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Solid dispersion, preparation, preparation method and application thereof

A technology of solid dispersion and carrier, which is applied in the direction of non-active ingredient medical preparations, medical preparations containing active ingredients, pill delivery, etc. It can solve the problems of low solubility and difficult preparations, and achieve low impurity content and dissolution rate Good, the effect of improving stability

Pending Publication Date: 2022-05-27
ASCENTAGE PHARMA SUZHOU CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The technical problem to be solved by the present invention is to overcome the defects of low solubility and difficult preparation of existing Bcl-2 inhibitors, and provide a solid dispersion, preparation, preparation method and application thereof

Method used

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  • Solid dispersion, preparation, preparation method and application thereof
  • Solid dispersion, preparation, preparation method and application thereof
  • Solid dispersion, preparation, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0122] Example 1: Preparation of compounds of formula (I)

[0123] The compound of formula (I) was prepared according to WO2018 / 027097A1, then the compound of formula (I) was placed in a bottle, an appropriate amount of 1,4-dioxane was added, and it was allowed to stand at room temperature for 2 days. The obtained crystal form was centrifuged and dried at room temperature. , to obtain the crystalline form of compound (I).

Embodiment 2

[0124] Example 2: Preparation of compounds of formula (I)

[0125] The compound of formula (I) was prepared according to WO2018 / 027097A1, and then the compound of formula (I) was placed in a bottle, an appropriate amount of ethanol was added, stirred at room temperature for 5 days, and centrifuged. , and dried at room temperature to obtain acetone solvate crystalline form.

Embodiment 3

[0126] Example 3: Preparation of compound of formula (I)

[0127] The compound of formula (I) was prepared according to WO2018 / 027097A1, then the compound of formula (I) was placed in a bottle, an appropriate amount of acetonitrile solvent was added, and stirred at room temperature for 5 days. The obtained crystal form was centrifuged and dried at room temperature to obtain acetonitrile solvate crystals form.

[0128] Amorphous or other crystalline forms of the compounds of formula (I) can also be used to prepare solid dispersions. Of course, it is also possible to prepare solid dispersions using salts of compounds of formula (I).

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Abstract

The invention discloses a solid dispersion, a preparation, a preparation method and application thereof. The solid dispersion comprises a carrier and an active component, wherein the active component is a compound shown as a formula (I) and / or a pharmaceutically acceptable salt thereof; the carrier is a homopolymer and a copolymer of N-vinyl lactam and / or a pH dependent cellulose derivative. The preparation comprises the solid dispersion, a filling agent and a disintegrating agent. The solid dispersion disclosed by the invention has good dissolution rate, the solubility of effective components is remarkably improved, the bioavailability of the Bcl-2 inhibitor can be effectively improved, the solid dispersion has good dissolution rate and stability, and the medication safety can be improved.

Description

technical field [0001] The present invention relates to a solid dispersion, a preparation, its preparation method and its application. Background technique [0002] Compounds of formula (I) 4-{4-{[6-(4-chloro-phenyl)-spiro[3,5]nonan-6-en-7-yl]methyl}-piperazine -1-yl}-N-{{3-nitro-4-[((2S)-[1,4]dioxan-2-ylmethyl)-amino]phenyl}sulfonyl}-2 -(1H-Pyrrolo[2,3-b]pyridin-5-yloxy)-benzamide is an inhibitor of Bcl-2, the first discovered member of the Bcl-2 family of regulatory proteins , which regulates cell death (apoptosis) by inducing (pro-apoptotic) or inhibiting (anti-apoptotic) apoptosis. [0003] [0004] The compound is usually in crystalline form, with very low solubility, hardly soluble in aqueous media and most organic solvents such as methanol, ethanol, isopropanol and acetone, in order to improve the solubility and dissolution of the drug in gastrointestinal solutions to improve oral bioavailability Therefore, there is an urgent need to develop a formulation contai...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/635A61K47/32A61K47/38A61K9/20A61K9/36A61P35/00A61P35/02
CPCA61K31/635A61K9/146A61K47/32A61K47/38A61K9/2054A61K9/2866A61P35/02A61P35/00A61K9/0019A61K47/20A61K47/10A61K9/1652A61K9/2027A61K9/284A61K47/02A61K47/26
Inventor 林艳琼徐华良徐峰吴琛郭洪涛贺晓玲
Owner ASCENTAGE PHARMA SUZHOU CO LTD
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