Preparation and in vitro, in vivo evaluation of clarithromycin microcapsules.

Purpose: To develop and validate a method to prepare clarithromycin (CLM) microcapsules to mask the bitter taste and provide effective treatment, and evaluate the quality of microcapsules in detail, especially the in vitro and in vivo pharmacokinetics behavior.

Methods: CLM microcapsules were prepared using ethyl cellulose as matrix material by an emulsion solvent diffusion method. The physicochemical property, in vitro release study, sensory test and stability test were evaluated. Self-made CLM dry suspension or conventional tablets containing 250 mg of CLM were orally administered with 250 mL of water. The plasma concentration was determined and the pharmacokinetic parameters were calculated by non-compartmental methods.

Results: Stable microcapsules could be prepared using ethyl cellulose as matrix material. The quality evaluation of prepared microcapsules was qualified, and the pharmacokinetic parameters of dry suspensions and conventional tablets were as following. Cmax were 1.32±0.62 and 1.40±0.58 μg.ml(-1); Tmax were 3.51±0.54 and 2.01±0.42 h; AUC were 7.65±2.54 and 7.12±2.10 μg.h.ml(-1).

Conclusion: The preparation method is easy and applicable. The self-made CLM dry suspension containing microcapsules sufficiently alleviate the bitterness of commercial CLM dry suspension, but not decrease the bioavailability and have better effect for delaying drug release in healthy volunteers.