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Pharmaceutical composition of aminopyrimidine compound and preparation method thereof

A composition and drug technology, which are applied in the field of pharmaceutical compositions of aminopyrimidine compounds and their preparation, can solve the problem that tyrosine kinase inhibitors cannot radically cure CML, cannot successfully treat CML patients, and reduce imatinib sensitivity, etc. To achieve the effect of improving bioavailability, controllable quality and safety, and strong operability

Active Publication Date: 2022-03-04
JIANGSU HANSOH PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The development and application of imatinib and second-generation and third-generation drugs have extended the survival time of patients with chronic myelogenous leukemia from 4-5 years to 10-20 years, but the application of tyrosine kinase inhibitors has not yet cure CML
[0004] Since imatinib does not really act on CML stem cells, CML patients must take the drug for a long time or even for life. Once the drug is stopped, the probability of disease recurrence or disease progression increases; Imatinib is mainly aimed at patients with early CML, and the complete remission rate for patients with middle and late stages is less than 30%, and a series of toxic reactions will occur after long-term use; especially some patients may develop imatinib resistance and the proportion is increasing year by year, a large number of reports show that this It is mainly related to the decreased sensitivity to imatinib caused by Bcr / abl mutation; in addition, the increased expression of the fusion protein caused by Bcr / abl gene amplification is also an important mechanism of its drug resistance
To address these problems, some new tyrosine kinase inhibitors such as Nilotinib and Dasatinib have been continuously developed and applied, but they still cannot successfully treat CML patients with T315I mutation
[0005] Before the discovery of imatinib, drugs active against Philadelphia chromosome (Ph)-positive myeloid leukemia (CML) were IFN-, cytarabine, and homoharringtonine (HHT), which could be used alone or in combination , but these already used drugs still have unsatisfactory effects

Method used

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  • Pharmaceutical composition of aminopyrimidine compound and preparation method thereof
  • Pharmaceutical composition of aminopyrimidine compound and preparation method thereof
  • Pharmaceutical composition of aminopyrimidine compound and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0082] Example 1 50mg / 100mg / 300mg / 400mg tablet

[0083] Raw materials Prescription Weight Percentage Meter active ingredient 40.0％ Low-substituted hydroxypropyl cellulose 20.0％ Calcium hydrogen phosphate 12.0％ silica 4.0％ Carboxymethyl Starch Sodium 4.0％ Magnesium stearate 1.0％ 50% ethanol in water 19.0％

[0084] Pass the active ingredients, fillers, and disintegrants through a 60-mesh sieve, respectively weigh the prescribed amount of active ingredients, fillers, disintegrators, and lubricants, mix them evenly, and add an appropriate amount of wetting agent to prepare a suitable soft material. , 24-mesh granulation, drying at 60°C, 30-mesh granulation, then adding the prescribed amount of lubricant, mixing evenly, testing the content of intermediates, determining the weight of the tablet, pressing the tablet, and putting the core into a high-efficiency coating machine. Set the air inlet temperature at 60°C ± 5°C, contr...

Embodiment 2

[0085] Example 2 50mg / 100mg / 200mg / 300mg tablet

[0086] Raw materials Prescription Weight Percentage Meter active ingredient 39.8％ Low-substituted hydroxypropyl cellulose 19.9％ Calcium hydrogen phosphate 11.9％ silica 4.0％ Carboxymethyl Starch Sodium 3.8％ Magnesium stearate 0.8％ 50% ethanol in water 19.8％

[0087] Pass the active ingredient, filler, and disintegrating agent through a 60-mesh sieve, weigh the prescribed amount of the active ingredient, filler, disintegrating agent, and lubricant, add them to the wet granulator, mix evenly, and add an appropriate amount of lubricant. Wet agent, prepare suitable wet granules, transfer them to the boiling dryer, set the air inlet temperature to 60°C, wait until the moisture content is ≤6%, discharge and granulate, then add the prescribed amount of lubricant, mix evenly, Test the content of intermediates, determine the weight of the tablet, press the tablet, put the core into...

Embodiment 3

[0088] Example 3 50mg / 100mg / 200mg / 300mg tablet

[0089] Raw materials Prescription Weight Percentage Meter active ingredient 42.0％ Low-substituted hydroxypropyl cellulose 19.0％ Calcium hydrogen phosphate 11.0％ silica 4.0％ Carboxymethyl Starch Sodium 4.0％ Magnesium stearate 1.0％ 50% ethanol in water 19.0％

[0090] Pass the active ingredient, filler, and disintegrating agent through a 60-mesh sieve, weigh the prescribed amount of the active ingredient, filler, disintegrating agent, and lubricant, add them to the wet granulator, mix evenly, and add an appropriate amount of lubricant. Wet agent, prepare suitable wet granules, transfer them to the boiling dryer, set the air inlet temperature to 60°C, wait until the moisture content is ≤6%, discharge and granulate, then add the prescribed amount of lubricant, mix evenly, Test the content of intermediates, determine the weight of the tablet, press the tablet, put the core into...

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Abstract

The present invention relates to a pharmaceutical composition of aminopyrimidine compounds and a preparation method thereof, specifically, the pharmaceutical composition comprises 4-[(4-methyl-1-piperazinyl)methyl]-N-[6-methyl yl-5-[(4-(3-pyridyl)-2-pyrimidinyl)amino]pyridin-3-yl]-3-(trifluoromethyl)-benzamide, its polymorphs, solvates Compounds, hydrates, pharmaceutically acceptable salts or combinations thereof as active ingredients, and at least one pharmaceutically acceptable excipient. The composition has good stability and drug dissolution rate, controllable product quality, simple preparation process, strong operability and is suitable for large-scale industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a pharmaceutical composition of aminopyrimidine compounds and a preparation method thereof. Background technique [0002] Chronic myeloid leukemia (CML) is a hematological malignancy originating from hematopoietic stem cells. The annual incidence in my country is about 0.36 / 100,000, and the median age of onset is 40-50 years old. CML manifests as unrestricted massive proliferation and aggregation of myeloid cells in the patient's bone marrow, which inhibits normal hematopoiesis in the bone marrow, and malignant granulocytes spread to the whole body through the blood, resulting in anemia, hemorrhage, infection and organ infiltration in the patient, thus seriously endangering the patient's body Health can even lead to death. About 95% of CML patients have a characteristic t(9:22) chromosomal translocation, which forms the Bcr / abl fusion gene, and the encoded ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/506A61P35/02A61K9/20
CPCA61K9/2095A61K31/506
Inventor 张克凤杨宝海宋阳王纯
Owner JIANGSU HANSOH PHARMA CO LTD
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