Abstract: A formulation and methods for inducing sustained regional local anesthesia in a patient comprising a substrate comprising a local anesthetic and an effective amount of a biocompatible, biodegradable, controlled release material prolonging the release of the local anesthetic from the substrate to obtain a reversible local anesthesia when implanted or injected in a patient, and a pharmaceutically acceptable, i.e., non-toxic, non-glucocorticoid augmenting agent effective to prolong the duration of the local anesthesia for a time period longer than that obtainable from the substrate without the augmenting agent.

Abstract: A medicament for nasal administration to be used for disease prevention or treatment comprising a vaccine or a pharmacologically active peptide compounded with an ion exchange resin or adsorbent resin powder whose mean particle size is not larger than 200 .mu.m.

Abstract: A stable solution, cream, salve, or spray composition containing activated chlorine dioxide and phosphates, such as disodium hydrogen phosphate, sodium dihydrogen phosphate, trisodium phosphate, and sodium monofluorophosphate, is disclosed for the treatment of vaginitis and endometriosis by reducing any of Candida, Actinobacillus actinomycetemcomitans, Pseudomonades, and Porphyromonas gingivalis present in the vagina or the uterus. The preferred concentration ranges are in the range of about 0.005% to about 2.0% of chlorine dioxide, and in the range of about 0.02% to about 3.0% of phosphate. The phosphate compound retards escape of chlorine dioxide in the pH range of 6.0 to 7.4, at which pH chlorine dioxide becomes activated and releases sufficient chlorine dioxide to reduce motility and become lethal to the involved micro-organisms.

Abstract: The use of .alpha.,.alpha.-diphenylacetic acid-4-(N-methyl-piperidyl) ester for the treatment of painful muscular cramp conditions in the region of the abdominal cavity or for the production of drugs for the treatment of painful muscular cramp conditions in the region of the abdominal cavity.

Abstract: A method for preventing, ameliorating, and/or treating memory and other cognitive disorders associated with aging, such as Age-Associated Memory Impairment (also known as Age-Related Cognitive Decline), and other age-related impairments of, and/or changes in, cognitive function. The method comprises administering to a subject a therapeutically effective amount of a lipid-soluble thiamine or a prodrug thereof in an amount averaging from about 0.02 to about 0.5 grams per day per 70 kg body weight over a period of three months or longer.

Abstract: The present invention relates to methods and compositions for the prevention and/or treatment of diabetes mellitus, using magnesium gluconate alone or in combination with one or more antioxidants or conventional diet and/or insulin therapy. The invention also relates to inhibition of production of oxygen free radicals and lipid peroxidation.

Abstract: In accordance with the present invention, there are provided in vivo methods for the reduction of cyanide levels. The present invention employs a scavenging approach whereby cyanide is bound in vivo to a suitable scavenger. The resulting complex renders the cyanide harmless, and is eventually excreted in the urine of the host. Further in accordance with the present invention, there are provided compositions and formulations useful for carrying out the above-described methods.

Abstract: A compound preparation for the treatment of hypogonadal men and men with hypophyseal diseases. This invention relates to compound preparations containing biogenous or synthetic androgens and biogenous or synthetic estrogens that are used for the treatment of imbalances of the testosterone metabolism in old age, of hypogonadal men, and of men with hypophyseal diseases. These compound preparations are present in various galenic formulations such as ointments, gels, sprays, TTS systems, tablets, lozenges, capsules, and suppositories. These preparations are used to treat the fluctuations of the testosterone metabolism occurring in old age and with certain diseases such as hypophyseal diseases (adenoma), hypogonadism and/or metabolic syndrome, to maintain the balance between androgens and estrogens found in young and healthy men in ill and/or elderly men as well.

Abstract: A method, and compositions for use therein capable, of delivering a bioactive agent to an animal entailing the steps of encapsulating effective amounts of the agent in a biocompatible excipient to form microcapsules having a size less than approximately ten micrometers and administering effective amounts of the microcapsules to the animal. A pulsatile response is obtained, as well as mucosal and systemic immunity.

Abstract: Therapeutic compounds and methods for inhibiting amyloid deposition in a subject, whatever its clinical setting, are described. Amyloid deposition is inhibited by the administration to a subject of an effective amount of a therapeutic compound comprising an anionic group and a carrier molecule, or a pharmaceutically acceptable salt thereof, such that an interaction between an amyloidogenic protein and a basement membrane constituent is inhibited. Preferred anionic groups are sulfonates and sulfates. Preferred carrier molecules include carbohydrates, polymers, peptides, peptide derivatives, aliphatic groups, alicyclic groups, heterocyclic groups, aromatic groups and combinations thereof.

