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Solid dispersion prepared from amorphous neratinib or pharmaceutically acceptable salt thereof and medicinal auxiliary materials and preparation method thereof

A solid dispersion, neratinib technology, applied in organic chemical methods, medical preparations containing active ingredients, pharmaceutical formulations, etc., can solve problems such as affecting the bioavailability of drugs, and achieve improved bioavailability and good stability. Sexual, widely applicable effects

Inactive Publication Date: 2017-06-13
CHANGZHOU AINUOXINRUI PHARMA LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, the drug is a poorly soluble drug, and its extremely low water solubility seriously affects the bioavailability of the drug

Method used

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  • Solid dispersion prepared from amorphous neratinib or pharmaceutically acceptable salt thereof and medicinal auxiliary materials and preparation method thereof
  • Solid dispersion prepared from amorphous neratinib or pharmaceutically acceptable salt thereof and medicinal auxiliary materials and preparation method thereof
  • Solid dispersion prepared from amorphous neratinib or pharmaceutically acceptable salt thereof and medicinal auxiliary materials and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] Dissolve neratinib (50 mg) in n-propanol (600 microliters) and water (900 microliters), heat to 60°C and stir to dissolve. The above solution was rapidly cooled to -10°C, and a white solid was precipitated, filtered, and dried to obtain amorphous neratinib free base, and the X-ray powder diffraction pattern was as follows: figure 1 As shown, there is no characteristic peak of neratinib crystal form in the X-ray powder diffraction pattern.

Embodiment 2

[0057] Lenatinib maleate (50 mg) was dissolved in ethanol (600 microliters) and water (600 microliters), and stirred at 40°C to mix well. The above solution is slowly concentrated to dryness in a rotary evaporator to obtain a white solid, which gives amorphous neratinib maleate, and the X-ray powder diffraction pattern is as follows: figure 2 As shown, there is no characteristic peak of neratinib maleate crystal form in the X-ray powder diffraction pattern.

Embodiment 3

[0059] Add lenatinib maleate (5 g) and povidone K30 (10 g) into water (300 ml), heat to 60°C and stir to dissolve. The above solution was dried with JISL micro-spray dryer LSD-48, the inlet temperature was maintained at 60°C and the outlet temperature was 50°C, and the outlet material was collected to obtain a white solid, which was further vacuum-dried to obtain amorphous neratinib maleate and povidone Solid Dispersion of Ketone-K30. X-ray powder diffraction pattern as image 3 As shown, in the X-ray powder diffraction pattern of the solid dispersion, there is no characteristic peak of neratinib maleate crystal form after deducting the background peak of pharmaceutical excipients.

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Abstract

Amorphous neratinib is characterized in that no characteristic peak of neratinib exists in an X-ray powder diffraction spectrum. Amorphous neratinib maleate is characterized in that no characteristic peak of neratinib maleate exists in an X-ray powder diffraction spectrum. The invention further discloses a preparation method of an amorphous state of the amorphous neratinib or pharmaceutically acceptable salt thereof, as well as a solid dispersion prepared from the amorphous neratinib or the pharmaceutically acceptable salt thereof and medicinal auxiliary materials and a preparation method thereof, wherein the neratinib or the pharmaceutically acceptable salt thereof are amorphous. The solid dispersion prepared from the neratinib or the pharmaceutically acceptable salt thereof and the medicinal auxiliary materials is good in stability and dispersion, so that the dissolution of the neratinib or the salt thereof is improved and thus the improvement on the bioavailability of a medicinal preparation and medicine absorption of a body is more facilitated; under an accelerated test condition, the solid dispersion keeps good physical and chemical stability. The preparation method of the amorphous solid dispersion is easy to operate, low in cost, good in reproducibility and easy to implement, and is suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and specifically relates to an amorphous neratinib and an amorphous neratinib maleate, and also relates to an amorphous neratinib or a pharmaceutically acceptable salt thereof and a medicine The solid dispersion with auxiliary materials also relates to a pharmaceutical composition containing amorphous neratinib or a pharmaceutically acceptable salt thereof and pharmaceutical auxiliary materials and a preparation method thereof. Background technique [0002] Neratinib (Neratinib, also known as HKI-272), the chemical name is (2E)-N-[4-[[3-chloro-4-[(pyridin-2-yl)methoxy]phenyl]amino ]-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide is an irreversible epidermal growth factor receptor (EGFR ) inhibitors. Neratinib is a small-molecule tyrosine kinase inhibitor targeting HER2 and HER1 following lapatinib. It is an irreversible pan-ErbB receptor tyrosine kinase inhibitor that c...

Claims

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Application Information

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IPC IPC(8): C07D401/12A61K31/4709A61K9/14A61P35/00
CPCA61K9/146A61K31/4709C07B2200/13C07D401/12
Inventor 张席妮熊志刚周涛易果
Owner CHANGZHOU AINUOXINRUI PHARMA LTD
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