马钱子超微粉对类风湿性关节炎模型大鼠的量效关系参数研究

The Dose-Effect Relationship Parameters of Ultrafine Powder of Strychni Semen on Rats Suffered From Rheumatoid Arthritis

目的比较马钱子超微粉及其粗粉对类风湿性关节炎模型大鼠的影响的量效关系差异。方法以佐剂性关节炎大鼠为模型动物,以雷公藤多苷片为阳性药,分别给予马钱子超微粉及粗粉50.0、35.0、24.5、17.2、12.0 mg/kg,计算不同给药组动物的足肿胀率、足肿胀抑制率及效应率、ED50及ED95。通过急性毒性试验计算马钱子超微粉与粗粉的LD50及LD5,并根据所得数据计算马钱子超微粉及粗粉的最大效能(Emax)、效价强度(KD)、治疗指数(TI)和安全界限(SF)。结果马钱子超微粉的ED50、ED95、LD50、LD5、KD、依次为14.3、24.1、131.4、91.6、14.21 mg/kg,Emax为97.11%,TI和SF为9.2和3.8。马钱子粗粉的ED50、ED95、LD50、LD5、KD、依次为23.2、28.6、156.8、110.4、21.63 mg/kg,Emax为93.96%,TI和SF为6.8和3.9。结论马钱子超微粉的药效明显优于其粗粉,临床使用剂量可以降低至其粗粉的2/3且有效剂量范围增大了1.13倍,但急性毒性较粗粉也相应增大。建议临床采取小剂量多次给药形式使用马钱子超微粉。

Objective： To compare the dose-effect relationship parameters of ultrafine powder of Strychni Semen on rats suffered from rheumatoid arthritis.Method： Rats suffered from adjuvant arthritis was model animals,Tripterygium wilfordii polyglycosides piece was positive drug,give ultrafine and coarse powder of Strychni Semen 50.0,35.0,24.5,17.2,12.0 mg/kg,animal paw swelling rate,paw swelling inhibition rate and effect,ED50 and ED95 were calculated.The LD50 and LD5 of ultrafine and coarse powder of Strychni Semen were calculated by acute toxicity test.And according to the data obtained the Emax,KD,TI,SF of ultrafine and coarse powder of Strychni Semen.Result： The ED50,ED95,LD50,LD5 and KD of ultrafine powder of Strychni Semen was 14.3,24.1,131.4,91.6,14.21 mg/kg,Emax was 97.11%,TI was 9.2 and SF was 3.8.The ED50,ED95,LD50,LD5 and KD of coarse powder of Strychni Semen was 23.2,28.6,156.8,110.4,21.63 mg/kg,Emax was 93.96%,TI was 6.8 and SF was 3.9.Conclusion： The effect of ultrafine powder is better than coarse powder,and its clinical dose can be reduced to 2/3 of their coarse and the effective dosage range is increased 1.13 times,but the acute toxicity also increases accordingly compared to coarser powder.It should use ultrafine powder of Strychni Semen by small and multiple dose.