Effect of voglibose combined with exenatide on blood glucose control and serumfibroblast growth factor 21expression in patients with type 2 diabetes mellitus / 中国医师进修杂志

Objective:To investigate the effect of voglibose combined with exenatide on blood glucose control and serum fibroblast growth factor 21 (FGF-21) expression in patients with type 2 diabetes mellitus (T2DM).Methods:Three hundred and eighty patients with T2DM admitted to Qingdao Municipal Hospital from October 2018 to September 2020 were selected and randomly divided into the control group and the observation group, with 190 patients in each group. The control group was treated with voglibose, and the observation group was treated with voglibose and exenatide. Both groups were treated for 16 weeks. Blood glucose, blood fat, insulin and other indicators as well as serum FGF-21 levels were compared between the two groups before and after the treatment, and the efficacy of drugs and the incidence of adverse reactions were compared.Results:The total effective rate in the observation group was higher than that in the control group: 97.89%(186/190) vs. 93.16%(177/190), χ2 = 5.00, P<0.05. After treatment, the levels of fasting plasma glucose (FPG), 2 h plasma glucose (2 h PG) and glycosylated hemoglobin (HbA 1c) in the observation group were lower than those in the control group: (6.95 ± 1.03) mmol/L vs. (8.29 ± 1.15) mmol/L, (7.88 ± 2.07) mmol/L vs. (10.03 ± 3.24) mmol/L, (7.17 ± 1.08)% vs. (8.13 ± 1.21)%, P<0.05. After treatment, the levels of triacylglycerol (TG), total cholesterol (TC) and low-density lipoprotein cholesterol (LDL-C) in the observation group were lower than those in the control group: (2.13 ± 0.23) mmol/L vs. (2.93 ± 0.34) mmol/L, (3.10 ± 1.01) mmol/L vs. (3.98 ± 1.14) mmol/L, (1.93±0.38) mmol/L vs. (2.73±0.54) mmol/L, P<0.05. After treatment, the level of islet β cell function index (HOMA-β) in the observation group was higher than that in the control group: 111.56 ± 20.78 vs. 102.23 ± 20.14, P<0.05. After treatment, the level of serum FGF-21 in the observation group was lower than that in the control group: (142.09 ± 26.82) ng/L vs. (150.22 ± 30.21) ng/L, P<0.05. The incidence of adverse reactions between the two groups had no significant difference ( P>0.05). Conclusions:Voglibose combined with exenatide has a definite effect on T2DM patients with metformin failure, which can effectively control their blood glucose level, reduce serum FGF-21 level, improve insulin resistance and glucose and lipid metabolism, and reduce body mass, with high safety.

Evaluation of voglibose on body weight in rats

Background: As of 2018, 2.1 billion people nearly 30% of the world’s population are either obese or overweight. Worldwide obesity has nearly tripled since 1975. It is an emerging health problem with major adverse effects on health. It is a risk factor for many chronic diseases but is best known for its role in metabolic syndrome, which can lead to type 2 diabetes mellitus as well as cardiovascular diseases. Anti-obesity drugs are available but have many side effects. Voglibose, an antidiabetic drug, is an alpha glucosidase inhibitor which shows promising results in the reduction of body weight with minimal side effects.Methods: Voglibose (7 mg/kg) was administered to rats fed with normal laboratory chows and high fat diet to see its effect on body weight, body mass index, abdominal and thoracic circumference, and lipid profile at the end of 12 weeks.Results: Administration of voglibose significantly reduced food consumption, feed efficiency and increase in body weight induced by high fat diet in rats. Rats fed on normal diet also showed reductions in the same parameters, suggesting its weight lowering effect. Reductions in the anthropometric measurements, hypolipidemic effects and glucose lowering effects were also observed.Conclusions: Voglibose prevented high fat diet-induced obesity and improvement in metabolic profile, which ultimately has systemic effects on body weight in rats. Further studies are needed to see its potential therapeutic use in obese patients with type 2 diabetes mellitus, and related complications.

