XÂY DỰNG CÔNG THỨC BÀO CHẾ THUỐC ĐẠN AZITHROMYCIN 100 MG

Abstract

Background: Azithromycin (AZI) is an antibiotic with strong antibacterial activity against bacteria causing diseases in the respiratory tract. However, its solubility in water is poor, so the bioavailability is low. Furthermore, its taste is extremely bitter, making it unsuitable for oral dosage forms, especially for children. A suppository is a drug form that helps substances increase the absorption into the circulation through the rectal venous system and helps to overcome active ingredients' bitter tastes appearing when administered orally. Objectives: research on a process to quantify azithromycin by the high-performance liquid chromatography method. Development of the formulation of the suppository containing azithromycin 100 mg with the support of software for designing and optimizing. Materials and research method: azithromycin dihydrate, excipients, and experimental research on designed formulations. Results: a procedure for quantifying azithromycin by the high-performance liquid chromatography method has been established. The formulation of the suppository containing azithromycin 100 mg consisted of azithromycin dihydrate (104.81 mg), PEG 4000 (740.54 mg), PEG 400 (587.13 mg), glycerin (639.37 mg), beeswax (106.15 mg), and tween 80 (22 mg). Conclusion: the suppository containing azithromycin 100 mg had the base of a combination of PEGs, glycerin, and lipophilic excipients, which produces an emulsion-like structure. The finished product had no phase separation and had a melting point of about 48 oC. Also, the percentage of its in vitro solubility was 49.5 % at 30 minutes.