Insecticide agent for extirpation of lice and ektoparazit domestik aminals

¹ The invention relates to an insectieid hair lotion having a prolonged residual effect for use in the human and veterinary field.

Older, not completely safe insecticides, such as DDT e gamme HCH, were applied against the head lice mostly in the form of 1% water emulsion, which had to be washed again after a long exposure time (6 to 24 hours) with soap or shampoo (Nerakain ).

Highly effective and fast acting pyrethroids have made it possible to produce insecticidal shampoos, which are often formulated as sprays. Their use is the most environmentally friendly in terms of hygiene and space. A prerequisite for their full and sustained successful use is a higher level of hygiene and prevention of reinfestation.

Both types of the above-mentioned anti-pediculosis preparations are characterized by very short efficacy residues, which generally limit to zero due to subsequent washing and wash-out of the active substances before they bind to the hair or due to their rapid degradation in the case of poorly stable active substances. eg light-decaying types of pyrethroids).

Ectoparasites of domestic animals, in addition to spraying and bathing used in large-scale farms, also use pyrethroid shampoos without residual efficacy or semi-dry sprays with organophosphates.

It has now been found that the disadvantages of the current state, ie short residual effects, are eliminated by means of lice control of infant and ectoperasite pet animals based on insecticidally active substances (pyrethroids, organophosphates and chlorinated insecticides), monoglycols or polyglycols, lower alcohols. , perfume and water, containing according to the invention 0.1 to 5% of polymers or copolymers or derivatives of vinylpyrrolidone with an average molecular weight of 10,000 to 1,000,000.

An advantage of the inventive additions is that when using macromolecular polymers with high affinity for hair or fur (i.e., polypeptides) and good solubility, respectively. The ability to form adducts with a number of organic compounds will significantly prolong the residual effects. It is therefore particularly suitable to use polyvinylpyrrolidone having a mean molecular weight of 10,000 to 1,000,000 or copolymers of polyvinylpyrrolidone, for example a copolymer of vinylimidazolium methochloride and vinylpyrrolidone. Substantivity to hair and skin due to the essentially peptide bond of pyrrolidone allows long-term fixation of these polymers to the hair or hair, as well as fixation of the insecticidally active compounds and thus conditional prolongation of biological activity. A further benefit of the use of polyvinylpyrrolidone and its copolymers is its protective effects, particularly desirable with respect to the use of organic solvents and application to the skin, particularly in the pediatric population. If safe, active substances (especially pyrethroids) are used in such a formulation, there is no increased toxicological risk.

He did

Hair water containing 0.5 parts of permethrin, 1 part of polyvinylpyrrolidone PVP K 30, parts of monopropylene glycol, 78.5 parts of anhydrous ethyl alcohol was filled into an aerosol can and supplemented with dichlorodifluoromethane in a ratio of 7: 3.

The product was applied by a spray with a prolonged nozzle to the jails of the pupils of the special school by spraying for 0.5 to 1 s at 8 to 10 hairstyles. Immediately after application, the product was spread over the entire surface of the skin covered with hair. At the same time, the same formulation without polyvinylpyrrolidone was tested in the same way for other probants.

When using the formulation with polyvinylpyrrolidone, 50 days after application, a new lice incidence was found in less than 10% of children. Using a polyvinylpyrrolidone-free formulation, lice began to appear significantly earlier, after 10 days in 10% of children. In two cases larvae were found on day 10, indicating survival of nits.

<td>Formulations · '</td><td>Number of</td><td colspan="3">% Attacked persons in days after application</td>

<td></td><td>1</td><td> ,0 20</td><td> 30</td><td> 50</td>

<td>without PVP</td><td> 57</td><td>in</td><td> 0</td><td> 9,6</td><td> 25,5</td><td> 42</td><td> -</td>

<td>8 PVP</td><td> 104</td><td></td><td> 0</td><td> 0</td><td> 1</td><td> -</td><td> 9,4</td>

When investigating ovicidal effects in vitro, using a formulation with polyvinylpyrrolidone did not hatch a significant percentage of nits at all, and none of the larvae was able to completely enclose the egg shells. When applying the formulation without polyvinylpyrrolidone, a certain percentage of nits also died, but 7% of the larvae left the egg shells.

Example 2

Hair water containing 2 parts of trichlorphone, 1 part of polyvinylpyrrolidone, 20 parts of monopropylene glycol, 77 parts of anhydrous ethyl alcohol was filled into an aerosol container and supplemented with dichloromethane in a 7: 3 ratio.

The formulation was applied as in Example 1 and at the same time the formulation without polyvinylpyrrolidone was tested in the same way.

When using the polyvinylpyrrolidone formulation, 20% of children were rewound within 10 days after dosing, while nearly 90% of children were rewound within 10 days using the same formulation without polyvinylpyrrolidone.

