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Diisopropylamine fenofibrate, preparation method of same, medicinal composition and use of same

A technology of acid diisopropylamine salt and fenofibrate acid, which is applied in the field of fenofibrate acid diisopropylamine salt and can solve problems such as toxic and side effects, poor water solubility and the like

Inactive Publication Date: 2010-09-08
曹桂英
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] An object of the present invention is to provide a kind of fenofibric acid diisopropylamine salt, its preparation method, pharmaceutical composition and its purpose

Method used

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  • Diisopropylamine fenofibrate, preparation method of same, medicinal composition and use of same
  • Diisopropylamine fenofibrate, preparation method of same, medicinal composition and use of same
  • Diisopropylamine fenofibrate, preparation method of same, medicinal composition and use of same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Preparation of fenofibric acid diisopropylamine salt:

[0036] Dissolve 31.8g of fenofibric acid in 150mL of ether, add 10.1g of diisopropylamine, reflux for 30min, cool to 15°C, a large amount of white solid is formed, suction filtered, the solid is washed once with 30mL of ether, and dried in vacuum (-0.1 MPa, 45°C, 3-5 hours), weighed 30.8g, yield 96.55%. 1HNMR(CDCl 3 )δ: 9.09 (br s, 2H), 7.74-7.76 (dt, 2H), 7.70-7.72 (dt, 2H), 7.44-7.46 (dt, 2H), 6.93-6.95 (dt, 2H), 3.37-3.40 (m, 2H), 1.7 (s, 6H), 1.46-1.48 (d, 12H). MS: 317, 102; elemental analysis, theoretical value: C 65.78%, H 7.20%, Cl 8.44%, N 3.34%; measured value of C 65.76%, H 7.22%, Cl 8.43%, N 3.33%.

Embodiment 2

[0038] Preparation of fenofibrate sodium:

[0039] Suspend 31.8g of fenofibric acid in 200mL of 0.5mol / L sodium hydroxide solution, raise the temperature to 50℃, stir for 30min, until all fenofibric acid is dissolved, add 50mL of ethanol, cool, and precipitate a white solid, water pump Vacuum filtration, vacuum drying (-0.1MPa, 45°C, 3-5 hours), weigh 31.6g, yield 92.75%. 1HNMR(D 2 O) δ: 7.74-7.76 (dt, 2H), 7.70-7.72 (dt, 2H), 7.44-7.46 (dt, 2H), 6.93-6.95 (dt, 2H), 1.7 (s, 6H). MS: 317; elemental analysis, theoretical value: C 59.93%, H 4.14%, Cl 10.40%; measured value of C 59.90%, H 4.16%, Cl 10.43%.

Embodiment 3

[0041] Preparation of fenofibric acid diisopropylamine salt composition tablet

[0042] Take the following raw materials, each serving 100 grams.

[0043] 100 parts of fenofibric acid diisopropylamine salt

[0044] Mannitol 60 parts

[0045] 100 servings of lactose

[0046] 50 parts starch

[0047] Sodium Carboxymethyl Starch 5 parts

[0048] 5 servings of talcum powder

[0049] Povidone 3 parts

[0050] After passing the above-mentioned raw materials through a 100-mesh sieve respectively, they are mixed uniformly according to the equal-volume progressive addition method, and directly compressed into 1000 tablets. The obtained tablet swells rapidly and disintegrates and disperses in water and 0.1 mol / L hydrochloric acid solution.

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Abstract

The invention discloses a diisopropylamine fenofibrate, a preparation method of the same, a medicinal composition and use of the same, relating to the field of medicaments for lowering blood fat and treating fatty liver. The problems that fenofibric acid products is poor in water solubility, has toxic and side effects and the like in the prior art are solved. A product of the invention is obtained through the following steps of: adding a fenofibric acid and diisopropylamine into a solvent, heating to 35-70 DEG C, cooling, separating out a solid, pumping a filtrate, washing the solid with ether, and drying to obtain a white solid which is the diisopropylamine fenofibrate. A diisopropylamine part in the invention can overcome the side effect that the fenofibric acid is heated to be converted into ammonia enzyme and blood sugar and exerts a synergetic effect of lowering the blood fat together with fenofibrate.

Description

Technical field [0001] The invention relates to a fenofibric acid diisopropylamine salt, a preparation method, a pharmaceutical composition and use thereof, and relates to the field of medicines for reducing blood lipids and treating fatty liver. Background technique [0002] Hyperlipidemia is a serious disease threatening human health. High blood lipids include: high cholesterol, high triglycerides, and high low-density lipids. These three types of high blood lipids are harmful to health. For example, they directly affect arteriosclerosis, which causes a series of clinically most common diseases, such as Coronary heart disease, angina pectoris, myocardial infarction, etc. Arteriosclerosis can also induce hypertension. After arteriosclerosis, high blood pressure rises even higher. After high blood pressure, there are cerebrovascular accidents and kidney changes, which are a series of problems. [0003] Fenofibrate is recommended for the treatment of endogenous hyperlipidemia, hy...

Claims

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Application Information

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IPC IPC(8): C07C59/90C07C51/41C07C211/06A61K31/205A61K31/192A61K31/4418A61P3/06A61P1/16A61P3/10
Inventor 刘葵花
Owner 曹桂英
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