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Feb 11, 2025Keywords:
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Main Article Content
Evaluation of azithromycin–resin suspension designed for taste-masking and sustained-release
Abstract
Purpose: To prepare azithromycin (AZI) sustained-release suspension containing AZI-coated
microcapsules (AZI-CM) impregnated with AZI-drug resin complex (AZI-DRC), in order to mask the
bitter taste of AZI and improve the oral compliance of patients.
Methods: The AZI-DRC was prepared using the bath method, with cation exchanger resin
Amberlite®IRP64 as a drug carrier, and it was characterized using scanning electron microscopy
(SEM), x-ray diffraction (XRD) and Fourier transform infrared (FTIR) spectroscopy. Pretreated AZI-DRC
was coated using emulsification-solvent evaporation method to achieve sustained-release effect. The
effect of coating on in vitro drug release of the microcapsules was investigated to obtain the optimal
AZI-CM through single-factor investigation. The optimized AZI-CM formulation was further dispersed in
the optimized suspension matrix to obtain AZI sustained-release suspension. Then, the
pharmacokinetics of AZI sustained release from the suspension was studied in rats and compared with
commercially available AZI dry suspension.
Results: Taste evaluation by volunteers showed that AZI-DRC had a good taste-masking effect on AZI.
Results from SEM, XRD and FTIR demonstrated that AZI was present in AZI-DRC solely in amorphous
form. Three batches of AZI-CM prepared after optimization produced a significant sustained release
effect (p < 0.05). The AZI sustained-release suspension did not change significantly after 10 days and 3
months, indicating good stability (F > 0.9; drug release: f2 > 50; drug leakage < 0.5 %). In vivo results
showed that AZI sustained-release suspension had a lower Cmax a higher Tmax and a better
bioequivalence than AZI dry suspension available in the market.
Conclusion: These findings depict a newly developed AZI sustained-release suspension with improved
bioavailability, sustained-release effect, masked bitterness, and good therapeutic effect.
