[The effect of changing the association properties of psychopharmaceuticals in colloidal solutions on their liberation. 4. The effect of chemical structure as well as environmental conditions on the elevation of critical micelle formation concentration and reduction of micelle weight with hydrotropic material].
As shown by 8 different tri- and tetracyclic psychiatric drugs the authors demonstrated that the rate of desaggregation is markedly influenced by the chemical structure of drugs. In presence of 0.1 mol/l nicotinamide the cmc increased between 1.3 times for Maprotiline-HCl and 3.5 times for Chlorprothixene-HCl in acetate buffer pH 5.0; I = 0.154. Investigations about influences on the micellar weights showed for Flupenthixol-di HCl, Clomipramine-HCl and Melitracen-HCl decreases of 21.5, 16.1 and 14.0 per cent conferred by addition of 0.3 mol/l nicotinamide. There was a good correlation to the increase of the cmc. Different hydrotropic substances may show great differences of influence on the micellar weights and the cmc respectively. The micellar weight of Flupenthixoldi HCl for example reduces for about 17 per cent by concentrations of 0.2 mol/l nicotinamide or 1 mol/l propandiol-1.2, but the cmc increases to the 3.6- and 1.4fold value.
Thoma
K
K
Institut für Pharmazie und Lebensmittelchemie, Ludwig-Maximilians-Universität München.
von Stein
C
C
D002626:Chemistry, Pharmaceutical; D005079:Excipients; D008823:Micelles; D008970:Molecular Weight; D011619:Psychotropic Drugs / Q000032:analysis*
D005079:Excipients; D008823:Micelles; D011619:Psychotropic Drugs
Freisetzungsbeeinflussung von Psychopharmaka in kolloidalen Lösungen durch Veränderung ihrer Assoziationseigenschaften. 4. Mitteilung: Einflüsse der chemischen Struktur sowie der Milieubedingungen auf die Erhöhung der kritischen Mizellbildungskonzentration und die Verminderung des Mizellgewichtes durch hydrotrope Stoffe.