Abstract: A dosage form article consisting of a hard capsule coated with a surface modifying coating wherein the coating is an aqueous composition comprising water and a muco-adhesive polymer selected from the group consisting of poly(acrylates), cellulose derivatives, hyaluronic acid, starch, poly(ethylene glycol), polysaccharides, collagen derivatives, and mixtures thereof, wherein the ratio of the muco-adhesive polymer to water is less than 0.15 by weight of the coating composition.

Abstract: The invention relates to nanoparticles for the systemic or topical delivery of lipophilic diagnostic or therapeutic agents to a subject in need thereof. The nanoparticles of the invention comprise a water soluble polymer and at least one of a biocompatible lipid and a lipophilic agent. The invention further relates to ophthalmic treatment using the nanoparticles of the invention. In addition, the invention pertains to compositions and formulations comprising the nanoparticle of the invention. Such formulation may be an eye drop formulation.

Abstract: Cationic polymers are provided for delivering anionic active agents, preferably in the form or nanoparticles and other nanostructures. The polymer can be a polycation homopolymer or a copolymer containing a polycation block. The polycations and polycation containing polymers can contain dicarboxylic acid ester units and units of (?-amino acid)-?,?-alkylene diester units. The nanoparticles can contain high loadings of anionic active agents, with sustained release of the active agents. Methods of making the polycations and polycation containing polymers are provided. Methods of making the nanoparticles and formulating them for administration to an individual in need thereof are also provided.

Abstract: It is an object of the present invention to provide a patch having practical adhesive force and cohesive force as a pharmaceutical product, and also exhibiting a fast-acting anesthetic action. The present invention provides a patch formed from an adhesive layer comprising 5% by weight or more and less than 20% by weight of a mixture of lidocaine and another local anesthetic, wherein the adhesive layer comprises at least a rubber-based pressure-sensitive adhesive and liquid paraffin and a content of a tackifier in the adhesive layer is 10% by weight or less.

Abstract: The present invention relates to a nalfurafine-containing percutaneous absorption patch having a support, a drug layer and a control layer which are laminated successively, wherein the drug layer contains at least one kind of a drug selected from the group consisting of nalfurafine and a salt thereof, and capable of maintaining a given level of drug skin permeation amount without permeation of an excess amount of the drug through the skin in a short time even when applied to the skin in which the horny cell layer and the like are damaged and the skin barrier is insufficient.

Abstract: A method for enhancing neurological health and development in a subject involving administering to the subject a nutritional composition including no greater than about 7 g/100 kcal of a fat or lipid source; no greater than about 7 g/100 kcal of a protein or protein equivalent source; at least about 5 g/100 kcal of a carbohydrate; and at least about 9 mg/100 kcal of inositol, wherein the ratio of exogenous inositol to inherent inositol is at least 50:50.

Abstract: The present invention relates to a composition which can effectively control bacteria by containing meso-2,3-butanediol, which is an isomer of 2,3-butane diol, and has excellent antiseptic power even without containing a chemical antiseptic agent.

Abstract: The present invention relates to calcifediol soft capsules, to their use in the treatment or prevention of diseases related to vitamin D deficiency, such as vitamin D deficiency, demineralization such as hypocalcemia and hypophosphatemia, renal osteodystrophy, rickets, osteoporosis, osteopenia, osteoarthritis, osteoarthrosis, osteomalacia, hypoparathyroidism, and inflammatory bowel disease, and to their process of manufacture.

Abstract: This invention relates to pharmaceutical composition and methods of using vitamin A and/or RAR? agonist for the treatment or prevention of diseases or conditions associated with high fat diet and/or vitamin deficiency.

Abstract: Disclosed herein are methods for treating subjects having ADHD identifiable by levels of 3-IS in blood.

Abstract: 2-hydroxy-benzoic anilide compounds and derivatives, compositions thereof, and methods for treating metabolic diseases and cancer through uncoupling mitochondria.

Abstract: The present invention relates to: a pharmaceutical composition for treating cancer containing, as an active ingredient, a metal lactate salt, which can be dissociated, in cancer cells, into lactate capable of effectively inhibiting actions such as proliferation, invasion, and metastasis of cancer cells by disturbing the metabolic processes of cancer cells; a pharmaceutical composition for inhibiting cancer metastasis; a food composition for alleviating cancer; and a method for treating cancer and a method for inhibiting cancer metastasis, both methods comprising a step of administering the lactate metal salt. The metal lactate salts of the present invention inhibits the growth of cancer cells and induces the death of cancer cells by disturbing the metabolic processes in the main energy production pathways of cancer, and inhibits the expression of factors inducing resistance against radiation exposure, while having no side effects.

