Dismiss
InnovationQ will be updated on Sunday, Oct. 22, from 10am ET - noon. You may experience brief service interruptions during that time.
Browse Prior Art Database

MODIFIED-RELEASE PHARMACEUTICAL COMPOSITIONS OF FENOFIBRIC ACID OR ITS SALTS AND PROCESS OF PREPARATION THEREOF

IP.com Disclosure Number: IPCOM000214223D
Publication Date: 2012-Jan-18
Document File: 17 page(s) / 60K

Publishing Venue

The IP.com Prior Art Database

Abstract

The present disclosure relates to a modified-release pharmaceutical composition of fenofibric acid or its salts, and process of preparation thereof. Further, the present disclosure relates to a pharmaceutical composition of fenofibric acid or its salts, in combination with rosuvastatin and process of preparation thereof.

This text was extracted from a Microsoft Word document.
This is the abbreviated version, containing approximately 7% of the total text.

MODIFIED-RELEASE PHARMACEUTICAL COMPOSITIONS OF FENOFIBRIC ACID OR ITS SALTS AND PROCESS OF PREPARATION THEREOF

Abstract

The present disclosure relates to a modified-release pharmaceutical composition of fenofibric acid or its salts, and process of preparation thereof.  Further, the present disclosure relates to a pharmaceutical composition of fenofibric acid or its salts, in combination with rosuvastatin and process of preparation thereof.

Fenofibrate, which belongs to the fibrate family, has been known for many years as a medicinal active principal because of its efficacy in lowering the blood triglyceride and cholesterol levels.  Thus, fenofibrate is widely recommended in the treatment of hyperlipidemia and hypercholesterolemia.  Fenofibrate is a prodrug that is absorbed and then hydrolyzed by tissue and plasma esterases to fenofibric acid, its active metabolite or active species.  Fenofibric acid, responsible for the pharmacological activity, has a plasma half-life of about 20 hours.  Fenofibrate suffers from the disadvantage of being poorly soluble in an aqueous medium, thus having an insufficient dissolution profile and, consequently, poor bioavailability within the organism, following oral administration.  The therapeutic dose required to be administered must thus be increased in order to obviate this disadvantage.  This particularly applies to numerous hypolipemiant active ingredients, such as those belonging to the fibrate family.  Indeed, due to its poor hydrosolubility, fenofibrate is poorly absorbed in the digestive tract and consequently its bioavailability is incomplete, irregular and often varies from one person to another.  To improve the dissolution profile of fenofibrate and its bioavailability, thereby reducing the dose required to be administered, it would be useful to increase its dissolution so that it could attain a level close to 100%.

Rosuvastatin, chemically is (E)-7-[4-(4-fluorophenyl)-6 isopropyl-2-[methyl(methyl-sulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid.  Rosuvastatin is a potent statin, an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase.  This enzyme catalyzes the conversion of HMG-CoA to mevalonate, an early and rate-limiting step in cholesterol biosynthesis.  Rosuvastatin calcium is marketed as Crestor® tablets for oral administration and has been approved for treatment of primary hypercholesterolemia, mixed dyslipidemia, hypertriglyceridemia, and homozygous familial hypercholesterolemia.  Dose range is 5 milligrams to 40 milligrams (mg) orally once daily, with starting doses of 5 mg to 20 mg once daily.  Doses may be titrated to 40 mg/day in those who do not meet their lipid lowering goals on 20 mg/day.

The products currently on the market are based on a formulation comprising micronized drug substance (TRICOR®) in capsules and/or tablets.  But due to the insolubility of fenofibrate in water there remains a tendency of said substance to recryst...