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Synthesis of a Borylated Ibuprofen Derivative Through Suzuki Cross-Coupling and Alkene Boracarboxylation Reactions
Published on: November 30, 2022
Optimization of taste-masking on ibuprofen microspheres with selected structure features
Wei Qin1,2, Yuanzhi He1,2, Zhen Guo2
1Ministry of Education, Jiangxi University of Traditional Chinese Medicine, Nanchang 330004, China.
Spray congealing processes significantly impact ibuprofen lipid microsphere structure, influencing drug release and taste-masking effectiveness. Citric acid cooling yielded more spherical microspheres with controlled release.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
- Drug Delivery
Background:
- Microspheres are key for taste-masking active pharmaceutical ingredients.
- Controlling microsphere structure is crucial for optimizing drug release and efficacy.
Purpose of the Study:
- To investigate how different spray congealing processes affect ibuprofen lipid microsphere architecture.
- To establish the relationship between microsphere structure and taste-masking performance.
Main Methods:
- Preparation of ibuprofen lipid microspheres using octadecanol and glycerin monostearate.
- Employing three spray congealing methods: air-cooling, water-cooling, and citric acid solution-cooling.
- Quantitative structural analysis using synchrotron radiation X-ray micro-computed tomography (SR-µCT).
Main Results:
- Spray congealing processes significantly influenced microsphere microstructure and morphology.
- Citric acid solution-cooling resulted in higher sphericity and more regular microsphere morphology.
- Quantitative structure parameters (porosity, sphericity, radius ratio) correlated strongly with drug release profiles.
Conclusions:
- Microsphere exterior morphology and internal structure are critical determinants of drug release behavior.
- The choice of congealing medium directly impacts microsphere architecture and subsequent drug release.
- Optimizing spray congealing processes can enhance taste-masking and control drug release of ibuprofen formulations.
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