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Claims for Patent: 9,040,088

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Claims for Patent: 9,040,088

Title:Nanoparticulate megestrol formulations
Abstract: The present invention is directed to nanoparticulate compositions comprising megestrol. The megestrol particles of the composition have an effective average particle size of less than about 2000 nm.
Inventor(s): Hovey; Douglas (Trooper, PA), Pruitt; John (Suwanee, GA), Ryde; Tuula (Malvern, PA)
Assignee: ALKERMES PHARMA IRELAND LIMITED (Dublin, IE)
Application Number:14/536,517
Patent Claims: 1. A method of increasing the body mass in a human patient suffering from anorexia, cachexia, or loss of body mass comprising administering to the human patient a megestrol acetate formulation, wherein: (a) the megestrol acetate formulation is a dose of about 40 mg to about 800 mg in about a 5 mL dose of an oral suspension; (b) the megestrol acetate formulation comprises megestrol acetate particles, wherein about 80% of the particles are between about 250 nm and about 50 nm, and at least one surface stabilizer is associated with the surface of the megestrol acetate particles; and (c) the administration is once daily; wherein after a single administration in a human subject of the formulation there is no substantial difference in the C.sub.max of megestrol when the formulation is administered to the subject in a fed versus a fasted state, wherein fasted state is defined as the subject having no food within at least the previous 10 hours, and wherein fed state is defined as the subject having a high-calorie meal within approximately 30 minutes of dosing.

2. The method of claim 1, wherein about 80% of the particles are between about 230 nm and about 70 nm.

3. The method of claim 1, wherein the anorexia, cachexia or loss of body mass is associated with a diagnosis of HIV or AIDS in the human patient.

4. The method of claim 1, wherein the anorexia, cachexia or loss of body mass is associated with a diagnosis of cancer in the human patient.

5. The method of claim 1, wherein there is a difference in the mean T.sub.max for the nanoparticulate megestrol acetate formulation when administered in fed versus fasted states, and that difference is selected from the group consisting of less than about 100%, less than about 90%, less than about 80%, less than about 70%, less than about 60%, less than about 50%, less than about 40%, less than about 30%, less than about 20%, less than about 15%, less than about 10%, less than about 5%, and less than about 3%.

6. The method of claim 1, wherein the formulation exhibits a mean C.sub.max, selected from the group consisting of greater than about 5%, greater than about 10%, greater than about 15%, greater than about 20%, greater than about 30%, greater than about 40%, greater than about 50%, greater than about 60%, greater than about 70%, greater than about 80%, greater than about 90%, greater than about 100%, greater than about 110%, greater than about 120%, greater than about 130% greater than about 140%, and greater than about 150% of the mean C.sub.max exhibited by a standard commercial, non-nanoparticulate composition of megestrol, administered at the same dosage.

7. The method of claim 1, wherein there is a difference in absorption (AUC) when the formulation is administered in fed versus fasted states, and the difference is selected from the group consisting of less than about 35%, less than about 30%, less than about 25%, less than about 20%, less than about 15%, less than about 10%, less than about 5%, and less than about 3%.

8. The method of claim 1, wherein a maximum blood plasma concentration of megestrol is attained in about 1 hour or less after administration of the megestrol acetate formulation in fasting subjects.

9. The method of claim 1, wherein a maximum blood plasma concentration of megestrol of at least about 700 ng/ml is obtained.

10. The method of claim 9, wherein the maximum blood plasma concentration of megestrol is at least about 700 ng/ml and is attained in less than 5 hours after administration of the megestrol acetate formulation.

11. The method of claim 1, wherein the maximum blood plasma concentration of megestrol is at least about 400 ng/ml and is attained in less than 5 hours after administration of the megestrol acetate formulation.

12. The method of claim 1, wherein a mean C.sub.max of about 300 ng/ml to about 2000 ng/ml is obtained after a single administration of the formulation in the human subject in a fasted state.

13. The method of claim 1, wherein the surface stabilizer is selected from the group consisting of nonionic surfactants, cationic surfactants, ionic surfactants, and zwitterionic surfactants.

14. The method of claim 1, wherein the surface stabilizer is selected from the group consisting of hydroxypropyl methylcellulose, hydroxypropylcellulose, polyvinylpyrrolidone, sodium lauryl sulfate, dioctylsulfosuccinate, polyoxyethylene alkyl etherspolyoxyethylene sorbitan fatty acid esters, 4-(1,1,3,3-tetramethylbutyl)-phenol polymer with ethylene oxide and formaldehyde, lysozyme, and random copolymers of vinyl pyrrolidone and vinyl acetate.

