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Vaginal inserted estradiol pharmaceutical compositions and methods

a technology of estradiol and vaginal insertion, which is applied in the field of pharmaceutical compositions, can solve the problems of poor compliance, less than desirable absorption, and the inability to dissolve estradiol with longer chains, and achieve the effects of reducing the number of parabasal vaginal cells, reducing and increasing the number of superficial vaginal cells

Active Publication Date: 2022-01-20
THERAPEUTICSMD INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0007]Disclosed herein is, among other things, a new soft gel vaginal pharmaceutical composition and dosage form containing solubilized estradiol for the treatment of VVA. The soft gel vaginal pharmaceutical composition has been designed to mitigate common limitations found with other vaginal forms of estradiol. The soft gel vaginal pharmaceutical composition eases vaginal administration, provides improved safety of insertion, minimizes vaginal discharge following administration, and provides a more effective dosage form having improved efficacy, safety and patient compliance.

Problems solved by technology

Generally, a thickening agent is added when the viscosity of the pharmaceutical composition results less than desirable absorption.
Longer chain glycerides appear to be not as well suited for dissolution of estradiol.
Patient irritation results in poor compliance.
Gels, hard fats, or other solid forms that are not liquid at room or body temperature are less desirable in embodiments of the pharmaceutical composition that are liquid.

Method used

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  • Vaginal inserted estradiol pharmaceutical compositions and methods
  • Vaginal inserted estradiol pharmaceutical compositions and methods
  • Vaginal inserted estradiol pharmaceutical compositions and methods

Examples

Experimental program
Comparison scheme
Effect test

example 1

Pharmaceutical Composition

[0296]In embodiments, estradiol is procured and combined with one or more pharmaceutically acceptable solubilizing agents. The estradiol is purchased as a pharmaceutical grade ingredient, often as micronized estradiol, although other forms can also be used. In embodiments, the pharmaceutical composition includes estradiol in a dosage strength of from about 1 μg to about 50 μg. In embodiments, the pharmaceutical composition includes 10 μg of estradiol. In embodiments, the pharmaceutical composition includes 25 μg of estradiol.

[0297]In embodiments, the estradiol is combined with pharmaceutically acceptable solubilizing agents, and, optionally, other excipients, to form a pharmaceutical composition. In embodiments, the solubilizing agent is one or more of CAPMUL MCM, MIGLYOL 812, GELUCIRE 39 / 01, GELUCIRE 43 / 01, GELUCIRE 50 / 13, and TEFOSE 63.

[0298]GELUCIRE 39 / 01 and GELUCIRE 43 / 01 each have an HLB value of 1. GELUCIRE 50 / 13 has an HLB value of 13. TEFOSE 63 has...

example 2

Delivery Vehicle

[0303]In embodiments, the pharmaceutical composition is delivered in a gelatin capsule delivery vehicle. The gelatin capsule delivery vehicle includes, for example, gelatin (e.g., Gelatin, NF (150 Bloom, Type B)), hydrolyzed collagen (e.g., GELITA®, GELITA AG, Eberbach, Germany), glycerin, sorbitol special, or other excipients in proportions that are well known and understood by persons of ordinary skill in the art. Sorbitol special may be obtained commercially and may tend to act as a plasticizer and humectant.

[0304]A variety of delivery vehicles were developed, as show in Table 2, Gels A through

[0305]F. In Table 2, each delivery vehicle A through F differs in the proportion of one or more components.

TABLE 2Gelatin Capsule Delivery VehiclesABCDEFIngredient% w / w% w / w% w / w% w / w% w / w% w / wGelatin, NF (150 Bloom, Type B)41.041.041.041.043.043.0Glycerin 99.7%, USP6.06.06.06.018.018.0Sorbitol Special, USP15.015.015.015.0GELITA ® ( hydrolyzed collagen)33.0Citric acid0.10.51...

example 3

Pharmaceutical Compositions and Delivery Vehicle

[0307]Various combinations of the pharmaceutical compositions from Table 1 and from Table 2 were prepared. The combinations are shown in Table 3.

TABLE 3DeliveryTrialPharmaceutical CompositionRatioBatch Size gVehicle1MCM:39 / 018:2750A2MCM:50 / 138:2750A3MCM:TEFOSE 638:2750A4MCM:TEFOSE 638:2750B5MIGLYOL 812:TEFOSE 639:1750A

[0308]Each aliquot of the pharmaceutical compositions of Table 3 about 300 mg to about 310 mg. Batch size was as listed in Table 3. To encapsulate the vehicle system, each 300 mg to about 310 mg pharmaceutical composition aliquot was encapsulated in about 200 mg of the gelatin capsule delivery vehicle. Thus, for example, in Trial 1, the pharmaceutical composition denoted by MCM:39 / 01 was encapsulated in gelatin capsule delivery vehicle A for a total encapsulated weight of about 500 mg to about 510 mg. The aliquot size is arbitrary depending on the concentration of the estradiol and the desired gelatin capsule delivery veh...

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Abstract

Disclosed herein is, among other things, a soft gel vaginal pharmaceutical composition and dosage form containing solubilized estradiol for the treatment of vulvovaginal atrophy (VVA) and female sexual dysfunction (FSD).

Description

CROSS-REFERENCES TO RELATED APPLICATIONS[0001]The present application claims priority to U.S. Provisional Pat. Appl. No. 62 / 264,309, filed Dec. 7, 2015; U.S. Provisional Pat. Appl. No. 62 / 296,552, filed Feb. 17, 2016; U.S. Provisional Pat. Appl. No. 62 / 324,838, filed Apr. 19, 2016; U.S. Provisional Pat. Appl. No. 62 / 329,940, filed Apr. 29, 2016; and U.S. Provisional Pat. Appl. No. 62 / 348,820, filed Jun. 10, 2016; which applications are incorporated herein by reference in their entirety.FIELD OF THE INVENTION[0002]This application is directed to pharmaceutical compositions, methods, and devices related to hormone replacement therapy.BACKGROUND OF THE INVENTION[0003]Postmenopausal women frequently suffer from atrophic vaginitis or vulvar and vaginal atrophy (hereinafter “vulvovaginal atrophy” or “VVA”) with symptoms including, for example, vaginal dryness, vaginal odor, vaginal or vulvar irritation or itching, dysuria (pain, burning, or stinging when urinating), dyspareunia (vaginal p...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/565A61K9/00A61K9/48A61K47/14A61K47/12
CPCA61K31/565A61K9/0034A61K47/12A61K47/14A61K9/4825A61K9/02A61K9/4858A61P5/30A61P7/04A61P13/10A61P15/00A61P15/02A61P17/04A61P25/04A61P25/26A61K9/025
Inventor MIRKIN, SEBASTIANAMADIO, JULIA M.BERNICK, BRIAN
Owner THERAPEUTICSMD INC
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