Abstract: The invention relates to the field of medicine and pharmaceuticals and particularly to a novel dosage form of an antitumor preparation, which ensures the hydrolytic and physical stability of said preparation, as well as to a method for producing a dosage form of this type. The stable dosage form is a lyophilizate comprising an etidronate-cytarabine conjugate or a pharmaceutically acceptable salt thereof, and a stabilizer, which is a divalent metal salt, in a molar ratio of stabilizer to conjugate of 1:1 to 20:1. A dosage form of this type ensures the hydrolytic and physical stability of the conjugate during long-term storage, and the stability of solutions of the conjugate for parenteral administration during clinical use.

Abstract: The present invention relates to means for protecting bioactive materials in mammalian food or feed formulations used to enhance the health status of mammals.

Abstract: This disclosure relates to gastro-resistant, controlled release dosage forms comprising Compound (I): or a pharmaceutically acceptable salt and/or solvate thereof, the pharmacokinetic properties of these dosage forms, and the preparation of the same. The novel dosage forms disclosed herein are useful in reducing the risk of QT prolongation in a subject and in treating a disorder in a subject in need thereof, e.g., a subject diagnosed with schizophrenia, for example, in treating the negative symptoms in a subject diagnosed with schizophrenia having the CYP2D6 EM genotype.

Abstract: The present invention relates to novel pharmaceutical formulations which have controlled, delayed release of active ingredient, and to a process for the preparation of such formulations. The invention additionally relates to the use of these novel pharmaceutical administration forms as medicaments for the treatment of diseases which require delayed release of the active ingredient, such as hypertension, or asthmatic diseases.

Abstract: The invention relates to a film-forming composition comprising a fluidised hydroxypropyl starch and sorbitol, and to a film-coating method using said composition. The invention further relates to film-coated solid forms comprising a fluidised hydroxypropyl starch and sorbitol in the coating.

Abstract: Disclosed is an immediate-release carvedilol formulation, which is configured such that a coating layer including a polymer, wax, fatty acid and/or fatty acid ester is formed on the surface thereof. This formulation has improved madescent, and thus can exhibit high stability, in which the initial appearance of the formulation can be maintained without cracking or breaking even under storage conditions at high relative humidity.

Abstract: Embodiments of the present disclosure include devices, and methods of making such devices, for delivery of one or more active agents with short or long zero-order release kinetics. Embodiments also include implantable or injectable drug delivery systems capable of controlled release over long periods of time for therapeutic agents.

Abstract: The present invention discloses a bexarotene softgel capsule and a preparation method thereof. The bexarotene softgel capsule including: a softgel capsule shell and contents, in which the contents include bexarotene, low molecular weight polyethylene glycol, high molecular weight polyethylene glycol, and polysorbate. The bexarotene softgel capsule of the formula can avoid a problem of drug degradation caused by high temperature heat release and degassing difficulty in a process of preparing the bexarotene softgel capsule in the prior art while maintaining the drug release characteristics, and the preparation method has a simple production process and can significantly improve a problem of poor dosage uniformity while filling a capsule in the prior art.

Abstract: The invention is directed to a three-dimensional polymer network for encapsulating a pharmaceutical ingredient, the polymer network comprising (a) at least one first polymer; and (b) at least one cross-linking agent. The three-dimensional polymer network is remarkable in that the at least one first polymer comprises a first polyuronate derivative, the first polyuronate derivative being modified with a hydrophobic moiety; and in that the at least one cross-linking agent is calcium chloride and/or a cyclodextrin derivative.

Abstract: Disclosed herein are delivery systems including coated and uncoated yarns, yarn precursors, threads, fibers, and other substrates for the constant or near-constant release of active compounds, as well as methods for manufacturing such delivery systems. The yarns, yarn precursors, threads, fibers, and other substrates can include a cross-linked hydrophobic elastomer and an active compound. One or more coatings that are impermeable or substantially impermeable to the active compound may partially or fully occlude the yarn or substrate to control release rates of the active compound. The delivery systems may be used in a variety of applications, including the making of articles of clothing, textiles, and fabrics, and may be used in methods of treating various conditions and diseases.

