Abstract: Embodiments of the present disclosure relates to a new and improved large scale commercial manufacturing process of making bupivacaine multivesicular liposomes (MVLs). Batches of bupivacaine MVLs prepared by the new process have high yields, improved stabilities, and desired particle size distributions.

Abstract: Compounds are provided to modulate the C5a receptor. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: Capsaicin compositions and methods for enhancing hydrophobicity of a molecule useful for pharmaceutical applications, including: (1) a prodrug using a linker such as a carbamate between capsaicin with other structures in order to optimize kinetic control of capsaicin cleavage; (2) a prodrug using a linker such as an unsaturated carboxylic ester between capsaicin with other structures in order to optimize kinetic control of capsaicin cleavage; (3) esters of long-chain fatty acids and capsaicin where hydroxyl groups provide handles for attachment of additional capsaicin molecules; and (4) the use of carboxylic acid diesters to increase overall hydrophobicity of two or more covalently-linked capsaicin molecules. Formulations of palmitated esters of capsaicin are also described, which are designed to enhance hydrophobicity of a molecule useful for pharmaceutical applications, for example to provide compounded mixtures designed to optimize analgesic efficacy.

Abstract: Provided herein is an amorphous form of a complement component 5a receptor having the formula of Compound 1 Also provided herein are pharmaceutical compositions and methods of treatment using the amorphous form of Compound 1, described herein.

Abstract: The present invention relates to a composition for topical application comprising: a first discontinuous phase comprising a first oil and tacrolimus; a second discontinuous phase comprising a second oil; and a continuous aqueous phase; wherein the first oil is different from the second oil.

Abstract: A non-addictive analgesic sustained-release drug delivery system, comprising: (1) a narcotic analgesic drug having a concentration of 1 mg/ml-160 mg/ml, the drug being selected from a group consisting of: a local analgesic drug, and the combination of the local analgesic drug and a nonsteroidal analgesic drug and/or an opioid analgesic drug; (2) a drug menstruum in a proportion of 1%-75% (v/v), the menstruum being selected from a group consisting of benzyl alcohol, ethanol, benzyl benzoate, ethyl lactate, and tetrahydrofurfuryl polyethylene glycol ether; and (3) a drug sustained-release formulation having a proportion of 25%-99% (v/v), the sustained-release formulation being selected from a group consisting of natural vegetable oil, synthetic lipid, artificially improved half-natural lipid and derivative thereof. Also disclosed are a preparation process and use of the sustained-release drug delivery system.

Abstract: A pharmaceutical composition for treating infertility in a female subject substantially consists of local anesthetic of amide type such as lidocaine, human albumin, viscosity controlling agent selected from recombinant hyaluronic acid and combination of recombinant hyaluronic acid and water-soluble cellulose ether, optionally citrate, glucose, and/or amino acid, water optionally comprising one or more ions selected from the group consisting of sodium, potassium, magnesium, calcium, acetate, chloride, sulfate. Also disclosed is a method of treating infertility by administration of the composition to a female subject in need thereof.

Abstract: The present invention relates to a system and method for real-time delivery of medical tests and related data from laboratories (12) or similar sources (18) to portable communication devices such as mobile phones (14), text-enabled pagers (14) and web-enabled personal digital assistance (PDA's) (14) and other WAP devices (14). The subject system enables physicians to access test results remotely as soon as they become available. Also, the system allows the physician to develop an electronic prescription and submit the electronic prescription to a pharmacy using the portable communications device (14).

Abstract: A compound having Formula I is an inhibitor of carbapenem-hydrolyzing class D beta-lactamases. The compound inhibits the activities of clinically-important and emerging subgroups of carbapenem-hydrolyzing class D beta-lactamases. A method of treating a bacterial infection includes administering to a subject suffering from a bacterial infection a composition including an effective amount of the compound having Formula I or the pharmaceutically acceptable salt thereof.

Abstract: A therapeutic agent or a preventive agent for alopecia areata has an ROR? antagonistic activity, and, there is a therapeutic agent or a preventive agent for alopecia areata, including a cyclic amine derivative typified by the following compound or a pharmacologically acceptable salt thereof as an active ingredient.

Abstract: The present invention relates in general to polymer-bioactive agent conjugates for delivering a bioactive agent to a subject. The polymer-bioactive agent conjugates contain triazole moieties in the polymer backbone and a bioactive moiety selected from quinolones, NSAIDs and mixtures thereof. The present invention also relates to methods for preparing the polymer conjugates using click cycloaddition chemical reactions, to monomer-bioactive agent conjugates suitable for preparing the polymer conjugates, and to pharmaceutical products comprising the polymer conjugates for the post-surgical care to treat or prevent infections, provide analgesia and treat inflammation.

