Unlock instant, AI-driven research and patent intelligence for your innovation.

Nicotinic acid derivative of fenofibrate and preparation method of nicotinic acid derivative

A technology of fenofibrate and niacin, applied in the field of medicine, can solve problems such as unsatisfactory effect

Inactive Publication Date: 2012-06-27
FUKANGREN BIO PHARMA
View PDF0 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It is currently used to treat hyperlipidemia in adults whose diet control therapy is not effective. Its effect of lowering triglyceride and mixed hyperlipidemia is more obvious than that of cholesterol.

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Nicotinic acid derivative of fenofibrate and preparation method of nicotinic acid derivative
  • Nicotinic acid derivative of fenofibrate and preparation method of nicotinic acid derivative
  • Nicotinic acid derivative of fenofibrate and preparation method of nicotinic acid derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] The preparation method of the compound shown in embodiment 1 formula I,

[0018] The preparation method comprises the following four steps:

[0019] The first step: fenofibrate acid reacts with alkali sodium hydroxide to generate fenofibrate sodium salt,

[0020] The second step: nicotinic acid and vinyl acetate react under the catalysis of mercury acetate and concentrated sulfuric acid to form nicotinic acid vinyl ester,

[0021] The third step: nicotinic acid vinyl ester reacts with hydrogen bromide acetic acid solution to generate nicotinic acid-α-bromo-ethyl ester,

[0022] Part Four: The reaction of fenofibrate sodium salt and nicotinic acid-α-bromo-ethyl ester produces the product fenofibrate nicotinate I.

[0023]

Embodiment 2

[0024] Embodiment 2: the preparation of dry suspension

[0025] formula

Dosage (% mass)

Micronized Fenofibrate Nicotinate

64.5

Neutral particles

21

Polysorbate 80

3.3

hypromellose

11.2

[0026] Preparation:

[0027] 1. Add micronized fenofibrate nicotinate, Polysorbate 80, and hypromellose into purified water and stir evenly to make an aqueous suspension;

[0028] 2. Spray the aqueous suspension on the neutral fine particles in a fluidized bed, and dry at 50°C to obtain small drug-containing particles.

[0029] 3. Mix other excipients in proportion, pack to obtain dry suspension.

Embodiment 3

[0030] Embodiment 3: the preparation method of capsule

[0031] formula

Dosage (% mass)

Micronized Fenofibrate Nicotinate

67.1

Neutral particles

17.2

sodium lauryl sulfate

3.3

hypromellose

11.5

35% dimethicone emulsion

0.2

Talc powder

0.5

[0032] Preparation:

[0033] 1. Take micronized fenofibrate nicotinate, sodium lauryl sulfate, and hypromellose and add them into purified water and stir evenly to make an aqueous suspension;

[0034] 2. Spray the aqueous suspension and 35% dimethicone emulsion on the neutral micro-particles in a fluidized bed, and dry at 50 degrees to obtain granules;

[0035] 3. Add an appropriate amount of talcum powder and put it into a No. 1 gelatin capsule to obtain a capsule.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

A nicotinic acid derivative of fenofibrate and a preparation method of the nicotinic acid derivative relate to a compound with the structure demonstrated as formula I, the preparation method, a medical combination and medical use. The compound can serve as medical active ingredient to be combined with auxiliary materials to prepare orally taking agent for treating various hyperlipemia.

Description

technical field [0001] The invention relates to a nicotinic acid derivative of fenofibrate and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Hyperlipidemia refers to high cholesterol (TC) and / or triglyceride (TG) or low high-density lipoprotein cholesterol (HDL-C) in the blood. The damage to the body of the disease is hidden, gradual, progressive and systemic. sexual. Its direct damage is to accelerate systemic atherosclerosis, because vital organs of the whole body rely on arterial blood supply and oxygen supply. Once the arteries are blocked by atherosclerotic plaques, serious consequences will result. Renal failure caused by arteriosclerosis is closely related to hyperlipidemia. A large number of research data show that hyperlipidemia is an independent and important risk factor for stroke, coronary heart disease, myocardial infarction, and sudden cardiac death. In recent years, a variety of blood lipid-lowerin...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): C07D213/80C07D213/803A61K31/455A61P3/06
Inventor 不公告发明人
Owner FUKANGREN BIO PHARMA