Abstract: The present invention is drawn to adhesive solidifying formulations, methods of drug delivery, and solidified layers for dermal delivery of a drug. The formulation can include a drug, a solvent vehicle, and at least two solidifying agents. The solvent vehicle can include a volatile solvent system including at least one volatile solvent, and a non-volatile solvent system including at least one non-volatile solvent, wherein at least one non-volatile solvent is flux-enabling non-volatile solvent(s) capable of facilitating the delivery of the drug at therapeutically effective rates over a sustained period of time. The formulation can have a viscosity suitable for application to a skin surface prior to evaporation of the volatile solvents system. When applied to the skin, the formulation can form a solidified layer after at least a portion of the volatile solvent system is evaporated.

Abstract: The present invention is drawn to adhesive formulations and methods of drug delivery. The formulation can include a drug, a solvent vehicle, and a solidifying agent. The solvent vehicle can include a volatile solvent system including at least two volatile solvents, and a non-volatile solvent system including at least one non-volatile solvent, wherein at least one non-volatile solvent is capable of facilitating the delivery of the drug at therapeutically effective rates over a sustained period of time. The formulation can have a viscosity suitable for application to a skin surface prior to evaporation of the volatile solvents system. When applied to the skin, the formulation can form a solidified layer after at least a portion of the volatile solvent system is evaporated.

Abstract: Methods for treating ocular and periocular disorders by administration to a human patient of a therapeutically effective amount of a compound that modulates muscle action.

Abstract: The present invention relates to a carrier composition comprising a phosphate compound of an electron transfer agent and a polar aprotic solvent. Biologically active compounds formulated with the carrier composition have been shown to have improved properties.

Abstract: Therapeutic compositions and methods for treatment of attention deficit disorder (ADD) or attention deficit hyperactivity disorder (ADHD) include dosage forms that deliver a therapeutic amount of active drug in a delayed and controlled release formulation. The dosage form can be administered at night and drug release is delayed for from 3 to 8 hours, followed by an ascending release rate.

Abstract: Embodiments of the present disclosure include a coordination complex, comprising a first biologically active moiety, a second biologically active moiety, and a metal, wherein the first biologically active moiety and second biologically active moiety are bound to the metal by covalent coordination bonds, and wherein the first biologically active moiety and second biologically active moiety are different. These complexes may enhance the pharmacodynamic properties of biologically active moieties.

Abstract: Described are methods of inhibiting heterotopic ossification (HO) in a subject in need thereof. The methods involve administering an effective amount of a proprioception inhibitor to the subject, whereby HO is inhibited or prevented. The present invention also relates to a method of treating a subject with bone trauma. This involves administering a proprioception inhibitor to the subject under conditions effective to treat the bone trauma, where the proprioception inhibitor prevents or inhibits HO.

Abstract: Provided herein are compositions and related methods useful for accelerating bone healing and growth. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity.

Abstract: A pharmaceutical composition comprises an active ingredient dissolved in an essentially non-aqueous carrier system comprising volatile and non-volatile components, in which the volatile component comprises a volatile non-solvent for the active ingredient and a volatile solvation additive for the non-solvent and the non-volatile component comprises a non-volatile non-solvent and optionally a non-volatile solvent for the active ingredient, the volatile and non-volatile non-solvents comprising silicone fluids of respectively different viscosity.

Abstract: Formulations and methods are provided for the treatment of pain, and neuropathic pain in particular. The formulations are eutectic mixtures of a capsaicinoid and a local anesthetic agent and/or an anti-pruritic agent.

Abstract: The invention provides a parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/ameliorating agent that has a function such as parakeratosis inhibition, pore shrinkage, or rough skin—inhibition/abatement, poses no safety problems such as sensory irritation, and is very safe, and further provides an external composition for skin to which a compound having the above-mentioned function has been added. The parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/ameliorating agent comprises one or more compounds selected from the group consisting of ?-alanine derivatives and salts thereof. The external composition for skin comprises the one or more compounds selected from the group consisting of ?-alanine derivatives and salts thereof as the above-mentioned parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/ameliorating agent.

Abstract: The present invention concerns new preservative-free hyperbaric compositions of prilocaine HCI intended for use in intrathecal narcosis, characterized by high stability at ambient temperature (15° C. -27° C.). The present invention also concerns a method for manufacturing said compositions.

Abstract: Disclosed is a transdermally absorbable preparation, in which an adhesive agent produced by crosslinking at least one copolymer is contained in an adhesive layer and the aging period in the production of the adhesive layer can be shortened. The transdermally absorbable preparation comprises a support and an adhesive layer arranged on the support and containing an adhesive agent and a medicinal component. The transdermally absorbable preparation is characterized in that the adhesive agent comprises a resin mixture comprising 100 parts by mass of a specific acrylic copolymer (A) and 0.1 to 30 parts by mass of a specific acrylic copolymer (B) or 0.05 to 2 part(s) by mass of a polyamine compound, and the adhesive layer additionally contains an organic acid.

