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Empagliflozin tablet and preparation process thereof

A technology for empagliflozin tablets and empagliflozin, which is applied in the field of empagliflozin tablets and their preparation, can solve the problems of explosion risk, reduced production efficiency, easy agglomeration and agglomeration, and achieves increased drug stability, increased Absorption and bioavailability, the effect of improving drug dissolution

Active Publication Date: 2020-06-02
SHANGHAI HANSOH BIOMEDICAL +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Patent CN102387783A improves the dissolution rate of empagliflozin by controlling the particle size distribution of raw materials and drug particle size, but the preparation method is relatively cumbersome, and the loss in the process of raw material micronization is large, and it is easy to agglomerate and agglomerate after micronization, which virtually reduces production efficiency
[0006] Patent CN104623684A prepares mannitol and empagliflozin into a solid dispersion through solid dispersion technology to improve the dissolution rate. However, a large amount of mannitol is used in this patent, and mannitol is hygroscopic, which is not conducive to long-term storage of the preparation and affects the stability of the preparation.
[0007] In patent CN105456211A, empagliflozin is mixed with succinic acid and avocado oil, and then clathrates are prepared with hydroxypropyl-ß-cyclodextrin and methacrylic acid, and clathrates are prepared with other pharmaceutical excipients However, hydroxypropyl-ß-cyclodextrin will be converted into glucose in the body, and relevant data show that it has certain nephrotoxicity, so it is not suitable for diabetic patients to take for a long time. In addition, the excipient succinic acid in the prescription is a dangerous excipient. It is combustible in case of open flame and high heat, and its powder and air can form an explosive mixture. When used in large quantities, there will be a risk of explosion

Method used

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  • Empagliflozin tablet and preparation process thereof
  • Empagliflozin tablet and preparation process thereof
  • Empagliflozin tablet and preparation process thereof

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0087]

[0088] (1) Weigh the prescription amount of poloxamer 188 and mannitol, mix evenly, and heat to melt at 170°C;

[0089] (2) Add Empagliflozin under the condition of slow stirring at 200-350r / min, and stir vigorously at 10000-20000r / min until it melts;

[0090] (3) The completely melted mixture obtained in (2) was frozen at -20°C for 5 hours, vacuum-dried at 40°C for 5 hours, taken out, crushed, and passed through an 80-mesh sieve to obtain a solid composition;

[0091] (4) Mix the obtained solid composition with the prescribed amount of pregelatinized starch, croscarmellose sodium, colloidal silicon dioxide and magnesium stearate, and further make tablets.

[0092] Dissolution method: according to the "Chinese Pharmacopoeia" 2015 edition four dissolution and release test method (general rule 0931 second method)

[0093] Temperature: 37℃±0.5℃

[0094] Dissolution medium: 0.1mol / L hydrochloric acid solution

[0095] Medium volume: 900ml

[0096] Speed: 50 rpm

...

experiment example 2

[0103]

experiment example 3

[0114]

[0115] According to the preparation method, the superior prescription was prepared again, and the relevant physical properties were investigated.

[0116] Formability data

[0117]

[0118] Dissolution Data

[0119] Dissolution in 0.1mol / L hydrochloric acid: According to the dissolution and release test method of the fourth part of "Chinese Pharmacopoeia" 2015 edition (general rule 0931 second method)

[0120] Temperature: 37℃±0.5℃

[0121] Dissolution medium: 0.1mol / L hydrochloric acid solution

[0122] Medium volume: 900ml

[0123] Speed: 50 rpm

[0124] Sampling: Take the solution after 5 minutes, 10 minutes, 15 minutes, and 30 minutes, filter it with a 0.45 μm microporous membrane, and replenish the corresponding dissolution medium at the same temperature in the operating container in time.

[0125] Detection method: HPLC method.

[0126]

[0127] Dissolution in pH 6.8 phosphate buffer solution: according to the dissolution and release test method o...

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Abstract

The invention provides an empagliflozin tablet and a preparation process thereof. The empagliflozin tablet comprises empagliflozin, carrier materials and other pharmaceutically acceptable auxiliary materials, and is characterized in that the carrier materials jointly consist of poloxamer and mannitol. The empagliflozin tablet disclosed by the invention has the advantages that the operation of thepreparation process is simple; and the characteristics of high dissolution rate, good stability and the like are realized.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to empagliflozin tablets and a preparation process thereof. Background technique [0002] At present, diabetes has become one of the five leading causes of death in the world, and the number of diabetic patients in the world has reached 150 million. Among them, type II diabetes has become an increasingly popular disease, especially in Asia, where the number and number of patients are increasing. Its high frequency of complications (such as diabetic foot, blindness, renal failure, etc.) not only affects the quality of life of patients, but also It may lead to a shortened lifespan. Studies have shown that about 70% of patients with type II diabetes die of complications (such as coronary heart disease, stroke, etc.). [0003] Empagliflozin is an antidiabetic drug with a new mechanism. It is a sodium-glucose cotransporter (SGLT-2) inhibitor and is clinically used for the trea...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K47/10A61K47/26A61K31/351A61P3/10
CPCA61K9/2018A61K9/2031A61K31/351A61P3/10
Inventor 张晓瑜李倩赵娜嵇海澄
Owner SHANGHAI HANSOH BIOMEDICAL
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