Abstract: A method and composition are disclosed utilizing the pure (R,R) isomer of formoterol, which is a potent bronchodilator with reduced adverse effects, having a low incidence of the development of tolerance and having increased bronchial distribution when administered by inhalation.

Abstract: Ulinastatin-containing suppository is produced by emulsifying an aqueous solution of ulinastatin in an oily base uniformly in the presence of an emulsifier and then solidifying the emulsion.The ulinastatin-containing suppository exhibits high stability even if it is stored for a prolonged time. In addition, it can be manufactured on an industrial scale.

Abstract: A transmucosal drug delivery device in the form of a sheet material. The device contains an acid-containing particulate polymeric resin dispersed throughout a polytetrafluoroethylene support matrix.

Abstract: Drug delivery systems and methods for administering a glucagon-like insulinotropic peptide to the buccal mucosa for transmucosal drug delivery are described. The drug delivery systems comprise a drug composition containing an effective amount of the glucagon-like insulinotropic peptide and an effective amount of a permeation enhancer for enhancing permeation of glucagon-like insulinotropic peptide through the buccal mucosa and means for maintaining the drug composition in a drug transferring relationship with with buccal mucosa. These systems can be in free form, such as creams, gels, and ointments, or can comprise a device of determined physical form, such as tablets, patches, and troches. A preferred glucagon-like insulinotropic peptide is GLP-1(7-36)amide.

Abstract: Topical formulations comprising an anti-irritant amount of aqueous-soluble lithium (Li.sup.+) or potassium (K.sup.+) cation, and methods for using the same to inhibit skin irritation, are disclosed.

Abstract: The present invention provides novel uses of compounds of general formula I: ##STR1## wherein R.sup.1, R.sup.4 and R.sup.5 are individually hydrogen, hydroxy, halogen, trifluoromethyl, lower alkyl, lower alkoxy or (tertiary amino)(lower alkoxy); and R.sup.2 and R.sup.3 are individually hydrogen or lower alkyl, or as a pharmaceutically acceptable salt thereof in combination with a pharmaceutically acceptable carrier for the manufacture of a pharmaceutical composition for the treatment or prophylaxis of atrophy of skin and/or mucous membranes.

Abstract: A composition for the controlled release of substances is provided that includes: (i) a non-polymeric, non-water soluble liquid carrier material (HVLCM) of viscosity of at least 5,000 cP at 37.degree. C. that does not crystallize neat under ambient or physiological conditions; and (ii) a substance to be delivered.

Abstract: Compositions for delivery of pharmacologically active agents and methods for their administration are provided. In one embodiment, the compositions include a complex of a polycationic polymer and a pharmacologically active agent in a pharmaceutically acceptable carrier. The compositions in one embodiment permit transport of pharmacologically active compounds across mucosal membranes for systemic delivery. The polycationic polymer may be, for example, a polycationic carbohydrate such as a chitosan or a chitosan salt or derivative. The therapeutic agent a preferred embodiment is a vaccine or a nucleic acid, such as a gene or antisense oligonucleotide. The composition may be provided in different forms such as a solution, dispersion, powder or in the form of microspheres.

Abstract: The invention relates to an oil-in-water emulsion and related method for administration of a drug to a mucosal surface. The emulsion has an aqueous continuous phase and a plurality of submicron particles having an average particle diameter of from 10 nm to 600 nm, with the particles having a hydrophobic core of a fat or oil which is surrounded by a surfactant layer. The emulsion further includes a drug and a mucoadhesive polymer which is a polymer or copolymer of acrylic acid or methacrylic acid, a poly(methyl vinyl ether/maleic anhydride) copolymer, pectin, alginic acid, hyaluronic acid, chitosan, gum tragacanth, karaya gum or carboxymethylcellulose. The hydrophobic core has less than 1% (w/w) protein, relative to the weight of the hydrophobic core, and the emulsion contains less than 5% (w/w) surfactant, relative to the weight of the hydrophobic core.

Abstract: Gelled vaginal pharmaceutical composition containing:a water-soluble bioadhesive polymer, a peroxide source and pH buffer wherein the composition has a pH between about 3.0 and about 6.0; and methods of using same.

Abstract: A composition for a foam and a process for preparing it are provided, the composition including by weight (a) more than 25% of an active ingredient in powder form; (b) from 1 to 20% of a surfactant; the balance being composed of water, wherein the powder of the active ingredient has a particle size below 20 .mu.m. Foams, notably for rectal administration, containing this composition with a propellant gas are also provided.

