Claims for Patent: 10,537,581

Summary for Patent: 10,537,581

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:	14/521,230
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 10,537,581
Patent Claims:	1. A pessary consisting of: a) a liquid pharmaceutical composition comprising: about 1 .mu.g to about 25 .mu.g of estradiol; and a solubilizing agent comprising a medium chain oil; wherein the viscosity of the liquid pharmaceutical composition ranges from about 50 cP to about 1000 cP at 25 .degree. C., and wherein the liquid pharmaceutical composition does not include a hydrophilic gel-forming bioadhesive agent; and b) a soft gelatin capsule encapsulating the liquid pharmaceutical composition; wherein estradiol is the only active hormone in the pessary; and wherein the pessary is for intravaginal administration. 2. The pessary of claim 1, wherein the liquid pharmaceutical composition comprises about 1 .mu.g to about 10 .mu.g of estradiol. 3. The pessary of claim 1, wherein the liquid pharmaceutical composition comprises about 10 .mu.g to about 25 .mu.g of estradiol. 4. The pessary of claim 1, wherein the estradiol is solubilized. 5. The pessary of claim 1, wherein the medium chain oil comprises at least one C6-C12 fatty acid or a glycol, monoglyceride, diglyceride, or triglyceride ester thereof. 6. The pessary of claim 5, wherein each glycol, monoglyceride, diglyceride, or triglyceride ester of the C6-C12 fatty acid is independently an ester of caproic acid, an ester of caprylic acid, or an ester of capric acid. 7. The pessary of claim 6, wherein the triglyceride ester of the C6-C12 fatty acid is a caprylic/capric triglyceride. 8. A pessary consisting of: a) a liquid pharmaceutical composition comprising: about 1 .mu.g to about 25 .mu.g of estradiol; a caprylic/capric triglyceride; and a non-ionic surfactant comprising PEG-6 stearate and ethylene glycol palmitostearate; wherein the viscosity of the liquid pharmaceutical composition ranges from about 50 cP to about 1000 cP at 25.degree. C., and wherein the liquid pharmaceutical composition does not include a hydrophilic gel-forming bioadhesive agent; and b) a soft gelatin capsule encapsulating the liquid pharmaceutical composition, wherein estradiol is the only active hormone in the pessary; and wherein the pessary is for intravaginal administration. 9. A pessary consisting of: (a) a liquid pharmaceutical composition comprising: about 1 .mu.g to about 25 .mu.g of estradiol and a solubilizing agent comprising a medium chain oil, wherein the viscosity of the liquid pharmaceutical composition ranges from about 50 cP to about 1000 cP at 25 .degree. C., and wherein the liquid pharmaceutical composition does not include a hydrophilic gel-forming bioadhesive agent; and (b) a soft gelatin capsule encapsulating the liquid pharmaceutical composition; wherein estradiol is the only active hormone in the pessary; and wherein administration of the pessary to the proximal region of the vagina of a patient provides a therapeutically effective concentration of estradiol over 24 hours in the proximal region of the vagina. 10. A method of treating an estrogen-deficient state, the method comprising administering to a patient in need thereof a pessary according to claim 1. 11. A method of treating an estrogen-deficient state, the method comprising administering to a patient in need thereof, a pessary according to claim 8.