Claims for Patent: 11,000,508

Summary for Patent: 11,000,508

Title:	Secnidazole for use in the treatment of trichomoniasis
Abstract:	Method of treating trichomoniasis in a subject in need thereof involving administering to the subject a therapeutically effective amount of secnidazole in a microgranule formulation, wherein the microgranule formulation comprises a plurality of microgranules having a volume-weighted particle size distribution within a microgranule population, wherein the volume-weighted particle size distribution as measured from a representative sample of the microgranule population comprises (a) at least 10% of the microgranule population having a volume-weighted particle size about no less than 470 micrometers; or (b) 50% of the microgranule population having a volume-weighted particle size between about no less than 640 micrometers and about no more than 810 micrometers; or (c) 90% of the microgranule population having a volume-weighted particle size about no more than 1170 micrometers; or (d) a combination thereof, which can include some or all of (a) through (c) above.
Inventor(s):	Pentikis; Helen S. (Timonium, MD), Palling; David (Glen Ridge, NJ), Braun; Carol J. (Ellicott City, MD), Holl; Richard (Somerset, NJ)
Assignee:	LUPIN INC. (Baltimore, MD)
Application Number:	16/901,739
Patent Claims:	1. A method of treating trichomoniasis in a subject in need thereof comprising: administering to the subject a microgranule formulation comprising a therapeutically effective amount of secnidazole, wherein the microgranule formulation comprises a plurality of microgranules having a volume-weighted particle size distribution within a microgranule population, wherein the volume-weighted particle size distribution as measured by laser diffraction from a representative sample of the microgranule population comprises: (a) at least 10% of the microgranule population having a volume-weighted particle diameter equal to or larger than 470 micrometers; and (b) 50% of the microgranule population having a volume-weighted particle diameter in a range of from 640 micrometers to 810 micrometers; and (c) 90% of the microgranule population having a volume-weighted particle diameter smaller than 1170 micrometers; wherein each microgranule comprises a sugar core or a microcrystalline cellulose core, and an outer layer on the sugar core or the microcrystalline cellulose core, the outer layer comprising secindazole; wherein the therapeutically effective amount of secnidazole is 2 grams, and the microgranule formulation provides a maximum plasma concentration of secnidazole in the subject of about 34.5 .mu.g/ml to about 58.3 .mu.g/ml; and wherein the therapeutically effective amount of secnidazole is 2 grams, wherein the secnidazole is the sole drug in the microgranule formulation. 2. The method of claim 1, wherein the therapeutically effective amount of secnidazole in the microgranule formulation is administered orally. 3. The method of claim 1, wherein the outer layer further comprises a copolymer of ethyl acrylate and methyl methacrylate. 4. The method of claim 1, wherein each microgranule further comprises an outer coat on top of the outer layer. 5. The method of claim 1, wherein each microgranule further comprises at least one compound selected from the group consisting of povidone, polyethylene glycol, a copolymer of ethyl acrylate and-methyl methacrylate, and talc. 6. The method of claim 1, wherein the microgranule formulation is integrated into a food substance or a liquid prior to administration. 7. The method of claim 6, wherein the food substance is a liquid, semisolid or a soft food. 8. The method of claim 1, wherein the subject is a female or pregnant female. 9. The method of claim 1, wherein the subject is suffering from bacterial vaginosis. 10. The method of claim 1, wherein the therapeutically effective amount of secnidazole in the microgranule formulation is administered as a single dose. 11. The method of claim 10, wherein the therapeutically effective amount of secnidazole in the microgranule formulation administered as a single dose is the only dose required to be administered to the subject to achieve a post treatment clinical outcome by resolution of one or more symptoms of trichomoniasis. 12. The method of claim 1, wherein the therapeutically effective amount of secnidazole in the microgranule formulation is co-administered with an additional compound selected from ethinyl estradiol, norethindrone, or a combination thereof. 13. The method of claim 12, wherein the additional compound is administered on the same day as the therapeutically effective amount of secnidazole in the microgranule formulation. 14. The method of claim 12, wherein the additional compound is administered on a different day than the therapeutically effective amount of secnidazole in the microgranule formulation. 15. The method of claim 12, wherein the secnidazole microgranule formulation does not affect a contraceptive efficacy of the additional compound. 16. A method of treating trichomoniasis in a subject in need thereof comprising: administering to the subject a microgranule formulation comprising a therapeutically effective amount of secnidazole, wherein the microgranule formulation comprises a plurality of microgranules having a volume-weighted particle size distribution within a microgranule population, wherein the volume-weighted particle size distribution as measured by laser diffraction from a representative sample of the microgranule population comprises: (a) at least 10% of the microgranule population having a volume-weighted particle diameter equal to or larger than 470 micrometers; and (b) 50% of the microgranule population having a volume-weighted particle diameter in a range of from 640 micrometers to 810 micrometers; and (c) 90% of the microgranule population having a volume-weighted particle diameter smaller than 1170 micrometers; wherein each microgranule comprises a sugar core or a microcrystalline cellulose core, and an outer layer on the sugar core or the microcrystalline cellulose core, the outer layer comprising secindazole; and the microgranule formulation provides a time to maximum plasma concentration (Tmax) of secnidazole of about 2 hours to about 6 hours after administering to the subject; and wherein the secnidazole is the sole drug in the microgranule formulation. 17. The method of claim 16, the Tmax of secnidazole is about 3 hours to about 4 hours after administering to the subject. 18. The method of claim 1, wherein the sugar core is a sugar sphere core. 19. The method of claim 16, wherein the sugar core is a sugar sphere core. 20. The method of claim 16, wherein the outer layer further comprises a copolymer of ethyl acrylate and methyl methacrylate. 21. The method of claim 16, wherein each microgranule further comprises an outer coat on top of the outer layer. 22. The method of claim 16, wherein each microgranule further comprises at least one compound selected from the group consisting of povidone, polyethylene glycol, a copolymer of ethyl acrylate and-methyl methacrylate, and talc. 23. The method of claim 16, wherein the microgranule formulation is integrated into a food substance or a liquid prior to administration. 24. The method of claim 23, wherein the food substance is a liquid, semisolid or a soft food.