STEROID HORMONE PHARMACEUTICAL FORMULATIONS
This disclosure provides pharmaceutical compositions for delivering estradiol to a subject in need thereof, as well as methods of administering the compositions, and methods of using them.
1 . A vaginal insert comprising a therapeutically effective amount of estradiol; and a solubilizing agent, wherein the solubilizing agent comprises at least one C 2 -C 5 fatty acid or a glycol ester, monoglyceride, diglyceride, or triglyceride thereof.
2 . The vaginal insert of claim 1 , wherein the therapeutically effective amount of estradiol is from about 1 microgram to about 25 micrograms.
3 .- 6 . (canceled)
7 . The vaginal insert of claim 1 , further comprising a second solubilizing agent selected from the group consisting of a mixture of PEG-6 stearate, ethylene glycol palmitostearate, and PEG-32 stearate; a mixture of hard fat, glyceryl ricinoleate, ceteth-20, and steareth-20; polyoxyl 40 hydrogenated castor oil USP; hard fat polyoxyl 20 cetostearyl ether; and combinations thereof.
8 . The vaginal insert of claim 7 , wherein the second solubilizing agent is a mixture of PEG-6 stearate, ethylene glycol palmitostearate, and PEG-32 stearate.
9 . The vaginal insert of claim 1 , wherein the viscosity of the composition is about 5 cP to about 3000 cP at room temperature.
10 . (canceled)
11 . The vaginal insert of claim 1 , wherein the insert further comprises a capsule encapsulating the therapeutically effective amount of estradiol and the solubilizing agent.
12 . (canceled)
13 . The vaginal insert of claim 1 , wherein the solubilizing agent comprises at least one C 3 fatty acid or a glycol mono- or di-ester thereof, a monoglyceride, diglyceride, or triglyceride thereof, or a combination of any of the foregoing.
14 . A vaginal insert comprising:
(a) a therapeutically effective amount of estradiol;
(b) a first solubilizing agent comprising one or more polyethylene glycol mono- or di-esters of a hydroxy C 16 -C 26 fatty acid; and
(c) a second solubilizing agent comprising a mixture of PEG-6 stearate, ethylene glycol palmitostearate, and PEG-32 stearate.
15 . The vaginal insert of claim 14 , wherein the therapeutically effective amount of estradiol is from about 1 microgram to about 25 micrograms.
16 .- 20 . (canceled)
21 . The vaginal insert of claim 14 , wherein the insert further comprises a capsule encapsulating the estradiol, the first solubilizing agent, and the second solubilizing agent.
22 . (canceled)
23 . A vaginal insert comprising:
(d) a therapeutically effective amount of estradiol;
(e) a first solubilizing agent comprising propylene glycol monolaurate; and
(f) a second solubilizing agent comprising polyoxyl 40 hydrogenated castor oil USP.
24 . The vaginal insert of claim 23 , wherein the therapeutically effective amount of estradiol is from about 1 microgram to about 25 micrograms.
25 .- 28 . (canceled)
29 . The vaginal insert of claim 23 , wherein the viscosity of the composition is about 5 cP to about 3000 cP at room temperature.
30 . (canceled)
31 . The vaginal insert of claim 23 , wherein the insert further comprises a capsule encapsulating the estradiol, the first solubilizing agent, and the second solubilizing agent.
32 . (canceled)
33 . A method of treating an estrogen-deficient state, comprising administering to a female in need thereof, the vaginal insert of claim 1 .
34 . (canceled)
35 . The method of claim 33 , wherein the estrogen-deficient state is selected from the group consisting of vulvovaginal atrophy, dysuria, dyspareunia, estrogen-deficient urinary state, and vaginal bleeding associated with sexual activity.
36 . (canceled)
37 . A method of treating an estrogen-deficient state, comprising administering to a female in need thereof, the vaginal insert of claim 14 .
38 . (canceled)
39 . The method of claim 37 , wherein the estrogen-deficient state is selected from the group consisting of vulvovaginal atrophy, dysuria, dyspareunia, estrogen-deficient urinary state, and vaginal bleeding associated with sexual activity.
40 . (canceled)
41 . A method of treating an estrogen-deficient state, comprising administering to a female in need thereof, the vaginal insert of claim 23 .
42 . (canceled)
43 . The method of claim 41 , wherein the estrogen-deficient state is selected from the group consisting of vulvovaginal atrophy, dysuria, dyspareunia, estrogen-deficient urinary state, and vaginal bleeding associated with sexual activity.
44 . (canceled)