Abstract: The present invention relates to a pharmaceutical composition which includes morphine gluconate or chemical equivalent thereof. In one embodiment, the present invention includes a method of making morphine gluconate or chemical equivalent thereof by mixing morphine sulfate with sodium gluconate. The present invention also includes a method for eliciting an analgesic or anesthetic response in a mammal which includes administering a therapeutically effective amount of a pharmaceutical composition including morphine gluconate or chemical equivalent thereof.

Abstract: A lipid or other hydrophobic or amphiphilic compound (collectively referred to herein as “hydrophobic compounds”) is integrated into a polymeric matrix for drug delivery to alter drug release kinetics. In embodiments where the drug is water soluble, the drug is released over longer periods of time as compared to release from the polymeric matrix not incorporating the hydrophobic compound into the polymeric material. In contrast to methods in which a surfactant or lipid is added as an excipient, the hydrophobic compound is actually integrated into the polymeric matrix, thereby modifying the diffusion of water into the microparticle and diffusion of solubilized drug out of the matrix. The integrated hydrophobic compound also prolongs degradation of hydrolytically unstable polymers forming the matrix, further delaying release of encapsulated drug.

Abstract: A mixed micellar pharmaceutical formulation includes a micellar proteinic pharmaceutical agent, an lkali metal C8 to C22 alkyl sulphate, alkali metal salicylate, a pharmaceutically acceptable edetate and at least one absorption enhancing compounds. The absorption enhancing compounds are selected from the group consisting of lecithin, hyaluronic acid, pharmaceutically acceptable salts of hyaluronic acid, octylphenoxypolyethoxyethanol, glycolic acid, lactic acid, chamomile extract, cucumber extract, oleic acid, linolenic acid, borage oil, evening of primrose oil, trihydroxy oxo cholanylglycine, glycerin, polyglycerin, lysine, polylysine, triolein and mixtures thereof. The amount of each absorption enhancing compound is present in a concentration of from 1 to 10 wt./wt. % of the total formulation, and the total concentration of absorption enhancing compounds are less than 50 wt./wt. % of the formulation.

Abstract: The present invention provides a bilayer structure for encapsulating multiple containment units. These containment units can attach or contain therapeutic or diagnostic agents that can be released through the bilayer structure. A suitable example of such a containment unit is a unilamellar or multilamellar vesicle.

Abstract: The present disclosure relates to novel dosage forms, drug delivery regimens, methods and pharmaceutical compositions which optimize the therapeutic effects of active therapeutic substances through the application of the concept of uneven dosing.

Abstract: Methods and compositions are provided for enhancing the bioadhesive properties of polymers used in drug delivery systems. The bioadhesive properties of a polymer are enhanced by incorporating an anhydride oligomer into the polymer to enhance the ability of the polymer to adhere to a tissue surface such as a mucosal membrane. Anhydride oligomers which enhance the bioadhesive properties of a polymer include oligomers synthesized from dicarboxylic acid monomers, preferably those found in Krebs glycolysis cycle, especially fumaric acid. The oligomers can be incorporated within a wide range of polymers including proteins, polysaccharides and synthetic biocompatible polymers. In one embodiment, anhydride oligomers can be incorporated within polymers used to form or coat drug delivery systems, such as microspheres, which contain a drug or diagnostic agent. The oligomers can either be solubilized and blended with the polymer before manufacture or else used as a coating with polymers over existing systems.

Abstract: Compositions for suppositories comprising (A) a fatty base, (B) monodecanoyl-glycerol, (C) monolauroyl-glycerol, (D) a powder insoluble in fatty base and (E) a drug for suppositories capable of giving highly useful suppositories which sustain a melting point higher than the body temperature under dry storage conditions and thus remain stable without melting during storage but, when inserted into body cavity, quickly melt or gel.

Abstract: The present invention provides novel compositions and methods for using the S(+) enantiomer of desmethylselegiline (N-methyl-N-(prop-2-ynyl)-2-aminophenylpropane), for the treatment of selegiline-responsive diseases and conditions. Diseases and conditions responsive to selegiline include those produced by neuronal degeneration or neuronal trauma and those due to immune system dysfunction. Effective dosages are a daily dose of at least about 0.015 mg/kg of body weight.

Abstract: The present invention relates to a composition for the delivery of a pharmaceutical agent to a patient that comprises polyethylene glycol, an aqueous solution containing polyvinylpyrrolidone, and a pharmaceutical agent. The invention also relates to methods of making a composition for the delivery of a pharmaceutical agent.

