抗炎症剤4-Butyl-4-(β-carboxypropionyloxymethyl)-1,2-diphenyl-3,5-pyrazolidinedione(Suxibuzone)の生体内動態(第1報)経口投与後の血漿中濃度および尿中排泄

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概要

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• The biological fate of 4-butyl-4-(β-carboxypropionyl-oxymethyl)-1,2-diphenyl-3,5-pyrazolidinedione (Suxibuzone, SB) was compared with that of phenylbutazone (PB) in rats, rabbits, beagle dogs and rhesus monkeys. The results obtained were as follows ; 1) When SB was administered orally, the main metabolites in the plasma were PB, oxyphenbutazone (Oxy-PB) and γ-hydroxyphenylbutazone (γ-Hydroxy-PB) in all species, though species differences were observed in the maximum plasma levels of the respective metabolites. Only in dogs and monkeys, was a small amount of SB detected in the plasma during the early time of dosing. 2) The metabolites and their maximum levels in plasma after the administration of SB were almost identical with those observed after the administration of PB. 3) After administration of SB, the main metabolites found in urine were PB, Oxy-PB, γ-Hydroxy-PB and their conjugates in all species, while species differences were observed in the percent excreted. In the dogs and monkeys, urinary excretion as the form of SB and 4-hydroxymethylphenylbutazone (4-HM-PB) glucuronides was observed in small amount for 0-12 hours. 4) There were no significant differences in the metabolites and their excreted percent in urine between SB and PB administration. 5) Differences between male and female in maximum plasma levels of PB and γ-Hydroxy-PB and in urinary excreted percent of γ-Hydroxy-PB were observed only in rats. 6) Species differences were observed in esterase activity on SB in vitro. 7) SB was bound to the albumin fraction as in the case of PB, but its binding percent was about 1/2 lower than that of PB. 8) SB showed anti-edematous action on carrageenin-induced edema and its activity was almost similar to that of PB. Anti-edematous activity of Oxy-PB was weaker than that of SB and γ-Hydroxy-PB had no effect on its action.

• 社団法人日本薬学会の論文
• 1979-12-25

著者

• 赤沢 明

  大鵬薬品工業株式会社技術研究部

• 安田 行寛

  大鵬薬品工業株式会社技術研究部

• 新藤 恭司

  大鵬薬品工業(株) 代謝分析研究所

• 神田 敦弘

  大鵬薬品工業株式会社薬理研究所

• 神田 敦弘

  大鵬薬品工業株式会社技術本部研究部

• 多比良 和基

  大鵬薬品工業株式会社技術本部研究部

• 三谷 鳴夫

  大鵬薬品工業株式会社技術本部研究部

• 赤沢 明

  大鵬薬品工業株式会社技術本部研究部

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