Claims for Patent: 10,940,157

Summary for Patent: 10,940,157

Title:	System for providing birth control
Abstract:	The present disclosure relates to a vaginal system that prevents pregnancy comprised of segesterone acetate and ethinyl estradiol and is configured for thirteen 28-day product-use cycles.
Inventor(s):	Variano; Bruce (New York, NY)
Assignee:	The Population Council, Inc. (New York, NY)
Application Number:	16/814,724
Patent Claims:	1. A reusable vaginal ring system for preventing pregnancy comprising: a) a silicone elastomer ring body, the ring body comprising a silicone elastomer having a platinum concentration of approximately 3 ppm to approximately 10 ppm and a hydride/vinyl ratio from approximately 1:1 to approximately 1.3:1 before curing; and i. a first cylindrical channel adapted to receive a first cylindrical core; and ii. a second cylindrical channel adapted to receive a second cylindrical core; b) a first cylindrical core disposed within the first cylindrical channel, wherein the first cylindrical core comprises first and second condensation-cure silicone elastomers, dibutyltin dilaurate, and a viscosity agent selected from the group consisting of diatomaceous earth, cellulose, talc, and silica; c) a second cylindrical core disposed within the second cylindrical channel, the second cylindrical core comprising a third condensation-cure silicone elastomer, wherein the second and third condensation-cure silicone elastomers are optionally the same, and dibutyltin dilaurate; and d) approximately 103 mg of segesterone acetate and approximately 17.4 mg of ethinyl estradiol, wherein both the segesterone acetate and ethinyl estradiol are contained within the cores of the vaginal ring system; wherein the first cylindrical core comprises approximately 50% segesterone acetate by mass; the second cylindrical core comprises approximately 40% segesterone acetate by mass and approximately 12% ethinyl estradiol by mass; the first and second cylindrical cores have a volume ratio of about 11:18; further wherein the system releases an approximate average of 0.15 mg/day of segesterone acetate and an approximate average of 0.013 mg/day of ethinyl estradiol, or bioequivalent amounts thereof, for up to 13 cycles of 21 days per cycle; and wherein approximately 80% to approximately 90% of the ethinyl estradiol is recoverable from the system after approximately 18 months of storage at 25.degree. C. and 60% relative humidity and wherein no more than approximately 10% to approximately 20% of the ethinyl estradiol undergoes hydrosilylation with unreacted hydrosilane in the ring body after approximately 18 months of storage at 25.degree. C. and 60% relative humidity; further wherein the contraceptive ring system achieves in a plasma sample of a female patient: i. a segesterone acetate C.sub.max of approximately 1,147 pg/mL+/-315 pg/mL of segesterone acetate over a twenty-one day first period during a first product-use cycle; ii. a segesterone acetate C.sub.max of approximately 363 pg/mL+/-133 pg/mL of segesterone acetate over a twenty-one day first period during a third product-use cycle; iii. a segesterone acetate C.sub.max of approximately 294 pg/mL+/-116 pg/mL of segesterone acetate over a twenty-one days first period during a thirteenth product-use cycle; iv. an ethinyl estradiol C.sub.max of approximately 129 pg/mL+/-39 pg/mL of ethinyl estradiol over a twenty-one day first period during the first product-use cycle; v. an ethinyl estradiol C.sub.max of approximately 60 pg/mL+/-32 pg/mL of ethinyl estradiol over a twenty-one day first period during the third product-use cycle; and vi. an ethinyl estradiol C.sub.max of approximately 39 pg/mL+/-16 pg/mL of ethinyl estradiol over a twenty-one day first period during the thirteenth product-use cycle. 2. The vaginal system of claim 1, wherein the first cylindrical core has a length of approximately 11 mm. 3. The vaginal system of claim 1, wherein the second cylindrical core has a length of approximately 18 mm. 4. The vaginal system of claim 1, wherein the first cylindrical core has a diameter of approximately 3 mm. 5. The vaginal system of claim 1, wherein the second cylindrical core has a diameter of approximately 3 mm. 6. The vaginal system of claim 1, wherein the first and second cylindrical channels each have a diameter of approximately 3 mm. 7. The vaginal system of claim 1, wherein the first and second cylindrical cores are secured in the first and second channels, respectively, with an adhesive. 