Abstract: This invention relates to a surgical or medical dressing which comprises a supporting and reinforcing layer of elastomeric material (as polyethylene homopolymer) embedded in the composition of honey/additives, to supplement the mechanical strength, which would be fabricated as a single integral piece, intended to provide multi-functional properties in the wound environment, particularly for promote or expedite the regeneration or repair deep tissue injuries or chronic wounds such as ulcers. Several additional characteristics of this new dressing provide an advantage to any wound care product developed from it. First, the biomaterial retains many biological properties of its major constituents (honey/additives). Second, the application of this safety dressing is greatly simplified particularly for pediatric burn Care.

Abstract: The present invention relates to products and methods for treatment of various symptoms in a patient, including treatment of pain suffered by a patient. The invention more particularly relates to self-supporting dosage forms which provide an active agent while providing sufficient buccal adhesion of the dosage form. Further, the present invention provides a dosage form which is useful in reducing the likelihood of diversion abuse of the active agent.

Abstract: The invention relates generally to pterostilbene and a related compound thereof active to inhibit complement at concentrations lower than 1 micromole per liter in human serum. The invention also relates to methods of using these orally active, well tolerated small molecules for the treatment of Alzheimer's disease and to prevent the development of schizophrenia by inhibiting the classical complement pathway. Methods for the treatment of complement-associated inflammatory and non-inflammatory diseases, including those of the skin, are also presented.

Abstract: There is provided a composition including a 3-bromo-4,5-dihydroxybenzaldehyde (BDB) for protecting human skin keratinocyte from ultraviolet, in which the BDB has a photo-protective effect against cell damage caused by ultraviolet in human HaCaT skin keratinocyte, activity of removing a free radical, and ultraviolet absorption activity, and inhibits formations of lipid peroxidation and protein carbonyl, inhibits DNA damage, protects a cell, and thereby exhibits cell protective activity. Thus, the BDB decreases apoptosis induced by ultraviolet, and then protect a cell to recover cell viability.

Abstract: The present invention relates to compositions of ion channel activators and methods of preparation, formulation, and the medical use of these compositions. In one aspect, the present invention features a composition formulated for oral administration, said composition comprising an effective amount of an ion channel activator (e.g., a TRPV1 channel activator, a TRPA1 channel activator, an ASIC channel activator, or combination thereof).

Abstract: A method of delivering a compound of interest to the lungs of a subject by the intravenous injection of Sertoli cells loaded with a plurality of chitosan nanoparticles coupled with the compound of interest is provided. Testis-derived rat Sertoli cells were pre-loaded with chitosan nanoparticles coupled with or without the drug curcumin, pre-labeled with a fluorescent cell marker and then injected intravenously into the control or asthmatic mouse model host. Intact pre-loaded, pre-labeled Sertoli cells were present in the lungs at 15 minutes post-injection, appeared entrapped in the pulmonary pre-capillary vascular bed around alveolar sacs but were not present one hour post-injection although Sertoli cell label and cellular debris was. Most of the injected nanoparticle load (70%) and curcumin load (80%) was present in the lungs 15 minutes post-injection, and remained at 70% and 80%, respectively, one hour post-injection.

Abstract: Disclosed herein are compositions including a topical agent that may be used to reduce and/or inhibit the effects of chemotherapy and/or radiotherapy, which can include reducing and/or inhibiting the effects of hair loss and/or hair shedding due to chemotherapy and/or radiotherapy. The topical agent can be a weak acting alpha-1 adrenergic receptor agonist such as synephrine. Some embodiments of the composition can include a weak acting alpha-1 adrenergic receptor agonist with a modulating agent to modulate deposition, mode of action, and/or metabolism of a chemotherapeutic agent and/or a reactive oxygen species agent.

Abstract: Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a chemosensory receptor ligand, such as a bitter receptor ligand. Also provided herein are chemosensory receptor ligand compositions, including bitter receptor ligand compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.

