Miglitol was orally administered at 40 mg/100 g of high-fat diet containing 45% kcal as fat to 12-week-old rats for 29 days, and age-matched rats without the agent were used as the respective controls

Absorption, Distribution and Excretion
Miglitol absorption is saturated at high doses; a 25 mg dose is completely absorbed, while a 100 mg dose is only 50-70% absorbed. There is no evidence that systemic absorption of miglitol enhances its therapeutic effect. Miglitol is not metabolized in humans or any of the animal species studied. It is excreted unchanged via the kidneys. 0.18 L/kg Miglitol absorption is saturated at high doses: a 25 mg dose is completely absorbed, while a 100 mg dose is only 50%-70% absorbed. Peak plasma concentrations are reached within 2-3 hours at all doses. The therapeutic effect is primarily due to its local action on the small intestine; there is no evidence that systemic absorption contributes to the therapeutic response. The protein binding rate of miglitol is negligible (<4.0%). The volume of distribution of miglitol is 0.18 L/kg, consistent with its predominant distribution in the extracellular fluid. Miglitol is primarily distributed in the extracellular fluid and concentrates in the intestinal cells of the small intestine. For more complete data on the absorption, distribution, and excretion of miglitol (9 items in total), please visit the HSDB record page. Metabolism/Metabolites Miglitol is not metabolized in humans or any of the animal species studied. No metabolites have been detected in plasma, urine, or feces, indicating no systemic or first-pass metabolism. Biological Half-Life The elimination half-life of miglitol from plasma is approximately 2 hours. ... Miglitol is rapidly eliminated from plasma, with an apparent elimination half-life of 0.4–1.8 hours. ... At very low concentration levels, the terminal elimination phase of radioactive substances is characterized by a half-life of 50–110 hours... The elimination half-life of miglitol from plasma is approximately 2 hours.

Hepatotoxicity
In several large clinical trials, the incidence of elevated serum transaminases in the miglitol group was not higher than in the placebo group, and all elevations were asymptomatic, returning to normal rapidly after discontinuation of the drug. Neither during these studies nor since miglitol's approval and widespread clinical use have there been reports of clinically significant liver injury caused by miglitol. Therefore, even if miglitol-induced liver injury occurs, it must be extremely rare. Furthermore, there are no reports of patients switching to miglitol after experiencing liver injury while taking acarbose. Probability Score: E (Unlikely to cause clinically significant liver injury). Pregnancy and Lactation Effects ◉ Overview of Use During Lactation Limited data suggest that miglitol is rarely excreted into breast milk. Due to the low oral absorption rate of miglitol, it is unlikely to have adverse effects on breastfed infants. ◉ Effects on Breastfed Infants As of the revision date, no relevant published information was found.
◉ Effects on Lactation and Breast Milk
As of the revision date, no relevant published information was found.

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Protein Binding
The protein binding rate of miglitol is negligible (<4.0%).

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Interactions
Several studies have explored the potential interaction between miglitol and glibenclamide. In a study of six healthy volunteers, subjects received a single 5 mg dose of glibenclamide in addition to a six-day course of miglitol (50 mg three times daily for four days; followed by 100 mg three times daily for two days) or placebo. Results showed that the mean Cmax and AUC values of glibenclamide were reduced by 17% and 25%, respectively, compared to miglitol alone. Another study in diabetic patients explored the effects of adding miglitol (100 mg three times daily for seven days) or placebo to a daily course of 3.5 mg glibenclamide. The results showed that the mean AUC value decreased by 18% in the miglitol treatment group, but this difference was not statistically significant. More information on potential interactions with glibenclamide comes from a large US clinical trial (Study 7). In this trial, patients received either miglitol or a placebo in addition to taking 10 mg glibenclamide twice daily. At 6 months and 1 year follow-up, patients taking 100 mg miglitol three times daily had a 16% and 8% lower mean Cmax value for glibenclamide, respectively, compared to patients taking glibenclamide alone. However, these differences were not statistically significant. Therefore, although there is a trend towards lower AUC and Cmax values for glibenclamide when used in combination with miglitol, based on the above three studies, no definitive conclusions can be drawn regarding potential interactions. The pharmacokinetics of miglitol on a single dose of 1000 mg metformin were investigated in healthy volunteers. Compared to the placebo group, volunteers taking miglitol experienced a 12% to 13% reduction in mean AUC and Cmax values for metformin, but this difference was not statistically significant. In a study of healthy volunteers, concomitant administration of miglitol and digoxin three times daily reduced mean plasma concentrations of digoxin by 19% and 28%, respectively. However, in diabetic patients receiving digoxin treatment, concomitant administration of miglitol did not alter plasma digoxin concentrations… Other studies in healthy volunteers have shown that miglitol significantly reduces the bioavailability of ranitidine and propranolol by 60% and 40%, respectively. No pharmacokinetic or pharmacodynamic effects of miglitol on nifedipine were observed. For more complete data on miglitol interactions (9 in total), please visit the HSDB records page.

