RU2022103663A - Новые композиции и способы - Google Patents
Новые композиции и способы Download PDFInfo
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- RU2022103663A RU2022103663A RU2022103663A RU2022103663A RU2022103663A RU 2022103663 A RU2022103663 A RU 2022103663A RU 2022103663 A RU2022103663 A RU 2022103663A RU 2022103663 A RU2022103663 A RU 2022103663A RU 2022103663 A RU2022103663 A RU 2022103663A
- Authority
- RU
- Russia
- Prior art keywords
- acid
- composition
- composition according
- sorbitan
- sodium
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title claims 32
- 108010010803 Gelatin Proteins 0.000 claims 8
- 229920000159 gelatin Polymers 0.000 claims 8
- 235000019322 gelatine Nutrition 0.000 claims 8
- 235000011852 gelatine desserts Nutrition 0.000 claims 8
- 208000012902 Nervous system disease Diseases 0.000 claims 6
- 208000025966 Neurological disease Diseases 0.000 claims 6
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 claims 6
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims 6
- 208000020016 psychiatric disease Diseases 0.000 claims 6
- 239000000546 pharmaceutical excipient Substances 0.000 claims 5
- 229920000642 polymer Polymers 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims 4
- RGHNJXZEOKUKBD-SQOUGZDYSA-N D-gluconic acid Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O RGHNJXZEOKUKBD-SQOUGZDYSA-N 0.000 claims 4
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 4
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 4
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 4
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims 4
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 claims 4
- 229910052784 alkaline earth metal Inorganic materials 0.000 claims 4
- -1 benzalkonium halides Chemical class 0.000 claims 4
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims 4
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims 4
- 150000001875 compounds Chemical class 0.000 claims 4
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 claims 4
- BDAGIHXWWSANSR-UHFFFAOYSA-N methanoic acid Natural products OC=O BDAGIHXWWSANSR-UHFFFAOYSA-N 0.000 claims 4
- JNYAEWCLZODPBN-JGWLITMVSA-N (2r,3r,4s)-2-[(1r)-1,2-dihydroxyethyl]oxolane-3,4-diol Chemical class OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O JNYAEWCLZODPBN-JGWLITMVSA-N 0.000 claims 3
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims 3
- 239000012458 free base Substances 0.000 claims 3
- 239000000600 sorbitol Substances 0.000 claims 3
- 235000010356 sorbitol Nutrition 0.000 claims 3
- HDTRYLNUVZCQOY-UHFFFAOYSA-N α-D-glucopyranosyl-α-D-glucopyranoside Natural products OC1C(O)C(O)C(CO)OC1OC1C(O)C(O)C(O)C(CO)O1 HDTRYLNUVZCQOY-UHFFFAOYSA-N 0.000 claims 2
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 claims 2
- ZORQXIQZAOLNGE-UHFFFAOYSA-N 1,1-difluorocyclohexane Chemical compound FC1(F)CCCCC1 ZORQXIQZAOLNGE-UHFFFAOYSA-N 0.000 claims 2
- LBLYYCQCTBFVLH-UHFFFAOYSA-N 2-Methylbenzenesulfonic acid Chemical compound CC1=CC=CC=C1S(O)(=O)=O LBLYYCQCTBFVLH-UHFFFAOYSA-N 0.000 claims 2
