Abstract

The present specification discloses a tegoprazan-zinc chloride cocrystal solid. In addition, the present specification also discloses polymorphs of various tegoprazan-zinc chloride cocrystal solids discovered through research and characteristics thereof, as well as a therapeutic use thereof.

IPC Classes  ?

• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
• A61K 9/14 - Particulate form, e.g. powders
• A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• A61P 31/04 - Antibacterial agents

Abstract

The present specification provides a co-amorphous solid comprising tegoprazan and a co-former. Specifically, the co-former is selected from inorganic salts such as zinc chloride, zinc sulfate, magnesium chloride, and calcium chloride. The co-amorphous form comprising tegoprazan and a co-former has higher water solubility than a crystalline form of tegoprazan and has the characteristic of stably maintaining a solid phase thereof even under harsh conditions of high temperature and high humidity. Furthermore, the co-former is an inorganic salt that does not show toxicity in the human body, and thus does not cause problems such as toxicity when the co-amorphous solid comprising the co-former is used as a therapeutic agent. Accordingly, the co-amorphous solid comprising tegoprazan and a co-former can be used as a suitable dosage form when using the tegoprazan for therapeutic purposes.

IPC Classes  ?

• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• A61K 9/14 - Particulate form, e.g. powders
• A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles

Abstract

The present invention relates to a bee venom injection composition comprising 50-99% of bee venom phospholipase A2 (bvPLA2) from a bee venom extract, and a preparation method therefor. The bee venom injection composition is prepared by combining: 75-90 wt% of a bvPLA2 bee venom extract comprising 50-99% of bvPLA2; 2-8 wt% of mannitol; 0.01-0.1 wt% of polysorbate; and a balance of purified water. The bee venom injection composition has been confirmed to maintain homogeneous form and properties after being freeze-dried and thus may be usefully employed as a bee venom injection composition which comprises high content of bee venom extract-derived bvPLA2 and has various pharmacological mechanisms of action.

IPC Classes  ?

• A61K 35/644 - BeeswaxPropolisRoyal jellyHoney
• A61K 38/46 - Hydrolases (3)
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharidesDerivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• A61K 9/19 - Particulate form, e.g. powders lyophilised

Abstract

The present invention relates to a method for preparing, from a bee venom extract, a bee venom composition containing bee venom phospholipase A2 (bvPLA2) as an active ingredient in an amount of 50-99%. A method, in which dilution is performed at an optimum condition by using sterile water tertiary-distilled 400-600 times on the basis of 1 g of a bee venom extract, and ultrafiltration is performed 11 to 15 times by using an ultrafiltration system, having a 10-20 kDa membrane filter mounted therein, at a condition of room temperature and nitrogen pressure so that a 20-30 mL concentration is achieved, has been identified, and thus can be effectively used as a method for preparing, from a bee venom extract, a bee venom composition containing bee venom phospholipase A2 (bvPLA2) as an active ingredient in an amount of 50-99%.

IPC Classes  ?

• C12N 9/18 - Carboxylic ester hydrolases

Abstract

The present invention relates to a composition for preventing or treating neuroinflammatory disorders, comprising a bee venom extract as an active ingredient. More specifically, the present invention provides a pharmaceutical composition or a health functional food composition for preventing or treating neuroinflammatory disorders, both of which comprise, as an active ingredient, a bee venom extract in which the amount of phospholipase A2 (PLA2) is 50 to 85%. The bee venom extract alleviates decreased motor functions caused by neurotoxicity and has neuroprotective and neuroinflammation-relieving effects, thereby enabling the prevention or treatment of neuroinflammatory disorders. Particularly, a pharmaceutical composition according to the present invention can further improve an effect of preventing or treating neuroinflammatory disorders by being subcutaneously administered or by being co-administered with a STAT3 inhibitor or an NF-κB inhibitor, thereby enabling more effective prevention or treatment of neuroinflammatory disorders.

