Miglitol crystal and method for preparing same

A technology for miglitol and crystals, which is applied to the field of crystalline miglitol and its preparation, can solve the problems of different and different bioavailability, and achieve the effects of easy purification, low hygroscopicity and simple preparation method.

Active Publication Date: 2008-10-22
ZHEJIANG MEDICINE CO LTD XINCHANG PHAMACEUTICAL FACTORY
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Problems solved by technology

Different crystal forms of the same drug may have significantly different dissolution properties, s

Method used

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  • Miglitol crystal and method for preparing same
  • Miglitol crystal and method for preparing same
  • Miglitol crystal and method for preparing same

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Embodiment Construction

[0019] The present invention will be specifically described below in conjunction with examples, and the examples of the present invention are only used to illustrate the technical solutions of the present invention, and are not intended to limit the present invention.

[0020] 1. Preparation of crystalline miglitol

[0021] Hydrogenation rearrangement of 6-(2-hydroxyethyl)-amino-6-deoxy-α-L-sorbofuranose: In a 50L hydrogenation reactor, 6-(2-hydroxyethyl)-amino-6 - Add 2.0Kg of crude deoxy-α-L-sorbofuranose to 30L of water, then add 1.0Kg of 5% palladium carbon, dissolve it, inhale into the reaction kettle, inject hydrogen, keep the pressure at 2.0-3.0Mpa and start the reaction for 24 hours. After the reaction, filter to recover palladium carbon.

[0022] Isolation purification of Miglitol: Pump the miglitol filtrate obtained above into an ion exchanger equipped with 50L of ion exchange resin D001, wash with 400L, control the flow rate of 20L / hr; then use 0.5N The ammonia wa...

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Abstract

The invention discloses a crystalline miglitol and a preparation method thereof. The technical contents related to the crystalline miglitol are not recorded in the existing literature. The miglitol crystal of the invention uses Cu-Ka radiation, and diffraction peaks are arranged at 14.1 degrees, 15.9 degrees, 19.5 degrees and 23.5 degrees of a powder X-ray diffraction spectrum which is embodied by a diffraction angle of 2 theta plus or abstract 0.2 degree. The crystalline miglitol has the advantages of low moisture absorption and being easy to purify except in the condition of high humidity; the crystalline miglitol which is excellent in stability is beneficial for the preparation of pharmaceutical preparation and improving bioavailability of drug.

Description

technical field [0001] The present invention relates to alpha-glucosidase inhibitors, in particular to crystalline miglitol and a preparation method thereof. Background technique [0002] Miglitol (Miglitol or Bay-m-1099), also known as Glyset, is a new type of hypoglycemic drug researched and developed by German Bayer Pharmaceutical Company in the early 1980s. It is an α-glucosidase inhibitor for the treatment of type 2 diabetes - non-insulin-dependent diabetes mellitus (NIDD). The chemical name of Miglitol is: [2R, 3R, 4R, 5S]-1-(2-hydroxyethyl)-2-(hydroxymethyl)-3,4,5-trihydroxypiperidinetriol. The structure of Miglitol is similar to that of glucose, and its molecular structure is as follows: [0003] Molecular formula: C 8 h 17 NO 5 , molecular weight: 207.1. [0004] Miglitol can reversibly competitively inhibit the pseudomonosaccharide α-glucosidase attached to the intestinal membrane, reduce the metabolism of monosaccharide, delay the release of glucose and re...

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Application Information

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IPC IPC(8): C07D211/40A61K31/44A61P3/10
Inventor 胡三明陶正利孙新强
Owner ZHEJIANG MEDICINE CO LTD XINCHANG PHAMACEUTICAL FACTORY
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