Abstract: A solution or gel composition containing activated stabilized chlorine dioxide and phosphates, such as disodium hydrogen phosphate, sodium dihydrogen phosphate, trisodium phosphate, and sodium monofluorophosphate, is disclosed for destroying HIV. The preferred concentration ranges are between about 0.005%-2.0% chlorine dioxide, and between about 0.02%-3.0% phosphate. The phosphate compound retards escape of chlorine dioxide in the pH range of 6.0 to 7.4, at which pH stabilized chlorine dioxide becomes activated and releases sufficient chlorine dioxide to reduce motility and become lethal to the involved micro-organisms. Using a lubricant as a vehicle for the chlorine dioxide/phosphate composition; development of vaginal itching due to Candida Albicans will be stopped.

Abstract: The present invention provides a rectum applicable preparation containing an antidementia medicament, wherein the antidementia medicament is incorporated a triglyceride of a fatty acid and/or a water-soluble macromolecule.

Abstract: Disclosed is a method for the therapeutic treatment of pain related to wind up in a human or animal. The method of the invention is practiced by administering to the subject an effective amount of an analgesic pharmaceutical composition which includes a NMDA receptor antagonist in an immediate release form combined with an NMDA receptor antagonist in a sustained release form. The immediate release form and sustained release forn are present in sufficient amounts to diminsh or abolish wind up.

Abstract: This invention pertains to a method that can control, treat, and prevent Diabetes Mellitus. The method includes means of administering a potent product, including mainly the active ingredient Linalool, in any one of several forms, alone or with other additives and catalysts, such as vitamin E to enable the body to handle and control, then correct the complications of Diabetes Mellitus. A modest percentage of users suffering from this disease can be cured completely while the majority of others improve remarkably and experience lower blood glucose and reduce the glycated hemoglobin HbAlc readings to what are medically acceptable and healthy levels. Others, who are vulnerable to the disease due to hereditary factors, or other reasons, can help prevent it. The method works in several ways, including activation of the pancreas and re-establishing the ability of body cells to utilize and handle better and well, the glucose in the blood, and regulate the level of natural insulin in the body.

Abstract: Spontaneously dispersible concentrates capable of forming ultramicroemulsions are described. The concentrates include esters of formula (I) and (II): wherein (a) R1, R3, R4, and R5 each independently represents a C6-22 alkyl, a C6-22 alkenyl or a C6-22 alkapolyene and R2 is glucose:(1,2); (b) R2, R3, R4, and R5 each independently represents a C6-22 alkyl, a C6-22 alkenyl or a C6-22 alkapolyene and R1 is glucose:(1,3); (c) R2, R3, R4, and R5 each independently represents a C6-22 alkyl, a C6-22 alkenyl or a C6-22 alkapolyene and R1 is rhamnose:(1,4); or (d) R2, R3, R4, and R5 each independently represents a C6-22 alkyl, a C6-22 alkenyl or a C6-22 alkapolyene and R1 is rutinose:(1,5); wherein (a) R1, R2, and R4 each independently represents a C6-22 alkyl, a C6-22 alkenyl or a C6-22 alkapolyene and R3 is rhamnose:(11,7); or (b) R2 and R4 each independently represents a C6-22 alkyl, a C6-22 alkenyl or a C6-22 alkapolyene, R1 is methyl, and R3 is rutinose:(11,8).

Abstract: A delivery system is disclosed for delivering a beneficial agent to an animal. The delivery system comprises a wall that surrounds a lumen, said wall comprising a composition that limits the passage of fluid into the system and a composition that permits the passage of fluid into the system. The lumen comprises a beneficial agent and an expandable member. The delivery system comprises an exit means for delivering the beneficial agent.

Abstract: A method for decreasing the frequency of transmission of human immunodeficiency virus or herpesviruses or for preventing the transmission of or treating a sexually transmitted bacterial infection by administering to a human an anti-human immunodeficiency virus amount or an anti-herpesvirus amount or an anti-bacterial amount of cellulose acetate phthalate (CAP) or hydroxypropyl methylcellulose phthalate (HPMCP), such as in micronized form, or a combination thereof, either alone or in combination with a pharmaceutically acceptable carrier or diluent. The CAP and/or HPMCP may be employed as a suspension of micronized particles and may further contain a water miscible, non-solvent for CAP or HPMCP, such as glycerol.

Abstract: The present invention relates to preparations alleviating the symptoms caused by drying of the mucous membranes of the body. The preparations contain trimethylglycine as an active agent. The invention also relates to the use of trimethylglycine as an agent alleviating the symptoms of dry mucous membranes in different preparations intended for the body care and hygiene, and to a method of alleviating the symptoms, caused by drying, appearing on the mucous membranes of the body.

