FI70136B - GEL ANVAENDBAR SOM BAERARE I ETT LOKALT APPLICERBART LAEKEMEDELPREPARAT FOER BEKAEMPNING AV HUDPARASITER - Google Patents

Description

ANNOUNCEMENT 7 η,

• SSff B 11 UTLÄGGNINGSSKRIFT / U I OO

C (45) Patent i-yjuiictty

Patent rcc.JOclat 15 00 1080 (51) Kv.lk.Vlnt.Ci. * A 61 K 7/40 (21) Patent applications - Patentansökning 78 1 8 1 5 (22) Application date - Ansöknlngsdag 07.06.78 (FI) (23) ) Start date - Giltighetsdag 07.06.78 (41) Has become public - Blivit offentllg 09.01.79

National Board of Patents and Registration / 44) Date of display and hearing. - 28 02 86

Patent- och registerstyrelsen '' Ansökan utlagd och utl.skrlften publicerad (32) (33) (31) Pyydetty etuoikeus - Begird priority 08.07.77

England-England (GB) 28722/77 (71) Mundipharma AG, AIban-Vorstadt 94, Postfach, 4006 Basel, Switzerland-Switzerland (CH) (72) Stewart Thomas Leslie, Aberdeen, Scotland,

Alan Rhodes, Aberdeen, Scotland, United Kingdom-Storbritannien (GB) (74) Oy Koister Ab (54) I Gel useful as a carrier for topical treatment hudparasiter

The present invention relates to a gel containing an anionic surfactant, nonionic surfactants and a polar solvent useful as a carrier in a topical pharmaceutical preparation for controlling lice, satin and the like.

Known cosmetic gels are generally flowable gels formed either by adding an inorganic salt to an alkyl ether sulfate or by incorporating cellulose, alginate or another known rubber-type thickener into the cosmetic preparation.

In the control of head lice, satin and other skin diseases, and in the treatment of other skin diseases, it has been found desirable to treat the body or hair with an active ingredient that is insoluble in water. Examples of such active ingredients are carbaryl, piperonyl butoxide and malathion.

701 36 2 Active ingredients of this type have been combined with ointment-type preparations which have been found to be very useful in temperate climates but which have considerable problems, for example in tropical climates. Thus, an anionic surfactant commonly used in tropical climates, for example sodium lauryl sulfate, dissolves in the preparation to form a liquid and not a cream. Upon cooling, the surfactant crystallizes out of solution to give a product containing short needle-like crystals. This is clearly not acceptable to the user.

Gel preparations intended for purposes other than topical use cannot be used for topical application because their components are irritating, for example, to the skin, causing rash, and to the eyes, causing conjunctivitis.

The gel of the invention contains as a gel-forming component a mild anionic surfactant, a nonionic surfactant and a polar solvent such as water. The ingredients and their proportions are selected so that the product does not irritate human or animal skin. The gel structure is maintained in any temperature range to which the product may be exposed, although the viscosity of the preparation may decrease somewhat with increasing temperature.

The gel of the invention can be applied topically to the skin of an animal or human without the risk of skin or eye irritation.

The gel according to the invention is characterized in that the anionic surfactant is sodium lauryl ether sulfate, the nonionic surfactants are nonylphenoxypoly (ethyleneoxy) ethanol, coconut fatty acid diethanolamide and ethoxylated ethanolamine, and ethoxylated toluene, the weight ratio of surfactant to nonionic surfactant is 1: 3 to 3: 1, preferably about 2: 1, and the total amount of anionic surfactant to nonionic surfactant in the preparation is 20 to 60% by weight. -% by weight of the preparation.

The final preparation contains gel-forming components, i.e. in addition to a mild anionic surfactant, a nonionic surfactant, and a polar solvent such as water, an active ingredient for controlling skin, lanolin, a foam synergist, a colorant, and a perfume.

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Preferred active ingredients for controlling lice and mites are carbaryl, piperonyl butoxide, malathion and mixtures thereof.

The foam synergist is preferably coconut diethanolamide.

The best effects of the gel preparation according to the present invention are achieved by maintaining the ratio of anionic surfactant to nonionic surfactant between about 1: 3 and 3: 1. The preferred ratio is 2: 1.

The total amount of anionic surfactant and nonionic surfactant in the total gel preparation is maintained between about 20-60% by weight. Since the components of the composition in the gel preparations of the invention may affect the viscosity of the final preparation, adjustment is necessary to determine the optimum percentage and ratio of anionic surfactant to nonionic surfactant.

Although the invention is not intended to be limited to any theory as to how a gel preparation with suitable properties is obtained in accordance with the present invention, the following theory is presented with a view to assisting further research in this field.

It is believed that the combination of an anionic surfactant and a nonionic surfactant in water or other polar solvent creates a co-cell phase in the solvent, leading to gel formation due to an increase in the specific volume of the co-cell phase. Thus, the specific volume of the two surfactants, or the combined percentage of the two surfactants, determines the gel confluence point of the preparation, and for this reason the preferred combined percentage of anionic surfactant and nonionic surfactant in the gel preparation ranges from 20 to 60 weight-%.

