RO128701A2 - Semi-solid pharmaceutical forms intended for topical administration, containing associations of atomized extracts of cynara scolymus, rosmarinus officinalis sp. and hyssopus officinalis sp. - Google Patents

Abstract

The invention relates to a pharmaceutical product intended for topical administration containing 0.01...10% by mass associated atomized extracts of Cynara scolymus, Rosmarinus officinalis and Hyssopus officinalis in a ratio of 40:30:30, 0.5...4% polyacrylate-type lattice forming agent, 1...10% lipophilic absorption promoter, namely polypropylene glycol, triethanol amine, 2...20% ethanol and water for the remainder up to 100%, the percentage being expressed by mass.

Description

Semi-solid pharmaceutical forms for local administration, containing combinations of atomized extracts of Cynara scolymus, Rosmarinus officinalis sp. and Hissopus officinalis sp.

The invention relates to semi-solid pharmaceutical forms for local administration to the skin and mucous membranes, with a content of between 0.1 and 5% combination of atomized extracts of Cynara scolymus, Rosmarinus officinalis sp. and Hissopus officinalis sp ..

Patent applications A / 011256; 2010 and A / 011257; 2010 [Andrieș AA et al] describe semi-solid and solid pharmaceutical forms, containing atomized extracts of plant products. The active principles contained in the active principles determine processes of inhibition of the action of metalloproteinases, generating after the administration of invivo a powerful antioxidant effect. It is correlated with the effects of combating the signs of tissue aging.

The invention that is the subject of this file adds to the complex of active principles the content of the atomized extract of Cynara scolymus, in some semi-solid pharmaceutical forms. Considering the advantage of the hydrophilic semi-solid pharmaceutical forms, as well as the variability of the physico-chemical and prospective characteristics, of the biopharmaceutical parameters for the molecular structures that constitute the complex mixture - active components of the extracts, it was followed the development of emulsion type gels. These two-phase vehicles have the potential to ensure optimum stability and bioavailability of active ingredients. The minimum amount of ethyl alcohol and lower polyol, propylene glycol was chosen. This cosolvent mixture was used to disperse the complex amount. The absorption promoter was represented by either isopropyl-myristate or its combinations with lanolin and oleic alcohol, both of which generate semi-solid pharmaceutical forms of emulsion type.

α-2 Ο 1 1 - Ο 1 2 7 4 - - 'Λ ^ν 2 9 * 11' 2011

The composition of the atomized powder combination (Cynara scolymus: Rosmarinus officinalis: Hyssopus officinalis, 40: 30: 30%), used in the preparation of the semi-solid pharmaceutical forms, was as follows:

Concentration parameter

Polyphenolcarboxylic acids,% (w / w)

- expressed in rosmarinic acid4.08

- expressed as caffeic acid 3.18

- expressed as chlorogenic acid3.98

Flavone,% (w / w)

-expressed in routine4.56

Rosmarinic acid, mg / 100g 2078.33

Cinarine, mg / 100g89.39

Chlorogenic acid, mg / 100g 246.40

Caffeic acid, mg / 100g68.34

Luteolin 7-glycoside, mg / 100g 800.77

Apigenin 7-glycoside, mg / 100g50.53

Routine, mg / 100g 305.08

Micro and macroelements, mg / 100g

-mangan2.07

-zinc1.83

-magnesium

807.50

ί

9 2011

The general composition of gel-emulsion formulations is shown below:

Component Quantity (g / 100g) Association of atomized powders (Cynara scolymus: Rosmarinus officinalis: 0.01 - 10.0

Hyssopus officinalis, 40: 30: 30%)

Macromolecular polyacrylic agent 0.5-4.0 triethanolamine at pH 7 propylene 1.0- 10.0

Isopropyl-myristate-type lipophilic absorption promoter or its combination with fatty acids and other biocompatible lipid components

Absolute ethanol

5.0 - 20.0

Purified water ad 100.0

Method of preparation

The polyacrylate network former (for example carbomer 934, 940) is hydrated, for 24 hours, in 75% of the amount of water provided in the formula. For this polyacrylic system, the gel was structured by neutralization with triethanol-amine.

