Clinical equivalence of intranasal estradiol and oral estrogens for postmenopausal symptoms

Abstract

In conclusion, pulsed estrogen therapy using Aerodiol is safe, easily used and highly efficient in alleviating postmenopausal symptoms with a dose of 300 microg. The dose of 300 microg in one administration per day offers the optimal therapy whilst being easily adaptable to each patient's clinical response.

Factors affecting nasal drug delivery and design strategies for intranasal drug delivery

“…环糊精是由α-1，4-糖苷键连接的葡萄糖单元组成的环状寡糖，具有亲水外表面和亲脂内腔，能够与亲脂性药物形成包合物，改善其溶解度，增强药物的鼻黏膜吸收，如添加环糊精的雌二醇鼻用制剂（Aerodiol ® ）已在欧洲上市 ［ 69 ］ 。同时，环糊精还可作为吸收促进剂，与上皮细胞直接相互作用，增加药物的黏膜渗透。Matsubara等 ［ 70 ］ 研究发现，二甲基-β环糊精能够与促黄体生成激素释放激素发生络合作用改善鼻黏膜通透性，从而增强药物吸收。但环糊精及其衍生物存在局部和全身毒性，易导致鼻腔组织学特征和纤毛摆动频率改变，其溶血毒性和细胞毒性也有报道 ［ 71 ］ 。因此，环糊精在鼻腔药物递送系统的用量及安全性须通过系统毒理实验验证。…”