Abstract: Pharmaceutical compositions comprising a calcitonin and a polyglycolysed glyceride and a method of enhancing the transdermal or transmucosal absorption of calcitonin in a mammal are disclosed.

Abstract: In a preferred embodiment, drugs having pharmacological properties which are useful in the medicinal therapy of fibrotic disease for the reparation and prevention of fibrotic lesional tissues, such drugs including as active ingredient(s) one or more N-substituted 2-(1H) pyridone(s) and/or N-substituted 3-(1H) pyridones. The composition of this invention is novel as an anti-fibrotic drug, namely, as an agent for treating fibrosis. Any existing compounds have not been shown to be effective for the reparation and prevention of fibrotic lesions.

Abstract: This invention relates to a composition, and method of forming said composition, for the controlled release of interferon. The controlled release composition of this invention comprises a biocompatible polymer and particles of metal cation-stabilized interferon, wherein the particles are dispersed within the biocompatible polymer.The method of the invention, for producing a composition for the controlled release of interferon, includes dissolving a polymer in a polymer solvent to form a polymer solution, dispersing particles of metal cation stabilized-interferon particles in the polymer solution, and then solidifying the polymer to form a polymeric matrix containing a dispersion of the interferon particles.

Abstract: A small, reusable, previously cooled or frozen bladder that is applied to the anal area of a user. The bladder consists of two two-ply sheets of a flexible, semi-porous material, such as polyethylene, hermetically heat sealed together at the edges to form an internal cavity. The cavity contains a cold-temperature storage means, such as water, glycerol, a combination thereof, or other chemical slurry, and a medicinal agent, such as witchhazel, shark oil, yarrow, other astringents, and lidocaine or other pain relievers.

Abstract: Water-soluble pressure-sensitive adhesives include a water-soluble polymer that is made tacky at room temperature by addition of a water-soluble plasticizer that is miscible with the polymer. Suitable polymers are solid at room temperature; and have a hydrophilicity as measured by water uptake greater than about 25%; they are liquid at room temperature and have a boiling point higher than about 80.degree. C. The adhesives according to the invention may conveniently be provided in dry film form. Preferred water-soluble pressure-sensitive adhesives of the invention adhere both to mucosal surfaces and to a variety of materials that may constitute a part of a device or prosthesis to be held in a body cavity that has a mucosal lining. Also, a laminated device for the controlled release of a substance within a mucosa-lined body cavity includes the substance dissolved or dispersed in either or both of a water-soluble pressure-sensitive adhesive layer and optionally one or more water-soluble polymer layers.

Abstract: The invention relates to the use of a substance P antagonist for the preparation of a pharmaceutical composition, in particular for topical application, for treating lichens, prurigo, pruriginous toxicoderma and severe pruritus of neurogenic origin.

Abstract: Vitamin B12 is used to stimulate heme oxygenase production. In turn, levels of the molecules 12(R)-HETE and 12(R)-DIHETE, which are arachidonic acid derivatives, are reduced. Various topical formulations containing vitamin B12, but no other vitamins, are described.

Abstract: Bioadhesive pharmaceutical composition for the controlled release of active principles locally across the buccal cavity or systemically across a mucous membrane, wherein it is composed of an active principle, a compound (A), a compound (B) and excipients as defined in the description.

Abstract: A method for preparing a pharmaceutical microdispersion exhibiting enhanced bioavailability, including the steps of providing a thermodynamically stable pharmaceutical composition comprising at least one lipophilic pharmaceutical agent incorporated in a physiologically acceptable liquid carrier, the liquid carrier comprising one or more lipophilic solvents such as fluorochemicals and preferably at least one nonfluorinated co-solvent, and combining the stable pharmaceutical composition with an amount of at least one miscible diluent sufficient to initiate phase separation of the lipophilic pharmaceutical agent from the pharmaceutical composition wherein a microdispersion of the pharmaceutical composition is formed. Also disclosed are microdisperse pharmaceutical compositions and kits for forming such compositions.

Abstract: A composition comprising material from the following herbs: Panax pseudo-ginseng Wall, Isatis Indigotica Fort, Ganoderma lucidum Karst, Dendranthema morifolium Tzvel, Glycyrrhiza glabra L., Scutellaria baicalensis Georgi, Rabdosia rubescens, Serenoa repens. Preferably, the material from each of such herbs is an alcohol extract of dried, cut plants and of the Panax the pseudo-ginseng Wall and each of the other materials are present in a dried, weight-to-weight range of about 1:1-6. The composition is administered orally or by suppository.