Abstract: A zero-calorie to near-zero-calorie snacking product that, when consumed, provides a feeling of fullness prior to absorption of energy-providing food, i.e., pre-absorptive satiation is disclosed. The snacking product is based on the stimulation of vagal nerve endings in the gastro-intestinal tract by encapsulated capsaicin. The encapsulation of capsaicin avoids the burning sensation in the mouth which may be objectionable to some consumers.

Abstract: The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.

Abstract: The present disclosure, in at least certain embodiments, is directed to shikimate (shikimic acid) analogues and compositions thereof, kits which contain the shikimate analogues or compositions thereof, and methods of use of the compounds and compositions for treating epithelial surfaces before or following exposure to irritants, allergens, and toxic agents (for example, urushiol).

Abstract: The present invention concerns the use of compounds for preventing and/or treating osteoporosis, for stimulating bone formation, for stimulating the differentiation and mineralization of osteoblasts, or for inhibiting bone resorption in a subject. These novel uses have been found for compounds represented by Formula I and pharmaceutically acceptable salts thereof. wherein: R1 and R2 are independently equal to H, F or OH; A is (CH2)mCOOH, W(CH2)mCOOH, or Y—CH(COOH)—(CH2)p-CH3 when B is H; or B is (CH2)mCOOH, W(CH2)mCOOH, or Y—CH(COOH)—(CH2)p—CH3 when A is H; or A and B are covalently bonded to form a five (5), six (6), or seven (7)-membered cycloalkyl substituted with COOH; where: Y is O, S, HN or CH2; W is 0, S or NH; m is 0-2; and p is 3-7; D is CO(CH2)nCH3 or CHOH(CH2)nCH3 or O(CH2)nCH3 where n is 2-6; and E is H or F.

Abstract: Treatment of intrahepatic cholestatic diseases by therapy with seladelpar or a salt thereof.

Abstract: The present invention features therapeutic compositions comprising an agent that specifically binds to a PIF pocket of Aurora A kinase and an agent that specifically binds to an ATP-binding site of Aurora A kinase, and the use of the therapeutic compositions to modulate Aurora A kinase for the treatment of cancer.

Abstract: Provided are compositions comprising beta-alanylhistidine peptides and/or beta-alanines, and methods for administering these peptides and amino acids. In one aspect, the compositions and methods cause an increase in the blood plasma concentrations of beta-alanine and/or creatine.

Abstract: The present invention provides methods and kits a) for predicting colorectal cancer patient survival, as well as the survival of patients harboring other invasive cancers where cellular proliferation and carcinogenesis is linked, in part, to high levels of ODC activity and increased cellular polyamine contents, and b) for selecting the corresponding treatment options for such patients based on the allelic nucleotide sequence or SNP at position +316 of the ODC1 promoter gene as well as cancer treatment methods, in each case, which include the determination of the ODC1 promoter +316 position genotype, as a means to guide treatment selection.

Abstract: A method of treating patients in need of treatment for a cardiac disorder has been found which comprises administering to the patient a seven carbon fatty acid compound or derivative thereof, wherein the compound or derivative thereof is able to readily enter the mitochondrion without special transport enzymes. A dietary formulation suitable for treatment of heart tissue in cardiac or surgical patients has been found which comprises a seven-carbon fatty acid chain, wherein the seven-carbon fatty acid chain is characterized by the ability to transverse the inner mitochondrial membrane by a transport mechanism which does not require carnitine palmitoyltransferase I, carnitine palmitoyltransferase II, or carnitine/acylcarnitine translocase and the ability to undergo mitochondrial ?-oxidation, and wherein the compound is selected from the group consisting of n-heptanoic acid or a derivative thereof, a triglyceride comprising n-heptanoic acid or a derivative thereof, and triheptanoin or a derivative thereof.

Abstract: The subject invention relates to a variety of formulations of bipolar trans carotenoids including pharmaceutical compositions for oral delivery of a bipolar trans carotenoid comprising i) a bipolar trans carotenoid, ii) a cyclodextrin, and iii) a coating. The invention also relates to preparation of such formulations and their uses.

