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Choline salt of hypolipidemic drug and preparation method and pharmaceutical use thereof

A technology of blood lipid-lowering drugs and choline salts, which is applied in the field of medicine, can solve problems affecting bioavailability, and achieve the effects of preventing abnormal fat accumulation, improving water solubility, and enhancing drug efficacy

Inactive Publication Date: 2010-10-20
北京利乐生制药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are certain defects in these drugs themselves, such as fenofibrate, because it is almost insoluble in water, only special pharmaceutical preparations are made to ensure good bioavailability, but due to the insolubility of fenofibrate in water, the preparation releases There is a tendency to recrystallize during the process, affecting bioavailability

Method used

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  • Choline salt of hypolipidemic drug and preparation method and pharmaceutical use thereof
  • Choline salt of hypolipidemic drug and preparation method and pharmaceutical use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0011] The preparation of embodiment 1 fenofibrate choline salt (I1)

[0012] Take 3.6g of fenofibrate, add 75ml of acetone to dissolve it, add 0.6g of sodium hydroxide-25ml of aqueous solution, heat and hydrolyze at 40°C, and monitor the reaction by TLC until the reaction is complete. Concentrate to remove acetone, add 25ml of water to the residue, filter, adjust the pH of the filtrate to 4 with dilute hydrochloric acid, filter, wash with water, and dry in vacuo at 45°C to obtain 2.9 g of a yellowish solid, namely fenofibric acid.

[0013] Suspend the fenofibric acid obtained above in 30ml of methanol, add 4.4g of 25% methanol solution of choline, and quickly dissolve into a light yellow transparent solution, add 60ml of ether, stir until a large amount of solids are precipitated, filter, wash with ether, After vacuum drying at 45°C, 3.2 g of white needle-like crystals were obtained. 1 H-NMR (water): 1.53 (S, 6H, N-CH3), 3.12 (S, 9H, C-CH3), 3.42-3.44 (m, 2H, CH2), 3.96-3.99...

Embodiment 2

[0014] The preparation of embodiment 2 ciprofibrate choline salt (I2)

[0015] Suspend 2.9g of ciprofibrate in 30ml of methanol, add 4.8g of 25% choline in methanol, and quickly dissolve into a light yellow transparent solution, add 60ml of diethyl ether, stir until a large amount of solids are precipitated, filter, wash with diethyl ether, 45°C After vacuum drying, 3.3 g of white solid was obtained. ESI-MS: 415.2 (M+Na + ). Elemental analysis: C (55.11%), H (6.94%), N (3.57%); calculated values: C (55.34%), H (6.82%), N (3.41%).

Embodiment 3

[0016] The preparation of embodiment 3 gemfibrozil choline salt (I3)

[0017] Referring to the method of Example 2, gemfibrozil was used instead of ciprofibrate to prepare I3 with a yield of 82%. ESI-MS: 376.7 (M+Na + ). Elemental analysis: C (67.95%), H (9.98%), N (3.96%); calculated values: C (68.22%), H (9.86%), N (3.84%).

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Abstract

The invention relates to a choline salt of a hypolipidemic drug and a preparation method and a pharmaceutical use thereof. The invention provides a choline salt of a class of hypolipidemic drugs, and the hypolipidemic drugs include but not limited to clofibrate, libet, fenofibrate, ciprofibrate, gemfibrozil, acipimox, niacin, lovastatin, simvastatin, pravastatin, fluvastatin, atorvastatin, rosuvastatin, pitavastatin, eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) and other unsaturated fatty acids. The choline salt of the hypolipidemic drug can be used for treating hyperlipidemia and other cardiovascular diseases. The invention also provides a preparation method of the choline salt of the hypolipidemic drug.

Description

technical field [0001] The invention relates to a blood lipid-lowering drug choline salt, a preparation method and a medical application thereof, and belongs to the technical field of medicine. technical background [0002] Choline is a strong organic base, β-hydroxyethyltrimethylammonia hydroxide. Choline is an important part of lecithin and has many physiological functions: it plays a key role in the formation of cholinergic neurons and synapses in the memory area of ​​the brain, so it can promote brain development and improve memory ability; phosphatidic acid choline and nerve Sphingomyelin can amplify external signals and mediate information transmission; choline is an important component of biomembrane to ensure membrane function; choline can also promote fat metabolism and prevent abnormal accumulation of fat; choline can regulate cell apoptosis and inhibit cancer Cell proliferation can also promote methyl metabolism in the body; choline and phospholipids have good em...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C215/40C07C69/708C07C59/72C07C59/68C07D241/24C07D215/14C07C57/03A61K31/14A61K31/216A61K31/192A61K31/4965A61K31/47A61K31/557A61K31/202A61P3/06A61P9/00
Inventor 姚勇敢
Owner 北京利乐生制药科技有限公司
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