Preparation and evaluation of azithromycin-loaded microspheres for oral administration

SU Rina; FAN Wanjun; ZHANG Ziqiang; HE Shuwang; YAO Jing

doi:10.11665/j.issn.1000-5048.20200307

Journal of China Pharmaceutical University > 2020 > 51(3): 299-304. > DOI: 10.11665/j.issn.1000-5048.20200307

SU Rina, FAN Wanjun, ZHANG Ziqiang, HE Shuwang, YAO Jing. Preparation and evaluation of azithromycin-loaded microspheres for oral administration[J]. Journal of China Pharmaceutical University, 2020, 51(3): 299-304. DOI: 10.11665/j.issn.1000-5048.20200307

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Preparation and evaluation of azithromycin-loaded microspheres for oral administration

Funds: This study was supported by the National Science and Technology Major Project (No. 2018ZX09721003-007-005)

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Received Date: February 04, 2020
Revised Date: May 17, 2020

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Abstract

To mask the bitterness of azithromycin（AZI） and improve patient compliance, an AZI-loaded microsphere (AZI-EC MS) for oral administration was prepared by O/W emulsion solvent evaporation with ethylcellulose (EC) as carrier. The release profiles and taste-masking effect of AZI-EC MS were preliminarily assessed. Its physical properties and morphology were then investigated by differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FTIR) and scanning electron microscope (SEM). The results indicated that the polymer weight of EC could influence the drug release behavior. With a drug polymer ratio of 1∶1 and mixed EC (N22/T10, 7∶3) as carrier, the cumulative release of AZI-EC MS at 0.5 h was less than 40% and reached 90% at 8 h; the drug loading efficiency of microspheres was (48.95 ± 0.86)% with smooth spherical morphology. The AZI bitterness threshold is 9.93 μg/mL with a strong bitter taste, which indicated a better taste masking effect. Therefore, AZI-EC MS prepared in this study can mask AZI bitterness and improve patient compliance, setting the stage for the research of new AZI preparations.
- azithromycin,
- microspheres,
- preparation,
- bitter taste threshold,
- ethylcellulose

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[1]	. Profiles Drug Subst Excip Relat Methodol， 2014， 39：1-40.
[2]	Hansen MP， Scott AM， McCullough A， et al. Adverse events in people taking macrolide antibiotics versus placebo for any indication［J］. Cochrane Database Syst Rev， 2019， 1：CD011825.
[3]	Walsh J， Cram A， Woertz K， et al. Playing hide and seek with poorly tasting paediatric medicines：do not forget the excipients［J］. Adv Drug Deliv Rev， 2014， 73：14-33.
[4]	Lopez FL， Ernest TB， Tuleu C， et al. Formulation approaches to pediatric oral drug delivery：benefits and limitations of current platforms［J］. Expert Opin Drug Deliv， 2015， 12（11）：1727-1740.
[5]	Ivanovska V， Rademaker CM， van Dijk L， et al. Pediatric drug formulations：a review of challenges and progress［J］. Pediatrics， 2014， 134（2）：361-372.
[6]	Mistry P， Batchelor H. Evidence of acceptability of oral paediatric medicines：a review［J］. J Pharm Pharmacol， 2017， 69（4）：361-376.
[7]	Sun JD，Zhang ZQ，He SW，et al.Progress on novel pediatric oral solid dosage forms［J］.J China Pharm Univ（中国药科大学学报），2019，50（6）：631-640.
[8]	Lopez FL， Mistry P， Batchelor HK， et al. Acceptability of placebo multiparticulate formulations in children and adults［J］. Sci Rep， 2018， 8（1）：9210.
[9]	Gandhi R， Kaul CL， Panchagnula R. Pharmacokinetic evaluation of an azithromycin controlled release dosage form in healthy human volunteers：a single dose study［J］. Int J Pharm， 2004， 270（1/2）：1-8.
[10]	Curatolo W. Interdisciplinary science and the design of a single-dose antibiotic therapy［J］. Pharm Res， 2011， 28（9）：2059-2071.
[11]	Kharb V， Saharan VA， Dev K， et al. Formulation， evaluation and 3（2） full factorial design-based optimization of ondansetron hydrochloride incorporated taste masked microspheres［J］. Pharm Dev Technol， 2014， 19（7）：839-852.
[12]	Pein M， Preis M， Eckert C， et al. Taste-masking assessment of solid oral dosage forms：a critical review［J］. Int J Pharm， 2014， 465（1/2）：239-254.

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Preparation and evaluation of azithromycin-loaded microspheres for oral administration

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