Claims for Patent: 10,682,338

Summary for Patent: 10,682,338

Title:	Secnidazole for use in the treatment of bacterial vaginosis
Abstract:	Method of treating bacterial vaginosis 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) 10% of the microgranule population having a volume-weighted particle size about no less than 470 micrometers; (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; (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:	16/049,032
Patent Claims:	1. A method of treating bacterial vaginosis 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 mean diameter using laser diffraction from a representative sample of the microgranule population comprises: (a) at least 10% of the microgranule population having a volume-weighted particle size equal to or larger than 470 micrometers; and (b) 50% of the microgranule population having a volume-weighted particle size in a range of from 640 micrometers to 810 micrometers; and (c) 90% of the microgranule population having a volume-weighted particle size smaller than 1170 micrometers; wherein each microgranule comprises a sugar core or a microcrystalline cellulose core, and a layer outside of the sugar core or the microcrystalline cellulose core, the layer comprising secnidazole; wherein the therapeutically effective amount of secnidazole is an amount of secnidazole that exhibits a maximum plasma concentration (Cmax) of secnidazole in the subject of about 34.5 .mu.g/ml to about 58.3 .mu.g/ml; and wherein 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 microgranule formulation is a taste-masked microgranule formulation. 4. The method of claim 1, wherein each microgranule further comprises an outer coat on top of the layer outside of the sugar core or the microcrystalline cellulose core. 5. The method of claim 1, wherein each microgranule further comprises at least one compound selected from the group consisting of povidone, polyethylene glycol, ethyl acrylate-methyl methacrylate copolymer, and talc. 6. The method of claim 1, wherein the microgranule formulation is administered to the subject by mixing or combining it with a food substance or a liquid. 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 a female with confirmed bacterial vaginosis or a female with suspected bacterial vaginosis. 10. The method of claim 9, wherein the female with confirmed bacterial vaginosis presents thin, homogeneous vaginal discharge, a positive KOH Whiff test, vaginal fluid pH greater than or equal to 4.7, the presence of clue cells greater than 20% of total epithelial cells, and a gram stain slide Nugent score equal to or higher than four on bacterial analysis of vaginal samples. 11. The method of claim 9, wherein the female with suspected bacterial vaginosis presents with thin, homogeneous vaginal discharge, a positive KOH Whiff test, vaginal fluid pH greater than or equal to 4.7, and the presence of clue cells greater than 20% of total epithelial cells. 12. The method of claim 1, wherein the therapeutically effective amount of secnidazole in the microgranule formulation is administered as a single dose. 13. The method of claim 12, 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 bacterial vaginosis. 14. The method of claim 1, wherein the therapeutically effective amount of secnidazole in the microgranule formulation is 2 grams. 15. 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, and a combination thereof. 16. The method of claim 15, wherein the additional compound is administered on the same day as the therapeutically effective amount of secnidazole in the microgranule formulation. 17. The method of claim 15, wherein the additional compound is administered on a different day than the therapeutically effective amount of secnidazole in the microgranule formulation. 18. The method of claim 15, wherein the secnidazole microgranule formulation does not affect the contraceptive efficacy of the additional compound selected from ethinyl estradiol, norethindrone, or a combination thereof. 19. The method of claim 1, wherein the subject has a resolution of one or more symptoms of bacterial vaginosis within up to about seven days after administration. 20. The method of claim 1, wherein the subject has an alleviation of one or more symptoms of bacterial vaginosis within up to about three days after administration. 21. A method of treating bacterial vaginosis 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 mean diameter using laser diffraction from a representative sample of the microgranule population comprises: (a) at least 10% of the microgranule population having a volume-weighted particle size about equal to or larger than 470 micrometers; and (b) 50% of the microgranule population having a volume-weighted particle size in a range of from 640 micrometers to 810 micrometers; and (c) 90% of the microgranule population having a volume-weighted particle size smaller than 1170 micrometers; wherein each microgranule comprises a sugar core or a microcrystalline cellulose core, and a layer outside of the sugar core or the microcrystalline cellulose core, the layer comprising secnidazole; wherein the therapeutically effective amount of secnidazole is an amount of secnidazole that exhibits a time to maximum plasma concentration (Tmax) of secnidazole in the subject of about 2 hours to about 6 hours; and wherein secnidazole is the sole drug in the microgranule formulation. 22. The method of claim 21, wherein the Tmax is about 3 hours to about 4 hours. 23. The method of claim 1, wherein the sugar core is a sugar sphere core. 24. The method of claim 21, wherein the sugar core is a sugar sphere core. 25. The method of claim 21, wherein the microgranule formulation is a taste-masked microgranule formulation. 26. The method of claim 21, wherein each microgranule further comprises an outer coat on top of the layer outside of the sugar core or the microcrystalline cellulose core. 27. The method of claim 21, wherein each microgranule further comprises at least one compound selected from the group consisting of povidone, polyethylene glycol, ethyl acrylate-methyl methacrylate copolymer, and talc. 28. The method of claim 21, wherein the therapeutically effective amount of secnidazole in the microgranule formulation is 2 grams.