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A kind of preparation method of neratinib or its pharmaceutically acceptable salt pharmaceutical composition

A technology of neratinib and solvate, which is applied in the field of preparation of neratinib or its pharmaceutically acceptable salt pharmaceutical composition, can solve the problem of inability to guarantee the stability and good dissolution properties of the final preparation, instability and easy degradation Chemical properties and other issues to achieve good dissolution properties

Active Publication Date: 2020-12-04
JIANGSU HENGRUI MEDICINE CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is no chemical property for Neratinib itself that is unstable and easy to degrade
However, merely improving cohesiveness during granulation does not guarantee good stability and good dissolution properties of the final formulation

Method used

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  • A kind of preparation method of neratinib or its pharmaceutically acceptable salt pharmaceutical composition
  • A kind of preparation method of neratinib or its pharmaceutically acceptable salt pharmaceutical composition
  • A kind of preparation method of neratinib or its pharmaceutically acceptable salt pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Neratinib maleate, mannitol, microcrystalline cellulose, crospovidone, and silicon dioxide will be granulated in a fluidized bed according to the ratio in Table 1, with 5% polyvinylpyrrolidone as the binding agent. After the granulation is completed, stop spraying the binder and dry the granules. Add sodium stearyl fumarate according to the ratio in Table 1. Mixing is performed using a rotary blender. The obtained blended granules are filled into capsules to prepare capsules.

[0047] Table 1: Prescription of Neratinib Maleate Capsules

[0048] Element Unit dose (mg) Proportion(%) Neratinib maleate (anhydrous) 290 48.33 Mannitol 202 33.67 microcrystalline cellulose 36 6.00 Crospovidone 18 3.00 colloidal silica 12 2.00 Polyvinylpyrrolidone 30 5.00 Sodium stearyl fumarate 12 2.00 total 600 100

[0049] According to the above prescription, the DPL-II fluidized bed (manufactured by Chongqing Jinggo...

Embodiment 2

[0061] Dissolution test results

[0062] Neratinib maleate capsules of prescription B1 and prescription A1 of Example 1 were investigated for dissolution rate. In Chinese Pharmacopoeia Dissolution Determination Method 2 Slurry Method, 900mL of hydrochloric acid solution with pH 1.0 was used as the dissolution medium to investigate the dissolution of capsules. The temperature of the dissolution medium was 37±0.5°C, and the paddle speed was 50rpm. Samples were collected at 5, 10, 15, 30, and 45 min, and measured at 266 nm by an ultraviolet spectrometer.

[0063] The dissolution measurement result and the dissolution curve of the neratinib maleate capsule prepared by the method of the present invention are shown in figure 1 middle. The ordinate shows the dissolution rate of neratinib, and the abscissa shows the time (min). The results showed that the neratinib capsules (B1) prepared by this method dissolved rapidly, and more than 80% could be dissolved in 15 minutes, which was...

Embodiment 3

[0065] Neratinib, mannitol, microcrystalline cellulose, crospovidone, and silicon dioxide were granulated in a fluidized bed according to the ratio in Table 1, and sprayed into The binder is granulated, and after the granulation is completed, the spraying of the binder is stopped, and the granules are dried. Add sodium stearyl fumarate according to the ratio in Table 1. Mixing is performed using a rotary blender. The obtained blended granules are filled into capsules to prepare capsules.

[0066] Table 5: Prescription of Neratinib Maleate Tablets

[0067] Element Unit dose (mg) Proportion(%) Neratinib maleate (anhydrous) 290 36.25 Mannitol 335 41.88 microcrystalline cellulose 60 7.50 Crospovidone 25 3.13 colloidal silica 16 2.00 Polyvinylpyrrolidone 42 5.25 Crospovidone 16 2.00 Sodium stearyl fumarate 16 2.00 total 800 100

[0068] According to the above prescription, the DPL-II fluidized bed (...

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Abstract

The invention relates to a preparation method of a medicinal composition of neratinib or a medicinal salt of the neratinib. A medicinal preparation with good stability can be prepared through keeping the maximum water content of a granule in the granulation period to be 10% or less or / and controlling the water content of a final granule or the medicinal composition to be 2% or less in the preparation process of the neratinib granule, and the medicinal preparation has good dissolving property.

Description

technical field [0001] The preparation method of the pharmaceutical composition containing neratinib and other pharmaceutical active ingredients described in the present invention, by controlling the maximum water content of the granules in the granulation preparation process to be below 10%, or / and controlling the water content of the final granules or compositions 2 % or less, a pharmaceutical preparation with good stability can be obtained, and the pharmaceutical composition prepared by the method of the present invention has better dissolution properties. Background technique [0002] (E)-N-(4-(3-Chloro-4-(pyridin-2-ylmethoxy)phenylamino-3-cyano-7-ethoxyquinolin-6-yl)-4- (Dimethylamino)but-2-enamide, also known as Neratinib, has the following specific structure and is a specific protein kinase inhibitor. [0003] [0004] Studies have shown that there are high or abnormal expressions of EGFR in many solid tumors. EGFR is related to tumor cell proliferation, angiogen...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K9/28A61K31/4709A61K47/26A61K47/32A61K47/12A61K47/38A61P35/00
CPCA61K9/1617A61K9/1623A61K9/1635A61K9/1652A61K9/2866A61K31/4709
Inventor 郭辰宁潘凯刘凯刘通
Owner JIANGSU HENGRUI MEDICINE CO LTD
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