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Details for Patent: 9,149,431

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Details for Patent: 9,149,431

Title:Itraconazole compositions with improved bioavailability
Abstract: A solid dispersion product comprising itraconazole and hydroxypropyl methylcellulose, which satisfies the Formula 0.35>.DELTA.H.sub.tr (1) (wherein .DELTA.H.sub.tr represents the endotherm (J/g) accompanying a transition at about 240.degree. C.). The solid dispersion product shows an improved bioavailability.
Inventor(s): Berndl; Gunther (Herxheim am Berg, DE), Degenhardt; Matthias (Limburgerhof, DE), Magerlein; Markus (Mannheim, DE), Dispersyn; Gerrit (Princeton, NJ)
Assignee: Abbvie Deutschland GmbH & Co KG (Wiesbaden, DE) Barrier Therapeutics, Inc. (Princeton, NJ)
Filing Date:Jun 21, 2013
Application Number:13/923,459
Claims:1. A method for preparing a solid dispersion product comprising itraconazole and hydroxypropyl methylcellulose, which method comprises: a) blending itraconazole and hydroxypropyl methylcellulose; b) heating the blend to a temperature of 195 to 300.degree. C. so as to obtain a homogenous melt and exerting a shearing and/or kneading action to the melt in an extruder selected from single screw extruders, intermeshing screw extruders and multi-screw extruders, wherein the screw(s) comprise(s) at least one of reverse-flighted elements, shear elements, kneading discs and rotor blades; c) forcing the thus obtained melt through one or more nozzles; d) allowing the melt to solidify to obtain a solid dispersion product; and e) optionally grinding the solid dispersion product; wherein the temperature and the conditions of shearing and/or kneading in step b) are adjusted such that the solid dispersion product satisfies the formula 0.35>.DELTA.H.sub.tr wherein .DELTA.H.sub.tr represents the endotherm (J/g) accompanying a transition at an endothermic peak temperature in the range of from 240.degree. C. to 250.degree. C.

2. The method of claim 1, wherein forcing the melt is carried out at a temperature of 195 to 300.degree. C.

3. The method of claim 2, additionally comprising compressing the ground solid dispersion product into a tablet.

4. The method of claim 1, additionally comprising sieving the ground solid dispersion product.

5. The method of claim 1, wherein the temperature and the conditions of shearing and/or kneading in step b) are adjusted such that the solid dispersion product satisfies the formula 0.20>.DELTA.H.sub.tr wherein .DELTA.H.sub.tr represents the endotherm (J/g) accompanying a transition at an endothermic peak temperature in the range of from 240.degree. C. to 250.degree. C.

6. The method of claim 1, wherein the solid dispersion product has a weight-average particle size ranging between 50 .mu.m to 600 .mu.m.

7. The method of claim 1, wherein the total content of methoxy and hydroxypropyl groups in the hydroxypropyl methylcellulose is in the range of 23 to 42% by weight.

8. The method of claim 7, wherein the methoxy group content is in the range of 19 to 30% by weight and the hydroxypropyl group content is in the range of 4 to 12% by weight.

9. The method of claim 8, wherein the hydroxypropyl methylcellulose has an apparent viscosity of from 3 to 15 mPas, as determined as a 2% by weight aqueous solution at 20.degree. C.

10. The method of claim 1, wherein the weight ratio of itraconazole:hydroxypropyl methylcellulose is in the range of 1:1 to 1:17.

11. The method of claim 1, wherein the extruder used in step b) is a twin screw extruder.
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