Diabetes research and clinical practice, Jan 18, 2018
The two dipeptidyl peptidase (DPP)-4 inhibitors, linagliptin and sitagliptin, were shown to exert... more The two dipeptidyl peptidase (DPP)-4 inhibitors, linagliptin and sitagliptin, were shown to exert different binding kinetics in vitro. Twenty-four hours after oral dosing particularly in vivo inhibition of renal-specific DPP-4 activity was more sustained in Sprague Dawley rats after exposure to linagliptin than it was after sitagliptin.
La presente invention concerne une composition pharmaceutique comprenant de la 1-[(3-cyano-pyridi... more La presente invention concerne une composition pharmaceutique comprenant de la 1-[(3-cyano-pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-[3-(R)-amino-piperidin-1-yl]-xanthine ou une forme de celle-ci pharmaceutiquement acceptable en tant que compose actif pour le traitement d'un trouble metabolique ou d'une maladie metabolique chez un animal non humain principalement carnivore. Elle est notamment utile pour le traitement du diabete et des maladies apparentees chez des mammiferes principalement carnivores comme les chats ou les chiens. L'invention concerne en outre les utilisations respectives de ces compositions et de 1-[(3-cyano-pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-[3-(R)-amino-piperidin-1-yl]-xanthine ou de ses formes pharmaceutiquement acceptables.
ABSTRACT Additive glycaemic control of combination of a single dose of empagliflozin with injecta... more ABSTRACT Additive glycaemic control of combination of a single dose of empagliflozin with injectable anti-diabetes drugs in ZDF rat. Ebrahim K Naderali, Leo Thomas, Rolf Grempler, Michael Mark, Eric Mayoux Arash Tahbaz Aims: Here we have investigated anti-glycaemic effects of empagliflozin, an SGLT2 inhibitor, in combination currently available injectable anti-diabetes agents such as insulin or GLP-1 analogue. Materials and methods: Male Zucker Diabetic Fatty (ZDF) rats with an age of 12-14 weeks, fasted overnight, were exposed to oral glucose load (oGTT) 15-45min after single oral dose of empagliflozin (3 mg kg -1) or s.c. injections of insulin (0.5U kg-1) or exendin-4 (0.01 mg kg -1) of each monotherapy or the respective combination. The area under a blood glucose-time curve (AUC) from 0 to 120 min was calculated by the trapezoidal rule without correction for baseline values. % AUC reduction from vehicle group were calculated and two-sided unpaired Student’s t tests was conducted between control and treated groups. Results: The combination of empagliflozin with insulin reduced the AUC vs control by 54% (p<0.01) and this reduction was significantly greater than those of empagliflozin monotherapy (31%, p<0.001) or insulin monotherapy (35%, p<0.05). Furthermore, the combination of empagliflozin with exendin-4 reduced the AUC by 51%, which was significantly (p<0.01 for both) greater than the effect achieved by each monotherapy (35% with empagliflozin and 25% with exendin-4). Summary: These data indicates that addition of empagliflozin to GLP1- agonist or insulin resulted in a greater improvement in glucose tolerance in ZDF rats compared to each individual monotherapy.
Diabetes research and clinical practice, Jan 18, 2018
The two dipeptidyl peptidase (DPP)-4 inhibitors, linagliptin and sitagliptin, were shown to exert... more The two dipeptidyl peptidase (DPP)-4 inhibitors, linagliptin and sitagliptin, were shown to exert different binding kinetics in vitro. Twenty-four hours after oral dosing particularly in vivo inhibition of renal-specific DPP-4 activity was more sustained in Sprague Dawley rats after exposure to linagliptin than it was after sitagliptin.
La presente invention concerne une composition pharmaceutique comprenant de la 1-[(3-cyano-pyridi... more La presente invention concerne une composition pharmaceutique comprenant de la 1-[(3-cyano-pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-[3-(R)-amino-piperidin-1-yl]-xanthine ou une forme de celle-ci pharmaceutiquement acceptable en tant que compose actif pour le traitement d'un trouble metabolique ou d'une maladie metabolique chez un animal non humain principalement carnivore. Elle est notamment utile pour le traitement du diabete et des maladies apparentees chez des mammiferes principalement carnivores comme les chats ou les chiens. L'invention concerne en outre les utilisations respectives de ces compositions et de 1-[(3-cyano-pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-[3-(R)-amino-piperidin-1-yl]-xanthine ou de ses formes pharmaceutiquement acceptables.
ABSTRACT Additive glycaemic control of combination of a single dose of empagliflozin with injecta... more ABSTRACT Additive glycaemic control of combination of a single dose of empagliflozin with injectable anti-diabetes drugs in ZDF rat. Ebrahim K Naderali, Leo Thomas, Rolf Grempler, Michael Mark, Eric Mayoux Arash Tahbaz Aims: Here we have investigated anti-glycaemic effects of empagliflozin, an SGLT2 inhibitor, in combination currently available injectable anti-diabetes agents such as insulin or GLP-1 analogue. Materials and methods: Male Zucker Diabetic Fatty (ZDF) rats with an age of 12-14 weeks, fasted overnight, were exposed to oral glucose load (oGTT) 15-45min after single oral dose of empagliflozin (3 mg kg -1) or s.c. injections of insulin (0.5U kg-1) or exendin-4 (0.01 mg kg -1) of each monotherapy or the respective combination. The area under a blood glucose-time curve (AUC) from 0 to 120 min was calculated by the trapezoidal rule without correction for baseline values. % AUC reduction from vehicle group were calculated and two-sided unpaired Student’s t tests was conducted between control and treated groups. Results: The combination of empagliflozin with insulin reduced the AUC vs control by 54% (p<0.01) and this reduction was significantly greater than those of empagliflozin monotherapy (31%, p<0.001) or insulin monotherapy (35%, p<0.05). Furthermore, the combination of empagliflozin with exendin-4 reduced the AUC by 51%, which was significantly (p<0.01 for both) greater than the effect achieved by each monotherapy (35% with empagliflozin and 25% with exendin-4). Summary: These data indicates that addition of empagliflozin to GLP1- agonist or insulin resulted in a greater improvement in glucose tolerance in ZDF rats compared to each individual monotherapy.
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