Department of Chemical Engineering, Massachusetts Institute of Technology, 50 Ames St, E19-502b, Cambridge, Massachusetts 02139, USA.
Pharm Res. 2013 Jan;30(1):238-46. doi: 10.1007/s11095-012-0868-4. Epub 2012 Aug 25.
To investigate the use of electrospinning for forming solid dispersions containing crystalline active pharmaceutical ingredients (API) and understand the relevant properties of the resulting materials.
Free surface electrospinning was used to prepare nanofiber mats of poly(vinyl pyrrolidone) (PVP) and crystalline albendazole (ABZ) or famotidine (FAM) from a suspension of the drug crystals in a polymer solution. SEM and DSC were used to characterize the dispersion, XRD was used to determine the crystalline polymorph, and dissolution studies were performed to determine the influence of the preparation method on the dissolution rate.
The electrospun fibers contained 31 wt% ABZ and 26 wt% FAM for the 1:2 ABZ:PVP and 1:2 FAM:PVP formulations, respectively, and both APIs retained their crystalline polymorphs throughout processing. The crystals had an average size of about 10 μm and were well-dispersed throughout the fibers, resulting in a higher dissolution rate for electrospun tablets than for powder tablets.
Previously used to produce amorphous formulations, electrospinning has now been demonstrated to be a viable option for producing fibers containing crystalline API. Due to the dispersion of the crystals in the polymer, tablets made from the fiber mats may also exhibit improved dissolution properties over traditional powder compression.
研究静电纺丝在形成含有结晶药物成分（API）的固体分散体中的应用，并了解所得材料的相关性质。
采用自由表面静电纺丝技术，从药物晶体在聚合物溶液中的悬浮液中制备聚（乙烯基吡咯烷酮）（PVP）和结晶阿苯达唑（ABZ）或法莫替丁（FAM）的纳米纤维垫。SEM 和 DSC 用于对分散体进行表征，XRD 用于确定结晶多晶型，溶解研究用于确定制备方法对溶解速率的影响。
对于 1:2 ABZ:PVP 和 1:2 FAM:PVP 配方，静电纺纤维分别包含 31wt%ABZ 和 26wt%FAM，两种 API 在整个加工过程中均保持其结晶多晶型。晶体的平均尺寸约为 10μm，并且在纤维中很好地分散，导致静电纺丝片的溶解速率高于粉末片。
静电纺丝以前曾用于制备非晶形配方，现在已被证明是一种可行的选择，可以制备含有结晶 API 的纤维。由于晶体在聚合物中的分散，因此由纤维垫制成的片剂在溶解性能方面可能优于传统的粉末压缩。