Hypolipidemic effect of sitagliptin, voglibose and glimepiride in combination with metformin in patients with type 2 diabetes mellitus at a tertiary care teaching hospital: a comparative study

Background: The prevalence of coronary artery disease has been increased in diabetic dyslipidemia; hence the present study would like to compare the dyslipidemic effects of Sitagliptin, Voglibose, and Glimepiride in combination with Metformin in type 2 diabetes mellitus patients.Methods: This study was a Prospective, Randomized Clinical trial conducted at SRM medical College Hospital and Research centre. Potheri, Kancheepuram District in diabetic outpatient department after obtaining approval from Institutional Ethics Committee. The patients receiving antidiabetic drugs were divided into three groups. Patients received Metformin with Sitagliptin were grouped as I, Metformin with Voglibose were named as Group II and Metformin with Glimepiride were marked as Group III. Based on the inclusion and exclusion criteria, in each group, 40 patients were assigned as per simple randomization method. The level of lipid profile and BMI was evaluated at the end of 6 months.Results: There was a significant reduction of Total Cholesterol (TC) in Group II and Group III (p value- <0.001, <0.006). Group I showed significant elevation of HDL-C level with the p value of <0.03. Group III showed significant reduction of Triglyceride (TG) level with the p value of <0.04, significant reduction of Low Density Lipoprotein Cholesterol (LDL-C) level with the p value of <0.02 and significant reduction in Very Low Density Lipoprotein Cholesterol (VLDL-C) level with the p value of <0.05. There was no significant reduction in Body Mass Index (BMI) among the groups. On multiple comparisons, Group III showed higher efficacy in reducing TC, TG, LDL-C and VLDL-C levels.Conclusions: The results of this study were analysed and it could be concluded as Metformin with Glimepiride combination (Group III) showed significant reduction of TC, TG, LDL-C and VLDL-C levels.

Efficacy and Safety of Voglibose Plus Metformin in Patients with Type 2 Diabetes Mellitus: A Randomized Controlled Trial

BACKGROUND: Combination of metformin to reduce the fasting plasma glucose level and an α-glucosidase inhibitor to decrease the postprandial glucose level is expected to generate a complementary effect. We compared the efficacy and safety of a fixed-dose combination of voglibose plus metformin (vogmet) with metformin monotherapy in drug-naïve newly-diagnosed type 2 diabetes mellitus. METHODS: A total of 187 eligible patients aged 20 to 70 years, with a glycosylated hemoglobin (HbA1c) level of 7.0% to 11.0%, were randomized into either vogmet or metformin treatments for 24 weeks. A change in the HbA1c level from baseline was measured at week 24. RESULTS: The reduction in the levels of HbA1c was −1.62%±0.07% in the vogmet group and −1.31%±0.07% in the metformin group (P=0.003), and significantly more vogmet-treated patients achieved the target HbA1c levels of <6.5% (P=0.002) or <7% (P=0.039). Glycemic variability was also significantly improved with vogmet treatment, estimated by M-values (P=0.004). Gastrointestinal adverse events and hypoglycemia (%) were numerically lower in the vogmet-treated group. Moreover, a significant weight loss was observed with vogmet treatment compared with metformin (−1.63 kg vs. −0.86 kg, P=0.039). CONCLUSION: Vogmet is a safe antihyperglycemic agent that controls blood glucose level effectively, yields weight loss, and is superior to metformin in terms of various key glycemic parameters without increasing the risk of hypoglycemia.

