Pharmacokinetic Studies of the Inhibition of Glucuronization of Pentazocine by Salicylamide
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The serum concentrations of unchanged and glucuronized drug were determined after intravenous injection of pentazocine (PA) in rabbits. A compartment model isolating the liver from the central compartment was proposed to explain the observed time courses of the concentration, and the resulting convolution equation was M (t)=∫^1_0D (t-θ) G (θ) dθ, where M (t) and D (t) are the serum concentrations of glucuronized PA and unchanged PA after intravenous injection, respectively. The weight function, G (t), which represents the response for a pulse input of glucuronized PA was estimated to be G (t)=0.00933 (e^<-0.00818t>-e^<-0.223t>) (min^<-1>). The simultaneous intravenous administration of salicylamide (SAM) had no effect on the glucuronization of PA in serum. The serum concentration of glucuronized PA calculated by numerical convolution of G (t) and the published serum concentration of unchanged PA after oral administration represents that of glucuronide produced from the unchanged PA which escaped the first-pass effect. This calculated value was far below the published serum concentration of glucuronized PA after oral administration, and the difference represents the glucuronized PA produced by the first-pass effect. The area under the concentration-versus-time curve of glucuronized PA produced by the first-pass effect was 274 times larger than that of glucuronized PA produced from unchanged PA in the serum. Simultaneous oral administration of SAM only inhibits the first-pass effect.
収録刊行物
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- Chemical & pharmaceutical bulletin
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Chemical & pharmaceutical bulletin 33 (8), 3436-3439, 1985-08-25
公益社団法人日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1573105977298913280
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- NII論文ID
- 110003625844
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- NII書誌ID
- AA00602100
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- ISSN
- 00092363
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- 本文言語コード
- en
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- データソース種別
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- CiNii Articles