Bremecker K D, Strempel H, Klein G
J Pharm Sci. 1984 Apr;73(4):548-52. doi: 10.1002/jps.2600730429.
Conventional adhesive ointments cause irritation to the mucous membranes. Therefore, a novel mucosal adhesive ointment based partly on neutralized polymethacrylic acid methyl ester was formulated. The flow curves of the ointment vehicle showed pseudoplastic properties. The rheological behavior as well as the adhesion on the mucosal membrane could be varied by the type and concentration of the polymer used and the base used for neutralization. During clinical studies, the ointment vehicle as well as a tretinoin (vitamin A acid) preparation for the treatment of lichen planus did not cause any local irritation or systemic side effects. Both vehicle and preparation were found to be pleasant for the patients to use. The new system of the mucosal adhesive ointment is not limited to the incorporation of tretinoin as the active agent; combined with other drugs the system could be applied to all types of mucosal membranes.
传统的粘性软膏会刺激粘膜。因此,研制出了一种新型的粘膜粘着软膏,其部分基于中和的聚甲基丙烯酸甲酯。软膏基质的流动曲线显示出假塑性特性。流变行为以及在粘膜上的粘附力可通过所用聚合物的类型和浓度以及用于中和的基质来改变。在临床研究中,软膏基质以及用于治疗扁平苔藓的维甲酸(维生素A酸)制剂均未引起任何局部刺激或全身副作用。发现基质和制剂对患者来说使用起来都很舒适。粘膜粘着软膏的新系统并不局限于加入维甲酸作为活性剂;与其他药物联合使用时,该系统可应用于所有类型的粘膜。