Abstract: A pain relieving composition that includes an anesthetic in the range of 0.5%-7.0% by weight (“w/w”), an anti-inflammatory agent in the range of 1.0%-11.0% w/w, a moisturizing agent in the range of 0.5%-12.0% w/w, a humescent in the range of 0.5%-13.0% w/w, a penetration enhancing agent in the range of 0.5%-7.0%, and a carrier solvent in the range of 40.0%-97.0% w/w to be used before and/or after procedures which cause damage to human skin.

Abstract: In one embodiment, the present invention provides a topical composition including a topically acting anesthetic active ingredient; an ester; a non-ionic surfactant; a polar solvent; water, and optionally a buffer, a pH adjusting agent or an anti-oxidant. The compositions are useful for alleviating pain especially associated with acute herpes zoster.

Abstract: The present specification generally relates to hydrogel compositions and methods of treating a soft tissue condition using such hydrogel compositions.

Abstract: This invention relates to a patch for the expulsion of insect poison from the skin after stings from membranous insects (Hymenoptera). The patch is characterized in comprising a poison-aspirating matrix comprising an expulsion agent as well as a swell layer, which swells after the addition of a liquid through a hole on the top of the patch and thus adds a light pressure to the poison-aspirating matrix towards the skin, whereby a local and relieving effect is achieved. In one embodiment, the matrix further comprises a local anesthetic. The expulsion agent is e.g. a carbohydrate. The swell layer consists e.g. of a silica gel.

Abstract: A composition suitable for use in a transdermal delivery patch for administration of a biologically active compound, the composition comprising a phosphate compound of tocopherol and a polymer carrier.

Abstract: A carrier composition of the present invention comprises a phosphate compound of an electron transfer agent and a relatively high concentration of a polar protic solvent. A biologically active compound may be formulated with a carrier composition of the present invention to provide a formulation.

Abstract: The present invention concerns prodrugs of mexiletine (and mexiletine's active metabolite) pharmaceutical compositions containing such prodrugs. Methods for treating myotonic conditions, while reducing the inherent adverse GI side effects associated with mexiletine, increasing the bioavailability of mexiletine, and improving the pharmacokinetic reproducibility of mexiletine with the aforementioned prodrugs are also provided.

Abstract: Method are provided for treating a patient having bladder pain and/or irritative voiding symptoms. The method includes administering to the patient's bladder lidocaine or another anesthetic agent continuously over a treatment period of 24 hours or more in an amount effective to achieve a therapeutic effect which is sustained beyond the end of the treatment period.

Abstract: Disclosed herein are compositions and methods for the treatment of otic disorders with CNS modulating agent compositions and compositions administered locally to an individual afflicted with an otic disorder, through direct application of these compositions and compositions onto or via perfusion into the targeted auris structure(s).

Abstract: The present invention relates to a method for slowing the development of mammalian organ, tissue and cellular damage and death by using a persistent sodium current blocker (or a pharmaceutically acceptable salt or derivative thereof). The present invention further relates to a method for preventing damage and death in mammalian organs, tissues and cells or reducing the extent of damage and death in mammalian organs, tissues and cells. In particular the invention relates to a method for the treatment, amelioration or prevention of non-neuronal and non-myocardial cell or tissue damage or death and for reducing the pain associated with non-neuronal and non-myocardial cell or tissue damage.

Abstract: The invention provides compounds, compositions, methods, and kits for the treatment of neurogenic inflammation.

Abstract: Compositions and methods are disclosed for inhibiting semicarbazide-sensitive amine oxidase (SSAO), also known as vascular adhesion protein-1 (VAP-1). The compounds disclosed are amine-containing and amide-containing compounds. The compounds and compositions are useful for treatment of diseases, including inflammation, inflammatory diseases and autoimmune disorders.

Abstract: One aspect of this disclosure relates generally to lipid compounds that exert diverse effects in the endocannabinoid system, such as regulating CB1 and CB2 receptor or moderating other bio-macromolecules within the endocannabinoid system. Some of the compounds showed improved receptor binding affinity, and/or improved receptor subtype selectivity, and improved bio-stability. Some of the compounds exhibit activities to regulate the enzymes that moderate the bio-disposal of endogenous cannabinoids, such as the fatty acid amide hydrolase (FAAH). Some of the compounds exhibit activities to inhibit the anandamide transporter. Other aspects of the invention are pharmaceutical preparations employing these ligands and methods of administering therapeutically effective amounts of the preparations to provide a physiological effect.