Abstract: A process for producing a small-sized, lipid-based cochleate is described. Cochleates are derived from liposomes which are suspended in an aqueous two-phase polymer solution, enabling the differential partitioning of polar molecule based-structure by phase separation. The liposome-containing two-phase polymer solution, treated with positively charged molecules such as Ca.sup.2+ or Zn.sup.2+, forms a cochleate precipitate of a particle size less than one micron. The process may be used to produce cochleates containing pharmaceutical agents or biologically relevant molecules. Small-sized cochleates may be administered orally or through the mucosa to obtain an effective method of treatment.

Abstract: Methods are provided for the therapy of immunodeficient, immunodepressed or hyperactive immune states and for the prevention and treatment of opportunistic infections in such states comprising administering to a subject a pharmaceutically acceptable composition comprising as an active ingredient the dipeptide L-Ile-L-Trp, linear and cyclic monomers and polymers thereof, and/or pharmaceutically acceptable salts thereof.

Abstract: The inventor provides suppositories comprising as the active ingredient 6-amino-5-chloro-1-isopropyl-2-(4-methyl-1-piperazinyl) benzimidazole (I). These suppositories are expected to exert drug effects based on serotonin.sub.3 antagonistic activity when administered rectally. More particularly, these suppositories are useful as antiemetic agents for vomiting accompanying chemotherapy for cancer or remedies for irritable bowel syndrome based on the serotonin.sub.3 antagonistic activity. These suppositories provide also excellent storage stability of benzimidazole derivative (I).

Abstract: Balanced pH, hyperosmotic, hypoosmotic, or isoosmotic gels are ideal vehicles for drug delivery. They are especially suited for topical body cavity or injection application of drugs or diagnostic agents; for drug or diagnostic agent delivery to the eye of a mammal; as protective corneal shields; or as ablatable corneal masks useful in laser reprofiling of the cornea. The compositions without the addition of a drug or diagnostic agent are useful as medical devices, for instance, in separating surgically or otherwise injured tissue as a means of preventing adhesions.

Abstract: Novel suppository pharmaceutical formulations of the platinum antitumor agent, JM216, are provided. Such dosage forms provide an alternative to the oral form currently available and offer improved bioavailability of this promising drug.

Abstract: There is provided a composition for rectal administration suitable for curing hemorrhoids or the like by which the concentration of a medicine in the affected tissue is increased and the potency of the medicine is expected to continue. The long acting composition for rectal administration includes an acrylic acid polymer, a vasoconstrictor and a rectal tissue-curing agent.

Abstract: Methods and compositions are provided for enhancing the bioadhesive properties of polymers used in drug delivery devices. The bioadhesive properties of a polymer are enhanced by incorporating a metal compound into the polymer to enhance the ability of the polymer to adhere to a tissue surface such as a mucosal membrane. Metal compounds which enhance the bioadhesive properties of a polymer include water-insoluble metal compounds such as water-insoluble metal oxides, including oxides of calcium, iron, copper and zinc. The metal compounds can be incorporated within a wide range of polymers including proteins, polysaccharides and synthetic biocompatible polymers. In one embodiment, metal oxides can be incorporated within polymers used to form or coat drug delivery devices, such as microspheres, which contain a drug or diagnostic agent.

Abstract: A method for treating or preventing urinary incontinence and other motility disorders involving the urethrogenital tract, by administering to a mammal an effective amount of the R-isomers of 4-diethylamino-2-butynyl cyclohexylphenylglycolate and 4-ethylamino-2-butynyl cyclohexylphenylglycolate and pharmaceutically acceptable salts thereof.

Abstract: A sustained-release microcapsule contains an amorphous water-soluble pharmaceutical agent having a particle size of from 1 nm-10 .mu.m and a polymer. The microcapsule is produced by dispersing, in an aqueous phase, a dispersion of from 0.001-90% (w/w) of an amorphous water-soluble pharmaceutical agent in a solution of a polymer having a wt. avg. molecular weight of 2,000-800,000 in an organic solvent to prepare an s/o/w emulsion and subjecting the emulsion to in-water drying.

Abstract: This invention is directed to a suppository-based vaccine delivery system for immunizing against urogenital infectious disease in humans and a method for treating same. More particularly, this invention is directed to a suppository-based vaccine delivery system for the prophylaxis against urogenital infectious diseases, such as urinary tract infections. The suppository-based vaccine delivery system is comprised of a vaccine comprised of inactivated bacteria which originate from cultures of 8 to 14 uropathogenic bacteria strains of the species: Escherichia coli, Klebsiella pnieumoniae, Proteus mirabilis, Proteus morganii, and Streptococcus faecalis; and polyethylene glycol suppository base; wherein the suppository is adapted to be inserted into a bodily orifice of a human so as to allow the suppository to be in contact with tissue of the bodily orifice to facilitate transfer of suppository material therethrough.

