Detail of "72432-03-2"

CAS Number:
72432-03-2
Name:
Miglitol
Molecular Structure:
Formula:
C₈H₁₇NO₅
Molecular Weight:
207.2243
Synonyms:
3,4,5-Piperidinetriol,1-(2-hydroxyethyl)-2-(hydroxymethyl)-, [2R-(2a,3b,4a,5b)]-;BAY 1099;BAY-m 1099;Diastabol;Glyset;3,4,5-Piperidinetriol,1-(2-hydroxyethyl)-2-(hydroxymethyl)-, (2R,3R,4R,5S)-;
EINECS:
276-661-6
Density:
1.458 g/cm³
Melting Point:
114 °C
Boiling Point:
453.7 °C at 760 mmHg
Flash Point:
284.3 °C
Appearance:
white to light yellow crystal powder

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Reference

Pharmacokinetics of miglitol: Pharmacokinetics of miglitol. Absorption, distribution, metabolism, and excretion following administration to rats, dogs, and man. Ahr, Hans Jurgen; Boberg, Michael; Brendel, Erich; Krause, Hans Peter; Steinke, Wolfram (Bayer A.-G., Wuppertal D-42096, Germany). Arzneimittel-Forschung, 47(6), 734-745 (English) 1997 Cantor. CODEN: ARZNAD. ISSN: 0004-4172. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The absorption, distribution, metab., and excretion of miglitol ((2R,3R,4R,5S)-1-(2-hydroxyethyl)-2-(hydroxymethyl)-3,4,5-piperidinetri ol, CAS 72432-03-2, BAY m 1099) have been studied following single and repeated administration of non-labeled and radiolabeled (3H, 14C) drug to rats, dogs, and human volunteers via different routes of administration (i.v., oral, intraduodenal) and at various doses (o.3-450 mg/kg). After i.v. administration, miglitol is excreted rapidly and completely via the renal route. No indication was found for a metabolization of radiolabeled miglitol. The (renal) clearance of miglitol is in the range of the glomerular filtration rate. Miglitol is rapidly eliminated from plasma with apparent elimination half-lives of 0.4-1.8 h. Miglitol is virtually not bound to plasma proteins. After oral administration miglitol is rapidly and at low doses also completely absorbed. At higher doses (3 5 mg/kg in rats and dogs, > 50 mg in humans) a satn. of absorption becomes evident. Miglitol is distributed predominantly in the extracellular space. The vols. of distribution are low (o.3-0.8 l/kg). In rats high concns. were initially found in the kidneys, the blood and some well-perfused tissues. The permeation across the blood/brain barrier is very low. Elimination from organs and tissues occurs rapidly resulting in very low residual radioactivity in the body 2 days after dosing (< 0.9% of the dose). At this very low concn. level a terminal elimination phase of radioactivity characterized by half-lives of 50-110 h was obsd. giving rise to a slight tendency for accumulation (accumulation factors < 6) following repeated administration to rats. In pregnant rats [14C]miglitol crossed the placental barrier slowly and to a limited extent. In lactating rats miglitol was found in milk in concns. similar to those in the maternal plasma.

Effect of 1-desoxynojirimycin derivatives on small intestinal disaccharidase activities and on active transport in vitro: Effect of 1-desoxynojirimycin derivatives on small intestinal disaccharidase activities and on active transport in vitro. Lembcke, B.; Foelsch, U. R.; Creutzfeldt, W. (Dep. Med., Univ. Goettingen, Goettingen 3400, Fed. Rep. Ger.). Digestion, 31(2), 120-27 (English) 1985. CODEN: DIGEBW. ISSN: 0012-2823. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The influence of 2 new 1-desoxynojirimycin derivs., BAY m 1099 (I) [72432-03-2] and BAY o 1248 [80879-63-6], on rat small intestinal disaccharidase [9068-06-8] and alk. phosphatase [9001-78-9] activity was investigated in vitro. Both compds. are very potent a-glucosidase inhibitors. Tested in the range of 0.1-5.0 mg/mL, inhibition is strongest on sucrase [37288-39-4] (up to 97.1%) and glucoamylase [9032-08-0] (up to 96.7%). BAY m 1099 also reduced (up to 56.4%) b-glucosidase (lactase) [9001-22-3] activity. For both inhibitors a competitive type of sucrase inhibition was demonstrated (Lineweaver-Burk plot). Affinity vs. sucrase was unusually tight. The Ki of BAY m 1099 vs. sucrase amounted to 1.14 ′ 10-7 M and of BAY o 1248 to 6.92 ′ 10-8 M (Dixon plot. Both inhibitors did not impair active transport of L-leucine or methyl-a-D-glucoside into everted rings of rat jejunum in vitro.

Detail of "72432-03-2"

Miglitol

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Reference