The Experts below are selected from a list of 75 Experts worldwide ranked by ideXlab platform
Norio Awata - One of the best experts on this subject based on the ideXlab platform.
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Contributions of Various Serum Proteins to the Binding of Prasterone Sulfate in Humans
Chemical & Pharmaceutical Bulletin, 1992Co-Authors: Takanori Sakai, Yoshiko Adachi, Mika Yatomi, Norio AwataAbstract:The binding of Prasterone Sulfate (PS) in human plasma was investigated. Binding percentages of PS to human plasma, human serum albumin (HSA), human alpha 1-acid glycoprotein (AGP) and human gamma-globulin (GGL) were independent of the PS concentration between 0.1 and 8.0 micrograms/ml. The mean binding percentages were 99.1% for human plasma, 98.3% for HSA, 12.6% for AGP and 8.1% for GGL. Though PS is an acidic drug, binding of PS to AGP was observed. From the binding index, it was found that PS mainly bound to HSA in human plasma and that the contributions of AGP and GGL to PS in plasma were negligible.
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the biological fate of sodium Prasterone Sulfate after vaginal administration i absorption and excretion in rats
Journal of pharmacobio-dynamics, 1992Co-Authors: Minoru Sakaguchi, Takanori Sakai, Yoshiko Adachi, Tsuneo Kawashima, Norio AwataAbstract:The absorption and excretion of sodium Prasterone Sulfate (PS) (sodium dehydroepiandrosterone Sulfate) were studied in rats after vaginal administration of 14C-PS. In late pregnant rats, maximum plasma level (Cmax) appeared at 2-4h after dosing and both Cmax and the area under the plasma concentration-time curve (AUC) increased proportionally with increased dose up to 4.0mg/kg. The radioactivity administered was almost completely recovered from urine and feces during a 72h postdosing period. The percentages of radioactivity excreted in urine and feces were 58% and 40% of the dose, respectively. The biliary excretion was 46% of the dose within 48h and about half of the radioactive biliary excreta entered the enterohepatic circulation system. The vaginal absorption of PS was markedly affected by the estrous cycle stage and the progress of pregnancy. The vaginal absorption of PS was predominant at metestrus and diestrus and during late pregnancy.
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the biological fate of sodium Prasterone Sulfate after vaginal administration ii distribution after single and multiple administration to pregnant rats
Drug Metabolism and Pharmacokinetics, 1992Co-Authors: Takanori Sakai, Yoshiko Adachi, Minoru Sakaguchi, Tsuneo Kawashima, Norio AwataAbstract:The distribution of sodium Prasterone Sulfate (PS, a common name is sodium dehydroepiandrosterone Sulfate) was studied in pregnant rats after single and multiple vaginal administration of 14C-PS. The radioactivity was high in the vagina, liver and kidney, and low in the central nervous system and fat tissues after single vaginal administration. During multiple vaginal administration, plasma levels of radioactivity and the rate of urinary and fecal excretion of radioactivity were almost constant. Tissue distribution of radioactivity after multiple vaginal administration was similar to that after single vaginal administration. There were no tissues showing a pronounced retaining of the radioactivity after the multiple vaginal administration. Unchanged PS and its metabolites were transported to the cervix of uterus being an action site for PS and its some metabolites, to much higher extent after vaginal administration than after intravenous administration.
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the biological fate of sodium Prasterone Sulfate after vaginal administration iii metabolism in pregnant rats
Drug Metabolism and Pharmacokinetics, 1992Co-Authors: Kazunobu Noumi, Takanori Sakai, Tsuneo Kawashima, Naoko Yamazaki, Norio AwataAbstract:The metabolism of sodium Prasterone Sulfate (PS) was investigated in pregnant rats after vaginal administration. Major metabolites in rat urine and bile were identified by means of thin layer chromatography/secondary ionization mass spectrometry and capillary gas chromatography/mass spectrometry. The urinary and biliary excretion of identified metabolites according to above menntioned methods were determined after vaginal administration of 14C-labelled PS. Main metabolites in the urine and bile were androst-5-ene-3β, 17β-diol 3-Sulfate (3β, 17β-diol-MS) and androst-5-ene-3β, 17β-diol 3, 17-diSulfate, respectively. Androst-5-ene-3β, 7α-diol 3-Sulfate, androst-5-ene-3β, 7β-diol 3-Sulfate and androst-5-ene-3β, 7α, 17β-triol 3-Sulfate were also identified as minor metabolites in the urine and/or bile. Furthermore, the excretion ratio of unchanged PS in the urine and bile after vaginal administration was lower than that after intravenous one. PS was also converted to 3β, 17β-diol-MS during the incubation with the 9000 × g supernatant of the vaginal membrane including uterine cervix. These results suggest that a part of PS was metabolized to 3β, 17β-diol-MS during the process of the absorption after vaginal administration.