Efficacy and safety of sitagliptin added to metformin and insulin compared with voglibose in patients with newly diagnosed type 2 diabetes

OBJECTIVE: To assess the efficacy and safety of sitagliptin compared with voglibose added to combined metformin and insulin in patients with newly diagnosed type 2 diabetes (T2DM). METHODS: In this 12-week prospective, randomized, parallel trial, 70 newly diagnosed T2DM patients with glycosylated hemoglobin (HbA1c) ≥9% and/or fasting plasma glucose (FPG) ≥11.1 mmol/L were randomized (1:1) to receive sitagliptin 100 mg per day + metformin + insulin glargine or voglibose 0.2 mg three times daily + metformin + insulin glargine. Change in HbA1c at week 12 was the primary endpoint. RESULTS: The mean baseline HbA1c was 11.0% in the patients. The changes in HbA1c from baseline were -6.00% in the sitagliptin group and -3.58% in the voglibose group, and the between-group difference was -2.42% (95% CI -1.91 to -2.93, p=0.02). The differences in FPG and homeostatic model assessment of β-cell function (HOMA-β) and the change in body weight between groups from baseline were -2.95 mmol/L (p=0.04), 43.91 (p=0.01) and -2.23 kg (p=0.01), respectively. One patient (2.9%) in the sitagliptin group and three patients (8.6%) in the voglibose group exhibited hypoglycemia. CONCLUSIONS: Sitagliptin added to combined metformin and insulin therapy showed greater efficacy and good safety regarding hypoglycemia in patients with newly diagnosed T2DM compared with voglibose.

Comparative study of safety and efficacy profile of repaglinide and voglibose on targeting post prandial hyperglycemia in patients with newly diagnosed type II diabetes mellitus

Background: In India the number of people with diabetes is increasing day-by-day. Due to a sole “Asian Indian Phenotype,” Indians develop diabetes an era earlier and have an earlier onset of complications. Therefore, it is essential to evaluate more effective treatment strategies at an earlier stage of disease progression.Methods: The present study was prospective, open label, comparative, randomized, parallel group, single center study. Comparison of two post prandial active treatment groups over a period of 3 months. Sixty patients of either sex in the age group of 30-60years with newly diagnosed type II diabetes mellitus, with prandial blood glucose levels >180mg% and <250mg% at screening as per ADA. The effect of repaglinide and voglibose were observed on various parameters i.e. HbA1c, FBS, PBS, BMI.Results: In repaglinide group the mean change in HbA1c from baseline to 3 months was 8.05 to 7.04 (-1.01); on the other hand, in voglibose group from baseline to 3 months was 8.0 to 7.18 (-0.82). Whereas, FBS from 137.57 to 122.90 (-16.67) in repaglinide group; in voglibose group from 139.87 to 125.13 (-14.74). Repaglinide statistically highly significant than voglibose group in improving glycemic indices.Conclusions: Though repaglinide and voglibose were equally effective in improving glycemic indices yet repaglinide showed better results in improving HbA1c, FBG, PBS as compared with voglibose. Repaglinide had minimal side effects as compared to voglibose.

Comparative efficacy and safety of DPP-4 inhibitors and ?-glucosidase inhibitors as add on therapy in type 2 diabetes

Background: Diabetes mellitus (DM) is a spectrum of metabolic disorders as a consequence of different pathogenic mechanisms resulting in hyperglycemia. A genetic predisposition to develop ?-cell dysfunction synergizes with insulin resistance to lead to type 2 DM. Adequate management of type 2 DM requires institution of non pharmacological treatment followed by pharmacological treatment. Monotherapy is started initially followed by combination therapy (dual/triple). Sitagliptin, a DPP-4 inhibitor and voglibose, an ?-glucosidase inhibitor has been implicated as an add on therapy to metformin and glimepiride. So, we aimed to assess the efficacy and safety of the sitagliptin and voglibose as add on therapy to metformin and glimepitide in type 2 DM.Methods: This open label randomized control trial was conducted in the department of Pharmacology among patients attending medicine OPD of a tertiary care hospital. 80 patients were randomly divided into two groups of 40 patients each. group A:sitagliptin + metformin + glimepiride and group B:voglibose + metformin + glimepiride. Patients were followed every week for a period of 12 weeks. Data was analysed using paired t test, unpaired t test and chi square test.Results: There was a significant decrease in HbA1c, FPG and PPG in both the groups. Intergroup comparison at 4, 8 and 12 weeks showed a better improvement in glycemic control in group A as compared to group B.Conclusions: Sitagliptin showed a better glycemic control than that with voglibose in patients with uncontrolled type 2 DM on metformin and glimepiride.

