Dreu Rok, Sirca Judita, Pintye-Hodi Klara, Burjan Tanja, Planinsek Odon, Srcic Stane
University of Ljubljana, Faculty of Pharmacy, Askerceva 7, SI-1000 Ljubljana, Slovenia.
Int J Pharm. 2005 Mar 3;291(1-2):99-111. doi: 10.1016/j.ijpharm.2004.07.047. Epub 2004 Dec 29.
The use of ethanol or ethanol/water mixtures as granulation liquids in the extrusion-spheronisation process results in the formation of pellets with significantly different mechanical and structural properties from those prepared using water alone. The product of surface tension (gammaL), relative permittivity (epsilonR) of the granulation liquid and the cosine of contact angle (Theta) of granulation liquid on pellets solid has been introduced in order to explain the mechanism of this phenomenon. A correlation is shown between the factor gammaL x cos(Theta) x epsilonR and the properties of the pellets produced. We have introduced the gammaL x cos(Theta) x epsilonR which can be considered to represent the driving and counteracting forces of pellet contraction during drying. The contact angles and surface tensions were evaluated using the Wilhelmy plate method. Pellets were produced by extrusion-spheronisation technique using water, ethanol and ethanol/water mixtures as granulation liquids. Subsequent characterization of the pellets showed that their tensile strength and disintegration times increase with increase in the proposed factor gammaL x cos(Theta) x epsilonR, while friability, average pore diameter and porosity decreases. The observed correlations show, that the granulation liquid influences the mechanical and structural properties of the pellets through the contraction driving and contraction counteracting forces during drying.
在挤出滚圆法中使用乙醇或乙醇/水混合物作为制粒液体,会导致所形成颗粒的机械性能和结构性能与仅用水制备的颗粒有显著差异。引入了制粒液体的表面张力(γL)、相对介电常数(εR)以及制粒液体在颗粒固体上的接触角(θ)的余弦值的乘积,以解释这一现象的机理。结果表明,γL×cos(θ)×εR这一因子与所生产颗粒的性能之间存在相关性。我们引入了γL×cos(θ)×εR,它可被视为代表干燥过程中颗粒收缩的驱动力和反作用力。使用Wilhelmy平板法评估接触角和表面张力。采用挤出滚圆技术,以水、乙醇和乙醇/水混合物作为制粒液体制备颗粒。随后对颗粒的表征显示,其拉伸强度和崩解时间随着所提出的γL×cos(θ)×εR因子的增加而增加,而脆碎度、平均孔径和孔隙率则降低。观察到的相关性表明,制粒液体在干燥过程中通过收缩驱动力和收缩反作用力影响颗粒的机械性能和结构性能。