Pharmaceutical preparation containing imatinib mesylate and preparation method thereof

A technology for imatinib mesylate and pharmaceutical preparations, applied in the field of pharmaceutical preparations, can solve the problems of unsuitable α crystal form and difficult medicinal use of imatinib mesylate, and achieves reduced types of excipients and high safety Effect

Active Publication Date: 2016-02-24
JIANGSU HANSOH PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The purpose of the present invention is to overcome the prejudice that the α crystal form is not suitable for the application of preparations in the development of the drug, provide a kind of imatinib mesylate tablet containing the α crystal form, turn disadvantages into advantages, and solve the problem of α crystal form mesylate. Difficult medicinal use of imatinib acid

Method used

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  • Pharmaceutical preparation containing imatinib mesylate and preparation method thereof
  • Pharmaceutical preparation containing imatinib mesylate and preparation method thereof
  • Pharmaceutical preparation containing imatinib mesylate and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0030] The preparation of embodiment 1~3 different wetting agent tablet

[0031] The composition of table 1 tablet (1000 pieces)

[0032] Element

Example 1

Example 2

Example 3

Imatinib mesylate

120g

120

120

microcrystalline cellulose

55g

55

55

Crospovidone

40g

40

40

silica

3g

3g

3g

Magnesium stearate

2g

2g

2g

Opadry

6.6g

6.6g

6.6g

lubricant

50% ethanol

75% ethanol

ethanol

[0033] 1.1 Preparation

[0034] Mix the pretreated imatinib mesylate and internal pharmaceutical excipients in a wet granulation pot, then granulate with a wetting agent, then dry and granulate, add external excipients and mix, then compress into tablets, package Clothes.

[0035] 1.2 Evaluation

[0036] Method: Chinese Pharmacopoeia 2010 Edition II XC Second Method Paddle Method

[0037] Medium: 900ml of hydrochloric acid solution with pH 1....

Embodiment 8-10

[0059] Adopt the preparation method of embodiment 1-3, wherein wetting agent is 75% ethanol

[0060] Element

Example 8

Example 9

Example 10

Imatinib mesylate

120g

120g

120g

microcrystalline cellulose

60.3g

49.5g

35.3g

Crospovidone

33g

44g

55g

silica

4.5g

3.3g

7.5g

Magnesium stearate

1.1g

2.2g

1.1g

Opadry

1.1g

1.1g

1.1g

lubricant

75% ethanol

75% ethanol

75% ethanol

[0061] Gained preparation dissolution rate result is as follows:

[0062] Table 5 Dissolution evaluation results

[0063]

[0064] Result: the dissolution results of the above examples show that the dissolution effects of the preparation examples of the present invention are stable and have good reproducibility.

experiment example 1

[0065] Experimental example 1, stability test

[0066] In order to verify whether the preparation containing the α crystal form in the present invention will transform into the β crystal form in a long-term storage environment, the inventor prepared 3 batches of samples using the prescription and preparation process of Example 2 and Example 9, respectively named For samples 2-1, 2-2, 2-3 and 9-1, 9-2, 9-3, samples were taken to detect the transformation of the preparation crystal form in different environments.

[0067] Table 6 Crystal Form Stability Monitoring (25±2°C, RH=60%±15%)

[0068]

[0069]

[0070] Table 7 Crystal Form Stability Monitoring (45±2°C, RH=75%±5%)

[0071]

[0072] Note: The criterion for distinguishing whether the crystal is transformed is that at least one diffraction peak deviates from the normal error by 0.2°. If the marker peak (diffraction peak with 2θ of 4.9) is missing, it can be determined that the α crystal form has undergone transform...

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Abstract

The invention discloses a medicinal preparation containing imatinib mesylate and a preparation method thereof, and particularly relates to a medicinal preparation by adopting Alpha-crystal imatinib mesylate as an active ingredient. The medicinal preparation comprises 45-65% of imatinib mesylate, 10-25% of a disintegrating agent, 20-40% of a diluent, 1-4% of a glidant and 0.5-1.5% of a lubricant. The medicinal preparation converts the disadvantage of high tenacity of Alpha-crystal imatinib mesylate into the advantage, eliminates an adhesive in a recipe, and is less in categories of used auxiliary materials and relatively higher in security compared with products sold in the market; the problem of Alpha-crystal crystal transformation is solved, and the problem that imatinib mesylate is difficult in medical use is solved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and specifically relates to a tablet prepared by using α-crystal imatinib mesylate as a raw material drug. Background technique [0002] Imatinib mesylate was developed by Novartis and is the world's first marketed tumorigenesis-related signal transduction inhibitor. It is clinically used for the treatment of chronic phase, chronic myelogenous leukemia (Ph+CML) with Philadelphia chromosome positive Accelerated phase or blast phase, for the treatment of adult patients with unresectable and / or metastatic malignant gastrointestinal stromal tumors (GIST). This variety was first launched in the United States in May 2001, and then entered the markets of Europe, Australia, Japan, Canada and other countries, and was launched in China in 2002. At present, it has obtained orphan drug status in the United States, the European Union and Japan, and its trade name is " "( ), its dosage form is o...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K31/506A61P35/00
Inventor 孙运栋王革
Owner JIANGSU HANSOH PHARMA CO LTD
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