Abstract: The present invention relates to a matrix for sustained-release preparation comprising an ester formed at a terminal carboxyl group of a straight-chain polyester which essentially consists of an .alpha.-hydroxymonocarboxylic acid. The matrix is stable to light, heat, moisture, coloring etc., and is of low toxicity. The sustained-release preparation produced by using the ester of the present invention offers stable drug release over an extended period of time, ensuring sustained stable effect. Furthermore, the sustained-release preparation does not show excess drug release just after administration.

Abstract: Emu oil is therapeutically used in methods for lowering cholesterol, triglycerides and low density lipoproteins and increasing high density lipoproteins; preventing and treating allergies; preventing scarring; treating headaches; preventing nose bleeds; treating and preventing cold and flu symptoms; and relieving discomfort associated with menstruation. Additionally, emu oil acts as an effective chemical buffer in combination with glycolic acid.

Abstract: The invention relates to an anti-emetic composition that comprises dexamethasone (DEX), metoclopramide (MTC) and an antihistamine or an anticholinergic agent. In a particular embodiment, a composition containing DEX:MTC:diphenhydramine in a relative weight ratio of about 1:1:2.5, respectively, is found to be effective in providing relief from the discomfort caused by symptoms of both vomiting and nausea in all patients receiving the composition. Alternatively, an effective composition may contain DEX:MTC:scopolamine in a relative weight ratio of about 1:1:0.025, respectively. Other effective compositions and methods of their use are also disclosed.

Abstract: A method for combatting cellulitis or reducing localized fatty excesses involves administering a body slimming amount of a composition which contains, as the sole slimming agent, an .alpha.-tocopherol, benzyl, xanthinol or hexyl nicotinate, or .alpha.-tocopherol acetate.

Abstract: The use of nor- and homo-bile acids derivatives as absorption enhancers for medicaments is described. Said derivatives show the advantage of improving the absorption of medicaments through mucosae without being metabolized by the intestinal flora, thus allowing a fast excretion. Moreover, the derivatives of the invention have a negligible toxicity.

Abstract: This invention relates to the use of L-acylcarnitine for the preparation of a drug and a technique for relieving the disease symptoms appearing in AIDS by administering an L-acylcarnitine. The invention furthermore relates to a drug for this purpose, characterized in content by L-acylcarnitine as active principle. The preferred L-acylcarnitine is L-acetylcarnitine.

Abstract: The present invention relates to novel formulations and combinations of lipophilic and hydrophilic antioxidants and the use thereof in the therapeutic, foodstuff, dietetic, and cosmetic fields. These formulations are based on the use of carotenoids, procarotenoids and derivatives thereof with polyphenols of catechic structures. Said formulations, containing a lipophilic antioxidant and an hydrophilic one, can be used in the prevention of physiopatological conditions related at least partially to an over-production of free radicals, particularly aging, atherosclerosis and cancer.

Abstract: Therapeutic compounds and methods for inhibiting amyloid deposition in a subject, whatever its clinical setting, are described. Amyloid deposition is inhibited by the administration to a subject of an effective amount of a therapeutic compound comprising an anionic group and a carrier molecule, or a pharmaceutically acceptable salt thereof, such that an interaction between an amyloidogenic protein and a basement membrane constituent is inhibited. Preferred anionic groups are sulfonates and sulfates. Preferred carrier molecules include carbohydrates, polymers, peptides, peptide derivatives, aliphatic groups, alicyclic groups, heterocyclic groups, aromatic groups and combinations thereof.

Abstract: This invention is a long acting moisturizer particularly suited for moisturizing the epithelia.

Abstract: Disclosed are methods and compositions for the suppression of expression of the neu oncogene, as well as suppression of neu oncogene-mediated transformation, tumorigenesis and metastasis. The method disclosed involves introduction of adenovirus early 1A gene (the E1A gene) products, so to large T antigen (the LT gene product), or both into affected cells. These products, which are preferably introduced by transfection of the E1A gene into affected cells, serve to suppress neu gene expression as measured by a reduction of p185 expression. Furthermore, the E1A gene products surprisingly serve to suppress the oncogenic phenotype, as indicated by a reduction in cell growth, growth in soft agar, as well as tumorigenic and metastatic potential in vivo. The inventors propose that E1A gene products, LT gene products or derivatives therefrom, may ultimately be employed a treatment modalities for neu-mediated cancers, such as cancers of the female genital tract and breast.

