Li Jing, Fan Na, Wang Xin, Li Chang, Sun Mengchi, Wang Jian, Fu Qiang, He Zhonggui
Wuya College of Innovation, Shenyang Pharmaceutical University, Shenyang, China.
Key Laboratory of Structure-Based Drug Design and Discovery, Shenyang Pharmaceutical University, Ministry of Education, Wenhua Road, No. 103, Shenyang 110016, China.
Eur J Pharm Sci. 2017 Aug 30;106:244-253. doi: 10.1016/j.ejps.2017.05.067. Epub 2017 Jun 1.
The present work studied interfacial interactions of amorphous solid dispersions matrix of indometacin (IMC) that established using PVP K30 (PVP) and PEG 6000 (PEG) by focusing on their interaction forces and wetting process. Infrared spectroscopy (IR), raman spectroscopy, X-ray photoelectron spectra and contact angle instrument were used throughout the study. Hydrogen bond energy formed between PEG and IMC were stronger than that of PVP and IMC evidenced by molecular modeling measurement. The blue shift of raman spectroscopy confirmed that hydrogen bonding forces were formed between IMC and two polymers. The contact angle study can be used as an easy method to determine the dissolution mechanism of amorphous solid dispersions through fitting the profile of contact angle of water on a series of tablets. It is believed that the track of interfacial interactions will certainly become powerful tools to for designing and evaluating amorphous solid dispersions.
本研究通过关注吲哚美辛（IMC）与聚乙烯吡咯烷酮K30（PVP）和聚乙二醇6000（PEG）形成的非晶态固体分散体基质的相互作用力和润湿过程，对其界面相互作用进行了研究。在整个研究过程中使用了红外光谱（IR）、拉曼光谱、X射线光电子能谱和接触角测量仪。分子模拟测量证明，PEG与IMC之间形成的氢键能比PVP与IMC之间的更强。拉曼光谱的蓝移证实了IMC与两种聚合物之间形成了氢键力。接触角研究可作为一种简便方法，通过拟合水在一系列片剂上的接触角曲线来确定非晶态固体分散体的溶解机制。据信，界面相互作用轨迹必将成为设计和评估非晶态固体分散体的有力工具。
