Olaparib release related pharmaceutical composition

A composition and measuring bottle technology, applied in the pharmaceutical field, can solve problems such as slow dissolution, high impurity levels, and heavy tablets

Active Publication Date: 2021-03-05
BEIJING KANG LISHENG PHARMA TECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, at present, the dosage of olaparib tablets is still relatively large, and the recommended dose is 300mg (two 150mg tablets), twice a day, which is equivalent to a total daily dose of 600mg. Poor sex
[0006] The purpo

Method used

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  • Olaparib release related pharmaceutical composition
  • Olaparib release related pharmaceutical composition
  • Olaparib release related pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0073] Get raw material according to prescription table, preparation method comprises the steps:

[0074] (1) For olaparib, add polyethylene glycol 6000, add water to dissolve, heat at 80°C, homogenize to obtain a olaparib suspension, spray dry, and make a dry olaparib solid dispersion;

[0075] (2) Gradually add sodium lauryl sulfate, mannitol, crospovidone, talc powder, and micropowder silica gel, sieve and mix repeatedly, and directly compress into tablets to obtain olaparib tablets.

[0076] test results:

[0077] Compressibility: good

[0078] Friability: in compliance with regulations

[0079] Appearance: smooth and beautiful

[0080] 45min average dissolution rate: 92.3%

[0081] Related substance results: OP-K, OP-B, OP-01 were not detected.

Embodiment 2

[0083] Get raw material according to prescription table, preparation method comprises the steps:

[0084] (1) Take olaparib and polyethylene glycol 6000, add water to dissolve, heat at 80°C, homogenize to obtain a olaparib suspension, spray dry, and make a dry olaparib solid dispersion;

[0085] (2) Gradually add sodium lauryl sulfate, mannitol, crospovidone, mannitol, and micropowdered silica gel, sieve and mix repeatedly, and directly compress into tablets to obtain olaparib tablets.

[0086] Related substance and stripping curve determination method are the same as embodiment 1

[0087] test results:

[0088] Compressibility: good

[0089] Friability: in compliance with regulations

[0090] Appearance: smooth and beautiful

[0091] 45min average dissolution rate: 71.5%

[0092] Related substance results: OP-K, OP-B, OP-01 were not detected.

Embodiment 3

[0094] Get raw material according to prescription table, preparation method comprises the steps:

[0095] (1) Take olaparib, add polyethylene glycol 6000, stir to mix evenly, heat at 80°C, homogenize to obtain olaparib suspension, spray dry to make dry olaparib solid Dispersions;

[0096] (2) Gradually add sodium lauryl sulfate, mannitol, crospovidone, mannitol, micronized silica gel, talcum powder, sieve and mix repeatedly, and directly compress into tablets to obtain olaparib tablets.

[0097] Related substance and stripping curve determination method are the same as embodiment 1

[0098] test results:

[0099] Compressibility: good

[0100] Friability: in compliance with regulations

[0101] Appearance: smooth and beautiful

[0102] 45min average dissolution rate: 79.3%

[0103] Related substance results: OP-K, OP-B, OP-01 were not detected.

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PUM

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Abstract

The invention relates to pharmaceutical compositions, in particular to an olaparib release related pharmaceutical composition. The invention discloses an olaparib composition containing impurities with relatively low levels and having relatively high release level, and a method for maintaining the stability of such pharmaceutical compositions.

Description

technical field [0001] The invention belongs to the field of medicines, in particular to a pharmaceutical composition related to the release of olaparib. Background technique [0002] Olaparib is a first-in-class, oral poly ADP ribose polymerase (PARP) inhibitor that exploits defects in the tumor DNA damage repair (DDR) pathway to preferentially kill cancer cells, a mode of action that confers olaparib Potential to treat a wide range of tumor types with defects in DNA damage repair, with the following structural formula: [0003] [0004] Olapali is the first PARP inhibitor to be marketed in the world, and was first approved by the US FDA in December 2014. AstraZeneca and Merck reached a global strategic cooperation in oncology in July 2017 to jointly develop and commercialize olaparib and another MEK inhibitor, selumetinib, to treat various types of tumors. In the field of PARP inhibitors, olaparib has the most extensive and advanced clinical trial development program....

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/502A61K47/32A61K47/40A61K47/26A61K47/04A61K47/10A61P35/00G01N30/02G01N30/06B01J20/281G01N30/34G01N30/36G01N30/74G01N30/86
CPCG01N30/48A61K9/205A61K9/2027A61K9/2018A61K9/2031A61K9/2009A61K31/502A61P35/00G01N30/02G01N30/06G01N30/34G01N30/36G01N30/74G01N30/8679
Inventor 程刚
Owner BEIJING KANG LISHENG PHARMA TECH DEV
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