Abstract: A mesosilicalite nanocarrier having a hierarchical silicalite characterized by a molar ratio of aluminum to silica in a range of 1:3000 to 1:1000. The hierarchical silicalite includes mesopores of a hexagonal structure, and micropores of silicalite structure with a microporous volume in the range of 0.05 cc/g to 0.1 cc/g. The nanocarrier has a mesophase content in the range of 30 wt % to 70 wt %, a microphase content in the range of 30 wt % to 70 wt %, and a mean pore diameter in the range of 1.5 nm to 5.5 nm. A method of preparing the stable mesosilicalite nanocarrier with hierarchical micro/mesopores to load an antioxidant or drug for targeted drug delivery is also described.

Abstract: The present invention relates to the field of seizures. More specifically, the present invention provides compositions and methods for treating refractory seizures in neonates. In one embodiment, the method comprises the steps of (a) administering to the patient an amount of a KCC2 agonist and/or trkB antagonist effective to restore KCC2 expression to normal physiological levels; and (b) administering to the patient an effective amount of an anti-seizure medication.

Abstract: A method of compounding a topical composition includes combining lidocaine and prilocaine, 2.5%/2.5%, cream, diclofenac sodium, 1.5%, topical solution, lidocaine hydrochloride, 4%, topical solution, diclofenac sodium USP powder, lidocaine hydrochloride USP monohydrate powder, and prilocaine hydrochloride USP powder and mixing to generate a cream.

Abstract: A method for administering citrulline to a patient during surgery without filtration of the hemolysis.

Abstract: The present invention is directed to novel anti-inflammatory immunomodulators including creatinine or a creatinine salt, for example, creatinine hydrochloride. The present invention is also directed to methods for treating inflammation and inducing an immunomodulatory response. In particular, the anti-inflammatory immunomodulators are useful for treating an inflammatory condition or an autoimmune disease.

Abstract: [Problem] To provide a composition for external skin use that has anti-inflammatory and antiallergic activity, and is very safe. [Solution] A composition for external skin use for inflammatory diseases contains dihomo-gamma-linolenic acid (DGLA) as the active ingredient thereof. It is preferable for the DGLA to be present as a glyceride, a phospholipid, or an alkyl ester. The amount of DGLA contained in the composition for external use is 0.1-50 wt %.

Abstract: Disclosed herein are methods of preventing, treating, and delaying the onset or progression of diseases associated with hepatic stellate cells (HSCs), such as non-alcoholic fatty liver disease (NAFLD), fibrosis, and liver cancer, using ammonia-lowering therapies.

Abstract: The present invention relates to a composition for neuroprotection comprising a phenyl carbamate compound and a method for providing neuroprotection therewith. The present invention ensures the enhancement of neuroprotection, such that it is promising for preventing or treating various diseases associated with neurological injury.

Abstract: Compounds, methods, and compositions are provided for the treatment of cancer, neurological disorders, and fibrotic disorders. Specifically, the invention includes administering an effective amount of a compound of Formula I, II, or III, or a pharmaceutically acceptable composition, salt, isotopic analog, prodrug, or combination thereof, to a subject suffering from a cancer, neurological disorder, or fibrotic disorder.

Abstract: The present invention features a composition comprising mupirocin and neomycin, a formulation thereof and a method of treating microbial infection using the composition.

Abstract: Amisulpride is used in the therapy of nausea, vomiting or retches. The therapy may utilize a novel injectable formulation, in unit dosage form, comprising less than 50 mg amisulpride.

Abstract: Methods for increasing the encapsulation or incorporation of Sunitinib into polymeric matrices have been developed. The resulting formulations provide for more sustained controlled release of sunitinib or other inhibitors of JNK signaling, which bind to DLK. Increased loading is achieved using an alkaline solvent system. The pharmaceutical compositions can be administered to treat or reduce neuronal death due to elevated intraocular pressure. Upon administration, the sunitinib or other inhibitor is released over an extended period of time at concentrations which are high enough to produce therapeutic benefit, but low enough to avoid unacceptable levels of cytotoxicity, and which provide much longer release than inhibitor without conjugate.

Abstract: Compositions and methods for the treatment of ocular diseases are disclosed.

Abstract: Disclosed herein are spirocyclic compounds, together with pharmaceutical compositions and methods of ameliorating and/or treating a cancer described herein with one or more of the compounds described herein.

Abstract: The present invention relates to pharmaceutical compositions for treating cancer comprising BRAF inhibitors, (e.g. vemurafenib) and/or MEK inhibitor, (e.g. trametinib, RO5068760), in combination with anti-tubulin compounds of the invention or other known tubulin inhibitors, and using such compositions for treating cancer such as melanoma, drug-resistant cancer, and cancer metastasis.

