低频超声波促进重酒石酸卡巴拉汀经皮渗透的研究

目的研究低频超声波对重酒石酸卡巴拉汀(rivastigmine hydrogen tartrate,RHT)经皮渗透的促进作用。方法通过对小鼠、大鼠、小型猪和乳猪皮肤性能的考察,选择乳猪腹部皮肤进行经皮渗透实验。采用20 k Hz的超声波,于单室扩散池中测定2%的RHT水溶液的经皮渗透速率,考察超声波强度和暴露时间的影响。结果当超声波暴露时间为3 min时,超声波强度从2 W·cm?2增加到11 W·cm?2,超声波对RHT的促渗倍数从9.15倍增加到84.79倍。超声波强度为2 W·cm?2时,超声时间从3 min增加到30 min,促渗倍数从9.15倍增加到42.85倍。结论低频超声波对RHT有很强的经皮渗透促进作用,增加超声的功率或者延长超声的时间,均能够明显增强超声对RHT的促渗作用。

Study on Enhancements of Low Frequency Ultrasound to Percutaneous Permeability of Rivastigmine Hydrogen Tartrate

OBJECTIVE To investigate the promoting effect of low frequency ultrasound on percutaneous penetration of rivastigmine hydrogen tartrate. METHODS Through investigating the skin performance of mice, rats, miniature pig and suckling pig, the suckling pig abdominal skin was used in percutaneous experiments. The percutaneous permeability of 2% rivastigmine tartrate solution was determined in one- chamber diffusion cell using 20 kHz ultrasoun. The effects of ultrasonic intensity and exposure time on enhancement were evaluated. RESULTS When the ultrasonic exposure time of 3 min, ultrasonic intensity was increased from 2 to 11 W?cm^-2, the enhance rate increased to 84.79 times from 9.15 times. Ultrasonic intensity of 2 W?cm^-2, ultrasonic time increased from 3 to 30 min, the enhance rate increased from 9.15 to 42.85 times. CONCLUSION Low frequency ultrasound can be effectively used to enhance transdermal delivery of rivastigmine hydrogen tartrate. The increase of ultrasonic intensity or extension of ultrasonic time, can significantly enhance the penetration effect.