Abstract: The present invention relates to a topical ophthalmic formulation comprising at least one antagonist of the endothelin receptor, preferably selected from sitaxentan, ambrisentan, atrasentran, bosentan, macitentan and tezosentan, or a mixture thereof, more preferably bosentan. It also relates to the use of a topical ophthalmic formulation comprising at least one antagonist of the endothelin receptor, preferably selected from sitaxentan, ambrisentan, atrasentran, bosentan, macitentan and tezosentan, or a mixture thereof, more preferably bosentan, as active ingredient for preventing and/or treating the retinal neurodegeneration induced by diabetes and/or aging.

Abstract: Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors.

Abstract: A decongestant composition is provided comprising: (a) a safe and effective amount of an adrenergic compound; (b) a safe and effective amount of a steroid; and (c) a pharmaceutically-acceptable carrier. Methods of treating congestion in a human or animal subject are also provided comprising administering to the subject a composition comprising: (a) an adrenergic compound; and (b) a steroid; where the daily dose of the adrenergic compound administered to the subject is from about 1 ?g to about 800 ?g, and the daily dose of the steroid administered to the subject is from about 1 ?g to about 400 ?g.

Abstract: The present invention relates to inhibitors of C5a activity and their use in the treatment of cutaneous, neutrophilic, inflammatory diseases in a subject.

Abstract: Since each of the site I sodium channel blockers have a unique activity and cannot be used to extrapolate the same effective dosage for another site I sodium channel blocker, studies were conducted to identify dosages of neosaxitoxin (“NeoSTX”) and bupivacaine, alone or in combination with epinephrine, to provide two to three days of pain relief in humans. Bupivacaine-NeoSTX combinations produce more reliable blockade and longer duration blockade compared to NeoSTX alone. The three-way combination of NeoSTX-bupivacaine-epinephrine produces more prolonged local anesthesia than the two-way combination of NeoSTX-bupivacaine. Addition of epinephrine to this NeoSTX-bupivacaine combination dramatically prolongs the duration of complete blockade to a mechanical stimulus. These results led to development of specific combination dosage formulations.

Abstract: The invention provides extended release pro-liposomal, non-aqueous, pharmaceutical formulations of a local anesthetic in the form of a clear oily solution and methods for making same. The formulations can be administered by infiltration into an incision, or by injection.

Abstract: A transcutaneous electronic nerve stimulation device configured to provide therapy to a patient includes a control unit assembly, a power source, and a therapy plate electrically coupled to the power source. The therapy plate includes an electrical source configured to deliver electrical stimulation to the patient, a heat source configured to deliver heat to the patient, and a radiation source configured to deliver radiation to the patient. The transcutaneous electronic nerve stimulation device further includes a rigid connector electrically coupling the therapy plate to the power source such that the therapy plate is fixed relative to the power source.

Abstract: The present invention is an analgesic for pain control not limited to postoperative pain control. The present invention discloses an opioid sparing anesthetic formulation comprising a local anesthetic, an N-methyl-D-aspartate (NMDA) receptor antagonist, and a cyclooxygenase (COX) inhibitor such as Bupivacaine, Ketamine, and Ketorolac, which is effective to significantly reduce postoperative nausea and vomiting and enhance postoperative pain relief as compared to existing prior art anesthetics. The formulation is administered to a mammal in need of pain treatment. The formulation may be used as a preemptive analgesic. The analgesic formulation has a buffer for enhancing its shelf life.

Abstract: Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by disregulation of a fatty acid synthase pathway by the administration of such compounds.

Abstract: The present invention aims to provide a novel low-molecular-weight compound having an orexin agonist activity, which is expected to be useful as a superior agent for the treatment or prophylaxis of narcolepsy. The present invention provides a compound showing superior orexin agonist activity which is represented by the formula (I) wherein each symbol is as defined in the DESCRIPTION, and a pharmaceutically acceptable acid addition salt thereof, as well as an orexin agonist containing the compound or a pharmaceutically acceptable acid addition salt thereof.

Abstract: A decongestant composition is provided comprising: (a) a safe and effective amount of an adrenergic compound; (b) a safe and effective amount of a steroid; and (c) a pharmaceutically-acceptable carrier. Methods of treating congestion in a human or animal subject are also provided comprising administering to the subject a composition comprising: (a) an adrenergic compound; and (b) a steroid; where the daily dose of the adrenergic compound administered to the subject is from about 1 ?g to about 800 ?g, and the daily dose of the steroid administered to the subject is from about 1 ?g to about 400 ?g.