Targeting Postprandial Hyperglycemia with fixed dose combination of repaglinide and voglibose in Type 2 Diabetes Mellitus

@#Present study evaluates efficacy and tolerability of fixed dose combination of Voglibose and Repaglinide in postprandial hyperglycemia (PPHG).A non-randomized, open labeled, non-comparative, multi-centric, study was conducted in 69 Type 2 diabetes mellitus (T2DM) patients, 53 (76.8%) men and 16 (23.2%) women. Each patient was administered a fixed dose combination of voglibose 0.3mg and repaglinide 1mg twice a day, just before each meal for 90 days. Fasting blood glucose (FBG) and postprandial blood glucose (PPBG) levels were measured at baseline (day zero), on day 30 and on day 90. Glycated Haemoglobin (HbA1c) was measured at baseline and on day 90. There was significant reduction in PPBG (31.2%), FBG (31.6%), and HbA1c (10.3%) on day 90 compared to baseline. Therefore fixed dose combination of voglibose 0.3mg and repaglinide 1mg has a considerable impact on PPBG control. This combination was found to be efficacious in controlling PPHG and no cases of hypoglycemia were reported.

Role of voglibose in prevention of type 2 diabetes in established case of impaired glucose tolerance: an observation study.

Background: The increased prevalence of type 2 diabetes mellitus is a major concern for the health providers. We have done an observation study in the diagnosed IGT patient who received α-glucosidase inhibitor (voglibose), which could prevent the development of type 2 diabetes in high-risk individuals. Methods: This study was an observational study comprising of voglibose and placebo in individuals with impaired glucose tolerance.66 eligible patients were on the standard diet and taking regular exercise with impaired glucose tolerance were randomly assigned to oral voglibose 0.2 mg three times a day (n=66) or placebo (n=60) in this study. Treatment was continued until participants developed type 2 diabetes (primary endpoint) or normoglycaemia (secondary endpoint). In the final analysis, 66 registered individuals fulfilled the inclusion criteria: 36 were randomly assigned to receive voglibose and 30 placebos (two participants in the placebo group did not take their medication and were excluded). Results: The mean duration of treatment was 48.3 weeks (SD: 36.4), i.e., 45.4 weeks (34.7) for voglibose and 51.7 weeks (37.4) for placebo. Voglibose was better than placebo (p= 0.0024) in individuals treated for an average of 48.3 weeks (SD 36.4). Patients treated with voglibose had a lower risk of progression to type 2 diabetes than did those on placebo. More people in the voglibose group achieved normoglycaemia than did those in the placebo group. Conclusion: Voglibose, in addition to lifestyle modification, can reduce the development of type 2 diabetes in high risk individuals with impaired glucose tolerance.

A Randomized Double-Masked Study of 50 mg of Acarbose versus 0.2 mg Voglibose in Overweight Type 2 Diabetes Patients Age Between 30 and 50 Years Having Isolated Postprandial Glycemia.