Abstract: A transdermal topical anesthetic formulation, which can be used to ameliorate or inhibit pain, has been developed. In the preferred embodiment, the topical anesthetic is a local anesthetic such as lidocaine, most preferably lidocaine free-base in a gel, and the dosage of the local anesthetic is effective in the painful area or immediately adjacent areas, to ameliorate or eliminate the pain. High concentration of local anesthetic in solution in the carrier is used to drive rapid release and uptake of the drug. Relief is typically obtained for a period of several hours.

Abstract: The present invention generally concerns microtubule protrusions in cancer cells, including detached cancer cells, and inhibition of the protrusions. In particular aspects, the inhibition of the protrusions interferes with attachment of the cell to a vessel wall, and in further aspects the cell is killed by forcing it to enter capillaries and be destroyed, for example by shearing. Inhibition by a variety of agents and methods is contemplated.

Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are styrenyl derivative compounds, including but not limited to stilbene derivative compounds, and compositions comprising these compounds, that are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.

Abstract: Implant devices for intravesical administration and local drug delivery. The device has a body which includes a hollow tube formed of a biocompatible material; at least one reservoir in the tube which contains a drug; and one or more apertures through which the drug can be released. The device is configured for minimally invasive insertion into a body cavity, such as the bladder. The hollow tube may be elastomeric to permit the device to be elastically deformed from its initial shape into an elongated shape for passage through a catheter, where following such passage the device can return to or toward its initial shape to facilitate retention of the device in the body cavity. The body may have a narrow, elongated shape effective to permit insertion of the drug delivery device through a catheter without necessarily deforming the body, yet include flexible projections which effect retention within the body cavity.

Abstract: The invention describes compounds, compositions, and methods of using the same comprising a chemical moiety covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.

Abstract: Device structure 100 for iontophoresis provides electrode 101 and electrically conductive layer 102. Electrically conductive layer 102 contains active ingredient D and basic water swelling methacrylate copolymer P1 and/or acidic water swelling methacrylate copolymer P2. Electrode 101 and electrically conductive layer 102 are placed into a hollow of backing 103 and electrode terminal 104 is connected to electrode 101 through backing 103. Adhesive layer 105 is set around backing 103, and liner 106 to be removed when using the device, is placed so as to cover the hollow of backing 103.

Abstract: There is disclosed the topical dermal use of vasocontrictor substances for regulating body temperature to treat, prevent or delay the onset of anesthetic induced hypothermia. Kits containing appropriate materials and instructions, and other embodiments, are also disclosed.

Abstract: In certain embodiments, the present invention is directed to a pharmaceutical formulation for topical administration on a mammal, comprising a unit dose of a therapeutically effective amount of a therapeutic agent and a pharmaceutically acceptable carrier medium therefor, said formulation being solid at ambient temperature and having a softening point of not higher than 35° C., such that when the formulation is placed in continuous contact with the skin of a mammalian patient, it is softened to a consistency to effect substantial application of the unit dose of said therapeutic agent onto a desired skin area of the mammalian patient within a time period of less than 10 minutes.

Abstract: The present invention relates to compounds that can be used as metal-ion-chelating agents or as depolluting agents, corresponding to general formula (I) below: and also to precursor compounds of formula (II) and labelled compounds of formula (III) deriving from the compounds of formula (I). The present invention also relates to the use of the compounds (I), (II) or (III) as a medicament, and also the use thereof for the diagnosis, prevention and treatment of neurodegenerative diseases such as Wilson's disease and Alzheimer's disease.

Abstract: An in situ film-forming sprayable methyl acetate-based solution of at least one absorbable, low-crystallinity, segmented copolymer contains at least one bioactive agent, which exhibits antimicrobial, anti-inflammatory, antiviral, anesthetic, hemostatic, and/or antineoplastic activity. The absorbable polymers can be a polyaxial copolyester, polyether-ester and polyether-ester urethane and the bioactive solution thereof can be applied onto animal and human skin or accessible body cavities to prevent or treat one or more disorder susceptible to the bioactive agent therein.

Abstract: The present invention provides a composition for external application to skin containing one type or two or more types of compounds selected from the group consisting of aminoacetoamide compounds represented by the following general formula (1) and salts thereof.

Abstract: The present invention describes a series of therapeutically active compounds of formula I, X—Y—Z??(I) that are useful for treating a disorder in a mammal. In the formula I, X and Z, which may be same or different, are independently selected from substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted heterocyclic group or substituted or unsubstituted heterocyclylalkyl; and Y is a linker selected from —O—, —S—, —NH—, —(CH2)n—, —CO—, —CONRa—, —NRaCO—, —NRaCOO—, —COO—, —CONRaCO—, —CONRaCOO— and —COOCOO—.

