Preparation and in vitro/in vivo evaluation of nano-sized crystals for dissolution rate enhancement of ucb-35440-3, a highly dosed poorly water-soluble weak base.

Ucb-35440-3 is a new drug entity under investigation at UCB S.A. Due to its physicochemical characteristics, the drug, a poorly water-soluble weak base, shows poor solubility and dissolution characteristics.

Preparation and characterization of nanocrystals for solubility and dissolution rate enhancement of nifedipine.

Poorly water-soluble drugs such as nifedipine (NIF) (approximately 20 microg/ml) offer challenging problems in drug formulation as poor solubility is generally associated to poor dissolution characteristics and thus to poor oral bioavailability. In order to enhance these characteristics, preparation of nifedipine nanoparticles has been achieved using high pressure homogenization. The homogenization procedure has first been optimized in regard to particle size and size distribution.

Correlation of extrusion forces, raw materials and sphere characteristics.

This communication reports on the correlation between extrusion forces and sphere characteristics. Dicalcium phosphate dihydrate, alpha-lactose monohydrate and anhydrous beta-lactose were models for respectively an insoluble, a medium soluble and a highly soluble drug and were used to produce spheres. Phase diagrams for ternary mixtures consisting of microcrystalline cellulose, water and a third excipient were constructed.

Instrumentation of a gravity feed extruder and the influence of the composition of binary and ternary mixtures on the extrusion forces.

A gravity feed extruder was adapted to monitor the extrusion forces, the temperature during processing and the rotational speed of the extruding cylinders. The extruder was used to evaluate the influence of particle size of insoluble material and of product solubility on the extrusion forces. Microcrystalline cellulose, dicalcium phosphate dihydrate and different lactoses were used as model compounds.

Comparison of techniques for detection of domestic infestations with Triatoma infestans in Brazil.

The detection of infestations of Triatominae in houses in regions endemic for Chagas's disease is a criterion frequently used in the selection of areas, or of individual houses, for treatment in insecticide campaigns as well as in the evaluation of insecticide performance. Several different methods for detecting domestic infestations with Triatominae were compared: night capture, capture of five bugs with the aid of a flushing-out agent and use of card boxes of the Gómez-Núñez type. The flushing-out and Gómez-Núñez box methods were found to be equally sensitive, although each failed to detect some infestations which the other detected.