Abstract: In certain embodiments, this disclosure relates to KRAS agonists, pharmaceutical composition, and uses in managing cancer. In certain embodiments, the KRAS agonist is 4-(4-(2-bromoacetamido)butyl)benzoic acid, salt, prodrug, or derivative thereof. In certain embodiments, this disclosure relates to methods of treating cancer comprising administering an effective amount of a compound of Formula I, salt, prodrug, or derivative thereof, to a subject in need thereof, wherein, substituents are reported herein.

Abstract: The objective of the present invention is to provide a capsule filling composition which can stably produce a capsule formulation by suppressing the flow of components out of the capsule body during capsule filling, regardless of the compressibility of an active ingredient such as drugs and health foods, so that a favorable capsule filling can be achieved; and a method of producing a capsule formulation with the use of such a capsule filling composition, as well as a capsule formulation. The objective is achieved by a method of producing a capsule formulation, comprising subjecting a capsule filling composition containing an active ingredient and a cellulose ether powder to a funnel system powder filling or a die-compression system powder filling to obtain the capsule formulation, and the like.

Abstract: Unpurified or low pure soy phosphatidylserine is used to make cochleates. The cochleates contain about 40-74% soy phosphatidylserine, a multivalent cation and a biological active. A preferred cochleate contains the antifungal agent amphotericin B.

Abstract: This invention discloses uses for sulindac in preparing anti-lung cancer products. This invention provides uses for sulindac in the preparation of products to treat lung cancer. From carrying out cancer drug repositioning for the FDA- and CFDA-approved drug sulindac, experiments for this invention show, based on screening of non-anti-cancer drugs for various cancer cell lines (tissue types) and mutation sites, that sulindac has a new use as an anti-lung cancer medication, thus achieving a new purpose for an old drug.

Abstract: An antimicrobial medical device that includes a substrate having a metal surface that is made from a metal or metal alloy that may include stainless steel, cobalt, and titanium. Disposed on the metal surface is a first antimicrobial oxide layer that includes an antimicrobial metal that may include silver, copper, and zinc, and combinations thereof. The atoms of antimicrobial metal in the first antimicrobial oxide layer are of a first concentration. The first antimicrobial oxide layer is positioned in a direction opposite that of the metal surface. The device further includes a second antimicrobial oxide layer that includes an antimicrobial metal that may be silver, copper, and zinc, and combinations thereof. The atoms of the antimicrobial metal present in the second antimicrobial oxide layer are of a second concentration. The first concentration and the second concentration are not equal. Methods for making the antimicrobial medical device are also disclosed.

Abstract: The present invention concerns a pet litter comprising a composition comprising 2,2-dimethyl-1,3-dioxolane-4-methanol. The present invention further relates to methods and uses of a composition comprising 2,2-dimethyl-1,3-dioxolane-4-methanol in pet litters, in particular for promoting in-litter elimination by pets.

Abstract: The invention discloses an instant hand-protection antibacterial gel, a method for preparing the same and use of the same, and belongs to the technical field of antibacterial disinfection. The instant hand-protection antibacterial gel of the present invention comprises: hydrolyzed sodium hyaluronate 0.01-0.5%, keratin care agent 0.01%-5%, thickener 0.1-0.5%, emollient 1-10%, pH regulator 0.1-0.5%, ethanol 56-75%, and the balance is water; and an average molecular weight of the hydrolyzed sodium hyaluronate is one or more of 500-20000 Daltons.

Abstract: The present application relates to a method for preparing a pharmaceutical composition, the method comprising providing pharmaceutical compound having a solubility in water of 1 mg/ml or less at 25° C. in a solvent enabling solubilizing the pharmaceutical compound at least partly into the solvent, providing an aqueous dispersion of nanostructured cellulose, and combining the pharmaceutical compound with the aqueous dispersion of nanostructured cellulose in an anti-solvent process to provide nanosized pharmaceutical particles having an average diameter of 50 nm or less, to provide a pharmaceutical composition. The present application also provides pharmaceutical composition, and use of the pharmaceutical composition.

Abstract: The current invention provides a method of activating fibroblast and myofibroblast apoptosis in a tissue of a mammal, comprising administering to the tissue a therapeutically effective amount of a composition comprising an siRNA molecule that binds to an mRNA that codes for TGFB1 protein in a mammalian cell, an siRNA molecule that binds to an mRNA that codes for COX-2 protein in a mammalian cell, and a pharmaceutically acceptable carrier comprising a pharmaceutically acceptable histidine-lysine polymer. The invention also provides additional methods for using this composition.

