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Mayós Servet Irene - One of the best experts on this subject based on the ideXlab platform.
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Perfil cinético de la suxibuzona para su uso en la clínica de équidos : estudio comparado con la fenilbutazona /
Bellaterra : Universitat Autònoma de Barcelona, 2005Co-Authors: Mayós Servet IreneAbstract:Consultable des del TDXTítol obtingut de la portada digitalitzadaLa Suxibuzona es un antiinflamatorio no esteroideo utilizado en la clínica equina. Químicamente se define como éster de la Fenilbutazona. Ambas moléculas están estrechamente relacionadas debido a que la Suxibuzona se metaboliza rápidamente a Fenilbutazona, ya sea al administrarla por vía oral como por vía intravenosa en el caballo. El objetivo del presente estudio es el de evaluar la relación del perfil de disponibilidad de la administración de la Fenilbutazona y de su principal metabolito la Oxifenbutazona tras la administración de la Suxibuzona o de Fenilbutazona a dosis equimoleculares, tanto en caballos en ayunas como en animales que siguen su dieta habitual. Asimismo se ha estudiado la disponibilidad de estas moléculas en el líquido sinovial evaluando su capacidad para desarrollar su efecto antiinflamatorio en las articulaciones. En una primera fase experimental se administraron a 19 caballos, siguiendo un diseño cruzado, 6.25 mg/kg de Suxibuzona (A) y 4.4 mg/kg de Fenilbutazona (B) por vía oral en ayunas. Tras realizar una serie de extracciones seriadas de plasma, se cuantificaron simultáneamente las concentraciones plasmáticas y en líquido sinovial de Suxibuzona y de sus principales metabolitos activos (Fenilbutazona y Oxifenbutazona) mediante un método de cromatografía líquida (HPLC) previamente validado. Se calcularon los parámetros farmacocinéticos siguiendo un análisis no-compartimental. No se detectó Suxibuzona en ninguna muestra ensayada. Los principales parámetros farmacocinéticos obtenidos para las concentraciones plasmáticas de Fenilbutazona fueron (media ± D.S.): Tmax (h) 4.9±3.1 (A), 3.2±2.7 (B); Cmax (µg/mL) 10.2±2.2 (A), 15.5 ± 3.6 (B); MRT0®t (h) 10.0±1.1 (A), 9.2±1.3 (B); T½(h) 7.5±1.8 (A), 7.2±1.5 (B); AUC0®t (µg.h/mL) 145.1±35.0 (A), 179.1±36.4 (B); AUC0®¥ (µg.h/mL) 172.6±44.7 (A), 206.2±45.5 (B). Obteniendo una disponibilidad relativa (FA/B) de 0.82±0.16 y para la Oxifenbutazona fueron (media ± D.S.): Tmax (h) 15.3±2.8 (A), 13.8±4.8 (B); Cmax (µg/mL) 2.1±0.4 (A), 2.5±0.6 (B); MRT0®t (h) 13.5±0.9 (A), 13.1±1.0 (B); AUC0®t (µg.h/mL) 34.9±6.4 (A), 42.9±9.2 (B); FA/B 0.85±0.26. Al comparar la administración oral de la Suxibuzona (A) con la de Fenilbutazona (B) sólo se han observado diferencias significativas (p
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Perfil cinético de la suxibuzona para su uso en la clínica de équidos
'Universitat Autonoma de Barcelona', 2002Co-Authors: Mayós Servet IreneAbstract:La Suxibuzona es un antiinflamatorio no esteroideo utilizado en la clínica equina. Químicamente se define como éster de la Fenilbutazona. Ambas moléculas están estrechamente relacionadas debido a que la Suxibuzona se metaboliza rápidamente a Fenilbutazona, ya sea al administrarla por vía oral como por vía intravenosa en el caballo.El objetivo del presente estudio es el de evaluar la relación del perfil de disponibilidad de la administración de la Fenilbutazona y de su principal