Abstract: This invention relates to a weight control composition, preferably in the form of a capsule or tablet, comprising a mixture of guggul extract and at least one phosphate salt selected from calcium phosphate, potassium phosphate and sodium phosphate. The composition evidences synergistic activity in reducing body weight and percent body fat in mammals. The guggul extract/phosphate salt product also reduces plasma lipid levels and cholesterol in overweight hyperlipidaemic humans. The inventive composition may also contain at least one additional component selected from phosphatidylcholine, hydroxycitric acid and L-tyrosine.

Abstract: A composition for treating impotence in human males contains a synergistic mixture of dried sturgeon roe and yohimbine hydrochloride wherein the weight percent ratio of said dried sturgeon roe:yohimbine hydrochloride is from about 25:1 to 1000:1, with an optimum ratio of about 132:1. The roe can be dried via either lyophilization or air drying under ambient temperature and pressure with reduced environmental humidity. A method of treating impotence in human males includes administration of such compositions containing the synergistic mixture of roe and yohimbine. Also, a method of treating impotence in human males by administration of dried roe in doses of from 300 to 900 mg. The roe is prepared either via lyophilization or air drying under ambient temperature and pressure with reduced environmental humidity.

Abstract: Enteral formulas that contain long-chain polyunsaturated fatty acids (PUFAs), as arachidonic acid (AA) and docosahexaenoic acid (DHA) that are essentially free of cholesterol, are described. More particularly, the invention relates to methods for reducing the incidence of necrotizing enterocolitis by administering compositions which provide .omega.-6 and .omega.-3 long chain PUFAs, phospholipids and/or choline. Compositions from egg yolk lipids are presently preferred as they contain .omega.-6 and .omega.-3 long chain PUFAs and are predominantly in a phosphtidylcholine form. This is believed to provide a synergistic effect.

Abstract: The present invention provides an improved mode of operation of an apparatus for angioplasty or cardiac catheterization, apparatus for angioplasty and cardiac catheterization, and method of angioplasty or cardiac catheterization. The improvement and improved mode of operation includes the step of administering a therapeutically effective amount of a lipid acceptor during angioplasty or cardiac catheterization of a subject with the apparatus or component thereof. The lipid acceptor is selected from the group consisting of a large liposome comprised of phospholipids substantially free of sterol and small acceptors. The effective period of time is in the range of about less than 1 minute to about two years from the time of the angioplasty or cardiac catheterization. The improved angioplasty or cardiac catheterization apparatus includes means for administering a therapeutically effective amount of a lipid acceptor, and optional co-administration means for administering the lipid acceptor and a diagnostic agent.

Abstract: Active ingredient system for the lipid exchange with target structures; methods for their manufacture and their use; and products containing active ingredient systems of this type are disclosed. The active ingredient system for the transfer of lipophilic and/or amphiphilic components to target structures or from such back to the active ingredient system, as well as to their exchange with the target structures, is formed from at least one lipid component with at least one transfer protein. In the method for the manufacture of the active ingredient system, lipid and protein components are combined into systems in different configurations depending on the purpose of its use and its place of use, whereby the specificity results from the lipid used and the transfer protein employed, as well as the direction of the lipid transfer. Active ingredient systems of this type are used in technology, such as the material technology, in medicine, pharmaceuticals and in the area of cosmetology.

Abstract: The invention concerns a novel use of phospholipids of animal origin in therapy and/or dietetics, more particularly the use of phospholipids rich in long-chain polyunsaturated fatty acids derived from animal brains or hen's eggs, to produce a pharmaceutical and/or dietetic composition to regulate melatonin secretion.

Abstract: A method and composition are provided for treating intracellular pathogens that reside in phagosomes. The compositions include antibiotics which are conjugated with transferrin or other ligands to form conjugates that target membrane-bound pathogens. The conjugates are selectively taken up by infected phagosomes. Conjugates are provided which utilize transferrin as the targeting ligand for treating mycobacterium which reside in membrane-bound phagosomes.