Abstract: Embodiments of the present disclosure include formulations of silk-based product (SBP) formulations and related methods of preparation and use in a variety of applications in the fields of human therapeutics, veterinary medicine, agriculture, and material science.

Abstract: This invention relates to a method of evaluating powder for lamination shaping by stable criteria. In this method, it is evaluated whether powder for lamination shaping can be spread into a uniform powder layer in the lamination shaping, wherein the powder is evaluated using, as a flowability of the powder, an adhesive force of the powder calculated from a failure envelope obtained by a shear test. The shear test is conducted by a powder rheometer, and the adhesive force is obtained from the relationship between a normal stress and a shearing stress at the powder rheometer. If the adhesive force is 0.450 kPa or less, the powder is evaluated to be spread into a uniform powder layer in the lamination shaping. Furthermore, if at least one of that the 50% particle size of the powder obtained by a laser diffraction method is 3 to 250 ?m and that the apparent density of the powder is 3.5 g/cm3 or more is satisfied, the powder is evaluated to be spread into a uniform powder layer in the lamination shaping.

Abstract: The present invention relates to combination therapies for treating Alzheimer's disease or an amyloidosis-associated pathological condition comprising co-administering a therapeutically effective amount of a first compound, and a therapeutically effective amount of a second compound. In certain embodiments, the first compound or the second compound inhibits AB peptide polymerization; is an anti-inflammatory; improves cognitive function, mood, or social behavior; is associated with Tau or alpha-synuclein; or regulates amyloid peptide washout.

Abstract: The present disclosure provides a composition that maintains a high and desirable viscosity while having a high amount of alcohol. Suitable thickeners and gelling agents are mixed with the alcohol to achieve this effect. An emulsion stabilizer can also be added. These components can also be combined with a sunscreen. The resulting composition provides benefits such as cooling and desirable skin feel, but is still easily spreadable and viscous enough to function effectively as a sunscreen.

Abstract: Provided are compositions for inhibiting a biological activity of an aldoketo reductase family 1, member C3 (AKR1 C3) polypeptide. In some embodiments, the compositions are indomethacin derivatives that are AKR1 C3-specific inhibitors. Also provided are methods for producing disclosed indomethacin derivatives that substantially lack cyclooxygenase inhibitory activity but that have AKR1C3 inhibitory activity, methods for inhibiting AKR1C3 polypeptide biological activities, and methods for treating prostate tumors in subjects.

Abstract: Novel drug carriers capable of targeted and/or pH dependent release of biologically active agents into selected pH environments including the gastrointestinal (GI), ophthalmic, urinary, or reproductive tracts. Unexpectedly, carriers including free fatty acids (FFA) are able to deliver biologically active agents to various pH environments. Such targeted delivery is tailorable and useful for active agents that are: (a) injurious to the upper GI tract (esophagus, stomach, and duodenum), (b) acid labile, (c) impermeable/insoluble compounds in GI fluids, (d) susceptible to first pass metabolism, and/or (e) cause stomach irritation, upset, or dyspepsia.

Abstract: Provided are methods, test devices, and diagnostic kits for predicting, assessing, and diagnosing the risk of a disease using salivary analysis. The methods comprise providing a whole (unfractionated) saliva sample from a subject; contacting an aliquot of the saliva with two or more lectins under conditions that allow the two or more lectins to bind to a lectin-binding component of the saliva; detecting the amount of bound lectin; and comparing the amount of bound lectin to the amount known to bind a saliva sample from a control patient, to predict the risk of a disease in the subject. Also provided are methods for reducing the risk of a disease and a method for assessing the risk of the disease at a defined level.

Abstract: A nanodevice composition including N-acetyl cysteine linked to a dendrimer, such as a PAMAM dendrimer or a multiarm PEG polymer, is provided. Also provided is a nanodevice for targeted delivery of a compound to a location in need of treatment. The nanodevice includes a PAMAM dendrimer or multiarm PEG polymer, linked to the compound via a disulfide bond. There is provided a nanodevice composition for localizing and delivering therapeutically active agents, the nanodevice includes a PAMAM dendrimer or multiarm PEG polymer and at least one therapeutically active agent attached to the PAMAM dendrimer or multiarm PEG polymer.

