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|Title:||Novel dosage form of fenofibrate|
|Abstract:||The present invention relates to a novel dosage form of fenofibrate containing fenofibrate and a solid surfactant which have been co-micronized. It also relates to the method for the preparation of this dosage form and its use for improving the bioavailabity in vivo.|
|Inventor(s):||Curtet; Bernard (Marsanny la Cote, FR), Teillaud; Eric (Talant, FR), Reginault; Philippe (Fontaine les Dijon, FR)|
|Assignee:||Fournier Innovation et Synergie (Paris, FR)|
1. A therapeutic composition, which is presented in the form of gelatin capsules and which is useful especially in the oral treatment of hyperlipidemia and
hypercholesterolemia, said composition containing a co-micronized mixture of particles of fenofibrate and a solid surfactant, wherein the mean particle size of said co-micronized mixture is less than 15 .mu.m.
2. The therapeutic composition according to claim 1 wherein the weight ratio surfactant/fenofibrate is between about 0.75/100 and 10.5/100.
3. The therapeutic composition according to claim 1 wherein the amount of fenofibrate is equal to 200 mg per therapeutic unit.
4. The therapeutic composition according to claim 1, wherein the solid surfactant is sodium lauryl-sulfate.
5. The therapeutic composition according to claim 4, wherein the amount of sodium lauryl-sulfate is between 0.5 and 7% by weight, relative to the total weight of the formulation.
6. The therapeutic composition according to claim 1, wherein said mean particle size is less than or equal to 10 .mu.m and said solid surfactant is sodium lauryl-sulfate.
7. The therapeutic composition according to claim 1, which also contains excipients such as dispersants, fillers and flow enhancers.
8. A method for the manufacture of a therapeutic composition according to claim 1, which comprises:
(i) intimately mixing and then co-micronizing the fenofibrate and a solid surfactant,
(ii) adding lactose and starch to the mixture obtained,
(iii) converting the whole to granules in the presence of water,
(iv) drying the granules until they contain no more than 1% of water,
(v) grading the granules,
(vi) adding polyvinylpyrrolidone and magnesium stearate, and
(vii) filling gelatin capsules.
9. The method according to claim 8, wherein the mean particle size of the co-micronized fenofibrate and sodium lauryl-sulfate is less than 15 .mu.m.
10. A method for improving the bioavailability of fenofibrate in vivo, which comprises co-micronization of the fenofibrate and a solid surfactant, the said co-micronization being carried out by micronization of a fenofibrate/solid surfactant mixture until the particle size of the powder obtained is less than 15 .mu.m.
11. A method for treatment of hyperlipidemia or hypercholesterolemia comprising orally administering the therapeutic composition of claim 6 to a patient.
12. The method of treatment of claim 11, wherein said particle size is less than or equal to 5 .mu.m.