Other

N. V. Sopar S.a.

Debiopharm S.a.

Dr. Rentschler Arzneimittel Gmbh & Co.

Pharmaceutical Society of Victoria

Peter P Speiser

Rajendra Kumar Joshi

Michel Roland

Patrick Couvreur

Jorg Kreuter

Piero Orsolini

Frederic Heimgartner

Richard Charles Oppenheim

Jennifer Joy Marty

Urs Schleuniger

M Orhan Vaizoglu

Gerd Birrenbach

Fumaric acid derivatives of the formula ##STR1## wherein R.sub.1 is a hydrogen atom, a C.sub.1 -C.sub.8 alkyl group or a metallic cation, and R.sub.2 is a saturated or unsaturated aliphatic C.sub.6 -C.sub.24 alkyl group, psoralen-9-yl, retinyl, .alpha.-tocopheryl (vitamin E), calciferyl, corticosteroid-21-yl or monosaccharid-.omega.-yl; a group of fumaric acid derivatives based on glycerol, alkane diol or polyol molecules; and fumaric acid derivatives of the formula ##STR2## wherein n is an integer from to 30 to 260,

Fumaric acid derivatives, process for the production thereof and

A pharmaceutical composition in dosage form for treating psoriasis and psoriatic arthritis includes, essentailly, as active substance (s), a fumaric acid monoalkylester salt having the formula ##STR1## wherein R is a methyl, propyl or isopropyl group, and M.sup.++ is calcium, alone or in combination with at least one of the fumaric acid alkyl ester salts as defined above, M.sup.++ is selected from the group consisting of magnesium, zinc and iron. The combination includes, by weight, 10-250 parts, 0-50 parts magnesium, and 0-50 parts zinc or iron salt of fumaric acid monoalkylester, in an amount of fumaric acid not exceeding 300 mg. per dosage form, in combination with ordinary pharmaceutically compatible solid adjuvants and vehicles.

Pharmaceutical composition and process for the production thereof

The pharmaceutical composition is intended in particular for the sustained and controlled release of an effective dose of a medicinal substance. It comprises, as a carrier for the medicinal substance, a biodegradable polymer or copolymer or a mixture of biodegradable polymers and/or copolymers derived from a dicarboxylic acid selected from the acids of the Krebs cycle, and from an aliphatic diol containing 4 carbon atoms or from cyclohexane-1,4-dimethanol.

Polyester-based composition for the controlled release of polypeptide

Fumaric acid derivatives of the formula ##STR1## wherein R.sub.1 is a hydrogen atom, a C.sub.1 -C.sub.8 alkyl group or a metallic cation, and

A composition including at least one salt of fumaric acid monoalkyl ester having the formula: ##STR1## alone or in combination with dialkyl fumarate having the formula: ##STR2## is provided for treatment of psoriasis and psoriatic arthritis. In particular, use of the calcium salt of fumaric acid monoalkyl ester in the composition is desirable.

Pharmaceutical preparation for the treatment of psoriatic arthritis

Process for the preparation of submicroscopic particles formed of a polymerized alkyl cyanoacrylate and containing a biologically active substance. At least one alkyl cyanoacrylate, in which the term 'alkyl' denotes an alkyl radical having 1 to 12 carbon atoms, is added, with stirring, to pure water or to an aqueous solution or aqueous colloidal solution of an acid and/or of another water-soluble substance, and the stirring is continued until substantially all the alkyl cyanoacrylate has been converted to submicroscopic particles formed of polyalkyl cyanoacrylate; a biologically active substance is introduced into the reaction medium before the introduction of the monomer or after formation of the submicroscopic particles. The submicroscopic particles are useful as carriers for substances such as medical substances or products for diagnosis.

Preparation of submicroscopic particles, particles thus obtained and

An excipient system containing a drug for peroral administration in the form of an ultrafine aqueous, colloidal suspension of lipid nano-pellets comprised of lipids and a surfactant of which the particle diameters of the nano-pellets range from 50-1,000 nm, preferably from 80-800 nm, the ratio of lipid to surfactant in the lipid nano-pellets ranging from 1:0.1 to 1:2.2, preferably from 1:0.22 to 1:1.2, especially from 1:1 to 1:0.22, and where the lipid nano-pellets are present in the suspension in a concentration of from 1-20% by weight. The lipid nano-pellets can be provided with pharmacologically active substances, making possible improved biological availability upon peroral administration.

Lipid nano-pellets as excipient system for perorally administered drugs

The present invention concerns a pharmacological vehicle or carrier system, which makes possible administration of the active ingredient with a high absorption thereof in the blood circulation of the patient treated therewith, in particular also in the case of oral administration. The pharmacological vehicle system according to the invention comprises ultrafine particles of a reaction product of a reactive derivative of an at least dibasic inorganic acid or an alkane-carboxylic acid having 2 or 3 carboxyl groups and optionally one or two hydroxy groups, wherein one bond of the dibasic inorganic acid or one carboxy group of the alkane-carboxylic acid is bonded to a pharmacological active ingredient containing a hydroxy group, SH group and/or a primary or secondary amino group having a ractive hydrogen atom on this group, and the other bond is bonded to the free hydroxy group of a glycerolipid having at least one free hydroxy group on the glycerol. The invention further concerns these reaction products and a process for the preparation of ultrafine particles of these reaction products.

Pharmaceutical formula

Biodegradable particles, with a diameter smaller than 500 nanometers, formed by the micellar polymerization of an alkyl-cyano-acrylate where the term 'alkyl' means a lower alkyl radical having 1 to 4 carbon atoms and containing a biologically active substance. Also provided are processes for making pharmaceutical compositions containing the biodegradable particles and using the particles in pharmaceutical and diagnostic applications.

Process for preparing biodegradable submicroscopic particles containing

Biodegradable particles, with a diameter smaller than 500 nanometers, formed by the micellar polymerization of an alkyl-cyano-acrylate where the term 'alkyl' means a lower alkyl radical having 1 to 4 carbon atoms and containing a biologically active substance.

Biodegradable submicroscopic particles containing a biologically active

There are described processes for the preparation of submicroscopic particles of physiologically acceptable polymer associated with a biologically active material, by polymerizing a monomer in the presence of the biologically active material or by adsorbing the biologically active material upon preformed submicroscopic polymer particles. Where the biologically active material is an antigen, the particles are useful as constituents of injectable vaccines having an adjuvant effect.

Biological materials

Particles in the size range from about 10 to about 1000 nm, preferably less than about 500 nm, which comprise a crosslinked matrix of macromolecules of natural origin. A biologically or pharmacodynamically active material may be supported on or incorporated into the matrix.

Injectable compositions, nanoparticles useful therein, and process of

The present invention is concerned with novel synthetic capsules which are colloid soluble in water or suspendible or colloid soluble in hydrophobic media and consist of compatible polymeric material, more especially of acrylamide and N,N'-methylene-bis-acrylamide gel or of acrylic acid and acrylic acid methyl ester gel, which are submicroscopic and mainly micellar in size, and which contain biologically or pharmacodynamically active material, more especially proteins, antigens, pharmacologically or therapeutically active substances or pesticides, fertilizers, dyes, color forming agents, adhesives and catalysts or other technically active substances in an incorporated and/or adsorbed form, together with the method for their production and their application.

Growing community of inventors

Zurich, Switzerland

Peter P Speiser