Abstract
The purpose of this study was to assess bioequivalence of two marketed formulations of celecoxib capsules in healthy human male volunteers. The study was conducted according to a single dose, randomized sequence, open label, two-period and crossover design. Both test and reference formulations comprised labeled dose of 200 mg celecoxib and were administered to each subject after an overnight fasting on two treatment days separated by one week of washout period. After drug administration, blood samples were collected at predetermined time points for a period of 48 h. Plasma separated from blood was analyzed for celecoxib concentrations using validated reverse phase-high performance liquid chromatographic (RP-HPLC) method. Various pharmacokinetic parameters including Cmax, Tmax, AUC0-t, AUC0-∞, T1/2 and Kel were determined from the plasma concentration for both formulations. Cmax, AUC0-t and AUC0-∞, were evaluated for bioequivalence after log-transformation of data. The 90% confidence intervals for the ratio of Cmax (93.26 to 100.70%), AUC0-t (87.00 to 117.50%) and AUC0-∞ (86.49 to 118.56%), values for the test and reference products were within the acceptance range of 80 to 125%, proposed by Food and Drug Administration (FDA) and European Medicines Evaluation Agency (EMEA). Based on these statistical inferences, it was concluded that two formulations of celecoxib are bioequivalent in their rate and extent of absorption. Key words: Celecoxib, pharmacokinetics, bioequivalence, healthy human male volunteers.
Highlights
Celecoxib (CEL) belongs to the group of non-steroidal anti-inflammatory drug (NSAID) approved for the treatment of rheumatoid arthritis and osteoarthritis that selectively inhibits cyclooxygenase-2 (COX-2) (Dutta et al, 2009)
The 90% confidence intervals for the ratio of Cmax (93.26 to 100.70%), AUC0-t (87.00 to 117.50%) and AUC0-∞ (86.49 to 118.56%), values for the test and reference products were within the acceptance range of 80 to 125%, proposed by Food and Drug Administration (FDA) and European Medicines Evaluation Agency (EMEA)
Metabolism of CEL takes place in liver by the enzymes cytochrome P450 2C9 (Cyp 2C9) (Sandberg et al, 2002; Sweetman et al, 2007), a cytochrome P450 isoform that is known to exist as several genetic variants (Stormer et al, 2003)
Summary
Celecoxib (CEL) belongs to the group of non-steroidal anti-inflammatory drug (NSAID) approved for the treatment of rheumatoid arthritis and osteoarthritis that selectively inhibits cyclooxygenase-2 (COX-2) (Dutta et al, 2009). Drug dissolution in gastrointestinal tract is the first step in intestinal absorption process after an orally administered dosage form (Shono et al, 2009). It is used in the treatment of orthopedics, familial adenomatous polyps (Devis et al, 2001) and in dental. The study employed the subjects to receive single oral dose of CEL 200 mg on an empty stomach with about 250 ml of water. The subjects were instructed to fast over night prior to treatment Both brands were administered randomly to two groups formulated for the study. The reverse phase system was consisted of base deactivated silica (BDS) Hypersil C8 column (150 × 4.6 mm I.D. × 5 μ particle size)
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