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Dapagliflozin tablet and preparation method thereof

A technology for dapagliflozin tablets and tablets, applied in the field of dapagliflozin tablets and their preparation, can solve the problems of poor content uniformity and stability, difficult industrialized production, complicated process steps, and the like, and achieve improved Fluidity and content uniformity, good mixing uniformity and good content uniformity

Active Publication Date: 2022-02-11
ZHEJIANG HISOAR PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method adopts the process of two-step mixing, dry granulation, granulation, and tabletting, and the process steps are complicated and the cost is high.
In addition, Dapagliflozin Propylene Glycol Monohydrate will undergo desolvation and crystallization at 45°C, and the use of dry granulation has the risk of exothermic desolvation
[0009] Therefore, the pharmaceutical preparation of dapagliflozin propylene glycol monohydrate and the preparation method thereof provided by the prior art have poor dissolution, poor content uniformity and stability, complex process, high production cost, and are not easy to industrialized production. question

Method used

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  • Dapagliflozin tablet and preparation method thereof
  • Dapagliflozin tablet and preparation method thereof
  • Dapagliflozin tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] 1) Use the following raw materials to prepare Dapagliflozin tablets (using Dapagliflozin C 21 h 25 ClO 6 Calculated, theoretical tablet core weight 250mg, 1000 tablets / batch) the prescription composition is as follows:

[0043]

[0044] 2) the preparation method of tablet, comprises the steps:

[0045] (1) Take the Dapagliflozin Propylene Glycol Monohydrate and Excipient Compound of the prescription amount; At normal temperature, pass the lactose microcrystalline cellulose compound of Dapagliflozin Monohydrate and 1 / 2 through a 45 mesh sieve After sieving and mixing, add it and the remaining lactose microcrystalline cellulose compound, crospovidone, and silicon dioxide into a high-speed mixing granulator for premixing, set the stirring blade at a speed of 4r / min, and cut The rotating speed of the cutter is 10r / min, and the premixed material is obtained after premixing for 30min;

[0046] (2) Add the above-mentioned premixed material and magnesium stearate into a ...

Embodiment 2

[0057] 1) Use the following raw materials to prepare Dapagliflozin tablets (using Dapagliflozin C 21 h 25 ClO 6 Calculated, theoretical tablet core weight 250mg, 1000 tablets / batch) the prescription composition is as follows:

[0058]

[0059] 2) the preparation method of tablet, comprises the steps:

[0060] (1) Take the Dapagliflozin Propylene Glycol Monohydrate and Excipient Compound of the prescription amount; At normal temperature, the lactose microcrystalline cellulose compound of Dapagliflozin Monohydrate and 1 / 3 is passed through a 45 mesh sieve After sieving and mixing, add it and the remaining lactose microcrystalline cellulose compound, crospovidone, and silicon dioxide to a high-speed mixing granulator for premixing, set the speed of the stirring paddle at 8r / min, and cut The rotating speed of the cutter is 15r / min, and the premixed material is obtained after premixing for 20min;

[0061] (2) Add the above-mentioned premixed material and magnesium stearate i...

Embodiment 3

[0072] 1) Use the following raw materials to prepare Dapagliflozin tablets (using Dapagliflozin C 21 h 25 ClO 6 Calculated, theoretical tablet core weight 250mg, 1000 tablets / batch) the prescription composition is as follows:

[0073]

[0074] 2) the preparation method of tablet, comprises the steps:

[0075] (1) Take the above-mentioned amount of Dapagliflozin propylene glycol monohydrate and the auxiliary material compound; After the sieve is sieved and mixed, it is added to the high-speed mixing granulator with the remaining silicified microcrystalline cellulose compound and crospovidone for premixing, and the rotating speed of the stirring blade is set to 10r / min. The rotating speed is 20r / min, and the premixed material is obtained after premixing for 20min;

[0076] (2) Add the above-mentioned premixed material and magnesium stearate into a multidimensional mixer for total mixing, set the multidimensional mixer speed to 12r / min, and mix for 3 minutes; the material ...

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Abstract

The invention provides a dapagliflozin tablet and a preparation method thereof. The dapagliflozin tablet is composed of a tablet core and a coating, wherein the tablet core is composed of the following raw and auxiliary materials in percentage by weight: 2.5-9.8% of dapagliflozin propylene glycol monohydrate; 80.2%-95.2% of an auxiliary material compound; 1.0%-5.0% of a disintegrating agent; 0.5%-2% of a lubricant; 0%-3% of a flow aid; wherein the auxiliary material compound is selected from a lactose microcrystalline cellulose compound or a silicified microcrystalline cellulose compound. The preparation method of the dapagliflozin tablet, provided by the invention, adopts a direct powder compression method, and the dapagliflozin tablet is obtained by uniformly mixing the dapagliflozin propylene glycol monohydrate raw material medicine with a controlled particle size with the auxiliary materials and then directly tabletting and coating. The dapagliflozin tablet provided by the invention is excellent in comprehensive performance, simple in preparation method, low in production cost and easy for industrial production.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a dapagliflozin tablet and a preparation method thereof. Background technique [0002] Diabetes mellitus is a metabolic disease characterized by hyperglycemia due to defects in insulin secretion or insulin action. Diabetes is divided into 4 major types, namely type Ⅰ diabetes (insulin-dependent), type Ⅱ diabetes (non-insulin-dependent), other special types of diabetes and gestational diabetes. Among them, type II diabetes is the most common form of diabetes, which accounts for 90% of diabetes cases. Its high-frequency complications, such as diabetes and renal failure, not only affect the quality of life of patients, but may also lead to shortened life expectancy. [0003] Dapagliflozin is a new type of anti-diabetic drug jointly developed by Bristol-Myers Squibb and AstraZeneca. It was approved for marketing by the European Medicines Agency (EMA)...

Claims

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Application Information

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IPC IPC(8): A61K9/36A61K31/351A61K47/38A61P3/10
CPCA61K31/351A61K9/2054A61K9/2866A61K9/2095A61P3/10
Inventor 张芳芳郑珊珊谭伟赵富录王永长
Owner ZHEJIANG HISOAR PHARMA
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