期刊
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
卷 94, 期 -, 页码 160-169出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ejpb.2015.04.035
关键词
L-Leucine; Polyvinylpyrrolidone; Surface mapping; Inter-particle cohesion; Spray drying
资金
- Monash Institute of Graduate Research (MIGR)
- Monash International Postgraduate Research Scholarship (MIPRS)
The amino acid L-leucine has been demonstrated to act as a lubricant and improve the dispersibility of otherwise cohesive fine particles. It was hypothesized that optimum surface L-leucine concentration is necessary to achieve optimal surface and bulk powder properties. Polyvinylpyrrolidone was spray dried with different concentration of L-Ieucine and the change in surface composition of the formulations was determined using X-ray photoelectron spectroscopy (XPS) and time of flight-secondary ion mass spectrometry (ToF-SIMS). Th e. formulations were also subjected to powder X-ray diffraction analysis in order to understand the relationship between surface concentration and solid-state properties of L-leucine. In addition, the morphology, surface energy and bulk cohesion of spray dried formulations were also assessed to understand the relation between surface L-leucine concentration and surface and bulk properties. The surface concentration of L-leucine increased with higher feed concentrations and plateaued at about 10% L-leucine. Higher surface L-leucine concentration also resulted in the formation of larger L-leucine crystals and not much change in crystal size was noted above 10% L-leucine. A change in surface morphology of particles from spherical to increasingly corrugated was also observed with increasing surface L-leucine concentration. Specific collapsed/folded over particles were only seen in formulations with 10% or higher L-leucine feed concentration suggesting a change in particle surface formation process. In addition, bulk cohesion also reduced and approached a minimum with 10% L-leucine concentration. Thus, the surface concentration of L-Ieucine governs particle formation and optimum surface L-Ieucine concentration results in optimum surface and bulk powder properties. (C) 2015 Elsevier B.V. All rights reserved.
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