Takanori Sakai - One of the best experts on this subject based on the ideXlab platform.
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Contributions of Various Serum Proteins to the Binding of Prasterone Sulfate in Humans
Chemical & Pharmaceutical Bulletin, 1992Co-Authors: Takanori Sakai, Yoshiko Adachi, Mika Yatomi, Norio AwataAbstract:The binding of Prasterone Sulfate (PS) in human plasma was investigated. Binding percentages of PS to human plasma, human serum albumin (HSA), human alpha 1-acid glycoprotein (AGP) and human gamma-globulin (GGL) were independent of the PS concentration between 0.1 and 8.0 micrograms/ml. The mean binding percentages were 99.1% for human plasma, 98.3% for HSA, 12.6% for AGP and 8.1% for GGL. Though PS is an acidic drug, binding of PS to AGP was observed. From the binding index, it was found that PS mainly bound to HSA in human plasma and that the contributions of AGP and GGL to PS in plasma were negligible.
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the biological fate of sodium Prasterone Sulfate after vaginal administration i absorption and excretion in rats
Journal of pharmacobio-dynamics, 1992Co-Authors: Minoru Sakaguchi, Takanori Sakai, Yoshiko Adachi, Tsuneo Kawashima, Norio AwataAbstract:The absorption and excretion of sodium Prasterone Sulfate (PS) (sodium dehydroepiandrosterone Sulfate) were studied in rats after vaginal administration of 14C-PS. In late pregnant rats, maximum plasma level (Cmax) appeared at 2-4h after dosing and both Cmax and the area under the plasma concentration-time curve (AUC) increased proportionally with increased dose up to 4.0mg/kg. The radioactivity administered was almost completely recovered from urine and feces during a 72h postdosing period. The percentages of radioactivity excreted in urine and feces were 58% and 40% of the dose, respectively. The biliary excretion was 46% of the dose within 48h and about half of the radioactive biliary excreta entered the enterohepatic circulation system. The vaginal absorption of PS was markedly affected by the estrous cycle stage and the progress of pregnancy. The vaginal absorption of PS was predominant at metestrus and diestrus and during late pregnancy.
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the biological fate of sodium Prasterone Sulfate after vaginal administration ii distribution after single and multiple administration to pregnant rats
Drug Metabolism and Pharmacokinetics, 1992Co-Authors: Takanori Sakai, Yoshiko Adachi, Minoru Sakaguchi, Tsuneo Kawashima, Norio AwataAbstract:The distribution of sodium Prasterone Sulfate (PS, a common name is sodium dehydroepiandrosterone Sulfate) was studied in pregnant rats after single and multiple vaginal administration of 14C-PS. The radioactivity was high in the vagina, liver and kidney, and low in the central nervous system and fat tissues after single vaginal administration. During multiple vaginal administration, plasma levels of radioactivity and the rate of urinary and fecal excretion of radioactivity were almost constant. Tissue distribution of radioactivity after multiple vaginal administration was similar to that after single vaginal administration. There were no tissues showing a pronounced retaining of the radioactivity after the multiple vaginal administration. Unchanged PS and its metabolites were transported to the cervix of uterus being an action site for PS and its some metabolites, to much higher extent after vaginal administration than after intravenous administration.
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the biological fate of sodium Prasterone Sulfate after vaginal administration iii metabolism in pregnant rats
Drug Metabolism and Pharmacokinetics, 1992Co-Authors: Kazunobu Noumi, Takanori Sakai, Tsuneo Kawashima, Naoko Yamazaki, Norio AwataAbstract:The metabolism of sodium Prasterone Sulfate (PS) was investigated in pregnant rats after vaginal administration. Major metabolites in rat urine and bile were identified by means of thin layer chromatography/secondary ionization mass spectrometry and capillary gas chromatography/mass spectrometry. The urinary and biliary excretion of identified metabolites according to above menntioned methods were determined after vaginal administration of 14C-labelled PS. Main metabolites in the urine and bile were androst-5-ene-3β, 17β-diol 3-Sulfate (3β, 17β-diol-MS) and androst-5-ene-3β, 17β-diol 3, 17-diSulfate, respectively. Androst-5-ene-3β, 7α-diol 3-Sulfate, androst-5-ene-3β, 7β-diol 3-Sulfate and androst-5-ene-3β, 7α, 17β-triol 3-Sulfate were also identified as minor metabolites in the urine and/or bile. Furthermore, the excretion ratio of unchanged PS in the urine and bile after vaginal administration was lower than that after intravenous one. PS was also converted to 3β, 17β-diol-MS during the incubation with the 9000 × g supernatant of the vaginal membrane including uterine cervix. These results suggest that a part of PS was metabolized to 3β, 17β-diol-MS during the process of the absorption after vaginal administration.
