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Medicinal dasatinib composition and preparation method thereof

A technology of dasatinib and a composition, applied in the field of pharmaceutical preparations, can solve problems such as unfavorable industrial production, complex process, long cycle, etc., and achieve the effects of avoiding unequal risks, improving microenvironment, and improving stability

Active Publication Date: 2014-06-11
QILU PHARMA HAINAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The disadvantage of this process is that the raw material of the required particle size is obtained by reprocessing the prepared dasatinib anhydrate (pure form N-6), the process needs to use a large amount of organic solvent, and the process Complex, long cycle, not conducive to industrial production

Method used

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  • Medicinal dasatinib composition and preparation method thereof
  • Medicinal dasatinib composition and preparation method thereof
  • Medicinal dasatinib composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Example 1. Dasatinib Tablets Prescription Composition: The specification is 70 mg (calculated as Dasatinib), and the prescription quantity is 1000 tablets.

[0050]

[0051]

[0052] Preparation method: mix the prescription amount of dasatinib anhydrous with lactose, microcrystalline cellulose, and hydroxypropyl methylcellulose evenly, add 90 g of purified water to hydroxypropyl cellulose to make a solution, and add the solution to the above-mentioned The dasatinib mixture was granulated by a high-shear wet granulator, dried, and then the prescribed amount of croscarmellose sodium and magnesium stearate was added, mixed evenly, and compressed into tablets.

[0053] The dasatinib tablet of embodiment 1 and test example and " Shi Da The comparison chart of the dissolution curves of "tablets in different dissolution media" Figure 1~3 shown.

Embodiment 2

[0054] Example 2. Dasatinib Tablets Prescription Composition: The specification is 70 mg (calculated as Dasatinib), and the prescription quantity is 1000 tablets.

[0055]

[0056] Preparation method: mix the prescription amount of dasatinib anhydrous with lactose, microcrystalline cellulose, methylcellulose and hydroxypropyl cellulose evenly, add 90g of purified water to wet granulate, dry, and then add the prescription amount The crospovidone and magnesium stearate were mixed evenly and compressed into tablets.

[0057] The dasatinib tablet of embodiment 2 and " Shi Da The comparison chart of the dissolution curves of "tablets in different dissolution media" Figure 4~6 shown.

Embodiment 3

[0058] Example 3. Dasatinib Tablet Prescription Composition: The specification is 70 mg (calculated as Dasatinib), and the prescription quantity is 1000 tablets.

[0059]

[0060] Preparation method: mix the prescribed amount of dasatinib anhydrous with lactose, microcrystalline cellulose, low-substituted hydroxypropyl cellulose, hydroxypropyl methyl cellulose and povidone, and add 90g of purified water to wet granulate , dried, then add the prescribed amount of magnesium stearate, mix well, and compress into tablets.

[0061] The dasatinib tablet of embodiment 3 and " Shi Da The comparison chart of the dissolution curves of "tablets in different dissolution media" Figure 7~9 shown.

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Abstract

The invention relates to a medicinal dasatinib composition and preparation method thereof. The composition comprises an effective amount of dasatinib and medicinal auxiliary materials, wherein dasatinib is an anhydride, and the medicinal materials comprise 3-15 percent by weight of retardant; the retardant is a hydrophilic gel material, and is selected from hydroxypropylmethyl cellose, methyl cellulose, carbopol or alginate. The invention also provides a preparation method of the medicinal dasatinib composition. According to the medicinal dasatinib composition, the microenvironment of the solid preparation can be improved due to the retardant, so that the preparation stability can be improved on one hand, and on the other hand, the dissolution velocity of the oral preparation can be controlled. The medicinal dasatinib composition is simple in process and low in cost, and does not have pollution.

Description

technical field [0001] The invention relates to a dasatinib pharmaceutical composition and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Dasatinib (dasatinib / Sprycel), developed by Bristol-Myers Squibb (BMS), was first launched in the United States in 2006 in the form of monohydrate tablets (the structural formula is shown in Formula I below), and is used for the treatment of Imatinib mesylate resistance, or intolerant Philadelphia chromosome positive (Ph+) chronic myeloid leukemia (CML) adult patients with chronic phase, accelerated phase and blast phase (acute myeloid change and acute lymphoblastic change). The drug is currently approved in most countries around the world. The curative effect is longer lasting and the safety is higher. [0003] The chemical name of dasatinib monohydrate: N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]- 2-Methyl-4-pyrimidinyl]amino]-5-thia...

Claims

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Application Information

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IPC IPC(8): A61K31/506A61K47/38A61K47/36A61K47/32A61P35/02
Inventor 郑晓清杨清敏邹永华赵娜娜张明会
Owner QILU PHARMA HAINAN
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