Indomethacin (I) (1.56-6.25 mg./kg.) and phenylbutazone (II) (25-100 mg./kg.) were administered by gavage alone or in combination with aspirin (100 mg./kg. by gavage) to rats with carrageenan (III)-induced foot edema.Aspirin, I, or II significantly inhibited (by ∼40-60%) III-induced edema in all experiments, and the degree of inhibition by I or II was dose-related.The combined administration of aspirin with I did not significantly change the inhibition obtained when the compounds were given sep.The combined administration of aspirin with II (25 mg./kg.) increased by ∼15-20% the inhibition of III-induced edema obtained with aspirin alone, but no significant differences were obtained with II at the high dosage when combined with aspirin.11 references.

01 Aug 1998·Journal of Chromatography B: Biomedical Sciences and Applications

Development of a sensitive liquid chromatography–electrospray ionization tandem mass spectrometry method for the measurement of 7-cyanoquinocarcinol in human plasma

Article

Author: Satoshi Kobayashi ; Michio Takashima ; Tohru Yasuzawa ; Takashi Kuwabara ; Eiichi Fuse ; Kazuo Yamaguchi

A sensitive method for the determination of an anti-cancer agent, DX-52-1 (7-cyanoquinocarcinol, I) and quinocarmycin (II) which is formed from I either by metabolism or degradation, in human plasma has been developed utilising liquid chromatography electrospray-ionization tandem mass spectrometry (LC-ESI-MS-MS). The procedure involves solid-phase extraction at pH 2 and low temperature (4-6 degrees C) to prevent the decomposition of I to II, the separation by reversed-phase HPLC and the multiple reaction monitoring (MRM) by ESI-MS-MS. The mean precision and accuracy at the lower limit of quantitation (LLOQ) of I, 0.25 ng ml(-1), were 8.7% and - 10.8%, respectively. Since an interfering peak eluting slightly earlier than II was observed on the HPLC of blank plasma, the LLOQ of II was set at 5 ng ml(-1) where the mean precision and accuracy were 15.6% and -9.8%. The results suggested that the method is useful for the simultaneous monitoring of I and II in the clinical trials of I.

01 Jan 1985·Chemical and Pharmaceutical BulletinQ4 · MEDICINE

Pharmacokinetic studies of the inhibition of glucuronization of pentazocine by salicylamide.

Q4 · MEDICINE

Article

Author: Koshiro Umemura ; Toshihiro Hayashi ; Nagahiko Yumita ; Kazuo Kigasawa ; Ryuichiro Nishigaki

The serum concentrations of unchanged and glucuronized drug were determined after i.v. injection of pentazocine (I) [359-83-1] 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) = ∫₀^tD(t - θ)G(θ)dθ, where M(t) and D(t) are the serum concentrations of glucuronized I and unchanged I after i.v. injection, resp.The weight function, G(t), which represents the response for a pulse input of glucuronized I was estimated to be G(t) = 0.00933 (e^-0.00818t - e^-0.223t) (min^-1).The simultaneous i.v. administration of salicylamide (II) [65-45-2] had no effect on the glucuronization of I in serum.The serum concentration of glururonized I calculated by numerical convolution of G(t) and the published serum concentration of unchanged I after oral administration represents that of glucuronide produced from the unchanged I which escaped the 1st-pass effect.This calculated value was far below the published serum concentration of glucuronized I after oral administration, and the difference represents the glucuronized I produced by the 1st-pass effect.The area under the concentration-vs.-time curve of glucuronized I was 274 times larger than that of glucuronized I produced from unchanged I in the serum.Simultaneous oral administration of II only inhibits the 1st-pass effect.

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