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VETERINARY COMPOSITION FOR RUMIANTS
ES2863583
The present invention refers to a composition that comprises a combination of eprinomectin with other active principles, such as meloxicam and danofloxacin, which allow a synergistic action of said principles, increasing the therapeutic action. This composition has a synergistic antiparasitic and anti-inflammatory or antibiotic effect useful in the treatment of ruminants. Macrocyclic lactones are usually secreted into milk during lactation, causing very long suppression times in dairy cattle. To solve this problem, several macrocyclic lactones have been developed, like the eprinomectin, as this molecule’s presence in the milk is nearly zero, causing no suppression time. Furthermore, ABC transporters participate in many cellular functions, as they actively export substances outside the cell. These transporters are important as they have a role in the cellular resistance functions against several drugs, affecting the absorption, distribution, metabolism, and excretion of these molecules. The innovation presented here provides a synergistic drug combination consisting on eprinomectin and either meloxicam or danofloxacin that, when applied together, increase and optimize the therapeutic action of the drugs. This combination has several advantages such as; it potentially generates a longer time of action of the analgesic action of the anti-inflammatory, it is the only formulation of two compounds with anti-inflammatory and endectocide action, the plasmatic levels of anti-inflammatory drug are higher at the same dosage, which improves the therapeutic effect, also allowing for lower doses of antibiotic. This technology has been tested in sheep with successful results.
The main advantages of this combination of drugs are: - When co-administered it can potentially generate a longer time of action of the analgesic action of the anti-inflammatory. - It is the only formulation of two compounds with anti-inflammatory and endectocide action. - Using this drug combination, the plasmatic levels of anti-inflammatory drug are higher at the same dosage, which improves the therapeutic effect. - Same occurs with danofloxacin, which would allow lower doses of the antibiotic, hence reducing the risk of developing antibiotic-resistant bacteria.
Problem solved by the invention:
Macrocyclic lactones with anthelmintic activity are antiparasitic drugs with remarkable broad-spectrum activity, widely used for the treatment of parasites. However, macrocyclic lactones are poorly metabolized in vivo, being their elimination mainly through feces. In addition, macrocyclic lactones are usually secreted into milk during lactation, causing very long suppression times in dairy cattle. For example, a treatment with ivermectin causes a 20-day suppression period, which may lead to substantial economic loses to the farmers. To solve this problem, several macrocyclic lactones have been developed, like the eprinomectin, as this molecule’s presence in the milk is nearly zero, causing no suppression time. These reasons make the eprinomectin one of the few approved antiparasitic drugs extensively used in cow, sheep and goat.
On the other hand, it has been proved through previous research that these macrocyclic lactones can interact with ATP-Binding-Cassette (ABC) membrane proteins. ABC transporters participate in many cellular functions, as they actively export substances outside the cell. These transporters are important as they have a role in the cellular resistance functions against several drugs, affecting the absorption, distribution, metabolism, and excretion of these molecules.
It is usual in the veterinary practice the concomitant use of different drugs, which can affect the pharmacokinetics and pharmacodynamics, as well as the elimination of the compounds due to their interactions between them and the ABC transporters, among other factors. These interactions are of core importance in dairy cattle, as the expression of ABCG2 at the mammary glands is inducted during the lactation and it can cause the presence of residue of the drugs in the milk.
Technology to solve the problem:
The innovation presented here provides a synergistic drug combination that, when applied together, increase and optimize the therapeutic action of the drugs. In this case, the present invention describes a combination of drugs consisting on eprinomectin and either meloxicam or danofloxacin. These two last drugs are broadly used in veterinary applications. The use of these drugs in combination modifies their pharmacokinetic properties making the anti-inflammatory drug last longer, expanding its therapeutic duration of action.
This combination has been tested in ruminants, specifically in sheep cattle. Also, the proportions of these drugs have been calculated and tested in vivo for their optimal therapeutic response.