Objective: To compare the efficacy of 50 mg acarbose versus 0.2 mg of voglibose in treating postprandial hyperglycemia. Material and methods: A randomized double-masked study was conducted at the Hassan Obesity and Diabetes Wellness Centre, Hassan, Karnataka, in coordination with Rajiv Gandhi University of Health Sciences, Karnataka. Sixty cases of isolated high postprandial blood sugar (PPBS > 200 mg/dL FBS < 126 mg/dL), including both males and females between age group 30 and 50 years, were included in the study group. Observation and results: Out of 30 patients in the group treated with acarbose 50 mg, the mean reduction of glycosylated hemoglobin (HbA1C) to their baseline values was 0.8% and mean reduction in the postprandial values was 64 mg/dL. Out of 30 patients in the group treated with voglibose 0.2 mg, the mean reduction in the HbA1C was 0.6% and mean reduction in the postprandial values was 57 mg/dL. Conclusions: Reduction of postprandial blood glucose and HbA1C were more in the group treated with acarbose with the difference of 0.2% in HbA1C and 7-8 mg/dL (mean) in postprandial plasma glucose. The side effects were more in the group treated with acarbose when compared with group treated with voglibose.

Comparison of Acarbose and Voglibose in Diabetes Patients Who Are Inadequately Controlled with Basal Insulin Treatment: Randomized, Parallel, Open-Label, Active-Controlled Study

We studied the efficacy and safety of acarbose in comparison with voglibose in type 2 diabetes patients whose blood glucose levels were inadequately controlled with basal insulin alone or in combination with metformin (or a sulfonylurea). This study was a 24-week prospective, open-label, randomized, active-controlled multi-center study. Participants were randomized to receive either acarbose (n=59, 300 mg/day) or voglibose (n=62, 0.9 mg/day). The mean HbA1c at week 24 was significantly decreased approximately 0.7% from baseline in both acarbose (from 8.43% +/- 0.71% to 7.71% +/- 0.93%) and voglibose groups (from 8.38% +/- 0.73% to 7.68% +/- 0.94%). The mean fasting plasma glucose level and self-monitoring of blood glucose data from 1 hr before and after each meal were significantly decreased at week 24 in comparison to baseline in both groups. The levels 1 hr after dinner at week 24 were significantly decreased in the acarbose group (from 233.54 +/- 69.38 to 176.80 +/- 46.63 mg/dL) compared with the voglibose group (from 224.18 +/- 70.07 to 193.01 +/- 55.39 mg/dL). In conclusion, both acarbose and voglibose are efficacious and safe in patients with type 2 diabetes who are inadequately controlled with basal insulin. (ClinicalTrials.gov number, NCT00970528)

Pharmacodynamic Comparison of Two Formulations of Voglibose 0.3-mg Tablet

BACKGROUND: Voglibose, an inhibitor of alpha-glucosidase of the small intestine brush border, is used to treat type 2 diabetic patients. Bioequivalence test based on pharmacokinetic parameters is difficult because voglibose does not cross the enterocytes after ingestion. This study was conducted to establish bioequivalence of two formulations of 0.3-mg voglibose with pharmacodynamic endpoints. METHODS: This study was an open, single-dose, randomized, 6-sequence, 3-period crossover design in healthy volunteers. In each period, subjects received placebo or three tablets of either test formulation or reference formulation with sucrose, with a 7-day washout period each dosing period. Serial blood samples were collected after each administration. The maximum concentrations of serum glucose and serum insulin (C(max)(G) and C(max)(I)) and the area under the serum concentration - time curve from dosing to 2 or 4 hours after dosing for serum glucose and insulin (AUC(0-2h)(G), AUC(0-4h)(G), AUC(0-2h)(I) and AUC(0-4h)(I), respectively) were determined by noncompartmental analysis. Formulation-related differences were tested in accordance with the Korean regulatory bioequivalence criteria. RESULTS: A total of 54 subjects completed study in accordance with protocol. The geometric mean ratios (GMRs) of the test formulation to the reference formulation for Cmax(G), AUC(0-2h)(G), AUC(0-4h)(G), C(max)(I), AUC(0-2h)(I) and AUC(0-4h)(I) were 0.945, 1.014, 0.995, 0.937, 0.985 and 0.983, respectively and the 90% confidence intervals (CIs) of corresponding values were 0.985-1.026, 0.991-1.038, 0.977-1.014, 0.830-1.057, 0.901-1.078 and 0.911-1.014, respectively. CONCLUSION: This single-dose study found that two formulations of 0.3-mg voglibose did not meet the regulatory criteria for bioequivalence in these healthy volunteers.

