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Imatinib mesylate polymorph and pharmaceutical composition

A technology of imatinib mesylate and polymorphs, which can be used in drug combinations, antipyretics, antitumor drugs, etc., and can solve the problems of cumbersome process, poor reproducibility, poor product purity, etc.

Active Publication Date: 2013-03-13
NANJING CAVENDISH BIO ENG TECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The existing method has the disadvantages of complicated process, poor reproducibility, not suitable for industrial production and poor product purity

Method used

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  • Imatinib mesylate polymorph and pharmaceutical composition
  • Imatinib mesylate polymorph and pharmaceutical composition
  • Imatinib mesylate polymorph and pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0101] The preparation of embodiment 1 polymorph I

[0102] plan 1,

[0103] Add 500.0 g of imatinib mesylate into the reaction flask, add 2500 ml of dimethylformamide, raise the temperature to 60°C, and stir to dissolve. 12.5 L of acetone was added, and the crystal was grown at 60° C. for 2 hours. After cooling down to room temperature naturally, refrigerated crystallization overnight. Suction filtration, filter cake rinse with a small amount of acetone. The filter cake was dried under reduced pressure at 50°C and -0.095MPa, and was assisted with phosphorus pentoxide. 445.1 g of light yellow solid was obtained. Yield: 89.0%, purity 99.92%

[0104]

[0105] Note: Imalic acid: 4-(4-methylpiperazinemethyl)-benzoic acid

[0106] Imamamine: N-(5-amino-2-methylphenyl)-4-(3-pyridine)-pyrimidinamine

[0107] The resulting product of scheme 1 has been detected as follows: XRPD detection (see figure 1 ); IR detection (see figure 2 ); DSC detection (see image 3 ); TGA (se...

Embodiment 2

[0115] The product obtained in scheme 3 has been detected as follows: XRPD detection (see Figure 5 ). The prescription and preparation technology of embodiment 2 imatinib mesylate tablet:

[0116] The above-mentioned imatinib mesylate polymorph I was formulated into tablets containing 100 mg with several excipients as follows.

[0117] Imatinib mesylate I (calculated as imatinib)

100g

microcrystalline cellulose

170g

hypromellose

6g

Crospovidone

20g

Micropowder silica gel

2g

Magnesium stearate

2g

suppress

1000 pieces

[0118] Weigh the microcrystalline cellulose, hypromellose and crospovidone according to the prescription, mix them uniformly to obtain auxiliary material powder, and set aside. Weigh the imatinib mesylate according to the prescription, and mix it evenly with the auxiliary material powder to obtain the drug-containing mixed powder. Add appropriate amount of water...

Embodiment 3

[0121] The prescription and preparation technology of embodiment 3 imatinib mesylate capsules:

[0122] The above-mentioned imatinib mesylate polymorph I was formulated into tablets containing 100 mg with several excipients as follows.

[0123] Imatinib mesylate I (calculated as imatinib)

100g

microcrystalline cellulose

240g

Crospovidone

50g

Micropowder silica gel

5g

Magnesium stearate

5g

filling

1000 capsules

[0124] Weigh microcrystalline cellulose, crospovidone, micropowder silica gel and magnesium stearate according to the prescription, and mix them uniformly to obtain auxiliary material powder. Weigh the imatinib mesylate according to the prescription, and mix it evenly with the auxiliary material powder to obtain the drug-containing mixed powder. The drug-containing mixed powder is filled into No. 00 hard capsules to prepare capsules.

[0125] Capsules containing 400 mg of imatinib c...

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Abstract

The invention discloses an imatinib mesylate polymorph I, which is a typical X-ray diffraction pattern and has a diffraction peak at 2theta of 17.7+ / -0.2 degrees, 18.1+ / -0.2 degrees, 18.6+ / -0.2 degrees, 19.1+ / -0.2 degrees, 19.7+ / -0.2 degrees and 20.4+ / -0.2 degrees. In addition, the invention also discloses a preparation method thereof and a pharmaceutical composition. The imatinib mesylate polymorph I has the advantages of high purity, excellent physicochemical property and high stability, and is more suitable for industrial mass production.

Description

technical field [0001] The present invention relates to a polymorphic form of a pharmaceutical compound, more specifically, to a polymorphic form of imatinib mesylate. In addition, the present invention also relates to a preparation method of the polymorphic form and a pharmaceutical composition thereof. Background technique [0002] Imatinib mesylate is a tyrosinase inhibitor developed by Novartis, Switzerland, for the treatment of gastrointestinal stromal tumors (GISTs). Its chemical name is 4-[(4-methylpiperazine-1-methyl)]-N-[4-methyl-3-[[4-(3-pyridyl)-2-pyrimidine]]phenyl ]-benzamide methanesulfonate, the chemical structure is as follows: [0003] [0004] Novartis disclosed two polymorphs α and β of imatinib mesylate in Chinese patent application-Application No. 98807303.X (hereinafter referred to as Patent Application No. 303). The α crystal form is characterized by needle crystals with hygroscopicity and poor fluidity. Its typical XRPD pattern shows that the α f...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D401/04A61K31/506A61P35/00A61P29/00A61P27/02A61P7/06A61P25/00A61P25/20A61P17/00A61P9/12
Inventor 严荣杨浩许永翔
Owner NANJING CAVENDISH BIO ENG TECH
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