The bioequivalence determination of two different formulations of enrofloxacin in heifers following intramuscular administration

Bu çalışmanın amacı, enrofloksasin içeren ve ülkemizde %10’luk enjektabl şeklinde satışa sunulan ürünlerden ikisinin sığırlarda tek doz (2.5 mg/kg.) olarak kas içi uygulama sonrası biyoeşdeğerliğini (BE) değerlendirmektir. Çalışma 6 adet sağlıklı (12-18 aylık 340-400 kg CA) İsviçre esmeri düvelerde tek doz çapraz dizayn esasına göre gerçekleştirildi. İlaç uygulaması öncesinde 0. dakika ve sonrasında 10, 20, 30, 45, 60 ve 90. dakikalar ile 2, 3, 4, 6, 8, 12 ve 24. saatlerde kan örnekleri toplandı. Plazma enrofloksasin düzeyleri yüksek performanslı likit kromatoğrafisinde (HPLC) ölçüldü. Her hayvan için ayrı ayrı çizilen konsantrasyon-zaman grafikleri iki kompartmanlı dışa açık modele uygunluk gösterdi ve tüm farmakokinetik parametreler bu esasa göre hesaplandı. BE’lik değerlendirmesinde temel alınacak parametrelerden sadece EAA0-24 ve EAAtop değerlerinin birbirlerinden istatistiksel olarak farklı (P

Anahtar Kelimeler:

kas içi enjeksiyon, farmakokinetik, farmakodinamik, hayvan sağlığı, farmasötik, ilaç metabolizması, enrofloksasin, düve

Enrofloksasin içeren iki müstahzarın düvelerde kas içi yolla uygulama sonrası biyoeşdeğerliğinin belirlenmesi

The aim of this study was to evaluate the bioequivalence (BE) of two medicinal products of enrofloxacin, which have been also marketed as 10% injectable solution in Turkey, after the intramuscular injection (IM) at a single dose of 2.5 mg/kg of BW in the heifers. The present study was performed on healthy 6 Swiss-Brown (12-18 months and 340-400 kg BW) heifers. This study was carried out on the based a single dose cross-over design. Blood samples were taken into sterilized tubes just before, and $10^{th}$, $20^{th}$, $30^{th}$, $45^{th}$, $60^{th}$ and $90^{th}$ min. and $2^{th}$, $3^{th}$, $4^{th}$, $6^{th}$, $8^{th}$, $12^{th}$ and $24^{th}$ hours following injections. The plasma concentrations of enrofloxacin (ENR) were measured by high performance liquid chromatography (HPLC) following the extraction process. The plasma concentration-time curves for each animals showed that both products distributed according two-compartment open model. The basic pharmacokinetic parameters at this study were only the AUC0-24 and AUCtotal were statistically significant (P<0.05) before logarithmic (log) transformation. Log transformed the AUC0-24, AUCtotal and Cmax parameters and observed tmax were used in BE evaluation. Minimum, maximum and mean AUC0-24 AUCtotal and Cmax for A and B products were found in the acceptable ranges (70-143%). For the tmax value log transformation has not been done and that were determined within the limits 80-125%. As a result; it is concluded that both products could be used instead of each other as an “inter-changeable drugs”.

Keywords:

intramuscular injection, pharmacokinetics, pharmacodynamics, animal health, drug formulations, drug metabolism, enrofloxacin, heifers,

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