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Orodispersible dosage unit containing an estetrol component

a technology of estetrol and dosage unit, which is applied in the direction of organic active ingredients, drug compositions, sexual disorders, etc., can solve the problem provide administration, and achieve the effect of rapid onset of action, easy manufacturing, and avoidance of first-pass liver exposur

Inactive Publication Date: 2016-12-22
MITHRA PHARMA SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The invention is a solid pharmaceutical dosage containing an estetrol component that can be quickly released in water. This dosage is easy to make and can be taken sublingually, buccally, or through the mouth. These modes of administration bypass the digestive system and liver exposure, providing a rapid response.

Problems solved by technology

Furthermore, these modes of administration provide a rapid onset of action.

Method used

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  • Orodispersible dosage unit containing an estetrol component

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0137]A sublingual tablet is prepared by means of the procedure described below.

[0138]A tabletting mixture having the composition shown in Table 1 is prepared by dry blending, using a low shear mixer.

TABLE 1IngredientsWt. %Milled estetrol112.5Mannitol47.5Lactose30PVP (polyvinylpyrrolidone)4Sodium crosscarmellose4Flavour0.5Aspartame1Magnesium stearate0.51D(v;0.5) = 15 μM

[0139]The tabletting mixture is compressed into 80 mg round tablets with a diameter of 6.5 mm. The estetrol content of these tablets is 10 mg.

example 2

[0140]A sublingual tablet is prepared by means of the procedure described below.

[0141]A tabletting mixture having the composition shown in Table 2 is prepared by dry blending using a low shear mixer.

TABLE 2IngredientsWt. %Milled estetrol112.5Mannitol37.5Xylitol10Microcrystalline cellulose33Sodium starch glycolate5Flavour0.5Aspartame1Magnesium stearate0.51D(v;0.5) = 15 μm

[0142]The tabletting mixture is compressed into 80 mg round tablets with a diameter of 6.5 mm. The estetrol content of these tablets is 10 mg.

example 3

[0143]Five different sets of sublingual tablets (formulations A to E) were prepared by means of the procedure described below and illustrated in FIG. 1.

[0144]The target amounts of estetrol per tablet were as follows: 100 μg for formulation A, 1 mg for formulation B, and 10 mg for formulations C, D and E.

[0145]The target weights for the tablets were as follows: 30 mg for formulation A, 1000 mg for formulation B, and 80 mg for formulations C, D and E.

[0146]The estetrol was mixed with a part of the main diluent and screened over a 800 μm screen. All other excipients were also screened over a 800 μm screen.

[0147]The materials were weighed and transferred into the mixing container (except for magnesium stearate) and mixed for 15 minutes. Finally, magnesium stearate was added and mixed for a further 3 minutes.

[0148]Compression was executed using a single punch machine equipped with a proper punch (5 mm punch for 30 mg tablets (A), 6 mm for 80 mg tablets (C, D and E) and 15 mm for 1000 mg ...

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Abstract

The invention provides an orodispersible solid pharmaceutical dosage unit having a weight between 30 and 1,000 mg, said dosage unit comprising:0.1-25 wt. % of estetrol particles containing at least 80 wt. % of an estetrol component selected from estetrol, estetrol esters and combinations thereof; and75-99.9 wt. % of one or more pharmaceutically acceptable excipients;the solid dosage unit comprising at least 100 μg of the estetrol component; and wherein the solid dosage unit can be obtained by a process that comprises compressing a dry blend of estetrol particles and one or more pharmaceutically acceptable excipients into a solid dosage unit.The solid dosage unit is easy to manufacture and perfectly suited for sublingual, buccal or sublabial administration.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]This non-provisional U.S. patent application claims priority to European Patent Application No. 15172747.6, filed Jun. 18, 2015, the contents of which are incorporated herein by their entirety by reference.TECHNICAL FIELD OF THE INVENTION[0002]The present invention provides an orodispersible solid pharmaceutical dosage unit having a weight of 30-1,000 mg and containing at least 0.1 mg of an estetrol component selected from estetrol, estetrol esters and combinations thereof. This solid dosage unit comprises:[0003]0.1-25 wt. % of estetrol particles containing at least 80 wt. % of the estetrol component; and[0004]75-99.9 wt. % of one or more pharmaceutically acceptable excipients.[0005]The invention also provides a process of preparing the aforementioned solid dosage unit.[0006]Furthermore, the invention relates to the use of the solid dosage unit in medical treatment, female hormone replacement therapy and female contraception, said use com...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/565A61K9/20A61K9/00
CPCA61K31/565A61K9/0056A61K9/006A61K9/2095A61K9/2059A61K9/2018A61K9/2027A61K9/2054A61K9/2013A61K9/2072A61P15/18A61P5/30A61P5/00A61P43/00A61K9/2009A61K9/2077
Inventor JASPART, SEVERINE FRANCINE ISABELLEPLATTEUW, JOHANNES JANVAN DEN HEUVEL, DENNY JOHAN MARIJN
Owner MITHRA PHARMA SA
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