Tsuneo Kawashima - One of the best experts on this subject based on the ideXlab platform.
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the biological fate of sodium Prasterone Sulfate after vaginal administration i absorption and excretion in rats
Journal of pharmacobio-dynamics, 1992Co-Authors: Minoru Sakaguchi, Takanori Sakai, Yoshiko Adachi, Tsuneo Kawashima, Norio AwataAbstract:The absorption and excretion of sodium Prasterone Sulfate (PS) (sodium dehydroepiandrosterone Sulfate) were studied in rats after vaginal administration of 14C-PS. In late pregnant rats, maximum plasma level (Cmax) appeared at 2-4h after dosing and both Cmax and the area under the plasma concentration-time curve (AUC) increased proportionally with increased dose up to 4.0mg/kg. The radioactivity administered was almost completely recovered from urine and feces during a 72h postdosing period. The percentages of radioactivity excreted in urine and feces were 58% and 40% of the dose, respectively. The biliary excretion was 46% of the dose within 48h and about half of the radioactive biliary excreta entered the enterohepatic circulation system. The vaginal absorption of PS was markedly affected by the estrous cycle stage and the progress of pregnancy. The vaginal absorption of PS was predominant at metestrus and diestrus and during late pregnancy.
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the biological fate of sodium Prasterone Sulfate after vaginal administration ii distribution after single and multiple administration to pregnant rats
Drug Metabolism and Pharmacokinetics, 1992Co-Authors: Takanori Sakai, Yoshiko Adachi, Minoru Sakaguchi, Tsuneo Kawashima, Norio AwataAbstract:The distribution of sodium Prasterone Sulfate (PS, a common name is sodium dehydroepiandrosterone Sulfate) was studied in pregnant rats after single and multiple vaginal administration of 14C-PS. The radioactivity was high in the vagina, liver and kidney, and low in the central nervous system and fat tissues after single vaginal administration. During multiple vaginal administration, plasma levels of radioactivity and the rate of urinary and fecal excretion of radioactivity were almost constant. Tissue distribution of radioactivity after multiple vaginal administration was similar to that after single vaginal administration. There were no tissues showing a pronounced retaining of the radioactivity after the multiple vaginal administration. Unchanged PS and its metabolites were transported to the cervix of uterus being an action site for PS and its some metabolites, to much higher extent after vaginal administration than after intravenous administration.
-
the biological fate of sodium Prasterone Sulfate after vaginal administration iii metabolism in pregnant rats
Drug Metabolism and Pharmacokinetics, 1992Co-Authors: Kazunobu Noumi, Takanori Sakai, Tsuneo Kawashima, Naoko Yamazaki, Norio AwataAbstract:The metabolism of sodium Prasterone Sulfate (PS) was investigated in pregnant rats after vaginal administration. Major metabolites in rat urine and bile were identified by means of thin layer chromatography/secondary ionization mass spectrometry and capillary gas chromatography/mass spectrometry. The urinary and biliary excretion of identified metabolites according to above menntioned methods were determined after vaginal administration of 14C-labelled PS. Main metabolites in the urine and bile were androst-5-ene-3β, 17β-diol 3-Sulfate (3β, 17β-diol-MS) and androst-5-ene-3β, 17β-diol 3, 17-diSulfate, respectively. Androst-5-ene-3β, 7α-diol 3-Sulfate, androst-5-ene-3β, 7β-diol 3-Sulfate and androst-5-ene-3β, 7α, 17β-triol 3-Sulfate were also identified as minor metabolites in the urine and/or bile. Furthermore, the excretion ratio of unchanged PS in the urine and bile after vaginal administration was lower than that after intravenous one. PS was also converted to 3β, 17β-diol-MS during the incubation with the 9000 × g supernatant of the vaginal membrane including uterine cervix. These results suggest that a part of PS was metabolized to 3β, 17β-diol-MS during the process of the absorption after vaginal administration.
Yoshiko Adachi - One of the best experts on this subject based on the ideXlab platform.
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Contributions of Various Serum Proteins to the Binding of Prasterone Sulfate in Humans
Chemical & Pharmaceutical Bulletin, 1992Co-Authors: Takanori Sakai, Yoshiko Adachi, Mika Yatomi, Norio AwataAbstract:The binding of Prasterone Sulfate (PS) in human plasma was investigated. Binding percentages of PS to human plasma, human serum albumin (HSA), human alpha 1-acid glycoprotein (AGP) and human gamma-globulin (GGL) were independent of the PS concentration between 0.1 and 8.0 micrograms/ml. The mean binding percentages were 99.1% for human plasma, 98.3% for HSA, 12.6% for AGP and 8.1% for GGL. Though PS is an acidic drug, binding of PS to AGP was observed. From the binding index, it was found that PS mainly bound to HSA in human plasma and that the contributions of AGP and GGL to PS in plasma were negligible.
