通过热熔挤出工艺制备的新型控释聚合物-脂质制剂
Novel Controlled Release Polymer-Lipid Formulations Processed by Hot Melt Extrusion.
作者信息
Maniruzzaman Mohammed, Islam Muhammad T, Halsey Sheelagh, Amin Devyani, Douroumis Dennis
机构信息
School of Sciences, Faculty of Engineering and Science, University of Greenwich, Chatham Maritime, Kent, ME4 4TB, UK.
Thermo Fisher Scientific, Stafford House, Boundary Way, Hemel Hempstead, HP2 7GE, UK.
出版信息
AAPS PharmSciTech. 2016 Feb;17(1):191-9. doi: 10.1208/s12249-015-0470-2. Epub 2015 Dec 21.
The aim of the study was to investigate the effect of novel polymer/lipid formulations on the dissolution rates of the water insoluble indomethacin (INM), co-processed by hot melt extrusion (HME). Formulations consisted of the hydrophilic hydroxypropyl methyl cellulose polymer (HPMCAS) and stearoyl macrogol-32 glycerides-Gelucire 50/13 (GLC) were processed with a twin screw extruder to produce solid dispersions. The extrudates characterized by X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC) and hot stage microscopy (HSM) indicated the presence of amorphous INM within the polymer/lipid matrices. In-line monitoring via near-infrared (NIR) spectroscopy revealed significant peak shifts indicating possible interactions and H-bonding formation between the drug and the polymer/lipid carriers. Furthermore, in vitro dissolution studies showed a synergistic effect of the polymer/lipid carrier with 2-h lag time in acidic media followed by enhanced INM dissolution rates at pH > 5.5.
本研究的目的是研究新型聚合物/脂质制剂对通过热熔挤出（HME）共处理的水不溶性吲哚美辛（INM）溶解速率的影响。制剂由亲水性羟丙基甲基纤维素聚合物（HPMCAS）和硬脂酰聚乙二醇-32甘油酯-Gelucire 50/13（GLC）组成，用双螺杆挤出机加工以制备固体分散体。通过X射线粉末衍射（XRPD）、差示扫描量热法（DSC）和热台显微镜（HSM）表征的挤出物表明在聚合物/脂质基质中存在无定形INM。通过近红外（NIR）光谱进行的在线监测显示出明显的峰位移，表明药物与聚合物/脂质载体之间可能存在相互作用和氢键形成。此外，体外溶出度研究表明，聚合物/脂质载体具有协同作用，在酸性介质中有2小时的滞后时间，随后在pH>5.5时INM的溶解速率提高。
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