You're using a free limited version of DrugPatentWatch: Upgrade for Complete Access

Last Updated: April 5, 2025

Claims for Patent: 9,289,382

✉ Email this page to a colleague

« Back to Dashboard

Summary for Patent: 9,289,382

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), Amadio; Julia M. (Boca Raton, FL)
Assignee:	TherapeuticsMD, Inc. (Boca Raton, FL)
Application Number:	14/624,051
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,289,382
Patent Claims:	1. A pessary comprising about 25 .mu.g of 17.beta.-estradiol in a solubilizing agent comprising a medium chain oil, wherein after a single administration of the pessary to a patient provides, in a plasma sample from the patient: 1) a corrected geometric mean peak plasma concentration (C.sub.max) of 17.beta.-estradiol of about 19 pghr/ml to about 29 pghr/ml; and 2) a corrected geometric mean area under the curve (AUC).sub.0-24 of 17.beta.-estradiol of about 75 pghr/ml to about 112 pghr/ml, wherein 17.beta.-estradiol is the only active hormone in the pessary. 2. The pessary of claim 1, wherein administration of the pessary to a patient provides, in a plasma sample from the patient: 1) a corrected geometric mean peak plasma concentration (C.sub.max) of estrone of about 9 pghr/ml to about 14 pghr/ml; and 2) a corrected geometric mean area under the curve (AUC).sub.0-24 of estrone of about 43 pghr/ml to about 65 pghr/ml. 3. The pessary of claim 1, wherein administration of the pessary to a patient provides, in a plasma sample from the patient: 1) a corrected geometric mean peak plasma concentration (Cmax) of estrone sulfate of about 416 pghr/ml to about 613 pghr/ml; and 2) a corrected geometric mean area under the curve (AUC).sub.0-24 of estrone sulfate of about 3598 pghr/ml to about 5291 pghr/ml. 4. A pessary comprising about 10 .mu.g of 17.beta.-estradiol in a solubilizing agent comprising a medium chain oil, wherein after a single administration of the pessary to a patient provides, in a plasma sample from the patient: 1) a corrected geometric mean peak plasma concentration (C.sub.max) of 17.beta.-estradiol of about 12 pghr/ml to about 18 pghr/ml; and 2) a corrected geometric mean area under the curve (AUC).sub.0-24 of 17.beta.-estradiol of about 42 pghr/ml to about 63 pghr/ml, wherein 17.beta.-estradiol is the only active hormone in the pessary. 5. The pessary of claim 4, wherein the pessary further provides a corrected geometric mean time to peak plasma concentration (T.sub.max) of 17.beta.-estradiol of about 1 hrs to about 3 hrs. 6. The pessary of claim 4, wherein administration of the pessary to a patient provides, in a plasma sample from the patient: 1) a corrected geometric mean peak plasma concentration (C.sub.max) of estrone of about 4 pghr/ml to about 7 pghr/ml; and 2) a corrected geometric mean area under the curve (AUC).sub.0-24 of estrone of about 20 pghr/ml to about 31 pghr/ml. 7. The pessary of claim 6, wherein the pessary further provides a corrected geometric mean time to peak plasma concentration (T.sub.max) of estrone of about 4 hrs to about 8 hrs. 8. The pessary of claim 4, wherein administration of the pessary to a patient provides, in a plasma sample from the patient: 1) a corrected geometric mean peak plasma concentration (C.sub.max) of estrone sulfate of about 10 pghr/ml to about 16 pghr/ml; and 2) a corrected geometric mean area under the curve (AUC).sub.0-24 of estrone sulfate of about 56 pghr/ml to about 84 pghr/ml. 9. The pessary of claim 8, wherein the pessary further provides a corrected geometric mean time to peak plasma concentration (T.sub.max) of estrone sulfate of about 4 hrs to about 7 hrs. 10. A pessary comprising about 4 .mu.g of 17.beta.-estradiol in a solubilizing agent comprising a medium chain oil, wherein after a single administration of the pessary to a patient provides, in a plasma sample from the patient: 1) a corrected geometric mean peak plasma concentration (Cmax) of 17.beta.-estradiol of about 4 pghr/ml to about 8 pghr/ml; and 2) a corrected geometric mean area under the curve (AUC).sub.0-24 of 17.beta.-estradiol of about 16 pghr/ml to about 26 pghr/ml, wherein 17.beta.-estradiol is the only active hormone in the pessary. 11. The pessary of claim 10, wherein the pessary further provides a corrected geometric mean time to peak plasma concentration (T.sub.max) of 17.beta.-estradiol of about 0.25 hrs to about 2 hrs. 12. The pessary of claim 10, wherein administration of the pessary to a patient provides, in a plasma sample from the patient: 1) a corrected geometric mean peak plasma concentration (C.sub.max) of estrone of about 1 pghr/ml to about 3 pghr/ml; and 2) a corrected geometric mean area under the curve (AUC).sub.0-24 of estrone of about 8 pghr/ml to about 13 pghr/ml. 13. The pessary of claim 12, wherein the pessary further provides a corrected geometric mean time to peak plasma concentration (T.sub.max) of estrone of about 1 hrs to about 4 hrs. 14. The pessary of claim 10, wherein administration of the pessary to a patient provides, in a plasma sample from the patient: 1) a corrected geometric mean peak plasma concentration (C.sub.max) of estrone sulfate of about 4 pghr/ml to about 7 pghr/ml; and 2) a corrected geometric mean area under the curve (AUC).sub.0-24 of estrone sulfate of about 22 pghr/ml to about 34 pghr/ml. 15. The pessary of claim 14, wherein the pessary further provides a corrected geometric mean time to peak plasma concentration (T.sub.max) of estrone sulfate of about 1 hrs to about 3 hrs. 16. 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. 17. The pessary of claim 1, wherein the medium chain oil comprises a monoglyceride, diglyceride, or triglyceride ester of the at least one C6-C12 fatty acid. 18. The pessary of claim 4, wherein the medium chain oil comprises at least one C6-C12 fatty acid or a glycol, monoglyceride, diglyceride, or triglyceride ester thereof. 19. The pessary of claim 4, wherein the medium chain oil comprises a monoglyceride, diglyceride, or triglyceride ester of the at least one C6-C12 fatty acid. 20. The pessary of claim 10, wherein the medium chain oil comprises at least one C6-C12 fatty acid or a glycol, monoglyceride, diglyceride, or triglyceride ester thereof. 21. The pessary of claim 10, wherein the medium chain oil comprises a monoglyceride, diglyceride, or triglyceride ester of the at least one C6-C12 fatty acid.

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

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.