ETOFIBRATE

Description

Etofibrate is a combination of niacin and clofibrate that acts as a hypolipidemic agent. In vivo, etofibrate decreases plasma cholesterol and triglyceride concentrations and increases bile cholesterol content in rats. It also decreases thromboxane formation, platelet aggregation, and plasma viscosity and inhibits neointima formation in a carotid artery balloon injury rat model. Formulations containing etofibrate have been used to treat hyperlipidemia.

Chemical properties

White to Off-White Solid

Originator

Lipo-Merz,Merz,W. Germany,1974

The Uses of ETOFIBRATE

Antilipemic; reducing lipid levels in the blood.

What are the applications of Application

Etofibrate is a combination of clofibrate and niacin, used to treat hyperlipidaemias

Definition

ChEBI: Etofibrate is a monocarboxylic acid.

Manufacturing Process

A stream of ethylene oxide is passed through a solution of 107 g of 2-(pchlorophenoxy)- 2-methylpropionic acid and 2 g of zinc chloride in 200 ml of toluene, previously heated to between 55°C and 60°C, until 24 g of the gas have been dissolved. The reaction is allowed to continue for five hours, with gentle stirring. After this time has elapsed, the solution is cooled and washed successively with water, dilute ammonia and water until its pH becomes neutral. It is dried over anhydrous sodium sulfate, the solvent is separated off under vacuum, and the resulting liquid is the monoglycol ester of 2-(pchlorophenoxy)- 2-methylpropionic acid.
The product thus prepared is sufficiently pure to be used in the subsequent reaction. In this way, 107 g of the ester are prepared, which represents a yield of 83%.
To a solution of 93.8 g of the monoglycol ester in 500 ml of benzene, there are added 55 g of nicotinic acid chloride and 25 g of trimethylamine dissolved in 200 ml of benzene. The solution is stirred gently at a temperature of 60°C for two hours. After this time, the solution is cooled and washed successively with water, dilute hydrochloric acid, dilute ammonia and water until neutrality, it is dried over anhydrous sodium sulfate, and the solvent is evaporated under vacuum: in this way 110 g of glycol 2-(p-chlorophenoxy)-2-methylpropionate nicotinate is prepared, which represents a yield of 84%. The product is a slighly yellow oil having a refraction index of nD 20 =1.5422 and which is distilled with decomposition at 214°C at a pressure of 0.3 mm.

Therapeutic Function

Antihyperlipidemic