WO1982000763A1

WO1982000763A1 - Dermatological composition

Info

Publication number: WO1982000763A1
Application number: PCT/AU1981/000124
Authority: WO
Inventors: F Kemp
Original assignee: Individual
Current assignee: Individual
Priority date: 1980-09-01
Filing date: 1981-08-31
Publication date: 1982-03-18
Anticipated expiration: 1983-03-01
Also published as: IT8168160A0; AU7474781A; IT1144829B; FR2489149A1; ZA815892B

Abstract

Une composition est utilisee dans un procede de traitement ou de prevention d'irritations, maladies ou infections dermatologiques et comprend une quantite effective de: (a) huile d'eucalyptus en majeure partie, (b) une composition detergente qui comprend un agent tensio-actif anionique, cationique ou non ionique ou un melange de ces agents tensio-actifs; et (c) de l'huile de noix de coco ou un derive d'huile de noix de coco.A composition is used in a method of treating or preventing skin irritation, disease or infection and comprises an effective amount of: (a) eucalyptus oil for the most part, (b) a detergent composition which comprises a surfactant anionic, cationic or nonionic active ingredient or a mixture of these surfactants; and (c) coconut oil or a derivative of coconut oil.

Description

DERMATOLOGICAL COMPOSITION

The present invention relates to a method of treating infections . The method in particular relates to infections related to the skin , but is not restricted thereto . Numerous methods of preventing or treating skin infections are known but none of the known methods have proved to be fully satisfactory . There is need for improved techniques of preventing and treating derma to logical irritations , diseases and infections .

Particular difficulties have included cross infection particularly in hospital environments and the emergence of new strains resistant to standard treatment . Moreover difficulties have been encountered with the treatment of insect bites of various kinds as well as jelly fish and snake bites . An object of the present invention is to overcome or at least alleviate some of the difficulties related to the prior art.

Accordingly , there is provided a composition for use in a method of treating or preventing derma to logical irritations , diseases and infections which comprises :

(a) eucalyptus oil in a major amount;

(b) a detergent composition which includes an anionic , cationic or non-ionic surfactant or mixture thereof ; and (c) a coconut oil or coconut oil derivative .

There is further provided a method of cleansing to treat or prevent infections which comprises topically administering to a patient an effective amount of the composition specified above . The composition as specified above has surprisingly been found to have bactericidal action on a number of pathogenic bacteria . For example , Propionibacterium acnes , Escherichia Coli , Pseudomonas aeruginosa and Staphylococcus aureaus have shown to be affected by the composition of the present application.

In a further aspect of the present invention there is provided a composition for treatment or prevention of dermatological irritations , diseases and infections which comprises : (a) a major amount of eucalyptus oil;

(b) a detergent composition which includes an anionic, cationic or non-ionic surfactant or mixture thereof; (c) a coconut oil or coconut oil derivative; and (d) an effective amount of aluminium sulfate. The abovementioned composition has been found to be particularly suitable for the treatment of insect bites and other bites such as those delivered by snakes, jelly fish etc. In respect of the first component of the composition, namely the eucalyptus oil, any suitable eucalyptus oil may be used, desirably having a eucalyptene or cineole content of about 35 - 90% by volume. In fact, industrial grade eucalyptus oil having approximately a 35 - 40% eucalyptene content may be used.

As regards component (b) any suitable detergent may be used. A suitable anionic detergent is a sulfuric acid detergent known under the trade name SSA/005 which is a 60% active detergent. An alternative preferred detergent is that known under the trade name SSAL, available from Albright and Wilson, Melbourne.

In respect of the coconut oil component, pure coconut oil may be used. Alternatively, a coconut oil derivative may be used. A preferred derivative is coconut oil diethanolamide which is available under the trade mark Decolamide FAG from Streetly Chemicals or under the trade name, Teric DCE from ICI Ltd. These agents are characterised in that they have a high free diethanolamide content. A particularly preferred composition comprises about 1 to 25 % by volume detergent, about 47 to 70% essential oil and from 5 to 25% coconut oil component. For other than topical administration, lighter grades of coconut oil, as used in the food industry, may also be used.

