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Anticoagulant immediate-release pharmaceutical preparation and preparation method thereof

A technology for pharmaceutical preparations and anticoagulants, which is applied in the field of medicine, can solve the problems such as the prescription process report of a single active ingredient preparation without vecagrel, and achieve high in vivo bioavailability and blood drug concentration, large drug absorption degree, and stability. excellent effect

Active Publication Date: 2018-08-21
JIANGSU VCARE PHARMATECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Patent CN103254211B has disclosed the preparation method of vicagrell and its derivatives, and patent CN103720700A has disclosed the composition of vicagrell and aspirin, which is used to prevent or treat diseases caused by thrombus, but at present, there is no single activity against vicagrell. Report on the formulation process of ingredients and preparations

Method used

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  • Anticoagulant immediate-release pharmaceutical preparation and preparation method thereof
  • Anticoagulant immediate-release pharmaceutical preparation and preparation method thereof
  • Anticoagulant immediate-release pharmaceutical preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Embodiment 1 vicagrel capsule

[0059]

[0060]

[0061] Vicagrelor was pulverized with a hammer mill (Frewitt) with a 0.20 mm screen, a rotating speed of 6000 rpm, and a feed rate of 1 kg / min, and the measured D90 = 43 μm. Mix the pulverized vicagrel with microcrystalline cellulose and lactose in a three-dimensional mixer for 15 minutes, add hydrogenated castor oil and mix, and fill the obtained granules into No. 3 capsules.

Embodiment 2

[0062] Embodiment 2 vicagrel capsules

[0063] Raw materials

[0064] Use QL-100 jet mill to pulverize the raw material, the pressure is 0.8MPa, the working temperature is 15°C, the pulverization time is 10min, D90=9μm. Mix the pulverized vicagrelor hydrochloride with microcrystalline cellulose, lactose, sodium carboxymethyl starch, and hydroxypropyl methylcellulose in a three-dimensional mixer at 35 rpm for 10 minutes, take it out and put it in a high-shear wet granulator, and stir at 500 rpm , cutting at 1000rpm and adding water to granulate, passing through a 16-mesh sieve for granulation, drying in a blast drying oven at 60°C, taking it out, passing through a 24-mesh sieve for granulation, adding magnesium stearate and blending. The drug-containing granules are filled into No. 3 capsules to obtain the vicagrel immediate-release capsules.

Embodiment 3

[0065] Embodiment 3 Vicarrel capsules

[0066]

[0067]

[0068] Put the pulverized vicagrel salt, pregelatinized starch, lactose, and sodium carboxymethyl starch in a fluidized bed, start the fluidized mixing for 10 minutes, and prepare 5% hydroxypropyl methylcellulose as a binder. The air inlet temperature is 80°C, and the binder is sprayed while maintaining the bed temperature at 40-50°C. After forming particles, maintain the bed temperature at 50-60°C and dry for 30 minutes. After discharging, add sodium stearyl fumarate and mix for 5 minutes. Capsules.

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Abstract

The invention relates to an anticoagulant immediate-release pharmaceutical preparation and a preparation method thereof, and belongs to the technical field of medicine, wherein the anticoagulant immediate-release pharmaceutical preparation contains a vicagrel compound or a pharmaceutically acceptable form thereof, wherein the preparation is in the form of tablets or capsules, the vicagrel or the pharmaceutically acceptable form has a suitable particle size, and the D90 is less than 50 [mu]m. According to the present invention, the in vitro dissolution test results of the pharmaceutical preparation formed by the drug-containing granules of the present invention show that the rapid release characteristic is provided, the considerable advantage is provided in pharmacokinetics in vivo, and thehigh area under the cure (AUC) and the rate (Cmax) are provided. The present invention further provides a preparation method of the anticoagulant immediate-release pharmaceutical preparation, whereinthe excellent-stability immediate-release preparation capsule or tablet can be obtained through the optional preparation step combination according to the drug-containing granule formula of the present invention.

Description

technical field [0001] The invention provides immediate-release pharmaceutical preparations, specifically including immediate-release tablets or capsules containing anticoagulant vicargrel and its acceptable salt carrier. The invention also provides a preparation method for the immediate-release pharmaceutical preparations, which belongs to the field of medical technology . Background technique [0002] Vicagrel is a new type of anti-platelet aggregation drug, which can be used to overcome the clinical application defects of existing anti-platelet drugs, such as "clopidogrel resistance" and high bleeding risk of prasugrel. Vicagrel has entered the clinical research stage and is expected to be developed into a safer and more effective new anti-platelet drug. [0003] Patent CN103254211B has disclosed the preparation method of vicagrell and its derivatives, and patent CN103720700A has disclosed the composition of vicagrell and aspirin, which is used to prevent or treat diseas...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K9/36A61K9/48A61K47/38A61K47/26A61K47/36A61K31/4365A61P7/02
CPCA61K9/1652A61K9/2866A61K31/4365A61K9/2013A61K9/2036A61K9/2077A61P7/02
Inventor 赵焱磊张建军刘雪芳高缘孙宏斌龚彦春刘永强
Owner JIANGSU VCARE PHARMATECH
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