Abstract: The present invention relates to a phospholipid composition comprising two or more phospholipids, the electric conductivity and pH of a 5 wt. % suspension of the phospholipid composition in deionized water being in the range of 130 to 220 .mu.S/cm and in the range of 6.5 to 9.5, respectively; a process for producing the same; and the use of the same.

Abstract: Synthetic lipid composition in which the content and the distribution of the fatty acids are similar to those of human milk fat, containing less than 2% by weight of free fatty acids, in which palmitic acid is predominantly at the 2-position of the triacylglycerols and the arachidonic and docosahexaenoic acids are distributed between the 1-, 2- and 3-positions and in particular predominantly at the 2-position of the triacylglycerols.

Abstract: .alpha.-Tocopherylphosphocholine and salts thereof have been discovered to possess antiviral, anti-fungal, anti-inflammatory, PAF-antagonist, and ultra-violet radiation-blocking activities. The compound and salts have also been discovered to be capable of forming liposomes. The present invention thus provides methods of treating viral and fungal infections, inflammatory disorders and pathophysiological conditions due to PAF activity in a mammal by administering to the mammal .alpha.-tocopherylphosphocholine or a pharmaceutically acceptable salt thereof. The invention also provides pharmaceutical compositions comprising .alpha.-tocopherylphosphocholine or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier. Further, the invention provides liposomes which comprise .alpha.-tocopherylphosphocholine or a salt thereof as a structural component of the liposome bilayer.

Abstract: The invention relates to a stable preparation which comprises a protein, such as thrombin, that is bound in and/or on (i.e., to) lipid vesicles and that was treated for the inactivation of potentially present viruses. Further, the invention relates to methods for the production of a stable preparation for the treatment of blood coagulation disorders, wherein a protein is bound in and/or on lipid vesicles, and the method comprises a step in which the protein lipid complex is subjected to a treatment for the inactivation of potentially present viruses.

Abstract: The severity of damage caused to the skin and mucosa of animals with cancer undergoing radiation therapy is mitigated by feeding the animal a nutritionally balanced food composition containing omega-6 polyunsaturated fatty acids which are supplemented with a mixture of a omega-3 polyunsaturated fatty acids and arginine.

Abstract: The invention is directed to methods and pharmaceutical compositions for the topical administration of analgesic drugs which affects peripheral muscarinic receptors such as neostigmine. In particular, the invention relates to topical administration of an analgesic agent, e.g., neostigmine, optionally in admixture with a skin- or mucosal-specific penetration enhancer, to produce a localized analgesic effect in inflamed or non-inflamed skin or mucosal tissue, and without a transdermal or transmucosal migration of the agent, e.g., into the central nervous system.

Abstract: The present invention provides compositions that inhibit apoptosis, methods for making the compositions, and methods of use thereof.

Abstract: The present invention relates to a delivery system which includes a bioactive drug or cosmetic substance presented in the form of submicron oil spheres alone, or drugs or cosmetic substances in a combination with the oil spheres in an aqueous suspension or emulsion. Optionally, a skin penetration enhancer may be included in such formulations. Such preparations achieve improved bioavailability and exert larger pharmacological effects than an equivalent dose of the drug or cosmetic formulated in conventional creams, lotions or oleaginous bases.

Abstract: The cosmetic preparation contains: (a) an oil-soluble active ingredient that is suitable for skin cosmetics, (b) a partial fatty acid ester of polyoxyethylene sorbitan, (c) at least one phospholipid, (d) ethanol, and (e) water as a carrier liquid. The phospholipid is dissolved in ethanol, and then the partial fatty acid esters of polyoxyethylene sorbitan and the active ingredient are added. The oil phase that is obtained is added to water and stirred. The preparation is obtained in the form of a nanodispersion.

Abstract: Compositions for preventing or treating memory loss in the brain, comprising an effective amount of a mixture of lecithin and vitamin B.sub.12.