The aluminium sulfate, component, when present, may be supplied in any effective amount. 5 - 25% by volume relative to the total composition has been found suitable. Further amounts may be used, they do not provide any appreciable advantage. The aluminium sulfate may be in the form of AL(S043.18 H₂0) and is suitably formed by addition to an aqueous composition of the other three components. A soap composition as discussed below to which the aluminium sulfate is added is particularly suitable.

The composition may be administered to the patient in any suitable manner. The composition may be administered directly e.g. orally, intravenously in like manner. For other than topical administration, component (b) may be omitted if desired. Preferably, and particularly in the cleansing aspect of the present invention, the composition is topically administered. For oral administration the composition may be provided with further components to place it into a pharmaceutically acceptable form. Such components are intended to encompass those ingredients which in themselves are pharmaceutically inactive and which are generally employed in the arts of granulation or tableting. These pharmaceutical excipients include diluents such as starch, cellulose, lactose, kaolin or powdered sugar. Additionally a binder may be used, such binder may be selected from starch, gelatine, sucrose, glucose or like materials. Other compounding ingredients generally used in the art such as flavouring agents may also be used.

For topical administration the composition may be included in known soap compositions. These may be prepared in any suitable form, for example in tablet, flake, powder or in liquid form. Alternatively the composition may be included in the form of creams, ointments, lotions etc. Lanolin may be included in the compounding of such composi tions. The amount of composition inckuded in such forms may vary but it has been found suitable to use the composition in an amount of about 3 - 35% per weight of the final product, preferably from 5 - 10% by weight.

Such compositions may be formed, for example, in the following manner: Eucalyptus oil is placed in a container, the detergent composition is added and mixed in the container and left for a short period e.g. 1 - 5 minutes. The coconut oil or coconut oil derivative may then be mixed in and blended for a period of approximately 3 minutes. This forms the basic composition en which may be used in the preparation of a soap by mixture with a soap base composition comprising an alkali metal hydroxide, water and a fatty acid source. A preferred fatty acid source is a composition which comprises 50% mutton fat and 50% beef fat but any other source of fatty acids may be used.

A liquid composition may be prepared by forming a solution or suspension of the soap described above in water after crushing the soap. A liquid composition may be prepared directly from the basic composition blend prepared as previously described. For example, a mixture of a further detergent composition, water and the blend may be prepared. A suitable further detergent is Kitalene 011 available from Lever and Kitchen. Where water is not included, a concentrate may be formed.

To such a composition may be added the aluminium sulfate preferably in an amount of from 5 - 25% by volume of the total liquid composition.

It will be understood that conventional emulsifiers and compounding ingredients may also be included in the liquid detergent and soap compositions. For example, compounding oils, builders, fillers, essences, perfumes, disinfectants, colouring agents, bleaches and/or brightening agents, may be included. The present invention will now be more fully described with reference to an embodiment thereof. The examples given illustrate the preparation of the basic composition and incorporation into a soap composition but it should be understood that. they are illustrative only and do not restrict the scope of the present invention. EXAMPLE 1

The basic composition blend was prepared with the components as follows :

Component $ by Volume Eucalyptus Oil 66 .67

Detergent Composition 14 .29

Coconut oil or coconut oil derivative 19 .05

100 .01

This represents a manufacturing formula as follows: Component Amount

Eucalyptus oil (industrial grade) 14 litres

SSAL Detergent 3 litres

Coconut Oil Diethanolamide (FAG) 4 litres

The components were mixed in the following manner: The eucalyptus was placed in a container and the detergent was added and mixed into same. The container was sealed and left for a short period e.g. 1 - 5 minutes. Coconut oil diethanolamide was then added and mixing continued for approximately 3 minutes.

