Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Silicon containing doai
Reexamination Certificate
1993-07-06
2003-02-04
Travers, Russell (Department: 1617)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Silicon containing doai
C514S539000
Reexamination Certificate
active
06514951
ABSTRACT:
BACKGROUND OF THE INVENTION
Pour-on formulations are utilized by the animal industry as a means for administering certain anthelmintic agents and veterinary medicines to animals. In practice, the medicated formulation is applied directly to the external skin or hide of the animal. As such, some practitioners have extended the term pour-on to include formulations which may be dispersed in water and applied as aqueous dips, baths or sprays. In the present specification, however, the term “pour-on” is not intended to suggest this type of application. Rather, the formulation of this invention is a non-aqueous formulation which is applied with the assistance of a suitable device such as a measuring cup, a squirt bottle or an automatic microspray device which permits directed application of a small amount of formulation onto the skin of the animal being treated.
While a number of anthelmintic agents and veterinary medicines such as tetramisole, levamisole, trichlorphon and fenthion, have been successfully prepared as pour-on compositions, all veterinary medicines do not lend themselves to such formulation. Moreover, those medicines that have been so formulated generally have been found to be significantly less effective as pour-on formulations than they are when administered orally or parenterally.
Presently, the art appears to describe no pour-on formulations which do not wash off during rainfall or which retain efficacy on wet animals. From a practical standpoint, a product which lacks efficacy on wet skin or hide is extremely inconvenient to use due to the extra burden on the part of the farmer to keep the animals dry in order to effectively treat them with pour-on medicine.
For successful formulation as a pour-on, a drug must be active when dissolved, dispersed or emulsified in a suitable solvent which is well tolerated by the animals skin. The drug must be readily adsorbable through the animals skin and the composition as a whole should disperse or spread well over the animals body and be relatively non-viscous when so spread. It must also be recognized that each drug has its own chemical and physical properties that require special consideration and limit the types of solvents, diluents, stabilizing agents and other formulatory agents that can be employed in the formulation of that particular drug or medicine.
It is, therefore, an object of the present invention to provide a non-irritating pour-on formulation which is effective on dry or wet skin and hide for the control of insects and internal and external parasitic infections and infestations of farm and companion animals and which resists wash off during normal precipitation.
It is also an object of this invention to provide an effective non-aqueous pour-on formulation that contains, as the active ingredient, an antibiotic selected from LL-F28249&agr;, a 23-oxo or 23-imino derivative of LL-F28249&agr;-&lgr;, a milbemycin molecule or an avermectin molecule, which exhibits excellent penetration of the animals hide or skin, spreads well and rapidly over the animals body, is non-malodorous, non-irritating and relatively non-viscous toward dust, dirt and foreign matter encountered by the treated animals.
It is a further object of this invention to provide a method for treating, controlling, preventing or protecting quadruped farm and companion animals from infestation and infection by helminths, acarids and arthropod endo- and ectoparasitic insects by topically applying to said animals a pour-on formulation containing an anthelmintically, acaricidally or arthropod endo- or ectoparasiticidally effective amount of the antibiotic LL-F28249&agr;, LL-F28249&bgr; or a 23-oxo or 23-imino derivative of LL-F28249&agr;, such as 23-(O-methyloxime)-LL-F28249&agr; or 23-(O-methyloxime)-LL-F28249&bgr;.
SUMMARY OF THE INVENTION
The present invention relates to non-aqueous pour-on, water-fast compositions and the method of use thereof for treating, controlling, preventing and protecting homothermic animals, such as mammalian quadrupeds, from infestation and infection by internal and external parasites. More particularly, this invention relates to non-aqueous pour-on compositions containing as the active ingredient an anthelmintically, acaricidally or arthropod endo- or ectoparasiticidally effective amount of a compound selected from compounds designated LL-F28249&agr;-&lgr;, a 23-oxo or 23-imino derivative of LL-F28249&agr;-&lgr;, a milbemycin molecule or an avermectin molecule.
