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Pharmaceutical preparation for rapidly releasing citric acid benzene ring tinib and preparation method thereof

A technology for cyclobenztinib citrate and a pharmaceutical preparation, which is applied in the field of rapid-release drug cyclobentinib tablets and the preparation thereof, can solve the problems such as the inability to meet the treatment requirements of different types of patients, and achieves shortening the granulation time, No serious toxicity occurs, the effect of avoiding the use of organic solvents

Inactive Publication Date: 2013-08-21
LIAONING UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The current domestic drug release standard is 80% in 45 minutes, which cannot meet the treatment requirements for different types of patients. Improving the drug release rate can be accomplished by preparing different dosage forms

Method used

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  • Pharmaceutical preparation for rapidly releasing citric acid benzene ring tinib and preparation method thereof
  • Pharmaceutical preparation for rapidly releasing citric acid benzene ring tinib and preparation method thereof
  • Pharmaceutical preparation for rapidly releasing citric acid benzene ring tinib and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] The preparation of embodiment 1 cyclobenztinib citrate and pharmacodynamic research result

[0040] (1) Preparation and structure confirmation of cyclobenztinib citrate

[0041] Add N-{4-methyl-3-[(4-pyridin-3-yl)pyrimidine-2-amino]phenyl}-5-(4-methylpiperazin-1-yl)-5 to the reaction flask, 6,7,8-tetrahydronaphthalene-2-amide (5.33 g, 10 mmol), 200 ml of absolute ethanol, citric acid (1.01 g, 10.5 mmol), stirred and refluxed at 70°C for 0.5 hours, After cooling to room temperature, a solid precipitated out, which was filtered out by suction and recrystallized by stirring with 180 ml of ethanol. Filter and dry to get the product N-{4-methyl-3-[(4-pyridin-3 base)pyrimidine-2-amino]phenyl}-5-(4-methylpiperazin-1-yl)- 5.94 g of 5,6,7,8-tetrahydronaphthalene-2-amide citrate, namely cyclobenztinib citrate, with a yield of 94.5%.

[0042] Molecular formula: C 32 h 35 N 7 O·C 6 h 8 o 7 .

[0043] Melting point: 191-193°C.

[0044] 1 H-NMR (DMSO-d 6 ppm): δ9.98(s,1H...

Embodiment 5

[0065] Embodiment 5 rapid release cyclobenztinib citrate tablet

[0066] (1) The formula is as follows:

[0067]

[0068]

[0069] (2) The preparation method is as follows:

[0070] 1) Pass cyclobenztinib citrate through a 200-mesh sieve;

[0071] 2) Weigh cyclobenztinib citrate, microcrystalline cellulose and crospovidone, and mix them evenly;

[0072] 3) Weigh the added part of talc powder and polyethylene glycol 6000, mix well;

[0073] 4) Dry granulation machine granulation, pressure 5MPa;

[0074] 5) Add the additional part of crospovidone, talcum powder and polyethylene glycol 6000 according to the prescription ratio, and mix well;

[0075] 6) Compressed into tablets, hardness 6-8Kg / cm 2 .

Embodiment 6

[0077] The tablet obtained in Example 5 was coated with Opadry.

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Abstract

The invention relates to a pharmaceutical preparation for rapidly releasing citric acid benzene ring tinib and a preparation method thereof. The citric acid benzene ring tinib and a medicinal excipient are prepared into tablets; the pharmaceutical preparation comprises the following components by weight percent: 40-65% of citric acid benzene ring tinib; and the medicinal excipient is a disintegrating agent, a filler and a lubricating agent, and contains the components by weight percent: 5-25% of disintegrating agent, 20-50% of filler and 0.5-5% of lubricating agent. The medicine tablet of the citric acid benzene ring tinib provided by the invention can achieve the complete release target after 8 minutes; use of a granulating organic solvent is avoided by adopting a dry granulation method; meanwhile, the granulation time is shortened; and the production safety is greatly improved. The medicine tablet of the citric acid benzene ring tinib provided by the invention belongs to a tetrahydronaphthalene amide compound, and can be used for treating chronic myelogenous granulocyte leukemia, gastrointestinal stromal tumor and the like.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a cyclobenztinib tablet for rapid drug release and a preparation method thereof. Background technique [0002] N-{4-methyl-3-[(4-pyridin-3-yl)pyrimidine-2-amino]phenyl}-5-(4-methylpiperazin-1-yl)-5,6,7, 8-Tetrahydronaphthalene-2-amide is a selective tyrosine kinase inhibitor, which belongs to tetrahydronaphthalene amides, and is used for the treatment of chronic myeloid leukemia and gastrointestinal stromal tumors. [0003] The release speed of the drug has a great influence on the absorption and distribution of the drug, which determines the onset speed of the drug. The current domestic drug release standard is 80% in 45 minutes, which cannot meet the treatment requirements for different types of patients. Improving the drug release rate can be accomplished by preparing different dosage forms. Therefore, developing how to improve the rapid release of drugs has always...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/506A61K9/20A61P35/02A61P35/00
Inventor 陈烨王洋
Owner LIAONING UNIVERSITY
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