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Pharmaceutical composition containing valibose, its preparation method and application

A velibose and composition technology, which is applied in the field of velibose-containing compositions, can solve the problems of no velibose preparation method, etc.

Inactive Publication Date: 2011-10-05
SHENZHEN TAITAI PHARMA IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] There is currently no literature showing that a single, specific daily dose of velibose has a particularly beneficial effect on glycemic control and therefore is particularly useful in the treatment of diabetes and diabetes-related diseases, nor is there any information on vitamins containing this single, specific daily dose. Report on the pharmaceutical composition of Libotang and its preparation method

Method used

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  • Pharmaceutical composition containing valibose, its preparation method and application
  • Pharmaceutical composition containing valibose, its preparation method and application
  • Pharmaceutical composition containing valibose, its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0088] 1. Preparation of raw material Validamine

[0089] The raw material Validamine can be prepared by methods disclosed in prior art documents, for example: methods described in J. Antibiotics 24: 57-58, 1971 and Chem. Lctt., 1989, 725-728 (Harii, s.j.T.Iwasa & Y.Kameda), In the preparation process of the present invention, the preparation of the raw material Validamine is to obtain validoxylamineA by hydrolysis of Jinggangmycin A (purchased from Zhejiang Qianjiang Biochemical Co., Ltd., content 60%), and then obtain validoxylamineA from validoxylamineA and N-bromosuccinyl Amine (NBS) reaction to obtain validamine. The reaction formula is as follows:

[0090]

[0091] The reaction product was treated with CG-50NH 4 + Weak acid type cationic resin column, 0.1N ammonia water elution separation to obtain pure Validamine and Valienamine.

[0092] 2. Preparation of velibose in crystal form

[0093] The reaction formula is as follows:

[0094]

[0095] In 2600 ml of a...

Embodiment 1

[0112] Taking Velibose as the test drug, the general condition, blood sugar, fructosamine, urine sugar, blood NAG enzyme activity, serum urea nitrogen and creatinine content, Renal pathological changes and the effects of lipids (including triglycerides, cholesterol and free fatty acids) and cardiac index.

[0113] In the long-term experiment (5 weeks) of streptozotocin (STZ) diabetic rats fed with high-sugar diet, when the daily dose of rats was ≥0.4 mg / kg body weight, (1) Velibose made three Multiple symptoms were significantly relieved and food intake was reduced, indicating that velibose can be used to treat overeating and the obesity caused by it; (2) velibose significantly reduced fasting blood sugar, non-fasting blood sugar, serum Fructosamine and urine sugar indicate that velibose can improve the glucose metabolism of hyperglycemic animals and can be used to prevent or treat diabetes; (3) velibose can significantly improve serum NAG enzyme activity, serum urea nitrogen ...

Embodiment 2

[0182] I prescription

[0183]

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PUM

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Abstract

The invention relates to a pharmaceutical composition containing Weilibo sugar and its preparing process, wherein the composition comprises 0.5-50mg of pharmaceutically acceptable Weilibo sugar and optional carrying agent. The invention also provides the use of the pharmaceutical composition in the preparation of medicament for the treatment or prevention of diabetes and diabetes-related diseases.

Description

technical field [0001] The invention relates to a composition containing velibose, in particular to a pharmaceutical composition containing velibose. [0002] The invention also relates to a preparation method of the pharmaceutical composition. [0003] The invention also relates to the application of the pharmaceutical composition in the field of medicine. Background technique [0004] Valibose (chemical name: (+)-(1S, 2S, 3S, 4R, 5R)-1-amino-5-hydroxymethyl-N-2-(1,3-dihydroxypropyl )-2,3,4-cyclohexanetriol) has been disclosed in US Pat. No. 4,701,559 and US4,777,294, and its structural formula [I] is: [0005] [0006] Velibose is an α-glucosidase inhibitor. After oral administration, it can competitively and antagonistically inhibit the disaccharide hydrolase (α-glucosidase) in the intestine, thereby delaying the digestion and absorption of carbohydrates, thereby improving the High blood sugar after meals. Postprandial hyperglycemia can hinder the secretion and act...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/133A61P3/10
Inventor 闫鹏常弘杰李志明张验军朱嘉蓉
Owner SHENZHEN TAITAI PHARMA IND
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