Eur J Pharmacol.2009 Dec 10;624(1-3):51-7;Horm Metab Res.2009 Mar;41(3):213-20.

Therapeutic Uses
1-Deoxynojirimycin/ analogues and derivatives; α-glucosidase/antagonists and inhibitors; enzyme inhibitors. In healthy individuals, a single dose may result in a sustained decrease in postprandial blood glucose levels for 3-4 hours. Miglitol is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes. /US product label contains/

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Drug Warnings Miglitol is contraindicated in patients with known hypersensitivity to this drug or diabetic ketoacidosis. This drug is contraindicated in patients with inflammatory bowel disease, ulcerative colitis, partial intestinal obstruction or those susceptible to this disease, chronic intestinal diseases with significant digestive or malabsorption disorders, and other comorbidities that may exacerbate the condition due to increased intestinal gas production. Miglitol alone, taken on an empty stomach or after a meal, does not cause hypoglycemia. The risk of hypoglycemia increases when miglitol is used in combination with insulin or sulfonylureas. If hypoglycemia occurs, the dosage of these medications should be adjusted accordingly. For mild to moderate hypoglycemia, oral glucose (dextrose) should be used instead of sucrose (table sugar, a disaccharide); miglitol does not delay the absorption of oral glucose (a monosaccharide). Severe hypoglycemia may require intravenous glucose infusion or glucagon injection. In stressful situations (e.g., fever, trauma, infection, surgery), patients taking miglitol may be at risk of losing glycemic control; temporary insulin use may be necessary. For more drug warnings about miglitol (full version) (11 in total), please visit the HSDB record page.

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Pharmacodynamics
Miglitol is an oral alpha-glucosidase inhibitor, a derivative of deoxynojirimycin, that delays the digestion of ingested carbohydrates, thereby reducing the postprandial rise in blood glucose concentration. Due to the reduced plasma glucose levels, miglitol can lower glycated hemoglobin levels in patients with type II (non-insulin-dependent) diabetes. Systemic non-enzymatic protein glycosylation, reflected in glycated hemoglobin levels, is a function of mean blood glucose concentration over time. Due to their different mechanisms of action, miglitol's effect in enhancing glycemic control has an additive effect when used in combination with sulfonylureas. Furthermore, miglitol can reduce the insulin-stimulating and weight-gaining effects of sulfonylureas. Miglitol has a weak inhibitory effect on lactase; therefore, at recommended doses, it is not expected to cause lactose intolerance.

C8H17NO5

207.22

207.11

72432-03-2

Miglitol-d4;2714473-10-4

441314

White to pale-yellow powder
Crystals from ethanol

1.5±0.1 g/cm3

453.7±45.0 °C at 760 mmHg

114ºC

284.3±27.4 °C

0.0±2.5 mmHg at 25°C

1.598

-1.4

5

6

3

14

179

4

O([H])[C@@]1([H])[C@@]([H])([C@]([H])(C([H])([H])N(C([H])([H])C([H])([H])O[H])[C@]1([H])C([H])([H])O[H])O[H])O[H]

IBAQFPQHRJAVAV-ULAWRXDQSA-N

InChI=1S/C8H17NO5/c10-2-1-9-3-6(12)8(14)7(13)5(9)4-11/h5-8,10-14H,1-4H2/t5-,6+,7-,8-/m1/s1

(2R,3R,4R,5S)-1-(2-hydroxyethyl)-2-(hydroxymethyl)piperidine-3,4,5-triol

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)

Solubility in Formulation 1: 100 mg/mL (482.58 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.

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