Abstract: The invention relates to a cellprotective, neuroprotective and retinoprotective composition. In an embodiment of the invention, said composition comprises (i) Ramipril or Ramiprilate and (ii) folic acid. The composition of the invention can be used, in particular, for the prevention of loss of vision, or even for improving visual acuity and visual field in normal subjects, as well as for treating ophthalmologic pathologies, in particular: glaucoma, diabetic retinopathy, age related macular degeneration, hereditary dystrophy of the retina, uveitis, ammetropia (myopia, presbyopia). This combination of active principles could also be used in general conditions for treating general pathologies (cancer . . . ).

Abstract: The present invention relates to nanocrystalline solid dispersion compositions having discrete particles, wherein each discrete particle comprises crystals of at least one pharmaceutical active; veterinary active; nutraceutical active dispersed in the matrix of at least one crystallization inducer and/or coexisting with crystals of crystallization inducer, optionally along with pharmaceutically acceptable excipients. The present invention also encompasses a novel one-step process for generation of nanocrystalline solid dispersions. The present invention is particularly of use for improving the dissolution of pharmaceutical actives, veterinary actives; nutraceutical actives exhibiting dissolution-limited bioavailability. Dissolution enhancement is because of the decreased crystallite size of the pharmaceutical active.

Abstract: The present invention relates to methods and compositions for the prevention or treatment of chronic obstructive pulmonary disease.

Abstract: There is provided compositions and methods for the treatment of respiratory conditions such as pulmonary hypertension and sickle-cell disease in a patient in need thereof. The composition and method are for treating a patient in need thereof by inhalation of a composition containing amino acid ester compounds comprising at least one nitric oxide releasing group and pharmaceutical salts thereof.

Abstract: The present invention relates to methods for producing particles of indomethacin using dry milling processes as well as compositions comprising indomethacin, medicaments produced using indomethacin in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of indomethacin administered by way of said medicaments.

Abstract: The present invention provides methods of reducing cutaneous scar formation by treating a cutaneous wound with a composition comprising a therapeutic agent that is a sodium channel blocker and/or an inhibitor of the Nax/SCN7A pathway. The present invention also provides wound cover components impregnated with such compositions, kits composed of such compositions with a wound dressing or sterile wipe, and mixtures of such compositions with a topical component (e.g., cream, ointment, or gel) suitable for application to a cutaneous wound. The present invention also provides compositions, kits, devices, and methods for treating skin conditions (e.g., dermatitis, psoriasis, or other skin conditions) with such compositions and devices. Examples of such therapeutic agents include, but are not limited to, an inhibitor of a gene or protein selected from: ENac, COX-2, PGE2, PI3K, PKB, Nax Prss8, IL-1?, IL-8, SAPK, Erk gene, p38 gene, PAR2, S100A8, S100A9, S100A12.

Abstract: The present invention provides a prophylactic or therapeutic agent for giant cell tumors occurring in a bone and soft tissue or for chondrosarcoma, which comprises a non-steroidal anti-inflammatory agent or thiazolidine derivative as an active ingredient, and the like

Abstract: Topical compositions are disclosed that are useful for delivering a therapeutic level of an NSAID to a target within a subject having a local inflammatory disorder. A composition of the present invention comprises a Drug and a solvent system, wherein the solvent system comprises at least two solvent alcohols and wherein the solvent system is present in an amount sufficient to solubilize the Drug, the solvent system is a low alkanol system, and the composition is a single phase composition. Exemplary solvent systems are those for which one of the at least two solvent alcohols is polyethylene glycol, glycerin, butylene glycol, dipropylene glycol, propylene glycol, ethanol, isopropanol, or a derivative thereof. Optionally the local inflammatory disorder is pseudofolliculitis barbae, dermatitis, psoriasis, wounds, or sunburn.

Abstract: Methods and compositions for reducing bladder spasms are disclosed. The methods comprise administering to a subject in need thereof a pharmaceutical composition comprising an effective amount of acetaminophen and an effective amount of at least one non-steroidal anti-inflammatory agent (NSAID). In another embodiment, a method for reducing bladder spasms comprising administering to a subject in need thereof a pharmaceutical composition comprising an effective amount of at least one prostaglandin (PG) pathway inhibitor, wherein the at least one PG pathway inhibitor is not acetaminophen or an NSAID.

