GB2222774A

GB2222774A - Lice control

Info

Publication number: GB2222774A
Application number: GB8919030A
Authority: GB
Inventors: James Beament; Daniel Frederick Cutts
Original assignee: Euro Celtique SA
Current assignee: Euro Celtique SA
Priority date: 1988-09-15
Filing date: 1989-08-21
Publication date: 1990-03-21
Anticipated expiration: 2009-08-21
Also published as: GB8919030D0; GB2222774B; GB8821586D0

Abstract

A method for controlling lice or their ova on a human subject consists of applying to the human subject a topical, pharmaceutical composition containing a sugar fatty acid ester, a hydrophilic cellulose derivative and a diluent or carrier. Preferably the sugar fatty acid ester is a sucrose fatty acid ester and the cellulose is a cellulose ether especially a hydroxyalkylcellulose ether. The composition may also contain a film-forming polymer and/or a lousicide/insect repellent. Application of the composition forms a thin film on the hair. This film causes the louse not to recognise the host as being a human head with hair. The louse then either leaves the site or fails to infest the site.

Description

A METHOD FOR CONTROLLING LICE OR THEIR OVA The present invention relates to a method for controlling lice or their ova on human subjects.

According to the present invention, there is provided a method for controlling lice or their ova on d human subject comprising applying to the human subject a topical, pharmaceutical composition comprising d sugar fatty acid ester, a hydrophilic cellulose derivative and a pharmaceutically acceptable diluent or carrier.

The sugar fatty acid ester is an ester of sugar and d fatty acid.

Preferably the sugar is selected from the disaccharides, sucrose, dextrose, maltose, fructose (and lactose. Sucrose is particularly preferred. The fatty acid preferably contains between 8 and 22 carbon atoms, especially between 10 dnd 20 carbon atoms.

The sugar fatty acid ester may be a single sugar fatty acid ester or a mixture of sugar esters of fatty acids, the residue of which (acids) contain different numbers of carbon atoms. The degree of esterification of the sugar fatty acid ester will depend on its method of production/purification/etc. In the present invention, monoesters or mixtures of esters having d high (preferably 40%, especially 45%, or more by weight) monoester content are preferred.

Examples of sugar fatty acid esters preferred for use in the present method are sucrose etc. caprylate, decanoate, laurate, myristate, palmitate, stedrate, pelargonate, undecanoate, tridecanoate, and heptadecanoate. Sucrose stearate and/or sucrose palmitate are particularly preferred. Although sugar esters of unsaturated fatty acids, such as sucrose etc oleate, linoleate, linolenate, arachidate and ricinoleate may also be used, the sugar esters of saturated fatty acids are preferred.

Alternatively, the sugar fatty acid ester may comprise a mixture of sugar fatty acid esters, derived from the esterification (with a sugar) of naturally occurring mixtures of fatty acids (or fatty acid triglycerides). Suitable natural sollrces of fatty acids (or thcir triglycerides) are palm oil, peanut oil, coconut oil or, which is preferred, tallow oil, especially beef tallow oil In this case, the mixture of sugar fatty acid esters preferably contains 40%, especially 45%, by weight or more of monoesters and 60%, especially 55%, by weight or less of diesters, triesters, polyesters and other residues (such a mono-, di- or triglycerides).

When sugar esters of beef tallow fatty acids are employed the fatty acid content is preferably about 70% (by weight) stearic acid and about 30% (hy weight) palmitic acid.

The hydrophilic cellulose derivative may be water soluble or water dispersib]e. It is preferably a cellulose ether, such as carboxymethyl cellulose, especially a hydroxyalkyl cellulose ether, such as hydroxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose or hydroxypropylmethyl cellulose.

The choice of pharmaceutically acceptable diluent or carrier will depend on the dosage form envisaged. In the case of a shampoo, Zotiorl, gel or spray, the sugar fatty acid ester and the cellulose derivative, together with other materials such as surfactants, antioxidants, stabilisers, preservatives and perfumes, may be dissolved or dispersed in an aqueous solution, an aqueous alcoholic solution or an alcoholic solution. Generally lower alkyl (C1-C4) alcohols, such as ethanol or isopropanol, are employed.

The sugar fatty acid ester content of the present composition is preferably from 0.2 to 2%, especially from 0.2 to 1%, (by weight). A preferred concentration of the cellulose derivative is from 0.1 to 5%, especially from 0.5 to 32, (by weight).