Abstract: This invention relates to formulations comprising film-forming components capable of forming per se a physical barrier to pathogens. Thermoreversible gels such as poloxamers are particularly preferred for that use. The film-forming formulations may further comprise microbicides, spermicides or any other drug, which choice is guided by the pathogen, organism or the disease to be inactivated or treated. The formulations are therefore efficient as a physical, and optionally, as a chemical or pharmacological barrier as well as usable as a sustained drug-release system at the locus of administration. A part of the drug may also be entrapped in liposomes or other drug carriers. These formulations are intended for use in the prevention of sexually transmitted diseases, as well as in the treatment of infections, cancer, inflammation or any disease or state which requires a pharmacological treatment. Formulations are applicable to mucosae, skin and eye, for example.

Abstract: The analgesic effectiveness of an analgesic selected from the group consisting of (R)-5-(2-azetidinylmethoxy)-2-chloropyridine, (S)-5-(2-azetidinylmethoxy)-2-chloropyridine and pharmaceutically acceptable salts thereof is significantly potentiated by administering an analgesic-potentiating amount for said analgesic of at least one nontoxic NMDA receptor antagonist.

Abstract: A liquid composition for the controlled release of gonodotropin releasing hormone (GnRH) or its analogs 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) GnRH or analogs thereof.

Abstract: The present invention provides novel compositions and methods for using the S(+) enantiomer of desmethylselegiline (N-methyl-N-(prop-2-ynyl)-2-aminophenylpropane), for the treatment of selegiline-responsive diseases and conditions. Diseases and conditions responsive to selegiline include those produced by neuronal degeneration or neuronal trauma and those due to immune system dysfunction. Effective dosages are a daily dose of at least about 0.015 mg/kg of body weight.

Abstract: Its subject is more specifically a process for making suppositories releasing carbon dioxide and endowed with a laxative action in which the fatty substances are melted separately and vegetable lecithin is added into the fluid mass resulting from the melting and then a mineral opacifying agent is incorporated, followed by the pouring of potassium acid tartrate and sodium bicarbonate accompanied by stirring, these two constituents having a particular granulometry, and stirring is then continued until perfect homogeneity is achieved before proceeding with the drawing-off of the fluid suspension.

Abstract: A galactolipid material from wheat, produced by extraction of crushed wheat grains and subsequent chromatography of the extracted material, and having a content of DGDG of 51.5%, was mixed with the polar solvents, water and glycerol in order to test the swellability. The samples, prepared in glass tubes, were alternately mixed with a rod and centrifugated at room temperature until homogeneous. The samples were inspected as to physical appearance after storing for at least a week at room temperature.Results:20% (w/w) of galactolipid material in water gave a slightly yellow, highly viscous dispersion. Small liposomes could be observed in a polarizing microscope. At higher galactolipid concentrations a stiff gel was formed.10% (w/w) of the same lipid material in anhydrous glycerol resulted in the formation of an opaque, highly viscous gel.

Abstract: Levobupivacaine or ropavicaine is used to treat migraine.

Abstract: Described is the use of vitamin E in topically applied compositions for the purpose of enhancing the penetration of therapeutically effective (cosmetically or pharmaceutically-active) drug or cosmetic ingredients. The topical compositions containing the penetration-enhancing concentration of vitamin E may be provided in a variety of forms including semi-solid (gel, paste, cream, lotion, ointment, etc.), liquid, suspension, film or laminate.

Abstract: (Meth)acrylic acid/maleic acid copolymers for improving mucosal permeability and pharmaceutical compositions containing them are described.

Abstract: A water soluble biodegradable ABA-type block copolymer made up of a major amount of hydrophobic poly(lactide-co-glycolide) copolymer A-blocks and a minor amount of a hydrophilic polyethylene glycol polymer B-block, having an overall average molecular weight of between about 3100 and 4500, possesses reverse thermal gelation properties. Effective concentrations of the block copolymer and a drug may be uniformly contained in an aqueous phase to form a drug delivery composition. At temperatures below the gelation temperature of the copolymer the composition is a liquid and at temperatures at or above the gelation temperature the composition is a gel or semi-solid. The gelation temperature is preferably at or below body temperature of a warm-blooded animal. The composition may be administered to a warm-blooded animal as a liquid by parenteral, ocular, topical, transdermal, vaginal, transurethral, rectal, nasal, oral, or aural delivery means and is a gel at body temperature.

