Manage your formulary budget
Proactively manage your pharmacy inventory
Deep knowledge on
small-molecule drugs and
the 110,000 global patents
Find generic entry opportunities
Drug patents …
… from Kazakhstan to Kalamazoo
Anticipate generic drug launch
Flat-rate pricing for predictable budgeting
Short-term plans for project- or client-based billing
Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing
|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|
|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.
Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.