In addition to the sugar fatty acid ester and the cellulose derivative, the present composition may also contain i. A film forming polymer such ds, Povidone-Vinyl Acetate copolymer, ii. A lousicide such as permethrin, carbaryl, malathion or phenothr in, iii. An insect repellent, such as dibutyl phthalate, diethyltoluamide, dimethyl phthalate and ethohexadiol.

iv. A phosphatide, such as lecithin.

v. A conditioner, such as a Quaternary ammonium derivative.

The present method is used to control lice or their ova in humans, by applying the composition to d site of infestation or to a site believed to be infested. Alternatively, the composition may be used prophylactically to prevent infestation.

Without wishing to limit the present invention in any way, it is believed that the mode of action of the present composition is ds follows: Application of the composition to an appropriate site (e.g.

the head) forms a thin film of the sugar fatty acid ester/cellulose derivative combination on the hair. (The formation of this thin film is enhanced by the additional presence of a phosphatide, such as lecithin). The presence of the thin film, which is not detectable by sight, touch or smell, causes the louse not to recognise the host as being, e.g. human head with hair. The louse then either leaves the site (if an infestation is treated) or refuses to infest the site (if the composition is used prophylactically).

In a further aspect of the present invention there is provided a topical, pharmaceutical composition for the control of lice or their ova on a human subject comprising a sugar fatty acid ester, a hydrophilic cellulose derivative and a pharmaceutically acceptahle diluent or carrier.

A still further aspect of the present invention provides the use of a sugar fatty acid ester and a hydrophilic cellulose derivative for the manufacture of a topical pharmaceutical composition for the control of lice or their ova on a human subject. The present method and composition will now be described by way of Example only.

Example 1 A gel composition having the following formulation was prepared, t w/w Hydroxypropylmethyl cellulose 15cps 2.0 DK Ester F140W (Trade Mark) 0.2 (Sucrose esters of stearic (70%) and palmitic (30t) acids containing 60% monoester).

Polyethylene Glycol 400 0.2 Water to 100.0 Example 2 A spray composition having the following formulation was prepared, t w/w Hydroxypropylmethyl cellulose, 15 cps 0.75 DK Ester F90W (Trade Mark) 0.2 (Sucrose esters of stearic (70S) and palmitic (30%) acids containing 45% monoesters) Povidone-Vinyl Acetate copolymer 0.75 Polyethylene Glycol 400 0.5 Cetyl Alcohol 2.0 Povidone 1.0 Perfume q.s.

Ethanol (95%) 50.0 Water to 100.0 Example 3 A gel composition having the following formulation was prepared, t (w/w) Sodium carboxymethyl cellulose 2.0 DK Ester Fl 60W (Trade Mark) 0.5 (Sucrose esters of stearic (70%) and palmitic (30%) acids containing 70t monoesters) Propylene glycol 0.2 Water 97.3 Example 4 A gel composition having the following formulation was prepared, t (w/w) Hydroxypropylmethyl cellulose 1.5 (Methocel El5, Trade Mark) DK Ester F140W (Trade Mark) 0.4 Quaternary ammonium functional polypeptide 2.0 (C10H21-C18H37), polypeptide backbone m.wt about 20000 (Croquat M, Trade Mark) Tsocetyl stearate 1.0 (Crodamol ICS, Trade Mark) Water 95.1 Example 5 A composition having the following formulation was prepared, % (w/w) Sodium carboxymethylcellulose 1.0 nK Ester F140W (Trade Mark) 0.4 Propylene glycol 0.2 Water 98.4 Example 6 A gel composition having the following formulation was prepared, S (w/w) Sodium carboxymethyl cellulose 1.0 Hydroxypropylmethyl cellulose (Methocel E15, Trade Mark) 0.3 DK Ester F340W (Trade Mark) 0.2 Polyethylene glycol 400 1.0 Water 97.5 Example 7 A spray composition having the following formulation was prepared, % (w/w) Hydroxypropylmethyl cellulose 1.5 (Methocel E15, Trade Mark) Povidone-Vinyl Acetate copolymer 1.5 (Kollidon-VA 64, Trade Mark) DK Ester F90W (Trade Mark) 0.2 Polyethylene glycol 400 1.0 Polyoxyethylene alkyl ether 1.0 (Brij 58, Trade Mark) 95% Ethanol 50.0 Water 44.8 Example 8 A spray composition having the following formulation was prepared as described in Example 7 except that the water ethanol medium was replaced by 95S ethanol (94.89).

Example 9 A spray composition having the following formulation was prepared.

