Abstract: There is disclosed an oral pharmaceutical formulation of bitter compounds that are agonists of TAS2R receptors for the treatment of pulmonary hypertension (PAH). More specifically, there is disclosed a PAH oral formulation comprising a bitter agent selected from the group consisting of 3-caffeoylquinic-1,5-lactone (3-CQL), chlorogenic acid (CGA), denatonium benzoate (DB), denatonium chloride (DC), denatonium saccharide (DS), denatonium acetate (DA), and combinations thereof and a PDE-5 inhibitor.

Abstract: There is disclosed an improved abuse-deterrent pharmaceutical composition comprising a controlled pharmaceutical substance in a formulation comprising at least two gel-forming excipients selected from the group consisting of PEG ester, poloxamer, water-soluble anionic polysaccharide, and carboxymethylcellulose, and a bitter-agonist compound selected from the group consisting of denatonium salts (including denatonium acetate (DA), denatonium benzoate (DB), denatonium chloride, denatonium citrate, denatonium maleate, denatonium saccharide, and denatonium tartrate) chlorpheniramine, diphenidol, famotidine, haloperidol, quinine, parthenolide, and aristolochic acid. Preferably, the controlled pharmaceutical substance is an amphetamine or a pharmaceutically acceptable salt thereof. Preferably, the bitter receptor agonist is a denatonium salt selected from DA, DB, denatonium chloride, denatonium citrate, denatonium maleate, denatonium saccharide, and denatonium tartrate provided at from about 0.

Abstract: There is disclosed an oral pharmaceutical formulation of bitter compounds that are agonists of TAS2R receptors for the treatment of asthma. More specifically, the present disclosure provides an asthma oral formulation comprising a bitter agent selected from the group consisting of denatonium benzoate (DB), denatonium chloride (DC), denatonium saccharide (DS), denatonium acetate (DA), and combinations thereof and formoterol.

Abstract: There is disclosed a novel monohydrate salt form of denatonium acetate. More particularly, the novel salt form and crystalline hydrate form is useful for the treatment and prevention of diseases and conditions, such as metabolic syndrome, obesity, NASH, glycemic control/diabetes, and IBD (intestinal bowel disease).

Abstract: There is disclosed a liquid resin extended-release oral naltrexone formulation suspension comprising from about 1.0 mg/ml to about 10.0 mg/ml naltrexone in a resin, wherein no more than 30% of the total naltrexone dose administered is released within one hour and wherein no more than 60% of the total naltrexone dose administered is released within two hours. Specifically, there is disclosed a method for treating a child with an autism-type disorder with approximately a teaspoon (about 5 ml) of a liquid resin extended-release oral naltrexone formulation suspension comprising from about 1.0 mg/ml to about 10.0 mg/ml naltrexone in a resin, wherein no more than 30% of the total naltrexone dose administered is released within one hour and wherein no more than 60% of the total naltrexone dose administered is released within two hours.

Abstract: There is disclosed a combination oral dosage form pharmaceutical composition comprising a bitter receptor agonist and a gut-signaling compound. i.e., a gut-signaling peptide analog and/or gut-signaling hormone enhancer. And there is disclosed a method for treating obesity, diabetes, metabolic syndrome, glycemic control hyperlipidemia, and effecting weight loss comprising administering an effective amount of a pharmaceutical composition comprising a bitter receptor agonist and a gut-signaling compound, i.e., a gut-signaling peptide analog and/or gut-signaling hormone enhancer, as described above and herein.

Abstract: There is disclosed a pharmaceutical composition comprising a bitter receptor agonist comprising a denatonium salt, wherein the denatonium salt is selected from the group consisting of denatonium acetate (DA), denatonium citrate, denatonium maleate, denatonium saccharide, and denatonium tartrate, for use in a method for preventing, preventing progression and/or treating a fatty liver disease. In some embodiments, the daily dose of the denatonium salt for preventing or preventing progression of a fatty liver disease is from 25 mg/kg to 45 mg/kg QD and the daily dose of the denatonium salt for treating an existing fatty liver disease is from 70 mg/kg to 200 mg/kg per day administered QD or BID.

Abstract: There is disclosed compositions and methods for treating and preventing Acute Respiratory Distress Syndrome (ARDS) including ARDS caused by viral respiratory disease of zoonotic origin such as coronaviruses. The present disclosure is based on a surprising discovery of significant efficacy in an acute lung injury model using intrapulmonary lipopolysaccharide (LPS) challenge in female CD-I mice. Based on these data, the test compound, denatonium acetate monohydrate (DA) (1) treats or prevents ARDS and, (2) treats severe acute respiratory syndrome (SARS) caused by a coronavirus. Therefore, the data achieved in these studies does have a story to tell and the story is that a DA pharmaceutical composition, administered orally, provided a method to treat or prevent ARDS and treat SARS. Preferably, the pharmaceutical composition for daily administration comprises DA delivering a daily total dose of from about 20 mg to about 2000 mg to a human adult.

