Arthropoda repellent composition

Abstract

The present invention refers to an Arthropoda repellent composition providing long-term protection, in particular against insects and ticks.

Claims

1. An Arthropoda repellent composition, comprising (i) icaridin (1-(1-methylpropoxycarbonyl)-2-(2-hydroxyethyl)piperidine) in an amount from 10 wt. % to 20 wt. %, (ii) PMD (para-menthan-3,8-diol) in an amount from 10 wt. % to 20 wt. % and optionally at least one further Arthropoda repellent compound selected from DEET (N,N-diethyl-m-methylbenzamide), IR 3535 (ethyl-3-acetylbutylaminopropanoate), KBR 3023 ((RS)-sec-butyl-(RS)-2-(2hydroxyethyl) piperidine-1-carboxylate), and ethyl antranilate (ethyl-2-aminobenzoate), and (iii) at least PPG-20 methyl glucose ether in an amount of from 0.1 wt. % to 1.5 wt. %, and optionally at least one further polyol, selected from PPG-10 methyl glucose ether, propylene glycol, butylene glycol, and pentylene glycol.

2. An Arthropoda repellent composition according to claim 1, wherein the at least one further polyol is selected from propylene glycol and pentylene glycol.

3. An Arthropoda repellent composition of claim 1, wherein the total amount of Arthropoda repellent compounds in the composition ranges from 20 wt. % to 60 wt. %, referring to the weight of the total composition.

4. An Arthropoda repellent composition of claim 1, wherein the total amount of said polyols in the composition ranges from 0.2 wt. % to 20 wt. %, referring to the weight of the total composition.

5. An Arthropoda repellent composition of claim 1, comprising icaridin and PMD in a weight ratio of from 3:1 to 1:2.

6. An Arthropoda repellent composition of claim 1, comprising (i) not more than 30 wt. % of any C1-5 alcohol, and/or (ii) no polymer compound having more than 100 monomeric units, and/or (iii) less than 5 wt. % of any surfactant.

7. An Arthropoda repellent composition of claim 1, fulfilling at least one of the following: (i) the composition is a liquid, a cream, a lotion, or a gel, (ii) the composition comprises water in an amount of from at least 5 wt. % to 65 wt. %, referring to the weight of the total composition, (iii) the composition has a viscosity of 0 to 200 Pa*s at 20° C.

8. An Arthropoda repellent composition of claim 1, comprising besides the polyols (iii) further a polyethylene glycol with a maximum of 80 EO units.

9. An Arthropoda repellent composition of claim 1, having a pH in a range of from pH 4 to pH 7.

10. An Arthropoda repellent composition of claim 1 provided in a container having a spraying device allowing to spray said composition in a form of fine droplets.

11. Use of the Arthropoda repellent composition of claim 1 to repel insects and/or ticks from contacting human or animal skin and/or from stinging.

12. A method for repelling insects or ticks from contacting human or animal skin and/or from stinging, comprising applying the Arthropoda repelling composition of claim 1 to the skin of the human or animal.

13. An Arthropoda repellent composition of claim 1, wherein the at least one further polyol is present.

14. An Arthropoda repellent composition of claim 13, wherein the at least one further polyol comprises PPG-10 methyl glucose ether.

15. An Arthropoda repellent composition of claim 13, wherein the at least one further polyol comprises propylene glycol.

16. An Arthropoda repellent composition of claim 13, wherein the at least one further polyol comprises butylene glycol.

17. An Arthropoda repellent composition of claim 13, wherein the at least one further polyol comprises pentylene glycol.

18. An Arthropoda repellent composition of claim 1, wherein the at least one further Arthropoda repellent compound is present.

19. An Arthropoda repellent composition of claim 1, wherein PPG-20 methyl glucose ether is present in an amount of about 0.5 wt. %.

20. An Arthropoda repellent composition of claim 1, wherein PPG-20 methyl glucose ether is present in an amount of 0.5 wt. %.

Description

EXAMPLES

(1) The following Examples show the effect of compositions according to the invention (E) in comparison to compositions not falling under the invention (V) to repel Mosquitoes Aedes aegypti from biting a human volunteer

(2) Female mosquitoes belonging to the genus Aedes were reared according to a standard protocol at a temperature of 27.5±0.5° C., a relative humidity of 65-85% and a 12:12 hour photo period. The light period (450 Lux) was set from 8:00 to 20:00. After hatching from the eggs, larvae were kept in water basins (30×30×10 cm) filled with a 1:1 mixture of deoxygenized tap- and deionized water and fed with fish food flakes (Tetra Min®). Prior to the emergence, pupae were transferred to a holding cage (40×30×20 cm). Adult mosquitoes were provided with sugar solution (10% dextrose) and used at an age of 5 to 15 days for the repellent tests.

(3) 30 of the mosquitos each have been placed into test cages having a volume of 27.000 cm.sup.3 (41×41×16 cm). Cage tests have been carried out in a climatized room (4.5×4.5×2.5 m) without windows at a temperature of 27.5±0.5° C. and a relative humidity of 65±5% rF. The light intensity was 450 Lux.

