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Trelagliptin clathrate, preparation method and application thereof

A technology of inclusion compounds and derivatives, applied in the directions of drug combination, drug delivery, pharmaceutical formulation, etc., can solve the problems of complex crystal form, affecting drug solubility and stability, etc., to enhance water solubility, solve polymorphic or Mixed crystal problem, the effect of improving bioavailability

Inactive Publication Date: 2016-05-11
SHANGHAI SHYNDEC PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Aiming at the above-mentioned technical problems in the prior art, the present invention provides a trexagliptin inclusion compound and its preparation method and application. The described trexagliptin inclusion compound and its preparation method and application solve the The technical problems of complex crystal forms in the trexagliptin drug in the prior art, which affect the solubility and stability of the drug

Method used

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  • Trelagliptin clathrate, preparation method and application thereof
  • Trelagliptin clathrate, preparation method and application thereof
  • Trelagliptin clathrate, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Example 1: Trexagliptin inclusion compound (1:1) A1

[0042] Weigh 5.0 g of α-cyclodextrin, add 100 ml of 50% methanol, add 5.0 g of trexagliptin succinate (crystal form A), sonicate for 3 hours, concentrate to dryness at 60°C to obtain a solid powder, and crush it. According to the water solubility test method, it dissolves in water. DSC analysis results meet the requirements.

Embodiment 2

[0043] Embodiment 2: Trexagliptin inclusion compound (1:1) A2

[0044] Weigh 5.0g of β-cyclodextrin, add 100ml of 75% ethanol, add 5.0g of trexagliptin succinate (crystal form B), stir for 5 hours, and concentrate to dryness at 60°C to obtain a solid powder, which can be obtained by crushing . According to the water solubility test method, it dissolves in water. DSC analysis results meet the requirements.

Embodiment 3

[0045] Embodiment 3: Trexagliptin inclusion compound (1:1) A3

[0046] Weigh 5.0 g of γ-cyclodextrin, add 100 ml of water, add 5.0 g of trexagliptin succinate (form C), stir magnetically for 3.5 hours, concentrate to dryness at 60°C to obtain a solid powder, and crush it. According to the test method of water solubility, it is easily soluble in water. DSC analysis results meet the requirements.

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Abstract

The invention provides a trelagliptin clathrate, which is composed of trelagliptin and cyclodextrin or derivatives of cyclodextrin, and the weight ratio of trelagliptin to cyclodextrin or derivatives of cyclodextrin is 1:1-1:30. The invention also provides a preparation method of the trelagliptin clathrate. According to the preparation method, cyclodextrin or derivatives of cyclodextrin is taken as the subject, trelagliptin is taken as the object, and through the clathration in the presence of a solvent, trelagliptin is included or embedded into cyclodextrin or derivatives of cyclodextrin to from the clathrate. The invention also provides an application of the trelagliptin clathrate in the preparation of drugs for treating diabetes. The trelagliptin clathrate is a new solid state of trelagliptin, the problems of multiple crystal forms or mixed crystals of trelagliptin are solved, thus the production technology is simplified, at the same time, trelagliptin clathrate has the advantages of increased water solubility and good stability, moreover, the preparation method has the advantages of simple and convenient operation, little material loss, and low cost.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and relates to a trexagliptin, in particular to a trexagliptin inclusion compound and a preparation method and application thereof. Background technique [0002] Dipeptidyl peptidase IV (DPP-4), also known as T cell surface antigen CD26, is a serine amino dipeptidase on the cell surface that can trigger incretin (glucagon-like peptide-1 (GLP- 1) and glucose-dependent insulinotropic polypeptide (GIP)), while GLP-1 and GIP play an important role in blood glucose regulation. Inhibition of DPP-4 can increase blood glucose level-dependent insulin secretion, thereby controlling blood glucose levels. DPP-4 inhibitors are the first new type 2 diabetes drugs that can control blood sugar levels by improving the body's own ability, and can be used as a single drug or in combination with other hypoglycemic drugs. Its mechanism of action is unique, and it has unique advantages such as no hypoglycemia, no ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/513A61P3/10
CPCA61K9/0019A61K9/146A61K9/19A61K9/28A61K9/4866A61K31/513
Inventor 黄文武邹凌燕王永祥罗文卿杜会静张超
Owner SHANGHAI SHYNDEC PHARMA CO LTD
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