Abstract: The invention relates to a pharmaceutically acceptable prodrug which is a covalent conjugate of a pharmacologically active compound and an intracellular transporting adjuvant, characterized by the presence of a covalent bond which is scission-sensitive to intracellular enzyme activity. The prodrug may be used in a technique for treating a condition or disease in a human related to supranormal intracellular enzyme (.e.g. phospholipase and/or esterase) activity, whereby on administering it to a human having such condition or disease, the bond is broken in response to such activity, and the pharmacologically active compound accumulates selectively within cells having such supranormal intracellular enzyme activity. Exemplary conjugates are esters of the carboxylic function in the formula, with e.g. heptanoyl-sn-3-glycerophosphoryl-choline or octanoyl-sn-3-glycerophosphoryl-choline.

Abstract: This invention herein describes a method of facilitating the entry of drugs into cells and tissues at pharmokinetically useful levels and also a method of targeting drugs to specific organelles within the cell. This polar lipid/drug conjugate targeting invention embodies an advance over other drug targeting methods because through this method, intracellular drug concentrations may reach levels which are orders of magnitude higher than those achieved otherwise. Furthermore, it refines the drug delivery process by allowing therapeutic agents to be directed to certain intracellular structures. This technology is appropriate for use with antiproliferative, antibiotic, antimycotic, antiviral and antineoplastic drugs, in particular in combination with a multiplicity of other emollients and agents to make up topically-active substances such as salves, for rapid and efficient introduction of such agents through the epidermis for treatment of skin diseases and other disorders.

Abstract: Somatic mammary cells are defended from an action of glucocorticoid hormones by an insect pheromones of non-steroid nature, its derivative or a synthetic analog.

Abstract: The present invention relates generally to the method for the production of liposomal microencapsulated boron-containing products to be used for agricultural formulations. More specifically, a new method of production of liposomal microencapsulated is disclosed for active agents such as pesticides. A lecithin is mixed with an organic solvent in a certain proportion so as to provide solutions with varied levels of solubilized lecithin. The particular solvent being used will depend on the amount of active agent (AA) desired in the final solution. The formulation of the lecithin/organic solvent mixture is then allowed to settle. After settling, the top layer is separated and saved, while the bottom layer is discarded. An AA is then added to form a concentrate that is added to water for vesicle formation. Boron-containing materials formulated according to the invention may now be applied to agricultural field crops and fruits.

Abstract: Disclosed are compositions comprising non-steroid anti-inflammatory drugs (NSAID'S) complexed with zwitterionic, neutral phospholipids, or both, having reduced gastrointestinal irritating effects and enhanced antipyretic, analgesic, and antiinflammatory activity. Also disclosed are improved methods of using the complexes for treating fever, inflammation, and preventing platelet aggregation. In some embodiments, the anti-pyretic activity of sub-therapeutically used amounts of NSAID's are enhanced to elicit anti-pyretic activity in vivo when associated (noncovalently) with zwitterionic phospholipids, such as dipalmitoyl phosphatidyl choline. Methods and compositions useful for enhancing the therapeutic activity of non-steroidal anti-inflammatory agents in the presence of anti-secretory agents are also discussed.

Abstract: Tangential flow filtration is used in the size separation of particles, such as liposomes and lipid particles. These particles may be passed through a tangential flow filtration device of any pore size desired. Tangential flow filter systems of various pore sizes may be used sequentially to obtain particles such as lipid particles or liposomes having a defined size range.

Abstract: The present invention comprises methods and compositions for topically treating and moisturizing keratinous structures of humans and animals including skin, hair, fingernails, toenails, hooves, and horns.

Abstract: An immunopotentiating and infection protective agent comprising riboflavin and/or a riboflavin derivative, which is safe for the human, animals or the like, an immunopotentiating and infection protective agent comprising riboflavin and/or a riboflavin derivative and (1) proline and/or glutamine, (2) an antibiotic, or (3) a water-soluble polymer or lecithin, which is safe for the human, animals or the like, and a process for the production thereof.

Abstract: Disclosed are methods and materials for visualizing or treating vasculature. The methods and materials in this invention relate to selective and non-invasive visualization, or treatment such as chemical occlusion, of vasculature in the mammalian eye. The methods utilize fluorescent dyes and tissue-reactive substances encapsulated within heat-sensitive liposomes which are subsequently heated to release the contents thereof at a pre-determined anatomical locus. The methods of this invention further utilize tissue-reactive agents which, when activated, are effective to cause localized tissue damage and occlusion of blood vessels and/or blood sinuses. The materials of this invention relate to diagnostic reagents and kits for visualizing or treating a mammalian blood vessel or sinus.

