Patent EA-004294-B1 (EA)
Title: Pharmaceutical composition containing fenofibrate and preparation method
Inventor: CRIERE BRUNO
IPC: A61K9/48
Filed: 2000-07-07
Abstract: 1. A pharmaceutical composition containing micronized fenofibrate, a surfactant and a binding cellulose derivative, as solubilizing adjuvant, characterized in that comprises an amount of fenofibrate higher or equal to 60 wt.%. 2. The composition according to claim 1, characterized in that binding cellulose derivative, as solubilizing adjuvant is hydroxypropylmethylcellulose. 3. The composition according to claim 2, characterized in that hydroxypropylmethylcellulose has an apparent viscosity 2.4 to 18 cP, preferably 2.4 to 3.6 cP. 4. The composition according to any one of claims 1 to 3, characterized in that comprises fenofibrate higher or equal to 70 wt.%, more preferably higher or equal to 75 wt.% relative to the mass composition. 5. The composition according to any one of claims 1 to 4, characterized in that the surfactant is selected from the group consisting of polyoxyethylene-20-monooleatsorbate, monolauratsorbate and sodium laurylsulfate. 6. The composition according to any one of claims 1 to 5, characterized in that the surfactant comprises 1 to 10 wt.%, preferably 3 to 5 wt.% relative to the fenofibrate mass. 7. The composition according to any one of claims 2 to 6, characterized in that the mass ratio fenofibrate/ hydroxypropylmethylcellulose (HPMC) is from 5/1 to 15/1. 8. The composition according to any one of claims 1 to 7, characterized in that binding cellulose derivative comprises 2 to 15 wt.%, preferably 5 to 12 wt.% relative to the composition mass. 9. The composition according to any one of claims 1 to 8, characterized in that comprises at least one excipient, such as diluent, in particular, lactose, anti-frothing agent, in particular, dimethylpolyoxsane, or polymethylsiloxane and dioxide silicon, or a lubricant, in particular, talc. 10. The composition according to any one of claims 1 to 9, characterized in that average fenofibrate particles size is below 15 mum, preferably below 8 mum. 11. The composition according to any one of claims 1 to 10, characterized in that preferably hydroxypropylmethylcellulose. The cellulose derivative represents less than 20 wt. % of the composition. The association of micronized fenofibrate with a binding cellulose derivative, as solubilizing adjuvant and a surfactant enables to enhance the bioavailability of the active principle. The invention also concerns a method for preparing said composition without using any organic solvent. 12. Process of preparing of composition according to any of claims 1-11, characterized in that the granules are prepared by applying on neutral microgranules by means of pulverization of aqueous suspension containing surfactant, solubilized cellulose derivative as binding and micronized fenofibrate in suspension. 13. Process of preparation of composition according to any of claims 1-11, characterized in that the granules are prepared by granulation of powder by wet method, according to which the components of the powder, in particular micronized fenofibrate, surfactant and cellulose derivative are granulated by wet method using an aqueous softening solution, then the granules are dried and calibrated.