➤ Get the DrugPatentWatch Daily Briefing

Get Daily Updates on Generic Entry, Litigation, Biosimilars, and more …

Serving leading biopharmaceutical companies globally:

McKinsey
Johnson and Johnson
Colorcon
Baxter
Boehringer Ingelheim
Merck

Last Updated: December 1, 2020

DrugPatentWatch Database Preview

Claims for Patent: 9,180,091

➤ Get the DrugPatentWatch Daily Briefing
» See Plans and Pricing

« Back to Dashboard

Summary for Patent: 9,180,091
Title:Soluble estradiol capsule for vaginal insertion
Abstract: According to various embodiments of this disclosure, pharmaceutical formulations comprising solubilized estradiol are provided. In various embodiments, such formulations are encapsulated in soft capsules which may be vaginally inserted for the treatment of vulvovaginal atrophy.
Inventor(s): Bernick; Brian A. (Boca Raton, FL), Amadio; Julia M. (Boca Raton, FL), Persicaner; Peter H. R. (Boca Raton, FL), Irani; Neda (Palm Beach Gardens, FL), Cacace; Janice Louise (Miami, FL), Thorsteinsson; Thorsteinn (Boca Raton, FL), Sancilio; Frederick D. (Palm Beach Gardens, FL)
Assignee: TherapeuticsMD, Inc. (Boca Raton, FL)
Application Number:14/136,048
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 9,180,091
Patent Claims: 1. A vaginal suppository comprising: a) a therapeutically effective amount of estradiol; and b) a solubilizing agent, wherein the solubilizing agent comprises at least one C6-C12 fatty acid or a glycol, monoglyceride, diglyceride, or triglyceride ester thereof; wherein the vaginal suppository comprises from about 1 micrograms to about 25 micrograms of estradiol; wherein estradiol is the only active hormone in the vaginal suppository; and wherein the vaginal suppository does not include a hydrophilic gel-forming bioadhesive agent in the solubilizing agent.

2. The vaginal suppository of claim 1, wherein the estradiol is solubilized.

3. The vaginal suppository of claim 1, wherein the estradiol is micronized.

4. The vaginal suppository of claim 1, wherein the estradiol is hydrated.

5. The vaginal suppository of claim 1, wherein the suppository comprises from about 1 microgram to about 10 micrograms of estradiol.

6. The vaginal suppository of claim 1, wherein the suppository comprises about 10 micrograms of estradiol.

7. The vaginal suppository of claim 1, wherein the suppository comprises about 5 micrograms of estradiol.

8. The vaginal suppository of claim 1, wherein the suppository comprises about 2.5 micrograms of estradiol.

9. The vaginal suppository of claim 1, wherein the suppository further comprises a capsule.

10. The vaginal suppository of claim 9, wherein the capsule is a soft gelatin capsule.

11. The vaginal suppository of claim 1, wherein the solubilizing agent comprises at least one of an ester of caproic fatty acid, an ester of caprylic fatty acid, an ester of capric fatty acid, and combinations thereof.

12. The vaginal suppository of claim 1, wherein the solubilizing agent comprises a monoglyceride, diglyceride, or triglyceride ester of the at least one C6-C12 fatty acid.

13. The vaginal suppository of claim 12, wherein the solubilizing agent comprises a caprylic/capric triglyceride.

14. A vaginal suppository comprising: (a) a pharmaceutical composition comprising: a therapeutically effective amount of estradiol; a caprylic/capric triglyceride; a non-ionic surfactant comprising PEG-6 palmitostearate and ethylene glycol palmitostearate; and (b) a soft gelatin capsule, wherein the pharmaceutical composition comprises from about 1 microgram to about 25 micrograms of estradiol; wherein estradiol is the only active hormone in the pharmaceutical composition; and wherein the pharmaceutical composition does not include a hydrophilic gel-forming bioadhesive agent.

15. A method of treating an estrogen-deficient state, the method comprising administering to a female in need thereof, a vaginal suppository comprising: a) a therapeutically effective amount of solubilized estradiol; and b) a solubilizing agent, wherein the solubilizing agent comprises at least one C6-C12 fatty acid or a glycol, monoglyceride, diglyceride, or triglyceride ester thereof; wherein the vaginal suppository comprises from about 1 microgram to about 25 micrograms of estradiol; wherein estradiol is the only active hormone in the vaginal suppository; and wherein the vaginal suppository does not include a hydrophilic gel-forming bioadhesive agent in the solubilizing agent.

16. The method of claim 15, wherein the estrogen-deficient state is vulvovaginal atrophy.

17. The method of claim 15, wherein the estrogen-deficient state is an estrogen-deficient urinary state.

18. The method of claim 15, wherein the estrogen-deficient state is selected from the group consisting of: vulvovaginal atrophy, dysuria, dyspareunia, estrogen-deficient urinary states, and vaginal bleeding associated with sexual activity.

Make Better Decisions: Try a trial or see plans & pricing

Serving leading biopharmaceutical companies globally:

Harvard Business School
McKesson
Express Scripts
Moodys
Baxter
Medtronic

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.