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Cangrelor monohydrate crystal and preparation method thereof

A monohydrate and crystal technology, applied in the field of medicine, can solve the problems of high impurity content, moisture absorption and weight gain, difficulty in purification, etc.

Inactive Publication Date: 2015-03-25
TIANJIN HANKANG PHARMA BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Cangrelor has great advantages in effectiveness and safety, but in the actual production process, the applicant found that there are problems such as difficult purification, high impurity content and certain moisture absorption and weight gain in the preparation process of cangrelor

Method used

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  • Cangrelor monohydrate crystal and preparation method thereof
  • Cangrelor monohydrate crystal and preparation method thereof
  • Cangrelor monohydrate crystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] In a 1L reaction flask equipped with stirring, thermometer, and condenser, add 50 g of cangrelor, 300 ml of water, and 1.2 ml of dichloromethane, stir for 30 minutes, filter, and cool the filtrate to 8°C for later use.

[0046] Cool 350ml of ethyl acetate mixed solution to 8°C, add it into the above standby solution with stirring, keep it warm for 15 hours, crystals precipitate out, filter and dry to obtain 52.5 grams of white crystals. Measured 3 times by Karl Fischer method, take the average value, containing 2.25% (weight ratio) of water. Purity 99.9% (HPLC normalization method), optical purity 99.97ee (chiral HPLC).

Embodiment 2

[0048] Injections containing cangrelor monohydrate

[0049] Prescription: cangrelor monohydrate 2.5% by weight, mannitol 13.2%, lactose 18.4%, water for injection 65.7%, made into 1000 sticks.

[0050] Process: Take cangrelor monohydrate, mannose, lactose, and water for injection and stir to dissolve, then add 5g of activated carbon, stir at room temperature for 10 minutes, filter out the activated carbon, use microporous membrane to filter and sterilize, and pack the filtrate into 1000 tubes. After pre-freeze-drying for 3 hours, freeze-dry under reduced pressure for 20 hours, then warm up to room temperature, and seal it.

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PUM

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Abstract

Belonging to the field of medical technologies, the invention in particular relates to a cangrelor monohydrate crystal and a preparation method thereof. The cangrelor monohydrate obtained by the invention has the advantage of: high purity and good stability, unobvious moisture absorption weight gain even under a high humidity condition. The invention also relates to application of compositions using the hydrate to treatment of cardiovascular and cerebrovascular system diseases.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to cangrelor monohydrate and a preparation method thereof, and also relates to the application of the composition of the compound in treating diseases of the cardiovascular and cerebrovascular systems. Background technique [0002] Vascular disease is a systemic disease. The clinical manifestations are different due to the different sites of thrombosis. A vascular event occurs in one vessel, which means that the risk of vascular events in other vessels increases. The pathological basis of vascular events is atherosclerosis. [0003] Atherosclerosis is a series of pathophysiological processes. Early lesions of atherosclerosis, that is, lipid streaks, can appear in preschool children. With age and risk factors, plaques gradually form, and the plaques become more and more serious. Large, there may be no clinical manifestations in the early stage. When the blood vessels ar...

Claims

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Application Information

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IPC IPC(8): C07H19/20C07H1/06A61K31/7076A61P9/10
CPCC07H19/20C07B2200/13C07H1/06
Inventor 严洁李轩
Owner TIANJIN HANKANG PHARMA BIOTECH
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