The invention is related to water-soluble products and pharmaceutical
formulations in solid or liquid form mainly for parenteral use. They
consist of or comprise a therapeutically active substance (having low
aqueous solubility and a substantial binding affinity to plasma proteins)
and a plasma protein fraction in controlled aggregation state, whereby
the said active substance and the said protein fraction are bound to each
other by way of non-covalent bonds. It also covers processes for the
preparation of the product and pharmaceutical formulation by dissolving
the water-insoluble active substance in a water-miscible,
pharmaceutically acceptable solvent, combining said solution with the
aqueous solution of a plasma protein fraction in controlled aggregation
state whereby a true solution is obtained containing the said active
substance and the said protein fraction bound together by way of
non-covalent bonds. Optionally a further pharmaceutically acceptable
auxiliary additive--such as a protein aggregation controller and/or a
stabilizer--may be present. The organic solvent is eliminated by
dialysing, ultrafiltrating, diafiltrating and/or lyophilising. The solid
products consisting of the active substance and the protein are also
protected. On optional dissolution in water clear, liquid compositions
are obtained suitable for direct parenteral or other administration.
Method of treatment is also covered. A series of water-insoluble
substances is enlisted with appropriate protein fractions to be used.