metabolito la Oxifenbutazona tras la administración de la Suxibuzona o de Fenilbutazona a dosis equimoleculares, tanto en caballos en ayunas como en animales que siguen su dieta habitual. Asimismo se ha estudiado la disponibilidad de estas moléculas en el líquido sinovial evaluando su capacidad para desarrollar su efecto antiinflamatorio en las articulaciones.En una primera fase experimental se administraron a 19 caballos, siguiendo un diseño cruzado, 6.25 mg/kg de Suxibuzona (A) y 4.4 mg/kg de Fenilbutazona (B) por vía oral en ayunas. Tras realizar una serie de extracciones seriadas de plasma, se cuantificaron simultáneamente las concentraciones plasmáticas y en líquido sinovial de Suxibuzona y de sus principales metabolitos activos (Fenilbutazona y Oxifenbutazona) mediante un método de cromatografía líquida (HPLC) previamente validado. Se calcularon los parámetros farmacocinéticos siguiendo un análisis no-compartimental. No se detectó Suxibuzona en ninguna muestra ensayada. Los principales parámetros farmacocinéticos obtenidos para las concentraciones plasmáticas de Fenilbutazona fueron (media ± D.S.): Tmax (h) 4.9±3.1 (A), 3.2±2.7 (B); Cmax (µg/mL) 10.2±2.2 (A), 15.5 ± 3.6 (B); MRT0®t (h) 10.0±1.1 (A), 9.2±1.3 (B); T½(h) 7.5±1.8 (A), 7.2±1.5 (B); AUC0®t (µg.h/mL) 145.1±35.0 (A), 179.1±36.4 (B); AUC0®¥ (µg.h/mL) 172.6±44.7 (A), 206.2±45.5 (B). Obteniendo una disponibilidad relativa (FA/B) de 0.82±0.16 y para la Oxifenbutazona fueron (media ± D.S.): Tmax (h) 15.3±2.8 (A), 13.8±4.8 (B); Cmax (µg/mL) 2.1±0.4 (A), 2.5±0.6 (B); MRT0®t (h) 13.5±0.9 (A), 13.1±1.0 (B); AUC0®t (µg.h/mL) 34.9±6.4 (A), 42.9±9.2 (B); FA/B 0.85±0.26.Al comparar la administración oral de la Suxibuzona (A) con la de Fenilbutazona (B) sólo se han observado diferencias significativas (pEn una segunda fase experimental se administraron las mismas dosis de Suxibuzona (C) y Fenilbutazona (D), incorporadas en su dieta habitual, a 10 animales (5 por tratamiento) de los utilizados en el primer estudio. Se obtuvieron los siguientes parámetros farmacocinéticos para las concentraciones de Fenilbutazona (media ± D.S.): Tmax (h) 9.8±8.5 (C), 6.2±8.1 (D); Cmax (µg/mL) 7.9±3.4 (C), 9.5±1.3 (D); MRT0®24h (h) 12.1±3.6 (C), 9.0±1.9 (D); AUC0®t (µg.h/mL) 83.3±24.4 (C), 100.2±20.2 (D). Mientras que para la Oxifenbutazona fueron: Tmax (h) 13.6±7.9 (C), 9.8±4.0 (D); Cmax (µg/mL) 1.7±0.5 (C), 1.6±0.3 (D); MRT0®24h (h) 13.1±2.5 (C), 11.5±1.5 (D); AUC0®t (µg.h/mL) 21.6±5.1 (C), 24.3±6.6 (D). La disponibilidad relativa entre los mismos animales administrando el producto en ayunas o con el alimento fue FC/A 0.76±0.18 y FD/B 0.65±0.16 para las concentraciones de Fenilbutazona, y FC/A 0.74±0.20 y FD/B 0.75±0.17 para la Oxifenbutazona. Por lo que se observa una disminución de la disponibilidad de la Fenilbutazona y Oxifenbutazona similar tras ambas administraciones cuando éstas se realizan con el alimento.Las concentraciones de Fenilbutazona y Oxifenbutazona observadas en el análisis del líquido sinovial tras la administración de Suxibuzona a la dosis de 6.25 mg/kg a animales en ayunas (N=6) fueron las siguientes respectivamente a las 6h: 2.3±1.4 (PBZ), 0.4±0.2 (OPBZ); a las 12h: 2.6±0.7 (PBZ), 0.7±0.3 (OPBZ) y a 24h: 1.0±0.3 (PBZ), 0.7±0.2 (OPBZ). Tampoco se detectaron concentraciones de Suxibuzona en el líquido sinovial.Suxibuzone is a widely used non-steroidal anti-inflammatory drug in equine medicine. Chemically it is a