15. The method of claim 14, wherein the surface stabilizer is selected from the group consisting of hydroxypropyl methylcellulose, dioctylsulfosuccinate, and a combination thereof.

16. A method of increasing the body mass in a human patient suffering from anorexia, cachexia, or loss of body mass comprising administering to the human patient a megestrol acetate formulation, wherein: (a) the megestrol acetate formulation is a dose of about 40 mg to about 800 mg in about a 5 mL dose of an oral suspension; (b) the megestrol acetate formulation comprises megestrol acetate particles, wherein about 90% of the particles are less than or equivalent to about 250 nm, and about 10% of the particles are less than or equivalent to about 50 nm, and at least one surface stabilizer is associated with the surface of the megestrol acetate particles; and (c) the administration is once daily; wherein after a single administration in a human subject of the formulation there is no substantial difference in the C.sub.max of megestrol when the formulation is administered to the subject in a fed versus a fasted state, wherein fasted state is defined as the subject having no food within at least the previous 10 hours, and wherein fed state is defined as the subject having a high-calorie meal within approximately 30 minutes of dosing.

17. The method of claim 16, wherein about 90% of the particles are less than or equivalent to about 230 nm, and about 10% of the particles are less than or equivalent to about 70 nm.

18. The method of claim 16, wherein the anorexia, cachexia or loss of body mass is associated with a diagnosis of HIV or AIDS in the human patient.

19. The method of claim 16, wherein the anorexia, cachexia or loss of body mass is associated with a diagnosis of cancer in the human patient.

20. The method of claim 16, wherein the surface stabilizer is selected from the group consisting of nonionic surfactants, cationic surfactants, ionic surfactants, and zwitterionic surfactants.

21. The method of claim 16, wherein the surface stabilizer is selected from the group consisting of hydroxypropyl methylcellulose, hydroxypropylcellulose, polyvinylpyrrolidone, sodium lauryl sulfate, dioctylsulfosuccinate, polyoxyethylene alkyl etherspolyoxyethylene sorbitan fatty acid esters, 4-(1,1,3,3-tetramethylbutyl)-phenol polymer with ethylene oxide and formaldehyde, lysozyme, and random copolymers of vinyl pyrrolidone and vinyl acetate.

22. The method of claim 21, wherein the surface stabilizer is selected from the group consisting of hydroxypropyl methylcellulose, dioctylsulfosuccinate, and a combination thereof.

23. A method of increasing the body mass in a human patient suffering from anorexia, cachexia, or loss of body mass comprising administering to the human patient a megestrol acetate formulation, wherein: (a) the megestrol acetate formulation is a dose of about 40 mg to about 800 mg in about a 5 mL dose of an oral suspension; (b) the megestrol acetate formulation comprises megestrol acetate particles, wherein about 90% of the particles have a size less than or equivalent to about 250 nm and about 90% of particles have a size greater than or equivalent to about 50 nm, and at least one surface stabilizer is associated with the surface of the megestrol acetate particles; and (c) the administration is once daily; wherein after a single administration in a human subject of the formulation there is no substantial difference in the C.sub.max of megestrol when the formulation is administered to the subject in a fed versus a fasted state, wherein fasted state is defined as the subject having no food within at least the previous 10 hours, and wherein fed state is defined as the subject having a high-calorie meal within approximately 30 minutes of dosing.

24. The method of claim 23, wherein about 90% of the particles have a size less than or equivalent to about 230 nm and about 90% of particles have a size greater than or equivalent to about 70 nm.

25. The method of claim 23, wherein the anorexia, cachexia or loss of body mass is associated with a diagnosis of HIV or AIDS in the human patient.

26. The method of claim 23, wherein the anorexia, cachexia or loss of body mass is associated with a diagnosis of cancer in the human patient.

27. The method of claim 23, wherein the surface stabilizer is selected from the group consisting of nonionic surfactants, cationic surfactants, ionic surfactants, and zwitterionic surfactants.

28. The method of claim 23, wherein the surface stabilizer is selected from the group consisting of hydroxypropyl methylcellulose, hydroxypropylcellulose, polyvinylpyrrolidone, sodium lauryl sulfate, dioctylsulfosuccinate, polyoxyethylene alkyl etherspolyoxyethylene sorbitan fatty acid esters, 4-(1,1,3,3-tetramethylbutyl)-phenol polymer with ethylene oxide and formaldehyde, lysozyme, and random copolymers of vinyl pyrrolidone and vinyl acetate.

29. The method of claim 19, wherein the surface stabilizer is selected from the group consisting of hydroxypropyl methylcellulose, dioctylsulfosuccinate, and a combination thereof.
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