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Effects of glucose supplementation on the pharmacokinetics of intravenous chlorzoxazone in rats with water deprivation for 72 h

All Rights Reserved. Effects of glucose supplementation on the pharmacokinetics of intravenous chlorzoxazone in rats with water deprivation for 72 h. Kim, Yu Chul; Lee, Inchul; Kim, Sang Geon; Ko, Seong-Hee; Lee, Myung Gull; Kim, So Hee (College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, Seoul, S. Korea). Life Sciences, 79(23), 2179-2186 (English) 2006 Elsevier B.V. CODEN: LIFSAK. ISSN: 0024-3205. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 7, 18 It was reported that in rats with water deprivation for 72 h with food (dehydration rat model), the expression of CYP2E1 was 3-fold induced with an increase in mRNA level and glucose supplementation instead of food during 72-h water deprivation (dehydration rat model with glucose supplementation) inhibited the CYP2E1 induction in dehydration rat model. It was also reported that chlorzoxazone (CZX) is metabolized to 6-hydroxychlorzoxazone (OH-CZX) mainly via CYP2E1 in rats. Hence, the effects of glucose supplementation on the pharmacokinetics of CZX and OH-CZX were investigated after i.v. administration of CZX at a dose of 25 mg/kg to control male Sprague-Dawley rats and dehydration rat model and dehydration rat model with glucose supplementation. Based on the above mentioned results of CYP2E1, it could be expected that increased formation of OH-CZX in dehydration rat model could decrease in dehydration rat model with glucose supplementation. This was proven by the following results.Several reagents with their cas registry numbers 1750-45-4 and 50-99-7 are used here. In dehydration rat model with glucose supplementation, the AUC of OH-CZX was significantly smaller (1900 vs. 1050 mg min/mL), AUCOH-CZX/AUCCZX ratio was considerably smaller (105 vs. 34.3%), Cmax was significantly lower (20.6 vs. 8.08 mg/mL), total amt. excreted in 24-h urine as unchanged OH-CZX was significantly smaller (62.3 vs. 42.7% of i.v. dose of CZX), and in vitro Vmax (2.18 vs. 1.20 nmol/min/mg protein) and CLint (0.0285 vs. 0.0171 mL/min/mg protein) were significantly slower than those in dehydration rat model. .