Abstract: The present invention is in the area of administration forms and delivery systems for drugs, vaccines and other biologically active agents. More specifically the invention is related to the preparation of suspensions of colloidal solid lipid particles (SLPs) of predominantly anisometrical shape with the lipid matrix being in a stable polymorphic modification and of suspensions of micron and submicron particles of bioactive agents (PBAs); as well as to the use of such suspensions or the lyophilizates thereof as delivery systems primarily for the parenteral administration of preferably poorly water-soluble bioactive substances, particularly drugs, and to their use in cosmetic, food and agricultural products. SLPs and PBAs are prepared by the following emulsification process: (1) A solid lipid or bioactive agent or a mixture of solid lipids or bioactive agents is melted.

Abstract: The present invention concerns the use of Linomide.RTM. or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for the treatment of retrovirus infections. Specifically the invention concerns the treatment of HIV infections.

Abstract: A DNA sequence coding for a biologically active recombinant human factor VIII derivative, comprising a first DNA segment coding for the amino acids 1 through 740 of human factor VIII and a second DNA segment coding for the amino acids 1649 through 2332 of human factor VIII, said segments being interconnected by a linker DNA segment coding for a linker peptide of at least 3 amino acid residues and up to about 10 amino acid residues which are selected from lysine and arginine; recombinant expression vector comprising such DNA sequence; host cells of animal origin transformed with such recombinant expression vector; a process for the manufacture of recombinant human factor VIII derivative; and human factor VIII derivative containing the heavy chain and the light chain linked by metal ion bond.

Abstract: The present invention relates to the relief or prevention of withdrawal syndrome resulting from addiction to non-opiate type drugs of abuse and/or the suppression of dependence on non-opiate type drugs of abuse by administering to a person in need thereof, an effective amount of certain diphenylbutyl-piperazine-carboxamides including 4-[4,4-bis(4-fluorophenyl)butyl]-N-ethyl-1-piperazine-carboxamide which is known as amperozide.

Abstract: The use of an anti-MS quinoline-3-carboxamide compound comprising the structure of formula (I), optionally with substituents for the H.sup.1-9 hydrogen, or a salt of said compound where (a) ------------- represents that there are two conjugated double bonds between atoms comprised by the dashed line (only formula I), (b) the hydrogens H.sup.7 and H.sup.8 are attached to different atoms selected from X.sub.1, X.sub.2 and the nitrogen atom in the quinoline ring, (c) X.sub.1 and X.sub.2 are independently selected from an oxygen atom or an NH.sup.9 group, said X.sub.1 and X.sub.2 being bound by a single bond to the ring when carrying H.sub.7 or H.sub.8 and by a double bond when not carrying H.sup.7 or H.sup.8, for the manufacture of a composition intended for the treatment of conditions associated with MS. Also described are treatment regimens for MS patients. The particularly preferred compound is roquinimex or a salt thereof.

Abstract: Thiosubstituted prostaglandin derivatives and related compounds having the general structure ##STR1## useful as intraocular pressure reducing agents; pharmaceutical compositions containing such compounds; and methods of treatment using such compositions are disclosed.

Abstract: A colon selective pharmaceutical composition for oral delivery of one or more therapeutically active substances, comprises (i) a matrix core having the active substance or substances dispersed therein, and (ii) an outer cover layer without any active substance, said matrix core and cover layer being selectively degradable by enzymes normally occurring in the colon. A method of preparing such a colon selective pharmaceutical composition comprises the steps of mixing at least one therapeutically active substance with a matrix material to prepare a matrix core having the active substance or substances dispersed therein, and coating said matrix core with a material without any active substance therein to provide the matrix core with a drug-free protective cover layer, said matrix and cover layer materials being based upon at least one substance which is selectively degradable by enzymes in the colon.

Abstract: A melt granulating method for the production of pellets (spheres) which contain a therapeutically active substance of high-dosage type. The method is characterized by: (i) mechanically working a mixture which contains (a) the active substance in cohesive form and (b) a binder (melting point 40.degree. C.-100.degree. C.) while supplying sufficient energy for the binder to melt and to form spherical overwetted pellets; (ii) adding further cohesive substance, while maintaining the mechanical working; (iii) interrupting the mechanical working and supply of energy and cohesive substance when the desired mean particle size of dry pellets (spheres) has been achieved; and (iv) removing the smallest and largest particles and dividing the remaining pellets into dosage batches. A novel pharmaceutical composition containing a dosage of 300-500 mg of pellets is obtainable from this process.

Abstract: The invention relates to a novel process for the preparation of 13,14-dihydro-15 (R)-17-phenyl-18,19,20-trinor-PGF.sub.2.alpha. isopropyl ester of the formula (I)--wherein R stands for saturated or unsaturated straight, branched or cyclic C.sub.