% (w/w) Hydroxypropylmethyl cellulose 0.75 (Methocel E15, Trade Mark) Povidone-Vinyl Acetate copolymer 0.75 (Kollidon-VA64, Trade Mark) DK Ester F90W (Trade Mark) 0.2 Polyethylene glycol 400 0.5 Brij 58 (Trade Mark) 1.0 Quaternary ammonium polymer 1.0 (Gafquat 755N, Trade Mark) Perfume 1.0.

Isopropyl Alcohol 50.0 Water 44.8 Example 10 A gel composition having the following formulation was prepared, t (w/w) Hydroxypropylmethylcel lulose 0.75 (Methocel E15, Trade Mark) Povidone - Vinyl Acetate copolymer 0.75 (Kollidon - VA 64, Trade Mark) DK Ester F9OW (Trade Mark) 0.2 Glycerin B.P. 1.0 Quaternary Ammonium Polymer . 2.0 (Gafquat 755N, Trade Mark) Carbomer (Carbopol 934P, Trade Mdrk) 0.35 Triethanolamine 0.53 Hydroxybenzoate Preservative 0.13 (Nipastat, Trade Mark) Perfume 1.0 Water 93.29 F.xample 11 A gel composition having the following formulation was prepared, 2 (w/w) Hydroxypropylmethyl cellulose 0.75 (Methocel E15, Trade Mark) Povidone - Vinyl Acetate copolymer 0.75 (Kollidon - VA 64, Trade Mark) DK Ester F90W (Trade Mark) 0.2 Polyethylene Glycol 400 0.5 Quaternary Ammonium Polymer 1.0 (Gafquat 755N, Trade Mark) Carbomer (Carbopol 934P, Trade Mark) 0.5 Tr ethanolamine 0.75 Polyoxyethylene dlkyl ether 1.0 (Brij 58, Trade Mark) Water 94.6 Example 12 The gel composition of Example 11 was prepared except that the level of Carbomer was reduced to 0.1t (w/w), the level of triethanolamine was reduced to 0.15t (w/w) and the level of water was increased to 95.6 (w/w).

Example 13 A gel composition having the following formulation was prepared, t (w/w) Hydroxypropylmethyl cellulose 2.0 (Methocel E15, Trade Mark) Povidone - Vinyl Acetate copolymer 2.0 (Kollidon - VA 64, Trade Mark) DK Ester F90W (Trade Mark) 0.2 Glycerin B.P. 1.0 Quaternary Ammonium Polymer 2.0 (Gafquat 755N, Trade Mark) Carbomer (Carbopol 934P, Trade Mark) 0.35 Triethaolamine 0.53 Water 91.9 Example 14 A spray compositioll having the following formulation was prepared, % (w/w) Hydroxypropylmethyl cellulose 1.5 (Methocol E15, Trade Mark) Povidone - Vinyl Acetate Copolymer 4.0 (Kollidon - VA 64, Trade Mark) DK Ester F70W (Trade Mark) 0.2 (Sucrose esters of stearic (70%) and palmitic (30%) acids containing 40% monoesters) Polyethylene glycol 400 2.0 Polysorbate (Tween 60, Trade Mark) 0.5 Ethanol (95%) 50 Water 41.8 Example 15 Treatment A lotion according to Example 9 was packed in a pump-action spray bottle.

The lotion was sprayed onto the wet hair of a subject and combed through until there was an even application over the hair. The hair was allowed to dry naturally.

Example 16 Treatment A gel according to Example 10 was applied to the wet hair of a subject and combed through until there was an even application over the hair. The hair was allowed to dry naturally.

Claims

1. A method for controlling lice or their ova on a human subject comprising applying to the human subject a topical, pharmaceutical composition comprising a sugar fatty acid ester, d hydrophilic cellulose derivative and a pharmaceutically acceptable diluent or carrier.

2. A method according to claim 1 wherein the sugar fatty acid ester comprises a disaccharide ester of a fatty acid.

3. A method according to claim 2 wherein the disaccharide comprises sucrose, dextrose, maltose, fructose or lactose.

4. A method according to claim 3 wherein the disdccharide comprises sucrose.

5. A method according to any one of claims 1 to 4 wherein the sugar fatty acid ester comprises a sugar ester of a C.-C22 fatty acid.

6. A method according to claim 5 wherein the sugar fatty acid ester comprises a sugar ester of d Clo~C2o fatty dCid.

7. A method according to any one oe claims 1 to 6 wherein the sugar fatty acid ester comprises a sugar ester of a saturated fatty acid.