8. The vaginal system of claim 1, wherein the first cylindrical core is substantially longitudinally centered in the first cylindrical channel, further wherein the second cylindrical core is substantially longitudinally centered within the second cylindrical channel. 9. The vaginal system of claim 1, wherein a) the first cylindrical core has a first end face and a second end face, wherein the first cylindrical core is fully disposed within the first cylindrical channel; b) the second cylindrical core has a first end face and a second end face, wherein the second cylindrical core is fully disposed within the second cylindrical channel; and c) an end face of the first cylindrical core is substantially coplanar with an end face of the second cylindrical core. 10. The vaginal system of claim 1, wherein the first cylindrical channel and the second cylindrical channels each have lengths of approximately 27 mm. 11. The vaginal system of claim 1, wherein the ring body has outer diameter, an inner diameter, and a cross-sectional diameter. 12. The vaginal system of claim 11, wherein the outer diameter is approximately 56 mm. 13. The vaginal system of claim 12, wherein the inner diameter is approximately 40 mm. 14. The vaginal system of claim 13, wherein the cross-sectional diameter is approximately 8.4 mm. 15. The vaginal system of claim 1, wherein the silicone elastomer has a platinum concentration of approximately 4 ppm to approximately 9 ppm. 16. The vaginal system of claim 15, wherein the silicone elastomer has a platinum concentration of approximately 5 ppm to approximately 8 ppm. 17. The vaginal system of claim 1, wherein the silicone elastomer ring body has a shore A hardness of approximately 25 to approximately 30, a mean fatigue parallel to the cores of approximately 95% and a mean fatigue perpendicular to the cores of approximately 98%. 18. The vaginal system of claim 1, wherein the first cylindrical core is impregnated with a first amount of segesterone acetate particles having a particle size distribution: D90 of not more than 10 microns and a D50 of not more than 5 microns; further wherein in the second cylindrical core is impregnated with a second amount of segesterone acetate particles and an amount of ethinyl estradiol particles, wherein the ethinyl estradiol particles have a particle size distribution of 100% max 15 microns, 99% max 12.5 microns, 95% max 10 microns and max 40% less than or equal to 1.3 microns. 19. The vaginal system of claim 1, wherein at least 75% of the segesterone acetate comprises segesterone acetate Polymorphic form I. 20. The vaginal system of claim 1, wherein the segesterone acetate comprises up to 25% segesterone acetate Polymorphic form II. 21. The vaginal system of claim 8, wherein any void spaces in the first and second cylindrical channels not occupied by the first and second cylindrical cores are filled with adhesive. 22. The vaginal system of claim 9, wherein any void spaces in the first and second cylindrical channels not occupied by the first and second cylindrical cores are filled with adhesive. 23. The vaginal system of claim 1, wherein after 18 months of storage, at least one degradation product selected from the group consisting of 6.alpha.-OH-EE, 6.beta.-OH-EE, 6.alpha.-OH-NES, 6.beta.-OH-NES, 17.beta.-estradiol, NES ST-alcohol, NES iso-ST-alcohol, 6,7-didehydro-EE & 9,11-didehydro-EE, estrone, .DELTA..sup.6-NES, Iso-NES, 3-enolacetate-NES, 3-methoxy-NES, and combinations thereof, is detectable but does not account for more than 5% of ring extractables as measured by HPLC. 24. The method of claim 23, wherein the at least one degradation product is detectable but does not account for more than 1% of ring extractables as measured by HPLC. 25. The vaginal system of claim 1, wherein the first and second cylindrical channels are substantially parallel to each other.