Abstract: High ratio active agent:lipid complexes, their preparation and use are disclosed. Particular reference is made to cephalosporin:lipid complex and iodinated contrast agent:lipid complex. Use of high ratio cephalosporin:lipid complex in bacterial prophylaxis, and particularly bacteremia prophylaxis, including a method of preventing bacterial infection in an animal over an extended period comprising the step of administering to said animal a high ratio cephalosporin:lipid complex is further disclosed as is the use of high ratio iodinated contrast agent:lipid complex in X-ray applications.

Abstract: 3.beta.-[4-iodophenyl]-tropan-2.beta.-carboxylic acid methyl ester tartrate is a high affinity binding ligand for cocaine receptors in mammalian brains. It and its congeners may be employed for imaging and other brain scanning techniques that allow the determination of the presence of cocaine receptors, such as dopamine and serotonin transporters and the like.

Abstract: A method of microencapsulating an agent to form a microencapsulated product, having the steps of dispersing an effective amount of the agent in a solvent containing a dissolved wall forming material to form a dispersion, combining the dispersion with an effective amount of a continuous process medium to form an emulsion that contains the process medium and microdroplets having the agent, the solvent and the wall forming material and adding rapidly the emulsion to an effective amount of an extraction medium to extract the solvent from the microdroplets to form the microencapsulated product.

Abstract: Biomodulators, optionally linked to imaging-active moieties, can be administered to a host to enhance images thereof, e.g., NMR-, X-ray- or radio-images, preferably by increasing aberrant tissue signal intensity. Biomodulators can also condition tissue to enhance uptake of otherwise non-specific imaging agents. When linked to drugs, biomodulators can target the same to particular sites in the body.

Abstract: Biomodulators, in conjunction with antibodies, tumor-specific agents or conjugates thereof, optionally linked to imaging-active moieties, can be administered to a host to enhance images thereof, e.g., NMR-, X-ray- or radioimages, preferably by increasing aberrant tissue signal intensity.

Abstract: Radioactively labelled peptides comprising oligopeptides of from 3 to 10 peptide units and containing the sequence RGD and particularly the oligopeptides RGDSY and RGDFY, are disclosed as in vivo thrombus, tumor or CAM markers for the in vivo diagnosis and detection of thrombi, tumors or CAM in mammals.

Abstract: Stable therapeutic radionuclide compositions comprising, for example, .sup.186 Re, .sup.188 Re and .sup.131 I stably bound to a proteinaceous targeting moiety and suitable for human in vivo administration are disclosed. Stabilizing agents preferably comprise antioxidants and challenging agents, and combination of HSA with an antioxidant and/or challenging agent provides enhanced long term stability. Ascorbic acid is an especially preferred stabilizing agent, which provides stability of therapeutic radionuclide compositions at levels of at least about 90% for several hours up to several days.

Abstract: Boronic acid adducts of technetium-99m and radioactive rhenium dioxime complexes, each of which include biochemically active groups, are useful as diagnostic and therapeutic agents, respectively.

Abstract: Gold sol coated with alkanethiols and alkanethiol derivatives, which provide groups on the sol available for the linking of binding moieties such as antibodies, antigens or ligands to the gold sol. Di- and tri-thiol compounds bound to gold sol also facilitate the adsorption of antibodies, antigens or ligands to the sol. The coating process, and test kits incorporating the coated sols are also included.

Abstract: Gentisic acid and its derivatives substantially inhibit peptide autoradiolysis. Gentisic acid or its derivatives may also be used in combination with other stabilizers such as inositol and ascorbic acid to inhibit autoradiolysis of radiolabeled peptides.

Abstract: A diagnostic composition suitable for administration to a warm-blooded animal comprising somatostatin or a molecule capable of interacting with the somatostatin receptor labeled with a radionuclide by means of a chelate ligand capable of administration to an animal to produce reliable visual imaging of tumors or therapeutic effects on tumors.

Abstract: Methods are described for controlling the transbilayer distribution of ionizable lipids and proteins in vesicles. Control of the ion gradient of the exterior bathing medium in relation to that of the interior entrapped aqueous compartment of the vesicles induces migration of ionizable lipids or proteins to one or the other of the monolayers comprising the bilayer. This can result in an asymmetric distribution of the ionizable lipid or ionizable protein. The basic ionizable lipids, such as stearylamine and sphingosine, are sequestered into the inner monolayer when the liposome interior is acidic relative to the liposome exterior. Conversely, acidic ionizable lipids such as oleic acid and stearic acid are sequestered into the inner monolayer when the liposome interior is basic relative to the liposome exterior bathing solution.