Abstract: Methods regarding DNA methylation signature of post-traumatic stress disorder (PTSD) in brains of susceptible, resilient animals methylated in response to trauma, and S-adensoyl methionine (SAM) treated animals for deriving targets for PTSD therapeutics. Method regarding pathway analysis of the DNA methylation landscape to derive novel targets for therapeutic interventions such as retinoic acid pathway or estrogen receptor pathways. A method of treatment of PTSD comprised of Epigenetic modulators using general DNA methylation modulators such as SAM. A method of treatment of PTSD comprised of retinoic acid or vitamin A and its natural and synthetic analogs such as all-trans-retinoic acid (Tretinoin), 9-cis-retinoic acid (Alitretinoin), and 13-cis-retinoic acid (Isotretinoin) to treat PTSD. A method of treatment of PTSD comprised of a combination of Sadenosylmethionine and retinoic acid or vitamin A and its synthetic and natural analogs such as Tretinoin, Alitretinoin, and Isotretinoin.

Abstract: The present invention relates to the field of medicine, specifically the field of treatment and prevention of cardiovascular diseases.

Abstract: The present invention provides a method and composition for treating a neurodegenerative disease. In particular, the present invention provides a method and composition to increase DJ-1 gene expression or DJ-1 protein activity to treat a neurodegenerative disease.

Abstract: In various embodiments, the present invention provides methods of treating and/or preventing cardiovascular-related disease and, in particular, a method of blood lipid therapy comprising administering to a subject in need thereof a pharmaceutical composition comprising eicosapentaenoic acid or a derivative thereof.

Abstract: A compound having antiestrogenic activity is used in a method for the treatment of BC or other estrogen-responsive tumors in a human patient, wherein the method comprises subjecting the patient to a fasting mimicking diet for a period of 24-190 hours while the patient is being treated with the compound having antiestrogenic activity, which can be a selective estrogen receptor modulator (SERM), a selective estrogen receptor downregulator (SERD) or an aromatase inhibitor (AI).

Abstract: A paclitaxel pharmaceutic composition and a pharmaceutic preparation, a preparation process therefor and use thereof are provided. The paclitaxel composition contains paclitaxel as an active ingredient and hydroxypropyl methyl cellulose derivative as a carrier material. The paclitaxel preparation is in the form of an oral solid preparation. The paclitaxel composition and pharmaceutic preparation thereof can be used for the preparation of a drug for preventing and treating malignancies and relevant diseases in mammals.

Abstract: The present invention is directed to compositions comprising physiologically active phenolic compounds and methods for making and using the same. In particular embodiments, the compositions described herein include suspension formulations including a physiologically active phenolic compound provided as a nanoparticulate material and dispersed within an edible lipid.

Abstract: Compounds of Formula I are described as are pharmaceutical compositions containing such compounds. Methods of treating neurological or psychiatric diseases and disorders in a subject in need are also disclosed.

Abstract: The present invention relates to a concentrated extract of cranberry (Vaccinium macrocarpon), the complex composition of which makes it possible to increase the antibacterial effects thereof, which is of use for the prevention or treatment of urinary infections, and in particular for the preventive treatment of urinary infections or treatment against the recurrence thereof. The invention also relates to a process for preparing such an extract, to food, nutraceutical or pharmaceutical compositions comprising the extract and to the use thereof in the treatment or prevention of urinary infections.

Abstract: Provided are compounds generated by conjugation of triptolide with glucose to form glucose-triptolide conjugates, provides compounds with effective anti-proliferative activity and improved tolerability as compared to naturally occurring triptolide compounds.

Abstract: Provided herein are methods and compositions for treating and/or reducing the risk of developing a condition associated with fibrosis and/or collagen deposition in a subject. In one embodiment, the method comprises administering an effective amount of an IRE1? inhibitor to the subject; wherein the subject is identified as having a risk of developing and/or a need for treatment of the condition associated with fibrosis and/or collagen deposition.

