The Biological Fate of 4-Butyl-4-(&amp;beta;-carboxypropionyloxymethyl)-1, 2-diphenyl-3, 5-pyrazolidinedione (Suxibuzone), Antiinflammatory Drug. II. The Biological Fate of Suxibuzone (SB) after Daily Oral Administration

Taira, Kazuki; Yasuda, Yukihiro; Shindo, Takashi; Mitani, Naruo; Akazawa, Akira

doi:10.1248/yakushi1947.100.3_272

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“…In humans and animals, suxibuzone is metabolised to PBZ and OPBZ following intravenous or oral administration ( Shindo et al ., 1979 ; Taira et al ., 1980 ; Delbeke et al ., 1993 ); however, some important pharmacokinetic differences between species have been reported. It has been shown that SBZ is immediately metabolised to PBZ when administered orally to rats, rabbits, dogs, monkeys and humans, though in humans, dogs and monkeys only a small amount of SBZ could be detected in plasma during the early time of dosing.…”

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confidence: 99%

Pharmacokinetics and bioequivalence of two suxibuzone oral dosage forms in horses

Jaraiz

Rodríguez

Andrés

et al. 1999

Vet Pharm & Therapeutics

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A disposition and bioequivalence study with a suxibuzone granulated and a suxibuzone paste oral formulation was performed in horses. Suxibuzone (SBZ) is a nonsteroidal anti-inflammatory drug, which was administered to horses (n = 6) at a dosage of 19 mg/kg bwt by the oral route (p.o.) in a two period cross-over design. Suxibuzone is very rapidly transformed into its main active metabolites, phenylbutazone (PBZ) and oxyphenbutazone (OPBZ). Therefore plasma and synovial fluid concentrations of SBZ, PBZ and OPBZ were simultaneously measured by a sensitive and specific high-performance liquid chromatographic method. The pharmacokinetic parameters were determined by noncompartmental analysis. Suxibuzone could not be detected in any plasma and synovial fluid samples (< 0.04 microgram/mL). Plasma PBZ and OPBZ concentrations were detected between 30 min and 72 h after granulate and paste administration. Mean plasma concentration of PBZ peaked at 5 h (34.5 +/- 6.7 micrograms/mL) and at 7 h (38.8 +/- 8.4 micrograms/mL), and mean area under the concentration-time curve (AUC0-->LOQ) was 608.0 +/- 162.2 micrograms.h/mL and 656.6 +/- 149.7 micrograms.h/mL after granulate and paste administration, respectively. Mean plasma concentration of OPBZ increased to 5-6.7 micrograms/mL, with the maximum concentration (Cmax) appearing between 9 and 12 h after administration of both formulations. The AUCs0-->LOQ for OPBZ were also similar (141.8 +/- 48.3 micrograms.h/mL granulate vs. 171.4 +/- 45.0 micrograms.h/mL paste). It was concluded that the suxibuzone products were bioequivalent with respect to PBZ. For OPBZ, the 95% confidence intervals of the pharmacokinetic parameters were within the acceptable range of 80-125%. The paste formulation provided greater bioavailability of PBZ and OPBZ.

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Section: Introductionmentioning

confidence: 99%

Pharmacokinetics and bioequivalence of two suxibuzone oral dosage forms in horses

Jaraiz

Rodríguez

Andrés

et al. 1999

Vet Pharm & Therapeutics

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Disposition and tolerance of suxibuzone in horses

Jaraiz

Rodríguez

Andrés

et al. 1999

Equine Veterinary Journal

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Summary Suxibuzone (SBZ), a nonsteroidal anti‐inflammatory drug, was administered to 6 horses at a dose rate of 7.5 mg/kg bwt by intravenous (i.v.) route. Plasma and synovial fluid concentrations of suxibuzone and its main active metabolites, phenylbutazone (PBZ) and oxyphenbutazone (OPBZ), were measured simultaneously by a sensitive and specific high‐performance liquid chromatographic method. The pharmacokinetic parameters were determined by noncompartmental analysis. Plasma SBZ concentrations rapidly decreased and were not detectable beyond 20 min after treatment. The parent drug was not detected in any synovial fluid samples. Average maximum plasma concentrations of PBZ (16.43 μg/ml) and OPBZ (2.37 μg/ml) were attained at 0.76 and 7.17 h, respectively. The mean residence time (MRT) of PBZ was 6.96 h in plasma. Oxyphenbutazone plasma concentrations were below those reached by phenylbutazone during the first 12 h after suxibuzone administration, even though its values were detectable for at least 24 h (MRT = 10.65 h). Plasma concentrations of PBZ and OPBZ exceeding EC50 and IC50 of TXB2 and PGE2 were reached by at least 12 h. Synovial fluid concentrations of PBZ and OPBZ were 2.87 ± 0.37 μg/ml and 0.97 ± 0.08 ug/ml at 9 h after suxibuzone administration and exceeded IC50 of PGE2 for at least this time. In the present study, suxibuzone was well tolerated following i.v. injection.

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The Biological Fate of 4-Butyl-4-(β-carboxypropionyloxymethyl)-1, 2-diphenyl-3, 5-pyrazolidinedione (Suxibuzone), Antiinflammatory Drug. II. The Biological Fate of Suxibuzone (SB) after Daily Oral Administration

Cited by 2 publications

References 0 publications

Pharmacokinetics and bioequivalence of two suxibuzone oral dosage forms in horses

Pharmacokinetics and bioequivalence of two suxibuzone oral dosage forms in horses

Disposition and tolerance of suxibuzone in horses

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