Abstract: A method of vehicle modulated administration of an anticonvulsive agent to the nasal mucous membranes of humans and animals is disclosed. The vehicle system is an aqueous pharmaceutical carrier comprising an aliphatic alcohol, a glycol and a biological surfactant such as a bile salt or a lecithin. The pharmaceutical composition provides a means to control and promote the rate and extent of transmucosal permeation and absorption of the medicaments via a single and multiple administration. Nasal administration of the pharmaceutical preparation produces a high plasma concentration of the anticonvulsant nearly as fast as intravenous administration. Such compositions are particularly suitable for a prompt and timely medication of patients in the acute and/or emergency treatment of status epilepticus and other fever-induced seizures.

Abstract: This invention discloses a pharmaceutical formulation for nasal administration which contains a pharmaceutically active polypeptide and a method producing the pharmaceutical formulation. The pharmaceutical for formulation comprises: (1) a pharmaceutically active polypeptide, (2) at least one compound selected from the group consisting of taurine, an ester thereof with C1˜6 alcohol, a base metal salt of taurine, hyaluronic acid and a base metal of hyaluronic acid and (3) at least one pharmacologically acceptable additive. It exhibited excellent pharmaceutical activity. No adverse effects such as irration were observed and hence, the present pharmaceutical formulation may suitably be administered nasal mucosa.

Abstract: Methods of preparing particulates for agglomeration, having a specified particle size distribution and desired convertible amorphous content, are described. The method involves a plurality of micronizing steps at least two of which are separated by a curing step. In the curing step, a stimulus such as humidity may be used to crystallize at least some, and in many instances preferably all, of the convertible amorphous content.

Abstract: A mixed micellar pharmaceutical formulation includes a micellar proteinic pharmaceutical agent, an alkali 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 cholanyiglycine, 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 invention is directed to self-assembling, polymer-based delivery systems for proteins. The delivery systems comprises an active agent and a polyol ester of the invention, having a linear polyol containing six or more hydroxyl groups as a central backbone and biodegradable hydroxy carboxylic ester groups attached to the central backbone.

Abstract: A composition of matter including a therapeutic or a cosmetic agent and at least one stinging capsule and methods of use are described.

Abstract: Provided is a sustained release composition for sustained release of a pharmaceutical substance. The composition includes a biocompatible polymer that is highly amorphous and a pharmaceutical substance in a hydrophobic ion complex with an amphiphilic material. Also provided is a compressed antisolvent method for manufacturing the composition, various product forms incorporating the composition and various uses for the composition.

Abstract: Compounds of the general formula P1-L-P2; wherein “P1” is a pyrazinoylguanidine sodium channel blocker, “L” is a linking group, and “P2” is either (i) a pyrazinoylguanidine sodium channel blocker or (ii) a P2Y2 receptor agonist, are disclosed. Pharmaceutical formulations containing the same and methods of use thereof to hydrate mucosal surfaces such as airway mucosal surfaces are also disclosed.

Abstract: The present invention is directed to a method for treating the symptoms associated with fibromyalgia and related conditions by administering flupirtine.

Abstract: Immune response modifier compounds—imidazoquinoline amines, imidazopyridine amines, 6,7-fused cycloalkylimidazopyridine amines, and 1,2-bridged imidazoquinoline amines—are useful for the treatment of TH2 mediated diseases by administering a therapeutically effective amount of such compounds in order to inhibit TH2 immune response, suppress IL-4/IL-5 cytokine induction and eosinophilia, as well as enhance TH1 immune response.

Abstract: Mucosal adjuvants for vaccines contain water-soluble polyanionic polymers which have anionic constitutional units obtained from acids such as acrylic acid, methacrylic acid, maleic acid, fumaric acid, ethylsulphonic acid, vinylsulphuric acid, vinylsulphonic acid, styrenesulphonic acid, vinylphenylsulphuric acid, 2-methacryloyloxyethane sulphonic acid, 3-methacryloyloxy-2-hydroxypropanesulphonic acid, 3-methacryl amido-3-methylbutanoic acid, acrylamidomethylpropanesulphonic acid, vinylphosphoric acid, 4-vinylbenzoic acid, 3-vinyl oxypropane-1-sulphonic acid, N-vinylsuccinimidic acid, and salts of the foregoing. The polyanionic polymers may further have hydrophobic constitutional repeating units, such as alkylesters, cycloalkylesters, hydroxyalkylesters, ethers, glycols, aromatic groups and salts thereof. The adjuvants containing the polyanionic polymers are used in vaccines for the induction or enhancement of mucosal immune responses.

