Superparamagnetic particles, process for their manufacture and u

Chemistry: analytical and immunological testing – Involving an insoluble carrier for immobilizing immunochemicals – Carrier is inorganic

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424 9323, 424 934, 424 935, 5303911, G01N 33553, A61K 916, C07K 1714

Patent

active

059289589

DESCRIPTION:

BRIEF SUMMARY
The present invention relates to superparamagnetic particles consisting of superparamagnetic one-domain particles and aggregates of superparamagnetic one-domain particles of iron oxides, mixed iron oxides or iron to whose surfaces are bound organic substances which optionally may have further binding sites for coupling tissue-specific binding substances, diagnostic substances or pharmacologically active substances.
Patent EP-B-0284549 describes superparamagnetic one-domain particles of iron oxide, mixed iron oxide or iron with a particle size ranging from 3 to 20 nanometers, to whose surfaces are chemically bound organic substances of the group of phosphate, diphosphate, polyphosphate, thiophosphate, phosphonate or thiophosphonate group-containing polyalkylene glycols, phosphate group-containing nucleotides, their oligomers or their polymers as well as phosphate group-containing carbohydrates, which may have further binding sites.
Patent DE-A-4309333 describes stable, degradable aggregates with a particle size ranging from between 10 and 1000 nanometers with defined behaviour in a magnetic field whereby the aggregates consist of several small superparamagnetic one-domain particles of iron oxide, mixed iron oxide or iron with a particle size ranging from 3 to 20 nanometers to whose surfaces are chemically bound substances of the group of phosphate, diphosphate, polyphosphate, thiophosphate, phosphonate or thiophosphonate group-containing polyalkylene glycols, carbohydrates or of the phosphate group-containing nucleotides, their oligomers or their polymers.
The object of the invention is to enlarge the range of substances which can be bound to the surfaces of the one-domain particles, in order to optimally adapt the physicochemical and physiological properties of the magnetic particles being formed to the respective fields of application whereby these substances should be stable and easy to manufacture.
A surprising finding was that mono- and polyhydroxylic group-containing aromatic substances, polyglycerin and their phosphate, diphosphate, polyphosphate, thiophosphate, phosphonate, thiophosphonate, carboxylate, sulphate, mercapto or silantriol group-containing derivatives, amino acid containing oligopeptides, polypeptides, proteins, proteids as well as their derivatives and denaturation products, mercapto and amino group-containing substances such as biotin, mercaptopurine, -cytosin, -guanine, -uracil, -thymine, -hypoxanthine, as well as their mercaptonucleosides and mercapto-desoxynucleosides, ortho-silicic acid and their condensation products with bivalent and polyvalent inorganic ions and/or organic acids and bases and ortho- or metaphosphoric acid and their condensation products enter stable bindings with the surface of the superparamagnetic particles leading to stable magnetic liquids and aggregation-stable, superparamagnetic aggregates.
According to the invention, stabilisation of the magnetic particles takes place by binding mono- and polyhydroxylic group-containing aromatic substances such as for example benzenoids, coumarins, lignans, terphenyls, flavonoids, tannins, xanthenes, benzophenones, naphthalenes, naphthoquinones, anthraquinones, anthracyclines, polycyclic condensated aromatic compounds and their phosphate, diphosphate, polyphosphate, thiophosphate, phosphonate, thiophosphonate, carboxylate, sulphate, mercapto or silantriol group-containing derivatives, of polyhydroxylic group-containing substances, selected from among polyglycerins and their phosphate, diphosphate, polyphosphate, thiophosphate, phosphonate, thiophosphonate, carboxylate, sulphate, mercapto or silantriol group-containing derivatives, of amino acid containing substances such as for example oligopeptides, polypeptides, proteins, proteids as well as their derivatives and denaturation products, of mercapto- and amino group-containing substances such as for example biotin, mercaptopurine, -cytosin, -guanine, -uracil, -thymine, -hypoxanthine, as well as their mercapto-nucleosides and mercapto-desoxynucleosides, of silicate group-

REFERENCES:
WPI Abstract of Japanese patent JP 1,315,494, Dec. 1989.

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