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
CN106565783AInactive Publication Date: 2017-04-19SHANDONG YUXIN PHARMA CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
SHANDONG YUXIN PHARMA CO LTD
Publication Date
2017-04-19
Estimated Expiration
Not applicable · inactive patent

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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.
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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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