Hot-melt extrusion process impact on polymer choice of glyburide solid dispersions: The effect of wettability and dissolution

被引:29
|
作者
Alshafiee, Maen [1 ]
Aljammal, Mohammad K. [1 ]
Markl, Daniel [2 ]
Ward, Adam [1 ]
Walton, Karl [3 ]
Blunt, Liam [3 ]
Korde, Sachin [4 ]
Pagire, Sudhir K. [4 ]
Kelly, Adrian L. [4 ,5 ]
Paradkar, Anant [4 ]
Conway, Barbara R. [1 ]
Asare-Addo, Kofi [1 ]
机构
[1] Univ Huddersfield, Dept Pharm, Huddersfield HD1 3DH, W Yorkshire, England
[2] Univ Strathclyde, Strathclyde Inst Pharm & Biomed Sci, 161 Cathedral St, Glasgow G4 0RE, Lanark, Scotland
[3] Univ Huddersfield, EPSRC Future Metrol Hub, Huddersfield HD1 3DH, W Yorkshire, England
[4] Univ Bradford, Ctr Pharmaceut Engn Sci, Bradford, W Yorkshire, England
[5] Univ Bradford, IRC Polymer Sci & Technol, Bradford, W Yorkshire, England
基金
英国工程与自然科学研究理事会;
关键词
Solid dispersion; Glyburide; Hot-melt extrusion; Contact angle; Soluplus (R); Kollidon (R) VA64; WATER-SOLUBLE DRUGS; GLUCOSAMINE HCL; STATE BEHAVIORS; FORMULATION; RELEASE; BIOAVAILABILITY; POLYSACCHARIDE; LYOPHILIZATION; MISCIBILITY; PIROXICAM;
D O I
10.1016/j.ijpharm.2019.01.038
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The aim of this study was to evaluate the choice of polymer and polymer level on the performance of the microstructure and wettability of hot-melt extruded solid dispersion of Glyburide (Gly) as a model drug. The produced solid dispersion were characterised using scanning electron microscopy (SEM), image analysis using a focus variation instrument (FVI), differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD), Xray microtomography (X mu T), dynamic contact angle measurement and dissolution analysis using biorelevant dissolution media (FASSIF). SEM and focus variation analysis showed that the microstructure and surface morphology was significantly different between samples produced. This was confirmed by further analysis using X mu T which showed that an increase in polymer content brought about a decrease in the porosity of the hot-melt extruded dispersions. DSC suggested complete amorphorisation of Gly whereas XRPD suggested incomplete amorphorisation. The static and dynamic contact angle measurement correlated with the dissolution studies using FASSIF media indicating that the initial liquid imbibition process as captured by the dynamic contact angle directly affects the dissolution performance.
引用
收藏
页码:245 / 254
页数:10
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