Examination of 19F-NMR as a tool for investigation of drug-cyclodextrin complexes.

Fluorine nuclear magnetic-resonance spectroscopy (19F-NMR) was used to measure complexation of three fluorine-containing drugs--dexamthasone, fluoxetine hydrochloride, and diflunisal sodium--with 2-hydroxypropyl-beta-cyclodextrin (HPbetaCD). Poor aqueous solubility inhibited investigation of dexamethasone complexes with this method. Complexation caused separation of the fluorine peaks that could be assigned to the two enantiomers of fluoxetine hydrochloride.

Self-association and cyclodextrin solubilization of drugs.

Phase-solubility diagrams are frequently used to calculate stoichiometry of drug/cyclodextrin complexes. Linear diagrams (A(L)-type systems) are thought to indicate that the complexes are first order with respect to cyclodextrin and first or higher order with respect to the drug. Positive deviation from linearity (A(P)-type systems) are thought to indicate formation of complexes that are first order with respect to the drug but second or higher order with respect to cyclodextrin.

Intranasal administration of midazolam in a cyclodextrin based formulation: bioavailability and clinical evaluation in humans.

Intranasal administration of midazolam has been of particular interest because of the rapid and reliable onset of action, predictable effects, and avoidance of injections. The available intravenous formulation (Dormicum i.v.

Cyclodextrin solubilization of benzodiazepines: formulation of midazolam nasal spray.

The cyclodextrin solubilization of three benzodiazepines, i.e. alprazolam, midazolam and triazolam, was investigated.

Methazolamide 1% in cyclodextrin solution lowers IOP in human ocular hypertension.

Purpose: To formulate aqueous eye drops containing methazolamide 1% in cyclodextrin solution and to evaluate their effect on intraocular pressure (IOP) in a double-blind randomized trial in humans. Methazolamide, a carbonic anhydrase inhibitor (CAI), has been used in oral doses in the treatment of glaucoma but hitherto has not been successfully formulated in eye drops. In this study the effects of methazolamide are compared with those of dorzolamide (Trusopt).

Influence of cyclodextrins on the stability of the peptide salmon calcitonin in aqueous solution.

The influence of beta-cyclodextrin (betaCD), and various betaCD derivatives, on both the chemical and the physical stability of the polypeptide hormone salmon calcitonin (sCT) in aqueous solutions was investigated at elevated temperature (55 degrees C). Also, the influence of various betaCD derivatives on the enzymatic degradaton of sCT was evaluated. At pH 6, the effect of CDs on the chemical stability of sCT was negligible at CD concentrations below 5% (w/v).