Abstract: A pharmaceutical composition includes dorzolamide or a salt thereof and brimonidine or a salt thereof and has a pH of 6.0 or more. The pharmaceutical composition preferably does not include a preservative or includes a prescribed amount thereof, wherein said prescribed amount is preferably such that the common logarithmic value of the ratio (B/A) of the number (B) of bacteria at the time of inoculation to the number (A) of bacteria when the number of viable bacteria is measured after inoculating bacteria in a test sample that consists of the preservative and water and mixing homogeneously such that the concentration of Escherichia Coli ATCC 8739 in the bacterial suspension is within the range of 105-106 cfu/mL, and collecting 1 mL of the test sample using a micropipette after the test sample has been stored for seven days at 20-25° C. while shielded from light, is 2.0 or less.

Abstract: The present invention relates to methods of treating autoimmune diseases with siponimod in patients receiving additionally a beta-blocker.

Abstract: The present invention relates to the use of indolinones of general formula substituted in the 6 position, wherein R1 to R5 and X are defined as in claim 1, the isomers and the salts thereof, particularly the physiologically acceptable salts thereof, as a medicament for the prevention or treatment of specific fibrotic diseases.

Abstract: IT-139, sodium trans-[tetrachlorobis(1H-indazole)ruthenate(III)], is an intravenously administered small molecule compound. In preclinical anti-tumor and mechanism of action studies, IT-139 showed activity against a broad range of tumor types, including those which are resistant to standard anti-cancer agents (e.g., platinums, vinca alkaloids, taxanes, anthracyclines). This activity is believed to arise from IT-139's novel mechanism of action that targets the GRP78 pathway. It was found that up-regulation of GRP78 is a key cancer cell survival pathway. Downregulation of GRP78 using IT-139 removes this resistance pathway allowing for chemotherapy and immuno-oncology agents to be more effective in treating cancer.

Abstract: Formulations for treating burns and burn wound healing comprising a Granzyme B inhibitor and a pharmaceutically acceptable carrier, and methods for treating burns and for burn wound healing using the formulations.

Abstract: There is herein provided a compound that is an mPGES-1 inhibitor, or a prodrug thereof, for use in the treatment or prophylaxis of a disease or disorder characterised by vasoconstriction.

Abstract: The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: wherein, R1 is a 5- to 6-membered ring group which may be substituted; X1 is a bond or the like; ring A is a 5- to 6-membered ring group which may be substituted; ring B is a 8- to 10-membered ring group which may be substituted; X2 is a bivalent group of 1 to 4 atoms; Z1 is a bivalent cyclic ring group or the like; Z2 is a bond or the like; and R2 is an amino group, a nitrogen-containing heterocyclic group which may be substituted or the like, or a salt thereof.

Abstract: It is an object of the present invention to provide a pharmaceutical composition, which can suppress a reduction in the content of an active ingredient caused by oxidation or decomposition of rapamycin or a derivative thereof, can ensure long-term stability, and has high safety. In the present invention, the inventors have found that (B) a tocopherol derivative and (C) a phospholipid are used in a pharmaceutical formulation comprising rapamycin or a derivative thereof, so that oxidation or decomposition of the rapamycin or a derivative thereof can be suppressed, thereby completing the present invention. The rapamycin or a derivative thereof, and (B) the tocopherol derivative and (C) the phospholipid are preferably in the form of a solid mixture produced by preparing a solution containing these components and then removing the solvent from the solution.

Abstract: Methods and compositions for treating a metabolic disease include administering gaboxadol or a pharmaceutically acceptable salt thereof to a patient diagnosed with a metabolic disease. In embodiments, administering gaboxadol or a pharmaceutically acceptable salt thereof to a patient diagnosed with a metabolic disease is effective to lower one or more of HbA1c level, fasting plasma glucose level, 2-hour oral glucose tolerance test (OGTT) result level, and random plasma glucose level. Gaboxadol or a pharmaceutically acceptable salt thereof may optionally be administered in combination with a hypoglycemic agent.

Abstract: The invention concerns compounds of Formula (I) or pharmaceutically-acceptable salts thereof, wherein R1 to R5 have any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of cell proliferative disorders.

Abstract: The invention relates to a novel salt of cytisine and pharmaceutical compositions comprising that salt. In particular, the invention relates to a succinate salt of cytisine which displays improved excipient compatibility, permitting the preparation of stable pharmaceutical compositions.