-sultopride to rat, rabbit and dog and single oral doses of sultopride to human volunteers were well absorbed. Mean blood levels of total 14C peaked at 0.4-1.1 h and declined with half-lives of 2, 1.5 and 3 h in rat, rabbit and dog, respectively. In man mean serum levels of unchanged drug attained a peak at 1.5 h and were eliminated with a half-life of 3.6 h. Highest concn. of radioactivity were found in rat liver, kidney, hypophysis, submaxillary gland and gastrointestinal tract. The concn. in the cerebrum and cerebellum were low. 14C-Sultopride passed through the placental barrier. 14C-Sultopride was poorly bound to plasma proteins (less than 25% bound) in all species. Repeated doses of the drug slightly increased the blood and tissue levels of 14C in the rat. Most of the dose was eliminated via the kidneys in all species. Male rats excreted larger amounts of 14C into bile and faeces. A high ratio of A.U.C. (milk)/(blood) (c. 3.5) was found in the lactating rat.

Absorption↗
PubMed1985

[Influence of immunopotentiators on the activation of 5-FU derivatives].

As it has been shown that various kinds of immunopotentiators inhibit the hepatic microsomal drug-metabolizing enzymes and reduce the activation of masked compounds such as tegafur, we investigated the influence of immunopotentiators (OK-432 and PSK) on the activation of carmofur (HCFU), which is known to be transformed spontaneously in to the tumor-active substance, 5-fluorouracil (5-FU), in vivo, and compared the results to those obtained for tegafur. After oral administration of tegafur, the area under the plasma concentration curves of 5-FU in rats pretreated with OK-432 and PSK were 72% and 79% of those in untreated rats, while in the case of HCFU almost similar plasma concentration curves for 5-FU were obtained in both treated and untreated rats. These results show that the activation of HCFU to 5-FU is not influenced by treatment with these immunopotentiators. Furthermore, our clinical investigation showed that the survival curves of cancer patients given combination therapy of tegafur with OK-432 tended to be lower than those given a single therapy of tegafur, supporting the above mentioned basic results.

Adjuvants, Immunologic↗
PubMed1984

Dose-dependent pharmacokinetics of aprindine in healthy volunteers.

The disposition of aprindine following a single oral dose can best be described by a two-compartment open model. The mean plasma half-life (t 1/2 beta) increased from 8.0 +/- 2.1 h (SD) after a 25 mg dose of 9.4 +/- 2.9 h after 50 mg and to 15.8 +/- 2.6 h after 100 mg, with a decrease in total plasma clearance (Cl/F) and volume of distribution at steady state (V dss/F) and during beta-phase (V d beta/F). The area under plasma concentration-time curve (AUC), maximum plasma concentration (C max) and the amount of unchanged aprindine excreted in the urine increased in a non-linear fashion with the increase in dose. The t 1/2 beta after multiple oral doses showed a 3-fold increase over the single dose value. These results indicate that aprindine shows dose-dependent non-linear kinetics.

Adult↗
PubMed1983

The incidence of simple renal cyst by computed tomography.

Five hundred and forty-two abdominal computed tomography (CT) scans, including the kidneys, were reviewed to investigate the incidence of simple renal cysts. Increasing frequency with age was clearly demonstrated. The incidence in patients 50 years of age and over was at least 27%. Two thirds of simple renal cysts were 2 cm or less in diameter. Cysts were usually observed as exo-endoparenchymal or endoparenchymal lesions on CT.

Adolescent↗
PubMed1983

[Cholecystography].

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Administration, Oral↗
PubMed1981

Metabolism of 1-hexylcarbamoyl-5-fluorouracil (HCFU), a new antitumour agent, in rats, rabbits and dogs.

1. 1-Hexylcarbamoyl-5-fluoro[6-14C]uracil (14C-HCFU) administered orally to rats, rabbits and dogs at a dose of 20 mg/kg was well absorbed and rapidly excreted via the kidney. 2. HCFU was extensively biotransformed, and its six metabolites including two new metabolites were detected in plasma and urine of all three species. Two new metabolites were identified by spectral analysis as 1-(5-hydroxyhexylcarbamoyl)5-fluorouracil and 1-(5-oxohexylcarbamoyl)-5-fluorouracil. 3. The metabolic pathways of HCFU in the three species involved oxidations and scission of the side-chain with successive degradation of the fluorouracil (FU) released. 4. The two main routes of oxidations of the side chain were omega-oxidation and omega-1-oxidation. Rats metabolized HCFU preferentially by the former reaction, while in rabbits and dogs the latter reaction predominated.

Absorption↗
PubMed1978

Metabolic fate of 1-hexylcarbamoyl-5-fluorouracil in rats.

1. The metabolic fate of a new antitumour agent, 1-hexylcarbamoyl-5-fluoro [6-14C]uracil (14C-HCFU) in rats after oral administration was compared with that of 5-fluoro[6-14C]uracil (14C-FU). 2. Tissue radioactivity reached a max. 1 to 3 h after administration of 14C-HCFU and 0.5 h after 14C-FU. 3. Both drugs were excreted rapidly, mostly in urine. Expired 14CO2 from 14C-HCFU was significantly less than that from 14C-FU. 4. Unchanged FU was not detected in plasma 3 h after administration of 14C-FU, whereas FU was detected in plasma 5 h after 14C-HCFU. The pyrimidine ring of 14C-HCFU might be degradated more slowly than that of 14C-FU. 5. 1-(5-Carboxypentylcarbamoyl)-5-fluorouracil and 1-(3-carboxypropylcarbamoyl)-5-fluorouracil were identified as the major urinary metabolites of 14C-HCFU.

Animals↗