Abstract

Objective: To assess the pharmacokinetics of clarithromycin (CLR) and its effects on oral and nasal microbiota in healthy volunteers in an open, randomized, two-period crossover design. Methods: A single 500 mg oral dose of CLR (Group 1: Merck; Group 2: Klaricid) was administered observing a 1-week interval between doses. Blood samples were collected from pre-dose to 24 h. Plasmatic concentrations of CLR were quantified by the LC-MS-MS method. Saliva and nasal mucosa swabs were obtained previously and after 1.33, 2, 6 and 12 h of drug administration. Pharmacokinetics and PK/PD (t > MIC, %t > MIC and AUC_0-24/MIC ratio) parameters were estimated. The microorganism counts were obtained on different culture media. Results: No statistically significant differences were observed between the two formulations (p > 0.05) regarding the pharmacokinetic parameters. Total microorganisms, staphylococci and streptococci counts did not show statistical differences (p > 0.05) between the two groups during each sampling time. Considering the microorganisms of each group, no statistically significant differences were found after drug administration, but all differed from pre-dose counts (p < 0.05). The observed t > MIC ranged from 14.45 h (± 1.69) to 1.19 h (± 2.17) considering MICs of 0.25 µg/ml and 2.0 µg/ml, respectively. There was no correlation between any t > MIC, %t > MIC or AUC_0-24 and bacterial reduction (between 0- and 12-h periods). However, the profile of reduction of microorganisms in both saliva and nasal samples were compatible with high values of t > MIC verified for both clarithromycin formulations. Conclusion: Both formulations of clarithromycin had similar pharmacokinetics and efficacy.

Author Details

Authors

• A.P. Del Bortolo Ruenis¹
• G.C. Nobre Franco²
• S. Baglie⁶
• R.H. Lopes Motta³
• R.P. Simões¹
• P.L. Rosalen¹
• L.M. Franco⁴
• R.A. Moreno⁵
• E. Abib Jr.⁵
• F.C. Groppo¹

Departments

• ¹ Piracicaba Dental School, State University of Campinas (UNICAMP), Piracicaba,
• ² University of Taubaté (UNITAU), Taubaté,
• ³ Department of Physiological Sciences, São Leopoldo Dentistry School, Campinas,
• ⁴ Faculty of Health Sciences, Methodist University of Piracicaba, Piracicaba,
• ⁵ Synchrophar Assessoria e Desenvolvimento de Projetos Clínicos, Campinas, SP,
• ⁶ Department of Pharmaceutical Sciences, Ponta Grossa State University, Ponta Grossa, PR, Brazil

Address

Prof. Dr. F.C. Groppo; Piracicaba Dental School, State University of Campinas (UNICAMP), Av. Limeira 901, ZIP 13414-903, Piracicaba, SP, Brazil
Email: [email protected]

Citation