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Pharmaceutical preparation composition containing WEE1 inhibitor and preparation method thereof

A technology for pharmaceutical preparations and compositions is applied in the field of pharmaceutical compositions containing WEE1 inhibitors as active ingredients and their preparation fields, and can solve the problems of poor water solubility and low bioavailability of compounds.

Pending Publication Date: 2022-08-02
SHOUYAO HLDG BEIJING CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Solve the problem of poor water solubility and low bioavailability of compounds of WEE1 inhibitor formula (I)

Method used

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  • Pharmaceutical preparation composition containing WEE1 inhibitor and preparation method thereof
  • Pharmaceutical preparation composition containing WEE1 inhibitor and preparation method thereof
  • Pharmaceutical preparation composition containing WEE1 inhibitor and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1～2

[0027] The pharmaceutical composition of the present invention, the preferred formula composition is as follows (%, w / w):

[0028]

[0029]

[0030] Particle size distribution of compounds of formula (I):

[0031] Particle size distribution Example 1 Example 2 D50 4.047μm 8.886μm D90 10.428μm 51.124μm

[0032] The preparation process is as follows:

[0033] 1) mix the compound of formula (I), microcrystalline cellulose PH102, lactose F100, sodium starch glycolate and magnesium stearate (internally added);

[0034] 2) Take the mixed material and add it to the hopper of the dry granulator for granulation. The feeding frequency is 20Hz, the tableting frequency is 10Hz, the granulation frequency is 10Hz, and the oil pressure is 40-50kg / cm 2 , the aperture of the secondary screen mesh is 1.0mm;

[0035] 3) Mix the prepared granules with the external materials evenly, press the tablet with a rotary tablet machine, and perform film coating. ...

Embodiment 3～4

[0037] The pharmaceutical composition of the present invention, the preferred formula composition is as follows (%, w / w):

[0038] Raw materials Proportion Compounds of formula (I) 40.0 Microcrystalline Cellulose PH101 44.0 Croscarmellose sodium 3.0 Povidone K30 5.0 Poloxamer 188 5.0 Croscarmellose sodium (extra) 2.0 Magnesium stearate (extra) 1.0 sum 100.0

[0039] Particle size distribution of compounds of formula (I):

[0040] Particle size distribution Example 3 Example 4 D50 5.785μm 10.697μm D90 25.863μm 101.713μm

[0041] The preparation process is as follows:

[0042] 1) adding poloxamer 188 and povidone K30 to a certain amount of purified water, stirring and dissolving to obtain a binder solution with a concentration of 20% of povidone K30;

[0043] 2) adding the compound of formula (I), microcrystalline cellulose PH101 and croscarmellose sodium into the wet granulator h...

experiment example 1

[0048] Determination of the Dissolution Profile of the Invention

[0049] The samples of the above-mentioned examples were taken, and the dissolution curve was determined by the second method of the Dissolution and Release Determination Method 0931 of the Fourth General Principles of the Chinese Pharmacopoeia 2020 Edition. The dissolution method is: paddle method, 0.1N HCl solution and pH4.5 phosphate buffer, 900ml, 75rpm, 37±0.5°C, sampling time 10, 15, 30 and 60min. The dissolution profile is attached Figures 5 to 6 . It can be seen that in the two dissolution media, the dissolution of Example 1 and Example 3 prepared by micronized raw materials are significantly faster than those of Example 2 and Example 4.

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Abstract

The invention relates to a pharmaceutical preparation composition containing a WEE1 inhibitor and a preparation method of the pharmaceutical preparation composition. The WEE1 inhibitor is shown as a compound in a formula (I).

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a pharmaceutical composition containing a WEE1 inhibitor as an active ingredient and a preparation method thereof. Background technique [0002] WEE1 kinase is a cell cycle regulatory protein that regulates the phosphorylation state of cyclin-dependent kinase 1 (CDK1), thereby regulating the activity of the complex between CDK1 and cyclin B (cyclin B). It regulates the cell cycle and plays an important role in the regulation of DNA damage checkpoints. WEE1 is a key gene in G2 / M phase arrest and plays an important monitoring role. Overexpression, inhibition or downregulation of WEE1 kinase in some cancers can trigger mitotic catastrophe. Therefore, WEE1 kinase inhibitors may have a key role in anticancer therapy. effect. [0003] WEE1 is overexpressed in many malignancies, such as liver cancer, breast cancer, glioblastoma, melanoma, and adult and pediatric brain tumors. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/519A61K9/20A61K9/48A61K9/16A61K47/20A61K47/10A61K47/38A61K47/32A61P35/00
CPCA61K31/519A61K9/2013A61K9/2031A61K9/2054A61K9/2027A61K9/4858A61K9/4866A61K9/1617A61K9/1641A61K9/1652A61K9/1635A61P35/00
Inventor 孙德广刘玲黄甜甜周广义莫芮马秋平杨利民佟鹤芳张茜宁张丹
Owner SHOUYAO HLDG BEIJING CO LTD
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