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Imatinib-containing composition and preparation method thereof

A composition and adhesive technology, which is applied in the directions of medical preparations, drug combinations, and pharmaceutical formulations containing active ingredients, can solve problems such as strong hygroscopicity and difficult preparations, and achieve low cost, good stability, and simple and efficient preparation. The effect of craftsmanship

Inactive Publication Date: 2011-11-16
HANGZHOU HUADONG MEDICINE GRP PHARMA RES INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] The invention adopts a reasonable ratio of raw materials and auxiliary materials, solves the problem of imatinib strong hygroscopicity and is difficult to prepare, provides a stable imatinib composition, a simple and efficient preparation process, and can achieve lower technical requirements for equipment, The wet preparation process based on a wider industrialized production produces imatinib oral solid preparations that also have significant clinical efficacy

Method used

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  • Imatinib-containing composition and preparation method thereof
  • Imatinib-containing composition and preparation method thereof
  • Imatinib-containing composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] prescription:

[0039]

[0040] Remarks: the povidone K30 used in composition 1-3 is absolute ethanol solution, the concentration is 3% (w / w), the concentration of povidone K30 absolute ethanol solution used in composition 4 is 1% (w / w) / w), the concentration of povidone K30 dehydrated alcohol used in composition 4-7 is 5% (w / w).

[0041] Preparation method: In addition to povidone, imatinib, microcrystalline cellulose, lactose, crospovidone, talcum powder, silicon dioxide and magnesium stearate are passed through 80-mesh sieve respectively, and set aside.

[0042] Weigh the imatinib of prescription quantity, the microcrystalline cellulose of 4 / 7 total prescription quantity, the crospovidone of 1 / 2 total prescription quantity put fast granulator, mix, add above-mentioned povidone K30 without Hydroalcoholic solution for wet granulation. Dry at about 55°C until the moisture content of the granules is <5%, and sieve the granules with a 24-mesh sieve. Add remaining mi...

Embodiment 2

[0049] prescription:

[0050]

[0051] Remarks: The povidone K30 used is an anhydrous ethanol solution with a concentration of 5% (w / w).

[0052] Preparation method: with embodiment 1.

[0053] In this embodiment, the inventors compared the compression molding and fluidity of the compositions when the respective compositions contained different types of lubricants, see compositions 8-10. The results show that the combined use of talcum powder, magnesium stearate and silicon dioxide as lubricants can effectively solve the problems of stickiness and poor fluidity of the composition during the preparation process. The present inventors further conducted a screening test on the dosage of talcum powder, magnesium stearate and silicon dioxide and the disintegrant crospovidone, see composition 11. The result shows that the optimal weight ratio of the lubricating composition lubricant magnesium stearate, talcum powder and micropowder silica gel that the present invention obtains ...

Embodiment 3

[0056] Example 3 pilot test

[0057] Prescription:

[0058]

[0059] Preparation Process:

[0060] (1) Preparation and screening of raw and auxiliary materials: except povidone K30, imatinib, microcrystalline cellulose, lactose, crospovidone, talcum powder, silicon dioxide, and magnesium stearate were passed through 80 meshes respectively Sieve and set aside.

[0061] (2) Preparation of povidone K-30 absolute ethanol solution: Weigh an appropriate amount of povidone K-30, add appropriate amount of absolute ethanol, stir to dissolve until clear, add appropriate amount of absolute ethanol to make a concentration of 1% ( g / g) of povidone K-30 absolute ethanol solution, to obtain.

[0062] (3) Mixing and granulation: Weigh the prescribed amount of imatinib, 4 / 7 of the total prescribed amount of microcrystalline cellulose and 1 / 2 of the total prescribed amount of crospovidone, and place them in a rapid granulator, mix well, Add the above-mentioned povidone K30 absolute eth...

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Abstract

The invention relates to an imatinib-containing composition and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. The imatinib-containing composition disclosed by the invention is composed of imatinib, a diluent, a disintegrating agent, an adhesive and a lubricant, wherein the imatinib is imatinib mesylate alpha crystal; the diluent is a mixture of microcrystalline cellulose and lactose; the disintegrating agent is cross-linked polyvidone; the adhesive is polyvidone K30; and the lubricant is a mixture of magnesium stearate, talc powder and silica micropowder. The preparation method is simple and efficient in process, and can be used for industrial mass production, and the problem that the imatinib mesylate alpha crystal has strong hydroscopicityis and is not easy to form preparation is completely solved.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a composition containing imatinib mesylate α crystal form and a preparation method thereof. [0002] Background technique [0003] Imatinib mesylate, chemically known as 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridyl) )-2-pyrimidinyl]amino]-phenyl]benzamide methanesulfonate, the molecular formula is C 29 h 31 N 7 O.CH 4 SO 3 , with a molecular weight of 589.7. [0004] The chemical structural formula of imatinib mesylate is as follows: [0005] [0006] Imatinib Mesylate is a specific tyrosine kinase inhibitor (tyrosine kinases inhibitors, TKI) developed by Swiss Novartis. On May 10, 2001, imatinib entered the U.S. FDA’s express approval channel with a breakthrough anti-tumor mechanism. Drugs for the treatment of leukemia. [0007] After extensive clinical verification, imatinib mesylate has been highly appraised by the global me...

Claims

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Application Information

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IPC IPC(8): A61K31/506A61P35/00A61P35/02
Inventor 卢良华赖观平
Owner HANGZHOU HUADONG MEDICINE GRP PHARMA RES INST
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