Abstract: A transdermal topical anesthetic formulation, which can be used to ameliorate or inhibit pain, has been developed. In the preferred embodiment, the topical anesthetic is a local anesthetic such as lidocaine, most preferably lidocaine free-base in a gel, and the dosage of the local anesthetic is effective in the painful area or immediately adjacent areas, to ameliorate or eliminate the pain. High concentration of local anesthetic in solution in the carrier is used to drive rapid release and uptake of the drug. Relief is typically obtained for a period of several hours.

Abstract: This invention relates to an externally applied ointment that aids in relieving irritation, pain or mild inflammation of the skin or mucous membranes associated with hemorrhoids and the method of using such ointment lotion. The formulation of the present invention contains phenylephrine HCl, lidocaine grape skin/seed/leaf extract and aloe plants extract.

Abstract: Pharmaceutical compositions comprising an aptamer and an amino acid ester or amide or an aptamer; a divalent metal cation; and a carboxylic acid, a phospholipid, a phosphatidyl choline, or a sphingomyelin. Methods of treating or preventing a condition in an animal comprising administering to the animal the pharmaceutical compositions.

Abstract: Disclosed is a stable aqueous gel formulation suitable for topical use comprising water, an anesthetic (e.g., lidocaine hydrochloride), a viscoelastic polymer, and a tonicity modifier, wherein the aqueous gel formulation is free of preservatives and phosphate buffer, is isotonic with physiological fluids, and is sterile and has low particulate count. Also disclosed is a method of inducing topical anesthesia on a tissue or organ, e.g., the eye, of an animal comprising providing a stable aqueous gel formulation comprising water, an anesthetic, a viscoelastic polymer, and a tonicity modifier, wherein the aqueous gel formulation is free of preservatives and phosphate buffer, is isotonic with physiological fluids, and is sterile, and topically administering an effective amount of the aqueous gel formulation to the tissue or organ of the animal.

Abstract: A method for affecting the timing of cervical ripening and the resultant onset of parturition in a pregnant female mammal, the method comprises administering to a pregnant female one or more than one dose of an agent that chemically mimics innervation of the cervix by the vagus nerve, thereby advancing the onset of parturition, or administering to a pregnant female one or more than one dose of an agent that chemically blocks innervation of the cervix by the vagus nerve, thereby delaying the onset of parturition.

Abstract: Compositions and methods are provided for obtaining stabilized quinol compositions, such as catecholamine drugs (e.g., epinephrine solutions), and also for obtaining stable pharmaceutical formulations that comprise a stabilized quinol composition and a second pharmacologically active component such as a local anesthetic or other active drug ingredient having a reversibly protonated amine group. Stability is achieved through the inclusion of an appropriately selected pH buffer and a thiol agent, based on redox and pH buffering principles including pKa of the buffer and of the reversibly protonated amine group.

Abstract: The present invention relates to semisolid transdermal pharmaceutical preparation having enhanced stability and bioavailability, wherein the particles are coated by a volatile silicon oil component and the thus obtained suspension is dispersed in a gel or cream base.

Abstract: The present invention is directed to compounds, combinations, compositions and methods for enhancing nitric oxide (NO) delivery to target sites, and in particular to muscle, both normal and dystrophic. Enhanced NO delivery according to the present invention may be achieved by using a combination of a muscle relaxant and an NO donor compound, or by using a compound of the invention: formula (I) wherein R1 is H, halo, C1-6 alkoxy or C1-6 alkyl; R2 is H, NO2 or C(O)NH2; R3 is H, NO2 or C(O)NH2; and at least one of R2 and R3 is NO2; or a pharmaceutically acceptable salt of the compound.

Abstract: The invention relates to procedures and methods of determining a susceptibility to cardiac arrhythmia, including Atrial Fibrillation, Atrial Flutter and Stroke, by assessing the presence or absence of alleles at polymorphic markers found to be associated with risk of these conditions. The invention further relates to kits encompassing reagents for assessing such markers, and diagnostic 5 methods, uses and procedures for utilizing such susceptibility markers.

Abstract: The present invention relates to a method of treating a life threatening condition in a critically ill human patient with a non-infectuous disorder, wherein the critically ill patient is a patient receiving enteral or parenteral nutrition, the method comprising the step of administering to said patient an autophagy inducing agent.

Abstract: Provided is a pharmaceutical composition for permeabilizing fetal membranes including an active ingredient having a log K in the range of 2 to 4, where K is the octanol/water partition coefficient. The active ingredient may be, for example, bupivacaine, sodium lauryl sulfate or oleic acid. Further provided is a system for transfetal membrane transport. The system includes a probe unit adapted for insertion into a female reproductive tract and releasing a substance onto fetal membranes that permeabilizes the membranes. The system is also configured to apply ultrasound radiation to the fetal membranes to further increase the membrane permeability.

Abstract: The disclosed invention provides new polyamine analogs and derivatives containing a hydrophobic region and a polyamine region as well as methods and compositions for their use.