18 results about "Orally active" patented technology

Pharmaceutical compositions comprising a therapeutically active agent and an absorption enhancer such as NAC, NAD, 5-CNAC, 4-MOAC, 4-CNAB or a salt thereof, for use in the treatment of a condition treatable by said therapeutically active agent, are provided. The compositions are for concomitant oral administration of two or more of the unit dosage form, which form together a therapeutically effective amount of the therapeutically active agent and an effective amount of the absorption enhancer. Multi-dose compositions comprising the two or more of the unit dosage form are also provided.

The present invention relates to the field of pharmaceutical compositions suitable for the oral administration of an active in animals. In particular, the present invention relates to a liquid drug-containing formulation and to the use thereof. The present invention further relates to the use of a liquid formulation aid composition comprising at least one natural oil of herbal origin in a liquid drug-containing formulation for improving the acceptance or voluntary acceptance of drug intake in animal.

The invention discloses an inhibitor acting on a TDP1 target spot and application of the inhibitor. The active ingredient of the inhibitor comprises Lawsone (2-hydroxy-1, 4-naphthoquinone) or SPI-112 (Sodium Sulfonate I-112). The Lawsone is a naphthoquinone compound with oral activity, has antibacterial, antitumor and antioxidant activity, has a molecular formula of C10H6O3, and has a molecular weight of 174.16. The SPI-112 is a protein tyrosine phosphatase inhibitor, the molecular formula of the SPI-112 is C22H17FN4O5S, and the molecular weight of the SPI-112 is 468.46. The inhibitor provided by the invention can be used for effectively reducing CTG trinucleotide repeated amplification in Mykylosing Dystrophy Type 1 (Mykylosing Dystrophy Type 1, DM1) by inhibiting the activity of TDP1 protein, and a new direction is provided for preparing a safe and effective medicine directly aiming at the CTG trinucleotide repeated amplification in DM1.

The invention provides an antibacterial peptide as well as application, a product and a preparation method thereof, and relates to the technical field of biology. The invention screens out a novel antibacterial peptide from kidney beans, which can specifically kill escherichia coli O157: H7 without damaging intestinal flora. By designing protective peptide chains at two ends of an effective sequence, an innovative strategy for keeping oral activity without embedding is established, and the stability and the utilization efficiency are remarkably improved. Meanwhile, a plant-based transgenic expression system is constructed, high-purity production of the antibacterial peptide is realized, and the antibacterial peptide can be directly applied to oral administration.

Disclosed are stable dosage forms for oral administration of active pharmaceutical ingredients in which any unpleasant taste sensation, caused by release of the active pharmaceutical ingredient and / or of the excipients in the oral and pharyngeal cavity of the patient, is masked by the use of theobromine-free cocoa.

The disclosure includes compounds in accordance with Formula (I) or Formula (II) wherein R1, R2, and R3 are defined herein and to methods of making those compounds. That disclosure extends 5 to those compounds for the treatment of neoplastic disease, or a method for treating neoplastic disease with these compounds.

A pharmaceutical composition is described herein, which comprises a therapeutically active agent, an absorption enhancer, a polymer comprising a plurality of alkaline groups, and a non-polymeric (small molecule) proton-accepting agent. The absorption enhancer is preferably a substituted fatty acid or a salt thereof. Further described herein are methods of treating a condition treatable by the therapeutically active agent, comprising orally administering the pharmaceutical composition.

The present invention pertains to the fields of biotechnology and neuroscience. More specifically, the invention discloses a novel use of the peptide SEQ ID NO:1 (Asp-Ile-Ile-Ala-Asp-Asp-Glu-Pro-Leu-Thr, or DIIADDEPLT, also known as Pep19) for the preparation of a supplement or drug for sleep modulation. Also disclosed is a method for modulating sleep preferably through oral administration of said peptide or a composition comprising same.

The application discloses an inhibitor acting on a TDP1 target point and application thereof. The active ingredient of the inhibitor comprises Lawsone (2-hydroxy-1, 4-naphthoquinone) or SPI-112. The Lawsone is an orally active naphthoquinone compound, has antibacterial, antitumor and antioxidant activity, and has a molecular formula of C 10 H6O3 and a molecular weight of 174.16. The SPI-112 is a protein tyrosine phosphatase inhibitor, has a molecular formula of C 22 H 17 FN4O5S and a molecular weight of 468.46. The inhibitor provided by the application can effectively reduce CTG trinucleotide repeat expansion in myotonic dystrophy type 1 (DM1) by inhibiting TDP1 protein activity, and provides a new direction for preparing a safe and effective drug directly aiming at the CTG trinucleotide repeat expansion in DM1.

A pharmaceutical composition is described herein, which comprises a therapeutically active agent, an absorption enhancer, and a polymer comprising a plurality of alkaline groups. A concentration of the polymer in the composition is at least 10 weight percent of the total weight of the composition. The absorption enhancer is preferably a substituted or non-substituted fatty acid or a salt thereof. Further described herein are methods of treating a condition treatable by the therapeutically active agent, comprising orally administering the pharmaceutical composition.

