Vaginal inserted estradiol pharmaceutical compositions and methods

  • US 10,806,697 B2
  • Filed: 10/22/2014
  • Issued: 10/20/2020
  • Est. Priority Date: 12/21/2012
  • Status: Active Grant
First Claim
Patent Images

1. An encapsulated liquid pharmaceutical formulation comprising about 25 μ

  • g of 17β

    -estradiol uniformly dispersed in a solubilizing agent comprising a medium chain oil, wherein the medium chain oil comprises at least one C6-C12 fatty acid or a glycol, monoglyceride, diglyceride, or triglyceride ester thereof, wherein the pharmaceutical formulation (i) is a liquid at room temperature and has a viscosity in the range of about 50 cP to about 1000 cP at 25°

    C., and (ii) does not include an amount of a hydrophilic gel-forming bioadhesive agent that increases the viscosity above about 1000 cP at 25°

    C., and wherein after a single administration of the pharmaceutical formulation into the vagina of a patient provides, in a plasma sample from the patient;

    1) a corrected geometric mean peak plasma concentration (Cmax) of 17β

    -estradiol of about 19 pg/ml to about 29 pg/ml; and

    2) a corrected geometric mean area under the curve (AUC)0-24 of 17β

    -estradiol of about 75 pg*hr/ml to about 112 pg*hr/ml,wherein the pharmaceutical formulation is encapsulated in a capsule; and

    wherein 17β

    -estradiol is the only active hormone in the encapsulated pharmaceutical formulation.

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