Granted Patent B2

US 12,702,641 · App. 18/061,082 · Granted Aug 11, 2026

Inventor: Bruce Variano (White Plains, NY)

Assignee: The Population Council, Inc.

A61K9/0036A61K31/565A61K31/57A61P15/18

Abstract

Claims (31)

1 . A process for preparing a reusable vaginal ring system for preventing pregnancy configured to release an approximate average of 0.15 mg/day of segesterone acetate and an approximate average of 0.013 mg/day of ethinyl estradiol for up to 13 cycles of 21 days each, the process comprising:

a) adding an uncured addition-cure 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 to a mold configured to provide a ring body comprising two channels adapted to receive first and second drug-containing cores;

b) curing the uncured addition-cure silicone elastomer in the mold to provide a ring body comprising first and second channels adapted to receive first and second drug-containing cores;

c) removing the ring body from the mold; and

d) inserting the first drug-containing core into the first channel and inserting the second drug-containing core into the second channel, wherein the first and second drug-containing cores contain, in total, approximately 103 mg of segesterone acetate, and approximately 17.4 mg of ethinyl estradiol and wherein the first drug-containing core contains segesterone acetate and the second drug-containing core contains segesterone acetate and ethinyl estradiol.

2 . The process of claim 1 , wherein the first drug-containing core comprises approximately 50% segesterone acetate by mass.

3 . The process of claim 1 , wherein the second drug-containing core comprises approximately 40% segesterone acetate by mass and approximately 12% ethinyl estradiol by mass.

4 . The process of claim 1 , wherein the first and second drug-containing cores comprise segesterone acetate having a particle size distribution: D90 of not more than 10 microns and a D50 of not more than 5 microns.

5 . The process of claim 1 , wherein at least 75% of the segesterone acetate within the first and second drug-containing cores comprises segesterone acetate Polymorphic form I.

6 . The process of claim 1 , wherein the segesterone acetate within the first and second drug-containing cores comprises up to 25% segesterone acetate Polymorphic form II.

7 . The process of claim 1 , wherein the second drug-containing core comprises ethinyl estradiol particles having 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.

8 . The process of claim 7 , wherein the first and second drug-containing cores have a volume ratio of about 11:18.

9 . The process of claim 1 , wherein the second drug-containing core is aged for at least 30 days before being inserted into the ring body.

10 . The process of claim 7 , wherein the first drug-containing core is prepared by:

a) adding segesterone acetate to one or more uncured condensation-cure silicone elastomers to form a segesterone acetate uncured elastomer mixture;

b) adding a curing agent to the segesterone acetate uncured elastomer mixture to form a second mixture;

c) shaping the second mixture into strings; and

d) curing the strings to form the first drug-containing core.

11 . The process of claim 10 , further comprising cutting the strings after curing.

12 . The process of claim 10 , wherein the curing agent is dibutyltin dilaurate.

13 . The process of claim 10 , wherein the curing occurs at a temperature of about 60° C. to about 120° C.

14 . The process of claim 1 , wherein the second drug-containing core is prepared by:

a) adding ethinyl estradiol to one or more uncured condensation-cure silicone elastomers to form an ethinyl estradiol uncured elastomer mixture;

b) adding segesterone acetate to the ethinyl estradiol uncured elastomer mixture to form a segesterone acetate ethinyl estradiol uncured mixture;

c) adding a curing agent to the segesterone acetate ethinyl estradiol uncured mixture to form a third mixture;

d) shaping the third mixture into strings; and

e) curing the strings to form the second drug-containing core.

15 . The process of claim 14 , further comprising cutting the strings after curing.

16 . The process of claim 14 , wherein the curing agent is dibutytin dilaurate.

17 . The process of claim 14 , wherein the curing occurs at a temperature from approximately 60° C. to approximately 90° C.

18 . The process of claim 14 , wherein the curing occurs at a relative humidity of approximately 1% to approximately 2%.

Assignments (1)

Continuity (3)

References Cited (121)