Permeability of porcine nasal mucosa correlated with human nasal absorption.

The Ussing chamber diffusion system was used as a model to study the apparent permeability across porcine nasal mucosa of eight drugs and molecules with different physicochemical characteristics, namely insulin, lidocaine, nicotine, PEG 4000, propranolol, sumatriptan, melagatran and an amino diether. A weak correlation was found between the apparent permeability coefficients and the corresponding literature data on the fraction absorbed after nasal administration in humans. In the case of passively transported drugs, a closer correlation was found than for the substances where other mechanisms such as carrier-mediated transport or possible efflux were involved.

Drug-fatty acid salt with wax-like properties employed as binder in melt granulation.

The tacky and deformable properties of a wax-like drug-fatty acid salt, propranolol oleate (POA), make particle size reduction and separation challenging. The aim of this study was to investigate the use of POA as binder in a melt granulation procedure to improve processing properties. POA is a suitable candidate for binder phase in melt granulation with a melting temperature of 50-56 degrees C.

Characterization of oleic acid and propranolol oleate mesomorphism using (13)C solid-state nuclear magnetic resonance spectroscopy (SSNMR).

Lipids regularly exhibit complicated thermotropic and lyotropic phase behavior. In this study, the utility of (13)C solid-state nuclear magnetic resonance spectroscopy (SSNMR) in characterizing the phase properties of pharmaceutical lipids was investigated. Variable temperature (13)C SSNMR spectra and spin-lattice relaxation times (T(1)(C)) were obtained for high-purity oleic acid (OA) and propranolol oleate (POA).

Characterisation of instantaneous water absorption properties of pharmaceutical excipients.

Powders absorb water by both capillary imbibition and swelling. The capillary process is almost instantaneous but swelling occurs over a period of time. An isothermal transient ionic current technique was used in this study to characterise the instantaneous absorption properties (rate and capacity) of a few selected pharmaceutical excipients.

Hydroxypropyl-beta-cyclodextrin inhibits spray-drying-induced inactivation of beta-galactosidase.

The single-step, fast spray-drying process may represent a valuable alternative to the multistep, time-consuming freeze-drying process in the area of formulation and processing of biopharmaceuticals. In this study, we tested the use of sucrose and hydroxypropyl-beta-cyclodextrin (HP-beta-CD) as stabilizing excipients in the spray-drying of a model protein, beta-galactosidase. The solutions were processed using a Büchi 190 cocurrent Mini Spray Dryer at an outlet temperature of 61 +/- 2 degrees C.