<td rowspan="2">Formulation</td><td rowspan="2">Number of treated</td><td rowspan="2">% Of persons attacked in 1</td><td colspan="2">days after application</td>

<td> 10</td><td> 20</td>

<td>without PVP</td><td> 8</td><td> 0</td><td> 87</td><td> 100</td>

<td>ε PVP</td><td> 20</td><td> 0</td><td> 20</td><td> 50</td>

Example 3

Hair water containing 0.5 parts of permethrin, 1 part of a copolymer of vinylimidazolium methochloride and vinylpyrrolidone, 6 parts of polyethylene glycol 300, 67 parts of ethyl alcohol, parts of water and 0.5 parts of perfume was tested in vitro compared to the same formulation without the above polyvinylpyrrolidone copolymers. Simultaneously, both formulations according to Example 1 were tested, and were used without propellant (dichlodifluoromethane). The insecticidal activity was determined by determining the% mortality of female housefly, a susceptible strain of SRS / WHu in 24 hours after bathing in an aqueous solution of the following concentration:

<td>Concentration</td><td colspan="4">% Mortality</td>

<td>% of the preparation</td><td>Example 1</td><td>Example 1</td><td>Example 3</td><td>Example 3</td>

<td></td><td>without PVP</td><td>with PVP</td><td>without Kop. PVP</td><td>with kick. PVP</td>

<td> 0,000 1</td><td> 100</td><td> 100</td><td> 100</td><td> 100</td>

<td> 0,000 01</td><td> 93</td><td> 100</td><td> 100</td><td> 100</td>

<td> 0,000 001</td><td> 86</td><td> 100</td><td> 100</td><td> 100</td>

<td> 0,000 000 1</td><td> 6</td><td> 27</td><td> 47</td><td> 86</td>

<td> 0,000 000 01</td><td> 6</td><td> 6</td><td> 33</td><td> 80</td>

<td> 0,000 000 001</td><td> 0</td><td> 0</td><td> 0</td><td> 6</td>

A good insectieid efficacy of the preparation of Example 3 against head lice is also obtained by comparing the effects of the samples of Example 1β according to Example 3 on housefly. The above results also show a positive effect of polyvinylpyrrolidone (or copolymers thereof) on the immediate insecticidal activity, in this case, due to the better binding of the preparation to the surface of the insect's body.

Example 4

Hair lotion containing 1 part molathion, 0.5 part quaternary derivative of PVP (poly (3-pyrrolidonyl-1- (N, N, N-trimethyl)) - 1-propylenylammonium chloride /), 5 parts nolvetlene ethylene in 300, 0.5 93 parts of perfume, 93 parts of isopropyl alcohol were filled into an aerosol container and supplemented with dichlorodifluoromethane in a ratio of 7: 3.

The formulation was applied as in Example 1 and the formulation without PVP derivative was again tested in the same manner.

When using a formulation without a PVP derivative, 27% of children were naïve 18 days after dosing, whereas there was no louse after 18 days when using the same formulation with a PVP derivative.

<td rowspan="2">Formulation</td><td colspan="2" rowspan="2">Number of treated 1</td><td colspan="2">% Attacked people after days of application</td>

<td> 8</td><td> 18</td>

<td>bez der. PVP</td><td> 41</td><td> 0</td><td> 14</td><td> 27</td>

<td>s der. PVP</td><td> 45</td><td> 0</td><td>0 x /</td><td>- o</td>

x / in three cases, the dead dead were piled

Example 5

Hair water containing 1 part methoxychlor, 1 part polyvinylpyrrolidone, 6 parts polyethylene glycol 300, 92 parts isopropanol was tested in vitro as in case 3, and the formulation without polyvinylpyrrolidone was again tested in the same way. The mortality rate of the female housefly 24 hours after bathing in the aqueous suspension of the preparation was again significantly cleared for the formulation containing PVP:

<td rowspan="2">Concentration% of preparation</td><td colspan="2">% Mortality</td>

<td>with PVP</td><td>without PVP</td>

<td> 0,001</td><td> 1 00</td><td> 100</td>

<td> 0,000 1</td><td> 100</td><td> 93</td>

<td>0,000 b,</td><td> ,00</td><td> 86</td>

<td> 0,000 00,</td><td> 86</td><td> 47</td>

<td> 0,000 000 1</td><td> 6</td><td> 0</td>

<td> 0,000 000 01</td><td> 0</td><td> 0</td>

<td>In the examples 1</td><td>1 to 5 polymers were used</td><td>with the following molecular weight:</td>

<td>Example</td><td> 1</td><td>approx</td><td> 40</td><td> 000</td>

<td>Example</td><td> 2</td><td>approx</td><td> 40</td><td> 000</td>

<td>Example</td><td> 3</td><td>approx</td><td> 150</td><td> 000</td>

<td>Example</td><td> 4</td><td>_ approx</td><td> 000</td><td> 000</td>

<td>Example</td><td> 5</td><td>approx</td><td>io</td><td> 000</td>

SUBJECT: THE INVENTION