Phenylbutazone ester. Both molecules are closely related because Suxibuzone is rapidly metabolized to Phenylbutazone when is orally or parenterally administered to the horse.The aim of this study is to evaluate the availability profile of Phenylbutazone, and its main metabolite Oxyphenbutazone, after Suxibuzone or Phenylbutazone administration at the same molecular doses, not only in fasting horses but also in animals following usual diet. Furthermore, the availability of these molecules in synovial fluid has been studied, as indicator of its ability to develop anti-inflammatory effects in the joints.In an firstly cross-over experimental phase, Suxibuzone 6.25 mg/kg (A) and Phenylbutazone 4.4 mg/kg (B) were orally administered to 19 fasting horses. Serial plasma samples were obtained and plasma and synovial fluid levels of Suxibuzone and its main active metabolites (Phenylbutazone and Oxyphenbutazone) were quantified by liquid chromatography (HPLC) using a previously validated method.Pharmacokinetic parameters were calculated using a non-compartimental analysis for all animals after both administrations. Suxibuzone was not detected in any sample. Main pharmacokinetic parameters obtained for plasma levels of Phenylbutazone were (mean ± S.D.): Tmax (h) 4.9±3.1 (A), 3.2±2.7 (B); Cmax (µg/mL) 10.2±2.2 (A), 15.5±3.6 (B); MRT0®t (h) 10.0±1.1 (A), 9.2±1.3 (B); T½(h) 7.5±1.8 (A), 7.2±1.5 (B); AUC0®t (µg.h/mL) 145.1±35.0 (A), 179.1±36.4 (B); AUC0®¥ (µg.h/mL) 172.6±44.7 (A), 206.2±45.5 (B). A relative availability of (FA/B) 0.82±0.16 was observed.Main pharmacokinetic parameters obtained for Oxyphenbutazone were (mean ± S.D.): Tmax (h) 15.3±2.8 (A), 13.8±4.8 (B); Cmax (µg/mL) 2.1±0.4 (A), 2.5±0.6 (B); MRT0®t (h) 13.5±0.9 (A), 13.1±1.0 (B); AUC0®t (µg.h/mL) 34.9±6.4 (A), 42.9±9.2 (B); FA/B 0.85±0.26.After the statistical analysis of the results obtained in this study we conclude that there are not significant differences (pSignificant differences (pIn a second experimental phase, the same doses of Suxibuzone (C) and Phenylbutazone (D) were administered with the usual diet, to 10 animals (5 per treatment) of the first study. Following pharmacokinetic parameters for Phenyl-butazone concentrations were obtained (mean ± S.D.): Tmax (h) 9.8±8.5 (C), 6.2±8.1 (D); Cmax (µg/mL) 7.9±3.4 (C), 9.5±1.3 (D); MRT0®24h (h) 12.1±3.6 (C), 9.0±1.9 (D); AUC0®t (µg.h/mL) 83.3±24.4 (C), 100.2±20.2 (D). For Oxyphenbutazone concentrations the values were as follows: Tmax (h) 13.6±7.9 (C), 9.8±4.0 (D); Cmax (µg/mL) 1.7±0.5 (C), 1.6±0.3 (D); MRT0®24h (h) 13.1±2.5 (C), 11.5±1.5 (D); AUC0®t (µg.h/mL) 21.6±5.1 (C), 24.3±6.6 (D). The relative availability between the same animals when the drug was administered in the fasting state or with food was FC/A 0.76±0.18 and FD/B 0.65±0.16 for Phenylbutazone concentrations; FC/A 0.74±0.20 and FD/B 0.75±0.17 for Oxyphenbutazone concentrations. A similar reduction of Phenylbutazone and Oxyphenbutazone availability was observed after both treatments when administered with food.Concentrations of Phenylbutazone and Oxyphenbutazone in synovial fluid after Suxibuzone 6.25 mg/kg in fasting animals (n=6) were after 6h: 2.3±1.4 (PBZ), 0.4±0.2 (OPBZ); after 12h: 2.6±0.7 (PBZ), 0.7±0.3 (OPBZ) and after 24h: 1.0±0.3 (PBZ), 0.7±0.2 (OPBZ). Suxibuzone concentrations in synovial fluid were not detected
J Homedes - One of the best experts on this subject based on the ideXlab platform.