Abstract: Zinc(II) complexes and methods relating thereto are disclosed. The zinc(II) complexes comprise a zinc(II) ion complexed by a multi-dentate ligand. Methods of this invention include the use of the zinc(II) complexes as anti-viral agents and/or as anti-inflammatory agents. Methods of this invention also include inhibition of viral infection, as well as inhibiting transmission of sexually transmitted diseases. Exemplary zinc(II) complexes include zinc(II):neocuproine (2:1) and zinc(II):bathocuproine disulfonic acid (2:1).

Abstract: A method for treating atopic dermatitis, hayfever, asthma and pruritis that includes topical or systemic application of an effective amount of buspirone or a buspirone derivative or its pharmaceutically acceptable salt, other than a quaternary salt, optionally in a pharmaceutically-acceptable diluent or carrier.

Abstract: The present invention relates to a composition for rectal administration which comprises a benzimidazole compound having antiulcer activity and a salt of C.sub.6-20 fatty acid, both of which are intermingled with each other in a base for rectal administration.The composition for rectal administration of the present invention is effective for the treatment of gastrointestinal ulcers, is excellent in the stability of the active ingredient therein and the absorption thereof to thereby insure an early attainment of therapeutically effective blood concentration and permits control of the rate of absorption of the drug. Furthermore, the composition for rectal administration of the present invention swells in the intestinal tract, attaches itself to the mucosa, and releases the active ingredient gradually over a long time to supply the drug at a high concentration and with high efficiency. Therefore, the expected therapeutic efficacy can be obtained at a low dosage level with a minimum of side effect.

Abstract: Suppositories, produced by a process in which a suppository basic mass is produced containing (a) 50-75% of 5-aminosalicylic acid as an active ingredient, (b) 2-5% talc, magnesium stearate and/or polyvinyl pyrrolidone and (c) 20-48% by weight of a polyethylene glycol having an average molecular weight of at least 4000, and the produced mass is compressed to suppositories in a tabletting machine.

Abstract: A method is disclosed for using a topical genital lubricant with a non-toxic, non-irritating zinc salt during sexual intercourse. The lubricant is spread upon one or more genital surfaces to create an anti-viral chemical barrier that reduces the risk of infection by the human immunodeficiency virus (HIV), the virus that causes AIDS. Suitable zinc salts include zinc acetate, zinc propionate, and other non-irritating water-soluble organic zinc salts that dissociate readily. When dissolved in water, these salts release divalent zinc ions (Zn.sup.++), which apparently can reduce HIV infectivity by at least three mechanisms. First, zinc ions form crosslinking bonds with cysteine and histidine residues in proteins (such as the gp120 protein of HIV), thereby "gluing" HIV particles to each other, to proteins in vaginal fluids, and to dead or dying cells that will soon be sloughed off from the genital surfaces. This reduces the ability of the HIV to infect susceptible cells.

Abstract: Atopic eczema, breast pain or premenstrual syndrome are treated by administering to a person in need of same a composition containing at least 20% di-linoleoyl-mono-gamma-linolenyl glycerol by weight.

Abstract: Atopic eczema, breast pain or premenstrual syndrome are treated by administering to a person in need of same a composition containing at least 20% di-linoleoyl-mono-gamma-linolenyl glycerol by weight.

Abstract: A sustained release medicinal preparation is produced by enclosing a macrocyclic compound represented by 17-allyl-1,14-dihydroxy-12-[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylviny l)-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1 .0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone or 17-ethyl-1,14-dihydroxy-12-[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylviny l]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1 .0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone, into the fine particles generally called microspheres which arc made of biodegradable polymer. This preparation, when, for example, given by injection, appreciably improves the transferance of said macrocyclic compound into the blood. Further, this is also used as an agent suitable for topical administration.

Abstract: A topical treatment for hemorrhoidal pain and for spasms of the sphincters and muscles located in the gastrointestinal (GI) tract is disclosed. The topical preparation includes the amino acid L-arginine in a pharmaceutically acceptable carrier substance, e.g., K-Y jelly, suppository, or ingestible formulation, and can be applied directly to the affected area. The topical preparation of the invention is effective for relieving the pain of hemorrhoids or for treating conditions resulting from spasms of sphincters of the GI tract including anal fissure, post operative rectal pain, hypertrophic pyloric stenosis, and pancreatitis, as well as conditions resulting from general spasm of the muscles of the GI tract.