The pharmacokinetics of glycyrrhizin and its restorative effect on hepatic function in patients with chronic hepatitis and in chronically carbon-tetrachloride-intoxicated rats

✍ Scribed by Yoshikazu Yamamura; Hajime Kotaki; Naomi Tanaka; Tatsuya Aikawa; Yasufumi Sawada; Tatsuji Iga

• Publisher: John Wiley and Sons
• Year: 1997
• Tongue: English
• Weight: 318 KB
• Volume: 18
• Category: Article
• ISSN: 0142-2782
• DOI: 10.1002/(sici)1099-081x(199711)18:8<717::aid-bdd54>3.0.co;2-u

✦ Synopsis

The relationships between the pharmacokinetic behaviour of glycyrrhizin and its restorative eect for hepatic function were investigated in patients with chronic hepatitis and in rats chronically treated with carbon tetrachloride (CCl 4 -treated rats). In patients, the restorative eects in plasma aspartate aminotransferase (AST) and alanine aminotransferase (ALT) activities were 62´2+7´4 and 64´4+7´5%, respectively, after daily 80 mg intravenous (i.v.) doses of glycyrrhizin for 2 weeks, and 63´1+19´1 and 68´7+15´2% after 120 mg doses. The present work suggests that the threshold plasma glycyrrhizin concentration for sucient eect is near 5 mg mL 71 . In rats, the total body clearance (Cl tot ) for glycyrrhizin in the CCl 4 -treated rats after i.v. administration of glycyrrhizin (5 mg kg 71 dose) was three-tenths of that of the control, and the t 1/2 for glycyrrhizin was 3´4-fold longer than that of the control. A good correlation was observed between Cl tot and AST (r À0´838) or ALT (r À0´873) activity in both rats. When glycyrrhizin was administered intraperitoneally (i.p.) three times a week for 2 weeks, both the AST and ALT activities in the CCl 4 -treated rats showed a greater improvement than for a 10 mg kg 71 dose. Furthermore, the ®nding on the threshold plasma concentration in patients as above was also supported from the results of the experiments in rats.