Abstract

Purpose: To compare the pharmacokinetic profiles and to evaluate the bioequivalence of two commercial amoxicillin suspension formulations (500 mg/5 mL AMOXIL^®, reference formulation and AMOXI-PED^®, test formulation) in healthy Brazilian volunteers. Methods: Under fasting condition, 25 volunteers (13 males and 12 females) were included in this randomized, open-label, two-period crossover (1-week washout interval) bioequivalence study. Blood samples were collected at pre-dose (0 hour) and 0.5, 1, 1.33, 1.66, 2, 2.5, 3, 4, 6, 8, and 12 hours after drug ingestion. Pharmacokinetic parameters (C_max, t_max, t_1/2, AUC_0–tlast, and AUC_0–∞) were calculated from plasma concentrations for both formulations in each subject. Results: Arithmetic mean values of the pharmacokinetic parameters were: C_max = 12.004 (± 2.824) μg×mL^–1; t_max = 1.118 (± 0.396) h; t_1/2 = 1.226 (± 0.179) h; AUC_0–tlast = 29.297 (± 6.007) μg×h×mL^–1; and AUC_0–∞ = 29.299 (± 6.007) μg×h×mL^–1 for reference formulation and C_max = 11.456 (± 2.825) μg×mL^–1; t_max = 1.331 (± 0.509) h; t_1/2 = 1.141 (± 0.133) h; AUC_0–tlast = 28.672 (± 5.778) μg×h×mL^–1; and AUC_0–∞ = 28.693 (± 5.796) μg×h×mL^–1 for test formulation. The confidence intervals (90% CI) for reference and test formulations were, respectively, 90.74 – 100.46% for C_max and 93.62 – 103.61% for AUC_0–t. Conclusion: Based on the results, both formulations of amoxicillin evaluated in this study were considered bioequivalent according to FDA and ANVISA/Brazil criteria.

Author Details

Authors

• Gilson C.N. Franco¹,⁸
• Sinvaldo Baglie²
• Ana P.B. Ruenis³
• Luiz M. Franco⁴
• Karina Cogo⁵
• Yoko Oshima-Franco⁶
• Paulo Silva⁷
• Francisco C. Groppo⁸
• Pedro Luiz Rosalen⁸

Departments

• ¹ Department of General Biology, Area of Physiology and Pathophysiology,
• ² Department of Pharmaceutical Sciences, Area of Pharmacology, State University of Ponta Grossa, Ponta Grossa,
• ³ Activa-CRO do Brasil, São Paulo,
• ⁴ Faculty of Health Sciences, Methodist University of Piracicaba, Piracicaba,
• ⁵ Department of Dentistry, Implantology Area, University of Santo Amaro, São Paulo,
• ⁶ Post Graduate Course in Pharmaceutical Sciences, University of Sorocaba, Sorocaba,
• ⁷ Bioagri Laboratórios Ltda, and
• ⁸ Department of Physiological Sciences, Piracicaba Dental School, University of Campinas, Piracicaba, Brazil

Address

Prof. Pedro Luiz Rosalen
Department of Physiological Sciences
Piracicaba Dental School, University of Campinas
Av. Limeira, 901, 13414-903 Piracicaba, SP, Brazil
Email: [email protected]

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