title: Comparative bioavailability and pharmacokinetic study of Cefadroxil capsules in male healthy volunteers of Pakistan.
abstract: The current study was aimed to judge bioequivalence between two formulations of cefadroxil capsules as guided by FDA guidelines. Another objective was to conduct pharmacokinetic evaluation in Pakistani population. A single-dose, randomized, cross-over pharmacokinetic study was conducted during the month of May'2013 to August'2013. Washout period was one week. Fourteen healthy male adult volunteers were enrolled in the study, however twelve completed the study. Cefadroxil plasma concentration was analyzed by using validated HPLC method. Protein precipitation was achieved by the addition of 6% tri chloro acetic acid in 1:1 ratio and detection was done at 260 nm. Retention time was 7.792 min and correlation coefficient (R2) was 0.9953 showing linearity of the method. Blood sampling was carried out at different time intervals after administration of either test (TEST 500 mg) or reference (REF® 500 mg) formulation. Pharmacokinetic parameters (AUC0→ ∞, AUC0→ t, Cmax, Tmax, t1/2 and kel) were calculated using Kinetica® PK/PD software. The geometric mean ratios and 90% confidence interval (CI) of these pharmacokinetic parameters for cefadroxil (test and reference) formulations were 0.986 (90.83-106.98%) for AUC0→ t; 0.967 (89.13-104.92%) for AUC0→ ∞ and 0.999 (91.06-109.69%) for Cmax. The differences between Tmax of both formulations were not found to be statistically significant (p-value was more than 0.05). The 90% CI of the test/reference AUC and Cmax ratio of cefadroxil were within the FDA recommended range for bioequivalence. Maximum plasma concentration Cmax was 12.5 μg/ml for test and 12.47 μg/ml for reference formulations. Average time to reach Cmax for test and reference formulation was 1.54 and 1.5 hrs. The two formulations of cefadroxil studied during the above study were verified bioequivalent. Maximum plasma concentration of cefadroxil was lower than those mentioned in some previous studies, while Tmax and half-life were near to values reported in literature.
authors.forename: Najia
authors.initials: N
authors.lastname: Rahim
authors.affiliation: Faculty of Pharmacy, Hamdard University, Karachi, Pakistan.
authors.forename: Syed Baqir Shyum
authors.initials: SB
authors.lastname: Naqvi
authors.affiliation: Institute of Pharmaceutical and Environmental Research, Dow University of Health Sciences, Karachi, Pakistan.
authors.forename: Mehtab
authors.initials: M
authors.lastname: Alam
authors.affiliation: Department of Research, Dow University of Health Sciences, Karachi, Pakistan.
authors.forename: Abdur
authors.initials: A
authors.lastname: Rasheed
authors.affiliation: Institute of Pharmaceutical and Environmental Research, Dow University of Health Sciences, Karachi, Pakistan.
authors.forename: Urooj Abdul
authors.initials: UA
authors.lastname: Khalique
mesh_terms: D000284:Administration, Oral; D000293:Adolescent; D000328:Adult; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D019540:Area Under Curve; D001682:Biological Availability; D002214:Capsules; D002434:Cefadroxil / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D002851:Chromatography, High Pressure Liquid; D018592:Cross-Over Studies; D006207:Half-Life; D064368:Healthy Volunteers; D006801:Humans; D016014:Linear Models; D008297:Male; D008657:Metabolic Clearance Rate; D010154:Pakistan; D055815:Young Adult
chemical_list: D000900:Anti-Bacterial Agents; D002214:Capsules; D002434:Cefadroxil