Abstract: There is disclosed a novel monohydrate salt form of denatonium acetate. More particularly, the novel salt form and crystalline hydrate form is useful for the treatment and prevention of diseases and conditions, such as metabolic syndrome, obesity, NASH, glycemic control/diabetes, and IBD (intestinal bowel disease).

Abstract: There is disclosed a method for treatment, prevention, and/or slowing of progression for various chronic inflammatory disorder groups including (1) type 2 diabetes group (metabolic syndrome (MET), obesity, hyperglycemia); (2) ARDS (acute respiratory distress syndrome); (3) chronic autoimmune inflammatory disorders (rheumatoid arthritis (RA), lupus, and psoriasis); (4) inflammatory bowel diseases (IBD), such as Crohn's disease and ulcerative colitis; (5) metabolome-mediated diseases (atherosclerosis, hypertension, and congestive heart failure); and (6) hyperphagia disorders such as Prader-Willi Syndrome and other monogenic and syndromic obesity disorders including leptin pathway deficiencies, each comprising administering orally a pharmaceutical composition comprising a denatonium salt.

Abstract: There is disclosed an oral pharmaceutical composition for the treatment of multiple diseases comprising a denatonium cation salt and a sour anion selected from the group consisting of acetate (DA), citrate (DC) tartrate (CT), maleate (DM) and combinations thereof (collectively “denatonium salt”) and pharmaceutical excipients for gastric release of the denatonium salt. There is further disclosed an oral immediate release pharmaceutical composition to substantially release an API (active pharmaceutical ingredient) in the gastric area of the GI tract formulation, wherein the API comprises an effective amount of the denatonium salt. Preferably, the oral immediate release pharmaceutical formulation comprises from about 0.5 g to about 5 g of the denatonium salt delivering a daily dose of the denatonium salt from about 20 mg to about 150 mg to a human adult.

Abstract: There is disclosed an oral pharmaceutical composition for the treatment of multiple diseases comprising a denatonium cation salt and a sour anion selected from the group consisting of acetate (DA), citrate (DC) tartrate (CT), maleate (DM) and combinations thereof (collectively “denatonium salt”) and pharmaceutical excipients for gastric release of the denatonium salt. There is further disclosed an oral immediate release pharmaceutical composition to substantially release an API (active pharmaceutical ingredient) in the gastric area of the GI tract formulation, wherein the API comprises an effective amount of the denatonium salt. Preferably, the oral immediate release pharmaceutical formulation comprises from about 0.5 g to about 5 g of the denatonium salt delivering a daily dose of the denatonium salt from about 20 mg to about 150 mg to a human adult.

Abstract: There is disclosed an oral pharmaceutical formulation of bitter compounds that are agonists of taste receptor type 2 (TAS2R) receptors for the function of appetite suppression for the treatment of obesity. More specifically, the present disclosure provides an anti-obesity oral formulation comprising a bitter agent selected from the group consisting of denatonium salts including benzoate (DB), chloride (DC), acetate (DA), citrate (DCl), saccharide (DS), tartarate (DT), maleate (DM), 3-caffeoylquinic-1,5-lactone (3-CQL), chlorogenic acids (CGA), combinations thereof, and pharmaceutical excipients to facilitate a sustained release during transit through the gastrointestinal (GI) tract. Preferably, the oral pharmaceutical formulation further comprises either or both a sweet antagonist selected from the group consisting of lactisole, gymnemic acid, ziziphin, hodulcine, and combinations thereof, and a sour organic acid.

Abstract: There is disclosed an oral pharmaceutical formulation of bitter compounds that are agonists of taste receptor type 2 (TAS2R) receptors for the function of appetite suppression for the treatment of obesity. More specifically, the present disclosure provides an anti-obesity oral formulation comprising a bitter agent selected from the group consisting of denatonium salts including benzoate (DB), chloride (DC), acetate (DA), citrate (DCl), saccharide (DS), tartarate (DT), maleate (DM), 3-caffeoylquinic-1,5-lactone (3-CQL), chlorogenic acids (CGA), combinations thereof, and pharmaceutical excipients to facilitate a sustained release during transit through the gastrointestinal (GI) tract. Preferably, the oral pharmaceutical formulation further comprises either or both a sweet antagonist selected from the group consisting of lactisole, gymnemic acid, ziziphin, hodulcine, and combinations thereof, and a sour organic acid.