A Placebo-Controlled, Single and Multiple Dose Study to Investigate the Appropriate Parameters for Evaluation of Pharmacodynamic Equivalence of Voglibose in Healthy Korean Volunteers

BACKGROUND: Voglibose is an alpha-glucosidase inhibitor. The purpose of this study was to evaluate the pharmacodynamic characteristics of voglibose for determining the appropriate study design and parameters for a pharmacodynamic equivalence study of voglibose. METHODS: This study consisted of two studies. The single dose study had an open and single sequence design. Nineteen subjects received placebo and then one tablet of voglibose on two consecutive days with sucrose. The multiple dose study was performed with the similar design, except that it was a multiple dose of the single dose study. Nine subjects who showed an effective response in the single dose study received placebo three times and then voglibose 4 times on two consecutive days. Serial blood samples for pharmacodynamic parameters were taken until 180 mins after each administration. The baseline adjusted maximum serum glucose level (G(max)) and area under the serum glucose level-time profiles were determined and compared. RESULTS: In the single dose study, the difference in G(max) was -10.6 +/- 28.7 mg/dL. The area under the serum glucose concentration-time curve (AUGC(0-1h)) of placebo and voglibose were 7825.0 +/- 1145.3 mg.min/dL, 7907.5 +/- 917.2 mg.min/dL, respectively. In the multiple dose study, the difference in G(max) was 46.6 +/- 16.1 mg/dL. The AUGC(0-1h) of placebo and voglibose were 8138.6 +/- 721.9 mg.min/dL and 6499.7 +/- 447.2 mg.min/dL, respectively. The G(max) and AUGC(0-1h) of the multiple dose study was significantly different between placebo and voglibose in paired t-test. CONCLUSION: The differences in G(max) and AUGC(0-1h) are suitable for pharmacodynamic parameters to evaluate bioequivalence of voglibose.

Comparative evaluation of voglibose versus pioglitazone on glycaemic control and lipid profile in patients of type 2 diabetes mellitus on glimepiride and metformin in punjabi population.

Background: Type 2 Diabetes mellitus (DM) is a heterogeneous group of disorders associated with both microvascular and macrovascular complications. Due to progressive nature of type 2 DM, dual / triple drug therapy produce additive effects, less side effects and allows the use of submaximal doses of individual agents. Therefore, the present study was designed to study the effect of voglibose in comparison to pioglitazone on glycaemic and lipid profile as an add-on drug in patients with DM whose glycaemic status was uncontrolled with glimepiride and metformin. Methods: The present study was open, randomized parallel group comparison of two active treatment groups over a six months period. Sixty patients of either sex in the age group of 30-75 years, suffering from type 2 DM, with FBG> 126 mg/dl and HbA1c between 7- 10 % were selected at random. The effect of voglibose and pioglitazone were observed on various parameters i.e. FBG, PPBG, HbA1c and lipid profile (Total cholesterol, TG, LDL, VLDL). Results: At the end of 6 months it was observed that though both pioglitazone and voglibose reduced FBG, PPBG and HbA1C significantly but pioglitazone caused a significantly greater percentage change in FBG as well as in PPBG whereas the difference in mean percentage change in HbA1C was not significant. Also, fall in total cholesterol, TG, LDL and VLDL was significantly greater with pioglitazone than voglibose. Few side effects were observed with voglibose and not with pioglitazone. Conclusions: Though pioglitazone and voglibose were equally effective in lowering HbA1C levels yet pioglitazone showed better results in improving FBG, PPBG and lipid profile as compared to voglibose. Pioglitazone had minimal side effects as compared to voglibose.