Hermens W A, Hooymans P M, Verhoef J C, Merkus F W
Department Clinical Pharmacy and Toxicology, Maasland Hospital, Sittard, The Netherlands.
Pharm Res. 1990 Feb;7(2):144-6. doi: 10.1023/a:1015872617511.
Sodium taurodihydrofusidate (STDHF) is one of the most promising absorption enhancers for nasal delivery of peptide drugs. Drugs and additives in nasal formulations should not interfere with the self-cleaning capacity of the nose by the ciliary epithelium. Measured in vitro on human adenoid tissue with a photoelectric method, STDHF was found to induce ciliostasis at concentrations of 0.3% (w/v) and higher. STDHF (0.3%) is less ciliostatic than laureth-9 (0.3%) or deoxycholate (0.3%). Glyco- and taurocholate (0.3%) show only very mild effects on nasal ciliary movement. Human insulin (1%) has no ciliostatic potency in vitro, whereas a combination of human insulin (1%) and STDHF (1%) is ciliostatic but not as potent as STDHF (1%) alone.
牛磺二氢fusidate钠（STDHF）是肽类药物鼻腔给药最有前景的吸收促进剂之一。鼻腔制剂中的药物和添加剂不应干扰鼻纤毛上皮的自我清洁能力。通过光电方法在人腺样体组织上进行体外测量，发现STDHF在浓度为0.3%（w/v）及更高时会诱导纤毛运动停滞。STDHF（0.3%）的纤毛运动抑制作用比月桂醇聚醚-9（0.3%）或脱氧胆酸盐（0.3%）小。甘氨胆酸盐和牛磺胆酸盐（0.3%）对鼻纤毛运动仅表现出非常轻微的影响。人胰岛素（1%）在体外没有纤毛运动抑制效力，而人胰岛素（1%）和STDHF（1%）的组合具有纤毛运动抑制作用，但不如单独的STDHF（1%）有效。
