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Application of biphenylacetic acid or salt thereof to preparation of Xa inhibitor medicament

A kind of technology of felbinac ammonium salt and felbinac manganese salt, applied in the field of new use of felbinac, can solve the problems such as reports of felbinac that have not been found yet, and achieve the effect of preventing cerebral infarction

Inactive Publication Date: 2019-04-05
SHIJIAZHUANG YILING PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Felbinac and its salts have not been found so far as inhibitors of blood coagulation factor Xa

Method used

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  • Application of biphenylacetic acid or salt thereof to preparation of Xa inhibitor medicament
  • Application of biphenylacetic acid or salt thereof to preparation of Xa inhibitor medicament
  • Application of biphenylacetic acid or salt thereof to preparation of Xa inhibitor medicament

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Embodiment 1: felbinac dry suspension

[0041] Preparation formula: 30 grams of felbinac, 670 grams of sucrose powder, 20 grams of sodium alginate, 3 grams of stevia, 15 grams of hydroxypropyl cellulose, 3 grams of sodium lauryl sulfate, 0.1 grams of sunset yellow, carboxymethyl Sodium starch starch 15 grams.

[0042] Preparation:

[0043] 1. Prepare each component according to the formulation of the preparation and crush it;

[0044] 2. Take 1 gram of steviol, 0.05 gram of sunset yellow, 3 grams of sodium lauryl sulfate, 30 grams of felbinac, and 500 grams of sucrose powder, mix them in equal increments, and granulate with 25ml of 20% ethanol aqueous solution , to obtain loose granules and powders that form into agglomerates when held by hand, loose by hand, and have rough edges, which is part A, with a total of 548 grams;

[0045] 3. Take the remaining 2 grams of stevia, 0.05 grams of sunset yellow, 170 grams of sucrose powder, 15 grams of hydroxypropyl cellulose, 15...

Embodiment 2

[0048] Embodiment 2: Felbinac tromethamine salt injection

[0049] Raw materials: 12.0 g of felbinac tromethamine salt, 1000 ml of water for injection, anhydrous sodium carbonate solution, and adjust the pH value to 8.2.

[0050] Preparation:

[0051] Take by weighing 12.0g of felbinac tromethamine salt, add 1000ml of cooled water for injection, dissolve in an appropriate amount of 0.1mol / L anhydrous sodium carbonate solution, add 0.1% activated carbon for needles (ie 0.8g) according to the total amount prepared , keep stirring at 60°C for 15 minutes, filter and decarburize, cool to room temperature, add cooled water for injection, adjust the pH value to 8.2, stir evenly, filter through a 0.22 μm microporous membrane, and seal in a 5ml vial. Each bottle was filled with 4ml, sealed, and sterilized by autoclaving at 121°C for 15 minutes to obtain a total of 232 finished products.

Embodiment 3

[0052] Embodiment 3 felbinac magnesium salt tablet

[0053] Raw materials: magnesium felbinac 50g, sodium carboxymethyl starch 9g, microcrystalline cellulose 22.5g, lactose 115.5g, povidone K 30 1.5g, micropowder silica gel 1.5g.

[0054] Preparation:

[0055] Weigh 50g of magnesium felbinac, 9.0g of sodium carboxymethyl starch, 22.5g of microcrystalline cellulose, 115.5g of lactose, and povidone K that were crushed through a 200-mesh sieve. 30 1.5g, micropowder silica gel 1.5g, fully mix magnesium felbinac, sodium carboxymethyl starch, microcrystalline cellulose, lactose, and mix povidone K 30 Dissolve it in 30ml of pure water as a binder to make a soft material, granulate it with a 18-mesh sieve, and dry it at 60°C. The dry granules pass through a 16-mesh sieve for granulation, add micropowder silica gel and mix well, and adjust the tablet weight to 200 mg / Tablets can be obtained by pressing tablets, and a total of 957 finished products are made.

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Abstract

The invention relates to application of biphenylacetic acid or a salt thereof to preparation of an Xa inhibitor medicament, and belongs to the technical field of new application of the biphenylaceticacid. The biphenylacetic acid or the salt thereof can be combined with pharmaceutically-acceptable auxiliary materials to prepare a medicament. The biphenylacetic acid and the salt thereof contain a coagulation factor Xa inhibitor, and can effectively treat or prevent cerebral infarction, cerebral embolism, myocardial infarction, stenocardia, pulmonary infarction, pulmonary embolism, Buerger's disease, severe phlebothrombosis, disseminated intravascular coagulation syndrome, thrombopoiesis after valve replacement or joint replacement, thrombogenesis and reclosure of revascularization, system inflammatory response complex disease, multiorgan dysfunction complex disease, and thrombogenesis during extracorporeal circulation.

Description

technical field [0001] The invention belongs to the technical field of new applications of felbinac and relates to the application of felbinac or its salts in the preparation of blood coagulation factor Xa inhibitor drugs. Experiments have shown that felbinac and its salts have a significant selective inhibitory effect on blood coagulation factor Xa, and can be used clinically to treat or prevent cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary infarction, pulmonary embolism, Berger's disease, Severe venous thrombosis, disseminated intravascular coagulation syndrome, thrombosis after valve replacement or joint replacement, thrombosis and reclosure of angioplasty, complications of systemic inflammatory response, complications of multiple organ dysfunction, cardiopulmonary bypass period of thrombosis. Background technique [0002] Felbinac has been used as a non-steroidal anti-inflammatory drug for decades. For example, CN1073094A disc...

Claims

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Application Information

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IPC IPC(8): A61K31/192A61K31/205A61K9/14A61K9/08A61K9/48A61P7/02A61P9/10A61P11/00A61P9/14
CPCA61K9/0019A61K9/08A61K9/146A61K9/4866A61K31/192A61K31/205A61P7/02A61P9/10A61P9/14A61P11/00
Inventor 葛兰王超周梦夏王猛王永刘翠
Owner SHIJIAZHUANG YILING PHARMA
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