三七总皂苷口服制剂的处方前研究

Pre-formulation study on panax notoginseng saponins oral formulation

目的:对三七总皂苷进行处方前研究,为设计优良的口服制剂处方奠定基础。方法:利用HPLC建立测定三七总皂苷的体外分析方法,并进行pH值、溶解度、油水分配系数、影响因素实验等处方前研究。结果:R1,Rb1和Rg1的线性范围分别为2.81～90μg.mL-1,2.91～93μg.mL-1和4.78～153μg.mL-1,线性良好(r=0.999 9)。处方前研究证实三七总皂苷极易吸湿、不耐光照、耐高温,弱酸性,在pH 4.5的缓冲液中溶解度最大,油水分配系数对数值均小于1。结论:建立的分析方法准确可靠。处方前研究表明三七总皂苷易吸湿,在酸性溶液中不稳定、易降解。

Objective：To study the properties of panax notoginseng saponins（PNS） so as to design the optimal oral formulation.Methods：An HPLC method was established to determine the content of PNS.Based on the method,the pH,saturate solubility,oil/water partition coefficient and stress testing on PNS were investigated.Results：A good linear relationship（r=0.9999） was obtained over the range of 2.81 to 90μg·mL-1 for notoginsenoside R1,2.91 to 93μg·mL-1 for ginsenoside Rb1 and 4.78 to 153μg·mL-1 for ginsenoside Rg1.The pre-formulation study proved that PNS was hygroscopic,week acid,unstable under strong light and stable at high temperature.The saturate solubility of PNS in a buffer of pH 4.5 was the maximum and its logarithmic oil/water partition coefficients were all less than 1.Conclusion：The HPLC method for determining the content of PNS is accurate and reliable.PNS is hygroscopic and unstable in acidic solution,and decomposes easily.