Abstract: Compounds of the general formula P1-L-P2; wherein “P1” is a pyrazinoylguanidine sodium channel blocker, “L” is a linking group, and “P2” is either (i) a pyrazinoylguanidine sodium channel blocker or (ii) a P2Y2 receptor agonist, are disclosed. Pharmaceutical formulations containing the same and methods of use thereof to hydrate mucosal surfaces such as airway mucosal surfaces are also disclosed.

Abstract: Acid-labile active compounds are prepared in suppository form, particularly for rectal administration.

Abstract: This invention provides a method of rapidly and reliably delivering codeine, alone or in combination with other compounds, to the systemic circulation by administration via the nasal route to produce rapid onset of beneficial effects in the treatment of pain or cough. The present invention further provides pharmaceutical compositions comprising codeine, and/or pharmaceutically acceptable salts thereof in a variety of unique pharmaceutical dosage forms, with and without other analgesic and/or antitussive compounds.

Abstract: The present invention relates to the use of oxidized thymosin &bgr;4 in therapy, more particularly in the treatment of diseases or conditions associated with an inflammatory response of septic shock.

Abstract: A composition for administration to the nasal mucosa of a subject comprises a solution of nicotine or a pharmaceutically acceptable salt thereof in a pharmaceutically acceptable solvent. The composition has a nicotine concentration less than 10 mg/ml. The composition used alone assists in reduction of the desire of a subject to smoke tobacco. It also reduces the nasal symptoms associated with administration of higher concentrations of nicotine to the nasal mucosa.

Abstract: The present invention includes a method for treating periodontal disease. The method comprises delivering to a pocket of a tooth with periodontal disease, a viscous, reddish-brown solution comprising sulfuric acid and sulphonated phenolic compounds. The method also comprises retaining the reddish-brown solution in the pocket for t time ranging from about 5 seconds to about 60 seconds.

Abstract: An intravaginal bio-erodible microbicidal barrier device. The device comprises (a) at least one micronized compound selected from the group consisting of cellulose acetate phthalate and hydroxypropylmethylcellulose phthalate, and (b) at least one pectin, such as an apple pectin, and optionally at least one water soluble or water dispersible cellulose compound selected from the group consisting of hydroxypropylmethylcellulose, methylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, hydroxyethylmethylcellulose, hydroxyethylethylcellulose and hydroxypropylethylcellulose. The device is prepared by a combination of foaming, freezing and freeze-drying processes.

Abstract: The invention concerns an aqueous solution capable of being injected by perinodular delivery or inhaled for use in the treatment of degenerative or autoimmune diseases or as immunomodulatory agent. Said solution is prepared by reacting camphor on ammonium hydroxide. The resulting product is then suspended in a saline solution. Said preparation having a basic pH is then neutralized with nitric acid. The resulting aqueous solution has pharmacological properties since it is an analogue of human cytokines, which makes it useful for treating degenerative or autoimmune diseases and/or as an immunomodulatory agent.

Abstract: A polymerized hydrogel composition and applicator for hydrating or dehydrating a surface, particularly a dermatological surface, to which it is applied and a method for forming the composition. The composition is comprised of a mixture of two polymerizable materials, a two-part redox catalyst system and a two-part polymerization medium. The percentage by weight of each element in the composition may be varied within stated percentage ranges. The rate at which hydration or dehydration occurs may be controllably altered by varying the percentages of certain of the composition elements. The applicator includes a thermoplastic center section and two reservoir sections each having a reservoir storage area for holding moisture and/or medicaments. The composition is mechanically bonded onto each of the reservoir sections and then hydrated. The applicator is designed for insertion into a human mouth after hydration and is used for treating xerostomia.