Abstract: A medicant composition is provided. The composition includes a film layer and a powder matrix layer. The powder matrix layer includes a medicant. The powder matrix layer is applied to the film layer by admixing particulate to form a powder matrix and by then applying the powder matrix to the film layer by any desired method. The composition of the powder matrix is varied to alter the dissolution rate of the medicant, the adhesion of the medicant composition, and other physical properties of the powder matrix. The powder matrix layer can be cured.

Abstract: This disclosure is directed to the methods of enhancing hematopoietic stem cells (HSPC) and progenitor cell (HSPC) engraftment procedure. Treatment in vivo of a HSPC donor with compounds that reduce PGE2 biosynthesis or PGE2 receptor antagonists alone, or in combination with other hematopoietic mobilization agents such as AMD3100 and G-CSF, increases the circulation of available HSPCs. Compounds that reduce the cellular synthesis of PGE2 include non-steroidal anti-infiammatory compounds such as indomethacin. Treatment ex vivo of HSPC with an effective amount of PGE2 or at least one of its derivatives such as 16,16-dimethyl prostaglandin E2 (dmPGE2), promotes HSPC engraftment. Similar methods may also be used to increase viral-mediated gene transduction efficacy into HSPC.

Abstract: Provided are compositions for inhibiting a biological activity of an aldoketo reductase family 1, member C3 (AKR1 C3) polypeptide. In some embodiments, the compositions are indomethacin derivatives that are AKR1 C3-specific inhibitors. Also provided are methods for producing disclosed indomethacin derivatives that substantially lack cyclooxygenase inhibitory activity but that have AKR1C3 inhibitory activity, methods for inhibiting AKR1C3 polypeptide biological activities, and methods for treating prostate tumors in subjects.

Abstract: Some aspects of this disclosure relate to a method of treating an ophthalmic disease affecting an eye of a patient comprising forming a covalently-crosslinked hydrogel in situ at a peri-ocular, intra-ocular, or intra-vitreal site for controlled release of a therapeutic agent.

Abstract: An organic compound nano-powder comprising a granular organic compound with an average particle diameter of 500 nm or less and a 90%-diameter of less than 1500 nm and a carbohydrate compound comprising at least any one of a sugar and a sugar alcohol and with amount of 0.3 times or more by mass relative to amount of the organic compound, a method for producing the same, and a suspension having the organic compound dispersed in a liquid dispersion medium in which the organic compound is insoluble or poorly soluble.

Abstract: A drug delivery system for sustained delivery of bioactive agents, the system includes a matrix including nanofibrillated cellulose derived from plant based material and at least one bioactive agent, and at least one support selected from synthetic polymers, bio compounds and natural polymers. Also, methods for the manufacture of the system and methods of using it.

Abstract: The present invention relates to methods for producing particles of indomethacin using dry milling processes as well as compositions comprising indomethacin, medicaments produced using indomethacin in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of indomethacin administered by way of said medicaments.

Abstract: The present invention relates to methods for producing particles of indomethacin using dry milling processes as well as compositions comprising indomethacin, medicaments produced using indomethacin in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of indomethacin administered by way of said medicaments.

Abstract: The present invention relates to a composition for enhancing transdermal absorption of a drug, containing a polyvalent alcohol having 3 to 8 carbon atoms, an organic acid having 2 to 20 carbon atoms, and a higher alcohol having 12 to 20 carbon atoms, and a patch preparation containing a support and a drug-containing adhesive layer containing the composition on one surface of the support.

Abstract: A method for producing a composition comprising nanoparticles of a biologically active compound, comprising the step of: dry milling a solid biologically active compound and a millable grinding compound in a mill comprising a plurality of milling bodies, for a time period sufficient to produce a solid dispersion comprising nanoparticles of the biologically active compound dispersed in an at least partially milled grinding compound is described as are various compositions produced using such methods.

Abstract: The present invention relates to methods for processing pharmaceutically active substances having poor water solubility in the presence of an inorganic matrix, e.g., magnesium aluminometasilicate, and a secondary polymer as a means of converting the crystalline API to substantially amorphous and stable form, i.e., the crystallinity is less than 5%. The methods of the invention result in more complete amorphization, increased solubility, drug loading and stability as compared to typical amorphization or literature methods.

Abstract: Disclosure of methods and compositions related to chemical conjugations to nanoparticles of polysaccharides cross-linked to poloxamers as well as nano-sized colloids comprised of polysaccharides and poloxamers. The nanoparticles may be produced by various methods including inverse miniemulsion polymerization processes which create nanogels of desired size, shape, and stability for controlled therapeutic drug delivery, imaging, and theragnostic applications.