(a) A soap composition was then prepared with the components as follows :

Component Amount Sodium Hydroxide 3000 gms

Fats (100% Beef) 3000 gms

Water 2 Litres

Additive Blend .20-.25 litres

The components were mixed in the following manner: The sodium hydroxide was dissolved in the water and added to an urn (preferably a stainless steel or cast iron container ) at approximately the same rate as the fats . The preparation of the soap mix then followed normal soap manu facturing conditions with stirring and boiling of the soap and separation of lye. (Alternatively the soap may be prepared in accordance with the process described in example 2 following) . Once the soap was prepared, the additive blend was mixed in until an even consistency was produced. (b) A liquid detergent composition was then prepared with the components as follows:

Component % by weight

Detergent 13.00

Additive Blend 5.00 pH regulating agent 2.50

H₂O 79.50

100.00

It will be appreciated that this represents a manufacturing formula as follows :

Component Amount ( grams )

Kitalene Detergent 117 gms

Blend 45 gms

KOH pH adj usting agent 22 .5 gms

H₂0 715 .5 gms

900 .0

The components were mixed in the following manner: The Kitalene was added to an urn (preferably a stainless steel or cast iron container) and warmed. The water and KOH were then added with stirring. Finally the blend is added with further stirring and the composition allowed to cool. (c) An aluminium sulfate containing detergent composition was the prepared with the components as follows : Component % by volume

Liquid Detergent Composition of (b) 90 Aluminium Sulfate 10

TESTING OF BACTERICIDAL ACTIVITY OF COMPOSITION Soap Solution

Soap prepared as described above (five bars) were grated using a sterile cheese grater and the shards suspended in sterile water to 20% w/w. mixed thoroughly and held for three days at 0° to assist solution of the solids: this was diluted 1:1 (w/w) before use. The pH measured (at 18°C) with a glass electrode (standardized at pH 9.0) was found to be in the range of approximately 7.9 to 8.5. This solution was warmed to 37° before use.

The level of contamination of the soap with aerobic microorganisms is low, being about 100 colony forming units/g. The soap at 0.1% concentration in buffered nutrient medium was without obvious effect on the growth of one species of pathogenic yeast and four species of pathogenic bacteria following high challenge. A 10% aqueous solution of the soap had no significant effect on Candida albicans over a 10 minute period at 37°C: the same solution had bactericidal action on four species of pathogenic bacteria under the same conditions . Microbial Content

The total aerobic microbial count of the 1055 solution was measured in three ways (USP XIX pp 590-591) . (a) Pour plate method

Using this method, 1 ml of the 10% solution yielded twelve colonies, and 0.1 ml yielded one. Estimated aerobic contamination 120 colony forming units/g of soap. (b) Most probable count by the multiple-tube method

A 0.1% solution of soap was prepared in tryptone- soya broth. This was divided into 10 ml lots, and diluted 1 in 10 and 1 in 100. Growth was observed in 6/6 tubes of the 0.1% solution and in 4/6 of the 0.01% dilution. The most probable number per gram of soap was thus 93/g. (c) By the membrane filtration method

100 ml of an 0.2% solution was filtered through two 0.45 μm membrane filters, which following washing with 3 x 100 ml lots of sterile 0.1% peptone solution, were incubated on TSA plates. Twenty colonies were detected, giving a microbial content of 100/g soap.

Minimum Inhibitory Concentration

A 0.2% solution of soap, sterilized by filtration through a 0.45 μm pore diameter membrane was mixed with an equal volume of sterile double strength nutrient broth. This sample was diluted in a half-log₁₀ dilution series and each dilution dispensed in 5 ml aliquots into sterile tubes .

Each dilution was separately challenged in triplicate with 10⁵- 10⁶ viable cells of each of the designated microbial species. After incubation at 37° for three days growth was observed in all tubes, including the highest soap concentra- tion tested (0.1%).

Germicidal Activitv of the Soap Solution

Soap solution (10 ml of 10%) held at 37° was mixed thoroughly (by pipetting) with 0.1-0.5 ml of suspension of each of five microorganisms. At 1 1/2 minutes a 0.5ml portion was transferred to 49.5ml diluent (quarter strength Ringers saline) . One ml of this dilution was immediately mixed with a 14ml molten tryptone soya agar (TSA) , and 0.5ml transferred to 49.5ml diluent, and 1.0ml of the latter plated out in the same way. These procedures were repeated for a further dilution. Thus 1ml of each of three dilution levels (10^-2, 10^-4 and 10^-6) was plated out in agar. The process was repeated for each organism under test after five minutes and ten minutes incubation with the soap solution.

