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A kind of prasugrel hydrochloride compound

A technology for prasugrel hydrochloride and a composition, which is applied in the field of medical research and can solve the problems of increased bleeding risk and the like

Active Publication Date: 2019-03-26
SICHUAN HAISCO PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Through the observation of healthy volunteers and its application in stable angina pectoris and acute coronary syndrome interventional surgery, it is found that it has faster, stronger and longer-lasting anti-platelet effect than clopidogrel, and can significantly reduce the incidence of ischemic events , but increased risk of bleeding

Method used

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  • A kind of prasugrel hydrochloride compound
  • A kind of prasugrel hydrochloride compound
  • A kind of prasugrel hydrochloride compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Example 1 - Preparation of Prasugrel Hydrochloride

[0021] 2.2 kg of prasugrel free base and 7.7 liters of ethyl acetate were added to the reaction kettle, heated to about 50° C. with stirring, and the solution was clarified. Stop heating, slowly stir and cool down to 25±5°C, keep stirring for 1 h, and filter with suction. The filter cake was slurried with ether / ethanol (0.5 liter / 1 liter), rinsed with ethanol for 2L×2 times, and drained, and the wet weight was about 1.6 kg. After vacuum drying at 45±5℃ for more than 12 hours, about 1.3 kg of prasugrel free base fine products are obtained.

[0022] Take another reactor, add 1.20 kilograms of the above-obtained prasugrel free base fine products and 12 liters of acetone (weight ratio) containing 10% β-pinene, and heat up to about 30° C. to stir and dissolve. Suction filtration, the filter paper is rinsed with 2L of acetone (weight ratio) containing 10% β-pinene, the filtrates are combined and poured into a clean reacti...

experiment example 1

[0025] Experimental Example 1 - Raw Material Metabolism and Efficacy

[0026] Experimental animals: 32 male Wistar rats, weighing 200-230 g, were purchased from Sichuan University.

[0027] Experimental method: Rats were randomly divided into 4 groups, with 8 rats in each group. They were reared under normal conditions and had free access to water. After 12 hours of fasting, each group was given Prasugrel hydrochloride (Example 1) with a solid gavage device, respectively, at a dose of 25 , 50, 100 and 150 mg kg -1 . Blood collection time points: 300 blood samples were collected from the retroocular venous plexus before administration and at 5, 15, 30 minutes and 1, 2, 3, 4, 6, 8, 10, 12, 24, 36, and 48 hours after administration. -500 microliters in heparinized Ep tubes.

[0028] Sample processing method: Heparin anticoagulated venous blood was centrifuged at 5000 r / min for 10 minutes at room temperature, 100 μl of plasma was taken, 1300 μl of ethyl acetate was added, vorte...

experiment example 2

[0030] Experimental Example 2 - Stability Investigation of Raw Materials

[0031] The present invention carried out the 6-month accelerated test (40°C±2°C, 75%±5%RH) and the 6-month long-term test (30°C±2°C, 65%±5%RH) of Example 1. For Example 1, the long-term test stability investigation will continue, and the investigation indicators include properties, specific rotation, acid value, moisture, related substances, chlorine content and content.

[0032]

[0033]

[0034] .accelerated test

[0035] Packing: packed in medicinal low-density polyethylene bag, and then covered with aluminum-plastic composite film bag after adding desiccant

[0036] Inspection conditions: 40℃±2℃, 75%±5%RH

[0037] Table-3 Prasugrel hydrochloride accelerated test results (40℃±2℃, 75%±5%RH)

[0038]

[0039] .Long term test

[0040] Table-4 Prasugrel hydrochloride long-term test results (30℃±2℃, 60%±5%RH)

[0041]

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Abstract

The present invention belongs to the technical field of medicines, and in particular relates to a prasugrel hydrochloride compound. Prasugrel is a new generation of potent thianthrene-pyridine antiplatelet drug. By observing on healthy volunteers and application in stable angina pectoris and acute coronary syndrome interventional operations, faster and stronger and more durable antiplatelet effect of the prasugrel hydrochloride compound, compared with that of clopidogrel, is found, the incidence of ischemic events can be significantly reduced, but the risk of bleeding is increased. In clinical use, more attention must be paid for identification of thrombosis high-risk patients and high-bleeding-risk groups.

Description

technical field [0001] The invention belongs to the field of medical research, in particular to a prasugrel hydrochloride compound. Background technique [0002] In February 2009, the European Commission approved a new oral antiplatelet drug, prasugrel, jointly developed by Daiichi-Sankyo and EliLilly, for the prevention of patients who have received emergency and will undergo delayed percutaneous coronary intervention. Atherothrombosis events in patients with acute coronary syndrome. This is the first time Prasugrel has been approved globally. [0003] Prasugrel is a new orally effective thienopyridine drug. Like clopidogrel, prasugrel is also an inactive prodrug, which can irreversibly inhibit the P2Y12 adenosine diphosphate receptor on platelets after being metabolized by cytochrome P450 enzymes to active metabolites. Prasugrel is more effective than clopidogrel, which can be explained by its improved pharmacokinetic properties: Prasugrel has a higher conversion rate o...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D495/04A61K31/4365A61P9/00A61P7/02
Inventor 林凡程汪东海万华范俊迈冯卫任东
Owner SICHUAN HAISCO PHARMA CO LTD
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