Qu S Y, Li W, Chen Y L, Sun Y, Zhang Y Q, Hong T
Academy of Traditional Chinese Medicine, Changchun.
Yao Xue Xue Bao. 1990;25(9):664-9.
Guaiacol acetylsalicylate (GASL) has been shown to possess significant anti-inflammatory, antipyretic and expectorant activities and has been used clinically in chronic bronchitis with fairly good results. In the present work, the absorption, distribution and excretion of metabolites of the drug were studied in rats using quantitative TLC scanning technique. GASL was shown to be unstable in rat gastrointestinal tract and guaiacol salicylate (GSLT) and salicylic acid (SLA) were found in plasma. The plasma SLA concentration-time curve obtained after oral administration of GASL to rats was shown to fit a one compartment open model with the following pharmacokinetic parameters: T1/2ka = 1.25 h, T1/2ke = 3.28 h, ka = 0.5554/h, ke = 0.2111/h, Tmax = 3.02 h, Cmax = 331.46 micrograms/ml, AUC = 2832.93 micrograms/ml.h The SLA concentration was found to be high in muscle, moderate in spleen, testicle, kidney, lung, plasma, heart and liver and low in brain. The GSLT concentration was found to be low in plasma and organs. Within 24 h following ig administration of GASL the total SLA excreted in urine and feces was 10.9 and 0.41 of the GASL dose, respectively.
愈创木酚乙酰水杨酸酯(GASL)已被证明具有显著的抗炎、解热和祛痰活性,并已在慢性支气管炎的临床治疗中应用,效果相当不错。在本研究中,采用定量薄层色谱扫描技术研究了该药物代谢产物在大鼠体内的吸收、分布和排泄情况。结果表明,GASL在大鼠胃肠道中不稳定,血浆中可检测到愈创木酚水杨酸酯(GSLT)和水杨酸(SLA)。给大鼠口服GASL后获得的血浆SLA浓度-时间曲线符合一室开放模型,其药代动力学参数如下:T1/2ka = 1.25小时,T1/2ke = 3.28小时,ka = 0.5554/小时,ke = 0.2111/小时,Tmax = 3.02小时,Cmax = 331.46微克/毫升,AUC = 2832.93微克/毫升·小时。发现SLA在肌肉中的浓度较高,在脾脏、睾丸、肾脏、肺、血浆、心脏和肝脏中的浓度中等,而在脑中的浓度较低。GSLT在血浆和各器官中的浓度较低。给大鼠灌胃GASL后24小时内,尿液和粪便中排泄的总SLA分别为GASL剂量的10.9%和0.41%。