辛苯聚醇阴道用温敏凝胶的流变学特性及缓释滞留性研究

Rheological Properties and Retention Ability of Octoxynol-9 Vaginal Thermosensitive in Situ Gel

目的:考察辛苯聚醇阴道用温敏凝胶[(O-9)-VTG]的流变学性质以预测其在体胶凝行为;评价其在阴道内的滞留性。方法:采用哈克旋转流变仪测定(O-9)-VTG在相变过程中及经阴道模拟液稀释后的流变学参数,考察其流变学性质。大鼠阴道给予自制(O-9)-VTG和O-9凝胶,分别测定阴道冲洗液中辛苯聚醇浓度,评价其滞留性。结果:(O-9)-VTG在室温条件下为黏弹性较低的牛顿流体,温度升至32.6℃时相变完成;且经阴道模拟液稀释后在体温条件下仍能形成凝胶。制备的(O-9)-VTG可在大鼠阴道滞留时间达8 h以上。结论:(O-9)-VTG具有适宜的胶凝温度和良好的流变学性质;与自制O-9凝胶相比,(O-9)-VTG具有显著的阴道黏附滞留性,能更好地满足阴道局部用药的要求。

Objective： To observe the rheological properties of octoxynol-9 vaginal thermosensitive in situ gel [ （ 0-9 ） -VTG ] for predicting the gelation behavior in vivo, and evaluate the retention ability in vagina. Methods ： The rheological parameters of （ 0-9 ） - VTG and （O-9）-VTG diluted by stimulant vaginal fluid （SVF） were measured by a Haake Rheomix to characterize the rheological properties. The vaginal samples after the administration of self-made （ 0-9 ） -VTG and 0-9 gel were withdrawn, and then the concentra- tion of octoxynol-9 in the samples was determined to evaluate the retentionability. Results ： （0-9） -VTG was Newtonian fluid with low viscoelasticity under room temperature and converted to gel at 32.6℃. The formula could still transform into gel at body temperature af- ter diluted by SVF, and resided in the vagina of mice above 8 h. Conclusion： （O-9） -VTG has suitable gelation temperature and rheo- logical properties. Compared with the self-made octoxynol-9 gel, （0-9）-VTG has satisfactory retention in vagina, which meets the re- auirements for vazinal topical use.