(4) For the Examples aqueous compositions were prepared comprising besides water and the below specified ingredients a suitable amount of PEG-8 (between 10 and 25 wt. %) and an amount of ethanol.

(5) A quantity of the respective compositions as defined in Table 1 below was applied to a defined area on the forearms of volunteers (carried out as triple test, n=3). Prior to the application the skin was washed with fragrance-free soap, rinsed with water and wiped with 50% isopropyl alcohol. An area larger than the test window was marked to ensure that the exposed skin was entirely treated with repellent substance. The marked area had a size of ca. 100 cm.sup.2.

(6) Test formulations were applied to a defined area on one forearm of each volunteer. Zero control tests were performed prior to each individual efficacy test and the exact time until 10 landings occurred was documented. With this time value, repellent protection on the treated arm could be calculated according to the following formula:

(7) $\mathrm{Protection}\mathrm{in}\%=100-\frac{.Math.\mathrm{of}\mathrm{probings}\mathrm{on}\mathrm{treated}\mathrm{skin}\mathrm{per}\mathrm{time}\mathrm{unit}}{.Math.\mathrm{of}\mathrm{probings}\mathrm{on}\mathrm{untreated}\mathrm{skin}\mathrm{per}\mathrm{time}\mathrm{unit}}\times 100$

(8) Repellent efficacy was verified for the first time shortly after product application and then again in regular 30 minutes intervals up to a maximum of 8 hours (Example V2 12 hours) or until repellency failed. Each single test lasted 2 minutes, during this time the number of landings and bites on the treated skin were recorded.

(9) Repellent efficacy was evaluated using 1. the time until first bite, 2. the time until protection from bites reached less than 95% compared to untreated skin (several bites within the same time frame).

(10) The <95% value represents the end of complete protection time and is used as the criterion for break-off for repellent tests.

(11) Tests were conducted with three volunteers. All volunteers were attractive to the test mosquito species, thereby meeting the requirements to participate in repellent efficacy studies. Each volunteer received his or her own cage. Cages were connected to the air ventilation system in between single tests (zero control and efficacy test) to avoid an accumulation of host odors and active ingredients inside the cage. Test mosquitoes that started to engorge blood during a test were replaced by new individuals to ensure that the number of host-seeking females stayed constant throughout the test day.

(12) TABLE-US-00001 TABLE 1 Amount Amount Amount First bite <95% Example PMD .sup.(1) Icaridin .sup.(2) Glucam .sup.(3) application [hours] [hours] V1 10% 1.67 mg/cm.sup.2 2.5 +/− 0.5 V2 10% 4 mg/cm.sup.2 3.5 +/− 0.5 V3 10% 0.5% 1.67 mg/cm.sup.2 2.8 +/− 0.62 3.5 +/− 1.71 V4 10% 0.5% 4 mg/cm.sup.2 4.2 +/− 1.03 V5 25% 2.0% 4 mg/cm.sup.2 4.5 +/− 0.6 V6 10% 1.67 mg/cm.sup.2 2.83 +/− 0.24 7.0 +/− 1.1 E1 10% 0.5% 1.67 mg/cm.sup.2 4.5 +/− 2.68 7.33 +/− 0.62 V7 20% 1.67 mg/cm.sup.2 4.0 +/− 1.3 8 +/− 1 E2 10% 20% 0.5% 1.67 mg/cm.sup.2 8.0 +/− 0 .sup.(4) 12 .sup.(5) .sup.(1) (1-(1-methylpropoxycarbonyl)-2-(2-hydroxyethyl)piperidine .sup.(2) para-menthan-3,8-diol .sup.(3) PPG-20 methyl glucose ether .sup.(4) No bite within 8 hours, next value was taken at 12 hours .sup.(5) Experiment stopped at 12 hours

(13) As can be seen by the Examples the addition of PPG-20 methyl glucose ether to the repellent Icaridin provides a noticeable increase in the time period protecting the skin against the first insect bite (see V6 vs E1), in fact the addition extends the time up to the first bite to become longer than for twice the amount of Icaridin (E1 vs. V7). However, only a slight effect can be observed for the addition of PPG-20 methyl glucose ether to the repellent PMD (see V1 vs. V3 and V2 vs. V4). Even if a considerable higher amount of PMD and PPG-20 methyl glucose ether is combined (V5 vs. V4), no convincing effect can be obtained.

(14) IF PPG-20 methyl glucose ether is added to a composition comprising a combination of Icaridin and PMD, both the time period until the insects bite the first time and the time until the repellent protection falls below 95% can be considerably extended (see E2) compared to all the other compositions, This effect was not foreseeable, since in E2 both repellents are present on the skin at the same time, thus, it would have been expected that for the combination of these two repellents an effective time should be obtained comparable to the time provided by Icaridin alone (which clearly is exceeding the effective time of PMD). Thus, the combination of the three ingredients Icaridin, PMD and PPG-20 methyl glucose ether result in a repellent having a superior effect compared to the single repellents.