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Avatrombopag maleate preparation composition as well as tablet or capsule prepared from composition and preparation method

A technology of alvatrombopag and composition, which is applied in capsule delivery, drug combination, pill delivery, etc. It can solve the problems of decreased dissolution rate, poor water solubility of active ingredients, decreased, accelerated investigation, etc., and achieves good uniformity and API Uniform particle size distribution and high dissolution stability

Pending Publication Date: 2022-02-08
南京唯创远医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the poor water solubility of the active ingredients, the raw materials are usually micronized, but due to electrostatic aggregation, after the micronized raw materials are made into preparations, the dissolution rate will gradually decrease during the long-term stability storage process, and the accelerated investigation will be 3 to 6 months. Dissolution decreased by 10-15%

Method used

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  • Avatrombopag maleate preparation composition as well as tablet or capsule prepared from composition and preparation method
  • Avatrombopag maleate preparation composition as well as tablet or capsule prepared from composition and preparation method
  • Avatrombopag maleate preparation composition as well as tablet or capsule prepared from composition and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] A stable alvatrombopag maleate tablet with a specification of 20mg / tablet per 1000 tablets prescription:

[0068] Name of raw material Prescription amount Alvatrombopag Maleate (calculated as Alvatrombopag) 20g lactose monohydrate 100g microcrystalline cellulose 60g Crospovidone 10g Hypromellose 4g Magnesium stearate 2g Micropowder silica gel 4g

[0069] Preparation Process:

[0070] a. Premix 20g of alvatrombopag maleate with 80g of lactose and 20g of microcrystalline cellulose, and grind together in a ball mill for 200 minutes;

[0071] b. Add 20g lactose, 40g microcrystalline cellulose, 4g hypromellose, 10g crospovidone, and 1g magnesium stearate to the co-grinding mixture for 10 minutes, then dry granulate, Number 24;

[0072] c. Add 1g of magnesium stearate and 4g of micropowder silica gel to the prepared granules, and mix in a three-position motion mixer for 10 minutes;

[0073] d. Compress the mixed mat...

Embodiment 2

[0075] A kind of stable alvatrombopag maleate capsules, the prescription composition in every 1000 tablets of 20mg / capsules is as follows:

[0076] Name of raw material Prescription amount Alvatrombopag Maleate (calculated as Alvatrombopag) 20g lactose monohydrate 80g microcrystalline cellulose 80g Crospovidone 10g Hypromellose 4g Magnesium stearate 2g Micropowder silica gel 4g

[0077] a. Premix 20g of alvatrombopag maleate with 80g of lactose and 20g of microcrystalline cellulose, and grind together for 100 minutes in a ball mill;

[0078] b. Then add 60g of microcrystalline cellulose, 4g of hypromellose, 10g of crospovidone, and 1g of magnesium stearate to the co-grind, mix for 10 minutes, then dry granulate, the whole grain size is 24 mesh ;

[0079] c. Add 1g of magnesium stearate and 4g of micropowder silica gel to the prepared granules, and mix in a three-position motion mixer for 10 minutes;

[0080] d. Fill t...

Embodiment 3

[0082] A kind of stable alvatrombopag maleate tablet, the prescription composition in every 1000 tablets of 20mg / tablet is as follows:

[0083]

[0084]

[0085] a. Premix 20g of alvatrombopag maleate with 80g of lactose and 20g of microcrystalline cellulose, and grind together in a ball mill for 200 minutes;

[0086] b. Add 10g lactose, 50g microcrystalline cellulose, 4g hypromellose, 10g crospovidone, and 1g magnesium stearate to the co-grinding mixture for 10 minutes, then dry granulate, granulate Number 24;

[0087] c. Add 1g of magnesium stearate and 4g of micropowder silica gel to the prepared granules, and mix in a three-position motion mixer for 10 minutes;

[0088] d. Compress the mixed materials into tablets at a rate of 200mg / tablet, and control the tablet hardness to 100-160N.

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Abstract

The invention discloses an avatrombopag maleate preparation composition. The composition comprises an active component avatrombopag maleate and a filler, the filler comprises lactose and microcrystalline cellulose, the mass ratio of the active component to the filler is 1:1 to 1:5, and the active component and the filler are co-ground to obtain the preparation composition. The composition prepared by the invention can be used for preparing the avatrombopag maleate tablets or capsules, the dissolution rate in a preparation batch is uniform, the shelf life and the dissolution rate are stable, and an effective and feasible production process can be provided for domestic popularization of the avatrombopag maleate preparation. The invention also discloses a tablet or a capsule prepared from the preparation composition. The invention also discloses a preparation method of a tablet or a capsule prepared from the avatrombopag maleate preparation composition.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a therapeutic drug for chronic liver disease (CLD)-associated thrombocytopenia, in particular to a stable preparation composition of alvatrombopag maleate and the prepared tablets or capsules thereof and Preparation. The invention provides an alvatrombopag maleate preparation composition with simple process, safe and effective, and stable quality. Background technique [0002] Alvatrombopag maleate is the second-generation, once-daily oral first thrombopoietin (TPO) receptor agonist, developed by AkaRx, approved by the FDA on May 21, 2018, for the treatment of Low platelet count (thrombocytopenia CIT) in adult patients with chronic liver disease (CLD) who are planning to undergo medical or dental surgery, is the first drug for this use, and in 2019, it was launched in the United States for chronic immune thrombocytopenia. On April 16, 2020, Alvatrobopag maleate was approved by t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/496A61K47/38A61K47/26A61K9/20A61K9/48A61P1/16A61P7/00A61P7/04
CPCA61K31/496A61K47/38A61K47/26A61K9/2018A61K9/2054A61K9/4866A61K9/4858A61P1/16A61P7/00A61P7/04
Inventor 朱磊贾元超陈林朱思思王宁张学智
Owner 南京唯创远医药科技有限公司
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