A compound of the formulawhere R1, R2, R3, R4, R5, R6a, and R6b are as defined in the specification and claims, or an enantiomer, stereoisomer or diastereoisomer thereof, or a pharmaceutically acceptable salt thereof, and the use thereof in the treatment of diseases, disorders, syndromes and conditions responsive to modulation of a melanocortin receptor.

Ectoparasite infestations in fish farming can pose significant challenges and issues for aquaculture operations. This disclosure generally relates to treatment or control of ectoparasite infestations (such as sea lice infestations) on fish (such as salmonids) using a particular dosing regimen of an isoxazoline. In particular, the dosing regimen includes oral administration of the active ingredient:(S)-3-methyl-N-(2-oxo-2-(prop-2-yn-1-ylamino) ethyl)-5-(5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl) thiophene-2-carboxamide, including salts, or N-oxide, or solvates thereof, of structural formulaThe active ingredient may be administered at a dosage (i.e., in a dose) of from about 0.025 mg / kg / d to about 0.250 mg / kg / d. The dosing regimen may include oral administration from about 3 to about 10 consecutive days.

An oral active agent delivery system for animals, including horses, that includes a flexible orally dissolving film (ODF) for delivery of an active agent (i.e., active ingredient) to the oral cavity. The ODF may be applied directly to an oral mucosal surface or be laminated onto a bit that, in turn, is placed in the oral cavity of, for example, a horse.

A pharmaceutical composition for oral administration is disclosed herein, comprising a therapeutically active agent, salt of NAC (8-N-(2-hydroxybenzoyl)aminocaprylate) and one or more small molecule proton accepting agent(s). Methods and uses utilizing the aforementioned pharmaceutical compositions, are also disclosed herein.

The invention discloses an application of bacteria in preparation of a synergist for an immune checkpoint inhibitor. The bacteria are active bacteria or inactive whole-cell gut microbiota. By using a monobacterial oral preparation of human endogenous gut microbiota Alistipes combined with an immune checkpoint inhibitor, an anti-tumor immune protective response and an effect of remodeling gut microbiota is generated by stimulation of oral administration of active human commensal gut microbiota or inactive whole-cell human commensal gut microbiota, which significantly enhances an efficacy of the immune checkpoint inhibitor on multiple tumor species, enhances anti-tumor immune function, is conducive to improving the response rate of cancer immunotherapy populations, and has better safety, prolongs overall survival time of cancer patients, expands cancer patient population benefited from cancer immunotherapy (immunotherapy checkpoint inhibitors), provides new combination therapy regimens and therapeutic drugs to treat immune checkpoint inhibitor-refractory tumor patients, and expands the patient benefited from cancer immunotherapy.

The application belongs to the technical field of medicine, and particularly relates to application of trifluperidol in treatment of cerebrovascular diseases. Trifluperidol is a D1 / D2 dopamine receptor antagonist with oral activity and a novel PI3K inhibitor, and trifluperidol has anti-proliferative activity on cancer cells and induces apoptosis. The application discloses trifluperidol for the first time, and no report is found on effective treatment of trifluperidol against ischemic stroke, especially the application creatively proposes that trifluperidol significantly reduces the volume of acute cerebral infarction of a mouse with focal cerebral ischemia, which indicates that trifluperidol can be used for treating ischemic stroke.

An orally active, brain penetrant first-in-class small molecule midkine inhibitor for use in the treatment of triple-negative breast cancer, brain tumors (including glioblastoma, medulloblastoma, and NF1-mutant optic pathway gliomas), ovarian and endometrial cancers, lung cancer, as well as gynecologic non-malignant conditions such as endometriosis, uterine fibroids, and preterm birth, in which tumor cells and / or pathological cells exhibit heightened midkine signaling and express multiple midkine receptors.

The invention relates to a hydrochloride of 4-[(5-chloropyridine-2-yl) methoxy]-1-[3-(propan-2-yl)-1H, 2H, 3H, 4H, 5H-[1, 4] diazacyclohepta [1, 7-a] indol-9-yl]-1, 2-dihydropyridine-2-one (compound 1), a preparation method of the hydrochloride, and a preparation method of the hydrochloride. The pharmaceutical composition can be used for treating and / or preventing obesity, co-diseases and complications related to obesity, diabetes, metabolic disorders, coronary artery diseases, cerebrovascular diseases, peripheral artery diseases, hypertension, endocrine dyscrasia, mental disorders, personality disorders, eating disorders, sleep-awakening cycle disorders, substance abuse and addiction disorders, chronic liver and kidney diseases, and the like. Potent oral active selective melanin aggregation hormone receptor 1 (MCHR1) antagonists for treating diseases of the gastrointestinal tract, chronic diseases of the musculoskeletal system, osteoporosis, cancer, and one or more symptoms of Prallard-Wili Syndrome (PWS) or PWS. The present invention also relates to crystalline forms of 4-[(5-chloropyridin-2-yl) methoxy]-1-[3-(propan-2-yl)-1H, 2H, 3H, 4H, 5H-[1, 4] diazepane [1, 7-a] indol-9-yl]-1, 2-dihydropyridin-2-one in the form of a free base, different crystalline forms of the hydrochloride thereof, processes for their preparation, pharmaceutical compositions thereof and therapeutic uses thereof.