抗HBV有效成分丁香苦苷纳米靶向冻干粉的质量及安全性评价

Quality and Safety Evaluation of Syringopicroside Nano-targeted Freeze-dried Po wder Resistant to HBV Active Ingredients

目的:对丁香苦苷固体脂质纳米粒(S-SLN)冻干粉进行质量评价及安全性评价,为临床用药提供参考依据。方法:按照2015版《中国药典》的方法进行S-SLN冻干粉制剂的性状、p H值、粒度分布、表面电荷及含量测定,采用动物急性毒性实验方法,进行S-SLN冻干粉制剂的安全性评价。结果:S-SLN冻干粉为白色松散块状物,透射电镜下观察可见S-SLN冻干粉呈类球形,表面较光滑,p H值为6.32,粒度分布为150~200 nm,平均粒径为192.8 nm,Zeta电位为-39.8 mV,平均相对含量为105.6%,急性毒性实验最大给药量为200 mg/kg,相当于临床用药量的最大耐受倍数的125倍。结论:S-SLN冻干粉制剂质量和安全性均符合要求。

Objective: To evaluate the quality and safety of syringopicroside solid lipid nanoparticles(S-SLN freeze-dried powder, and provide reference for clinical drug use. Methods: According to the method of 2015 edition of "Chinese Pharmacopoeia", the properties, p H value, particle size distribution, surface charge and content of S-SLN lyophilized powder preparation were determined, and the safety evaluation of S-SLN freeze-dried powder preparation was carried out by using animal acute toxicity test method. Results: S-SLN freeze-dried powder was a white loose block, and it was observed under transmission electron microscope that S-SLN freezedried powder was spherical, the surface was smooth. The p H value was 6.32, the particle size was distributed between 150-200 nm, the average particle size was 192.8 nm, Zeta potential was-39.8 mV, the average relative content was 105.6%, and the maximum dose of acute toxicity test was 200 mg/kg, which was equivalent to 125 times the maximum tolerance multiple of clinical dosage. Conclusion: The quality and safety of S-SLN freezedried powder preparations are in accordance with the requirements of clinical application.