Kablitz Caroline Désirée, Harder Kim, Urbanetz Nora Anne
Institute of Pharmaceutics and Biopharmaceutics, Heinrich-Heine-Universität Düsseldorf, Universitätsstrasse 1, 40225 Düsseldorf, Germany.
Eur J Pharm Sci. 2006 Feb;27(2-3):212-9. doi: 10.1016/j.ejps.2005.10.001. Epub 2005 Nov 14.
A highly efficient dry coating process was developed to obtain an enteric film avoiding completely the use of organic solvents and water. Using hydroxypropyl methylcellulose acetate succinate (HPMCAS) an enteric coat should be obtained without adding talc as anti-tacking agent because of problems arising from microbiological contamination. Further on, a method was developed preparing isolated films in order to determine the glass transition temperature (T(g)) and the required process temperature. The process was conducted in the rotary fluid bed with a gravimetric powder feeder achieving an exact dosage in contrast to volumetric powder feeder. A three way nozzle was aligned tangential to the pellet bed movement feeding simultaneously powder and plasticizer into the rotary fluid bed. The determined coating efficiency of the talc-free formulation was high with 94% and storage stability regarding tacking could be achieved using colloidal silicium dioxide as top powder. The T(g) of the enteric coat could be determined analyzing the T(g) of isolated films obtained by coating celluloid spheres instead of pellets using the dry coating process in rotary fluid bed. The dry coating process has been demonstrated to be a serious alternative to conventional solvent or water based coating processes.
开发了一种高效的干包衣工艺，以获得肠溶衣，完全避免使用有机溶剂和水。使用醋酸羟丙基甲基纤维素琥珀酸酯（HPMCAS），由于微生物污染产生的问题，无需添加滑石粉作为抗粘剂即可获得肠溶衣。此外，还开发了一种制备分离膜的方法，以确定玻璃化转变温度（T(g)）和所需的工艺温度。该工艺在旋转流化床中进行，使用重量式粉末进料器，与容积式粉末进料器相比，可实现精确计量。一个三通喷嘴与颗粒床运动相切排列，同时将粉末和增塑剂送入旋转流化床。不含滑石粉配方的包衣效率高达94%，使用胶体二氧化硅作为顶粉可实现关于粘性的储存稳定性。通过分析在旋转流化床中使用干包衣工艺包衣赛璐珞球而非颗粒所获得的分离膜的T(g)，可以确定肠溶衣的T(g)。干包衣工艺已被证明是传统溶剂型或水基包衣工艺的一种重要替代方法。
