Prasugrel eutectic and preparation method, medicinal composition and application thereof

A drug and forming technology, applied in the field of prasugrel co-crystal and its preparation, can solve the problems of not being able to cover up the benefits of ischemic events, affect anti-platelet therapy, increase the risk of bleeding, etc., to facilitate preparation and storage, and overcome bleeding Risky, easy-to-handle effects

Inactive Publication Date: 2012-08-01
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is also a downside in the prasugrel study, namely that it significantly increased the risk of bleeding, including fatal bleeding, at the cost of stronger platelet inhibitors
In addition, increased bleeding can affect antiplatelet therapy, and discontinuation of antiplatelet therapy itself can increase ischemic events
Although the application of prasugrel increases the risk of bleeding, it cannot cover the benefits of reducing ischemic events

Method used

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  • Prasugrel eutectic and preparation method, medicinal composition and application thereof
  • Prasugrel eutectic and preparation method, medicinal composition and application thereof
  • Prasugrel eutectic and preparation method, medicinal composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Embodiment 1: Preparation of prasugrel co-crystal

[0042] Mix 187 mg of prasugrel and 55 mg of p-hydroxybenzoic acid with 2 ml of acetone, vortex or sonicate to dissolve and form a clear solution, let it stand at room temperature and slowly evaporate until the solvent is completely evaporated, and then dry it under reduced pressure with an oil pump for 12 hours , to obtain the prasugrel cocrystal.

Embodiment 2

[0043] Embodiment 2: Preparation of prasugrel co-crystal

[0044] Mix 187 mg of prasugrel and 55 mg of p-hydroxybenzoic acid with 2 ml of acetonitrile, vortex or sonicate it to dissolve to form a clear solution, let it stand at room temperature and slowly evaporate until the solvent is completely evaporated, and then dry it under reduced pressure with an oil pump for 12 hours , to obtain the prasugrel cocrystal.

Embodiment 3

[0045] Embodiment 3: the preparation of prasugrel co-crystal

[0046] Add 747 mg of prasugrel and 276 mg of p-hydroxybenzoic acid into a 5 ml ball mill jar, then add 0.2 ml of pure water, grind with a ball mill at room temperature for 60 minutes, and stand at room temperature until the water is completely evaporated Dry, and then use an oil pump to dry under reduced pressure for 12 hours to obtain the prasugrel eutectic.

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PUM

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Abstract

The invention provides a prasugrel eutectic with a structure shown in the specification, and a preparation method, a medicinal composition and application thereof. The prasugrel eutectic does not contain a solvent and is low in hygroscopicity, so that the preparation and storage of Chinese herbal medicines are facilitated. Experiments for testing dissolubility prove that the prasugrel eutectic is relatively low in dissolution speed, so the prasugrel eutectic can be used as a sustained-release agent for prasugrel medicines to overcome the defect of increasing hemorrhagic risks. In addition, the method for preparing the prasugrel eutectic is simple, and easy to operate.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to prasugrel co-crystal and its preparation method, pharmaceutical composition and application. Background technique [0002] Pharmaceutical co-crystal refers to the crystal formed by the combination of active pharmaceutical ingredient (active pharmaceutical ingredient, API) and cocrystal former (cocrystal former, CCF) in a fixed stoichiometric ratio under the action of hydrogen bonds or other non-covalent bonds. , both API and CCF are solid at room temperature. A co-crystal is a multi-component crystal, including both a binary co-crystal formed between two neutral solids and a multi-element co-crystal formed between a neutral solid and a salt or solvate. Different solid forms of the same drug often have different physical and chemical properties, efficacy and preparation process. Common solid forms such as solvates and salts are limited in application due to the sma...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D495/04C07C65/03C07C51/41A61K31/4365A61P9/04A61P9/10A61P25/00
Inventor 梅雪锋张奇
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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