超微粉碎对银翘散急性毒性和主要药效学的影响

目的:探讨超微粉碎对银翘散急性毒性、解热、抗炎及体外抗菌活性的影响。方法:以最大给药量法进行两种粉体的急性毒性对比研究。以2,4-二硝基苯酚致热模型和二甲苯致炎模型,比较银翘散超微粉碎前后的解热抗炎药效学差异。以平皿打孔法和试管二倍稀释法对比研究银翘散普通粉及其超微粉的抗菌活性。结果:急性毒性试验结果表明银翘散及其超微粉1日内最大给药量为45.75 g·kg-1,相当于人的临床日用量的152.5倍,未见由药物引起的毒性反应。解热和抗炎药效学结果表明银翘散的超微粉对2,4-二硝基苯酚所致发热大鼠具有显著的解热作用(P<0.05),对二甲苯所致小鼠耳肿胀具有显著的抑制作用(P<0.05),与等剂量银翘散的细粉相比,作用更明显。且超微粉剂量减半后仍能达到原剂量细粉的药效学效应。抗菌活性实验结果表明银翘散超微粉和细粉水提物对肺炎链球菌和乙型溶血性链球菌的MIC分别为24.22 mg·m L-1、48.43 mg·m L-1;细粉对两种细菌的MIC是超微粉的2倍。结论:超微粉碎后银翘散仍是安全有效的,且可考虑保证药效的基础上减少银翘散的服用剂量,并为银翘散超微粉的临床应用提供一定的实验依据。

Effect of ultrafine process on the acute toxicity and major pharmacodynamics of Yinqiao San

OBJECTIVE To investigate the effect of ultrafine process on the acute toxicity, antipyretic, anti-inflammatory and antibacterial activity of Yinqiao San. METHODS The acute toxicity test was carried out with the maximum dose method. The antipyretic and antipyretic effects were examined in the 2,4-dinitrophenol induced pyrogen model and the xylene induced inflammation model. The antimicrobial activity was examined by using the plate punching method and double dilution method. RESULTS The results of acute toxicity test showed that the maximum dosage of Yinqiao San and its ultrafine powder was 45.75 g·kg^-1, which was equivalent to 152.5 times of the daily dose of human, and no toxic reaction was caused by drug. The results of antipyretic and antiinflammatory pharmacodynamics showed that the ultrafine powder of Yinqiao San had significant antipyretic effect on 2,4-dinitrophenol induced fever rats (P<0.05), and significant inhibitory effect on P-xylene induced mouse ear swelling (P<0.05). Compared with ordinary powder at the same dose, the role of ultrafine powder was more obvious. And ultrafine powder at half dose and full dose ordinary powder had equivalent effects. The results of antimicrobial activity showed that the MICs of the water extract of ultrafine powder and ordinary powder were 24.22 mg·mL^-1 and 48.43 mg·mL^-1 for Streptococcus pneumoniae and beta Streptococcus hemolyticus, respectively. CONCLUSION After the ultrafine process, Yinqiao San is still safe and effective. It can be considered to reduce the dose of Yinqiao San based on ensuring the efficacy, and provide a certain experimental basis for the clinical application of ultrafine powder.