Abstract: The invention relates to ophthalmological compositions for topical treatment of glaucoma or ocular hypertension comprising an effective intraocular pressure reducing amount of a prostaglandin derivative of PGA, PGB, PGD, PGE or PGF, in which the omega chain contains a ring structure, in an ophthalmologically compatible carrier. The invention further relates to the preparation of said compositions and their use for treatment of glaucoma or ocular hypertension.

Abstract: This invention relates a method for topical treatment of glaucoma or ocular hypertension by administration of an effective intraocular pressure reducing amont of a prostaglandin derivative of PGA, PGB, PGE and PGF, in which the omega chain contains a ring structure. The invention further relates to compositions comprising said prostaglandin derivatives in an ophthalmologically compatible carrier.

Abstract: This invention relates a method for topical treatment of glaucoma or ocular hypertension by administration of an effective intraocular pressure reducing amount of a prostaglandin derivative of PGA, PGB, PGE and PGF, in which the omega chain contains a ring structure. The invention further relates to compositions comprising said prostaglandin derivatives in an ophthalmologically compatible carrier.

Abstract: A compound of the formula Het--NR--SO.sub.2 --Ph.sup.2 --A--Ph.sup.1 (COOH)(OH) and tautomeric form, salts, solvates, C.sub.1-6 alkyl esters and pharmaceutical compositions of the compound. Ph.sup.1 and Ph.sup.2 are benzene rings with the proviso that carboxy and hydroxy are ortho to one another. Het includes an optionally substituted heterocyclic ring which includes conjugated double bonds and binds to nitrogen in NR. The compound is characterized in that A is a bridge which is stable against reduction because it is not azo, and in that R is hydrogen or lower alkyl.The invention also includes the preparation of the compound and its use as a drug, particularly for treating autoimmune diseases.

Abstract: The invention relates to the use of hGH, hGRF, hIGF-1, hIGF-2 or analogs of these or a mixture of two or more of these, alone or in conjunction with lactational enhancers for the treatment of human lactation failure. It also relates to the use of hGH, hGRF, hIGF-1, hIGF-2 or analogs of these or a mixture of two or more of these, alone or in conjunction with lactational enhancers for the manufacturing of a medicament for the treatment of human lactation failure, also a profphlactic treatment. Preferably human growth hormone is used. The invention also relates to a method for the treatment of human lactation failure as well as compositions and methods for their manufacturing.

Abstract: The present invention provides an O-Glycosylated Insulin-like Growth Factor 1 (IGF-1) analog of Insulin-like Growth Factor 1, a seventy amino acids single polypeptide chain which displays relatively high homology with proinsulin, essentially free from unglycosylated IGF-1.

Abstract: A prefilled syringe including a vial containing a measured quantity of an injectable product is provided Adjacent an end the vial is a displaceable wall adapted to be urged by plunger means so as to expel the product from the vial through a needle. The syringe also includes a two part housing for the vial and the plunger. One of the housing parts includes a stop surface that cooperates with a pair of corresponding surfaces extending from an external surface of the plunger. The plunger stop surfaces are positioned on opposite sides of the housing part stop surface to limit the displacement of the plunger within the vial. The position of the stop surfaces on the plunger relative to the vial may be varied by rotating the threadably connected housing parts relative to each other. A click-stop mechanism provided with the housing parts permits the housing parts to be rotated relative to each other in predetermined increments. A graduated dosing ring may be rotatably mounted about the housing parts.

Abstract: A natural antioxidant for stabilizing polyunsaturated oils is disclosed. This oil-soluble antioxidant is prepared by dissolving ascorbic acid in a polar solvent, dissolving phospholipid in a non-polar solvent and then mixing the ascorbic acid solution with the phospholipid solution. After removing the solvent a product is formed which has anti-oxidant properties and is soluble in non-polar solvents.

Abstract: A method is provided for cleansing a protein from multivalent metal ions bound thereto, these ions being released from the protein by exchanging the ions with monovalent metal ions, whereafter the multivalent metal ions are removed. The release and removal of these ions is effected, in particular, by diafiltration or gel filtration processes.

Abstract: The invention is related to the field of treating gastric and duodenal disorders and more specifically to the use of certain 13,14-dihydro-prostaglandin E derivatives, especially of PGE.sub.2, which are modified to contain a ring structure in the omega chain. The invention relates also to pharmaceutical compositions containing an active amount of these derivatives.

Abstract: Intraocular implants having optical lenses that are light, non-toxic, biocompatible, nonleachable in the presence of eye fluids and absorb at least 90% of the ultraviolet light in the 300-380 nm wavelength range but are transparent to most of the visible radiation. The intraocular implants will have a haptic for fixation in the posterior or anterior chamber of the eye. The optical lens has uniformly dispersed therein an ultraviolet light absorbing amount of 2-(hydroxy-lower alkylphenyl) benzotriazole which may be halogen substituted in the 4, 5, 6 or 7 positions.