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Stable telaprevir compound

A technology of telaprevir and its compound, which is applied in the application field of telaprevir compound and its preparation, and the treatment of hepatitis C, and can solve the problems of high total amount of impurities, large number of telaprevir impurities, etc.

Inactive Publication Date: 2016-06-08
TIANJIN HANKANG PHARMA BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Telaprevir has a great advantage in effectiveness, but in the course of the research, by repeating the method recorded in the existing literature, the number of impurities in telaprevir is more, and the total amount of impurities is higher

Method used

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  • Stable telaprevir compound
  • Stable telaprevir compound
  • Stable telaprevir compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] In a 3000ml reaction bottle equipped with stirring, thermometer and condenser, add 300g of telaprevir and 2700ml of acetone-water (2:4.5) mixture, start stirring, heat up to 75°C, and wait for all to dissolve. Strain while hot. Cool down to 35°C and keep warm for 3 hours; then, cool down to 25°C and keep warm for 4 hours to precipitate crystals, filter, and dry to obtain 276.1 g of high-purity telaprevir compound crystals with an optical purity of 99.88%. The detection of solvent residues meets the requirements.

[0034] Microparticles or microspheres are prepared by combining the compounds of the 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 the preparation of oral preparations. It is given by way of example only and in no way is it intended to limit the scope of the invention in any way.

Embodiment 2

[0036] Tablets containing telaprevir compound

[0037] Prescription: 375 grams of telaprevir compound, 50 grams of lactose, 260 grams of microcrystalline cellulose, 50 grams of sodium carboxymethyl starch, 5 grams of magnesium stearate, appropriate amount of distilled water, made into 1000 tablets.

[0038] Process: Pulverize the telaprevir compound, pass through a 60-mesh sieve, mix with other materials, use distilled water to make a soft material, granulate with a 16-mesh sieve, dry in a drying oven at 40-45°C, add magnesium stearate to the dry granules Mix well and press into tablets.

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PUM

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Abstract

The invention belongs to the technical field of medicines, and specifically relates to a telaprevir compound and a preparation method thereof. The telaprevir compound provided by the invention has the following advantages: high purity, good stability, and inconspicuous moisture absorption and weight increase under a condition of high humidity.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a telaprevir compound and a preparation method thereof. The invention also relates to a composition using the compound and an application of the composition using the compound to treat hepatitis C. Background technique [0002] Telaprevir (VX-950) is a new drug developed by Vertex Pharmaceuticals of the United States for the treatment of hepatitis C. It was approved by the FDA on May 23, 2011, and its trade name is Incivek. The drug is an oral tablet, which is a reversible protease inhibitor, used in combination with pegylated α-interferon and ribavirin, can effectively inhibit the replication of HVC virus, and is used for chronic hepatitis C. It has a good clinical application prospect. [0003] Its structural formula is: [0004] [0005] Telaprevir has a great advantage in effectiveness, but during the research process, repeating the method recorded in the exi...

Claims

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Application Information

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IPC IPC(8): C07K7/06C07K1/30A61P31/14
Inventor 严洁李轩
Owner TIANJIN HANKANG PHARMA BIOTECH
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