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Claims for Patent: 8,158,645

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Claims for Patent: 8,158,645

Title:Compound, corresponding compositions, preparation and/or treatment methods
Abstract: Disclosed is a novel crystalline form of topotecan monohydrochloride pentahydrate, which is a pentahydrate of 10-[(dimethylamino)methyl]-4-ethyl-4,9-dihydroxy-1H-pyrano[3',4':6,7]indo- lizino[1,2-b]quinoline-3,14(4H,12H)dione monohydrochloride, corresponding pharmaceutical compositions, methods preparation and/or use thereof to treat anti-viral and/or cancer-related diseases.
Inventor(s): Dell'Orco; Philip C. (King of Prussia, PA), Diederich; Ann Marie (King of Prussia, PA), Su; Qiaogong (King of Prussia, PA), Wood; Jeffery Lee (King of Prussia, PA)
Assignee: GlaxoSmithKline LLC (Philadelphia, PA)
Application Number:12/770,898
Patent Claims: 1. A pharmaceutical composition prepared by dispersing topotecan monohydrochloride in a mixture of glyceryl monostearate and hydrogenated vegetable oil, wherein the topotecan monohydrochloride is a topotecan monohydrochloride pentahydrate product having an X-ray powder diffraction pattern that is substantially the same as FIG. 1.

2. A pharmaceutical composition prepared by dispersing topotecan monohydrochloride in a mixture of glyceryl monostearate and hydrogenated vegetable oil, wherein the topotecan monohydrochloride is a topotecan monohydrochloride pentahydrate product having an X-ray powder diffraction pattern that is substantially the same as FIG. 1, and wherein the topotecan monohydrochloride pentahydrate product is prepared by a process comprising the steps of: [a] forming an aqueous organic solvent mixture containing topotecan monohydrochloride, wherein the organic solvent of the aqueous organic solvent mixture is selected from the group consisting of acetone and tetrahydrofuran, and wherein the ratio of organic solvent to aqueous solvent in the aqueous organic solvent mixture is from about 1.5:1 to about 3:1; [b] recrystallizing the topotecan monohydrochloride from the aqueous organic solvent mixture to precipitate the topotecan monohydrochloride pentahydrate product; and [c] collecting, by filtration, the topotecan monohydrochloride pentahydrate product.

3. The pharmaceutical composition according to claim 2, wherein the aqueous organic solvent mixture comprises an aqueous mineral acid solution, wherein the aqueous mineral acid solution is a 0.05 N aqueous hydrochloric acid solution.

4. The pharmaceutical composition according to claim 2, wherein the aqueous organic solvent mixture comprises a mixture of acetone and a 0.05 N aqueous hydrochloric acid solution.

5. The pharmaceutical composition according to claim 2, wherein process step [b] comprises recrystallizing the topotecan monohydrochloride from the aqueous organic solvent mixture which comprises acetone and 0.05 N aqueous hydrochloric acid, wherein the v/v ratio of acetone to aqueous hydrochloric acid is about 2:1.

6. The pharmaceutical composition according to claim 2, prepared by a process further comprising the steps of: first dissolving topotecan monohydrochloride in a heated aqueous organic solvent solution mixture; crystallizing or recrystallizing the topotecan monohydrochloride pentahydrate from the heated solution by cooling the solution; and filtering the resulting recrystallized topotecan monohydrochloride pentahydrate product and drying.

7. The pharmaceutical composition according to claim 6, wherein the heated aqueous organic solvent solution mixture is a mixture of acetone and 0.05 N aqueous hydrochloric acid heated to a temperature of about 58.degree. C. and the v/v ratio of acetone to aqueous hydrochloric acid is about 2:1.

8. The pharmaceutical composition according to claim 6, wherein the heated solution is cooled at a rate of about 0.1.degree. C./min to about 1.degree. C./min.

9. The pharmaceutical composition according to claim 6, wherein the heated solution is cooled at a rate of about 0.25.degree. C./min.

10. The pharmaceutical composition according to claim 6, wherein, in the crystallization or recrystallization process, the solution is cooled to a temperature of about room temperature to about 0.degree. C.

11. A pharmaceutical composition prepared by dispersing topotecan monohydrochloride in a mixture of glyceryl monostearate and hydrogenated vegetable oil, wherein the topotecan monohydrochloride is a topotecan monohydrochloride pentahydrate product having an X-ray powder diffraction pattern that is substantially the same as FIG. 1, and wherein the topotecan monohydrochloride pentahydrate product is prepared by a process comprising the steps of: [a] forming an aqueous organic solvent mixture containing topotecan monohydrochloride, wherein the aqueous solvent of the aqueous organic solvent mixture is an aqueous mineral acid solution, the organic solvent of the aqueous organic solvent mixture is selected from the group consisting of acetone and tetrahydrofuran, and wherein the v/v ratio of organic solvent to aqueous solvent is about 8:1; [b] slurrying the topotecan monohydrochloride with the aqueous organic solvent mixture to form the topotecan monohydrochloride pentahydrate product; and [c] collecting, by filtration, the topotecan monohydrochloride pentahydrate product.

12. The pharmaceutical composition according to claim 11, wherein the aqueous organic solvent mixture comprises a 0.05 N aqueous hydrochloric acid solution.
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