Pharmaceutical preparations containing highly volatile silicones

Pending Publication Date: 2014-03-20
EGIS PHARM PLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent text discusses the use of volatile silicon oils as adjuvants in pharmaceutical preparations. These oils help to improve the stability and penetration properties of ointments and gels containing active ingredients. The silicone coating formed around the active ingredient particles protects them from chemical and microbiological impacts, ensuring good stability. When the gel is applied to the skin, the silicone compound evaporates, leaving the active substance particles on the surface of the skin. These particles easily release into the layers of the skin, resulting in effective absorption without any interaction with the human organism. Overall, this approach provides improved efficacy and safety of the pharmaceutical product.

Problems solved by technology

In case of lung oedema the strongly foamy mucus originating from the lung and making a barrier in the normal ventilation and in the oxygen uptake can cause anoxia or suffocation in lack of treatment.
According to these patents highly volatile siloxanes serve exclusively in order to obtain a good distribution on the surface of the human skin, but not to attain chemical and microbiological stability.
A disadvantage of the ointments having fatty or oily bases is that the penetration of the active ingredient is slow and the amount of the released active substance is low, because in the lipophil phase the solubility of the ointment is higher, especially in case of active substances having low aqueous solubility, and therefore, the distribution is not equal, the ointment base contains more active substance.
Gel compositions containing the active ingredient in a suspended form are known from the literature, wherein the release of the active substance is adequate, but stability problems can occur during storage.
These problems are caused by the chemical and microbiological reactions on the contact areas of the different surfaces, which may change the chemical condition of the active substance.
These kind of stability problems can occur for example during the storage of Hotemin® cream containing piroxicam, Voltaren® emulgel (diclofenac) or Rozex® gel containing metronidazol.

Method used

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  • Pharmaceutical preparations containing highly volatile silicones
  • Pharmaceutical preparations containing highly volatile silicones
  • Pharmaceutical preparations containing highly volatile silicones

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0089]Gel composition containing piroxicam as active ingredient:

Piroxicam0.500gSilicone fluid 0.65 cSt0.500gSilicone fluid 100 cSt2.150gCarbopol 980 NF0.250gTriethanolamine0.200gHydroxypropyl-methylcellulose1.000gPurified waterad 50,000g

[0090]According to the recipe of the above example the gel was prepared in a batch size of 7 kg with a Brogtech apparatus suitable for the preparation of ointments.

1.1. Method of Preparation of the Suspension Containing the Active Ingredient:

[0091]Micronized piroxicam powder (70.0 g) is mixed with Silicone fluid 0.65 cSt (301.0 g) and Silicone fluid 100 cSt (70.0 g) in an 800 ml beaker glass, and the mixture in an Ultra-Turrax apparatus, at 4000 revs / minute for 5 minutes. The prepared suspension is stored in an airtight place until application.

1.2. Method of Preparation of the Gel Base:

[0092]Purified water (6000 g) is poured into the Brogtech apparatus and the temperature is set at 25° C. In an anchor mixer in position 4, hydroxypropyl-methylcellulos...

example 2

[0094]Gel composition containing clotrimazol as active ingredient:

Clotrimazol0.200gSilicone fluid 0.65 cSt1.000gSilicone fluid 100 cSt0.200gCarbopoI 980 NF0.100gTriethanolamine0.200gHydroxypropyl-methylcellulose0.400gPurified waterad 20,000g

[0095]According to the recipe of the above example the gel was prepared in a batch size of 7 kg with a Brogtech apparatus suitable for the preparation of ointments.

2.1. Method of Preparation of the Suspension Containing the Active Ingredient:

[0096]Micronized clotrimazol powder (70.0 g) is mixed with Silicone fluid 0.65 cSt (350.0 g) and Silicone fluid 100 cSt (70.0 g) in a 800 ml beaker glass, and the mixture is homogenized in an Ultra-Turrax apparatus, at a 4000 revs / minute for 5 minutes. The prepared suspension is stored in an airtight place until application.

2.2. Method of Preparation of the Gel Base:

[0097]Purified water (6000 g) is put into the Brogtech apparatus and the temperature is set at 25° C. In an anchor mixer in position 4, hydroxypr...

example 3

[0100]Gel composition containing metranidazol as active ingredient:

Metronidazol1.000gSilicone fluid 0.65 cSt2.000gSilicone fluid 100 cSt0.200gCarbopol 980 NF0.250gTriethanolamine0.200gHydroxypropyl-methylcellulose0.400gPurified waterad 20,000g

[0101]According to the recipe of the above example the gel was prepared in a batch size of 7 kg with a Brogtech apparatus suitable for the preparation of ointments.

3.1. Method of Preparation of the Suspension Containing the Active Ingredient:

[0102]Micronized metronidazol powder (350.0 g) is mixed with Silicone fluid 0.65 cSt (700.0 g) and Silicone fluid 100 cSt (70.0 g) in a 800 ml beaker glass, and the mixture in an Ultra-Turrax apparatus, at a 4000 revs / minute for 5 minutes. The prepared suspension is stored in an airtight place until application.

3.2. Method of Preparation of the Gel Base:

[0103]Purified water (5500 g) is put into the Brogtech apparatus and the temperature is set at 25° C. In an anchor mixer in position 4, hydroxypropyl-methyl...

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Abstract

The subject of the present invention is a transdermal preparation containing pharmaceutically active ingredient, wherein the particles of the active ingredient are coated with highly volatile silicones or a mixture thereof, and these coated particles are dispersed in a gel or cream base. The volatile silicone component is hexamethyldisiloxane and / or octamethyltrisiloxane and / or decamethylpentacyclo-siloxane. A further subject of the present invention is a method for the preparation of such pharmaceutical compositions.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]This application claims priority to U.S. patent application Ser. No. 12 / 672,696, filed Apr. 9, 2010, which claims priority to PCT Application, PCT / HU2008 / 000083, filed Jul. 10, 2008 entitled “PHARMACEUTICAL PREPARATIONS CONTAININING HIGHLIY VOLATILE SILICONES,” which claims priority to Hungarian Application HU2007 / 0000473, filed Jul. 10, 2007. The aforementioned applications are hereby incorporated by reference as if fully set forth herein.BACKGROUND OF THE INVENTION[0002]The subject of the present invention is a transdermal preparation containing a pharmaceutically active ingredient, wherein the particles of the active ingredient are coated with highly volatile silicones or a mixture thereof and these coated particles are dispersed in a gel or cream base. A further subject of the present invention is a method for the preparation of such pharmaceutical compositions.[0003]The application of the silicone derivatives in medicine started in t...

Claims

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Application Information

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IPC IPC(8): A61K47/34A61K31/495A61K31/4164A61K31/5415A61K31/4174
CPCA61K47/34A61K31/5415A61K31/495A61K31/4164A61K31/4174A61K9/0014A61K9/06A61K9/1611A61K47/02A61P31/04A61P37/08A61K31/59A61K47/50
Inventor MIKULASIK, ENDREFAZEKAS, PATRIK
Owner EGIS PHARM PLC
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