Abstract: Crystalline, anhydrous hydrochloride salts of 4,5?-epoxy-3,14-dihydroxy-17-methylmorphinan-6-one (oxymorphone) are disclosed and three polymorphic forms of these salts are reported. The invention further relates to a method for the production of such salts, a pharmaceutical composition comprising an effective amount of such a salt and such a salt as a medicament and for the treatment and/or prevention of pain.

Abstract: A solid oral controlled-release dosage form of hydrocodone is disclosed, the dosage form comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and controlled release material.

Abstract: A method of inhibiting the growth of cancer cells is disclosed in which cancer cells that contain an enhanced amount relative to non-cancerous cells of one or more of phosphorylated mTOR, Akt1, ERK2 and serine2152-phosphorylated filamin A are contacted with an FLNA-binding effective amount of a compound or a pharmaceutically acceptable salt thereof that binds to the pentapeptide of filamin A (FLNA) of SEQ ID NO: 1 and exhibits at least about 60 percent of the FITC-labeled naloxone binding amount when present at a 10 ?M concentration and using unlabeled naloxone as the control inhibitor at the same concentration. A compound that binds to the FLNA pentapeptide preferably also contains at least four of the six pharmacophores of FIGS. 19-24.

Abstract: A neutral poly(ethyl acrylate, methyl methacrylate) copolymer is employed as a carrier in the manufacture of pharmaceutical formulations containing an active ingredient. The formulations are preferably made by melt extrusion, and can have rubbery characteristics and can exhibit tamper resistance.

Abstract: Disclosed in certain embodiments is a controlled release oral dosage form comprising a therapeutically effective amount of a drug susceptible to abuse together with one or more pharmaceutically acceptable excipients; the dosage form further including a gelling agent in an effective amount to impart a viscosity unsuitable for administration selected from the group consisting of parenteral and nasal administration to a solubilized mixture formed when the dosage form is crushed and mixed with from about 0.5 to about 10 ml of an aqueous liquid; the dosage form providing a therapeutic effect for at least about 12 hours when orally administered to a human patient.

Abstract: Disclosed in certain embodiments is a controlled release oral dosage form comprising a therapeutically effective amount of a drug susceptible to abuse together with one or more pharmaceutically acceptable excipients; the dosage form further including a gelling agent in an effective amount to impart a viscosity unsuitable for administration selected from the group consisting of parenteral and nasal administration to a solubilized mixture formed when the dosage form is crushed and mixed with from about 0.5 to about 10 ml of an aqueous liquid; the dosage form providing a therapeutic effect for at least about 12 hours when orally administered to a human patient.

Abstract: A method of providing a patient with controlled release of a phenolic opioid using a prodrug capable, upon enzymatic activation, of releasing the phenolic opioid through intra-molecular cyclization leading to formation of a cyclic urea, carbamate or thiocarbamate.

Abstract: The present invention generally relates to processes for preparing highly pure morphinan-6-one products. The processes involve reducing the concentration of alpha, beta unsaturated ketone compounds present as impurities in morphinan 6 one products or reaction mixtures including morphinan 6 one compounds by treatment with a sulfur-containing compound.

Abstract: Disclosed in certain embodiments is a controlled release oral dosage form comprising a therapeutically effective amount of a drug susceptible to abuse together with one or more pharmaceutically acceptable excipients; the dosage form further including a gelling agent in an effective amount to impart a viscosity unsuitable for administration selected from the group consisting of parenteral and nasal administration to a solubilized mixture formed when the dosage form is crushed and mixed with from about 0.5 to about 10 ml of an aqueous liquid; the dosage form providing a therapeutic effect for at least about 12 hours when orally administered to a human patient.

Abstract: The invention is directed to sustained release formulations containing oxycodone or a pharmaceutically acceptable salt thereof which provide a mean C24/Cmax oxycodone ratio of 0.6 to 1.0 or 0.7 to 1 after oral administration at steady state to patients and methods thereof.

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: Disclosed are compositions for affecting weight loss comprising a first compound and a second compound, where the first compound is an opioid antagonist and the second compound causes increased agonism of a melanocortin 3 receptor (MC3-R) or a melanocortin 4 receptor (MC4-R) compared to normal physiological conditions. Also disclosed are methods of affecting weight loss, increasing energy expenditure, increasing satiety in an individual, or suppressing the appetite of an individual, comprising identifying an individual in need thereof and treating that individual to antagonize opioid receptor activity and to enhance ?-MSH activity.