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multicentre controlled randomised and blinded field study comparing efficacy of Suxibuzone and phenylbutazone in lame horses
Equine Veterinary Journal, 2009Co-Authors: D Sabate, J Homedes, M Salichs, M Sust, L MonrealAbstract:Reasons for performing study In horses, it has been demonstrated that Suxibuzone (SBZ) has a lower gastric ulcerogenic effect than phenylbutazone (PBZ). However, no field trials have been reported comparing the efficacy of the drugs in alleviating lameness. Objectives To compare the therapeutic effect of SBZ to that of PBZ when administered orally in lame horses. Acceptability of both products was also compared. Methods Lame horses (n = 155) were used in a multicentre, controlled, randomised and double-blinded clinical trial. Horses were treated orally with either SBZ or PBZ at equivalent therapeutic dosages. PBZ was given to 79 horses at a dose of 4.4 mg/kg bwt/12 h for 2 days, followed by 2.2 mg/kg bwt/12 h for 6 days. SBZ was given to 76 horses at 6.6 mg/kg bwt/12 h for 2 days, followed by 3.3 mg/kg bwt/ 12 h for 6 days. Efficacy of treatments was evaluated by clinicians in equine practices according to lameness progression throughout the study. Product ingestion was checked daily to evaluate product acceptability. Results Although SBZ showed a statistically significant tendency to have a better efficacy than PBZ (Odds ratio = 2.7; P = 0.016), significance dissipated once the analysis was adjusted for some imbalanced baseline covariates, confirming that they were actually related to the apparent advantage of SBZ over PBZ. Product acceptability was significantly higher in the SBZ group than in the PBZ group (96.1% vs. 77.2%; P = 0.001). Conclusions SBZ and PBZ did not show significant differences in alleviating lameness in horses. However, SBZ had better product acceptability when administered orally with some food. Potential relevance SBZ is a good therapeutic alternative to PBZ in horses since there is no significant difference in alleviating lameness between the 2 therapies.
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lower gastric ulcerogenic effect of Suxibuzone compared to phenylbutazone when administered orally to horses
Research in Veterinary Science, 2004Co-Authors: L Monreal, D Sabate, Didac Segura, I Mayos, J HomedesAbstract:The objective was to compare the gastrointestinal and general toxicity of Suxibuzone (SBZ) to that of phenylbutazone (PBZ) when administered orally in horses. Fifteen healthy horses were allocated to three treatment groups. One group received a high dose of PBZ for two weeks; the second group was given an equimolecular dosage of SBZ; and a third group received placebo. Horses were daily monitored, and blood samples were collected before and during the study. On day 18, complete post-mortem examinations were performed. One horse treated with PBZ showed clinical signs of NSAID toxicosis. Small oral ulcers were also detected in other two horses from the PBZ group and in two horses from the SBZ group. There were no statistical differences in the blood parameters among groups. Ulcers in the stomach's glandular mucosa were observed in all horses of the PBZ group, while only two horses of the SBZ group showed ulcerations. PBZ horses had a significant higher ulcerated area, and gastric ulcers were significantly deeper than those in the SBZ and placebo groups. No other lesions were found in any other tissue. In conclusion, SBZ causes significantly lower gastric ulcerogenic effect than PBZ when administered orally at equimolecular doses in horses.