Abstract: A formulation for the delivery of an anti-inflammatory agent to a subject is described. In one particular application of the invention, the formulation comprises oil-based or aqueous droplets comprising indomethacin (1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1-H-indole-3-acetic acid) or celecoxib (4-[5-(4-methylphenyl)-3-(trifluoromethyl) pyrazol-1-yl]benzenesulfonamide) stabilized by nanoparticles, particularly silica nanoparticles.

Abstract: The present invention relates to methods for producing particles of indomethacin using dry milling processes as well as compositions comprising indomethacin, medicaments produced using indomethacin in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of indomethacin administered by way of said medicaments.

Abstract: A pharmaceutically delivery system is described comprising a pharmaceutically active agent and acidified nitrite as an agent to produce local production of nitric oxide at the skin surface. The dosage form may be in any pharmaceutically acceptable carrier means and comprises an acidifying agent adapted to reduce the pH at the environment. In one embodiment, a barrier consisting of a membrane allows diffusions of the anaesthetic and nitrite ions while preventing direct contact of the skin and acidifying agent.

Abstract: In alternative embodiments the invention provides compositions, e.g., pharmaceutical compositions and preparations, formulations, kits and other products of manufacture, e.g., exemplary drug combinations packaged together or separately in blister packs, lidded blisters or blister cards, or wrapped in paper, plastic or cellophane wrappers (e.g., a shrink wrap), comprising a combination regimen of at least two active ingredients designed to diminish systemic inflammation by targeting (inhibiting) two different, but convergent, signaling pathways, i.e., the sympathetic nervous system and the lipid-derived autacoid system; and methods for making and using these compositions. In alternative embodiments, the compositions of the invention (e.g., the combination of drugs) are used to ameliorate, diminish, treat, block or prevent an inflammatory response secondary to an infection, e.g., a viral infection and/or a reactivation.

Abstract: Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in an extended-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients formulated for extended-release. Yet another method comprises administering to a subject in need thereof an effective amount of a diuretic followed with another administration of a pharmaceutical composition comprising an analgesic agent formulated for extended-release.

Abstract: There is provided compositions and methods for the treatment of respiratory conditions such as pulmonary hypertension and sickle-cell disease in a patient in need thereof. The composition and method are for treating a patient in need thereof by inhalation of a composition containing amino acid ester compounds comprising at least one nitric oxide releasing group and pharmaceutical salts thereof.

Abstract: The present invention relates to methods for producing particles of indomethacin using dry milling processes as well as compositions comprising indomethacin, medicaments produced using indomethacin in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of indomethacin administered by way of said medicaments.

Abstract: The invention includes compositions comprising selective AKR1C3 inhibitors. The invention also includes compositions comprising bifunctional AKR1C3 inhibitors and selective androgen receptor modulators. The invention further includes methods of treatment using the compositions of the invention.

Abstract: Novel drug carriers capable of targeted and/or pH dependent release of biologically active agents into selected pH environments including the gastrointestinal (GI), ophthalmic, urinary, or reproductive tracts. Unexpectedly, carriers including free fatty acids (FFA) are able to deliver biologically active agents to various pH environments. Such targeted delivery is tailorable and useful for active agents that are: (a) injurious to the upper GI tract (esophagus, stomach, and duodenum), (b) acid labile, (c) impermeable/insoluble compounds in GI fluids, (d) susceptible to first pass metabolism, and/or (e) cause stomach irritation, upset, or dyspepsia.

Abstract: Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in an extended-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients formulated for extended-release. Yet another method comprises administering to a subject in need thereof an effective amount of a diuretic followed with another administration of a pharmaceutical composition comprising an analgesic agent formulated for extended-release.

Abstract: The present invention provides an indomethacin-containing external liquid preparation which provides good feeling of use, which exhibits high percutaneous absorption of indomethacin, and which, particularly in a low-temperature environment, does not cause precipitation of crystals with time. The present invention is drawn to an external liquid preparation containing indomethacin, a lower alcohol, water, a sulfite, and polyethylene glycol having an average molecular weight of 3,000 to 15,000.

Abstract: The present disclosure relates generally to binder powders for use in powder material processing and processes for their preparation. The disclosure further relates to binder powders for use in making solid powder compact forms, solid powder compact forms containing said binder powders and methods for making solid powder compact forms.