Detail of "77-30-5"

Reference

Prediction of in Vivo Tissue Distribution from in Vitro Data

Some chemicals with cas registry numbers like 27653-63-0 and 77-30-5 are also used. Prediction of in Vivo Tissue Distribution from in Vitro Data. 2. Correlation Between in Vitro and in Vivo Tissue Distribution of a Homologous Series of Nine 5-n-Alkyl-5-Ethyl Barbituric Acids. Ballard, Peter; Leahy, David E.; Rowland, Malcolm (Discovery-DMPK, AstraZeneca, Cheshire SK10 4TG, UK). Pharmaceutical Research, 20(6), 864-872 (English) 2003 Kluwer Academic/Plenum Publishers. CODEN: PHREEB. ISSN: 0724-8741. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) To evaluate the ability to det. accurate in vivo tissue-to-unbound plasma distribution coeffs. (Kpue) from in vitro data. Fresh pieces of fifteen rat tissues/organs were incubated at 37°C with a homologous series of nine barbiturates covering a wide range of lipophilicity (Log P 0.02 to 4.13). Steady-state in vivo Kpue values were estd. from the tissue and plasma concns. following simultaneous dosing by const. rate i.v. infusion of all nine barbiturates. Drug concns. in the tissues and media were detd. by HPLC with UV or mass spectrometric detection. The pharmacokinetics of the barbiturate series following const. rate i.v. infusion indicated a range of clearance (0.49 to 30 mL.min-1.kg-1) and vol. of distribution at steady state (0.51 to 1.9 l.kg-1) values. Good agreement was obsd. between the in vitro and in vivo Kpu values, although for the most lipophilic barbiturates the in vitro data underpredicted the in vivo tissue distribution for all tissues. The in vitro system for predicting the extent of in vivo tissue distribution works well for compds. of widely differing lipophilicity, although for the most lipophilic drugs it may result in an underprediction of in vivo values. .