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Pharmaceutical composition of imatinib salt for injection and preparation method thereof

A technology of imatinib and imatinib mesylate, applied in the field of medicine, can solve the problems of patients being unable to take oral administration, limiting the onset speed of imatinib, etc., so as to achieve good reproducibility of the preparation method and avoid long-term effects. Timed injection or multiple injections for highly controllable effects

Pending Publication Date: 2022-04-12
JIANGSU SIMCERE PHARMA
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0008] Aiming at the technical problem that the current imatinib product is only suitable for oral administration, which limits the onset speed of imatinib in the body and cannot be administered orally in some patients, the present invention provides a high-concentration imatinib for injection The pharmaceutical composition of Nisalin greatly increases the rate of increase in blood drug concentration, shortens the onset time of the drug, avoids large-volume injections or multiple injections, and reduces side effects caused by large-volume injections or multiple injections

Method used

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  • Pharmaceutical composition of imatinib salt for injection and preparation method thereof
  • Pharmaceutical composition of imatinib salt for injection and preparation method thereof
  • Pharmaceutical composition of imatinib salt for injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Add imatinib free base (5.0g, 10mmol) and methanesulfonic acid (1.06g, 11mmol) into ethanol (50ml) respectively to obtain a mixture, heat the mixture to 60°C, stir for 1h, filter the reaction solution hot, and cool down After stirring at room temperature for 2 h, the product was filtered and dried to obtain imatinib mesylate (5.19 g, yield 88%) as a white solid powder. Other salt forms were prepared in a similar manner.

[0042] The properties, solubility and pH value of imatinib salt were tested respectively, and the results are shown in Table 1:

[0043] Table 1

[0044]

[0045]

[0046]- indicates a solubility of less than 25 mg / ml, + indicates a solubility of 25-50 mg / ml, ++ indicates a solubility of 50-100 mg / ml, +++ indicates a solubility of more than 100 mg / ml.

[0047] Solubility test method: Take imatinib salt, add a certain amount of purified water, shake or ultrasonically check whether it is dissolved or not, if it is not dissolved, continue to incre...

Embodiment 2

[0052] The salt of the present invention was dissolved in 0.9% sodium chloride aqueous solution, 5% glucose aqueous solution and 5% mannitol aqueous solution respectively, and the solubility at different temperatures was tested as shown in Table 2.

[0053] Table 2

[0054]

[0055]

[0056] - indicates a solubility of less than 25 mg / ml, + indicates a solubility of 25-50 mg / ml, ++ indicates a solubility of 50-100 mg / ml, +++ indicates a solubility of more than 100 mg / ml.

[0057] The result shows: in 0.9% sodium chloride solution, the solubility of most of the salts is low, there are different degrees of precipitation, and the storage stability is poor; although the solubility of tartrate in 0.9% sodium chloride aqueous solution is still 50~100mg / ml, but with the decrease of tartrate concentration, precipitation will occur. The pharmaceutical composition of the present invention is stable in storage and not easy to separate out.

Embodiment 3

[0059] Preparation of imatinib tartrate injection composition

[0060]

[0061] Preparation method: According to the prescription, add imatinib tartrate and additives into 60-70ml of water, stir until completely dissolved, and then dilute to 100ml with water. After being filtered through a 0.22 μm microporous membrane, the mixture was divided into vials to obtain the imatinib tartrate injection composition. The composition can also be freeze-dried to obtain a freeze-dried powder injection.

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Abstract

The invention provides the high-concentration pharmaceutical composition of the imatinib salt for injection, which does not need to be additionally prepared into an infusion bag, realizes small-volume rapid intravenous administration, greatly improves the rising speed of the blood concentration, shortens the onset time of the medicine, is particularly suitable for patients needing rapid administration and patients with dysphagia, and has a wide application prospect. The pharmaceutical composition disclosed by the invention has the beneficial effects of remarkably improved stability, few degraded impurities, no drug precipitation, simple prescription, stable quality, easiness in operation of the preparation method, strong controllability and the like.

Description

[0001] This application claims to be submitted to the State Intellectual Property Office of China on September 30, 2020. The patent application number is 202011054707.2, and the invention title is "a pharmaceutical composition of imatinib salt for injection and its preparation method". priority. The entirety of the aforementioned prior application is incorporated by reference into the present application. technical field [0002] The invention relates to the technical field of medicine, in particular to a pharmaceutical composition of imatinib salt for injection and a preparation method thereof. Background technique [0003] Imatinib mesylate, trade name Gleevec (Gleevec), is a tyrosine kinase inhibitor for the treatment of chronic myelogenous leukemia, gastrointestinal stromal tumors, acute lymphoblastic leukemia, systemic diseases such as mastocytosis. The structural formula is as follows: [0004] [0005] The currently marketed products are mainly imatinib mesylate...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/506A61K9/19A61K9/08A61K47/10A61K47/26A61P9/10A61P35/00A61P35/02
Inventor 杨磊黄常康杨少宁张斐胡玉林孙政王鹏任晋生
Owner JIANGSU SIMCERE PHARMA
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