The resulting gels are neutralized by adding the neutralizing agent.

The association of atomized powders is dissolved or dispersed in the mixture of propylene glycol and ethanol, in which the lipophilic absorption promoter was previously dispersed.

The neutralized gel and the micellar system containing the components of the powders in the association are combined and homogenized by slow agitation.

ÎX-2 Ο 1 1 - Ο 1 2 7 4 - 2 9 -11- 2011

Example 1 Component Quantity (g / 100g) Association of atomized powders (Cynara scolymus; Rosmarinus officinalis: Hyssopus officinalis, 40: 30: 30%) 0.5 Carbomer 940 0.5 triethanolamine at pH 7 propylene 5 Isopropyl-myristate 5 Absolute ethanol 10

Purified water up to

100

Example 2

Component Quantity (g / 100g) Association of atomized powders (Cynara scolymus: Rosmarinus officinalis: Hyssopus officinalis, 40: 30: 30%) 0.5 Carbomer 940 0.5 triethanolamine at pH 7 propylene 5 Isopropyl-myristate, lanolin and oleic acid mixture 5 Absolute ethanol 10 Purified water up to 100

^ - 2 0 1 1 - 0 1 2 7 4-- '7

9-11-11, 2011

Example 3

Component

Quantity (g / 1OOg)

Association of atomized powders (Cynara scolymus: Rosmarinus officinalis: 1

Hyssopus officinalis, 40: 30: 30%)

Carbomer 940

0.5

Triethanolamine at pH 7

propylene

Isopropyl-myristate

Absolute ethanol

Purified water up to

100

Example 4

Component Quantity (g / 100g) Association of atomized powders (Cynara scolymus: Rosmarinus officinalis: Hyssopus officinalis, 40: 30: 30%) 1 Carbomer 940 0.5 triethanolamine at pH 7 propylene 5 Isopropyl-myristate, lanolin and oleic acid mixture 5 Absolute ethanol 10

Purified water up to

100

t \ - 2 O 1 1 - O 1 2 7 4 - - .7

9-11-11, 2011

Example 5

Component Quantity (g / 100g) Association of atomized powders (Cynara scolymus: Rosmarinus officinalis: 0.5

Hyssopus officinalis, 40: 30: 30%)

Carbomer 940

Triethanolamine at pH 7

propylene

Isopropyl-myristate

Absolute ethanol

Purified water up to

100

Example 6 Component Quantity (g / 100g) Association of atomized powders (Cynara scolymus: Rosmarinus officinalis: Hyssopus officinalis, 40: 30: 30%) 0.5 Carbomer 940 1 triethanolamine at pH 7 propylene 5 Isopropyl-myristate, lanolin and oleic acid mixture 5 Absolute ethanol 10

Purified water up to

100

Example 7 (χ- 2 Ο 1 1 - Ο 1 2

9 -11- 2Π11

Component Quantity (g / 100g) Association of atomized powders (Cynara scolymus: Rosmarinus officinalis: Hyssopus officinalis, 40: 30: 30%) 1

Carbomer 940

Triethanolamine at pH 7

propylene

Isopropyl-myristate

Absolute ethanol

Purified water up to

100

Example 8

Component Quantity (g / 100g) Association of atomized powders (Cynara scolymus: Rosmarinus officinalis: 1

Hyssopus officinalis, 40: 30: 30%)

Carbomer 940 1 triethanolamine at pH 7 propylene 5 Isopropyl-myristate, lanolin and oleic acid mixture 5

Absolute ethanol

Purified water up to

Claims (1)

claims 1. Semi-solid pharmaceutical form for local administration on the skin and mucous membranes, characterized in that it includes between 0.1 and 5% an association of atomized extracts of Cynara scolymus, Rosmarinus officinalis sp. and Hissopus officinalis sp ..