Abstract: A process for preparing a radiopharmaceutical composition comprising a technetium 99m chelate complex, comprises the steps of:(1) mixing (a) HSCH.sub.2 CO--NHCH.sub.2 CO--NHCH.sub.2 CO--NHCH.sub.2 COOH (mercaptoacetylglycylglycylglycine, MAG3), (b) a watersoluble reducing agent, (c) a water-soluble stabilizing agent in an amount of not less than 70 mol per 1 mol of the water-soluble reducing agent and (d) a pertechnetate at a pH of about 8 to 11; and(2) heating the resultant mixture at a temperature of about 90 to 140.degree. C.Said process removes any troublesome labeling operation at the diagnostic site and relieve the practitioners from the exposure to radiation during the labeling operation.

Abstract: The present invention relates to novel preorganized hexadentate ligands suitable for complexing with a radionuclide to form imaging agents for diagnostic purposes. The ligands have the formula: ##STR1## wherein a) R.sub.2 is hydrogen and R.sub.3 is methyl; or R.sub.2 and R.sub.3 together form a methoxy benzene ring.

Abstract: Novel thiol-reactive maleimido-based radiolabeling reagents are disclosed which are useful for binding and receptor studies and assays. The reagents are also useful as diagnostic imaging agents, and as radiotherapeutic drugs.

Abstract: The present invention relates to a method of preparing microcapsules suitable for encapsulation of therapeutic and diagnostic agents. The capsular coats are prepared from biodegradable polymers. In a particular aspect of the invention, surface charge of the polymeric material is altered by conjugation of an amino acid ester to the polymer, providing targeting to specific tissue cells. Encapsulation of hydrophilic radiodiagnostic agents in 1 .mu.m capsules provides improved opacification. Encapsulation of cytotoxic agents in 100 .mu.m capsules is useful in chemoembolization procedures.

Abstract: To prepare an aqueous dispersion of lamellar lipid vesicles, at least one lipid is dissolved in at least one water-immiscible organic solvent; the organic phase thus obtained is added to an aqueous phase in such amounts that a dispersion of the oil-in-water type is obtained by vigorous stirring; the evaporation of the solvent(s) is carried out with vigorous stirring, the continuous phase of the dispersion always remaining the aqueous phase; and, should it become necessary, the dispersion is concentrated. The process can be carried out at low temperature (of the order of 35.degree. to 55.degree. C.), which makes it possible to encapsulate in the aqueous phase or to introduce into the vesicle sheets heat-sensitive active substances; the lipid concentration in the organic phase can reach up to 50% by weight.

Abstract: A method for the encapsulation of pigment particles utilized in ink formulations by means of vinyl polymerization, within an aqueous medium, and the cosmetic products prepared with said ink formulations are disclosed. The method of encapsulation can be either that of free-radical polymerization, wherein a peroxide catalyst and a antioxidant are employed or that of a redox system wherein an ion-producing metallic pigment is utilized. The resultant cosmetic products are characterized by their overall smoothness, uniform color, and increased dispersibility of the ink formulations utilized therein, and, due to the presence of the ink formulation having the encapsulated pigment particles dispersed therein.

Abstract: The present invention relates to labelled resiniferatoxin and congeners thereof. Preferably, the labelled compounds of the invention are radio or fluorescently labelled. The invention is further directed to compositions comprising these labelled compounds, as well as to methods of using these compounds.

Abstract: Benzalkonium chloride and benzethonium chloride are each useful in radiopharmaceutical preparations as bacteriostatic agents which are compatible with anti-oxidants.

Abstract: The subject invention provides a method of encapsulating viable tissue or cells within a double walled bead, the double-walled bean produced as a result of the method, as well as a method of pretreating the tissue or cells with an immunosuppressant such as UV-B irradiation prior to their encapsulation.

Abstract: Microcapsules which comprise, (A) a wall comprising a mixture of zirconium chloride and at least one member selected from the group consisting of poly(vinyl alcohol) and its derivatives, and (B) a core material enclosed with the wall; and a process for producing the same. In this invention, any substance can be used as the core material irrespective of its hydrophicity or hydrophobicity, and there can be obtained microcapsules excellent in heat resistance, water resistance, and transparency by simple steps.