Abstract: The present invention involves a method of imaging tissue sites of inflammation which takes advantage of the up-regulation of surface antigenic markers on leukocytes upon activation thereof. A recognition agent selected from the group of chemotactic peptides, eosinophilic peptides and agents which are capable of selective interaction with a chemotactic receptor associated with activated leukocytes is radiolabeled. The radiolabeled recognition agent is infused into a patient and the patient's tissue sites are thereafter imaged in order to detect, evaluate or monitor tissue damage mediated by inflammation.

Abstract: Functionalized water soluble macrocyclic complexes of lanthanide, actinide and yttrium ions were obtained by metal templated, Schiff-base, cyclic condensation of: (1) a functionalized 1,2-diaminoethane and a dicarbonyl compound selected from the group consisting of 2,6-dicarbonylpyridine, 2,6-diformylpyridine, 2,5-dicarbonylfuran, 2,5-diformylfuran, 2,5-dicarbonylthiophene and 2,5-diformylthiophene; or (2) 1,2-diaminoethane and a ring-substituted heterocyclic dicarbonyl compound selected from a group consisting of substituted 2,6-dicarbonylpyridine, substituted 2,6-diformylpyridine, substituted 2,5-dicarbonylfuran, substituted 2,5-diformylfuran; substituted 2,5-dicarbonyl thiophene, and substituted 2,5-diformylthiophene. Coordination complexes thus formed are kinetically stable in dilute aqueous solution.

Abstract: A diagnostic composition suitable for administration to a warm-blooded animal comprising hirudin or a molecule capable of interacting with the hirudin receptor labeled with a radionuclide by means of a chelate ligand capable of administration to an animal to produce reliable visual imaging of thrombus.

Abstract: This invention relates to reagents and methods for detecting and imaging cardiovascular lesions such as atherosclerotic plaques, vascular clots including thrombi and emboli, myocardial infarction, and other organ infarcts. Monospecific antibody imaging agent conjugates specific for one type of leukocyte, as well as multispecific antibody imaging agent conjugates specific for at least one type of leukocyte and for antigens associated with fibrin, myosin or platelets, are used in the present invention. Multispecific antibody imaging agent conjugates specific for at least two different antigens selected from the group consisting of fibrin-, myosin- and platelet associated antigens are also provided.

Abstract: A novel process for producing powdered carotenoid preparations, in which a suspension of a carotenoid in a high-boiling oil is brought into contact with superheated steam during a maximum period of 30 seconds, and subsequently emulsified the liquified solution of said carotenoid in oil produced by said contact with superheated steam in an aqueous solution of a colloid and then spraying and drying said emulsion to a powder.

Abstract: A process for the microencapsulation of oil droplets containing a medical drug for oral administration, comprises the steps of mixing the drug with liquid oil by sonication for 5-30 seconds to disperse the drug homogeneously in the oil, and adding the drug-dispersed oil to an aqueous solution mixture to form a two phase system. The aqueous solution mixture will form a capsule material, and comprises a polysaccharide which has metal chelating capacity, a biocompatible and water-soluble polymer for improving the physical properties of the capsule material, and emulsifying agents. The two phase system is then subjected to sonication to produce an oil-in-water emulsion containing the drug-dispersed oil in the form of droplets having a diameter in the range of 1-5 .mu.m. As soon as possible after formation of the emulsion, the emulsion is added to a multivalent cation-containing solution to harden the capsule material.

Abstract: A continuous process for forming spheroidal high bulk density nitroguanid crystals from an aqueous solution of nitroguanidine which contains methylcellulose and partially hydrolyzed poly(vinyl alcohol) as crystal habit modifiers. A saturated aqueous solution of nitroguanidine is formed at a temperature T.sub.1 where 70.degree. C..ltoreq.T.sub.1 .ltoreq.100.degree. C. and crystallization occurs at a lower temperature T.sub.2 where 20.degree. C..ltoreq.T.sub.1 -T.sub.2 .ltoreq.50.degree. C.

Abstract: The invention provides chemically modified lymphokines comprising a lymphokine moiety and at least one polyethylene glycol moiety of the formula: R.paren open-st.O--CH.sub.2 CH.sub.2 .paren close-st..sub.n wherein R is a protective group for the terminal oxygen and n is at least one, bonded directly to at least one primary amino group of the lymphokine moiety, and a method of producing the same.The chemically modified lymphokines according to the invention can be produced by reacting a lymphokine with an aldehyde of the formula R.paren open-st.O--CH.sub.2 CH.sub.2 .paren close-st..sub.n-1 O--CH.sub.2 CHO wherein R and n are as defined above, in the presence of a reducing agent.The chemically modified lymphokines according to the invention are useful as drugs, among others.