Abstract: Compositions useful to reduce cholesterol absorption. The compositions may be dosed in capsule or tablet form, or by adding either in liquid or dry powder form to foods and beverages. The compositions are an aqueous based homogeneous micellar mix which is dried to provide a mixture of finely-divided plant sterol, preferably sitostanol and lecithin. The mole ratio of the plant sterol, preferably sitostanol to lecithin, should be within the range of 1:1 to 1:10, preferably at least 1:2.

Abstract: An oil-free and wax-free solid or powder-based cosmetic material having beneficial oil and wax characteristics without the detrimental effects thereof. The cosmetic material comprises pigments and/or pigment extenders which are surface treated with a hydrophobidizing material to become hydrophobic. The hydrophobidized cosmetic material is admixed with oil-free and wax-free binders in an aqueous slurry and then vacuum dehydrated and dried at an elevated temperature to provide the finished cosmetic product with excellent skin "feel", adhesiveness, extendibility, payoff (i.e., pickup of the product by an applicator) and uniformity characteristic of oil-containing cosmetics but without oil and its detrimental effects.

Abstract: The present invention is based, in part, upon the discovery that the use of pyruvate in combination with a cortisol blocker, such as phosphatidylserine, produces a synergistic effect in increasing lean body mass or muscle tissue, decreasing fat deposition, increasing endurance and athletic performance of a mammal consuming same. The invention also relates to a method of treating the catabolic effects of diseases such as cancer and AIDS by the administration of pyruvate and a cortisol blocker.The present invention also discloses a synergistic composition comprising pyruvate and a cortisol blocker. More specifically, the present invention relates to a composition which comprises pyruvate and/or derivatives of pyruvate and phosphatidylserine.

Abstract: Disclosed are injectable suspensions of gas filled microbubbles in an aqueous carrier liquid usable as contrast agents in ultrasonic echography. The suspensions comprise amphipathic compounds of which at least one may be a laminarized phospholipid as a stabiliser of the microbubbles against collapse with time and pressure. The concentration of phospholipids in the carrier liquid is below 0.01% wt but is at least equal to or above that at which phospholipid molecules are present solely at the gas microbubble-liquid interface. Also disclosed is a method of preparation of the stable suspensions of air or gas filled microbubbles.

Abstract: A cerebration improver having a prominent action for increasing brain glucose level has an effect of improving the cerebration of a subject administered with the improver. The cerebration improver contains as the effective ingredient phosphatidyl-L-serine, or lysophosphatidyl-L-serine produced by eliminating the fatty acid chain at the position .alpha. or .beta. of phosphatidyl-L-serine, or the salts thereof. The phosphatidyl-L-serine has a structural fatty acid chain derived from at least one raw material lecithin selected from the group consisting of soy bean lecithin, rapeseed lecithin or egg yolk lecithin. Using the raw material lecithin as the substrate, phosphatidyl-L-serine can be produced by utilizing transphosphatidylation.

Abstract: A composition is disclosed containing nonesterified fatty acids having 14-22 carbon atoms of saturated, unsaturated and polyunsaturated fatty acid, monoglycerides which are monoesters of glycerol and fatty acids having 14-22 carbon atoms of saturated, unsaturated and polyunsaturated fatty acid, lysophosphatidylcholine in which the fatty acid moiety has 14-22 carbon atoms of saturated, unsaturated and polyunsaturated fatty acid and bicarbonate. The compositions can optionally also contain bile salts. These compositions form submicron size colloidal particles and can act as vehicles for transporting orally administered drugs, sources of calories in the form of readily absorbable and sustained absorption of fats, sources of readily absorbable polyunsaturated fat and as particles for topical application to the skin. A method of making these particles is also described.

Abstract: Disclosed herein are methods for increasing the bioavailability of pharmaceutical agents by conjugation to phosphocholine. Also disclosed are phosphocholine-derivatized steroids, peptides and other biologically active agents and pharmaceutical formulations comprising these compounds.

