Claims for Patent: 11,602,522

Summary for Patent: 11,602,522

Title:	Secnidazole for use in the treatment of sexually transmitted infection
Abstract:	Method of treating sexually transmitted infection 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. Pharmaceutical compositions and uses thereof are included herein.
Inventor(s):	Helen S. PENTIKIS, David Palling, Carol J. BRAUN, Richard Holl
Assignee:	Evofem Biosciences Inc
Application Number:	US17/314,833
Patent Claims:	1. A method of treating a sexually transmitted infection (STI) in a subject in need thereof, the method 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 comprises 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 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 STI is chlamydia, gonorrhea, bacterial vaginosis, trichomoniasis, herpes simplex virus type 2 (HSV-2), human papillomavirus (HPV), or a combination thereof. 3. The method of claim 1, wherein the therapeutically effective amount of secnidazole in the microgranule formulation is administered orally. 4. The method of claim 1, wherein the microgranule formulation is a taste-masked formulation. 5. The method of claim 1, wherein the sugar core is a sugar sphere core. 6. 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 acetate and methyl methacrylate, and talc. 7. The method of claim 1, wherein the microgranule formulation is integrated into a food substance or a liquid prior to administration. 8. The method of claim 7, wherein the food substance is a liquid, semisolid or soft food. 9. The method of claim 1, wherein the therapeutically effective amount of secnidazole in the microgranule formulation is administered as a single dose. 10. The method of claim 1, wherein the therapeutically effective amount of secnidazole in the microgranule formulation is 2 grams. 11. 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. 12. The method of claim 11, wherein the additional compound is administered on the same day as the therapeutically effective amount of secnidazole in the microgranule formulation. 13. The method of claim 11, wherein the additional compound is administered on a different day as the therapeutically effective amount of secnidazole in the microgranule formulation. 14. The method of claim 11, wherein the microgranule formulation does not affect a contraceptive efficacy of the additional compound selected from ethinyl estradiol, norethindrone or a combination thereof. 15. A method of treating a sexually transmitted infection (STI) in a subject in need thereof, the method 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 comprises 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. 16. The method of claim 15, wherein the STI is chlamydia, gonorrhea, bacterial vaginosis, trichomoniasis, HSV-2, HPV, or a combination thereof. 17. The method of claim 15, wherein the Tmax of secnidazole is about 3 hours to about 4 hours. 18. A method of treating trichomoniasis in a subject in need thereof, the method 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 comprises 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 maximum plasma concentration (Cmax) of secnidazole in the subject of about 34.5 μg/ml to about 58.3 μg/ml or 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. 19. A pharmaceutical composition comprising 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 comprises 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 maximum plasma concentration (Cmax) of secnidazole in the subject of about 34.5 μg/ml to about 58.3 μg/ml or 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. 20. The pharmaceutical composition of claim 19, wherein the volume-weighted particle size distribution as measured by laser diffraction from a representative sample of the microgranule population further comprises (a) 50% of the microgranule population having a volume-weighted particle diameter size in a range of from 640 micrometers to 810 micrometers, and (b) 90% of the microgranule population having a volume-weighted particle diameter smaller than 1170 micrometers. 21. A method for treating an STI in a subject in need thereof, the method comprising co-administering the pharmaceutical composition of claim 19 to the subject with an additional compound selected from the group consisting of ethinyl estradiol, norethindrone, and a combination thereof. 22. The method of claim 21, wherein the STI is chlamydia, gonorrhea, bacterial vaginosis, trichomoniasis, HSV-2, HPV, or a combination thereof.