CEFIXIME

DISPOSITION KINETICS AND BIOAVAILABILITY COMPARISON OF TWO FORMULATIONS OF CEFIXIME IN HEALTHY ADULT MALE SUBJECTS.

Abstract

Cefixime is a third generation and orally acting cephalosporin. It is a cell wall
synthesis inhibitor and is well stable to presence of beta lactamase enzymes. Environmental
and genetic differences play a greater role in disposition kinetics of a drug. Objectives: To
determine disposition kinetics of cefixime in local population and to evaluate the bioequivalence
of multinational and national brands of cefixime. Period: 2013-2014. Setting: Institute of
Pharmacy, Physiology and Pharmacology, University of Agriculture, Faisalabad. Methods: In
present study disposition kinetics and bioequivalence of two brands of cefixime, cefspan and
ceforal-3, were investigated in 10 adult healthy male subjects after a single oral dose of 400 mg
capsule of each with a 7 days washout period. After blood sampling, plasma concentration of
cefixime was determined by HPLC method. For computing disposition kinetic parameters, one
compartment open model was applied. Results: Mean values of disposition kinetic parameters;
t1/2β 5.01 and 4.72 hours, Vd 1.10 and 1.29 L/kg and ClB 0.16 and 0.21 L/hr/kg of cefspan and
ceforal-3, respectively, were found non significantly (P 0.05) different. Similarly mean values of
bioavailability parameters; AUC 36.58 and 32.99 μg.hr/mL, AUMC 282.95 and 264.13 μg.hr2/mL
and MRT 7.79 and 7.83 hours of cefspan and ceforal-3, respectively, remained non significantly
(P > 0.05) different. All the parameters were compared by paired t-test. Relative bioavailability
was found to be within the range 80-125% which is acceptable for bioequivalence. Conclusions:
The test formulation, ceforal-3, was found bioequivalent to the reference formulation, cefspan.