Abstract: The invention relates to pharmaceutical compositions comprising: (a) at least one angiotensin receptor blocker or a pharmaceutically acceptable salt thereof, and (b) at least one chemokine receptor pathway inhibitor or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising: (a) at least one angiotensin receptor blocker or a pharmaceutically acceptable salt thereof; and (b) at least one chemokine receptor pathway inhibitor or a pharmaceutically acceptable salt thereof which inhibits a component of the chemokine receptor pathway other than the chemokine receptor. Oral sustained release pharmaceutical compositions comprising the pharmaceutical composition, as well as injectable sustained release pharmaceutical compositions comprising the pharmaceutical composition are described. The invention further relates to tablets, capsules, injectable suspensions, and compositions for pulmonary or nasal delivery comprising the pharmaceutical composition.

Abstract: The present disclosure relates to the use of 2-iminobiotin for treating brain cell injury, in particular in adults. The treatment may be used for the treatment of cerebral hypoxia-ischemia and/or reperfusion injury, including one or more symptoms thereof. Provided are methods of treatment comprising administering a therapeutically effective dose of 2-iminobiotin to an individual in need thereof.

Abstract: Various compounds, compositions, and methods for inhibition of Rit1 are presented. In especially preferred aspects, contemplated compounds and compositions are suitable for treatment of cancers and other diseases associated with Rit1 signaling.

Abstract: The present invention relates to novel 5-(fluoroalkyl)-1-aryl-1,2,4-triazole derivatives, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of renal and cardiovascular diseases.

Abstract: A pharmaceutical composition comprising antibacterial agent and tazobactam, wherein the ratio of tazobactam to the antibacterial agent in the composition is in the range of from about 0.5 to about 2 gram of tazobactam per gram of the antibacterial agent, are disclosed.

Abstract: The present invention provides methods and compositions for treating chemotherapy induced peripheral neuropathy. One embodiment of the present invention is directed to a method of treating chemotherapy induced peripheral neuropathy by administering to a patient in need at least one thiosemicarbazone compound.

Abstract: The present invention provides dosing regimens for administering pharmacological chaperones to a subject in need thereof. The dosing regimens can be used to treat disorders caused by improper protein misfolding, such as lysosomal storage disorders.

Abstract: Behavioral pharmacological data with the compound of formula (I), a novel and selective 5HT2A/2C receptor inverse agonist, demonstrate in vivo efficacy in models of psychosis and dyskinesias. This includes activity in reversing MK-801 induced locomotor behaviors, suggesting that this compound may be an efficacious anti-psychotic, and activity in an MPTP primate model of dyskinesias, suggesting efficacy as an anti-dyskinesia agent. These data support the hypothesis that 5HT2A/2C receptor inverse agonism may confer antipsychotic and anti-dyskinetic efficacy in humans, and indicate a use of the compound of formula (I) and related agents as novel therapeutics for Parkinson's Disease, related human neurodegenerative diseases, and psychosis.

Abstract: The present invention provides for a method of treating cancer and/or reducing proliferation of cancer cells, the method comprising administering to a subject in need of such treatment a composition comprising a PIM kinase inhibitor that exhibits changes of mRNA splicing in combination with a compound that modulates/inhibits activity of an RNA splicing factor protein. Further, changes in splicing of mRNAs and phosphorylation of RNA splicing factors can be used as biomarkers for patient responsiveness to anti-PIM treatment and also suggest effective combinatorial therapies, including synergistic combination.

Abstract: In one aspect, the invention relates to substituted 1-phenyl-3-(piperidin-4-yl)urea analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the DCN1-UBC12 interaction inhibitors of DCN1-mediated cullin-RING ligase activity, methods of making same, pharmaceutical compositions comprising same, methods of treating disorders using the disclosed compounds and compositions, methods of treating disorders associated with a DCN1-UBC12 interaction dysfunction, methods of treating disorders associated with a DCN1-mediated cullin-RING ligase activity dysfunction, methods of male contraception comprising the disclosed compounds and compositions, and kits comprising the disclosed compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: Methods of selectively inhibiting Akt3 are provided. It has been discovered that 4-[(6-nitroquinolin-4-yl)amino]-N-[4-(pyridin-4-ylamino)phenyl]benzamide selectively inhibits Akt3. Because Akt3 modulates the suppressive function of natural Tregs and the polarization of induced Tregs, 4-[(6-nitroquinolin-4-yl)amino]-N-[4-(pyridin-4-ylamino)phenyl]benzamide can be used for modulating immune responses.

