Voglibose targets intestinal α-glucosidases (maltase, sucrase, and others) located in the brush border of the small intestine. It competitively inhibits these enzymes, delaying the hydrolysis of oligosaccharides and disaccharides into absorbable monosaccharides. This reduces postprandial glucose absorption and blunts post-meal hyperglycemia. Ki values are approximately 10⁶-10⁵ times smaller than Km values for sucrase and maltase.

In vitro, voglibose demonstrates potent inhibitory activity against α-glucosidases, including maltase and sucrase. It is one of the most important α-glucosidase inhibitors. Enzyme inhibition assays confirm its competitive mechanism of action against sucrase and maltase with extremely low Ki values.

In vivo, voglibose reduces postprandial hyperglycemia in diabetic animal models and humans. It lowers blood glucose levels after meals by delaying carbohydrate digestion and absorption. In patients with type 2 diabetes, it improves glycemic control, especially postprandial glucose, without causing significant hypoglycemia.

α-Glucosidase inhibitory activity is assessed using enzyme preparations from rat intestinal acetone powder or purified enzymes (sucrase, maltase). Enzyme is incubated with substrate (sucrose or maltose) and voglibose at various concentrations. Glucose production is measured colorimetrically using glucose oxidase-peroxidase reagents. IC₅₀ and Ki values are calculated from enzyme kinetics.

In vitro cell-based assays using intestinal epithelial cell lines (e.g., Caco-2) evaluate glucose transport inhibition. Cells are cultured on transwell inserts to form polarized monolayers. Glucose transport is measured by adding glucose to the apical side and quantifying glucose in the basolateral compartment. The effect of voglibose on glucose transport is assessed.

In vivo efficacy is evaluated in animal models of diabetes (e.g., streptozotocin-induced diabetic rats, db/db mice, or Zucker diabetic fatty rats). Voglibose is administered orally before or with a carbohydrate-containing meal. Postprandial blood glucose is measured at various time points. Oral glucose tolerance tests (OGTT) are performed to assess glucose-lowering efficacy.

Absorption, Distribution and Excretion
Absorption is slow and poor. The pharmacokinetic parameters reported for voglibose in combination with metformin are: Cmax 1.38 mcg/ml, AUC 8.17 mcg·h/ml, and tmax 2.5 hours. Metabolism/Metabolites Metabolism is minimal; no metabolites have been identified to date. Biological Half-Life The half-life of voglibose is very similar to that of metformin, reported to be 4.08 hours.
Voglibose is poorly absorbed from the gastrointestinal tract, with minimal systemic bioavailability. It acts locally in the intestinal lumen. The drug is primarily excreted unchanged in feces. Its lack of systemic absorption contributes to its favorable safety profile, with minimal risk of systemic adverse effects.

Voglibose is generally well-tolerated with a favorable safety profile. The most common adverse effects are gastrointestinal, including flatulence, abdominal distension, and diarrhea due to increased carbohydrate fermentation in the colon. These effects are dose-dependent and tend to diminish with continued use. Hypoglycemia is rare when used as monotherapy.

Voglibose is an organic molecular entity. Voglibose is an alpha-glucosidase inhibitor used to lower postprandial blood glucose levels in patients with diabetes. It is manufactured by Ranbaxy Laboratories in India and marketed under the brand name Volix. Voglibose is a valine amine derivative and also an alpha-glucosidase inhibitor with hypoglycemic activity. Voglibose binds to and inhibits the activity of alpha-glucosidase. Alpha-glucosidase is an intestinal enzyme located in the brush border of the small intestine that hydrolyzes oligosaccharides and disaccharides into glucose and other monosaccharides. This prevents larger carbohydrates from breaking down into glucose, thereby reducing the rise in postprandial blood glucose levels. Pharmacological Indications: For the treatment of diabetes. It is specifically designed to lower postprandial blood glucose levels, thereby reducing the risk of macrovascular complications. Mechanism of Action: Alpha-glucosidase inhibitors are sugars that act as competitive inhibitors of the enzymes required to digest carbohydrates: specifically alpha-glucosidase in the brush border of the small intestine. Membrane-bound intestinal alpha-glucosidases hydrolyze oligosaccharides, trisaccharides, and disaccharides into glucose and other monosaccharides in the small intestine. Acarbose, in addition to inhibiting membrane-bound alpha-glucosidase, also blocks pancreatic alpha-amylase. Pancreatic alpha-amylase hydrolyzes complex starch into oligosaccharides in the lumen of the small intestine. Inhibiting these enzyme systems reduces the rate of digestion of complex carbohydrates. Because carbohydrates cannot be broken down into glucose molecules, less glucose is absorbed. For diabetic patients, the short-term effect of these drugs is to lower current blood glucose levels; the long-term effect is a slight reduction in glycated hemoglobin A1c levels. (Excerpt from Nursing Drug Therapy, Second Edition)

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Pharmacodynamics
Voglibose is an alpha-glucosidase inhibitor, a synthetic compound with potent and long-lasting therapeutic effects on sensory, motor, and autonomic nervous system disorders caused by diabetes. It was approved in Japan in 1994 for the treatment of diabetes, and Takeda Pharmaceutical Company is conducting further research on it for the treatment of impaired glucose tolerance. Alpha-glucosidase inhibitors are oral hypoglycemic agents used to treat type 2 diabetes. Their mechanism of action is to inhibit the digestion of complex carbohydrates, such as starch. Complex carbohydrates are normally converted into monosaccharides, which are absorbed through the intestines. Therefore, alpha-glucosidase inhibitors reduce the effect of complex carbohydrates on blood glucose.
Voglibose (Basen, Glustat, AO-128) is an α-glucosidase inhibitor approved for the treatment of type 2 diabetes mellitus. It is marketed in Japan, India, and other Asian countries. It is typically administered orally at doses of 0.2-0.3 mg three times daily before meals. Its low systemic absorption makes it a safe option for managing postprandial hyperglycemia.

C10H21NO7

267.2762

267.131

83480-29-9

444020

White to off-white solid powder

1.6±0.1 g/cm3

601.9±55.0 °C at 760 mmHg

162-163ºC

274.1±22.1 °C

0.0±3.9 mmHg at 25°C

1.636

-2.36

8

8

5

18

263

5

C1[C@@H]([C@@H]([C@H]([C@@H]([C@]1(CO)O)O)O)O)NC(CO)CO

FZNCGRZWXLXZSZ-CIQUZCHMSA-N

InChI=1S/C10H21NO7/c12-2-5(3-13)11-6-1-10(18,4-14)9(17)8(16)7(6)15/h5-9,11-18H,1-4H2/t6-,7-,8+,9-,10-/m0/s1

(1S,2S,3R,4S,5S)-5-(1,3-dihydroxypropan-2-ylamino)-1-(hydroxymethyl)cyclohexane-1,2,3,4-tetrol

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

H2O : ~250 mg/mL (~935.35 mM)
DMSO : ~100 mg/mL (~374.14 mM)

Solubility in Formulation 1: ≥ 2.5 mg/mL (9.35 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 2: ≥ 2.5 mg/mL (9.35 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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Solubility in Formulation 3: 100 mg/mL (374.14 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

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 (Please use freshly prepared in vivo formulations for optimal results.)