药用涂膜剂物理特性评价方法的建立及其在延龄草总皂苷涂膜剂处方筛选中的应用

An evaluation method for physical properties of medicinal film and its application in screening film formulation of Trillium tschonoskii total saponins

针对中药涂膜剂制剂学特性评价方法的客观性差,且无量化和标准化评价方法的现状,该研究使用了流动指数、失重率、伸长率这3个与涂膜剂制剂学性能关联密切的物理特性参数构建了新的评价方法。在此基础上,以延龄草总皂苷为模型药物,用上述参数做指标优化涂膜剂处方,验证了所建方法和参数在制剂处方优化中应用的可行性及适宜性。该文采用自制流动性测定装置和黏度计来测定和表征流动性,其中流动指数是指单位时间涂膜剂样本的流经距离与其黏度比值;采用3M胶带法测定失重率,通过测定一定时间内样品的失重率来表征其成膜性能;采用电子拉力机测定样品干燥后所成薄膜的伸长率,来表征涂膜剂所成薄膜的延展性。结果证明,实验所建立的流动指数、失重率、伸长率测定方法稳定可靠。以其为指标进行优选,得到了较优的延龄草总皂苷涂膜剂处方。研究表明,流动指数、失重率、伸长率3个评价指标能够指导制剂处方优化设计,据此构建的新评价方法在涂膜剂的处方优化和制剂学质量评价方面展现出较好的应用前景。

At present, the evaluation methods for pharmaceutical properties of Chinese medicinal films have many problems, such as poor objectivity for the indexes and no quantitative and standardized evaluation methods. This study established a new method using three important physical property parameters, i.e., flow index, weight loss rate, and elongation rate, which were closely related to the pharmaceutical properties of films. On this basis, the above parameters were taken as indicators to optimize the film formulation of Trillium tschonoskii total saponins and verify the feasibility and suitability of the established method and parameters in formulation optimization. A self-made flow distance detection device and a viscometer were used to measure and characterize the fluidity, where the flow index refers to the ratio of the flow distance per unit time to the viscosity. The weight loss rate was measured by the 3 M transpore^(TM)surgical tape. The film-forming property was characterized by the weight loss rate of the sample within a certain period of time. An electronic tension machine was employed to measure the elongation rate after drying, which was used to characterize the ductility of the film. The results showed that the established method for the determination of flow index, weight loss rate, and elongation rate was stable and reliable. The optimal film formulation of T. tschonoskii total saponins could be obtained by optimization with those indicators. As demonstrated, the above evaluation indicators(flow index, weight loss rate, and elongation rate) can guide the optimization and design of formulation, and the new evaluation method constructed based on this shows a good application prospect in formulation optimization and formulation quality evaluation of medicinal films.