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目的:建立聚乙二醇负载葛根素前药的载药量测定方法。方法:将葛根素溶于不同浓度的氢氧化钠溶液中在60℃水浴中进行水解,HPLC跟踪筛选出较适宜的水解方法,并将水解产物用NMR进行表征。将葛根素前药通过相应方法水解后,紫外分光光度法测定其水解产物吸光度从而确定葛根素前药载药量。结果:实验发现,葛根素在1 mol.L-1氢氧化钠溶液60℃水浴孵育30 min后水解完全,水解后葛根素转化形成的产物经结构鉴定为二氢葛根素,该物质在碱性溶液中在336 nm处有稳定吸收峰,并且在1.378～28.947μg.mL-1范围内浓度与吸光度呈良好的线性关系,回归方程为:Y=0.0432X+0.077,r=0.9996;平均回收率为99.1%。结论:本方法简便、快速、准确且成本低,可用于葛根素前药的质量控制。
Objective: To establish a method for determination of drug loading of polyethylene glycol loaded puerarin prodrugs. Methods: The puerarin was dissolved in sodium hydroxide solution of different concentrations and hydrolyzed in a water bath at 60 ℃. The suitable hydrolysis method was screened out by HPLC and the hydrolyzate was characterized by NMR. After the puerarin prodrug was hydrolyzed by the corresponding method, the absorbance of its hydrolyzate was determined by ultraviolet spectrophotometry to determine the drug loading amount of puerarin prodrug. Results: The results showed that the puerarin was completely hydrolyzed in a 1 mol. L-1 sodium hydroxide solution at 60 ℃ for 30 min. After the hydrolysis, the product of puerarin was identified as dihydropalcium, The solution had a stable absorption peak at 336 nm, and the linearity was linear with the absorbance in the range of 1.378-28.947 μg · mL-1. The regression equation was Y = 0.0432X + 0.077, r = 0.9996. The average recovery Is 99.1%. Conclusion: The method is simple, rapid, accurate and low cost and can be used for the quality control of puerarin prodrugs.