Preparation method of empagliflozin microcrystalline cellulose composition

A technology of microcrystalline cellulose and empagliflozin, applied in the field of medicine, can solve problems such as complicated production, increased contact area between production workers and drugs, explosion, etc., and achieve cost saving and production time, good in vitro dissolution behavior, and preparation method simple effect

Active Publication Date: 2015-05-06
ZHEJIANG HUAHAI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

To achieve this particle size, the drug needs to be micronized, which requires special mechanical pulverization or jet pulverization equipment, which is cumbersome in production and reduces production efficiency.
In addition, during the micronization process of the drug, the drug is easy to float in the air, which greatly increases the contact area between the production workers and the drug, so special protective equipment is required, otherwise it is not good for the health of the workers, and when the dust in the environment When the amount increases to a certain level, it is easy to cause an explosion, and there is also a certain safety hazard for production.

Method used

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  • Preparation method of empagliflozin microcrystalline cellulose composition
  • Preparation method of empagliflozin microcrystalline cellulose composition
  • Preparation method of empagliflozin microcrystalline cellulose composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] The preparation of Empagliflozin microcrystalline cellulose composition:

[0035] Weigh 10g of empagliflozin and 20g of microcrystalline cellulose and mix them into a jacketed granulator for granulation. The temperature is set at 160°C, stirred for 15 minutes, taken out and cooled, and passed through a 20-mesh sieve.

Embodiment 2

[0037] The preparation of Empagliflozin microcrystalline cellulose composition:

[0038] Weigh 10g of Empagliflozin and 50g of microcrystalline cellulose, mix them into a jacketed granulator for granulation, set the temperature at 200°C, stir for 5 minutes, take it out and cool it, and use a rotating granulator with an aperture of 1.0mm Machine can be granulated.

Embodiment 3

[0040] The preparation of Empagliflozin microcrystalline cellulose composition:

[0041] Weigh 10g of empagliflozin and 100g of microcrystalline cellulose and mix them into a jacketed granulator for granulation. The temperature is set at 170°C, stirred for 15 minutes, taken out and cooled, and passed through a 30-mesh sieve.

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Abstract

The invention provides a preparation method of an empagliflozin microcrystalline cellulose composition. The preparation method comprises the following steps: mixing empagliflozin and microcrystalline cellulose to obtain a mixture of empagliflozin and microcrystalline cellulose; heating the mixture to melt the empagliflozin, and stirring the mixture; and cooling to obtain an empagliflozin microcrystalline cellulose composition. The empagliflozin composition prepared by the method provided by the invention has stable and controllable quality and is quickly dissolved out.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a preparation method of an empagliflozin microcrystalline cellulose composition. Background technique [0002] Type II diabetes has become an increasingly popular disease, and its high-frequency complications (such as diabetic foot, blindness, renal failure, etc.) not only affect the quality of life of patients, but may also lead to shortened life span. [0003] Empagliflozin is an oral sodium-glucose cotransporter-2 (SGLT-2) inhibitor. SGLT-2 is the transporter mainly responsible for the reabsorption of glucose from the glomerular filtrate into the systemic circulation. By inhibiting SGLT-2, empagliflozin reduces the renal reabsorption of filtered glucose and lowers the renal threshold of glucose, Thereby increasing the excretion of urinary sugar. This product is used for Blood sugar control for adults with type 2 diabetes, jointly developed by Boehringer Ingelh...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/48A61K9/00A61K31/7048A61K47/38A61P3/10
Inventor 彭俊清余慧曹宇陈浩胡功允
Owner ZHEJIANG HUAHAI PHARMA CO LTD
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