Claims for Patent: 12,303,518

Summary for Patent: 12,303,518

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):	Bruce Variano
Assignee:	Population Council Inc
Application Number:	US17/520,323
Patent Claims:	1. A vaginal system for preventing pregnancy, the system comprising: a) a methyl siloxane-based polymer ring body, wherein the methyl siloxane-based polymer comprised in the ring body has a hydride/vinyl ratio from approximately 1:1 to approximately 1.3:1 before curing, the ring body having an overall diameter of 56 mm and a cross-sectional diameter of approximately 8 mm, and comprising: i. a first cylindrical channel having a length of approximately 27 mm and a diameter of approximately 3 mm wherein the channel is adapted to receive a first cylindrical core; ii. a second cylindrical channel having a length of approximately 27 mm and a diameter of approximately 3 mm wherein the channel is adapted to receive a second cylindrical core; and iii. TiO2; b) a first cylindrical core disposed within the first cylindrical channel, wherein the first cylindrical core has a diameter of approximately 3 mm and comprises at least one silicone elastomer, dibutyltin dilaurate, and a viscosity agent; c) a second cylindrical core disposed within the second cylindrical channel, wherein the second cylindrical core has a diameter of approximately 3 mm and comprises at least one silicone elastomer 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 and wherein the segesterone acetate has a particle size D90 of not more than 10 microns; wherein the methyl siloxane-based polymer ring body further comprises a platinum concentration of approximately 3 ppm to approximately 10 ppm and a plurality of ethinyl estradiol molecules covalently linked to the methyl siloxane-based polymer as shown in Formula I further wherein approximately 80% to approximately 90% of the ethinyl estradiol is recoverable from the system after approximately 18 months of storage at 25° C. and 60% relative humidity; and wherein the methyl siloxane-based polymer 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%; further wherein the vaginal system achieves in a plasma sample of a female patient: i. a segesterone acetate Cmax of approximately 1,147 pg/mL+/−315 μg/mL over a twenty-one day first period during a first product-use cycle; ii. a segesterone acetate Cavg of approximately 191 μg/mL+/−34 μg/mL over a twenty-one day first period during a first product-use cycle; iii. a segesterone acetate AUC0-21 day of approximately 96.2 ng*hr/mL+/−16.9 ng*hr/mL over a twenty-one days first period during a first product-use cycle; iv. an ethinyl estradiol Cmax of approximately 129 μg/mL+/−39 μg/mL of ethinyl estradiol over a twenty-one day first period during the first product-use cycle; v. an ethinylestradiol Cavg of approximately 44 pg/mL+/−19 μg/mL over a twenty-one day first period during the first product-use cycle; and vi. an ethinyl estradiol AUC0-21 day of approximately 22.2 ng*hr/mL+/−9.8 ng*hr/mL over a twenty-one day first period during the first product-use cycle. 2. The vaginal system of claim 1, wherein the ethinyl estradiol is present in the cores in a first polymorphic form and a second polymorphic form. 3. The vaginal system claim 1, wherein the methyl siloxane-based polymer ring body has a specific gravity from approximately 1 to approximately 1.5. 4. The vaginal system of claim 3, wherein the methyl siloxane polymer-based ring body has a specific gravity of from approximately 1.07 to approximately 1.17. 5. The vaginal system of claim 1, wherein the total weight of the vaginal system is approximately 9 grams. 6. The vaginal system of claim 1, wherein after 36 months of storage the system comprises a total percentage of ethinyl estradiol and segesterone acetate degradation products of not more than 5 Liquid Chromatography Area Percent. 7. The vaginal system of claim 1, further comprising one or more suitable medical adhesives. 8. The vaginal system of claim 7, wherein the one or more medical adhesives comprise 15-25% trimethylsilanamine and less than 5% methylsilanetriol triacetate. 9. The vaginal system of claim 1, wherein the methyl siloxane-based polymer ring body is prepared from a first component and a second component, wherein each component comprises uncured vinyl-terminated silicone polymers. 10. The vaginal system of claim 9, wherein the first component comprises 65-75% mono(vinyl group) terminated dimethylsiloxanes and dimethylsilicones and the second component comprises 65-75% mono(vinyl group) terminated dimethylsiloxanes and dimethylsilicones, 10-15% diloxanes and silicones (dimethyl and methyl) and a platinum catalyst. 11. The vaginal system of claim 10, wherein the methyl siloxane-based polymer ring body is prepared by mixing an approximately 9:1 to approximately 11:1 ratio of the first component to the second component. 12. The vaginal system of claim 1, wherein the release rate of ethinyl estradiol from the system 48 hours after initial insertion is about 62 μg/mL. 13. The vaginal system of claim 1, wherein the release rate of ethinyl estradiol from the system 48 hours after initial insertion is about 50 μg/mL. 14. The vaginal system of claim 1, wherein the release rate of ethinyl estradiol from the system 48 hours after initial insertion is about 45 μg/mL. 15. The vaginal system of claim 1, wherein the ethinyl estradiol achieves steady state from about 168 and about 504 hours after initial insertion.