The Comparision Of Chemical Ingredients And Pharmacodynamics Between Classical And Ultramicro Sini Decoction

OBJECTIVE: Most researches about ultramicro prescriptions are concentrated on such Chinese medical materials as ginseng, American ginseng and notoginseng, et al. The results of these researches indicate that the active ingredients in these Chinese medical materials which are ultramicrosized are extracted more completely and their pharmacodynamic action are strengthened too. However, if those Chinese medical materials that contain some poisonous ingredients are ultramicrosized, will the patient be safe after taking in them? Few scholars pay close attention to this problem. We are to investigate the difference in the chemical ingredients and pharmacodynamics action of classical and ultramicro sini decoction and provide some useful information and proof for their clinical use.METHOD: We respectively isolated and determined the content of the chemical components as alkaloids and glycyrrhetic acid by HPLC in classical and ultramicro sini decoction. We also compared their effects on cardiac contractile force and cardiac output and HR in normal isolated toad heart.RESULT: 1,We established a HPLC moethod for simultaneous content of mesaconitine, hypaconitine and aconitine in sini decoction. Kromasil C₁₈ (150 mm×4．6 mm,5μm) was used as chromatographic column, Phenomenex C₁₈ as protective column,30 mmol·L^-1 ammonium acetate (include 2．5‰HAc, 5‰NH₃·H₂O,pH=8．5) : acetonitrile (67 : 33) as mobile phase. The detection wavelength was set at 230 nm, the flow rate at 1．6 mL·min^-1 and the column temperature at 40℃.The pH value of mobile phase can protect the chromatographic column effectively, and other ingredients in sini decoction don't interfere the determination of the three alkaloids. The sample sizes of mesaconitine, hypaconitine, aconitine had good lineae relationship with their peak areas in the range of 0．0047～0．188μg (r=0．9995) , 0．005～0．20μg ( r=0．9998 ) , and 0．0052～0．204μg (r=0．9999) ,respectively. Their average recoveries were 96．39 %～97．58% (RSD=2．01～2．59%) .The established method is convenient and accurate with satisfactory separation effect, wide linear range, and high sensitivity, and can be available for the quality control of sini decoction.2,We established a HPLC moethod for glycyrrhetic acid in sini decoction. Kromasil C₁₈ (150 mm×4．6 mm,5μm) was used as chromatographic column, 3．6%acetic acid-methanol (20:80) as mobile phase. The detection wavelength was set at 254nm,the flow rate at 1．0 mL·min^-1 and the column temperature at 30℃. The sample sizes of glycyrrhetic acid had good lineae relationship with their peak areas in the range of 0．01～2．5μg (r=0．9994) . Their average recoveries of classical and ultramicro sini decoction were 97．70% (RSD=2．36%) ,97．1% (RSD=2．50%) ,respectively. The established method is convenient and accurate with satisfactory separation effect, wide linear range, and high sensitivity, and can be available for the quality control of sini decoction.3,The experimental results indicated that the chemical ingredients in ultramicro decoction were higher than in the classical decoction. The reason is those alkaloids are hydrolyzed at high temperature especially and can form undissolved complex with glycyrrhizic acid or glycyrrhetic acid in the process of decoction. The poisonous ingredients were lowered in the process of decoction, and glycyrrhetic acid as well.4,The pharmacodynamics experiment results indicated that both classical and ultramicro sini decoction can significantly increase the cardiac contractile force and cardiac output and HR in normal isolated toad heart (P<0．05) . But there were no obvious difference in them (P> 0．05) . CONCLUSION: 1,We established a HPLC moethod for simultaneous content of mesaconitine,hypaconitine and aconitine in sini decoction. The established method can be available for the quality control of sini decoction. We established a HPLC moethod for glycyrrhetic acid in sini decoction. The established method can be available for the quality control of sini decoction.2,The process of decoction changed the contents of major chemical ingredients. The poisonous ingredients were lowered in the process of decoction and glycyrrhetic acid as well.3,When the classical and ultramicro sini decoction are taked in at the same dosage, their pharmacodynamic actions have no obvious difference.SO the ultramicro sini decoction has no obvious advantages compared with it's classical decoction. If the ultramicro sini decoction is used in normal clinical effective dosage, we should guard it's toxicity.