IPC Classes  ?

• A61K 35/64 - Insects, e.g. bees, wasps or fleas
• A61K 38/46 - Hydrolases (3)
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

Abstract

The present invention relates to a composition for preventing or treating neuroinflammatory disorders, comprising a bee venom extract as an active ingredient. More specifically, the present invention provides a pharmaceutical composition or a health functional food composition for preventing or treating neuroinflammatory disorders, both of which comprise, as an active ingredient, a bee venom extract in which the amount of phospholipase A2 (PLA2) is 50 to 85%. The bee venom extract alleviates decreased motor functions caused by neurotoxicity and has neuroprotective and neuroinflammation-relieving effects, thereby enabling the prevention or treatment of neuroinflammatory disorders. Particularly, a pharmaceutical composition according to the present invention can further improve an effect of preventing or treating neuroinflammatory disorders by being subcutaneously administered or by being co-administered with a STAT3 inhibitor or an NF-κB inhibitor, thereby enabling more effective prevention or treatment of neuroinflammatory disorders.

IPC Classes  ?

• A61K 35/64 - Insects, e.g. bees, wasps or fleas
• A61K 38/46 - Hydrolases (3)
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A23L 33/10 - Modifying nutritive qualities of foodsDietetic productsPreparation or treatment thereof using additives

Abstract

The present invention relates to a pharmaceutical composition for treating or preventing a disease related to abnormal suppression of regulatory T cell activity comprising a polypeptide comprising a bee venom-PLA2 amino acid sequence exclusive of a leader sequence as an active ingredient. The secretory bee venom-phospholipase A2 of the present invention activates a regulatory T cell and suppress a differentiation of Th1/Th7. Therefore, the present polypeptide can be used as a pharmaceutical composition for treating or preventing a disease related to abnormal suppression of regulatory T cell activity, i.e. autoimmune diseases, allergic diseases, or neurodegenerative diseases.

IPC Classes  ?

• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A61K 38/46 - Hydrolases (3)
• C12N 9/20 - Triglyceride splitting, e.g. by means of lipase
• A61K 35/64 - Insects, e.g. bees, wasps or fleas
• A61K 9/00 - Medicinal preparations characterised by special physical form

Abstract

The present invention relates to a pharmaceutical composition for treating or preventing a disease related to abnormal suppression of regulatory T cell activity comprising a polypeptide comprising a bee venom-PLA2 amino acid sequence exclusive of a leader sequence as an active ingredient. The secretory bee venom-phospholipase A2 of the present invention activates a regulatory T cell and suppress a differentiation of Th1/Th7. Therefore, the present polypeptide can be used as a pharmaceutical composition for treating or preventing a disease related to abnormal suppression of regulatory T cell activity, i.e. autoimmune diseases, allergic diseases, or neurodegenerative diseases.

IPC Classes  ?

• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A61K 38/46 - Hydrolases (3)
• C12N 9/20 - Triglyceride splitting, e.g. by means of lipase
• A61K 35/64 - Insects, e.g. bees, wasps or fleas
• A61K 9/00 - Medicinal preparations characterised by special physical form

Abstract

The present invention relates to a pharmaceutical composition for treating or preventing a disease related to abnormal suppression of regulatory T cell activity comprising a polypeptide comprising a bee venom-PLA2 amino acid sequence exclusive of a leader sequence as an active ingredient. The secretory bee venom-phospholipase A2 of the present invention activates a regulatory T cell and suppress a differentiation of Th1/Th7. Therefore, the present polypeptide can be used as a pharmaceutical composition for treating or preventing a disease related to abnormal suppression of regulatory T cell activity, i.e. autoimmune diseases, allergic diseases, or neurodegenerative diseases.

IPC Classes  ?

• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A61K 38/46 - Hydrolases (3)
• C12N 9/20 - Triglyceride splitting, e.g. by means of lipase