- OSWFIVFLDKOXQC-UHFFFAOYSA-N 4-(3-methoxyphenyl)aniline Chemical compound COC1=CC=CC(C=2C=CC(N)=CC=2)=C1 OSWFIVFLDKOXQC-UHFFFAOYSA-N 0.000 claims 2
- XZIIFPSPUDAGJM-UHFFFAOYSA-N 6-chloro-2-n,2-n-diethylpyrimidine-2,4-diamine Chemical compound CCN(CC)C1=NC(N)=CC(Cl)=N1 XZIIFPSPUDAGJM-UHFFFAOYSA-N 0.000 claims 2
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims 2
- 239000005711 Benzoic acid Substances 0.000 claims 2
- BVKZGUZCCUSVTD-UHFFFAOYSA-M Bicarbonate Chemical class OC([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-M 0.000 claims 2
- 208000020925 Bipolar disease Diseases 0.000 claims 2
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims 2
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims 2
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims 2
- RGHNJXZEOKUKBD-UHFFFAOYSA-N D-gluconic acid Natural products OCC(O)C(O)C(O)C(O)C(O)=O RGHNJXZEOKUKBD-UHFFFAOYSA-N 0.000 claims 2
- HMFHBZSHGGEWLO-SOOFDHNKSA-N D-ribofuranose Chemical compound OC[C@H]1OC(O)[C@H](O)[C@@H]1O HMFHBZSHGGEWLO-SOOFDHNKSA-N 0.000 claims 2
- 206010012289 Dementia Diseases 0.000 claims 2
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims 2
- 239000004386 Erythritol Substances 0.000 claims 2
- UNXHWFMMPAWVPI-UHFFFAOYSA-N Erythritol Natural products OCC(O)C(O)CO UNXHWFMMPAWVPI-UHFFFAOYSA-N 0.000 claims 2
- SQUHHTBVTRBESD-UHFFFAOYSA-N Hexa-Ac-myo-Inositol Natural products CC(=O)OC1C(OC(C)=O)C(OC(C)=O)C(OC(C)=O)C(OC(C)=O)C1OC(C)=O SQUHHTBVTRBESD-UHFFFAOYSA-N 0.000 claims 2
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims 2
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims 2
- WHXSMMKQMYFTQS-UHFFFAOYSA-N Lithium Chemical compound [Li] WHXSMMKQMYFTQS-UHFFFAOYSA-N 0.000 claims 2
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 claims 2
- 229930195725 Mannitol Natural products 0.000 claims 2
- 239000002202 Polyethylene glycol Substances 0.000 claims 2
- 229920001213 Polysorbate 20 Polymers 0.000 claims 2
- 229920001219 Polysorbate 40 Polymers 0.000 claims 2
- 229920001214 Polysorbate 60 Polymers 0.000 claims 2
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 claims 2
- PYMYPHUHKUWMLA-LMVFSUKVSA-N Ribose Natural products OC[C@@H](O)[C@@H](O)[C@@H](O)C=O PYMYPHUHKUWMLA-LMVFSUKVSA-N 0.000 claims 2
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims 2
- IYFATESGLOUGBX-YVNJGZBMSA-N Sorbitan monopalmitate Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O IYFATESGLOUGBX-YVNJGZBMSA-N 0.000 claims 2
- HVUMOYIDDBPOLL-XWVZOOPGSA-N Sorbitan monostearate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O HVUMOYIDDBPOLL-XWVZOOPGSA-N 0.000 claims 2
- 229930006000 Sucrose Natural products 0.000 claims 2
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims 2
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 claims 2
- HDTRYLNUVZCQOY-WSWWMNSNSA-N Trehalose Natural products O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@@H](O)[C@@H](CO)O1 HDTRYLNUVZCQOY-WSWWMNSNSA-N 0.000 claims 2
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims 2