Abstract: Derivatives of 1,2,3,4-tetrahydroisoquinoline (THIQ) having the general formula A-(CH2)n—B are provided, wherein A is THIQ or a substituted derivative thereof and B is an aryl, cycloalkylaryl, or cycloalkyl group, wherein A and B are linked to each other by an alkyl or substituted alkyl chain. The compounds are useful as selective ligands (agonists or antagonists) of central nervous system receptors, and in particular of the seratonin receptors. The compounds or their salts can be formulated into pharmaceutical in need thereof by any route of administration suitable for a desired treatment protocol and especially for the treatment of psychiatric disorders.

Abstract: Provided herein are compounds and methods for achieving a sustained therapeutic effect of small molecule anti-cancer agents when administered in vivo.

Abstract: An abuse-deterrent pharmaceutical composition has been developed to reduce the likelihood of improper administration of drugs, especially drugs such as opiods. In the preferred embodiment, the drug is modified to increase its lipophilicity by forming a salt between the drug and one or more fatty acids wherein the concentration of the one or more fatty acids is one to 15 times the molar amount of the active agent, preferably two to ten times the molar amount of the active agent. In one embodiment the modified drug is homogeneously dispersed within microparticles composed of a material that is either slowly soluble or not soluble in water. In some embodiments the drug containing microparticles or drug particles are coated with one or more coating layers, where at least one coating is water insoluble and preferably organic solvent insoluble.

Abstract: An abuse-deterrent pharmaceutical composition has been developed to reduce the likelihood of improper administration of drugs, especially drugs such as opioids. In a preferred embodiment, a drug is modified to increase its lipophilicity. In some embodiments the modified drug is homogeneously dispersed within spherical microparticles composed of a material that is either slowly soluble or not soluble in water. In some embodiments the drug containing microparticles or drug particles are coated with one or more coating layers, where at least one coating is water insoluble and/or organic solvent insoluble. The abuse-deterrent composition retards the release of drug, even if the physical integrity of the formulation is compromised (for example, by chopping with a blade or crushing) and the resulting material is placed in water, snorted, or swallowed. However, when administered as directed, the drug is slowly released from the composition as the composition is passes through the GI tract.

Abstract: The present invention relates generally to the co-administration of an opioid agonist compound and an analgesic compound. In addition, the invention relates to, among other things, dosage forms for co-administration of an opioid agonist compound and an analgesic compound, methods for administering an opioid agonist compound and an analgesic compound, compositions comprising an opioid agonist compound and an analgesic compound, dosage forms comprising an opioid agonist compound and an analgesic compound, and so on.

Abstract: Provided herein are prodrugs of opioid receptor antagonists such as nalmefene and naltrexone, pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of behavioral disorders.

Abstract: The invention provides compounds and compositions useful for the modulation of certain enzymes. The compounds and compositions can induce of cell death, particularly cancer cell death. The invention also provides methods for the synthesis and use of the compounds and compositions, including the use of compounds and compositions in therapy for the treatment of cancer and selective induction of apoptosis in cells.

Abstract: The disclosed embodiments relate to methods of initiating aripiprazole treatment in a patient who is a CYP2D6 poor metabolizer or a CYP3A4 poor metabolizer, or both.

Abstract: The present invention provides a urea derivative or a pharmacologically acceptable salt thereof that has a formyl peptide receptor like 1 (hereinafter may be abbreviated as FPRL1) agonist effect, a pharmaceutical composition containing the urea derivative or the pharmacologically acceptable salt thereof, and a pharmaceutical use thereof. It has been found that a urea derivative represented by the general formula (I) below or a pharmacologically acceptable salt thereof has a superior FPRL1 agonist effect. Compound (I) or a pharmacologically acceptable salt thereof is highly useful for treatment, prevention, or suppression of inflammatory diseases, chronic airway diseases, cancers, septicemia, allergic symptoms, HIV retrovirus infection, circulatory disorders, neuroinflammation, nervous disorders, pains, prion diseases, amyloidosis, immune disorders and the like.

Abstract: The present invention relates to a tablet comprising Afatinib or a pharmaceutically acceptable salt thereof, wherein the tablet is obtained by direct compression. The present invention further relates to a process for manufacturing a tablet of the invention as well as the use of the tablet of the invention.

Abstract: Methods of treatment of conditions or diseases associated with myeloid differentiation primary response (MYD88) protein using a selective HCK inhibitor are provided herein.

Abstract: Disclosed are methods of synthesis and/or purification of certain 3,7-diamino-phenothiazin-5-ium compounds (“diaminophenothiazinium compounds”) including Methylthioninium Chloride (MTC) (Methylene Blue), and the resulting high purity characterized by a purity greater than 98%, and very low levels of heavy metals and organic impurities Azure A, B, C and MVB. Also disclosed are methods of treatment of a tauopathy or methemoglobinemia in a patient in need thereof, comprising administering to the patient a therapeutically effective amount of the high-purity diaminophenothiazinium compound.