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A robust and rapid reversed-phase UHPLC method for routine determination of vildagliptin (VILDA) and metformin (MET) was developed and validated with DAD detection (207 nm). Chromatographic analysis was carried out with isocratic ...
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A robust and rapid reversed-phase UHPLC method for routine determination of vildagliptin (VILDA) and metformin (MET) was developed and validated with DAD detection (207 nm). Chromatographic analysis was carried out with isocratic separation by C18 column (150mm x 2.1mm, 5 pm) using a mobile phase with a mixture of 1.36 g phosphate buffer (pH 4.2) set to phosphoric acid and acetonitrile (80:20, v/v) with 0.6mL/min flow rate. The procedure was validated as per International Conference on Harmonization (ICH) guidelines for linearity (correlation coefficient r2 = 0.999), accuracy, intermediate precision, and robustness. Accuracy was 99.79%±0.54% and 100.07 %±0.34% for VILDA and MET, respectively. For precision, the %RSD was founded to be less than 2% for three concentrations analyzed from three replicates. The proposed method was used for successful determination of VILDA and MET in a pharmaceutical preparation.
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A mild and economical method to prepare vildagliptin had been reported with a good yield. In this paper, vildagliptin was synthesized from L-proline and 3-amino-1-adamantanol through chloride acetylation, amination, dehydration an...
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A mild and economical method to prepare vildagliptin had been reported with a good yield. In this paper, vildagliptin was synthesized from L-proline and 3-amino-1-adamantanol through chloride acetylation, amination, dehydration and substitution. The total yield of the target compound was 59%.
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We previously reported that combination therapy with an α-glucosidase inhibitor (αGI) and a dipeptidyl peptidase-4 (DPP-4) inhibitor increased active glucagon-like peptide-1 (GLP-1) levels and decreased total glucose-dependent i...
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We previously reported that combination therapy with an α-glucosidase inhibitor (αGI) and a dipeptidyl peptidase-4 (DPP-4) inhibitor increased active glucagon-like peptide-1 (GLP-1) levels and decreased total glucose-dependent insulinotropic polypeptide (GIP) levels, compared with monotherapy, in non-diabetic men. However, the peptide YY (PYY), cholecystokinin (CCK), ghrelin, and obestatin levels in patients receiving a combination of αGIs and DPP-4 inhibitors have not been previously reported. We evaluated the effect of miglitol, vildagliptin, or their combination on these parameters. Miglitol and/or vildagliptin were administered according to four different intake schedules in eleven non-diabetic men (C: no drug, M: miglitol; V: vildagliptin, M+V: miglitol+vildagliptin). Blood samples were collected at 0, 30, 60, and 120 min after the start of breakfast. The plasma glucose, serum insulin, serum total PYY (PYY_(1-36) and PYY_(3-36)), plasma CCK, plasma active ghrelin, and plasma obestatin levels were measured. The area under the curve (AUC) of the serum total PYY level in the M group was significantly greater than that in the C group, and the AUC of the serum total PYY level in the M+V group was significantly lower than that in the M group. The combination therapy did not change the AUC of the plasma CCK, plasma active ghrelin, plasma obestatin, and ghrelin/obestatin levels, compared with the control. The results of our study suggested that combination therapy with miglitol and vildagliptin had no effect on appetite regulation hormones, such as total PYY, CCK, active ghrelin, and obestatin, compared with the levels in the control group.
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A novel approach to synthesize the of heterocycle-containing adamantane derivatives l-{[(3-hydroxy-1-adamantyl)amino]acetyl}-2-cyaho-(S)-pyrrolidine and N-{2-[4-(2-pyrimidinyl)-1-piperazinyl]ethyl}adamantane-1-carboxamide, which w...
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A novel approach to synthesize the of heterocycle-containing adamantane derivatives l-{[(3-hydroxy-1-adamantyl)amino]acetyl}-2-cyaho-(S)-pyrrolidine and N-{2-[4-(2-pyrimidinyl)-1-piperazinyl]ethyl}adamantane-1-carboxamide, which were effective in treatment of diabetes and depression respectively, have been described. The target compounds were synthesized by raw materials of inexpensive L-proline and available 1 -(2-pyrimidinyl) piperazine respectively. Compared with traditional synthetic routes, the method provides several advantages such as inexpensive and readily available raw materials, convenient manipulation and high yield.
