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Pharmaceutical composition of sitagliptin

A technology of sitagliptin phosphate and its composition, which is applied in the field of pharmaceutical preparations, can solve the problems of poor particle fluidity, poor stability, and low release rate, and achieve large-scale industrial production, good stability, and good dissolution rate Effect

Inactive Publication Date: 2016-12-07
TIANJIN HANRUI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Conventional preparation methods in the prior art prepare sitagliptin preparations. Due to the physical and chemical properties of sitagliptin materials, it is easy to cause poor fluidity, stickiness, poor stability, and low release rate of the particles in the prepared tablet. The process is complicated and the production High cost, difficult to achieve industrialized mass production
[0006] In order to improve product quality and overcome the problem of incapable of industrialized production, we have carried out a lot of design and research on technical solutions, selected the optimal prescription and process, and solved the above technical defects

Method used

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  • Pharmaceutical composition of sitagliptin
  • Pharmaceutical composition of sitagliptin
  • Pharmaceutical composition of sitagliptin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] (1) Prescription

[0061] sitagliptin phosphate 128.5

[0062] Microcrystalline Cellulose 80g

[0063] Calcium hydrogen phosphate 80g

[0064] Croscarmellose Sodium 6.5g

[0065] Magnesium Stearate 12.5g

[0066] Coating agent 12.5g

[0067] 50% ethanol aqueous solution appropriate amount

[0068] Makes 1000 pieces

[0069] (2) Preparation method

[0070] 1) Preparation and processing of raw and auxiliary materials: pass sitagliptin phosphate and other auxiliary materials through an 80-mesh sieve for later use;

[0071] 2) Weighing and mixing: Weigh the above raw and auxiliary materials according to the prescription amount and calculate the feeding amount after checking by two people;

[0072] 3) Mixing: Mix the prescribed amount of sitagliptin phosphate with the prescribed amount of calcium hydrogen phosphate, and then mix it with the prescribed amount of microcrystalline cellulose to make it fully mixed;

[0073] 4) Granulation: Add 50% ethanol water solution t...

Embodiment 2

[0082] (1) Prescription

[0083] Sitagliptin Phosphate 128.5g

[0084] Microcrystalline Cellulose 128.5g

[0085] Calcium hydrogen phosphate 128.5g

[0086] Croscarmellose Sodium 6.5g

[0087] Magnesium Stearate 12.5g

[0088] Coating agent 12.5g

[0089] 50% ethanol aqueous solution appropriate amount

[0090] Makes 1000 pieces

[0091] (2) The preparation method is the same as in Example 1.

Embodiment 3

[0093] (1) Prescription

[0094] Sitagliptin Phosphate 128.5g

[0095] Microcrystalline Cellulose 96.5g

[0096] Calcium hydrogen phosphate 64.5g

[0097] Croscarmellose Sodium 6.5g

[0098] Magnesium Stearate 12.5g

[0099] Coating agent 12.5g

[0100] 50% ethanol aqueous solution appropriate amount

[0101] Makes 1000 pieces

[0102] (2) The preparation method is the same as in Example 1.

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Abstract

Belonging to the technical field of pharmaceutical preparations, the invention in particular relates to a pharmaceutical composition of sitagliptin and a preparation method thereof. The pharmaceutical composition of sitagliptin provided by the invention employs the process of mixing sitagliptin and specific auxiliary materials in certain proportion, and obviously overcomes the defects of poor stability, complex production process and incapability of mass production in the prior art. At the same time, the invention accidentally finds that the tablet prepared by the method involved in the invention has better dissolution rate.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a sitagliptin pharmaceutical composition and a preparation method thereof. Background technique [0002] Sitagliptin was developed and marketed by Merck. The drug was launched in the United States in October 2006. As of April 2008, the drug has been listed in several European countries. In October 2007, the drug was approved by the US FDA for combination therapy with metformin. [0003] Sitagliptin Phosphate Tablets is the first DPP-4 inhibitor approved for the treatment of type 2 diabetes. It can inhibit the apoptosis of β cells, promote the regeneration of β cells, increase the number of β cells in patients with type 2 diabetes, and significantly reduce the blood sugar of patients. And it still has a significant hypoglycemic effect on patients who have failed sulfa drugs. Sitagliptin Phosphate Tablets mainly achieve blood sugar control in patie...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/28A61K45/06A61K31/4985A61K47/38A61K47/04A61P3/10
Inventor 严洁
Owner TIANJIN HANRUI PHARMA
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