Claims for Patent: 11,000,507

Summary for Patent: 11,000,507

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) 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):	Helen S. PENTIKIS, David Palling, Carol J. BRAUN, Richard Holl
Assignee:	Evofem Biosciences Inc
Application Number:	US16/817,246
Patent Claims:	1. A method of treating bacterial vaginosis in a subject in need thereof comprising: administering to the subject a therapeutically effective amount of secnidazole in a microgranule formulation, wherein the microgranule formulation comprises a plurality of microgranules, 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 secnidazole, at least 10% of the plurality of microgranules have a volume-weighted particle diameter equal to or larger than 470 micrometers as measured by laser diffraction; wherein the microgranule formulation provides a maximum plasma concentration (Cmax) of secnidazole in the subject of about 34.5 μg/ml to about 58.3 μg/ml; and 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 microgranule formulation is a taste-masked microgranule formulation. 4. The method of claim 1, wherein the sugar core is a sugar sphere core. 5. The method of claim 1, wherein the microgranule formulation 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 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, or 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 microgranule formulation does not affect a contraceptive efficacy of an 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 therapeutically effective amount of secnidazole in a microgranule formulation, wherein the microgranule formulation comprises a plurality of microgranules, 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 secnidazole, wherein at least 10% of the plurality of microgranules have a volume-weighted particle diameter equal to or larger than 470 micrometers as measured by laser diffraction; wherein 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. 22. The method of claim 21, wherein the Tmax of secnidazole is about 3 hours to about 4 hours. 23. The method of claim 21, wherein the therapeutically effective amount of secnidazole in the microgranule formulation is administered orally. 24. The method of claim 21, wherein the microgranule formulation is a taste-masked microgranule formulation. 25. The method of claim 21, wherein the sugar core is a sugar sphere core. 26. The method of claim 21, wherein the microgranule formulation 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. 27. The method of claim 21, wherein the therapeutically effective amount of secnidazole in the microgranule formulation is 2 grams. 28. The method of claim 21, wherein the method reduces the incidence or risk of the subject acquiring a sexually transmitted infection (STI) from a sexual partner. 29. The method of claim 28, wherein the STI comprises chlamydia, gonorrhea, trichomoniasis, herpes simplex virus type 2 (HSV-2) or human papillomavirus (HPV). 30. The method of claim 28, wherein the STI is trichomoniasis. 31. The method of claim 1, wherein the method reduces the incidence or risk of the subject acquiring a STI from a sexual partner. 32. The method of claim 31, wherein STI comprises chlamydia, gonorrhea, trichomoniasis, HSV-2 or HPV. 33. The method of claim 31, wherein STI is trichomoniasis.