Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai
Reexamination Certificate
2002-01-24
2003-12-16
Wilson, James O. (Department: 1623)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Carbohydrate doai
C514S329000, C514S355000, C536S007100, C536S017200
Reexamination Certificate
active
06664237
ABSTRACT:
Companion animals, including but not limited to dogs, cats, and horses, are an increasingly important part of today's society. They provide pleasure and companionship to human friends, which leads to what has been termed the human-animal bond. Unfortunately, a number of insect pests and parasites can infest or infect these animals. Such pests include, for example, fleas, lice, mosquitoes, mites, ticks and certain fly species. Safe, effective ways to eliminate these pests are desired, both for the animal's well-being and for the comfort of its human associate.
The most common ectoparasites of cats and dogs world-wide are the cat and dog fleas,
Ctenocephalides felis felis
and
Ctenocephalides canis
, respectively. Interestingly, the cat flea very commonly infests dogs. Fleas annoy the animal it infests and the pet's owner. Frequently, fleas cause more serious problems by inducing flea-allergy dermatitis. It has been estimated that flea-related diseases account for over 50% of the dermatological cases reported to veterinarians [D. E. Bevier-Tournay, “Flea and Flea Control”
Curr. Vet. Therapy
10: 586-592 (1989)]. In addition, the cat flea is known to transmit tapeworms in dogs and has been implicated in the transmission of cat scratch disease and murine typhus. Other pests of companion animals, such as ticks and mosquitoes, are also known to transmit disease. For example, ticks are known to transmit bacterial and viral diseases; and mosquitoes can infect dogs and cats with the filarial nematode that causes heartworm disease.
Furthermore, economic expenses involved in flea control are high. In the United States, for example, pet owners spend over $1 billion dollars for flea control products annually [R. Conniff, “When It Comes to Pesky Flea, Ignorance is Bliss,”
Smithsonian
: 26: 76-85 (1995)].
Treatments currently available achieve varying degrees of success. Most treatments involve chemicals applied to indoor and outdoor surfaces, as well as to the pet. The chemicals used include a variety of carbamates, organophosphates, pyrethrins and pyrethroids. These compounds often have toxic side effects that are a problem for both the pet and its owner. For example, concentrated forms of pyrethroids available for use on dogs are extremely toxic and lethal to cats and thus cannot and should not be used on cats. In addition, there is evidence that the use of these chemicals has led to multiple category insecticide resistance [N. K. Rust and M. W. Dryden,
Ann. Rev. Entomol
. 42: 451-473 (1997)]. Thus, there continues to be a need for relatively safe, effective agents for controlling ectoparasites on companion animals, such as cat and dog fleas.
The spinosyns (also known as A83453 factors) are agricultural insecticides that have shown activity against southern armyworm and other insects in the order Lepidoptera, and cotton aphid and other members of the order Homoptera. (See, for example, U.S. Pat. No. 5,571,901).
The spinosyns were also known to have some ectoparasiticidal activity, i.e., they had in vitro activity against mosquito larvae, black blowfly larvae and adult stable flies, which are members of the insect order Diptera, and transient systemic activity against larval blowfly and adult stable fly in guinea pigs and sheep (see U.S. Pat. No. 5,571,901, col 26-32). Although it was suggested that the spinosyns would be active against a number of ectoparasites in a number of animals by a variety of routes, there have been no subsequently reported studies to support these suggestions.
This invention came about by the discovery that spinosyns, such as spinosyn A, can provide prolonged residual control of an ectoparasite infestation on a companion animal when a single dose of a spinosyn is administered orally to the animal. Thus, the invention provides a method for prolonged control of the ectoparasite in a safer manner than that achieved with previously known treatments.
In one aspect, this invention relates to a long-acting, single-dose oral formulation for controlling an ectoparasite infestation on a companion animal, said formulation comprising an ectoparasiticidal amount of a spinosyn, or a physiologically acceptable derivative or salt thereof, and a physiologically acceptable carrier, in an oral dosage form.
In another aspect the invention relates to the use of a single, long-acting oral formulation of a spinosyn, or a physiologically acceptable derivative or salt thereof, for controlling an ectoparasite infestation on a companion animal.
It also relates to the use of a spinosyn, or a physiologically acceptable derivative or salt thereof, for the manufacture of a long-acting single-dose oral medicament for controlling an ectoparasite infestation on a companion animal.
This invention also relates to a method of controlling an ectoparasite infestation on a companion animal for a prolonged time, comprising orally administering a single dose of an effective amount of a spinosyn, or a physiologically acceptable derivative or salt thereof, to the animal. An especially useful method of this invention is a method for controlling cat or dog fleas on a companion animal for a prolonged time comprising orally administering a single dose of an effective amount of a spinosyn, or a physiologically acceptable derivative or salt thereof, to the animal.
The invention further relates to an article of manufacture, comprising packaging material and a formulation for controlling an ectoparasite infestation on a companion animal contained within said packaging material, wherein said formulation comprises
an oral long-acting unit dose of an ectoparasiticidal amount of a spinosyn, or a physiologically acceptable derivative or salt thereof, and
a physiologically acceptable carrier; and
wherein said packaging material comprises a label or package insert with instructions for orally administering the dose to the animal.
This article of manufacture or kit is particularly appropriate when the companion animal is a dog or a cat. When the animal is a dog, the formulation contained in the packaging material will generally be in tablet form, and the label or package insert will indicate the number of tablets to be given by mouth to the dog and the timing of such administration. The timing of doses will generally be every 30 days. When the animal is a cat, the formulation contained in the packaging material will generally be a liquid formulation and the label or package insert will indicate the unit dose to be given by mouth to the cat. The timing of doses will generally be every 30 days. The contents of each kit would typically be sufficient to control the ectoparasite infestation for a period of several months.
Spinosyns are naturally derived fermentation products. They are macrolides produced by cultivation of
Saccharopolyspora spinosa
. The fermentation produces many factors, including spinosyn A and spinosyn D (also called A83543A and A8354D). Spinosyn A and spinosyn D are the two spinosyns that are most active as insecticides. A product comprised mainly of these two spinosyns is available commercially under the trade name “spinosad”. The major spinosyn factor, spinosyn A, is known to have an excellent human and animal safety and toxicological profile.
Each spinosyn has a 12-membered macrocyclic ring that is part of an unusual tetracyclic ring system to which two different sugars are attached, the amino-sugar forosamine and the neutral sugar 2N,3N,4N-(tri-O-methyl)rhamnose. This unique structure sets the spinosyns apart from other macrocyclic compounds.
Spinosyn A was the first spinosyn isolated and identified from the fermentation broth of
Saccharopolyspora spinosa
. Subsequent examination of the fermentation broth revealed that
S. spinosa
produced a number of spinosyns that have been called spinosyns A to J (A83543A to J). The primary components are spinosyns A and D. Additional spinosyns, lettered from K to W, have been identified from mutant strains of
S. spinosa
. The various spinosyns are characterized by differences in the substitution patterns on the
Demeter John C.
Eli Lilly and Company
McIntosh Traviss
Wilson James O.
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