Abstract: Polymeric compositions having improved capability of solubilizing a drug in a hydrophilic environment to form a solution, comprising: a biodegradable polyester oligomer; and biodegradable AB-type, ABA-type, or BAB-type block copolymers are disclosed. The copolymers are comprised of about 50.1 to 65% by weight of a biodegradable, hydrophobic A polymer block comprising a biodegradable polyester, and about 35 to 49.9% by weight of a hydrophilic B polymer block comprising a polyethylene glycol (PEG), and wherein the block copolymer has a weight averaged molecular weight of between 2400 to 4999. The biodegradable polyester oligomer of said composition is within a range of 0.01% to 30% by weight of the total polymer mixture, and the content of the biodegradable AB-type, ABA-type, or BAB-type block copolymer is within a range of 70% to 99.99% by weight of the total polymer mixture.

Abstract: Disclosed are solid dose nanoparticulate compositions comprising a poorly soluble active agent, at least one polymeric surface stabilizer, and dioctyl sodium sulfosuccinate (DOSS). The solid dose compositions exhibit superior redispersibility of the nanoparticulate composition upon administration to a mammal, such as a human or animal. The invention also describes methods of making and using such compositions.

Abstract: A process for producing a small-sized, lipid-based cochleate. Cochleates are derived from liposomes which are suspended in an aqueous two-phase polymer solution, enabling the differential partitioning of polar molecule based-structures by phase separation. The liposome-containing two-phase polymer solution, treated with positively charged molecules such as Ca2+ or Zn2+, forms a cochleate precipitate of a particle size less than one micron. The process may be used to produce cochleates containing biologically relevant molecules.

Abstract: A composition containing therapeutic agents and/or breath freshening agents for use in the oral cavity is disclosed. The carrier comprises water-soluble polymers in combination with certain ingredients and provides a therapeutic and/or cosmetic effect. The film is coated and dried utilizing existing coating technology and exhibits instant wettability followed by rapid dissolution/disintegration upon administration in the oral cavity.

Abstract: A powdered, dispersible composition having stable dispersibility over time is provided. The composition exhibits a characteristic glass transition temperature (Tg) and a recommended storage temperature (Ts), wherein the difference between Tg and Ts is at least about 10° C. (i.e. Tg−Ts is greater than 10° C.). The composition comprises a mixture of a pharmaceutically-acceptable glassy matrix and at least one pharmacologically active material within the glassy matrix. It may be further mixed with a powdered, pharmaceutically-acceptable carrier. It is particularly valuable in unit dosage form having a moisture barrier, in combination with appropriate labelling instructions.

Abstract: The invention relates to a new process for producing powdered preparations for inhalation.

Abstract: The present invention relates to a layered pharmaceutical delivery device for the administration of pharmaceuticals or other active compounds to mucosal surfaces. The device may also be used by itself without the incorporation of a therapeutic. The device of the present invention consists of a water-soluble adhesive layer, a non-adhesive, bioerodable backing layer and one or more pharmaceuticals if desired in either or both layers. Upon application, the device adheres to the mucosal surface, providing protection to the treatment site and localized drug delivery. The “Residence Time”, the length of time the device remains on the mucosal surface before complete erosion, can be easily regulated by modifications of the backing layer.

Abstract: A method for assuaging tobacco addiction comprises pulsing doses of nicotine into a user's bloodstream so it reaches the brain before passing through the liver. A nicotine-burst tablet is held in the mouth by a user to receive each nicotine-pulse dose. The tablet is configured to suddenly release its entire nicotine payload from an otherwise inert or benign material. Such nicotine payload is relatively small, e.g., under one milligram. The therapeutic effects depend on the change of nicotine levels in the blood over a change in time. Rapid nicotine onset of a small dose is more assuaging than a slow build-up to a high dosage. An oral carrier comprises a nicotine saturated instant-dissolve paper that delivers one nicotine pulse. An additive prevents abuse by causing excessive use to catalyze a foul taste or sickening sensation.

Abstract: The present invention provides a gastric and/or duodenal adhesive pharmaceutical composition obtained by coating a composition, which comprises a medicament acting at the stomach and/or duodenum and one or more of ingredients selected from water insoluble polymers, polyglycerin fatty acid esters, lipids and waxes, with a polymer having adhesive capacity onto the surface of the mucosa of a digestive tract under acid conditions and separates from the mucosa of the digestive tract in neutral or alkaline conditions. This composition adheres only to the mucosa of the stomach and/or duodenum and releases the medicament over long hours so that sufficient effects are available by a small amount of the medicament.