L Monreal - One of the best experts on this subject based on the ideXlab platform.
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multicentre controlled randomised and blinded field study comparing efficacy of Suxibuzone and phenylbutazone in lame horses
Equine Veterinary Journal, 2009Co-Authors: D Sabate, J Homedes, M Salichs, M Sust, L MonrealAbstract:Reasons for performing study In horses, it has been demonstrated that Suxibuzone (SBZ) has a lower gastric ulcerogenic effect than phenylbutazone (PBZ). However, no field trials have been reported comparing the efficacy of the drugs in alleviating lameness. Objectives To compare the therapeutic effect of SBZ to that of PBZ when administered orally in lame horses. Acceptability of both products was also compared. Methods Lame horses (n = 155) were used in a multicentre, controlled, randomised and double-blinded clinical trial. Horses were treated orally with either SBZ or PBZ at equivalent therapeutic dosages. PBZ was given to 79 horses at a dose of 4.4 mg/kg bwt/12 h for 2 days, followed by 2.2 mg/kg bwt/12 h for 6 days. SBZ was given to 76 horses at 6.6 mg/kg bwt/12 h for 2 days, followed by 3.3 mg/kg bwt/ 12 h for 6 days. Efficacy of treatments was evaluated by clinicians in equine practices according to lameness progression throughout the study. Product ingestion was checked daily to evaluate product acceptability. Results Although SBZ showed a statistically significant tendency to have a better efficacy than PBZ (Odds ratio = 2.7; P = 0.016), significance dissipated once the analysis was adjusted for some imbalanced baseline covariates, confirming that they were actually related to the apparent advantage of SBZ over PBZ. Product acceptability was significantly higher in the SBZ group than in the PBZ group (96.1% vs. 77.2%; P = 0.001). Conclusions SBZ and PBZ did not show significant differences in alleviating lameness in horses. However, SBZ had better product acceptability when administered orally with some food. Potential relevance SBZ is a good therapeutic alternative to PBZ in horses since there is no significant difference in alleviating lameness between the 2 therapies.
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lower gastric ulcerogenic effect of Suxibuzone compared to phenylbutazone when administered orally to horses
Research in Veterinary Science, 2004Co-Authors: L Monreal, D Sabate, Didac Segura, I Mayos, J HomedesAbstract:The objective was to compare the gastrointestinal and general toxicity of Suxibuzone (SBZ) to that of phenylbutazone (PBZ) when administered orally in horses. Fifteen healthy horses were allocated to three treatment groups. One group received a high dose of PBZ for two weeks; the second group was given an equimolecular dosage of SBZ; and a third group received placebo. Horses were daily monitored, and blood samples were collected before and during the study. On day 18, complete post-mortem examinations were performed. One horse treated with PBZ showed clinical signs of NSAID toxicosis. Small oral ulcers were also detected in other two horses from the PBZ group and in two horses from the SBZ group. There were no statistical differences in the blood parameters among groups. Ulcers in the stomach's glandular mucosa were observed in all horses of the PBZ group, while only two horses of the SBZ group showed ulcerations. PBZ horses had a significant higher ulcerated area, and gastric ulcers were significantly deeper than those in the SBZ and placebo groups. No other lesions were found in any other tissue. In conclusion, SBZ causes significantly lower gastric ulcerogenic effect than PBZ when administered orally at equimolecular doses in horses.
D Sabate - One of the best experts on this subject based on the ideXlab platform.
