期刊
INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 497, 期 1-2, 页码 136-149出版社
ELSEVIER
DOI: 10.1016/j.ijpharm.2015.11.039
关键词
Multiparticulate dosage forms; Taste masking; Triglyceride; Polymorph; Hot-melt coating; Immediate release; Stability
资金
- Austrian COMET Program by the Austrian Federal Ministry of Transport, Innovation and Technology (BMVIT)
- Austrian Federal Ministry of Economy, Family and Youth (BMWFJ)
- State of Styria (Styrian Funding Agency SFG)
Multiparticulate dosage forms are a recent strategy to meet the special needs of children, elderly people and patients suffering from dysphagia. Our study presents a novel and cost-efficient approach for the manufacturing of a taste-masked multiparticulate system with a stable immediate release profile by applying lipid-based excipients in a solvent-free hot melt coating process. The thermosensitive N-acetylcysteine (N-ac) was used as model drug and hot-melt coated with a mixture of tripalmitin and polysorbate 65. A predictive in vitro method for the evaluation of the taste masking efficiency was developed based on the deprotonation of the carboxyl group of N-ac and the decline of pH, responsible for the unpleasant sour taste of the compound. The method was confirmed using in vivo studies. Differential scanning calorimetry and X-ray scattering experiments revealed polymorphic transformation and its dependency on transformation time, temperature and emulsifier concentration. During the process, the coating was transformed almost completely into the stable b-polymorph, leading to an unaltered dissolution profile during storage. A statistical design was conducted that revealed the critical process parameters affecting the taste masking efficiency and drug release. This study shows the successful application of solvent-free hot-melt coating in the development of a taste-masked and stable formulation. (C) 2015 Elsevier B.V. All rights reserved.
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