Abstract: An intravaginal bio-erodible microbicidal barrier device. The device comprises (a) at least one micronized compound selected from the group consisting of cellulose acetate phthalate and hydroxypropylmethylcellulose phthalate, and (b) at least one water soluble or water dispersible cellulose compound selected from the group consisting of hydroxypropylmethylcellulose, methylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, hydroxyethylmethylcellulose, hydroxyethylethylcellulose and hydroxypropylethylcellulose. The device is prepared by a combination of foaming, freezing and freeze-drying processes.

Abstract: The present invention provides solid pharmaceutical compositions for improved delivery of a wide variety of pharmaceutical active ingredients contained therein or separately administered. In one embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier including a substrate and an encapsulation coat on the substrate. The encapsulation coat can include different combinations of pharmaceutical active ingredients, hydrophilic surfactant, lipophilic surfactants and triglycerides. In another embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier being formed of different combinations of pharmaceutical active ingredients, hydrophilic surfactants, lipophilic surfactants and triglycerides. The compositions of the present invention can be used for improved delivery of hydrophilic or hydrophobic pharmaceutical active ingredients, such as drugs, nutrionals, cosmeceuticals and diagnostic agents.

Abstract: An aqueous-based sprayable composition comprises a therapeutic or palliative agent, water and a mixture of microcrystalline cellulose and alkali metal carboxyalkylcellulose. In one embodiment, the composition is a non-Newtonian nasal spray exhibiting a very rapid viscosity recovery upon removal of shear forces.

Abstract: The present invention provides compositions and methods of preparing a bilayer structure for encapsulating multiple containment units. These containment units can contain therapeutic, diagnostic agents or imaging 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 invention encompasses a solid dose delivery vehicle for ballistic administration of a bioactive material to subcutaneous and intradermal tissue, the delivery vehicle being sized and shaped for penetrating the epidermis. The delivery vehicle further comprises a stabilizing polyol glass loaded with the bioactive material and capable of releasing the bioactive material in situ. The present invention further includes methods of making and using the solid dose of the invention.

Abstract: Methods and pharmaceutical compositions for using desmethylselegiline. In particular, the present invention provides novel compositions and methods for using desmethylselegiline for 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. Desmethylselegiline is the R-(−) enantiomer of N-methyl-N-(prop-2-ynyl)-2-aminophenylpropane. Claimed compositions include both the R-(−) isomer and mixtures of the R-(−) and S(+) isomers. Pharmaceutically acceptable acid addition salts may also be used. Effective dosages are a daily dose of at least about 0.015 mg/kg of body weight.

Abstract: The invention provides the use of an antigen which is a mucosally immunogenically active substance comprising the 50 kD C fragment of tetanus toxin, an immunogenic fragment thereof, or a derivative thereof formed by amino acid deletion, substitution or insertion for the manufacture of a vaccine composition for administration to a mucosal surface to induce an immune response in the mucosal surface against tetanus infection. The Vaccine composition preferably contains the P.69 outer membrane protein of B. pertussis, and B. pertussis filamentous haemaglutiuin. The invention also provides vaccine compositions per se and a method of treating tetanus and optionally whooping cough using the vaccine compositions.

Abstract: Bioadhesive compositions in a flexible, finite form for topical application to skin or mucous membranes comprising a composition which results from an admixture of at least one PVP polymer, at least one bioadhesive, optionally a pharmaceutically acceptable solvent suitable for use with an active agent, and methods of administering active agents to a subject, are disclosed. The bioadhesive composition can either include an active agent incorporated directly in the composition, or a separate source of an active agent.

Abstract: The application is directed to the treatment of one or more symptoms associated with drug withdrawal by administering desmethylselegiline.

Abstract: A nasal and pharyngeal spray solution for use in spraying into the nose and mouth to protect the mucosa from noxious viruses, bacteria and fungi and excessive drying, in situations of high risk, such as the cabins of commercial aircraft, comprises a saline solution of Proanthocyanidins and ascorbic acid. The “fresh mix” delivery system is an appropriately closed, sterile, oxygen-excluding, pressurized container.