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multicentre controlled randomised and blinded field study comparing efficacy of Suxibuzone and phenylbutazone in lame horses
Equine Veterinary Journal, 2009Co-Authors: D Sabate, J Homedes, M Salichs, M Sust, L MonrealAbstract:Reasons for performing study In horses, it has been demonstrated that Suxibuzone (SBZ) has a lower gastric ulcerogenic effect than phenylbutazone (PBZ). However, no field trials have been reported comparing the efficacy of the drugs in alleviating lameness. Objectives To compare the therapeutic effect of SBZ to that of PBZ when administered orally in lame horses. Acceptability of both products was also compared. Methods Lame horses (n = 155) were used in a multicentre, controlled, randomised and double-blinded clinical trial. Horses were treated orally with either SBZ or PBZ at equivalent therapeutic dosages. PBZ was given to 79 horses at a dose of 4.4 mg/kg bwt/12 h for 2 days, followed by 2.2 mg/kg bwt/12 h for 6 days. SBZ was given to 76 horses at 6.6 mg/kg bwt/12 h for 2 days, followed by 3.3 mg/kg bwt/ 12 h for 6 days. Efficacy of treatments was evaluated by clinicians in equine practices according to lameness progression throughout the study. Product ingestion was checked daily to evaluate product acceptability. Results Although SBZ showed a statistically significant tendency to have a better efficacy than PBZ (Odds ratio = 2.7; P = 0.016), significance dissipated once the analysis was adjusted for some imbalanced baseline covariates, confirming that they were actually related to the apparent advantage of SBZ over PBZ. Product acceptability was significantly higher in the SBZ group than in the PBZ group (96.1% vs. 77.2%; P = 0.001). Conclusions SBZ and PBZ did not show significant differences in alleviating lameness in horses. However, SBZ had better product acceptability when administered orally with some food. Potential relevance SBZ is a good therapeutic alternative to PBZ in horses since there is no significant difference in alleviating lameness between the 2 therapies.
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lower gastric ulcerogenic effect of Suxibuzone compared to phenylbutazone when administered orally to horses
Research in Veterinary Science, 2004Co-Authors: L Monreal, D Sabate, Didac Segura, I Mayos, J HomedesAbstract:The objective was to compare the gastrointestinal and general toxicity of Suxibuzone (SBZ) to that of phenylbutazone (PBZ) when administered orally in horses. Fifteen healthy horses were allocated to three treatment groups. One group received a high dose of PBZ for two weeks; the second group was given an equimolecular dosage of SBZ; and a third group received placebo. Horses were daily monitored, and blood samples were collected before and during the study. On day 18, complete post-mortem examinations were performed. One horse treated with PBZ showed clinical signs of NSAID toxicosis. Small oral ulcers were also detected in other two horses from the PBZ group and in two horses from the SBZ group. There were no statistical differences in the blood parameters among groups. Ulcers in the stomach's glandular mucosa were observed in all horses of the PBZ group, while only two horses of the SBZ group showed ulcerations. PBZ horses had a significant higher ulcerated area, and gastric ulcers were significantly deeper than those in the SBZ and placebo groups. No other lesions were found in any other tissue. In conclusion, SBZ causes significantly lower gastric ulcerogenic effect than PBZ when administered orally at equimolecular doses in horses.
Didac Segura - One of the best experts on this subject based on the ideXlab platform.
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lower gastric ulcerogenic effect of Suxibuzone compared to phenylbutazone when administered orally to horses
Research in Veterinary Science, 2004Co-Authors: L Monreal, D Sabate, Didac Segura, I Mayos, J HomedesAbstract:The objective was to compare the gastrointestinal and general toxicity of Suxibuzone (SBZ) to that of phenylbutazone (PBZ) when administered orally in horses. Fifteen healthy horses were allocated to three treatment groups. One group received a high dose of PBZ for two weeks; the second group was given an equimolecular dosage of SBZ; and a third group received placebo. Horses were daily monitored, and blood samples were collected before and during the study. On day 18, complete post-mortem examinations were performed. One horse treated with PBZ showed clinical signs of NSAID toxicosis. Small oral ulcers were also detected in other two horses from the PBZ group and in two horses from the SBZ group. There were no statistical differences in the blood parameters among groups. Ulcers in the stomach's glandular mucosa were observed in all horses of the PBZ group, while only two horses of the SBZ group showed ulcerations. PBZ horses had a significant higher ulcerated area, and gastric ulcers were significantly deeper than those in the SBZ and placebo groups. No other lesions were found in any other tissue. In conclusion, SBZ causes significantly lower gastric ulcerogenic effect than PBZ when administered orally at equimolecular doses in horses.
