(WO202089942) A liquid injectable composition 机翻标题: 暂无翻译,请尝试点击翻译按钮。

源语言标题
(WO202089942) A liquid injectable composition
公开号/公开日
WO2020/089942WO2020/089942 / 2020-07-232020-05-07
申请号/申请日
WOIN2019/050808 / 2019-11-01
发明人
VENKITACHALAM PADMADAWRE SHILPA;
申请人
AMATERASU LIFESCIENCES;
主分类号
IPC分类号
A61K-009/107 A61K-031/357 A61K-047/10 A61K-047/30 A61K-047/40 A61K-047/44 C07C-215/38
摘要
(WO2020/089942) A liquid injectable composition comprising (a) at least one surfactant; (b) at least one gel strength enhancer; (c) at least one solvent; (d) optionally release retarding agent(s); (e) optionally stabilizing agent(s); (f) optionally pharmaceutical excipient(s); and (g) active pharmaceutical ingredient(s) (API).& its use in treating a subject suffering from a disease or disorder.
机翻摘要
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地址
代理人
代理机构
;
优先权号
2018IN-21041493
主权利要求
(WO2020/089942) CLAIMS 1. A liquid injectable composition comprising:   (a) at least one surfactant;   (b) at least one gel strength enhancer;   (c) at least one solvent;   (d) optionally release retarding agent(s);   (e) optionally stabilizing agent(s);   (f) optionally pharmaceutical excipient(s); and   (g) active pharmaceutical ingredient(s) (API). 2. The composition of claim 1, wherein the surfactant is present in about 5-80 wt.% of the composition. 3. The composition of claim 1, wherein the surfactant is non-ionic. 4. The composition of claim 1, wherein the surfactant is selected from sorbitan esters, polyoxyethylene sorbitan ester, polyoxyethylated castor oil, hydrogenated polyoxyethylated castor oil, phospholipids, D-alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS 1000), polyoxyethylene stearates, hydrophilic block polymers, glycerides, polyethylene ether, dodecyl betaine, coco amphoglycinate, cocamidopropyl betaine, and ethoxylated linear alcohol. 5. The composition of claim 1, wherein the surfactant comprises at least one of polysorbate 80, -polyoxyl 35 castor oil, polyoxyl 40 hydrogenated castor oil, lecithin, D-alpha-tocopheryl polyethylene glycol succinate 1000, andpolyoxyethylated 12-hydroxy stearic acid. 6. The composition of claim 1 , wherein the surfactant forms a lyotropic liquid crystalline phase or a gel. 7. The composition of claim 1, wherein the gel strength enhancer is present in about 5- 80 wt.% of the composition. 8. The composition of claim 1, wherein the gel strength enhancer is a lipophilic liquid and comprises at least one of fatty acid, salt of fatty acid, fatty acid esters, medium chain triglycerides, glycerides, and propylene glycol derivative of medium chain triglcerides. 9. The composition of claim 1, wherein the gel strength enhancer comprises at least one of oleic acid/ ethyl oleate, sodium oleate, linoleic acid, linolenic aciddibutyl sebacate, benzyl benzoate, caprylic capric mono- & diglycerides, and glyceroltricaprylate/caprate. 10. The composition of claim 1, wherein the release retarding agent is present in about 0.01- 40 wt.% of the composition. 11. The composition of claim 1 , wherein the release retarding agent comprises at least one of a polymer and lipid. 12. The composition of claim 1, wherein the release retarding agent comprises at least one of poly lactide co glycolide, polylactide, polyglycolide, polyethylene glycol, polylactide co caprolactone, polycaprolactone, polyethylene glycol-PLGA, glyceryl monostearate,   polyglyceryl-distearate, glyceryl palmitostearate, palmitic, stearic, arachidic, behenic, and lignoceric acids and esters thereof. 13. The composition of claim 1, wherein the solvent is present in about 5-80 wt.% of the composition. 14. The composition of claim 1, wherein the solvent comprises at least one of N-methyl-2- pyrrolidone, 2-pyrrolidone, glycofurol, dimethylacetamide, propylene glycol and benzyl alcohol. 15. The composition of claim 1, containing less than about 1 wt% moisture. 16. The composition of claim 1, wherein the stabilizing agent is present in about 0.001-10 wt.% of the composition. 17. The composition of claim 1, wherein the stabilizing agent comprises at least one of tocopherol, ascorbyl palmitate, butylated hydroxy anisole, and butylated hydroxy toluene, propyl gallate, hydroxypropyl betacyclodextrin and derivatives thereof. 18. The composition of claim 1, where the active pharmaceutical ingredient is selected from analgesics, anti allergic drugs, anti dementia/ Alzheimer drugs, anti-epileptic drugs, anti- infective drugs, antibiotics, antifungal drugs, anti-inflammatory drugs, antimalarial drugs, antineoplastic drugs, anti Parkinson’s drug, anti -ulcerative drugs, cardiovascular drugs, dermatological drugs, endocrinology drugs, gastrointestinal drugs, hormones, muscle relaxants, neurologic drugs, ophthalmic drugs, psychiatric drugs, renal drugs, respiratory drugs, rheumatologic drugs, urologic drugs, and various mixtures, salts, prodrugs and co-drugs thereof. 19. The composition of claim 1, wherein the active pharmaceutical ingredient   comprises antimalarial agent(s). 