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Topical pharmaceutical compositions

a technology compositions, applied in the field can solve the problems of poor solubility of mometasone furoate, limited development of topical pharmaceutical compositions, and formulations that lack the required activity, etc., and achieve better skin hydration values and skin adsorption times.

Inactive Publication Date: 2014-07-17
ALMIRALL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent describes a new pharmaceutical composition that contains mometasone furoate, hexylene glycol, water, and oil phase. This composition is stable and effective in treating skin conditions such as eczema. It is easy to apply, absorbs quickly, and is not irritant to the skin. Patients who used this composition had better skin hydration and adsorption times than those who used other mometasone furoate compositions.

Problems solved by technology

The exceptionally poor solubility of mometasone furoate is a limitation for the development of topical pharmaceutical compositions.
U.S. Pat. No. 4,808,610 indicates that when mometasone furoate is partially dissolved and partially suspended in propylene glycol based cream formulations, the resulting formulations do not possess the necessary efficacy; and when mometasone furoate is completely dissolved in oleyl alcohol / propylene glycol based cream formulations, the resulting formulations not only lack the required activity but also are irritant in a rabbit dermal test.
Additionally, according to U.S. Pat. No. 4,808,610, formulations containing drug solubilizing agents may result in poor activity.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

[0068]A cream according to the invention was prepared having the composition indicated in Table 1 (wt. % based on the total weight of the composition)

TABLE 1Mometasone furoate creamIngredientswt. %Mometasone furoate0.1Liquid Paraffin17.5White Soft Paraffin26.5Cetostearyl Alcohol17.2Macrogol Cetostearyl Ether22.8Cetyl Alcohol1.0Hexylene Glycol10.0Glycerol1.0Xanthan Gum0.1Purified Waterup to 100%pH adjusted to 3.5-4.51Emulsifiying Cetostearyl Alcohol Type A2Having 20-30 units of ethylene oxide per molecule

[0069]Said cream was prepared in the following manner:

1) Oil phase: white soft paraffin, liquid paraffin, cetostearyl alcohol, macrogol cetostearyl ether and cetyl alcohol were added to a main vessel equipped with anchor stirrer and homogeniser. The ingredients were heated to 70° C. and melted while stirring until obtaining an homogenous mixture.

2) Xanthan gum phase: Xanthan gum was pre-dispersed in hexylene glycol.

3) Water phase: About 90 wt. % of the total amount of water was added...

example 2

[0070]The viscosity of the cream of Example 1 was measured at 20° C. using a DIN-Rotations Rheometer (Paar Physica); Measuring System Z 3 DIN; D=57 1 / s.

[0071]Additionally, the viscosity of a commercially available mometasone cream such as ECURAL® Fettcreme 0.1% of Essex Pharma GmbH (Comparative Example 1) using the same measuring conditions.

[0072]According to the product information, each gram of ECURAL® Fettcreme 0.1% contains: 1 mg mometasone furoate in a cream base of hexylene glycol; phosphoric acid; propylene glycol stearate; stearyl alcohol and ceteareth-20; titanium dioxide; aluminum starch octenylsuccinate; white wax; white petrolatum; and purified water. The water content of ECURAL® Fettcreme is about 3 to 5 wt. %.

[0073]The results are indicated in Table 2.

TABLE 2Viscosity valuesExample 1Comparative Example 1aprox. 5,000 mPa · saprox. 20,000 mPa · s

[0074]From the experimental results it can be concluded that the cream of Example 1 (according to the invention) can be more ea...

example 3

[0075]A vasoconstrictor assay measuring skin blanching (assay described by Mckenzie and Stoughton, Arch. Dermatol., 86, 608-610 (1962)) was used to determine the bioequivalence of the cream of Example 1 (according to the invention) to ECURAL® Fettcreme 0.1% (Comparative Example 1)

[0076]Study population: 30 Subjects with healthy skin in the area of the test fields, demonstrating adequate vasoconstriction to corticosteroids, aged 18 years or older, were investigated.

[0077]Test performance: Single topical non-occlusive application to test fields located on the volar surface of the forearms. Skin colour in the treated and untreated test fields was measured using chromametry. In addition, the degree of vasoconstriction was clinically assessed compared to the untreated test fields.

[0078]Efficacy: Under the conditions in the present vasoconstrictive assay the topical bioavailability of the cream of Example 1 was shown by a strong blanching effect. The strong blanching effect of the cream o...

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Abstract

Topical pharmaceutical compositions are described comprising, based on the total weight of the composition: a) 0.01 to 0.2 wt. % of mometasone furoate, b) 5 to 18 wt. % of hexylene glycol, c) 20 to 40 wt. % of water, and d) 25 to 70 wt. % of an oil phase. Said compositions are stable and can be safely and easily applied over large surface areas of the skin in an acceptable way by the general patient population for the treatment or prevention of psoriasis, atopic dermatitis (atopic eczema) and other skin disorders or diseases.

Description

FIELD OF THE INVENTION[0001]The present invention relates to topical pharmaceutical compositions comprising mometasone furoate. Said compositions are stable and can be safely and easily applied over large surface areas of the skin in an acceptable way by the general patient population. The invention further relates to a process for the preparation of said compositions and to methods of treatment by administering the compositions.BACKGROUND OF THE INVENTION[0002]Topical corticosteroids, as a class, demonstrate anti-inflammatory, anti-pruritic and vasoconstrictive actions. They are generally used to relieve the redness, skin edema (swelling), itching, crusting, flaking, blistering, cracking, oozing and discomfort of psoriasis, atopic dermatitis (atopic eczema) and other pathologies of the skin like contact dermatitis, seborrheic dermatitis, xerotic eczema, discoid eczema, venous eczema, dermatitis herpetiformis, neurodermatitis or autoeczematization.[0003]Commercially, topical cortico...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/58
CPCA61K47/06A61K9/06A61K47/10A61K9/0014A61K9/107A61K31/58A61P17/00A61P17/04A61P17/06A61P29/00
Inventor EVERS, FRITJOFMALLWITZ, HENNINGWESSEL, RICARDAWILLERS, CHRISTOPH
Owner ALMIRALL
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