Purpose:
To examine the
pharmacokinetics of a formulated aceclofenac sustained
release tablet formulation and determine if it is
bioequivalent to a commercial brand of aceclofenac
immediate release tablet (Zerodol® 100 mg).
Methods:
Each of two groups of
twelve fasting volunteers received either the reference
standard (Zerodol 100 mg tablets) or the test
formulation (200 mg aceclofenac) orally once, using a
cross-over design with a one week wash-out period. Their
blood samples were obtained at regular time intervals
over 24 h and analyzed by high performance liquid
chromatography (HPLC). Using the non-compartmental
approach, plasma levels of aceclofenac were employed to
compute their individual disposition kinetics, including
peak plasma concentration (Cmax), peak time (Tmax),
area under the plasma level-time curve (AUC 0-t),
elimination rate constant (Kel)and
elimination half life ( t 1/2).
Results:
The Cmax values of 11043 ± 3073 ng/ml and
12301 ± 3000 ng /ml were attained in 2.58 ± 1.22 h and
1.29 ± 0.75 h for the test and reference products,
respectively, while AUCO-∞
was 45996 ± 10427 and 50253 ± 8283 ng.h/ml,
respectively. At 90% confidence interval, the C
max,, AUC 0-t and AUC0-∞
values of
the test preparation were 96.4 - 101.3 , 100.2 -101.9
and 98.5 - 99.8 %, respectively, of the values for the
reference. The t1/2 values were found to be
4.50 ± 1.25 and 2.20 ± 2.59 h for the reference and test
products.
Conclusion:
On the basis of the
pharmacokinetic data, it can be said that the test
aceclofenac sustained release formulation and the
reference product were bioequivalent in some respects.
However, the test formulation exhibited a longer
elimination half-life (t1/2), thus
demonstrating sustained release properties, unlike the
reference.
Keywords:
Pharmacokinetics; Bioequivalence; Sustained release
aceclofenac formulation.
