Targeted Drug Delivery Research Center, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran ; Department of Pharmaceutics, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran.
Department of Pharmaceutics, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran.
Iran J Basic Med Sci. 2013 Oct;16(10):1100-8.
OBJECTIVE(S): This study was performed aiming to investigate the effect of particle engineering via spray drying of hydroalcoholic solution on solid states and physico-mechanical properties of acetaminophen.
Spray drying of hydroalcoholic solution (25% v/v ethanol/water) of acetaminophen (5% w/v) in the presence of small amounts of polyninylpyrrolidone K30 (PVP) (0, 1.25, 2.5 and 5% w/w based on acetaminophen weight) was carried out. The properties of spray dried particles namely morphology, surface characteristics, particle size, crystallinity, dissolution rate and compactibility were evaluated.
Spray drying process significantly changed the morphology of acetaminophen crystals from acicular (rod shape) to spherical microparticle. Differential scanning calorimetery (DSC) and x-ray powder diffraction (XRPD) studies ruled out any polymorphism in spray dried samples, however, a major reduction in crystallinity up to 65%, especially for those containing 5% w/w PVP was observed. Spray dried acetaminophen particles especially those obtained in the presence of PVP exhibited an obvious improvement of the dissolution and compaction properties. Tablets produced from spray dried samples exhibited excellent crushing strengths and no tendency to cap.
The findings of this study revealed that spray drying of acetaminophen from hydroalcoholic solution in the presence of small amount of PVP produced partially amorphous particles with improved dissolution and excellent compaction properties.
本研究旨在考察通过喷雾干燥水醇溶液对扑热息痛的固体状态和物理力学性质的影响。
在少量聚乙烯吡咯烷酮 K30（PVP）（基于扑热息痛重量的 0、1.25、2.5 和 5% w/w）存在下，对 5% w/v 的扑热息痛水醇溶液（25% v/v 乙醇/水）进行喷雾干燥。评估喷雾干燥颗粒的性质，如形态、表面特性、粒径、结晶度、溶出率和可压缩性。
喷雾干燥过程显著改变了扑热息痛晶体的形态，从针状（棒状）变为球形微颗粒。差示扫描量热法（DSC）和 X 射线粉末衍射（XRPD）研究排除了喷雾干燥样品中的任何多晶型现象，但观察到结晶度大幅下降，最高可达 65%，特别是含有 5% w/w PVP 的样品。喷雾干燥的扑热息痛颗粒，尤其是在 PVP 存在下获得的颗粒，表现出明显改善的溶解和压实性能。由喷雾干燥样品制成的片剂表现出优异的抗压强度，且无崩解倾向。
本研究结果表明，在少量 PVP 的存在下，从水醇溶液中喷雾干燥扑热息痛可产生部分无定形颗粒，具有改善的溶解性能和优异的压实性能。
