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Imatinib mesylate tablet cores, coated tablets, and preparation method thereof

A technology of imatinib mesylate and coated tablets is applied in the field of medicine to achieve the effects of improving drying rate, uniform content and improving compliance

Inactive Publication Date: 2013-05-08
SHANGHAI YINGLI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The technical problem to be solved by the present invention is to overcome the defect that the pharmaceutically active ingredients in the existing imatinib mesylate preparations are the mesylate β crystal form of imatinib, and a kind of imatinib mesylate is provided. Matinib tablet core, coated tablet and preparation method thereof, the imatinib mesylate coated tablet of the present invention has the advantages of high dissolution rate and fast release, and combines the properties of the imatinib mesylate drug itself , can be prepared by a variety of processes, which is conducive to controlling production costs and realizing large-scale industrialization

Method used

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  • Imatinib mesylate tablet cores, coated tablets, and preparation method thereof
  • Imatinib mesylate tablet cores, coated tablets, and preparation method thereof
  • Imatinib mesylate tablet cores, coated tablets, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Example 1: Tablet formulation (50 mg tablet)

[0057] 1.1 The formula of imatinib mesylate tablet core in the present embodiment is as shown in Table 1.

[0058] The imatinib mesylate tablet core formula of table 1 embodiment 1 (making 10000 altogether)

[0059]

[0060] 1.2 Prepare the imatinib mesylate tablet core of the above-mentioned formula, carry out according to the following steps:

[0061] 1.2.1 The raw material is air-pulverized, and the particle size is less than 20um.

[0062] 1.2.2 Mix imatinib mesylate, microcrystalline cellulose and sodium carboxymethyl starch evenly, add polyvinylpyrrolidone K30 solution with a concentration of 12% by mass percentage, carry out rapid stirring and granulation, and obtain soft material Fluidized bed drying under the condition of wind temperature 65 ℃.

[0063] 1.2.3 After drying, add sodium carboxymethyl starch, micropowder silica gel and magnesium stearate, mix well, and press into tablets. Among them, the diamete...

Embodiment 2

[0069] Example 2: Tablet formulation (100 mg tablet)

[0070] 2.1 The formula of imatinib mesylate tablet core in the present embodiment is as shown in Table 3.

[0071] The imatinib mesylate tablet core formula of table 3 embodiment 2 (making 5000 altogether)

[0072]

[0073] 2.2 To prepare the imatinib mesylate tablet core of the above prescription, proceed according to the following steps:

[0074] 2.2.1 Raw materials are air-pulverized, particle size <20um.

[0075] 2.2.2 Add imatinib mesylate, microcrystalline cellulose and croscarmellose sodium into the fluidized bed equipped with top spray equipment as the base, and hydroxypropyl cellulose is dissolved in water to form a mass percentage The mixed liquid with a concentration of 11.8% is sprayed onto the substrate in a fluidized state to form granules. The material temperature is about 35°C for spraying and granulation, and the inlet air temperature is 70°C for drying.

[0076] 2.2.3 After drying, add microcrystall...

Embodiment 3

[0081] Example 3: Tablet formulation (100 mg tablet)

[0082] 3.1 The formula of imatinib mesylate tablet core in the present embodiment is as shown in Table 5.

[0083] The imatinib mesylate tablet core formula of table 5 embodiment 3 (making 5000 altogether)

[0084]

[0085] 3.2 To prepare the imatinib mesylate tablet core of the above prescription, follow the steps below:

[0086] 3.2.1 Raw materials are air-pulverized, particle size <20um.

[0087] 3.2.2 Mix imatinib mesylate, microcrystalline cellulose and cross-linked polyvinylpyrrolidone evenly, add a hydroxypropyl methylcellulose solution with a mass percentage concentration of 11.1% for rapid stirring and granulation, and obtain a soft material Fluidized bed drying at an inlet air temperature of about 65°C.

[0088] 3.2.3 After drying, add microcrystalline cellulose, cross-linked polyvinylpyrrolidone, micropowder silica gel and magnesium stearate, mix well, and press into tablets. Wherein, the diameter of the ...

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Abstract

The invention discloses imatinib mesylate tablet cores comprising, by weight, 20-70% of imatinib mesylate alpha crystalline form, 10-50% of a filling agent, 0-10% of an adhesive, 10-30% of a disintegrant, 0.1-5% of a flow aid, and 0.1-2% of a lubricant. According to the tablet core preparation method, granulation and tabletting are carried out with the formula. The invention also discloses imatinib mesylate coated tablets and a preparation method thereof. The coated tablets comprise, by weight, 95-97% of the imatinib mesylate tablet cores, 0.5-4% of a film forming agent, 0.1-1% of a plasticizer, 0.1-1% of a coloring agent, and 0.1-1% of a lubricant. The preparation method of the coated tablets comprises the steps that the tablet cores are coated, such that the imatinib mesylate coated tablets are prepared. The tablets have the advantages of high dissolution rate and fast release.

Description

technical field [0001] The invention relates to the field of medicines, in particular to an imatinib mesylate tablet core, a coated tablet and a preparation method thereof. Background technique [0002] Imatinib mesylate, chemically known as 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridyl) )-2-pyrimidinyl]amino]-phenyl]benzamide methanesulfonate. Imatinib mesylate is indicated for the treatment of Philadelphia chromosome-positive chronic myelogenous leukemia (CML) and Kit (CD117)-positive unresectable and / or metastatic malignant gastrointestinal stromal carcinoma (GIST). [0003] The mechanism of action of imatinib is to competitively inhibit the binding site of adenosine triphosphate (ATP) and thymidine kinase (TK) receptors such as KIT, block TK phosphorylation, thereby inhibiting signal transduction, and inhibiting the kinase activity-related KIT mutation (causes KIT receptor activation) and wild-type KIT. There are three main targets: Abelson (ABL) pro...

Claims

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Application Information

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IPC IPC(8): A61K9/28A61K31/506A61P35/02A61P35/04
Inventor 施斌周耀
Owner SHANGHAI YINGLI PHARM CO LTD
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