The method was modified for Propionibacterium acnes in that 0.1ml of each dilution was spread on blood agar plates and the plates incubated at 37° in an atmosphere of 95% H₂, 5% CO₂ for three days. In the repeat experiment with Pseudomonas aeruginosa 0.1ml of each diluent was spread on TSA plates. All plates (other than those for Propionibacterium acnes) were read after overnight aerobic incubation at 37°. Representative colonies from plates with growth were checked for identity using gram stain and appropriate disgnostic media. Plates showing no growth were challenged with a few viable organisms of the appropriate species to check fertility. All negative plates were found to support growth on such challenge . The results are recorded in the Table.

Claims

CLAIMS :

1. A composition for use in a method of treating or preventing dermatological irritations, diseases or infections which comprises an effective amount of

(a) eucalyptus oil in a major amount, (b) a detergent composition which includes an anionic, cationic or non-ionic surfactant or mixture thereof; and (σ) a coconut oil or coconut oil derivative.

2. A composition as claimed in claim 11 wherein the eucalyptus oil is present in an amount of from 35 - 90% by volume.

3. A composition according to claim 2 wherein the eucalyptus oil has an approximate 35 - 40% eucalyptene content.

4. A composition according to any one. of the preceding claims wherein the detergent composition is a sulfuric acid detergent.

5. A composition according to any one of the preceding claims wherein the coconut oil is present as the derivative coconut oil diethanolamide .

6. A composition as claimed in any one of the preceding claims which further comprises as a further component aluminium sulfate in an effective amount.

7. A composition as claimed in any one of the preceding claims wherein the dermatological infection results from one of the following bacteria: Propionibacterium acnes, Escherichia Coli, Pseudomonas aeruginosa and Staphylococcus aureus .

8. A composition for use in a method of treating insect bites which comprises an effective amount of

(a) eucalyptus oil in a major amount; lb) a detergent composition which includes an anionic, cationic or non-ionic surfactant or mixture thereof; (c) a coconut oil or coconut oil derivative; and (d) aluminium sulfate in an effective amount.

9. A method of treating or preventing dermatological, irritations , diseases or infections which comprises administering to a patient an effective amount of composition which comprises an effective amount of

(a) eucalyptus oil in a major amount,

(b) a detergent composition which includes an anionic, cationic or non-ionic surfactant or mixture thereof; and

(c) a coconut oil or coconut oil derivative.

10. A method as claimed in claim 9 wherein the eucalyptus oil is present in an amount of from 35 - 90% by volume.

11. A method according to claim 9 wherein the eucalyptus oil has an approximate 35 - 40% eucalyptene content.

12. A method according to any one of claims 9 to 11 wherein the detergent composition is a sulfuric acid detergent.

13. A method according to any one of claims 9 to 12 wherein the coconut oil is present as the derivative coconut oil diethanolamide .

14. A method as claimed in any one of claims 9 to 13 which further comprises as a further component aluminium sulfate in an effective amount.

15. A method as claimed in any one of claims 9 to 14 wherein the dermatological infection results from one of the following bacteria: Propionibacterium acnes, Escherichia Coli, Pseudomonas aeruginosa and Staphylococcus aureus.

16. A method for treating insect bites which comprises an effective amount of

(a) eucalyptus oil in a major amount;

(b) a detergent composition which includes an anionic, cationic or non-ionic surfactant or mixture thereof; (c) a coconut oil or coconut oil derivative; and (d) aluminium sulfate in an effective amount.

17. A composition as claimed in claim 1 substantially as hereinbefore described with reference to any one of the examples .

18. A method of treating or preventing dermatological irritations , diseases or infections as claimed in claim 9 substantially as hereinbefore described with reference to any one of the examples.