40435-27-6Relevant academic research and scientific papers
Enhancement of the hypnotic potency of barbiturates by inclusion complexation with β-cyclodextrin
Koizumi,Miki,Kubota
, p. 319 - 322 (1980)
The 50% effective doses of five barbiturate-β-cyclodextrin complexes on oral administration to mice were compared with those of the corresponding barbiturates. In all cases tested, the complex gave a smaller ED50 than the intact drug. ED50 of phenobarbital, which forms the most stable complex and consequently shows the greatest enhancement in solubility, was reduced most markedly by complexation. With the exception of barbitural, sleeping lag (the time from oral administration to loss of righting reflex) on administration of the complex to mice was shorter than that on giving an equimolar amount of the intact drug (p 0.001), and sleeping time the time from loss to recovery of righting reflex) was significantly increased by inclusion complexation with β-cyclodextrin.
Quantitative structure-stability relationships among inclusion complexes of cyclodextrins I: Barbituric acid derivatives
Lopata,Darvas,Stadler-Szoke,Szejtli
, p. 211 - 213 (2007/10/02)
Quantitative structure-stability relationships (QSSRs) are formulated for the inclusion complexation of 17 barbituric acid derivatives with α- and β-cyclodextrin. The variation in the complex stability constants K(α) and K(β) is found to be partly accounted for by the molar refractivity or the hydrophobicity of the substituent R1 at position 5 of the barbiturate ring. In addition K(α) also depends upon whether or not R1 is branching or cyclic, and K(β) also depends upon whether the guest molecule is a barbiturate or a thiobarbiturate. The results suggest that in α-cyclodextrin-barbiturate complexes the cyclodextrin cavity includes only R1, while in β-cyclodextrin complexes both R1 and (part of) the barbiturate ring are included. This complexation model is compared with those proposed by other authors.