DESCRIPTION OF THE PREFERRED EMBODIMENTS
The compounds designated LL-F28249&agr;-&lgr; are (collectively) isolates from the fermentation broth of the microorganism
Streptomyces cyaneogriseus
subspecies
noncyanogenus,
deposited in the NRRL under deposit accession No. 15773. The method for preparation of the LL-F28249 compounds is disclosed in U.S. Pat. No. 5,106,994 and is incorporated herein by reference thereto.
The 23-oxo (keto) and 23-imino derivatives of LL-F28249&agr;-&lgr; compounds, useful in the pour-on formulations of this invention, are disclosed in U.S. Pat. No. 4,916,154, incorporated herein by reference thereto. Although U.S. Pat. No. 4,916,154 indicates that the 23-oxo (keto) and 23-imino derivatives of LL-F28249&agr;-&lgr; may be administered by pouring on the skin of an animal via a solution, it only suggests that the active compound may be dissolved in dimethylsulfoxide, propylene glycol or the like or in a combination of solvents. These formulations are not entirely satisfactory since the use of dimethylsulfoxide can cause instability of the 23-(oxo) or 23-imino derivatives of LL-F28249&agr;-&lgr; and/or leave a malodorous scent on the treated animal. The propylene glycol compositions tend to be sticky and collect dust and dirt and debris from the animals' surroundings.
The pour-on veterinary compositions of this invention have the following formulations:
% w/v
Compound
(A)
0.1-5.0
Active ingredient
5.0-20.0
Aromatic solvent
2.0-15.0
PPG-2 Myristyl ether
propionate (spreader)
0-15.0
Polybutene
(number average molecular
weight range from 320 to 3000)
QS to 100%
Mineral or vegetable oil; or
(B)
0.1-5.0
Active ingredient
0-15.0
Polysorbate 80
QS to 100%
Butoxyethoxyethanol
These compositions may be prepared by dissolving, dispersing or emulsifying about 0.1% to 5.0% w/v of the active ingredient, i.e. a compound selected from the group consisting of LL-F28249&agr;-&lgr;, a 23-oxo or 23-imino derivative of said compound LL-F28249&agr;-&lgr;, a milbemycin molecule or an avermectin molecule, in a mixture consisting essentially of 5.0% to 20.0% w/v of an aromatic solvent having a Kauri-butanol value between about 90 to about 96, a mixed aniline point between about 13.4° C. to about 15.4° C. and a specific gravity @ 15.6°/15.6° C. of about 0.872 to about 0.985; about 1.0% to about 15.0% w/v of PPG-2 myristyl ether propionate; if present, about 1.0% w/v to about 15.0% w/v of a polybutene having a number average molecular weight range of 320 to 3000; and the remainder of the mixture a pharmacologically acceptable oil such as mineral or vegetable oil. Pour-on formulations prepared as described above with LL-F28249&agr;, LL-F28249&bgr;, 23-(O-methyloxime)-LL-F28249&agr; or 23-(O-methyloxime)-LL-F28249&bgr;, are especially effective for controlling endo- and ectoparasites on mammalian quadrupeds.
The pour-on compositions of the invention may also be prepared by dissolving, dispersing or emulsifying about 0.1% to 5.0% w/v of a compound selected from the group consisting of LL-F28249&agr;-&lgr;, a 23-oxo or 23-imino derivative of said antibiotic LL-F28249&agr;-&lgr;, a milbemycin molecule and an avermectin molecule, in butoxyethoxyethanol. Pour-on formulations prepared as described above with LL-F28249&agr;, LL-F28249&bgr;, 23-(O-methyloxime)-LL-F28249&agr; or 23-(O-methyloxime)-LL-F28249&bgr;, are especially effective for controlling endo- and ecto-parasites on mammalian quadrupeds. The admixture of up to about 15.0% w/v of polysorbate 80 with the above composition is optional.
Excipients such as dyes, antimicr
Quinlan James
Wood Irwin B.
American Cyanamid Company
Mazzarese Joseph M.
Travers Russell
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