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.

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Materials

Azithromycin (AZI) was product of Jiuzhou Kangda Biology Co. Ltd, China. Amberlite®IRP64, a cation exchanger resin, was purchased from Rohm & Hass, USA. Eudragit®RS100 was supplied by Shanghai Changwei Pharmaceutical Accessories Technology Co. Ltd, China. Span 80, PEG 400 and PEG 4000 were sourced from Sinopharm Chemical Reagent Group, China, while Roxithromycin (ROX) was purchased from Central Inspection Institute, China.

Following excipients are mentioned in the study besides other: Eudragit® RL100

Tianxiang Chen, Quanzhu Yang, Yongjian Yang, Yingshu Feng, Caleb Kesse Firempong, Xin Zhang, Haibing He, Jingwei Jin, Hongfei Liu, Evaluation of azithromycin–resin suspension designed for taste-masking and sustained-release, Tropical Journal of Pharmaceutical Research November 2024; 23 (11): 1807-1818 ISSN: 1596-5996 (print); 1596-9827 (electronic)

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