8. A method according to claim 7 wherein the sugar fatty acid ester comprises sucrose caprylate, sucrose decanoate, sucrose laurate, sucrose myristate, sucrose palmitate, sucrose stearate, sucrose pelargonate, sucrose undecanoate, sucrose tridecanoate or sucrose heptadecanoate.

9. A method according to claim 8 wherein the sugar fatty acid ester comprises sucrose palmitate or sucrose stearate.

10. A method according to any one of claims 1 to 9 wherein the sugar fatty acid ester is a single monoester.

11. A method according to any one of claims 1 to 9 wherein the sugar fatty acid ester is a mixture of esters.

12. A method according to claim 11 wherein the monoester content of the mixture of esters is at least 45% (by weight).

13. A method according to either claim 11 or claim 12 wherein the mixture of esters is derived from the esterication with a sugar of a naturally occurring mixture of fatty acids or fatty acid triglycerides.

14. A method according to claim 13 wherein the naturally occurring mixture of fatty acids or fatty acid triglycerides is derived from palm oil, peanut oil, coconut oil or tallow oil.

15. A method according to claim 14 wherein the naturally occurring mixture of fatty acids or fatty acid triglycerides is derived from tallow oil.

16. A method according to claim 15 wherein the tallow oil is beef tallow oil.

17. A method according to claim 16 wherein the sugar fatty acid ester has a fatty acid content of about 70% (by weight) stearic acid and about 302 (by weight) palmitic acid.

18. A method according to any one of claims 1 to 17 wherein the hydrophilic cellulose derivative comprises a cellulose ether.

19. A method according to claim 18 wherein the cellulose ether comprises a hydroxyalkyl cellulose ether.

20. A method according to claim 19 wherein the cellulose ether comprises hydroxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose or hydroxypropylmethyl cellulose.

21. A method according to any one of claims 1 to 20 wherein the diluent or carrier comprises water, aqueous alcohol or alcohol.

22. A method according to claim 21 wherein the alcohol comprises a C-C4 alcohol.

23. A method according to claim 22 wherein the alcohol comprises ethanol or isopropanol.

24. A method according to any one of claims 1 to 23 wherein the topical pharmaceutical composition contains from 0.2% to 2% (by weight) of sugar fatty acid ester.

25. A method according to claim 24 wherein the composition contains from 0.2% to 1% (by weight) of sugar fatty acid ester.

26. A method according to any one of claims 1 to 25 wherein the topical, pharmaceutical composition contains from 0.1% to 5% (by weight) of hydrophilic cellulose derivative.

27. A method according to claim 26 wherein the composition contains from 0.58 to 3t (by weight) of hydrophilic cellulose derivative.

28. A method according to any one of claims 1 to 27 wherein the topical, pharmaceutical composition further comprises a film forming polymer.

29. A method according to claim 28 wherein the film forming polymer comprises povidone-vinyl acetate copolymer.

30. A method according to any one of claims 1 to 29 wherein the topical, pharmaceutical composition further comprises a lousicide.

31. A method according to claim 30 wherein the lousicide comprises permethrin, carbdryl, malathion or phenothrin.

32. A method according to any one of claims 1 to 31 wherein the topical, pharmaceutical composition further comprises an insect repellent.

33. A method according to claim 32 wherein the insect repellent comprises dibutyl phthalate, diethyltoluamide, dimethyl phthalate or ethohexadiol.

34. A method according to any one of claims 1 to 33 wherein the topical, pharmaceutical composition further comprises a phosphatide.

35. A method according to claim 34 wherein the phosphatide comprises lecithin.

36. A method according to any one of claims 1 to 35 wherein the topical, pharmaceutical composition further comprises a conditioner.

37. A method according to claim 36 wherein the conditioner comprises a quaternary ammonium derivative.

38. A method for controlling lice or their ova on a human subject substantially as hereinbefore described with particular reference to Example 15.

39. A topical, pharmaceutical composition for the control of lice or their ova on a human subject comprising a sugar fatty acid ester, a hydrophilic cellulose derivative and a pharmaceutically acceptable diluent or carrier.

40. A topical pharma:eutical composition substantially as hereinbefore described with particular reference to any one of the Examples 1 to 14.

4]. The use of a sugar fatty acid ester and d hydrophilic cellulose derivative for the manufacture of a topical, pharmaceutical composition for the control of lice or their ova on a human subject.