Pharmaceutical compositions of a combination of metformin and a dipeptidyl peptidase-IV inhibitor

A technology of metformin hydrochloride and composition, which is applied in the field of combined pharmaceutical composition of metformin and dipeptidyl peptidase-IV inhibitor, which can solve problems such as difficult treatment plan, insufficient control of blood sugar, and complexity

Inactive Publication Date: 2011-01-26
MERCK & CO INC
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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 glycemia during long-term treatment, resulting in the need for combination therapy for years after diagnosis
However, the total of two or more oral antidiabetic drugs. Prescribing can lead to complex and difficult treatment regimens for many patients using

Method used

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  • Pharmaceutical compositions of a combination of metformin and a dipeptidyl peptidase-IV inhibitor
  • Pharmaceutical compositions of a combination of metformin and a dipeptidyl peptidase-IV inhibitor
  • Pharmaceutical compositions of a combination of metformin and a dipeptidyl peptidase-IV inhibitor

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Experimental program
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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 US Patent No. 7,326,708, the entire contents of which are incorporated herein by reference.

[0021] The unit dose concentrations of sitagliptin free base anhydrate (active moiety) for inclusion into the fixed dose combination pharmaceutical compositions of the present invention are 25, 50 and 100 mg. Sitagliptin phosphate monohydrate was used in the pharmaceutical composition in an amount equivalent to that of sitagliptin free base anhydrate, ie 32.125, 64.25 and 128.5 mg, respectively.

[0022] The unit dose concentrations of metformin hydrochloride incorporated into the fixed dose combinations of the present invention are 250, 500, 750, 850 and 1000 mg. These unit dosage concentrations of metformin hydrochloride represen...

Embodiment 1

[0112] 50 or 100 mg of sitagliptin coated with sustained release polymer (3% w / w level) and Fixed-dose combination of 1000 mg of metformin hydrochloride

[0113] Element 100 / 1000 100 / 1000 50 / 1000 50 / 1000

[0114] mg / tablet %w / w mg / tablet %w / w

[0115] 1. Chip tablet

[0116] Metformin HCl 1000 76.725 10007 6.725

[0117] PVP K29 / 32 75.27 5.775 75.27 5.775

[0118] Avicel PH 102 TM 195.50 15 195.50 15

[0119] Silica 6.517 0.5 6.517 0.5

[0120] Sodium stearyl fumarate 26.067 2.0 26.067 2.0

[0121] Total amount of chips 1303.36 100 1303.36 100

[0122] 2. Cellulose acetate

[0123] (CA) polymer bag

[0124] Clothes

[0125] CA-398-10 19.55 1.5 19.55 1.5

[0126] PEG 3350 9.775 0.75 9.775 0.75

[0127] Triacetin 9.775 0.75 9.775 0.75

[0128] Total CA SR coating 39.1 3 39.1 3

[0129] SR coated tablet 1342.46 103 1342.46 103

[0130] 3. Sitagliptin pack

[0131] Clothes

[0132] Sitagliptin phosphate 12...

Embodiment 2

[0167] 50 or 100 mg of sitagliptin and 1000 mg coated with sustained release polymer (5% w / w) fixed-dose combination of metformin hydrochloride in milligrams

[0168] Element 100 / 1000 100 / 1000 50 / 1000 50 / 1000

[0169] mg / tablet %w / w mg / tablet %w / w

[0170] 1. Chip tablet

[0171] Metformin HCl 1000 76.725 1000 76.725

[0172] PVP K29 / 32 75.27 5.775 75.27 5.775

[0173] Avicel PH 102 TM 195.50 15 195.50 15

[0174] Silica 6.517 0.5 6.517 0.5

[0175] Sodium stearyl fumarate 26.067 2.0 26.067 2.0

[0176] Total amount of chips 1303.36 100 1303.36 100

[0177] 2. Cellulose acetate

[0178] (CA)

[0179] polymer coating

[0180] CA-398-10 32.58 2.53 2.58 2.5

[0181] PEG 3350 16.29 1.25 16.29 1.25

[0182] Triacetin 16.29 1.25 16.29 1.25

[0183] Total CA SR coating 65.16 5 65.16 5

[0184] SR coated tablet 1368.42 105 1368.42 105

[0185] 3. Sitagliptin pack

[0186] Clothes

[0187] Sitagliptin phosphate 128.52* ...

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Abstract

Disclosed are pharmaceutical compositions comprising fixed-dose combinations of an extended-release form of metformin, or a pharmaceutically acceptable salt thereof, coated with an immediate-release form of the DPP-4 inhibitor sitagliptin, or a pharmaceutically acceptable salt thereof.

Description

Background of the invention [0001] Type 2 diabetes is a chronic and progressive disease resulting from a complex pathophysiology of dual endocrine defects involving insulin resistance and impaired insulin secretion. Treatment of type 2 diabetes generally begins with diet and exercise, followed by oral antidiabetic drug monotherapy. For many patients, these regimens do not adequately control glycemia during long-term treatment, resulting in the need for combination therapy for years after diagnosis. However, the total of two or more oral antidiabetic drugs. Prescribing can lead to complex and difficult treatment regimens for many of the patients employed. Combining two or more oral antidiabetic agents into a single tablet provides a possible way to deliver combination therapy without adding complexity to a patient's daily regimen. Such preparations have been widely accepted in other disease conditions such as hypertension (HYZAAR is a combination of losartan potassium and ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A01N37/52A61K31/155A61K9/22
CPCA61K31/155A61K9/209A61P3/10
Inventor N·普尔卡沃斯
Owner MERCK & CO INC
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