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Characterization of taste-masking dry emulsion of azithromycin by in vitro and in vivo evaluation
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Ri HUANG1, 2, Tao WANG2, Xi YANG2, Dong-qin QUAN2, *, Yang WANG1, *
Acta Pharmaceutica Sinica | 2017, 52(5) : 795 - 801
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Acta Pharmaceutica Sinica | 2017, 52(5): 795-801
Characterization of taste-masking dry emulsion of azithromycin by in vitro and in vivo evaluation
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Ri HUANG1, 2, Tao WANG2, Xi YANG2, Dong-qin QUAN2, *, Yang WANG1, *
Affiliations
  • 1. Experimental Teaching Administration Department, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China
  • 2. Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences, Beijing 100850, China
Published: 2017-05-12 doi: 10.16438/j.0513-4870.2016-1214
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To develop a taste-masking oral preparation of azithromycin for pediatrics, the reversed lipid nano-micelle techniques were used to mask the bitterness of azithromycin. Dry emulsion (DE) for taste-masking was prepared by solidifying the reversed-micelle oil solution containing azithromycin. Colloidal silicon dioxide was used as absorbent and solid carrier. Solidification was confirmed through dying test and observed by scanning electron microscope (SEM). The DE formulation was characterized by X-ray powder diffraction and SEM in order to investigate the crystal state of drug. Reconstitution emulsion droplet size and morphology were also determined using Nano ZS90 Zetasizer and transmission electron microscopy (TEM). The taste testing was performed in two different ways, namely, human taste panel test and the measurement of the amount of drug released in simulated oral cavity condition. The intestinal mucosal irritation test of DE formulation was also investigated in rats in comparison with commercial product (Zithromax). The optimal taste-masking formulation of azithromycin can be re-dispersed immediately with mean diameter of 530.1 nm after agitation in water. The results of taste testing showed that the bitterness of azithromycin was successfully masked by DE formulation similar with Zithromax at the same dose, moreover reduced intestinal irritation compared to Zithromax. These results indicate that the DE formulation for taste-masking of azithromycin is promising and valuable in the future development of azithromycin for pediatrics.

azithromycin  /  taste masking  /  dry emulsion  /  silicon dioxide  /  intestinal mucosal injury
Ri HUANG, Tao WANG, Xi YANG, Dong-qin QUAN, Yang WANG. Characterization of taste-masking dry emulsion of azithromycin by in vitro and in vivo evaluation[J]. Acta Pharmaceutica Sinica, 2017 , 52 (5) : 795 -801 . DOI: 10.16438/j.0513-4870.2016-1214
Year 2017 volume 52 Issue 5
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doi: 10.16438/j.0513-4870.2016-1214
  • Receive Date:2016-12-23
  • Online Date:2026-01-14
  • Published:2017-05-12
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  • Received:2016-12-23
  • Revised:2017-02-07
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    1. Experimental Teaching Administration Department, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China
    2. Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences, Beijing 100850, China
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表12种不同金属材料的力学参数

Family
属数
Number of
genus
种数
Number of
species
占总种数比例
Percentage of
total species (%)

Genus
种数
Number of
species
占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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