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Anti-diabetic agent-related hypoglycemia is a serious complication in type 2 diabetic patients on hemodialysis. Therefore, we assessed the efficacy and tolerability of 24weeks of monotherapy with vildagliptin, a dipeptidyl peptida...
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Anti-diabetic agent-related hypoglycemia is a serious complication in type 2 diabetic patients on hemodialysis. Therefore, we assessed the efficacy and tolerability of 24weeks of monotherapy with vildagliptin, a dipeptidyl peptidase four inhibitor, which is a new class of antidiabetic agent. This open-label, single-arm clinical trial was performed on 26 patients on hemodialysis. The primary assessments were changes in postprandial glucose level and glycated albumin (GA). During the study, three patients dropped out, and data from 23 patients were analyzed. Significant reductions were seen in postprandial glucose (-2.60±3.80mmol/L, P<0.001) and GA (-2.59±2.33%, P<0.001) levels. No serious drug-related adverse events were observed. Vildagliptin monotherapy can be recommended for glycemic control in type 2 diabetic patients on hemodialysis. This trial was registered with the University Hospital Medical Information Network (no. UMIN000003661).
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Aim: To investigate whether vildagliptin, one of the dipeptidylpeptide-4 (DDP-4) inhibitors, improves not only glycemic control but also glycemic fluctuation when added to ongoing sulfonylurea (SU) based oral hypoglycemic agents (...
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Aim: To investigate whether vildagliptin, one of the dipeptidylpeptide-4 (DDP-4) inhibitors, improves not only glycemic control but also glycemic fluctuation when added to ongoing sulfonylurea (SU) based oral hypoglycemic agents (OHA) therapy in patients with type 2 diabetes mellitus (T2DM). Methods: A total of 19 patients with T2DM were recruited from outpatients. Vildagliptin was initiated with a dose of 100 mg per day in the patients who had inadequate glycemic control and glycemic fluctuation with ongoing SU based OHA therapy. Glycemic excursion was defined by seven-point self-monitoring blood glucose (SMBG) on three days at baseline and 12 weeks after vildagliptin-combined therapy, as well as HbA1c levels. M-value and J-index were calculated to evaluate glycemic excursion. Results: Addition of vildagliptin to ongoing SU based OHA therapy significantly decreased HbA1c values from 8.2 ± 3.8% at baseline to 7.3 ± 0.8% at 12-week. The average of blood glucose profiles was significant improved. As a result, M-value was significantly corrected from 20.9 ± 14.4 to 12.2 ± 13.5 and J-index from 55.1 ±25.5 to 39.1 ±19.8. Conclusions: Vildagliptin when added to ongoing SU based OHA therapy for 12 weeks significantly improved glycemic fluctuation as well as glycemic control in Japanese patients with T2DM.
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Bullous pemfigoid (BP), an autoimmune disorder, can also be induced by some medications. Vildagliptin is a new drug used to treat diabetes mellitus (DM). Recently, a few cases of vildagliptin-induced BP have been described in the ...
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Bullous pemfigoid (BP), an autoimmune disorder, can also be induced by some medications. Vildagliptin is a new drug used to treat diabetes mellitus (DM). Recently, a few cases of vildagliptin-induced BP have been described in the literature. We report a patient with BP in which vildagliptin was thought to be as a possible causative agent. The awareness of BP development risk during gliptin therapy can prevent unnecessary usage of systemic drugs with serious side effects.
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Aims. Vildagliptin promotes beta cell survival by inhibiting cell apoptosis. It has been suggested that chronic ER (endoplasmic reticulum) stress triggers beta cell apoptosis. The objective of the study is to explore whether the p...
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Aims. Vildagliptin promotes beta cell survival by inhibiting cell apoptosis. It has been suggested that chronic ER (endoplasmic reticulum) stress triggers beta cell apoptosis. The objective of the study is to explore whether the pro-survival effect of vildagliptin is associated with attenuation of endoplasmic reticulum stress in islets of db/db mice.
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Background: This study investigated the safety and efficacy of metformin up-titration in Japanese patients with type 2 diabetes mellitus treated with vildagliptin (100 mg/day) and low-dose metformin (500 or 750 mg/day).
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