Detail of "66695-14-5"

Reference

Therapeutic concentration of coumarin and predicted dosage regimens

Therapeutic concentration of coumarin and predicted dosage regimens. Ritschel, W. A. (Med. Cent., Univ. Cincinnati, Cincinnati, OH 45267, USA). Arzneim.-Forsch., 34(8), 907-10 (English) 1984. CODEN: ARZNAD. ISSN: 0004-4172. DOCUMENT TYPE: Journal CA Section: 63 (Pharmaceuticals) Section cross-reference(s): 1 The plasma concn. of coumarin (I) [91-64-5] was detd. in patients at the time clin. effectiveness was obsd. in episiotomy patients. A dosage regimen of 2 controlled-release tablets, Venalot (15 mg I/tablet) at 7.00, 13.00, and 19.00 h was used. I concns. at the end of the 7.00 h dose was 0.011 mg/mL and 0.036 mg/mL 0.5 h after the following dose. Large interindividual variations were obsd. for the I concns. An analog computer fit was performed for multiple dosing using the trough I concn. at the end after the 7.00 h dose on day 3 and the 0.5 h concn. after the 13.00 h dose. The mean I concn. was 0.02 mg/mL. The ratios of the metabolites, 7-hydroxycoumarin [93-35-6] to 7-hydroxycoumarin glucuronide [66695-14-5], at the end of 7.00 h-dose were 7.4 and 0.09, resp., and 14.8 and 0.17, resp., at the end of 13.00-h dose.

Dynamics of xenobiotic metabolism by isolated rat hepatocytes using a multichannel perifusion system

Dynamics of xenobiotic metabolism by isolated rat hepatocytes using a multichannel perifusion system. Orton, T. C.; Sorman, A. E.; Crisp, D. N.; Sturdee, A. P. (Pharm. Div., Imp. Chem. Ind. PLC, Macclesfield SK10 4TG, UK). Xenobiotica, 13(12), 743-53 (English) 1983. CODEN: XENOBH. ISSN: 0049-8254. DOCUMENT TYPE: Journal CA Section: 4 (Toxicology) The multichannel perifusion system in recirculating and nonrecirculating (single-pass) mode was used to monitor the rate of oxidative metab. of 3 model substrates-7-ethoxycoumarin [31005-02-4], dichloronitroanisole [99-30-9], and aldrin (I) [309-00-2]. With control hepatocytes, the rate of deethylation of 7-ethoxycoumarin derived from recirculating mode was essentially similar to the rate obtained with conventional flask-incubated cell suspensions. The formation of 7-hydroxycoumarin glucuronide [66695-14-5] and sulfate [69526-88-1] by hepatocytes exposed to 7-ethoxycoumarin demonstrated the retention of conjugative ability of cells in the perifusion system. The rate of demethylation of dichloronitroanisole to dichloronitrophenol [26761-59-1] was low, while I epoxidn. to dieldrin [60-57-1] was rapid using control hepatocytes in recirculating mode. The inductive effect of phenobarbitone on hepatic mixed-function oxidases was demonstrated by a marked increase in the rate of 7-ethoxycoumarin (9-fold) and dichloronitroanisole (64-fold) dealkylation by hepatocytes from phenobarbitone-treated animals in recirculating mode. The rate of substrate oxidn. by hepatocytes perfused in the recirculating and the single-pass mode were the same. With dichloronitroanisole as substrate and a single-pass mode, the rate of dichloronitrophenol formation declined rapidly on perifusion with substrate-free medium and rapidly reattained steady state on reintroduction of the substrate; the presence of metyrapone effectively inhibited dichloronitroanisole metab. The perifusion system is recommended to study the dynamics of xenobiotic metab. by isolated mammalian hepatocytes.