Hoffmann-la Roche Inc.

F. Hoffmann-la Roche Ag

Weidmann Plastics Technology Ag

Pion Inc.

Manfred Kansy

Thomas Zumstein

Holger Fischer

Tilo Callenbach

Alex Avdeef

Karl Mazenauer

Heinrich Büttgen

Hansjörg Tschirky

Bjoern Wagner

Lei Du-Cuny

Jörg Huwyler

Werner Schneider

The invention deals with a method for the assessment of the effect of excipients, pH and combinations thereof on the predicted absorption properties of low solubility compounds, comprising the step of assessing a change in a flux function for a combination of a low solubility compound and an excipient at at least one predefined pH value. The method allows a fast, accurate, and economic evaluation of an excipient being capable of optimizing the absorption of drug molecules, i.e. low solubility compounds. Furthermore, animal experiments can be excluded and use of compounds can be reduced in such evaluation. Thus, screening for future formulation efficacy (pH and excipient effects on solubility and permeability) of drug candidates can be justified, since the method is fast, compound-sparing, cost-effective, and reasonably accurate.

Method for assessing absorption properties of low solubility compounds

The present invention relates to automated generation of multi-dimensional structure activity and structure property relationships.

Automated generation of multi-dimensional structure activity and structure property relationships

The present invention relates to a novel method for determining the lipophilicity of a compound of interest comprising a) providing a layer, b) impregnating said layer with a solvent A, c) applying a dissolved compound of interest on the impregnated layer, d) adding a solvent B, e) removing the solvent B after the distribution equilibrium has been reached, and f) determining the quantity of the compound of interest in at least one of the solvent phases.

Determination of high lipophilicity values

A method for crystallization of a weakly acidic and/or weakly basic compound having an uncharged form and at least one charged form comprises the steps of:

Method for crystallization of a weakly acidic and/or weakly basic compound

An integrally built, linear array of cuvettes is made of a plastic material. Every cuvette of the array has the same shape and dimensions. Neighboring cuvettes are connected to each other by a single web. Each of the single webs has a curved shape and each cuvette has means forming integral part thereof and serving for accurately positioning the cuvette into an opening of a cuvette holder and means for removably connecting the cuvette to the cuvette holder. Each cuvette has an upper chamber and a lower chamber having a common symmetry axis passing through the centers of both chambers. Each of the upper and lower chambers has a substantially cylindrical shape. The cross-section of the upper chamber at the central part thereof is larger than the cross-section of the lower chamber. The lower chamber has an open lower end. The upper chamber has an open top end and an annular bottom wall having a central circular opening which connects the upper chamber with the lower chamber. The inner surface of the bottom wall of the upper chamber () is part of a conical surface the cross-section of which forms an angle of about 80 degrees with the symmetry axis, so that there is an abrupt change of cross-section between the upper chamber and the lower chamber. A two-dimensional array of cuvettes comprises a plurality of linear cuvette arrays inserted into a cuvette holder having a matrix array of cuvette receiving openings. A system of two-dimensional cuvette arrays is built by stacking two or more of such two-dimensional arrays of cuvettes. Foil shaped layers serving, e.g. as a filter, are adapted to be attached to each cuvette to cover at least one opening thereof.

Cuvette arrays

Growing community of inventors

Freiburg, Germany

Manfred Kansy