Heinämäki Jyrki, Halenius Anna, Paavo Maaja, Alakurtti Sami, Pitkänen Pauliina, Pirttimaa Minni, Paaver Urve, Kirsimäe Kalle, Kogermann Karin, Yliruusi Jouko
Department of Pharmacy, Faculty of Medicine, University of Tartu, Nooruse 1, 50411 Tartu, Estonia.
Division of Pharmaceutical Chemistry and Technology, Faculty of Pharmacy, University of Helsinki, P.O. Box 56 (Viikinkaari 5E), FI-00014, Finland.
Int J Pharm. 2015 Jul 15;489(1-2):91-9. doi: 10.1016/j.ijpharm.2015.04.066. Epub 2015 Apr 29.
We showed that the addition of suberin fatty acids (SFAs) even at small concentrations significantly improves the water vapor barrier properties of hydroxypropyl methylcellulose (HPMC) films. SFAs were isolated from the outer birch bark using extractive hydrolysis. The effects of SFAs on the film formation of aqueous HPMC were investigated with free films plasticized with polyethylene glycol (PEG 400). Special attention was paid on the physical solid-state, moisture barrier and mechanical stress-strain properties of films intended for tablet film coatings. Topography and surface morphology, glass transition temperature (Tg), tensile strength, Young's modulus, and water vapor permeation (WVP) of films were studied. The addition of SFAs lowered the Tg of films suggesting partial enhancement in film plasticization. The WVP of films decreased with increasing SFAs concentration up to 15% (calculated as a % w/w from a polymer weight). The WVP value for a non-suberized reference film and suberized film plasticized with PEG 400 was 2.13×10(-6) and 0.69[×10(-6) g/(mm(2)×h)×mm/Pa], respectively. The addition of SFAs impaired the mechanical stress-strain properties of HPMC films by reducing the deformation capacity of film. In conclusion, the film properties and performance of aqueous HPMC can be modified by including SFAs in the films.
我们发现,即使添加低浓度的软木脂脂肪酸(SFAs)也能显著改善羟丙基甲基纤维素(HPMC)薄膜的水蒸气阻隔性能。通过萃取水解从桦树外皮中分离出SFAs。使用聚乙二醇(PEG 400)增塑的游离薄膜研究了SFAs对水性HPMC成膜的影响。特别关注了用于片剂薄膜包衣的薄膜的物理固态、防潮和机械应力-应变性能。研究了薄膜的形貌和表面形态、玻璃化转变温度(Tg)、拉伸强度、杨氏模量和水蒸气透过率(WVP)。SFAs的添加降低了薄膜的Tg,表明薄膜增塑有所增强。薄膜的WVP随着SFAs浓度增加至15%(以聚合物重量的% w/w计算)而降低。未添加软木脂的参比薄膜和用PEG 400增塑的软木脂化薄膜的WVP值分别为2.13×10(-6)和0.69[×10(-6) g/(mm(2)×h)×mm/Pa]。SFAs的添加通过降低薄膜的变形能力而损害了HPMC薄膜的机械应力-应变性能。总之,通过在薄膜中加入SFAs可以改变水性HPMC的薄膜性能和性能表现。