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  Use of polysiloxanes having quaternary ammonium groups as formulation auxiliaries, and compositions comprising themUSPTO Application #: 20060111323Title: Use of polysiloxanes having quaternary ammonium groups as formulation auxiliaries, and compositions comprising them Abstract: The present invention relates to the use of polysiloxanes containing at least one quaternary ammonium group as formulation auxiliaries in formulations of pharmaceutically and veterinary active compounds, and to compositions comprising a) a pharmaceutically or veterinary active compound and b) a polysiloxane derivative containing at least one quaternary ammonium group per molecule, if appropriate, further auxiliaries and carriers. (end of abstract)
Agent: Patent Department Bayer Corporation - Pittsburgh, PA, US Inventors: Kirkor Sirinyan, Kerstin Heinen USPTO Applicaton #: 20060111323 - Class: 514063000 (USPTO) Related Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Designated Organic Active Ingredient Containing (doai), Silicon Containing Doai The Patent Description & Claims data below is from USPTO Patent Application 20060111323. Brief Patent Description - Full Patent Description - Patent Application Claims
[0001] A large number of polysiloxanes having terminal quaternary amino groups and their use as so-called "Conditioners" in shampoos and hair-care compositions are known from EP-A 0 017 121, 0 017 122, 0 282 720, 0 294 642, 0 166 122 and 0 164 668. [0002] A problem which is frequently encountered in the preparation of active compound formulations in the field of pharmacy and veterinary medicine is, in particular in the case of aqueous formulations, the insufficient solubility of the active compounds, and the associated insufficient storage-stability of the finished formulations. [0003] To use active compounds, some of which are difficult to dissolve in water, in the form of dermally applicable liquid formulations, it is necessary to prepare homogeneous solutions or emulsions based on organic solvents and insecticidally active compounds. To this end, the active compounds are usually dissolved in organic solvents, such as isopropanol, 2-butoxyethyl acetate, ethylene glycol diacetate, and, if appropriate, mixed with further additives. The preparation of such formulations is described in U.S. Pat. No. 4,874,753, EP-A 137 627 and GB 2 135 886. Said systems have the disadvantages that, for example when active compounds from the class of the pyrethrins and pyrethroids, in particular .alpha.-cyanopyrethroids are used, they lead to severe skin irritations and furthermore have a short long-term action. It is desirable to replace these formulations by formulations which are skin-compatible and toxicologically acceptable and have a long-term action of several weeks. [0004] To remedy said disadvantage, for example of the known pyrethroids and pyrethrins, patents AU-627 847, EP-A 413 610 propose to dissolve these active compounds in high-boiling solvents, such as monopropylene glycol, which additionally contain natural skin-compatible oils, such as pine oil, sunflower oil or soya oil. Furthermore, patent WO 91/13545 discloses that highly effective skin-compatible liquid formulations can be prepared by dissolving said active compounds in amounts of >50% in aliphatic solvents, such as 2-(2-butoxyethoxy)ethanol or 2-(2meth-oxyethoxy)ethanol. These formulations have the disadvantage that they require the use of relatively large amounts of active compounds and, furthermore, lead to skin irritations in sensitive animal varieties. To achieve an acceptable biological effect with the use of low amounts of active compound, U.S. Pat. No. 5,466,458 proposes the use of emulsions based on said active compounds with long-chain aliphatic amines or alcohols, such as hexadecan-1-ol, 1-octadecylamine. The use of the long-chain amines has the disadvantage that, over the course of time, they degrade said active compounds. In most cases, formulations based on long-chain alcohols have insufficient long-term action. [0005] Surprisingly, these objects are achieved by the use according to the invention of the abovementioned polysiloxanes. Clear solutions or emulsions of high