Abstract: Disclosed is a method of treating respiratory diseases comprising treating the lungs with an therapeutically-effective amount of .alpha.-tocopheryl-phosphocholine or a pharmaceutically-acceptable salt thereof, wherein the amount is administered is effective to make breathing easier.

Abstract: A dietary supplement for canines and felines includes taurine in a liquid lecithin base. The dietary supplement has proven effective in reducing epileptic seizures in canines and in reducing behavioral problems, such as aggression, in canines. In addition, the dietary supplement is more easily digestible than conventional tablet forms of taurine and is more effectively administered to felines for treatment of cardiomyopathy.

Abstract: Carnitine, aminocarnitine and cysteic acid serve as carriers to bring pharmaceutically active compounds to desired sites in the body, e.g. skeletal muscle or the heart. The pharmaceutically active compound can be a protease inhibitor, a cardioactive drug for combating arrythmia, etc. The linkage is chemical through one or more alcohol, carboxyl or amine groups using reagents such as glutaraldehyde, dicarboxylic acid anhydrides and acid halides and carbodiimides. Carnitine derivatives are also incorporated into liposomes which are then used as carriers of active pharmaceutical agents.

Abstract: Polypeptide analogs of human the human lung surfactant protein, SP-C, are provided. The polypeptides have the following structure: ##STR1## wherein A is H or Phe, B is Phe or Trp, and C is Ile, Leu, or Ser. They exhibit surfactant activity and are useful in the treatment of respiratory distress syndromes in premature infants and adults.

Abstract: Disclosed is a novel transdermal delivery system for dehydroepiandrosterone (DHEA). Using phospholipids as vehicles, DHEA can be administered into and through the skin when topically applied. Numerous advantages apply to this modality of therapy.

Abstract: The present invention is directed to a method for making in vivo a lecithin gel which provides for the sustained release of a biologically active compound contained in the gel. The present invention is also directed to a method for the sustained treatment of a human or other mammal with a therapeutic amount of a biologically active compound using the gel for the sustained release of the biologically active compound.

Abstract: Perfluoroalkylated amphiphilic phosphorus compounds, corresponding to the formulae: ##STR1## wherein V is O or S;R.sup.1, R.sup.2 and R.sup.3 are H or substituted or unsubstituted perfluoroalkylated or hydrocarbon radicals;provided thatR.sup.1, R.sup.2 or R.sup.3 is a perfluoroalkylated radical; and Y and Z are radicals which can bear a part derived from a sugar, a polyol, or a hydrophilic polymer such as polyethyleneglycol, a perfluoroalkylated part or a part derived from a pharmaceutically active molecule, and method for their preparation and use. These compounds can be included in preparations, emulsions, dispersions, gels, microemulsions, notably for biomedical uses.

Abstract: A method of treating a site of systemic infection which includes administering a therapeutic compound entrapped in liposomes. Also included is a liposomal composition and a method of preparing a liposomal composition for use in concentrating a therapeutic compound to an infected region via the bloodstream. The liposomes, which contain the agent in entrapped form, are composed of vesicle-forming lipids, a vesicle-forming lipid derivatized with hydrophilic biocompatible polymer, and have sizes in a selected size range between 0.07 and 0.2 microns. After parenteral administration, the liposomes are selectively taken up by the infected region within 24-48 hours, for release of entrapped compound into the infected region.

Abstract: This invention provides novel methods and reagents for specifically delivering biologically active compounds to phagocytic mammalian cells. The invention also relates to specific uptake of such biologically active compounds by phagocytic cells and delivery of such compounds to specific sites intracellularly. The invention specifically relates to methods of facilitating the entry of antiviral and antimicrobial drugs and other agents into phagocytic cells and for targeting such compounds to specific organelles within the cell. The invention specifically provides compositions of matter and pharmaceutical embodiments of such compositions comprising conjugates of such antimicrobial drugs and agents covalently linked to particulate carriers generally termed microparticles. In particular embodiments, the antimicrobial drug is covalently linked to a microparticle via an organic linker molecule which is the target of a microorganism-specific protein having enzymatic activity.