Abstract: The present invention relates to co-extruded pharmaceutical compositions and dosage forms including an active agent, such as an opioid agonist, and an adverse agent, such as an opioid antagonist. Such compositions and dosage forms arc useful for preventing or discouraging tampering, abuse, misuse or diversion of a dosage form containing an active pharmaceutical agent, such as an opioid. The present invention also relates to methods of treating a patient with such a dosage form, as well as kits containing such a dosage form with instructions for using the dosage form to treat a patient.

Abstract: The invention relates to the compounds of formula I and formula II 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 or formula II, and methods for treating chronic pain in a disease may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection.

Abstract: Disclosed in certain embodiments is a controlled release oral dosage form comprising a therapeutically effective amount of a drug susceptible to abuse together with one or more pharmaceutically acceptable excipients; the dosage form further including a gelling agent in an effective amount to impart a viscosity unsuitable for administration selected from the group consisting of parenteral and nasal administration to a solubilized mixture formed when the dosage form is crushed and mixed with from about 0.5 to about 10 ml of an aqueous liquid; the dosage form providing a therapeutic effect for at least about 12 hours when orally administered to a human patient.

Abstract: Disclosed in certain embodiments is a controlled release oral dosage form comprising a therapeutically effective amount of a drug susceptible to abuse together with one or more pharmaceutically acceptable excipients; the dosage form further including a gelling agent in an effective amount to impart a viscosity unsuitable for administration selected from the group consisting of parenteral and nasal administration to a solubilized mixture formed when the dosage form is crushed and mixed with from about 0.5 to about 10 ml of an aqueous liquid; the dosage form providing a therapeutic effect for at least about 12 hours when orally administered to a human patient.

Abstract: The present invention relates to processes for removal of Michael acceptors from certain compositions wherein the composition is treated with a thiol-containing compound under conditions sufficient to remove Michael acceptors and the resulting thiol-Michael adducts. Certain embodiments of the present invention enable quantification and/or removal of Michael acceptors and/or Michael acceptor precursors.

Abstract: The present invention relates to a plurality of dosage forms comprising a first dosage form and second dosage form each comprising a therapeutic agent, such as an opioid; wherein the dosage strength of the second dosage form is greater than that of the first dosage form; and wherein the steady state Cave and the steady state AUC of the first and second dosage forms are dose proportional and the single dose Cmax of the second dosage form is less than the minimum level for dose proportionality with respect to the first dosage form. The present invention also relates to methods of administering such dosage forms to a patient, as well as to kits comprising such dosage forms and instructions for administration of the dosage forms to a patient. The inventors believe that the dosage forms and methods of the present invention will lead to improved safety and patient acceptance.

Abstract: The invention relates to an improved method of preparing oxymorphone or a salt thereof from oripavine. In particular, the invention relates to a method of preparing oxymorphone with a content of alpha-beta-unsaturated ketones (ABUK) <10 ppm, wherein the content of 8,14-dihydroxydihydromorphinone in the prepared oxymorphone is >10 ppm.

Abstract: The present invention relates to an intranasal pharmaceutical dosage form comprising a dosing unit comprising naloxone or a pharmaceutically acceptable salt thereof in an amount of equivalent to ?0.5 mg naloxone HCl dissolved in an application fluid of a volume of ?250 ?l. Furthermore, the present invention relates to such an intranasal pharmaceutical dosage form for use in the treatment of opioid overdosing and/or at least one symptom thereof.

Abstract: Controlled release formulations and methods for preparing controlled release formulations for delivery of active drug substances are described herein. The formulations described herein may be employed to produce pharmaceutical compositions, such as controlled release dosage forms, adjusted to a specific administration scheme.

Abstract: Pro-drugs containing an electron withdrawing substituent, as defined in the specification, are useful in a method for providing a patient with post administration-activated, controlled release of a biologically active compound.

Abstract: Described are immediate release oral dosage forms that contain abuse-deterrent features. In particular, the disclosed dosage forms provide deterrence of abuse by ingestion of multiple individual doses. In addition, the disclosed dosage forms provide protection from overdose in the event of accidental or intentional ingestion of multiple individual doses.

Abstract: Described are immediate release oral dosage forms that contain abuse-deterrent features. In particular, the disclosed dosage forms provide deterrence of abuse by ingestion of multiple individual doses. In addition, the disclosed dosage forms provide protection from overdose in the event of accidental or intentional ingestion of multiple individual doses.