Abstract: Two embodiments of a process for producing concentrated suspensions of polyurea microcapsules especially suitable for manufacturing carbonless copy paper (CCP) are disclosed. Either embodiment can be a batch or continuous process. In the first embodiment, a liquid hydrophobic phase comprising a core material and polyisocyanate at least partially soluble therein is emulsified with an aqueous continuous phase including a polyhydroxylated colloidal stabilizer to form a suspension of microdroplets of the hydrophobic phase. A polyamine such as diethylenetriamine reactive with the polyisocyanate and a catalytic amount of an alkaline base are then added, initiating an interfacial polyaddition reaction at alkaline pH which forms the polyurea microcapsules. The alkaline base is preferably NaOH, KOH, or LiOH; the polyisocyanate is preferably a biuretized or isocyanurate-modified triisocyanate of a lower alkyl diisocyanate; and the polyamine is preferably added in a stoichiometric ratio relative to the isocyanate.

Abstract: A stable basic zirconia sol can be prepared by adding to an acidic aqueous zirconia sol a dispersion stabilizer selected from the group consisting of a water-soluble organic acid having a hydroxyl group and a water-soluble organic compound having at least two hydroxyl groups, and thereafter adjusting the sol with a basic compound to pH 6 to 14.

Abstract: Applicants describe the synthesis of fluorotamoxifen and iodotamoxifen analogs with the halogen atom positioned on the aliphatic chain of the tamoxifen molecule. The halogenated-tamoxifen derivatives possess superior binding affinities to estrogen receptors of pig uteri compared with tamoxifen. The fluorinated tamoxifens have potential use in imaging estrogen receptors by PET whereas the iodinated tamoxifens have potential use in imaging estrogen receptors by SPECT. Rapid and efficient methods of preparing fluorotamoxifen and iodotamoxifen derivatives with high specific activity are also disclosed. Fluorotamoxifen and iodotamoxifen derivatives may advantageously be used as anti-cancer therapeutic agents to halt estrogen-receptor positive tumors.

Abstract: A method of preparing a stable, therapeutic radiopharmaceutical composition comprised of an alpha- or beta-emitting radionuclide and a ligand by lyophilizing a solution of the complex. The radionuclide preferably has a half-life of at least twelve hours. The invention also is directed to stable lyophilized radiopharmaceutical compositions prepared by this method. The invention is particularly suited to the preparation of radionuclide-labeled antibodies in a stable form which merely requires reconstitution at the point of use.

Abstract: A fibrin-binding protein such as t-PA is labeled with a detectable substance, such as a radionuclide, and administered to a patient for diagnosis of blood clots and for monitoring the dissolution thereof during therapy. The detectable substance preferably is attached to t-PA through linkers which specifically bind to the portion of the t-PA protein responsible for enzymatic activity, thereby diminishing this activity while leaving the fibrin-binding property of the protein intact.

Abstract: This invention relates to a large scale method for the production of medical grade lipid-coated microbubbles, to the paramagnetic labeling of such microbubbles and to therapeutic applications for the microbubbles. More particularly, the invention relates to a method of the production of medical grade, concentrated suspensions of stable, paramagnetically derivatized or underivatized microbubbles useful for ultrasonic and magnetic resonance imaging and also relates to therapeutic interventions such as selective tumor destruction.

Abstract: A process for the production of microcapsules containing a core material is provided and includes the steps of providing a polar solvent, and adding thereto a dispersion of a tertiary aliphatic isocyanate and a core material in an oleophilic liquid and an amine-containing composition having at least three primary amine groups to form a mixture. The mixture containing these components is reacted to form microcapsules containing the core material. The tertiary aliphatic isocyanate preferably comprises an adduct of m-tetramethylxylene diisocyanate and trimethylolpropane. The core material may contain a dyestuff precursor which is capable of reacting with a color developer to form a color. The microcapsules containing dyestuff precursor may be used to coat a support sheet to form carbonless copy paper.

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: A process for producing melamine-formaldehyde microcapsules using a reactive protective colloid is provided. The reactive protective colloid is prepared by reactively coupling a surface active polymer with a first melamine-formaldehyde pre-condensate. An aqueous solution which includes the reactive protective colloid and a second melamine-formaldehyde pre-condensate is then prepared. A substance to be encapsulated, preferably an oily solution containing a dyestuff precursor, is dispersed as droplets into the aqueous solution. The reactive protective colloid surrounds the droplets to form an emulsion. The second melamine-formaldehyde pre-condensate and the reactive protective colloid are made to self-condense to form melamine-formaldehyde microcapsule walls around the droplets of the substance to be encapsulated.

Abstract: Serotype-specific human anti-Pseudomonas monoclonal antibodies which bind to determinants of the cell wall lipopolysaccharides of P. aeruginosa are prepared from hybrid cell lines. The antibodies may be of any isotype. These antibodies may be used to treat infections caused by P. aeruginosa.