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Fosaprepitant-meglumine crystal compound, preparation method thereof, and pharmaceutical composition

The technology of a crystal compound and fosaprepitant, which is applied in the field of medicine, can solve the problems of easy moisture absorption and change in quality, increase in moisture absorption capacity, and deteriorate in fluidity, etc., and achieves good fluidity, improved hygroscopicity, and medication safety. improved effect

Inactive Publication Date: 2017-04-19
SHANDONG YUXIN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] Therefore, the known solid form of fosaprepitant dimeglumine has certain defects, especially its hygroscopicity. After it is prepared into a freeze-dried powder injection, its hygroscopicity becomes stronger, its fluidity becomes poorer, and it is easy to absorb moisture. Spoilage and fill discrepancies

Method used

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  • Fosaprepitant-meglumine crystal compound, preparation method thereof, and pharmaceutical composition
  • Fosaprepitant-meglumine crystal compound, preparation method thereof, and pharmaceutical composition
  • Fosaprepitant-meglumine crystal compound, preparation method thereof, and pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0073] Embodiment 1, the preparation of crystal compound of the present invention

[0074] (1) Add 10 g of the crude product of Fosaprepitant Diglumine and 150 ml of methanol into the reaction vessel, under the protection of nitrogen, stir for 30 minutes to dissolve the crude product of Fosaprepitant Diglumine to form methanol of Fosaprepitant Diglumine Solution, cooled to 5 ~ 15 ° C, filtered;

[0075] (2) Prepare 675ml of a mixture of methyl tert-butyl ether and isopropanol (1:1), lower the temperature to 5-15°C, protect it under nitrogen, and divide it into three parts on average;

[0076] (3) Under the protection of nitrogen, slowly add the methanol solution in step (1) dropwise to one of the mixed solutions at 5-15°C, and drop it for about 0.5-1 hour. After the drop, a small amount of white solid is precipitated;

[0077] (4) Slowly add the reaction solution in step (3) to another part of the mixed solution, about 15min to 30min after the addition, after the addition, un...

Embodiment 2

[0080] Embodiment 2, the preparation of crystalline compound of the present invention

[0081] (1) Add 10 g of the crude product of Fosaprepitant Diglumine and 175 ml of methanol into the reaction vessel, under nitrogen protection, stir for 30 minutes to dissolve the crude product of Fosaprepitant Diglumine to form methanol of Fosaprepitant Diglumine Solution, cooled to 5 ~ 15 ° C, filtered;

[0082] (2) Prepare 1050ml of a mixture of methyl tert-butyl ether and isopropanol (1:1), lower the temperature to 5-15°C, protect it under nitrogen, and divide it into three parts on average;

[0083] (3) Under the protection of nitrogen, slowly add the methanol solution in step (1) dropwise to one of the mixed solutions at 5-15°C, and drop it for about 0.5-1 hour. After the drop, a small amount of white solid is precipitated;

[0084] (4) Slowly add the reaction solution in step (3) to another part of the mixed solution, about 15min to 30min after the addition, after the addition, unde...

Embodiment 3

[0087] Embodiment 3, the preparation of crystal compound of the present invention

[0088] (1) Add 10 g of the crude product of Fosaprepitant Diglumine and 125 ml of methanol into the reaction vessel, under the protection of nitrogen, stir for 30 minutes to dissolve the crude product of Fosaprepitant Diglumine to form methanol of Fosaprepitant Diglumine Solution, cooled to 5 ~ 15 ° C, filtered;

[0089] (2) Prepare 500ml of a mixture of methyl tert-butyl ether and isopropanol (1:1), lower the temperature to 5-15°C, protect it under nitrogen, and divide it into three parts on average;

[0090] (3) Under the protection of nitrogen, slowly add the methanol solution in step (1) dropwise to one of the mixed solutions at 5-15°C, and drop it for about 0.5-1 hour. After the drop, a small amount of white solid is precipitated;

[0091] (4) Slowly add the reaction solution in step (3) to another part of the mixed solution, about 15min to 30min after the addition, after the addition, un...

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Abstract

The invention relates to the field of medicines, and discloses a fosaprepitant-meglumine crystal compound, a preparation method thereof, and a pharmaceutical composition. The fosaprepitant-meglumine crystal compound is different from those available in the prior art, wherein Cu-K alpha rays are adopted for measurement to obtain an X-ray powder diffraction pattern as shown in FIG. 1. The fosaprepitant-meglumine crystal compound is good in stability, good in fluidity, not easy to absorb moisture, simple in preparation method and easy to operate. When the fosaprepitant-meglumine crystal compound is prepared as the pharmaceutical composition, the medication safety is greatly improved. Therefore, the fosaprepitant-meglumine crystal compound is very suitable for clinical application.

Description

technical field [0001] The invention belongs to the field of medicine, and discloses a fosaprepitant dipeglumine crystal compound, a preparation method and a pharmaceutical composition thereof. Background technique [0002] Fosaprepitant Dimeglumine (Fosaprepitant Dimeglumine) is clinically used as an adjuvant drug in the treatment of brain tumors to prevent acute and delayed nausea and vomiting caused by chemotherapy. Fosaprepitant is a neurokinin‐1 (NK‐1) receptor antagonist, or substance P antagonist, that works primarily by blocking nausea and vomiting signals in the brain. The NK‐1 receptor is the binding site for tachykinin (NKA) substance P (SP), located in the brainstem vomiting center and the gastrointestinal tract. Animal experiments have proved that SP can induce vomiting, and drugs that specifically block this receptor can prevent vomiting caused by all emetogenic stimuli (including cisplatin). [0003] Fosaprepitant dipglumine is a prodrug of aprepitant, which...

Claims

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Application Information

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IPC IPC(8): C07F9/6558C07C215/10C07C213/08A61K31/675A61P35/00A61K9/19
CPCC07F9/65583A61K9/0019A61K9/19
Inventor 李俊广李公存孙运贝
Owner SHANDONG YUXIN PHARMA CO LTD
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