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: A shape transformable medical implant or optical lens capable of substantial recoverable deformation in all dimensions is rapidly inserted and positioned into a target site such as an eye through an ejector having a small diameter, elongate, generally tubular outlet. The medical implant or optical lens is formed of a material having an elongation at break greater than 100% facilitating its ejection into the eye through a tubular outlet having an inner diameter of 3 mm or less. The ejector is provided with a precisely pressurizable chamber for the controlled displacement of the medical implant or optical lens through the small diameter, elongate, generally tubular outlet.

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: Optically transparent, high refractive index hydrogels are provided. Expansile hydrogel intraocular lenses are fabricated from the hydrogels by heating them above their elastic deformation temperatures and deforming them into an elongated configuration having at least one reduced dimension suitable for insertion through a small surgical incision. The lenses are allowed to cool in this configuration and retain the deformed shape prior to surgical implantation. Following implantation the lenses hydrate into an enlarged elastic form reassuming the original lens configuration of full capsule size.

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: A product in a closed container, (A) the product releasing and/or containing H.sub.2 S, and (B) the container being permeable to gases, another container, largely impermeable to gases and holding an H.sub.2 S absorber, being arranged around said container. The product especially may be infusion solutions containing substances which can release or generate H.sub.2 S, in addition to other amino acids, if desired. The solutions according to the invention clearly are more durable and contain less H.sub.2 S than comparable known solutions of the art.

Abstract: Organosiloxane compositions curable to optically clear, high refractive index elastomers are disclosed. The cured compositions have superior post-folding high resolution recovery making them suitable for fabricating foldable intraocular lenses used in small-incision ophthalmic surgeries. The organosiloxane compositions include first and second vinyl terminated organosiloxanes differing in molecular weights, each containing diphenylsiloxane and dimethylsiloxane, and, in addition, fumed silica, a crosslinking reagent, a platinum containing catalyst, and optionally an ultraviolet absorbing compound.

Abstract: Non-hydrolyzable, hydrophilic, heterocyclic cross-linking agents for cross-linking vinyl comonomers are provided. The cross-linked copolymers form optically transparent, high water content, and high refractive index hydrogels having long term stability which are useful as intraocular lenses and superabsorbents. The crosslinkers are selected from 4,6 divinyl pyrimidine, 2,5 divinyl pyrazine, 1,4 divinyl imidazole and 1,5 divinyl imidazole.

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: A process for preparing antibodies specific for an amino acid sequence which comprises immunizing a mammal with a fused protein comprising said amino acid sequence fused to an immunogenic IgG binding protein is disclosed.

Abstract: An intraocular lens includes an optic body and a pair of cantilevered spiral support members or haptics extending outwardly from a peripheral portion of the optic body. The haptics are formed as portions of an elongate cylindrical body. A method of making the haptics is disclosed which allows the haptic to be of variable cross sectional area, to be aplanar, and to include bends and curves, for example, without introducing undesirable molecular level changes or damage into the material of the haptic, which molecular level changes result in conventional haptics undesirably having a memory of their former shape and resulting dimensional changes (creep) of the conventional haptics over time.

Abstract: The present invention relates to a process for fabricating biocompatible implants. In particular, the present invention process involves punching out implants from sheet stock. In the exemplary embodiment, the implant is an intraocular lens, wherein the lens haptic is punched from ribbon stock fed through a punch press. The punching operation can be accomplished in a planar punch and die arrangement, or the die can be situated on cooperatively rotating drums. In an alternative embodiment, the entire intraocular lens is punched from sheet stock. In this process, the lens optics are formed first in the sheet stock to provide individual convex or concave hemispheres, spaced along the length and width of the sheet. The sheet stock is aligned with a die, and the die punches out the lens such that the lens optic coincides with the hemispheres and the lens haptics are punched therealong simultaneously.

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.