Preparation, characterization, and pharmacokinetics of tilmicosin taste-masked formulation via hot-melt extrusion technology
| Autor: | Xin Feng, Li Lv, Ruihan Deng, Jianbo Peng, Xin Deng, Qiuling Liang, Guoqing Yan, Jiakang He, Min Ji, Liqin Wu, Xuemei Wen |
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| Rok vydání: | 2020 |
| Předmět: |
Taste
Materials science Drug Compounding Electronic tongue Absorption effect 02 engineering and technology 01 natural sciences chemistry.chemical_compound Colloid and Surface Chemistry Pharmacokinetics 0103 physical sciences Tilmicosin Physical and Theoretical Chemistry Hot melt Chromatography 010304 chemical physics Hot Melt Extrusion Technology Surfaces and Interfaces General Medicine 021001 nanoscience & nanotechnology Solubility chemistry Tylosin Extrusion 0210 nano-technology Oral retinoid Biotechnology |
| Zdroj: | Colloids and Surfaces B: Biointerfaces. 196:111293 |
| ISSN: | 0927-7765 |
| Popis: | Tilmicosin (TMS) is a macrocyclic antibiotic specially used in veterinary clinics, but its extreme bitterness limits its use. This study aimed to obtain a taste-masked formulation of TMS by hot melt extrusion (HME) technology and to investigate the formulation’s characterization, stability, and effects in vitro/in vivo. Eudragit® E PO was selected as the carrier, and TMS dissolution in artificial saliva was used as a reference. The HME parameters were optimized via an orthogonal design. The optimized results were as follows: 135 ℃ extrusion temperature, 100 rpm screw speed and 30 % drug load. The masking efficiency of the formulation was evaluated by both simulated oral drug release in vitro and electronic tongue tests. The release of the taste-masked formulation in artificial saliva medium was significantly reduced within 60 s (less than 2%), while the release in 0.1 M HCl buffer was fast (more than 80 %) within 30 min. As suggested by the results of the electronic tongue, the taste-masked formulation had a better taste-masked effect than the commercial premix and the commercial enteric granules. Finally, a pharmacokinetic study was performed. Analysis of variance demonstrated that the pharmacokinetic behavior of the TMS taste-masked formulation was similar to that of the commercial premix, while the absorption effect was better than that of the commercially available enteric granules. This research indicates that the taste-masked formulation has the potential for future commercialization. |
| Databáze: | OpenAIRE |
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