Product Development, Prinston Pharmaceutical Inc., Somerset, New Jersey, USA.
College of Pharmacy, University of Iowa, Iowa City, Iowa, USA.
AAPS PharmSciTech. 2018 Aug;19(6):2740-2749. doi: 10.1208/s12249-018-1113-1. Epub 2018 Jul 5.
Most film coatings in the pharmaceutical industry are prepared using organic solvents or aqueous solvents. Due to different film-formation mechanisms, their properties are significantly different from each other. Curing can alter the microstructure of films by improving the coalescence of polymer particles for aqueous dispersion-based films or accelerating macromolecule relaxation for organic solvent-based films. The aim of this study was to investigate the effects of preparation methods and curing on the physicochemical properties of Kollicoat® SR30D and Kollicoat® MAE100P films. The film's properties, including water diffusion coefficient, mechanical properties, plasticizer loss, swelling behavior, and contact angle, were measured for uncured or cured aqueous dispersion-based or organic solvent-based films. The results indicated that curing decreased water diffusivities in films and increased film's tensile strength. Curing resulted in plasticizer loss from SR30D films but not from MAE100P films due to strong interaction between plasticizer and MAE100P. The surface of organic solvent-based films was more hydrophobic than that of aqueous dispersion-based films. The contact angle of organic solvent-based films was increased after curing possibly because curing decreased roughness of the film surface. Organic solvent-based SR30D films had better mechanical properties than the corresponding aqueous dispersion-based films because of higher degree of polymer-polymer entanglement in the organic solvent-based films. However, contradictory phenomena were observed in MAE100P films possibly due to a "core-shell" structure reserved in the aqueous dispersion-based MAE100P films. In summary, casting methods and curing have significant impact on the film properties due to different film structures, coalescence, or film relaxation, and other concurrent effects including evaporation of residue solvent and plasticizers.
大多数制药行业的薄膜包衣都是使用有机溶剂或水溶剂制备的。由于成膜机制不同,它们的性质彼此有很大的差异。固化可以通过提高聚合物颗粒的聚集程度来改变水性分散体基膜的微观结构,或加速大分子松弛来改变有机溶剂基膜的微观结构。本研究旨在研究制备方法和固化对 Kollicoat® SR30D 和 Kollicoat® MAE100P 薄膜的物理化学性质的影响。对未固化或固化的水性分散体基或有机溶剂基薄膜,测量了薄膜的性质,包括水扩散系数、力学性能、增塑剂损失、溶胀行为和接触角。结果表明,固化降低了薄膜中的水扩散系数,并提高了薄膜的拉伸强度。固化导致 SR30D 薄膜中的增塑剂损失,但 MAE100P 薄膜中没有,因为增塑剂与 MAE100P 之间存在强烈的相互作用。有机溶剂基薄膜的表面比水性分散体基薄膜更疏水。由于固化降低了薄膜表面的粗糙度,有机溶剂基薄膜的接触角增大。有机溶剂基 SR30D 薄膜的力学性能优于相应的水性分散体基薄膜,因为有机溶剂基薄膜中聚合物-聚合物缠结程度更高。然而,在 MAE100P 薄膜中观察到了相反的现象,这可能是由于水性分散体基 MAE100P 薄膜中保留了“核壳”结构。总之,由于不同的薄膜结构、聚集或薄膜松弛以及其他并发效应,如残留溶剂和增塑剂的蒸发,浇铸方法和固化对薄膜性能有显著影响。