Fenofibrate medicament composition

A technology of fenofibrate and a composition, which is applied in the field of fibrate drugs, can solve the problems of low bioavailability of fibrate drugs, and achieve the effects of improving bioavailability, simple production process and reducing differences in bioavailability

Inactive Publication Date: 2009-08-12
安徽省食品药品检验研究院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In order to solve the problem of low bioavailability of fibrates represented by fenofibrate, the present invention provides a fibrate pharmaceutical composition that significantly improves in vitro dissolution rate and bioavailability

Method used

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  • Fenofibrate medicament composition
  • Fenofibrate medicament composition
  • Fenofibrate medicament composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Preparation of Fenofibrate Sustained Release Capsules

[0035] Take fenofibrate 2.4g, glyceryl behenate (compritol 888 ATO) 2.4g, polyethylene glycol 6000 (polyethylene glycol with a polymerization degree of 6000) 6g, polyethylene glycol laurate 0.6g, Polyoxyethylene hydrogenated castor oil (CremophorRH40) 0.4g.

[0036] Add the above materials into a 50ml beaker, heat to about 90°C to melt, stir at low speed for about 10 minutes, and oscillate ultrasonically. Keep warm at 55°C and fill gelatin hard capsules or vegetable capsules. 190 mg per capsule (calculated as fenofibrate).

[0037] Get this product, according to the dissolution test method of European Pharmacopoeia, adopt the device of the second method of dissolution method, with 2% Tween 80 solution 1000ml as dissolution medium, rotating speed is 75 revolutions per minute, operate according to law. After 1, 4, and 6 hours, take 10ml of the solution and filter it, and add 10ml of the above-mentioned dissolution...

Embodiment 2

[0040] Preparation of sustained-release capsules

[0041] Take 2.4g of fenofibrate, 2.4g of glyceryl palmitostearate (Precirol ATO5), 4076g of poloxamer, 0.6g of polyethylene glycol laurate, and 0.4g of polyoxyethylene castor oil.

[0042] Add the above materials into a 50ml beaker, heat to about 90°C to melt, stir at low speed for about 10 minutes, and homogenize under high pressure. Keep warm at 55°C and fill gelatin hard capsules or vegetable capsules. 190 mg per capsule (calculated as fenofibrate).

[0043] Get this product, according to the dissolution test method of European Pharmacopoeia, adopt the device of the second method of dissolution method, with 2% Tween 80 solution 1000ml as dissolution medium, rotating speed is 75 revolutions per minute, operate according to law. After 1, 4, and 6 hours, take 10ml of the solution and filter it, and add 10ml of the above-mentioned dissolution medium in the operation container in time; accurately measure 2ml of the subsequent ...

Embodiment 3

[0046] Preparation of Fenofibrate Sustained Release Dropping Pills

[0047] Take fenofibrate 0.6g, glycerol palmitostearate 4.2g, polyethylene glycol 6000 (polyethylene glycol with a polymerization degree of 6000) 6g, ethylene glycol monoethyl ether 0.4g, polyoxyethylene castor Sesame oil 0.4g. 48 mg per capsule (calculated as fenofibrate).

[0048] Add the above materials into a 50ml beaker, heat to about 90°C to melt, and stir at a low speed for about 10 minutes. Insulate at 55°C, drop and cool to prepare sustained-release dropping pills.

[0049] Get this product, according to the dissolution test method of European Pharmacopoeia, adopt the device of the second method of dissolution method, take 2% Tween 80 solution 1000ml as the dissolution medium, and the rotating speed is 75 revolutions per minute, according to the law. After 1, 4, and 6 hours, take 10ml of the solution and filter it, and add 10ml of the above-mentioned dissolution medium in the operation container in...

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Abstract

The invention relates to a fibrate drug combination and solves the problem of the low bioavailability of fenofibrate. The drug combination comprises the following materials according to part by weight: 6 to 42 parts of fenofibrate, 60 to 80 parts of polyethylene glycol 6000 or poloxamer 407, 6 to 42 parts of compritol 888 ATO or precirol AT05, 2 to 12 parts of polyethylene glycol glyceryl dilaurate or ethylene glycol monoethyl ether and 2 to 12 parts of cremophor RH40 or cremophor EL. The invention can finish the processes of drug micronization and micronized drug dispersion in one-step operation based on the physical and chemical properties of raw materials and auxiliary materials; the compritol 888 ATO can achieve the purpose of sustaining the drug release owing to the hydrophobicity thereof, and the compritol 888 ATO has the release characteristics of zero-order sustained release at a particular ratio in a continuous and complete state; the hydrophilic matrix formed by polyethylene glycol 6000 can prevent the drug release from being affected by acid and alkali and reduce the possibility of bioavailability difference caused by the individual difference; and the invention has the advantages of simple production process, low cost and controllable quality.

Description

technical field [0001] The invention relates to fibrate drugs (selected from phenoxyaromatic acid drugs, salts thereof, solvates and active metabolites thereof), specifically a stable solid dosage form of fenofibrate and a preparation method thereof. Background technique [0002] Fenofibrate is a second-generation phenoxyaromatic acid drug developed by French company Fournier and launched in the United States in 1998. Because of its good lipid-lowering effect, it has been widely used in clinical practice. [0003] Fenofibrate has a good curative effect, but because it is insoluble in water, the dissolution rate is insufficient, resulting in low bioavailability after oral administration. In the digestive tract, it is only about 60% absorbed after oral administration. Its bioavailability is incomplete, and varies from person to person, with large individual differences. Generally required to be used with food to enhance bioavailability. [0004] Therefore, if the dissoluti...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/48A61K9/20A61K31/216A61K47/44A61P3/06A61K47/34A61K47/14A61K47/10
Inventor 刘羽王辉吕凌孙备王贺路小冬李姜晖刘燕戴萍萍崔颖
Owner 安徽省食品药品检验研究院
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