生物等效性和生物利用度杂志

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Pharmacokinetic and Bioequivalence Studies of Oral Cefuroxime Axetil 250 mg Tablets in Healthy Human Subjects

Iyad Naeem Muhammad, Muhammad Harris Shoaib, Rabia Ismail Yousuf and Rabia Ismail Yousuf

The objective of this study was to determine the bioequivalence of two Cefuroxime oral 250 mg tablet formulation. One was the innovators brand (Zinnat®), was taken as reference brand (REF) and the other was a newly developed, optimized and cost effective formulation (TEST). A single dose, open, random sequence, cross over, two treatment study with a one week washout period in between was carried out in 12 healthy male Pakistani young volunteers. Reference and Test tablets were administered to these volunteers with 150 mL of water after an overnight fast. Blood samples were drawn 15 min prior to the administration of dose and at 0.5, 1, 1.5, 2, 3, 4, 5, 6, 7 and 8 hours post dose. The cefuroxime concentrations in the plasma were determined by a modified, simple HPLC method in which the mobile phase was 10 mM solution of ammonium acetate and acetonitrile, pH was adjusted to 5 ± 0.2 with glacial acetic acid. The wavelength of detection was 254 nm having a flow rate of 1ml/min and the retention time of 5.8 min. The method was validated as per the ICH requirements. Both compartmental and non-compartmental methods were used to determine the various PK parameters such as Cmax. Tmax, AUC0-t, AUC0-∞ , AUMC, MRT, t1/2, Kel, Vd and Cl using Kinetica® ver 4.4.1 The bioequivalence between the REF and TEST cefuroxime axetil 250mg formulations was established as the Latin square design of ANOVA does not show any significant difference with a p≥0.05 for period and the 90% confidence interval lies within the acceptable range (80-125%) for the log transformed data of Cmax, Tmax, AUC0-t, AUC0-∞, t1/2, AUMC, MRT, Vd and Cl, showing a comparable plasma profiles generated by both the formulations. It is, thus concluded that both the formulations were bioequivalent.