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FORMULATIONS COMPRISING LIPID-REGULATING AGENTS

IP.com Disclosure Number: IPCOM000008767D
Publication Date: 2002-Jul-11
Document File: 1 page(s) / 8K

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Fenofibrate Formulation

Introduction

Fenofibrate, is a lipid regulating agent available as capsules and tablets for oral administration (Abbot laboratories). Many patents and patent applications describe methods for increasing the bioavailability of Fenofibrate. For example US Patent 6,074,670 describes a procedure in which fenofibrate is co- micronized with Sodium Lauryl Sulfate. Published US Patent application 2001/0006662 A1 describes a procedure for preparation of amorphous fenofibrate, and US Patent no 6,027,747 describes a method for preparation of solid dispersions of Fenofibrate in hydrophilic polymer. The general purpose of these patents and applications is formation of a physical stable state in which micronized particles of the active ingredient are separated from each other. This physical state increases the surface area of the active ingredient, a parameter that has a significant effect on dissolution and bioavailability. Our experimental work was focused on a search for a new and different pharmaceutical procedure which will enable a physically stable state of the active ingredient where the active ingredient exhibits a maximal surface area. Fenofibrate, when formulated in a common granulation procedure, results in a composition in which the active principal has a poor surface area, even if a raw material with reduced particle size is used (approx. 7 microns ), a result which is related to its strong tendency to agglomerate. . Within our experimental work it was found that strong and aggressive milling of granulate of fenofibrate resulted with a significant increase in surface area of the active drug . The theoretical explanation for this phenomena was as follows: Fenofibrate has a very strong tendency to agglomerate during a regular granulation processes (wet granulation o...