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Ticagrelor sesquihydrate and preparation method thereof

A technology of sesquihydrate and ticagrelor, which is applied in the field of medicine, can solve the problems of moisture absorption, weight gain, difficult purification, and high impurity content

Active Publication Date: 2014-06-11
TIANJIN HANKANG PHARMA BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Ticagrelor 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 ticagrelor

Method used

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  • Ticagrelor sesquihydrate and preparation method thereof
  • Ticagrelor sesquihydrate and preparation method thereof
  • Ticagrelor sesquihydrate and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] In a 10L reaction kettle equipped with stirring, thermometer and condenser, add 250g of ticagrelor, 910.0ml of n-butanol, 10.5ml of piperidine, and 970.0ml of water, start stirring, heat until dissolved, and cool the filtrate naturally to 25°C -30°C, then let it stand for 3.5 hours, precipitated crystals, filtered, and dried indoors to obtain 234.6 grams of white crystals of ticagrelor sesquihydrate, with a melting point of 220.3°C-223.9°C and a content of 99.86%. A single impurity is less than 0.06%. As determined by the Karl Fischer method, it contains 4.91% (weight percent) of water.

[0051] Microparticles or microspheres are prepared by combining the compounds of the present invention with a pharmaceutically acceptable solid or liquid carrier, and optionally with pharmaceutically acceptable adjuvants and vehicles, using standard and conventional techniques. The composition is used for preparing oral preparations and injections. It is given by way of example only ...

Embodiment 2

[0053] Tablets containing ticagrelor sesquihydrate

[0054] Prescription: ticagrelor sesquihydrate 100g, microcrystalline cellulose 10g, pregelatinized starch 15.4g, sodium starch glycolate 4.4g, lactose 150g, PEG-4000 20g, magnesium stearate 4g, 29 gram of povidone K30, 30 grams of croscarmellose sodium, appropriate amount of distilled water, made into 1000 tablets.

[0055] Process:

[0056] Preparation of tablet core: according to the determined prescription, the main ingredient and auxiliary materials are mixed uniformly, granulated, and the granules are ventilated and dried below 40°C, granulated with a 16 mesh sieve, added magnesium stearate and remaining starch, and compressed into tablets to obtain final product .

[0057] Isolation layer coating: add talcum powder to 5% polyvinylpyrrolidone (PVP) absolute ethanol solution, stir evenly, and prepare a 20% suspension as the isolation layer coating solution. Coating is carried out in a fluidized bed, and the process co...

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Abstract

The invention belongs to the technical field of medicines and specifically relates to a ticagrelor sesquihydrate and a preparation method thereof. The ticagrelor sesquihydrate disclosed by the invention contains semi-crystalline water and has the advantages that the purity is high; the stability is good, and the moisture absorption weight gain is not obvious even under high-humidity conditions; the inhibition effect against platelet aggregation of the ticagrelor sesquihydrate is improved by nearly 20%. The invention further relates to an application of a composition of the hydrate in treatment of cardiovascular and cerebrovascular diseases.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to ticagrelor sesquihydrate and a preparation method thereof, and also relates to the application of the hydrate composition in treating diseases of the cardiovascular and cerebrovascular systems. Background technique [0002] History of vascular disease is a systemic disease with different clinical manifestations due to the different sites of thrombosis, and the occurrence of vascular events in one vessel means that the risk of vascular events in other vessels increases. According to statistics, the death caused by atherosclerotic thrombosis accounts for 28.7% of the total death of the population, mainly due to coronary artery events and cerebral artery events, followed by other peripheral arterial diseases, and two or even three vascular lesions may coexist . The pathological basis of vascular events is atherosclerosis, and the first step in pathophysiology is platel...

Claims

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Application Information

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IPC IPC(8): C07D487/04A61K31/519A61P9/10
CPCC07D487/04
Inventor 严洁李轩
Owner TIANJIN HANKANG PHARMA BIOTECH
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