Abstract: Described herein is the DP2 antagonist 2-(3-(2-((tert-butylthio)methyl)-4-(2,2-dimethyl-propionylamino)phenoxy)-4-methoxyphenyl)acetic acid, or a pharmaceutically acceptable salt thereof. Also described are methods of preparing the DP2 antagonist, or a pharmaceutically acceptable salt thereof. Also described herein are pharmaceutical compositions suitable for administration to a mammal that include the DP2 antagonist, or a pharmaceutically acceptable salt thereof, and methods of using such pharmaceutical compositions for treating respiratory diseases or conditions, allergic diseases or conditions, inflammatory diseases or conditions, as well as other prostaglandin D2-dependent or prostaglandin D2-mediated diseases or conditions.

Abstract: The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, R4, R6, R11, X1, X2, and X3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.

Abstract: The present application discloses compositions and methods useful for treating and preventing inflammation associated with inflammatory diseases and disorders.

Abstract: The present invention provides a compound of the Formula II: wherein X is: R1 is H, —CN, or F; R2 is H or methyl; R3 is H; and R4 is H, methyl, or ethyl; or R3 and R4 joined together form a cyclopropyl ring; or a pharmaceutically acceptable salt thereof.

Abstract: Draw solutions comprising at least one N-cyclicalkyl-cycloalkylamine and a secondary solvent. The N-cyclicalkyl-cycloalkylamine comprises the chemical structure: wherein n is 0, 1, or 2, n? is 0, 1, or 2, and each of R1-R6 is independently selected from the group consisting of an alkyl group, an alkoxy group, an acetyl group, an aryl group, a hydrogen group, a hydroxyl group, and a phosphorus-containing group. Methods of treating a liquid using the draw solution are also disclosed.

Abstract: The present invention relates to an acetaminophen injectable aqueous solution for use in the treatment or in the prevention of pain by spinal administration, wherein said acetaminophen injectable solution is supersaturated. In certain embodiments, the acetaminophen injectable aqueous solution is administered simultaneously, separately or sequentially with a local anaesthetic by spinal administration.

Abstract: A scleral lens is provided with a sodium channel blocker or a sodium channel modulator disposed in the pre-corneal tear film between the scleral lens and the cornea. This system can be used to deliver sodium channel blockers or a sodium channel modulators not currently used because of poor bioavailability. Methods of using this sodium channel blocker delivery system or a sodium channel modulator delivery system are also disclosed.

Abstract: A silicone gel (“silogel”) composition used to deliver pharmaceutical products transdermally as well as a method for producing the silogel composition, which may contain up to 80% additive ingredients. Preferred embodiments of the invention may include silogel compositions which provide high viscosity/no separation due to API. They are not temperature-sensitive, have no shear stress from the ointment mill/EMP, have no gumming up/stickiness, and no hardening.

Abstract: The invention provides extended release pro-liposomal, non-aqueous, pharmaceutical formulations of a hydrophobic active pharmaceutical ingredient (API) of low water solubility but readily dissolved in alcohols and methods for making same. The formulations can be administered by infiltration into an incision, or by injection.

Abstract: Biocompatible, biodegradable copolymer-xerogel nanocomposites contain a biodegradable, biocompatible copolymer, silica nanoparticles and one or more therapeutic agents, that are useful for wound dressings, medical devices and drug delivery applications.

Abstract: A system is described for long-term controlled release delivery of a drug or a therapeutic agent. According to the invention, one or more drugs or therapeutic agents contained in microspheres are mixed with a temperature sensitive hydrogel which is then introduced directly to the desired situs of the drug or therapeutic agent. The temperature sensitive hydrogel may also contain a drug or a therapeutic agent, for example, a pain relieving drug, for a short-term controlled release. The temperature sensitive hydrogel is in liquid state at room temperature, but upon injection, shortly becomes gelatinous. This system is particularly suitable for treatment of diseases, disorders, or conditions, for example, tumors, discogenic back pain, or arthritis, warranting localized administration of a drug or a therapeutic agent. In addition, the specification provides a method for production of a drug- or therapeutic agent-containing microspheres.

Abstract: Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors.

Abstract: The disclosure provides for means for a method to facilitate food intake and food retention in a mammal by applying a sufficient dose of a local anesthetic drug in the lumen of the pharyngeal-esophageal-gastric-duodenal tract before or during or after eating. The local anesthetic can be amethocaine, articaine, benzocaine, bupivacaine, chloroprocaine, cinchocaine, cyclomethycaine, dibucaine, diethocaine, etidocaine, larocaine, levobupivacaine, lidocaine, lignocaine, mepivacaine, novocaine, piperocaine, prilocaine, procaine, proparacaine, propoxycaine, QX-222, QX-314, ropivacaine, tetracaine, trimecaine, menthol, eugenol or a safe pharmaceutical formulations of tetrodotoxin, saxitoxin, or neosaxitoxin. The disclosure is useful for patients having problems with food intake or food retention.

Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.

Abstract: A method for treating a disease characterized by excessive lipofuscin accumulation in the retina in mammals afflicted therewith, comprising administering to the mammal an effective amount of a non-retinoid antagonist compound or a pharmaceutically acceptable salt thereof.

Abstract: The present disclosure is drawn to an adhesive peel-forming formulation for dermal delivery of a drug, comprising a drug, a solvent vehicle, and a polymer peel-forming agent. The solvent vehicle can comprise a volatile solvent system comprising one or more volatile solvent, and a non-volatile solvent system comprising two or more non-volatile solvents. The non-volatile solvent system can have a solubility with respect to the drug that is within a window of operable solubility such that the drug is deliverable at therapeutically effective rates over a sustained period of time.

Abstract: The present invention provides a compound of the Formula II: wherein X is: R1 is H, —CN, or F; R2 is H or methyl; R3 is H; and R4 is H, methyl, or ethyl; or R3 and R4 joined together form a cyclopropyl ring; or a pharmaceutically acceptable salt thereof.

Abstract: The invention generally relates to methods of using adrenergic receptor agonists for the treatment of skin and mucosal superficial wounds. Some of the preferred adrenergic receptor agonists include epinephrine, phenylephrine, norepinephrine, methoxamine, and mixtures thereof. Methods according to the invention are especially effective to control superficial skin and mucosal bleeding and accelerate healing time.

Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of local pain may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of moderate to severe pain, neuropathic pain, post herpetic neuralgia and rheumatic pains.

Abstract: The present invention relates to novel anesthetic compositions containing a non-polymeric carrier material and an anesthetic, where the compositions are suitable for providing a sustained local anesthesia without an initial burst and having a duration for about 24 hours or longer. Certain compositions are also provided that include a first anesthetic and a second anesthetic. In such compositions, the second anesthetic is a solvent for the first anesthetic and provides an initial anesthetic effect upon administration to a subject. The non-polymeric carrier may optionally be a high viscosity liquid carrier material such as a suitable sugar ester. The compositions can further include one or more additional ingredients including active and inactive materials. Methods of using the compositions of the invention to produce a sustained anesthetic effect at a site in a subject are also provided.

Abstract: A system for dermal delivery of lidocaine, bupivacaine, diclofenac, or ketoprofen is provided which comprises at least two components, for example, a sheet of a solid and flexible material, and a vehicle liquid comprising a solvent and optionally other ingredients. A drug, selected from group consisting of lidocaine, bupivacaine, diclofenac, and ketoprofen, can be impregnated in the sheet or contained in the vehicle liquid. These two components can be stored separately and joined either shortly before or at the time of application. To use the system, the vehicle liquid may be applied either on the target skin area or on the sheet, and the sheet may then be applied on the target skin area so that the vehicle liquid is positioned between the sheet and the skin and brought into contact with the ingredients impregnated in the sheet.

Abstract: The invention provides extended release pro-liposomal, non-aqueous, pharmaceutical formulations of a local anesthetic in the form of a clear oily solution and methods for making same. The formulations can be administered by infiltration into an incision, or by injection.

Abstract: Methods and compositions for controlling plant pests, particularly weeds and/or plant phytopathogens using sarmentine and/or analogs thereof are disclosed.

Abstract: A method for treating subjects experiencing neuropathic pain is provided. The method involves the application of a solid-forming local anesthetic formulation to a skin surface of the subject experiencing the neuropathic pain and then maintaining the formulation on the skin surface for a period of time sufficient to allow itself to transdermally deliver the local anesthetic to the subject thereby providing relief from the neuropathic pain within about 45 minutes.

Abstract: The present invention is directed to kits and methods for the treatment of a patient suffering from post-traumatic stress disorder (PTSD) and/or hot flashes by an administration of a mixture produced by a combination of a long acting local anesthetic combined with clonidine. The combination of the two pharmaceuticals produces a significant increase in duration and speed of onset of sympathetic blockade, increased intensity of the sympathetic blockage as well as the reduction of local anesthetic absorption locally. The combination significantly improves the efficacy, speed of onset and block intensity of a right sided cervical sympathetic ganglion injection (RCSGI) leading to increased length of resolution of PTSD and hot flashes as well as reducing the potential for complications related to absorption of the local anesthetic.

Abstract: The invention relates to novel formulations for topical local anaesthesia and for the use thereof as analgesics, antalgics, or as sexual retardants.

Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.