Claims for Patent: 11,351,182

Summary for Patent: 11,351,182

Title:	Vaginal inserted estradiol pharmaceutical compositions and methods
Abstract:	According to various embodiments of this disclosure, pharmaceutical compositions comprising solubilized estradiol are provided. In various embodiments, such compositions are encapsulated in soft capsules which may be vaginally inserted for the treatment of vulvovaginal atrophy.
Inventor(s):	Bernick; Brian A. (Boca Raton, FL), Thorsteinsson; Thorsteinn (Boynton Beach, FL), Persicaner; Peter H. R. (Boca Raton, FL), Cacace; Janice Louise (St. Petersburg, FL), Sancilio; Frederick D. (Stuart, FL), Irani; Neda (Palm Beach Gardens, FL), Amadio; Julia (Boca Raton, FL)
Assignee:	TherapeuticsMD, Inc. (Boca Raton, FL)
Application Number:	16/833,186
Patent Claims:	1. A method for treating vulvovaginal atrophy 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 .mu.g to about 25 .mu.g of estradiol, about 90 wt % of a mixture of caprylic and capric triglyceride, and about 10 wt % of a mixture of PEG-6 stearate, ethylene glycol palmitostearate and PEG-32 stearate, wherein the composition has a viscosity from about 50 cP to about 1000 cP at 25.degree. C., wherein estradiol is the only active hormone in the composition, 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 vulvovaginal atrophy in the subject within two to six weeks from the first administration. 2. The method of claim 1, wherein the capsule is a soft gelatin capsule. 3. 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. 4. 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. 5. The method of claim 1, wherein administration of the composition results in a decrease in vaginal pH within two weeks from the first administration. 6. The method of claim 1, wherein the administration comprises inserting the composition once daily for two weeks and twice weekly thereafter. 7. The method of claim 1, wherein the vulvovaginal atrophy is due to menopause. 8. The method of claim 1, wherein the composition contains 4 .mu.g estradiol or 10 .mu.g estradiol. 9. The method of claim 1, wherein the viscosity of the composition is from about 50 cP to about 380 cP at 25.degree. C.