Abstract: A method of treatment of osteo-articular disease which includes administering an effective amount of a pharmaceutical composition containing a compound of specified formula and an excipient to a patient in need of such treatment. The compounds of specified formula have a phosphonate group on one end and a silanol or silanol precursor on the opposite end, and can inhibit serine proteases.

Abstract: The invention relates to novel methods for making oil-in-water emulsions having mucoadhesive properties which are primarily intended for administration of biologically active compounds to mucosal surfaces. 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 phase of a fat or oil which forms a hydrophobic core that is surrounded by a surfactant layer. The emulsion further includes 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 surrounding the hydrophobic one. A biologically active compound may also be included, if desired.

Abstract: Bioadhesive/mucoadhesive composition in a suspension or emulsion form that delivers drugs to the target tissue in a sustained manner is formulated. A composition, method of manufacture and its application in treatment of mammalian tissue are disclosed. The composition includes a bioadhesive/mucoadhesive polymer in an emulsion or suspension form along with a treating agent. The treating agent could be as simple as water as in the case of mucoadhesive moisturizing agent. The bioadhesive/mucoadhesive polymer is a water dispersible high molecular weight crosslinked polyacrylic acid copolymer with free carboxylic acid groups further crosslinked with a combination mono, di and polyvalent metal ions, cationic polymers and surfactants. Type of metal ion and their concentration can be adjusted to get the desired bio/mucoadhesive properties along with several physical properties that are important to the formulation of dosage forms.

Abstract: The invention relates to a pharmaceutical composition containing an association of active principles, wherein the active principles are clopidogrel and aspirin, each constituent being present in a free form or in the form of a pharmaceutically acceptable salt.

Abstract: Compositions and methods for delivering agents across cell membranes are disclosed. The compositions include an agent to be delivered, a viscous material, such as a hydrogel, lipogel or viscous sol, and, optionally, a carrier that includes a ligand that binds to or interacts with cell surface receptors. The agent to be delivered binds to or otherwise interacts with cell surface receptors, is attached, either covalently or ionically to a molecule that binds to or interacts with a cell surface receptor, or is associated with the carrier. Agents to be delivered include bioactive compounds and diagnostic agents. The compositions have an apparent viscosity roughly equal to the viscosity of the cytosol in the cell to which the agent is to be delivered. The rate of cellular internalization is higher when the viscosity of the viscous material and that of the cytosol in the cell are approximately the same, relative to when they are not the same.

Abstract: A method for decreasing the frequency of transmission of human immunodeficiency virus or herpesviruses by administering to a human an anti-human immunodeficiency virus amount or an anti-herpesvirus amount of cellulose acetate phthalate (CAP) or hydroxypropyl methylcellulose phthalate (HPMCP), such as in micronized form, or a combination thereof, either alone or in combination with a pharmaceutically acceptable carrier or diluent. The CAP and/or HPMCP may be employed as a suspension of micronized particles and may further contain a water miscible, non-solvent for CAP or HPMCP, such as glycerol.

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 medicament for use in the treatment of anorectal inflammation in hemorrhoids and the like contains a petroleum base, water, phenylephrine hydrochloride, squalene, and 8-hydroxyquinoline.

Abstract: The availability of serotonin, norepinephrine and dopamine in the brain is increased by administering a serotonin reuptake inhibitor with a serotonin 1A antagonist and L-tryptophan or 5-hydroxy-L-tryptophan.

Abstract: Balanced pH, hyperosmotic, hypoosmotic, or isoosmotic gels are ideal vehicles for drug delivery. They are especially suited for topical body cavity or injection application of drugs or diagnostic agents; for drug or diagnostic agent delivery to the eye of a mammal; as protective corneal shields; or as ablatable corneal masks useful in laser reprofiling of the cornea. The compositions without the addition of a drug or diagnostic agent are useful as medical devices, for instance, in separating surgically or otherwise injured tissue as a means of preventing adhesions.

Abstract: The present disclosure relates to novel dosage forms, drug delivery regimens, methods and pharmaceutical compositions which optimize the therapeutic effects of active therapeutic substances through the application of the concept of uneven dosing.

Abstract: This invention relates to (R)-5-(aminosulphonylmethyl)-3-(N-methylpyrrolidin-2-ylmethyl)-1H-indole and its pharmaceutically acceptable salts. This compound is particularly useful in treating disorders arising from deficient serotonergic neurotransmission, especially migraine.

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.