Abstract: (Meth)acrylic acid copolymers are used to increase mucosal permeability, comonomers present being (meth)acrylic esters and/or other monomers capable of free-radical polymerization, and the (meth)acrylic acid:comonomer molar ratio varying from 99:1 to 1:99.

Abstract: Pregnanes of formula I, and pharmaceutical compositions and products containing them, are useful in weight promotion by administration to the vomeronasal organ.

Abstract: Pharmaceutical compositions are provided which comprise effective amounts of antimicrobials, anti-inflammatories, and antihistamines, to provide an ulcer medication which prevents secondary infections and promotes healing while providing immediate relief from pain. The composition may be used to treat a variety of ulcers including but not limited to intraoral aphthous ulcers and non-oral lesions. The compositions of the present invention may also be combined with materials capable of forming seals over ulcers or lesions to further promote the healing process.

Abstract: Varying the daily dose of either or both of the estrogen and the progestogen administered for hormone replacement therapy (HRT) is readily and inexpensively accomplished, without the necessity of the physician prescribing a new product each time the daily dose of the estrogen or progestogen is changed, by administering preferably transdermally the estrogen and the progestogen contained in separate extrudable pharmaceutical compositions from a dispenser which contains means, preferably adjustable only by the attending physician or dispensing pharmacist, for varying the volume of either or both of the respective compositions which is dispensed as a single dose from the dispenser in response to a defined digital dispensing manipulation of the dispenser thereby facilitating optimal compliance to a combination of HRT with individually adjusted dosages of the estrogen and progestogen.

Abstract: A patient's upper airway condition such as snoring and sleep apnea is treated by selecting a particulate material selected for limited migration within tissue and for encouraging a fibrotic response of tissue to the material. A bolus of the particulate material is injected into the tissue area to structurally stiffen the tissue.

Abstract: A composition for relieving a sensation of respiratory discomfort and/or for promoting natural regeneration of mucous membranes of the nasal cavity. The composition contains levomenthol at a concentration between 10 and 250 mg/l, dissolved in an aqueous ionic solution having an osmolarity at least equal to that of an aqueous solution of sodium chloride at 9 g/l. The aqueous ionic solution is pure sea water, diluted sea water, an aqueous sodium chloride solution, an aqueous sodium chloride solution further containing at least one salt found in sea water, or a mixture thereof.

Abstract: The invention relates to methods and composition for improving absorption and dissolution of active ingredients of drugs. The invention provides a method of administration of an active ingredient to a mammal through a transmucosal route that includes delivering the active ingredient to a desired site in a body of the mammal, and, sequentially, at the desired site, promoting dissolution and absorption of the active ingredient. In a preferred embodiment, the pH of the localized environment of the active ingredient is sequentially modified to promote dissolution and absorption.

Abstract: The invention provides a composition of matter comprising a stable oil-in-glycerin emulstion containing at least one oil, at least one emulsifier and glycerin.

Abstract: The invention relates to the co-administration in human or veterinary medicine of 1,2,3,9-tetrahydro-9-methyl-3-[(2-methyl-1H-imidazol-1-yl)methyl]-4H-carbazol-4-one or a physiologically acceptable salt or solvate thereof and dexamethasone or a physiologically acceptable salt or ester thereof. The two active ingredients, which may be administered separately either simultaneously or sequentially, or may be combined in a single pharmaceutical preparation, are useful in the relief and/or prevention of nausea and vomiting.

Abstract: The invention relates to a mixture for use as wound dressing, which comprises: a) paraffins complying with DAB and/or synthetic waxes selected from the group consisting of montan waxes, petroleum waxes, Fischer-Tropsch waxes, polyolefin waxes, petrolatum, wax alcohols, and oxidates of the aforementioned substances; b) at least one metal hydroxide. The mixture is stable on prolonged storage at room temperature and promotes collagen regeneration in vivo in cases of bone trauma.

Abstract: The invention relates to nanoscale particles suited especially for use in tumor therapy by hyperthermia. Said particles comprise a (preferably superparamagnetic) iron oxide-containing core and at least two shells surrounding said core. The (innermost) shell adjoining the core is an envelope which comprises groups capable of forming cationic groups and is broken down by human or animal tissue at such a slow rate as to allow for association of the core surrounded by said envelope with the surface of cells and/or for absorption of said core into the inside of cells.