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Comparative bioavailability of Enrofloxacin in dogs when concealed in non-commercial morsels, either as tablet or as Enrofloxacin-Alginate preparation

Abstract

Lilia Gutierrrez

It has been postulated that to obtain optimal clinical efficacy with enrofloxacin, the appropriate pharmacokinetics / pharmacodynamics (PK/PD) ratios must be achieved i.e.,  that the maximum serum concentration (CMAX) reach a peak at or above 10 to 12 times the value of the minimum inhibitory concentration (MIC) (CMAX ≥ 10–12 MIC), and/or the ratio of the area under the concentration vs. time curve (AUC0–24) divided by MIC should be equivalent or higher than 125 (AUC0–24/MIC ≥ 125). Moreover, it has been postulated that if CMAX/MIC values ≥ 16 are achieved, mutant inhibitor concentration can be expected. Enrofloxacin tablets are indicated once a day and they should be administered without food. Yet, pet-owners often fail to comply with this indication and often hide the tablet in a treat or morsel i.e., within a piece of sausage (S), or covered with jelly (J) or with yogurt (Y) to avoid the drug’s unpleasant flavor. There is a lack of formal PK data published when enrofloxacin tablet is administered with a morsel. This study presents a pharmaceutical preparation (PhP) based on coating enrofloxacin with alginate derivatives in a very efficient chemical procedure (>then 98%) that eliminates completely the unpleasent flavor of this drug and allows precise and easy dosing, as it can be easily concealed in a sausage. The figure below shows the serum-pharmacokinetic profiles of the original preparation (B®) and the PhP, administered with the 3 types of morsels (S, J or Y). The highest bioavailability (Fr) was achieved by PhP + S (307%). It is concluded that B® decreases its bioavailability when administered with morsels, even up to 70%, while PhP increases Fr, particularly when administered with sausage or yogurt morsels. This maneuver will facilitate dosing by pet owners and will improving compliance with prescription.

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