Design and pharmacodynamic evaluation of novel dual release formulations of triazolam.

Triazolam is an effective hypnotic that can cause amnesia and psychomotor performance decrements, particularly after a 0.5 mg dose. Previous pharmacodynamic studies suggested a relationship between these effects and triazolam plasma concentration.

Stoichiometric model of alpha-cyclodextrin complex formation.

The solubility, spectral, and kinetic methods were used to study complexing between alpha-cyclodextrin (ligand, L) and 3,5-dimethoxycinnamic acid, benzalacetone, and methyl cinnamate (substrates, S). In aqueous solution at 25 degrees and with an ionic strength of 0.01 M, the following stability constants were found (K11 for SL and K12 for SL2): 3,5-dimethoxycinnamic acid, K11=1965 M-1 and K12=0; benzalacetone, K11=105 M-1 and K12=15 M-1; and methyl cinnamate, K11=1200 M-1 and K12=50 M-1.

trans-Cinnamic acid--alpha-cyclodextrin system as studied by solubility, spectral, and potentiometric techniques.

Complex formation in aqueous solutions of trans-cinnamic acid or trans-cinnamate ion (the substrate, S) and alpha-cyclodextrin (the ligand, L) can be described quantiatively as the 1:1 and 1:2 complexes, SL and SL2. The solubility, spectral, and potentiometric data over a wide range of ligand concentrations yielded consistent estimates of the complex association constants. For cinnamic acid at 25 degrees K11 = 2260 M-1, delta H degree 11 = 9.