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Pharmaceutical composition containing sitagliptin and metformin, and preparation method thereof

A technology for metformin and a composition, which is applied in the field of pharmaceutical compositions containing sitagliptin and metformin and the preparation thereof, can solve the problems of increased substance content, decreased stability and the like, and can reduce the generation of related substances, reduce content, The effect of improving stability

Pending Publication Date: 2022-02-15
HEFEI PINGGUANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The original research patent of the drug CN 101932241A discloses its prescription and process. However, it was found during research and development that the drug had stability problems. After storage under high temperature, high humidity and light conditions, the stability decreased significantly, and the content of related substances increased significantly.

Method used

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  • Pharmaceutical composition containing sitagliptin and metformin, and preparation method thereof
  • Pharmaceutical composition containing sitagliptin and metformin, and preparation method thereof
  • Pharmaceutical composition containing sitagliptin and metformin, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] A pharmaceutical composition containing sitagliptin and metformin, consisting of a metformin sustained-release layer and a sitagliptin immediate-release layer; the metformin sustained-release layer is composed of the following raw and auxiliary materials in parts by weight: 200 parts of metformin hydrochloride; 55 parts of methylcellulose; 9 parts of polyvinylpyrrolidone; 36 parts of pure water; 3 parts of magnesium stearate; 100 parts of lactose monohydrate; 1.5 parts of hypromellose; 20 parts of pure water; 0.75 parts of magnesium stearate; 0.38 parts of L-ascorbic acid.

[0028] Its preparation method comprises the following steps:

[0029] (1) Preparation of metformin sustained-release mixed granules:

[0030] After mixing 200 parts of metformin hydrochloride and 55 parts of hypromellose in a high-efficiency wet granulator, spray 36 parts of pure water, 9 parts of polyvinylpyrrolidone, 1.5 parts of L- Ascorbic acid mixed with the binder mixture, the soft material ...

Embodiment 2

[0036] A pharmaceutical composition containing sitagliptin and metformin, consisting of a metformin slow-release layer and a sitagliptin immediate-release layer; the composition of the metformin sustained-release layer is the same as in Example 1; the sitagliptin immediate release The layer comprises the following raw and auxiliary materials in parts by weight: 50 parts of sitagliptin; 100 parts of mannitol; 1.5 parts of hypromellose; 20 parts of pure water; 0.75 parts of magnesium stearate; It is prepared by the same method as in Example 1 according to the formula. After observation, the obtained sample has good appearance, uniform color, and the film coating is intact without damage.

Embodiment 3

[0038] A pharmaceutical composition containing sitagliptin and metformin, consisting of a metformin sustained-release layer and a sitagliptin immediate-release layer; the metformin sustained-release layer is composed of the following raw and auxiliary materials in parts by weight: 300 parts of metformin hydrochloride; 100 parts of methyl cellulose; 20 parts of polyvinyl alcohol; 50 parts of pure water; 2.5 parts of calcium stearate; 60 parts of gliptin; 80 parts of mannitol; 3 parts of polyvinyl alcohol; 15 parts of pure water; 0.8 parts of calcium stearate; 0.8 parts of propyl gallate.

[0039] Its preparation method comprises the following steps:

[0040] (1) Preparation of metformin sustained-release mixed granules:

[0041] After mixing 300 parts of metformin hydrochloride and 100 parts of hypromellose in a high-efficiency wet granulator, spray 50 parts of pure water, 20 parts of polyvinyl alcohol, and 3 parts of gallic acid with a high-pressure atomizing two-fluid spray gu...

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Abstract

The invention discloses a pharmaceutical composition containing sitagliptin and metformin. The pharmaceutical composition is composed of a metformin sustained-release layer and a sitagliptin quick-release layer, and the metformin sustained-release layer is composed of the following raw and auxiliary materials in parts by weight: 200-300 parts of metformin hydrochloride; 50-100 parts of hydroxypropyl methylcellulose; 8-20 parts of an adhesive; 30-50 parts of a wetting agent; 1-3 parts of a lubricant; and 1-5 parts of an antioxidant; and the sitagliptin quick release layer comprises the following raw and auxiliary materials in parts by weight: 20-60 parts of sitagliptin; 40-100 parts of a hydrophilic diluent; 1-5 parts of the adhesive; 10-20 parts of the wetting agent; 0.05-1 part of the lubricant; and 0.1-1 part of the antioxidant. The stability of sitagliptin is improved by optimizing a prescription and a process, and the impurity content of the sitagliptin and metformin composition is obviously superior to that of an original developed preparation.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a pharmaceutical composition containing sitagliptin and metformin and a preparation method thereof. Background technique [0002] Type 2 diabetes (type 2diabetes mellitus, T2DM) is a metabolic disease characterized clinically by chronic hyperglycemia. According to the statistics of the World Health Organization (WHO), there are 347 million diabetic patients in the world, 90% of which belong to T2DM. Strict blood sugar control is the key to the treatment of T2DM. [0003] Metformin (metformin, MET) is a first-line treatment drug recommended by multiple diabetes treatment guidelines, and its efficacy and safety have been clinically confirmed. DPP-4 is an enzyme in the human body, its main function is to decompose proteins in the body, and it is an upstream regulator of GLP-1. DPP-4 inhibitors can achieve similar therapeutic effects to GLP-1 agonists. Since DPP-4 inhib...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K31/4985A61K31/155A61K47/24A61K47/12A61K47/38A61K47/14A61P3/10
CPCA61K9/209A61K9/2013A61K9/2054A61K31/4985A61K31/155A61P3/10A61K2300/00
Inventor 解启慧杨超宇聂甜甜王龙龙
Owner HEFEI PINGGUANG PHARMA
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