The gel preparations of the invention are prepared by heating an anionic surfactant paste (in the form of a concentrate in water, e.g. as a 70% concentrate) together with a nonionic surfactant (in pure liquid form), adding water (or other polar solvent) and stirring to form a clear solution. . Upon cooling, a product is formed which, depending on the ratios of the two surfactants, can vary from a viscous liquid to a hard gel. The active ingredient is dissolved in the nonionic surfactant before the nonionic surfactant is heated with the anionic surfactant.

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Similarly, the other optional ingredients are dissolved in the phase (surfactant or water) in which they are most soluble. Any fragrance added as the last ingredient is added at the lowest possible temperature.

The following examples are provided to illustrate the invention in more detail.

Example 1

Ingredients Weight in grams

Carbaryl 1.0

Nonylphenoxypoly (ethyleneoxy) ethanol 12.5

Sodium lauryl ether sulfate (70%) 25.0

Coconut diethanolamide 1,5 en Coloring agent - F.D. and C Yellow No 5 0.01 n

Perfume - Glarland Flora 0.2

Up to 100 g of water

Sodium lauryl ether sulfate, coconut diethanolamide and ethoxylated lanolin are mixed together at a temperature of 70-80 ° C. Carbaryl is dissolved in nonylphenoxypoly (ethyleneoxy) ethanol by heating to 40-50 ° C. The mixture is stirred to form a clear solution. The resulting solution is added to a mixture of sodium lauryl ether sulfate, coconut diethanolamide and ethoxylated lanolin and stirred to obtain a homogeneous solution.

The colorant is completely dissolved in a calculated amount of water and the resulting solution is heated just below the boiling point and then slowly added to the homogeneous solution prepared above. The resulting mixture is kept at a high temperature to allow air to escape. The mixture is then cooled to 55-60 ° C and the perfume is slowly mixed into it. Upon cooling to room temperature, a gel is formed which retains its gel pattern and pattern for at least two years when stored at room temperature or 30 ° C. 701 36 5

Example 2

Ingredients Weight in grams

Malathion 1.10

Nonylphenoxypoly (ethyleneoxy) ethanol 20.00

Sodium lauryl ether sulfate (70%) 25.00

Coconut diethanolamide 2.50

Ethoxylated Lanolin 1.25 β Dyestuff - F.D. - and C Yellow No. 5 0.01

Fragrance - May & Baker No. 1658 β 0.2

Sufficient dilute hydrochloric acid to pH 5.2

Up to 100 g of water

Sodium lauryl ether sulfate, coconut diethanolamide and ethoxylated lanolin are mixed together at 70-80 ° C: nonylphenoxypoly (ethyleneoxy) ethanol is then added to the mixture, which is stirred to obtain a homogeneous solution. The colorant is completely dissolved in an amount of water and the resulting solution is heated to a temperature just below the boiling point and then slowly added to the homogeneous solution prepared above.

The resulting mixture is kept at a high temperature to allow air to escape. The mixture is then cooled to 55-60 ° C and adjusted to pH 5.2 with dilute hydrochloric acid. The malathion and fragrance are then slowly added to the mixture with stirring. Upon cooling to room temperature, a gel is formed which retains its gel shape and pattern when heated to a temperature of at least 30 ° C.

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Example 3

Ingredients Weight in grams

Carbaryl 1.00

Piperonylbutoxide 5.00

Alkylphenol polyoxyethylene ether 12.50

Sodium lauryl ether sulphate 30.00

Isopropyl myristate 3.00

Coconut diethanolamide 1.00

Ethoxylated Lanolin 2.00 Dyestuff FD and C Yellow No. 5β 0.0025 FD and C Blue No. 1® 0.0025 n

Perfume - Fresco 0.4

Up to 100 g of water

Sodium lauryl ether sulfate, coconut diethanolamide and ethoxylated lanolin are mixed together at a temperature of 70-80 ° C. Carbaryl, piperonyl butoxide and isopropyl myristate are dissolved in nonylphenoxypoly (ethyleneoxy) ethanol by heating to 40-50 ° C. The mixture is stirred to form a clear solution.

The resulting solution is added to a mixture of sodium lauryl ether sulfate, coconut diethanolamide and ethoxylated lanolin and stirred to obtain a homogeneous solution. The colorant is completely dissolved in a calculated amount of water and the resulting solution is heated to a temperature just below the boiling point and then slowly added to the homogeneous solution prepared above. The resulting mixture is kept at a high temperature to allow air to escape.

The mixture is then cooled to 55-60 ° C and the perfume is slowly mixed into it.

Upon cooling to room temperature, a gel is formed which retains its gel shape and pattern when heated to a temperature of at least 30 ° C.

Although the invention has been described in terms of typical blends, it will be apparent that variations and modifications may be made therein.