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Pharmaceutical compositions of combinations of dipeptidyl peptidase-4 inhibitors with metformin

A technology of dipeptidyl peptidase and metformin hydrochloride, which is applied in drug combinations, active ingredients of heterocyclic compounds, sugar-coated pills, etc., can solve problems such as difficult treatment options, inability to fully control blood sugar, and complications

Active Publication Date: 2009-02-11
MERCK SHARP & DOHME BV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For many patients, these regimens do not adequately control blood sugar during long-term treatment, leading to the need for combination therapy years after diagnosis
However, co-prescription of two or more oral antidiabetic drugs leads to complex and difficult treatment regimens for many patients using

Method used

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  • Pharmaceutical compositions of combinations of dipeptidyl peptidase-4 inhibitors with metformin
  • Pharmaceutical compositions of combinations of dipeptidyl peptidase-4 inhibitors with metformin
  • Pharmaceutical compositions of combinations of dipeptidyl peptidase-4 inhibitors with metformin

Examples

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preparation example Construction

[0020] The preparation of sitagliptin and its pharmaceutically acceptable salts is disclosed in US Patent No. 6,699,871, the entire contents of which are incorporated herein by reference. The preparation of sitagliptin phosphate monohydrate is disclosed in International Patent Publication WO 2005 / 0031335 published on January 13, 2005, the entire content of which is incorporated herein by reference.

[0021] The dose concentration of the DPP-4 inhibitor incorporated in the pharmaceutical composition of the present invention is about 1 mg to about 250 mg of the active part. Preferably, the dose concentration of the DPP-4 inhibitor is about 25 mg to about 200 mg of the active part. Discrete dose concentrations are 25, 50, 75, 100, 150, and 200 mg DPP-4 inhibitor active part equivalents. The "active fraction" refers to the free base form of the DPP-4 inhibitor in the anhydrous form.

[0022] The unit dose concentration of sitagliptin free base anhydrate (active part) incorporated into...

Embodiment 1

[0083] Fixed-dose combination of 50 mg sitagliptin and 500 mg metformin hydrochloride per tablet-wet granulation

[0084]

[0085] * Equivalent to 50mg sitagliptin free base anhydrate.

[0086] ** Removed during processing.

[0087] Production method:

[0088] The sitagliptin phosphate monohydrate and metformin hydrochloride are fed into a high-shear granulator or a fluidized bed granulator. In the case of high-shear granulation, in addition to the polyvinylpyrrolidone binder, purified water containing sodium lauryl sulfate is added to APIs (active pharmaceutical ingredients) within 3-5 minutes. The wet material is either dried in a rack at 40°C or in a fluidized bed dryer at an inlet temperature of 45-60°C for 3-6 minutes. In the case of fluidized bed granulation, the purified water containing polyvinylpyrrolidone and sodium lauryl sulfate is added to the APIs within 30-60 minutes. The wet material is dried in a fluidized bed dryer at an inlet temperature of 45-60°C. Then, the ...

Embodiment 2

[0090] Fixed-dose combination of 50 mg sitagliptin and 850 mg metformin hydrochloride per tablet-wet granulation

[0091]

[0092] * Equivalent to 50mg sitagliptin free base anhydrate.

[0093] ** Removed during processing.

[0094] Production method:

[0095] The tablets were prepared by wet granulation using basically the same method as in Example 1, thereby providing 1117 mg uncoated tablets. Tablets are optionally coated with 27.9mg standard Film-coated formulations to provide 1145mg film-coated tablets.

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Abstract

Disclosed are pharmaceutical compositions comprising fixed-dose combinations of a dipeptidyl peptidase-4 inhibitor and metformin, methods of preparing such pharmaceutical compositions, and methods of treating Type 2 diabetes with such pharmaceutical compositions.

Description

Background of the invention [0001] Type 2 diabetes is a chronic and progressive disease caused by a complex pathophysiology involving dual endocrine defects involving insulin resistance and impaired insulin secretion. The treatment of type 2 diabetes generally starts with diet and exercise, followed by oral monotherapy with anti-diabetic drugs. For many patients, these programs do not adequately control blood sugar during long-term treatment, which leads to the need for combination therapy within a few years after diagnosis. However, the co-prescription of two or more oral antidiabetic drugs can lead to complex and difficult treatment options for many patients. Combining two or more anti-diabetic agents into a single tablet provides a possible way to deliver combination therapies that does not increase the complexity of the patient's daily treatment regime. The preparation has been widely accepted in other disease symptoms, such as hypertension (HYZAAR TM It is a combination of Lo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/132A61K31/403A61K47/12A61K31/40A61K31/4985A61P3/10
CPCA61K38/04A61K9/2813A61K9/284A61K9/2077A61K31/4985A61K45/06A61K31/155A61K9/1635A61P3/10A61P43/00A61K2300/00
Inventor A·卡马利L·阿拉尼K·A·弗利萨S·高希M·蒂赫里纳
Owner MERCK SHARP & DOHME BV
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