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Alvatrepap maleate tablet and preparation method thereof

The invention relates to a technology for palatine tablets and maleic acid, which is applied in the field of avatrombopag maleate tablets and their preparation, which can solve problems such as poor in vitro dissolution of avatrombopag maleate and achieve process tolerance. Good, the curative effect is confirmed, and the effect of ensuring the uniformity of mixing

Pending Publication Date: 2020-12-04
REYOUNG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The object of the present invention is to provide a kind of alvatrombopag maleate tablet, and this tablet is quick-release film-coated tablet, has solved the problem of poor dissolution of avaltrombopag maleate in vitro, and has improved its in vivo The bioavailability of its in vitro dissolution curve in the medium of pH 1.0~6.8 is similar to that of the reference preparation; the present invention also provides its preparation method

Method used

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  • Alvatrepap maleate tablet and preparation method thereof
  • Alvatrepap maleate tablet and preparation method thereof
  • Alvatrepap maleate tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] A kind of alvatrombopag maleate tablet, the tablet specification is 20mg, consists of the following components:

[0039]

[0040] Appropriate amount of purified water.

[0041] Preparation:

[0042] (1) Mix 20g alvatrombopag maleate, 95g lactose monohydrate, 0.4g colloidal silicon dioxide and 3g crospovidone, and pulverize through a 16-mesh sieve;

[0043] (2) The physical mixture obtained in step (1) is mixed uniformly with 0.5g magnesium stearate, and dry granulation is carried out;

[0044] (3) Pass the granules obtained in step (2) through a 24-mesh sieve for granulation, add 5g microcrystalline cellulose, 3g crospovidone, and 0.5g magnesium stearate and mix uniformly;

[0045] (4) Add the material obtained in step (3) into a tablet press to compress the tablet, and coat it with a coating solution until the weight gain is 3%, to obtain alvatrombopag maleate tablet.

Embodiment 2

[0047] A kind of alvatrombopag maleate tablet, the tablet specification is 20mg, consists of the following components:

[0048]

[0049] Appropriate amount of purified water.

[0050] Preparation:

[0051] (1) Mix 20g avatrombopag maleate, 110g lactose monohydrate, 5g colloidal silicon dioxide and 2g croscarmellose sodium, and pulverize through a 16-mesh sieve;

[0052] (2) The physical mixture obtained in step (1) is mixed uniformly with 0.2g magnesium stearate, and dry granulation is carried out;

[0053] (3) Pass the granules obtained in step (2) through a 24-mesh sieve for granulation, add 16g of microcrystalline cellulose, 2g of croscarmellose sodium, and 0.2g of magnesium stearate and mix uniformly;

[0054] (4) Add the material obtained in step (3) into a tablet press to compress the tablet, and coat it with a coating solution until the weight gain is 5%, to obtain alvatrombopag maleate tablet.

Embodiment 3

[0056] A kind of alvatrombopag maleate tablet, the tablet specification is 20mg, consists of the following components:

[0057]

[0058] Appropriate amount of purified water.

[0059] Preparation:

[0060] (1) Mix 20g avatrombopag maleate, 110g lactose monohydrate, 1.45g silicon dioxide and 9g croscarmellose sodium, and pulverize through a 16-mesh sieve;

[0061] (2) The physical mixture obtained in step (1) is mixed uniformly with 2.5g sodium stearate fumarate, and dry granulated;

[0062] (3) Pass the granules obtained in step (2) through a 24-mesh sieve for granulation, add 16g of microcrystalline cellulose, 3g of croscarmellose sodium, and 2.5g of sodium fumarate stearate and mix uniformly;

[0063] (4) Add the material obtained in step (3) into a tablet press to compress the tablet, and coat it with a coating solution until the weight gain is 5%, to obtain alvatrombopag maleate tablet.

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Abstract

The invention relates to the technical field of pharmaceutical preparations, and particularly relates to an avatrepap maleate tablet and a preparation method thereof. The avatrepap maleate tablet comprises a medicine tablet core and a coating layer, wherein the medicine tablet core is prepared from the following components in parts by weight: 1 part of avatrepap maleate, 5-9 parts of a filling agent, 0.2-0.6 part of a disintegrating agent, 0.02-0.25 part of a flow aid and 0.02-0.25 part of a lubricating agent; and the filling agent, the disintegrating agent and the lubricating agent are addedinternally and externally. The avatrepap maleate tablet is a quick-release film-coated tablet, the problem of poor in-vitro dissolution of avatrepap maleate is solved, the in-vivo bioavailability of avatrepap maleate is improved, and the detection result of the in-vitro dissolution curve of avatrepap maleate in a medium with pH being 1.0-6.8 is similar to that of a reference preparation. The invention further provides the preparation method of avatrepap maleate tablet.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to an alvatrombopag maleate tablet and a preparation method thereof. Background technique [0002] Alvatrombopag maleate is a drug developed by AkaRxInc mainly for adult patients with chronic liver disease-associated thrombocytopenia undergoing elective diagnostic procedures or surgery. It was approved for marketing by the US FDA on May 21, 2018, and was approved for marketing by the European Union on June 20, 2019. It was launched in China on April 14, 2020, under the product name "Su Kexin". [0003] Alvatrombopag maleate molecular formula is C 29 h 34 C l2 N 6 o 3 S 2 ·C 4 h 4 o 4 , the structural formula is as follows: [0004] [0005] Alvatrombopag maleate is an oral, small-molecule thrombopoietin (TPO) receptor (c-Mpl) agonist, which can simulate the biological effects of TPO, stimulate platelet production, and increase platelet count, which i...

Claims

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Application Information

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IPC IPC(8): A61K9/36A61K47/26A61K47/38A61K47/32A61K47/36A61K31/496A61P7/04
CPCA61K9/2866A61K9/2018A61K9/2027A61K9/2059A61K9/2054A61K31/496A61P7/04
Inventor 苗得足胡清文李荣丽宋洋吕帅王向华
Owner REYOUNG PHARMA
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