-
the biological fate of sodium Prasterone Sulfate after vaginal administration i absorption and excretion in rats
Journal of pharmacobio-dynamics, 1992Co-Authors: Minoru Sakaguchi, Takanori Sakai, Yoshiko Adachi, Tsuneo Kawashima, Norio AwataAbstract:The absorption and excretion of sodium Prasterone Sulfate (PS) (sodium dehydroepiandrosterone Sulfate) were studied in rats after vaginal administration of 14C-PS. In late pregnant rats, maximum plasma level (Cmax) appeared at 2-4h after dosing and both Cmax and the area under the plasma concentration-time curve (AUC) increased proportionally with increased dose up to 4.0mg/kg. The radioactivity administered was almost completely recovered from urine and feces during a 72h postdosing period. The percentages of radioactivity excreted in urine and feces were 58% and 40% of the dose, respectively. The biliary excretion was 46% of the dose within 48h and about half of the radioactive biliary excreta entered the enterohepatic circulation system. The vaginal absorption of PS was markedly affected by the estrous cycle stage and the progress of pregnancy. The vaginal absorption of PS was predominant at metestrus and diestrus and during late pregnancy.
-
the biological fate of sodium Prasterone Sulfate after vaginal administration ii distribution after single and multiple administration to pregnant rats
Drug Metabolism and Pharmacokinetics, 1992Co-Authors: Takanori Sakai, Yoshiko Adachi, Minoru Sakaguchi, Tsuneo Kawashima, Norio AwataAbstract:The distribution of sodium Prasterone Sulfate (PS, a common name is sodium dehydroepiandrosterone Sulfate) was studied in pregnant rats after single and multiple vaginal administration of 14C-PS. The radioactivity was high in the vagina, liver and kidney, and low in the central nervous system and fat tissues after single vaginal administration. During multiple vaginal administration, plasma levels of radioactivity and the rate of urinary and fecal excretion of radioactivity were almost constant. Tissue distribution of radioactivity after multiple vaginal administration was similar to that after single vaginal administration. There were no tissues showing a pronounced retaining of the radioactivity after the multiple vaginal administration. Unchanged PS and its metabolites were transported to the cervix of uterus being an action site for PS and its some metabolites, to much higher extent after vaginal administration than after intravenous administration.
Minoru Sakaguchi - One of the best experts on this subject based on the ideXlab platform.
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the biological fate of sodium Prasterone Sulfate after vaginal administration i absorption and excretion in rats
Journal of pharmacobio-dynamics, 1992Co-Authors: Minoru Sakaguchi, Takanori Sakai, Yoshiko Adachi, Tsuneo Kawashima, Norio AwataAbstract:The absorption and excretion of sodium Prasterone Sulfate (PS) (sodium dehydroepiandrosterone Sulfate) were studied in rats after vaginal administration of 14C-PS. In late pregnant rats, maximum plasma level (Cmax) appeared at 2-4h after dosing and both Cmax and the area under the plasma concentration-time curve (AUC) increased proportionally with increased dose up to 4.0mg/kg. The radioactivity administered was almost completely recovered from urine and feces during a 72h postdosing period. The percentages of radioactivity excreted in urine and feces were 58% and 40% of the dose, respectively. The biliary excretion was 46% of the dose within 48h and about half of the radioactive biliary excreta entered the enterohepatic circulation system. The vaginal absorption of PS was markedly affected by the estrous cycle stage and the progress of pregnancy. The vaginal absorption of PS was predominant at metestrus and diestrus and during late pregnancy.
-
the biological fate of sodium Prasterone Sulfate after vaginal administration ii distribution after single and multiple administration to pregnant rats
Drug Metabolism and Pharmacokinetics, 1992Co-Authors: Takanori Sakai, Yoshiko Adachi, Minoru Sakaguchi, Tsuneo Kawashima, Norio AwataAbstract:The distribution of sodium Prasterone Sulfate (PS, a common name is sodium dehydroepiandrosterone Sulfate) was studied in pregnant rats after single and multiple vaginal administration of 14C-PS. The radioactivity was high in the vagina, liver and kidney, and low in the central nervous system and fat tissues after single vaginal administration. During multiple vaginal administration, plasma levels of radioactivity and the rate of urinary and fecal excretion of radioactivity were almost constant. Tissue distribution of radioactivity after multiple vaginal administration was similar to that after single vaginal administration. There were no tissues showing a pronounced retaining of the radioactivity after the multiple vaginal administration. Unchanged PS and its metabolites were transported to the cervix of uterus being an action site for PS and its some metabolites, to much higher extent after vaginal administration than after intravenous administration.