Abstract: Described are oral dosage forms that contain abuse-deterrent features and that contain core-shell polymers that include an active pharmaceutical ingredient, with particular examples including immediate release dosage forms that contain a drug that is commonly susceptible to abuse.

Abstract: A compound of formula I is disclosed. Compounds of formula I are useful as analgesics, anti-inflammatory agents, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.

Abstract: Described are oral dosage forms that contain abuse-deterrent features and that contain core-shell polymers that include an active pharmaceutical ingredient, with particular examples including immediate release dosage forms that contain a drug that is commonly susceptible to abuse.

Abstract: Described are oral dosage forms that contain abuse-deterrent features and that contain core-shell polymers that include an active pharmaceutical ingredient, with particular examples including immediate release dosage forms that contain a drug that is commonly susceptible to abuse.

Abstract: This invention relates to the use of a composition comprising opioid/Toll-like receptor 4 (TLR4) antagonists and dextro enantiomers thereof for the treatment of pain, where the opioid antagonists treat pain by blocking TLR4. More preferably, the dextro opioid/TLR4 antagonist enantiomer treats pain by blocking TLR4 while not affecting the opioid receptors and therefore avoiding adverse effects associated with blocking the opioid receptors. Examples of opioid antagonist and their dextro enantiomers include naltrexone, naloxone and nalmefene, and pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof and their use in the treatment of pain, particularly neuropathic pain.

Abstract: Disclosed are compositions for treatment of pain comprising, a first compound and a second compound, the first compound is an opioid antagonist that treats pain by blocking Toll-like receptor (TLR4) and the second compound is an alpha-2-delta ligand that enhances the pain treatment effect of the first compound. Examples of opioid antagonist include naltrexone, naloxone and nalmefene. Examples of an alpha-2-delta ligand include gabapentin and pregabalin, synergistic pharmaceutical compositions thereof, and their use in the treatment, prevention, and reversal of neuropathic pain.

Abstract: A solid oral controlled-release dosage form of hydrocodone is disclosed, the dosage form comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and controlled release material.

Abstract: Combinations comprise a therapeutically effective amount of one or more stimulants and and/or pharmaceutically acceptable analogs, salts, or hydrates of the one or more stimulants, and one or more non-selective opioid receptor antagonists, and/or pharmaceutically acceptable analogs, salts or hydrates of the one or more non-selective opioid receptor antagonists. These combinations may be used for treating obesity via administration to a subject having a need thereof.

Abstract: Disclosed are oral dosage forms, comprising (i) a therapeutically effective amount of an opioid agonist; (ii) an opioid antagonist in releasable form; and (iii) a sequestered opioid antagonist which is not released when the dosage form is administered intact, and methods thereof.

Abstract: The present invention provides processes for preparing nal-opiates without the isolation of intermediates. In general, the process provides for alkylation and reduction in the same pot to give the nal-opiate.

Abstract: Naloxol-polyethlyene glycol conjugates of the formula: are provided in oxalate or phosphate salt forms including crystalline forms. Methods of preparing the salt forms and pharmaceutical compositions comprising the salt forms are also provided.

Abstract: Methods, compositions, systems, and packaging are disclosed for reducing postoperative nausea and/or vomiting (PONV) in a human patient in need of general anesthesia for surgery. Such methods may include scheduling a surgery for the human patient, and administering to the patient one or more series of prescribed medicines for at least three successive days during a regimen immediately preceding general anesthesia. Compositions may include cholinergic receptor agonists, muscarinic receptor agonists, dopamine receptor agonists, MAO inhibitors, serotonin receptor agonists, selective serotonin reuptake inhibitors, serotonin-norepinephrine reuptake inhibitors, selective serotonin releasing agents, serotonin-norepinephrine-dopamine reuptake inhibitors, opioids, or analgesics.

Abstract: Disclosed in certain embodiments is a controlled release oral dosage form comprising a therapeutically effective amount of a drug susceptible to abuse together with one or more pharmaceutically acceptable excipients; the dosage form further including a gelling agent in an effective amount to impart a viscosity unsuitable for administration selected from the group consisting of parenteral and nasal administration to a solubilized mixture formed when the dosage form is crushed and mixed with from about 0.5 to about 10 ml of an aqueous liquid; the dosage form providing a therapeutic effect for at least about 12 hours when orally administered to a human patient.

