Fluphenazine (CAS 69-23-8) concentrations in plasma of schizophrenic patients after oral (fluphenazine hydrochloride, Moditen) or intramuscular (fluphenazine enanthate, Moditen Retard, or fluphenazine decanoate, Modecate) administration of drug were measured by means of high-performance liquid chromatography. The extracted compound was identified by gas chromatography with mass selective detector. Pharmacokinetics of fluphenazine has been studied.
It has been shown that calcium acetylhomotaurinate (Ca AOTA; Meram Patent, France) decreased voluntary ethanol intake in rats (1); this was antagonized by bicuculline. Homotaurine did not have this effect. We thought this was due to a different blood-brain barrier crossing ability for the two drugs. The present study was, therefore, planned to confirm blood-barrier crossing by Ca AOTA and to study the drug's physicochemical and pharmacokinetic characteristics. Both in vitro and in vivo (i.p.) administration of Ca AOTA increased the accumulation of [3H] GABA in rat striatal synaptosomal preparations. The chemical study confirmed Ca AOTA's great stability in biological and hydrophilic media, excluding a "homotaurine-dispensing" effect. The molecule was totally dissociated in such media, but the absence of any detectable acid form at any pH indicates that ion pairs are formed to cross barriers, and/or that a carrier system is used. The pharmacokinetic study showed short half-lives (5 and 30 min for the distribution and elimination phases) and small distribution volumes. However, the elimination phase distribution volume was dose-dependent, a further argument for a carrier transport system. From the present study it appears that Ca AOTA is an extremely stable drug, totally dissociated in hydrophilic media, which acts centrally as a GABA agonist after crossing the blood-brain barrier. It is not a precursor of homotaurine and presumably crosses barriers with the help of a transporter.
La formation d'un chélate entre les ions cuivriques et la vancomycine, molécule à propriétés antibiotiques sur les bactéries Gram positif, est montrée par des methodes spectrales, polarographiques et potentiométriques. En particulier, les valeurs des potentiels de demi-vague de réduction et l'évolution des courbes intensité-potentiel permettent de mettre en évidence la stoechiométrie du compośe d'addition formé et d'apprécier la stabilité du complexe obtenu. Cette propriété complexante est utilisée pour proposer une methode de dosage en flux continu, en utilisant une phase mobile contenant des ions cuivriques et une détection ampérometrique á l'aide d'une cellule électrochimique de type couche mince.