storage stability are formed. [0006] Furthermore, the use according to the invention of these polysiloxanes surprisingly leads to improved compatibility and an activity-enhancing synergistic effect, in particular in combination with pyrethroids and pyrethrins. [0007] Accordingly, the present invention relates to the use of polysiloxanes containing at least one quaternary ammonium group as formulation auxiliaries in formulations of pharmaceutically and veterinary active compounds. [0008] The present application further provides novel compositions, comprising [0009] a) at least one pharmaceutically or veterinary active compound and [0010] b) a polysiloxane derivative containing at least one quaternary ammonium group per molecule, [0011] if appropriate, further auxiliaries and carriers. [0012] The compositions according to the invention are, in particular, highly suitable for preparing aerosol sprays, pump sprays, spot-on formulations and pour-on formulations for use in the control of parasites on animals. [0013] To prepare the compositions according to the invention, it is possible to use, in general, all active compounds from the pharmaceutical and veterinary field. [0014] By way of example, but not by way of limitation, the active compounds which are also mentioned as suitable combination partners in this publication (see below) may be mentioned (for example chloronicotinyl compounds and pyrazoles). [0015] Particularly suitable active compounds are the pyrethins and pyrethroids with common names such as fenvalerate [.alpha.-cyano-3-phenoxybenzyl .alpha.-(p-Clphenyl)-isovalerate], flumethrin [(.alpha.-cyano-4-fluoro-3-phenoxy)benzyl 3-[2-(4-chlorophenyl)-2-chlorovinyl]-2,2-dimethylcyclopropane carboxylate] and its enantiomers and stereoisomers, cyfluthrin [(.alpha.-cyano-4-fluoro-3-phenoxy)benzyl 2,2dimethyl-3-2,2-(2,2-dichlorovinyl)cyclopropanecarboxylate, permethrin [3-phenoxybenzyl cis, trans-3-(2,2-dichlorovinyl)-2,2-dimethylcyclopropanecarboxylate], cypermethrin [.alpha.-cyano-3-phenoxybenzyl 2,2-dimethyl3-(2,2-dichlorovinyl)cyclopropanecarboxylate, deltamethrin [.alpha.-cyano-3-phenoxybenzyl cis, trans-3-(2,2-dibromovinyl)-2,2-di-methylcyclopropanecarboxylate], fluvalinate (2-cyano-3-phenoxybenzyl 2-(2-chloro-.alpha.,.alpha.,.alpha.-trifluoro-p-toluido)3-methylbutyrate, where pyrethroids having acaricidal action are preferred for preparing the novel formulations and those based on .alpha.-cyanopyrethroids, such as esters of the .alpha.-cyano-3-phenylbenzyl alcohols or 4-fluoro-.alpha.-cyano-3-phenoxybenzyl alcohols are particularly preferred. Very particular preference is given to flumethrin. [0016] The amounts of active compound can be varied within wide limits, between 0.1 and 15%. Amounts in the range of 0.1-7.5% are preferred. Particular preference for preparing the novel formulations according to the invention is given to using amounts in the range from 0.2-2.0%. Here, percentages are based on percent by weight. [0017] It is, of course, also possible to use further active compounds as combination partners in the compositions according to the invention. [0018] Combination compounds which may be mentioned as being preferred are the insecticides used in the control of ectoparasitic insects, such as nicotinyl and, in particular, chloronicotinyl insecticides, N-phenylpyrazoles, carbamates, phosphoric and phosphonic esters, growth inhibitors or mixtures of these active compounds with one another, and their mixtures with synergists. In the context of this application, synergists are understood as meaning compounds which do not on their own have the desired activity but which, as mixing partners, lead to an increase of the activity of the a.i. [0019] Chloronicotinyl insecticides which may be mentioned are compounds of the Formulae (I), (II) and (III): [0020] in which [0021] n represents 1 or 2, [0022] m represents, 0, 1 or 2, [0023] Subst. represents one of the substituents listed above, in particular halogen, very particularly chlorine, [0024] A, Z, X and E are as defined above. [0025] In particular, the following compounds may be mentioned: [0026] Particular emphasis is given to the compounds Continue reading... 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