Abstract: The present invention relates to immediate release pharmaceutical compositions for oral administration that are resistant to abuse by intake of alcohol. In particular, this disclosure provides immediate release pharmaceutical compositions comprising a polyglycol having a molecular weight of from about 900 to about 17,000 daltons, a drug substance, one or more effervescent agents, and, optionally, one or more disintegrants, such that the composition is formulated to be resistant to abuse by intake of alcohol.

Abstract: A tablet that includes a solid solution of soluble fiber and one or more sugar alcohols, the solid solution having a glass transition temperature of less than 40° C., and one or more additives dispersed in the solid solution such that at least one additive is released from the tablet when the tablet is chewed or dissolved within an oral cavity.

Abstract: An improved process for the N-alkylation of tertiary morphinan alkaloid bases to form the corresponding quaternary morphinan alkaloid derivatives.

Abstract: Disclosed in certain embodiments is a controlled release oral dosage form comprising a therapeutically effective amount of a drug susceptible to abuse together with one or more pharmaceutically acceptable excipients; the dosage form further including a gelling agent in an effective amount to impart a viscosity unsuitable for administration selected from the group consisting of parenteral and nasal administration to a solubilized mixture formed when the dosage form is crushed and mixed with from about 0.5 to about 10 ml of an aqueous liquid; the dosage form providing a therapeutic effect for at least about 12 hours when orally administered to a human patient.

Abstract: Disclosed in certain embodiments is a method of treating or preventing an opioid-induced adverse pharmacodynamic response comprising administering to a patient in need thereof an effective amount of buprenorphine.

Abstract: The instant application relates to morphinan derivatives of formula I with enhanced oral bioavailability for the treatment of diseases associated with opioid receptor activity or blockade including alcohol and opiate addiction.

Abstract: The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydrocodone (morphinan-6-one, 4,5-alpha-epoxy-3-methoxy-17-methyl) to form novel prodrugs/compositions of hydrocodone, including benzoates and heteroaryl carboxylic acids, which have a decreased potential for abuse of hydrocodone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

Abstract: The disclosed invention is drawn to pharmaceutical tablets that provide delivery of active agents having at least three oxygen-containing groups, a tri-oxy active agent, as well as a second active ingredient. Non-limiting examples of three oxygen-containing group active agents include guaifenesin, codeine, hydrocodone, and their pharmaceutically acceptable salts. In one embodiment, a pharmaceutical tablet for oral administration once every 12 hours is provided. The tablet includes a first active agent that is a tri-oxy active agent, a second active agent, and a release rate controlling non-ionic oxyl-containing hydrophilic polymer. The total oxyl content of the hydrophilic polymer in the tablet is from about 4×10?4 moles to about 2.0×10?3 moles.

Abstract: The present invention provides sustained-release oral pharmaceutical compositions and methods of use. The sustained-release oral pharmaceutical compositions include an opioid (including salts thereof) and a salt of a non-steroidal anti-inflammatory drug (NSAID).

Abstract: The present invention concerns a needle-less drug delivery device being suitable for delivering drugs through a skin surface into a human or animal body comprising a pharmaceutical composition with at least one analgesic agent preferably being an opioid. The present invention also relates to the use of at least one analgesic agent, preferably being at least one opioid in a needle-less drug delivery device being suitable for injecting medication through a skin surface into the human or animal body. Further, the invention is concerned with a method of treating breakthrough pain by injecting at least one analgesic agent preferably being an opioid into the human or animal body using a needle-less drug delivery device.

Abstract: The present invention relates to methods for treating pruritus with anti-pruritic compositions.

Abstract: Provided are nutraceutical or dietary supplemental compositions comprising esterified capsaicinoids. The esterified capsaicinoids may converted to the active parent capsaicinoid compound following enzymatic or chemical hydrolysis. In various embodiments, these esterified capsaicinoids have a higher lipophilicity, lipid solubility and result in less irritation to the stomach than the parent capsaicinoid, and hence may be included in certain dietary supplement formulations, including capsules, pills and tablets dietary supplement formulations. The dietary supplement compositions may be used for pain management in mammals in vivo and/or in the treatment of various pathological conditions in humans.

Abstract: Disclosed is a pharmaceutical composition comprising from about 5 to about 20 mg of hydrocodone or a pharmaceutically acceptable salt thereof and from 0.055 to about 0.56 mg naltrexone or pharmaceutically acceptable salt thereof.