Detail of "31637-97-5"

Reference

Disposition of etofibrate, clofibric and nicotinic acid esters, and their products in dogs

Disposition of etofibrate, clofibric and nicotinic acid esters, and their products in dogs. Garrett, Edward R.; Altmayer, Paul (Coll. Pharm., Univ. Florida, Gainesville, FL 32610, USA). J. Pharm. Sci., 74(3), 295-9 (English) 1985. CODEN: JPMSAE. ISSN: 0022-3549. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Etofibrate (I) [31637-97-5], the ethylene glycol diester of clofibric and nicotinic acids, after i.v. infusion into dogs, has a terminal half-life of 2 min. The intermediate half-esters, the nicotinate half-ester [3612-80-4] and the clofibrate half-ester [31637-96-4] have, resp., terminal half-lives of 4.6 and 1.7 min and appear fleetingly when etofibrate is administered. In contrast to the 42-h terminal half-life of clofibric acid [882-09-7], the other final transformation product, nicotinic acid [59-67-6], shows saturable or dose-dependent pharmacokinetics in dogs that conform to the Michaelis-Menten equation with a terminal half-life of 4.4 min at low concns. (<6.9 mM/kg). Three distinct metabolites of nicotinic acid can be identified and assayed chromatog. in the urine. The partition properties were similar to those of nicotinic acid. Nicotinic acid is excreted 30% unchanged into urine, with a renal clearance of 70 mL/min in 27-kg dogs.

Plasmolysis, red blood cell partitioning, and plasma protein binding of etofibrate, clofibrate, and their degradation products

Plasmolysis, red blood cell partitioning, and plasma protein binding of etofibrate, clofibrate, and their degradation products. Altmayer, Paul; Garrett, Edward R. (J. Hillis Miller Health Cent., Univ. Florida, Gainesville, FL 32610, USA). J. Pharm. Sci., 72(11), 1309-18 (English) 1983. CODEN: JPMSAE. ISSN: 0022-3549. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Etofibrate (I) [31637-97-5] the ethylene glycol diester of clofibric acid [882-09-7] and nicotinic acid [59-67-6], degrades almost equally through both half-esters with half-lives of ~10 and 1 min in fresh dog and human plasma, resp. 2-Hydroxyethyl nicotinate [3612-80-4] degrades with half-lives of ~12 h and 50 min in fresh dog and human plasma, resp. 2-Hydroxyethyl 2-(4-chlorophenoxy)-2-methylpropionate [31637-96-4] and clofibrate [637-07-0] degrade by saturable Michaelis-Menten kinetics in fresh human plasma, with similar max. initial rates and resp. terminal 1st-order half-lives of 12 and 26 min. Tetra-Et pyrophosphate at 100 mg/mL inhibited human plasma and red blood cell esterases, permitting plasma protein binding and red blood cell partitioning studies. The red blood cell-plasma water partition coeff. was 5. 637-07-0 and 59-67-6 are cas registry numbers of chemicals which are used as reagents here.4 for 0.2-80 mg/mL of I. Clofibrate showed a saturable erythrocyte partitioning that decreased from 7.8 (10 mg/mL) to 1 (50 mg/mL). The strong binding of I and clofibrate to ultrafiltration membranes necessitated the detn. of their plasma protein binding by the method of variable plasma concns. of erythrocyte suspensions, to give 96.6% and 98.2% binding, resp. Methods for the detn. of the parameters of saturable and nonsaturable plasma protein binding for unstable and membrane-binding drugs by the method of variable plasma concns. in partitioning erythrocyte suspensions are presented. .