Pour-on formulations containing polymeric material
AssigneeMerck & Co., Inc.
InventorsHoo-Kyun Choi, James B. Williams
Life of this patent
Estimating the term…
Abstract
There is disclosed a topical multiple-point-application formulation containing a solution of a polymeric material and an avermectin compound (active ingredient) which has been discovered to provide superior efficacy against ectoparasites, such as fleas and ticks and endoparasites such as nematodes and heartworms, when compared to conventional formulations. The formulation contains the avermectin active ingredient and up to 50% of the polymeric material.
Claims5
A topical formulation for direct application to the skin of an animal, effective for treatment of ecto and endoparasitic infestations for four weeks, consisting of from about 0.01 to about 20% w/v of polyvinyl pyrrolidone, having a molecular weight of about 20,000 to about 65,000, from about 1 to from about 95% v/v of ethanol, 100% v/v obtained with addition of water, and from about 0.05 to from about 10% w/v of an avermectin compound having the formula:
- ##STR4## where the broken line indicates a single or a double bond at the 22,23-positions;
- R.sub.1 is hydrogen or hydroxy, provided that R.sub.1 is present only when the broken line indicates a single bond;
- R.sub.2 is alkyl of from 1 to 6 carbon atoms or alkenyl of from 3 to 6 carbon atoms or cycloalkyl of from 3 to 6 carbon atoms;
- R.sub.3 is hydroxy, methoxy, or .dbd.NOR.sub.5 ;
- where R.sub.5 is hydrogen or lower alkyl;
- R.sub.7 is hydrogen, hydroxy or lower alkyl;
- and
- R.sub.4 is hydrogen, hydroxy, poly C(1-6) alkoxy, or ##STR5## where R.sub.6 is hydroxy, amino, mono- or di-C.sub.1 -C.sub.6 alkylamino or C.sub.1 -C.sub.6 alkanolylamino.
A method for the treatment of internal and external parasites of animals for four weeks, which comprises applying a formulation consisting of 20% w/v of polyvinyl pyrrolidone, from about 1 to from about 95% v/v of ethanol, 100% v/v obtained with addition of water, and from about 0.05 to from about 10% w/v of an avermectin compound having the formula:
- ##STR6## where the broken line indicates a single or a double bond at the 22.23-positions;
- R.sub.1 is hydrogen or hydroxy, provided that R.sub.1 is present only when the broken line indicates a single bond;
- R.sub.2 is alkyl of from 1 to 6 carbon atoms or alkenyl of from 3 to 6 carbon atoms or cycloalkyl of from 3 to 6 carbon atoms;
- R.sub.3 is hydroxy, methoxy, or .dbd.NOR.sub.5 ;
- where R.sub.5 is hydrogen or lower alkyl;
- R.sub.7 is hydrogen, hydroxy or lower alkyl;
- and
- R.sub.4 is hydrogen, hydroxy, poly C(1-6) alkoxy, or ##STR7## where R.sub.6 is hydroxy, amino, mono- or di-C.sub.1 -C.sub.6 alkylamino or C.sub.1 -C.sub.6 alkanolylamino, to two to six points on the skin, along the back, of the animal.
Dependencies are inferred from the claim text.