Bosutinib compound

A technology for bosutinib and a composition, which is applied to bosutinib monohydrate and its preparation, and the application field of medicine, can solve the problems of difficult to effectively improve product purity, difficult to achieve, poor quality reproducibility, etc.

Inactive Publication Date: 2015-03-25
TIANJIN HANKANG PHARMA BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the monohydrate crystal form obtained above has the following problems in the production process: (1) the yield is low, and it is difficult to realize in industrial product

Method used

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  • Bosutinib compound
  • Bosutinib compound
  • Bosutinib compound

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

Example 1

Add 250g Bosutinib, 1250ml DMF, 1250ml isopropanol to a 10L reactor equipped with stirring, thermometer and condenser, start stirring, heat to dissolve, and cool the filtrate to 5℃-15℃ naturally, and then keep it standing for heat preservation After 3 hours, crystals were precipitated, filtered, and dried indoors to obtain 245.5 grams of white crystals of bosutinib monohydrate, with a content of 99.95% and a single impurity less than 0.06%. Measured by Karl Fischer method, it contains 3.26% (weight percent) of water.

Using standard and conventional techniques, the compound of the present invention is combined with a pharmacologically acceptable solid or liquid carrier, and optionally combined with pharmacologically acceptable auxiliary agents and excipients to prepare particles or microspheres. The composition is used to prepare oral preparations and injections. Illustrating only by way of example does not mean that it limits the scope of the present invention in a...

Example Embodiment

Example 2

Tablets containing Bosutinib monohydrate

Prescription: Bosutinib monohydrate 100g, microcrystalline cellulose 10g, pregelatinized starch 15.4g, sodium starch glycolate 4.4g, lactose 150g, 20g PEG-4000, 4g magnesium stearate, 29 Gram povidone K30, croscarmellose sodium 30 grams, distilled water appropriate amount, made into 1000 tablets.

Process:

Preparation of tablet core: mix the main drug and auxiliary materials uniformly according to the determined prescription, granulate, ventilate and dry the granules below 40℃, sizing with 16 mesh sieve, add magnesium stearate and remaining starch, and press to obtain .

Isolation layer coating: add talc powder to 5% polyvinylpyrrolidone (PVP) absolute ethanol solution, stir evenly, and prepare a 20% suspension as the isolation layer coating liquid. Coating is carried out in a fluidized bed, and the process conditions are as follows: spray pressure 0.3MPa, liquid inlet speed 5mL / min, inlet temperature 37℃, outlet temperatur...

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Abstract

Belonging to the technical field of medicine, the invention in particular relates to a bosutinib monohydrate and a preparation method thereof. The bosutinib monohydrate obtained by the invention contains a crystal water, and has the advantages of: good stability, easy industrialized preparation process, good quality reproducibility, and well controlled product purity. The invention also relates to application of compositions using the hydrate in drugs treating chronic myeloid leukemia.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to bosutinib monohydrate and a preparation method thereof. The present invention also relates to the application of the hydrate composition in medicine for treating chronic myelogenous leukemia. Background technique [0002] Bosutinib is a potent protein kinase (Src-Abl) inhibitor, which can not only inhibit the autophosphorylation of Src protein in a variety of human tumor cells, but also inhibit the phosphorylation of Src and Abl substrates process. The drug was developed by Wyeth Pharmaceuticals, a subsidiary of Pfizer in the United States, and was first launched in the United States in September 2012. It is approved for chronic phase, accelerated phase or blast phase that is resistant or intolerant to previous treatment The treatment of adult patients with Philadelphia chromosome-positive chronic myelogenous leukemia (CML), the product name is Bosulif, and the spe...

Claims

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Application Information

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IPC IPC(8): C07D215/54A61K31/496A61P35/02
CPCC07D215/54
Inventor 严洁李轩
Owner TIANJIN HANKANG PHARMA BIOTECH
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