20. The composition of claim 19, wherein the active pharmaceutical ingredient   comprises at least one artemisinin derivative selected from arteether, artemether, artesunate, dihydroartemisinin, and artemotil & lumefantrine. 21. The composition of claim 19, wherein the active pharmaceutical ingredient comprises lumefantrine and at least one artemisinin derivative selected from arteether, artemether,   artesunate, dihydroartemisinin, and artemotil; and wherein the weight ratio of   artemisinin derivative to lumefantrine is about 1:4 to about 1:8. 22. The composition of claim 19, wherein the active pharmaceutical ingredient comprises at least one artemisinin derivative selected from arteether, artemether, artesunate,   dihydroartemisinin, and artemotil & lumefantrine; and wherein the weight ratio of   artemisinin derivative to lumefantrine is about 1 :6. 23. The composition of claim 1, for treatment of malaria by administering a single or multiple dose of at least about 0.l25mg/Kg one artemisinin derivative selected from arteether, artemether, artesunate, dihydroartemisinin, and artemotil & at least about 0.75mg/Kg   lumefantrine. 24. The composition of claims 22 formulated as a unit dosage form which is administered as single or multiple dose therapy for prevention or treatment of malaria. 25. The composition of claims 1-24, which is at least one of (a)-(k):   (a) liquid injectable dosage form;   (b) water-free self microemulsifying drug delivery system (SMEDDS), which on contact with water forms a microemulsion;   (c) liquid injectable dosage form, capable of forming a depot in situ ;   (d) liquid injectable dosage form, capable of forming a depot in situ, which releases the one or more active pharmaceutical ingredients over a period of time;   (e) liquid injectable dosage form, capable of forming a gel in situ in contact with aqueous fluids;   (f) liquid injectable dosage form, capable of forming a gel in situ, in contact with aqueous fluid and releases the one or more active pharmaceutical ingredients over a period of time;   (g) controlled release liquid injectable dosage form;   (h) modified release liquid injectable dosage form;(i) sustained release liquid injectable dosage form;   (j) extended release liquid injectable dosage form; and   (k) liquid injectable dosage form, capable of forming a depot in situ with a reduced burst effect. 26. The composition of claim 25, wherein the liquid injectable dosage form is a ready to inject dosage form in vials or prefilled syringe. 27. The composition of claim 1, which is a unit dosage form of about 400-4, OOOmcL, the composition comprising arteether or artemeter and lumefantrine. the composition comprising   (i) about7.5-30mg arteether or artemeter;   (ii) about 45-180 mg lumefantrine, and one or more excipients selected from   aboutl00-800 mcL oleic acid or about 200-1200mcL polyoxyethylene sorbitan ester or about 100 - lOOOmcL benzyl benzoate or about 100-1200 mcL N-methyl pyrrolidone, and about 5-40 mg Poly lactide/glycolide; 50:50 (PLGA). 28. The composition of claims 1 to 27, which does not comprise dibutyl sebacate, 2- pyrrolidone polyglyceryldistearate (PGDS), or any combination thereof. 29. The composition of claims 1 to 28 wherein the gel strength of the composition is at least 0.07 mJ. 30. The composition of claim 27 or 28, wherein the active pharmaceutical ingredient comprises antimalarial agents and the composition is formulated as a single or multiple dose therapy unit dosage form for the treatment of malaria. 31. The composition of any one of the above claims, used to prepare a medicament. 32. A method of treating a subject suffering from a disease or disorder ameliorated by one or more active pharmaceutical ingredients, the method comprising administering the composition of any one of the claims 1 to 31, in an amount and for a period of time sufficient to treat the subject. 33. The method of claim 32, wherein the subject is a human. 34. The method of claim 33, wherein the disease or disorder is malaria. 35. The method of claim 34, wherein composition is administered in a single or multiple dose which effectively treats the disease or disorder. 36. The method of claim 31 to 35 wherein the administration is intramuscular or   subcutaneous. 37. The method of claim 31 to 36, wherein the active pharmaceutical ingredient comprises an antimalarial and the composition is formulated as a single or multi dose therapy unit dosage form, equal to or greater than 0.l25mg/Kg of artemisinin derivative and 0.75mg/Kg of lumefantrine, for the treatment of malaria. 38. The method of claim 31 to 36, wherein the active pharmaceutical ingredient comprises an antimalarial and the composition is formulated as a single or multiple dose therapy unit dosage form, equal to or greater than 0.l25mg/Kg of artemisinin derivative and 0.75mg/Kg of lumefantrine, for the treatment of malaria caused by P. falciparum.
法律状态
PENDING
专利类型码
A3A2
国别省市代码
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