Abstract: The invention relates to the use of a mixture of(a1) a naturally occurring, zwitterionic phosphatide or a mixture of naturally occurring zwitterionic phosphatides and(a2) cholic acid and/or a salt of cholic acid and/or deoxycholic acid and/or a salt of deoxycholic acid and/or ricinoleic acid and/or a salt of ricinoleic acid and/or oleic acid and/or a salt of oleic acidas an emulsifier for the preparation of aqueous polymer dispersions which can be prepared by free radical emulsion polymerization of monomers which can be polymerized by free radicals or mixtures of monomers which can be polymerized by free radicals.

Abstract: A polar lipid composition of plant origin is provided for conveying an active agent and/or making it penetrate into a target cell. The composition is characterized in that it is comprised of an injectable, intra-articular, topical or ingestible aqueous emulsion of a polar lipid mixture rich in phospholipids, in glycolipids and in ceramides, having a composition which is substantially similar to that of the polar lipid constituents of lipid cytomembranes of cells. The mixture is obtained from a plant compound such as cereal flour or an extract such as bran or lipids extracted from cereals by means of chlorinated solvents.

Abstract: Compounds wherein therapeutic peptides, including HIV protease inhibitors, are covalently linked to phospholipids, glycerides or other membrane-targeting and membrane-anchoring species, and their pharmaceutically acceptable salts, together with processes for their preparation. The invention also provides novel HIV protease inhibitors. The compounds of the present invention possess useful pharmacological properties such as antiviral activity towards viral infection and inhibitory activity towards viral proteases. Therefore, these compounds can be used in the prophylaxis or treatment of viral infections, in particular infections caused by HIV and other retroviruses. The targeting technology as described for the protease inhibitors is also applicable to a variety of inhibitors of other enzymes.

Abstract: A method of reducing the extent to which microorganisms, particularly bacteria, will adhere to a surface, which comprises providing a surface having pendant groups of formula (I), in which each group R is the same or different and is alkyl of 1 to 4 carbon atoms and a is from 1 to 4, use of compounds containing a group of formula (I) in reducing the extent to which microorganisms would adhere to a surface and use of articles comprising such surfaces in environments susceptible to microorganism adhesion. The method has application in a wide variety of industrial or domestic fields wherever it is desirable to prevent growth of microorganisms as well as in the medical field.

Abstract: A composition of matter comprising a therapeutically active compound with antiseptic and osmotic characteristics for treatment or therapy for burns and open wounds experienced by animals and man and in particular to the treatment of thermal burns on humans by use of spray, mist, dropper or saturated bandage application of the solution disclosed. The compound in solution form composed of colloidal silver, helichrysum angustifolium or helichrysum italicum oil and raw honey emulsified with water soluble lecithin by agitation.

Abstract: A medicament for reduction of intraocular pressure comprises both carbachol and a locally applicable betablocker.

Abstract: The severity of metabolic disturbance in animals with cancer is mitigated by feeding the animal a nutritionally balanced food composition having a fat content of about 27 to 35%, on a dry matter basis, a carbohydrate content of about 15 to about 27% on a dry matter basis in which is present a mixture of arginine, omega-3 polyunsaturated fatty acids and omega-6 polyunsaturated fatty acids, the weight ratio of omega-3, omega-6 fatty acid being in the range of 0.3:1 to 3.5:1.

Abstract: This invention is directed to a homogenous water-in-perfluorochemical stable liquid dispersion for acceptable therapeutic administration of a drug to the lung of an animal. The dispersion includes a perfluorochemical liquid, water, surfactant and drug, wherein the water is homogeneously dispersed in the perfluorochemical to form a stable water-in-perfluorochemical liquid dispersion. The perfluorochemical constitutes greater than 50% by volume of the dispersion, and the drug is contained in the dispersion in an effective therapeutic amount.The invention further includes a method of delivering a drug to the lung of an animal. This aspect of the invention includes administering a stable homogenous water-in-perfluorochemical liquid dispersion to the animal lung or a section thereof. If desired, the method may further include delivering a breathable gas to the lung with a mechanical ventilator during the administration.