das Neves José, Amaral Maria Helena, Bahia Maria Fernanda
Department of Pharmaceutical Technology, Faculty of Pharmacy of the University of Porto, Porto, Portugal.
Eur J Pharm Biopharm. 2008 Jun;69(2):622-32. doi: 10.1016/j.ejpb.2007.12.007. Epub 2008 Jan 14.
The purpose of this work was to develop an in vitro mucoadhesion testing method for vaginal semisolid formulations. The proposed method was based on the measurement of the force (detachment force, Fdt) and the work (work of adhesion, Wad) needed to detach a sample of cow vaginal mucosa from a semisolid formulation, using a commercially available texture analyzer. Several testing conditions and instrumental parameters were tested in order to evaluate the mucoadhesive potential of a model vaginal semisolid formulation (1% Carbopol 974P gel). Also, mucoadhesive potential of several commercially available vaginal semisolid products was evaluated. Obtained results showed that the method is reproducible even when the same cow mucosa sample is used up to six times. The similarity of the fluid used to bathe the vaginal mucosa to the one naturally occurring in the vagina influenced considerably the performance of the test, advising that simulation of vaginal fluid properties is important when measuring mucoadhesive properties. Also, temperature of experiment was an important fact to be considered, as results showed slight but significant differences between body (37 degrees C) and room (20 degrees C) temperature. Fdt and Wad increased with increasing instrumental parameters while a plateau region was observable at higher values of probe speed, probe force, and mucosa/sample contact time. Comparison between results for Fdt and Wad demonstrated that although both parameters are generally in agreement, Wad seems to be more reliable and reproducible when evaluating mucoadhesion. Evaluation of commercially available formulations confirmed that experimental conditions are important features that can influence significantly the determination of mucoadhesive potential, being the proposed method an interesting and useful tool in the in vitro evaluation of vaginal semisolids.
这项工作的目的是开发一种用于阴道半固体制剂的体外黏膜黏附测试方法。所提出的方法基于使用市售的质构分析仪测量将牛阴道黏膜样本从半固体制剂上分离所需的力（分离力，Fdt）和功（黏附功，Wad）。测试了几种测试条件和仪器参数，以评估一种典型阴道半固体制剂（1%卡波姆974P凝胶）的黏膜黏附潜力。此外，还评估了几种市售阴道半固体产品的黏膜黏附潜力。获得的结果表明，即使同一牛黏膜样本使用多达六次，该方法仍具有可重复性。用于冲洗阴道黏膜的液体与阴道中自然存在的液体的相似性对测试性能有很大影响，这表明在测量黏膜黏附特性时模拟阴道液体特性很重要。此外，实验温度也是一个需要考虑的重要因素，因为结果显示体温（37摄氏度）和室温（20摄氏度）之间存在轻微但显著的差异。Fdt和Wad随着仪器参数的增加而增加，而在较高的探头速度、探头力和黏膜/样品接触时间值时可观察到一个平稳区域。Fdt和Wad结果的比较表明，虽然这两个参数总体上一致，但在评估黏膜黏附时，Wad似乎更可靠且可重复。对市售制剂的评估证实，实验条件是可显著影响黏膜黏附潜力测定的重要因素，所提出的方法是体外评估阴道半固体的一种有趣且有用的工具。
