Vaginal inserted estradiol pharmaceutical compositions and methods
View Patent ↗In one aspect, compositions and methods for the treatment of vulvovaginal atrophy (VVA) are provided. In one embodiment, the method comprises administering an estrogen to a subject having VVA by inserting a dosage form comprising a liquid pharmaceutical composition.
1. A method for treating moderate to severe dyspareunia in a human subject comprising:
intravaginally administering estradiol to the subject by manually inserting about two inches into the vagina a liquid pharmaceutical composition comprising about 4 μg to about 25 μg of estradiol, wherein the composition has a viscosity from about 50 cP to about 1000 cP at 25° C., wherein the composition comprises all of the estradiol and is encapsulated in a capsule, and wherein the composition is inserted while the subject is in a reclining position or in a standing position;
wherein administration of the composition results in a decrease in the severity of moderate to severe dyspareunia in the subject within two to six weeks from the first administration.
2. The method of claim 1 , wherein the method further comprises instructing the subject that once the composition has been administered, the subject may be ambulatory.
3. The method of claim 1 , wherein the capsule is a soft gelatin capsule.
4. The method of claim 1 , wherein administration of the composition results in an increase in the percentage of vaginal superficial cells within two weeks from the first administration.
5. The method of claim 1 , wherein administration of the composition results in a decrease in the percentage of vaginal parabasal cells within two weeks from the first administration.
6. The method of claim 1 , wherein administration of the composition results in a decrease in vaginal pH within two weeks from the first administration.
7. The method of claim 1 , wherein the administration comprises inserting the composition once daily for two weeks and twice weekly thereafter.
8. The method of claim 1 , wherein the moderate to severe dyspareunia is due to menopause.
9. The method of claim 1 , wherein the composition contains 4 μg estradiol or 10 μg estradiol.
10. The method of claim 1 , wherein the viscosity of the composition is from about 50 cP to about 380 cP at 25° C.