- IJCWFDPJFXGQBN-RYNSOKOISA-N [(2R)-2-[(2R,3R,4S)-4-hydroxy-3-octadecanoyloxyoxolan-2-yl]-2-octadecanoyloxyethyl] octadecanoate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@@H](OC(=O)CCCCCCCCCCCCCCCCC)[C@H]1OC[C@H](O)[C@H]1OC(=O)CCCCCCCCCCCCCCCCC IJCWFDPJFXGQBN-RYNSOKOISA-N 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- 150000007513 acids Chemical class 0.000 claims 2
- 239000003513 alkali Substances 0.000 claims 2
- 150000001342 alkaline earth metals Chemical class 0.000 claims 2
- HDTRYLNUVZCQOY-LIZSDCNHSA-N alpha,alpha-trehalose Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 HDTRYLNUVZCQOY-LIZSDCNHSA-N 0.000 claims 2
- HMFHBZSHGGEWLO-UHFFFAOYSA-N alpha-D-Furanose-Ribose Natural products OCC1OC(O)C(O)C1O HMFHBZSHGGEWLO-UHFFFAOYSA-N 0.000 claims 2
- WQZGKKKJIJFFOK-PHYPRBDBSA-N alpha-D-galactose Chemical compound OC[C@H]1O[C@H](O)[C@H](O)[C@@H](O)[C@H]1O WQZGKKKJIJFFOK-PHYPRBDBSA-N 0.000 claims 2
- BJEPYKJPYRNKOW-UHFFFAOYSA-N alpha-hydroxysuccinic acid Natural products OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 claims 2
- 229910000147 aluminium phosphate Inorganic materials 0.000 claims 2
- 150000003863 ammonium salts Chemical class 0.000 claims 2
- 239000003945 anionic surfactant Substances 0.000 claims 2
- 235000010323 ascorbic acid Nutrition 0.000 claims 2
- 239000011668 ascorbic acid Substances 0.000 claims 2
- 229960005070 ascorbic acid Drugs 0.000 claims 2
- SRSXLGNVWSONIS-UHFFFAOYSA-N benzenesulfonic acid Chemical compound OS(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-N 0.000 claims 2
- 229940092714 benzenesulfonic acid Drugs 0.000 claims 2
- 235000010233 benzoic acid Nutrition 0.000 claims 2
- 229910052791 calcium Inorganic materials 0.000 claims 2
- 239000011575 calcium Substances 0.000 claims 2
- 150000004649 carbonic acid derivatives Chemical class 0.000 claims 2
- 229920002678 cellulose Polymers 0.000 claims 2
- 239000001913 cellulose Substances 0.000 claims 2
- 235000010980 cellulose Nutrition 0.000 claims 2
- 235000015165 citric acid Nutrition 0.000 claims 2
- 239000000625 cyclamic acid and its Na and Ca salt Substances 0.000 claims 2
- HCAJEUSONLESMK-UHFFFAOYSA-N cyclohexylsulfamic acid Chemical compound OS(=O)(=O)NC1CCCCC1 HCAJEUSONLESMK-UHFFFAOYSA-N 0.000 claims 2
- 239000008121 dextrose Substances 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- GVGUFUZHNYFZLC-UHFFFAOYSA-N dodecyl benzenesulfonate;sodium Chemical compound [Na].CCCCCCCCCCCCOS(=O)(=O)C1=CC=CC=C1 GVGUFUZHNYFZLC-UHFFFAOYSA-N 0.000 claims 2
- UNXHWFMMPAWVPI-ZXZARUISSA-N erythritol Chemical compound OC[C@H](O)[C@H](O)CO UNXHWFMMPAWVPI-ZXZARUISSA-N 0.000 claims 2
- 235000019414 erythritol Nutrition 0.000 claims 2
- 229940009714 erythritol Drugs 0.000 claims 2
- 150000002170 ethers Chemical class 0.000 claims 2
- 150000002191 fatty alcohols Chemical class 0.000 claims 2
- 235000019253 formic acid Nutrition 0.000 claims 2
- 229940013688 formic acid Drugs 0.000 claims 2
- FBPFZTCFMRRESA-GUCUJZIJSA-N galactitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-GUCUJZIJSA-N 0.000 claims 2
- 229930182830 galactose Natural products 0.000 claims 2
- 239000000174 gluconic acid Substances 0.000 claims 2
- 235000012208 gluconic acid Nutrition 0.000 claims 2
- 239000008103 glucose Substances 0.000 claims 2
- 150000004676 glycans Chemical class 0.000 claims 2
- 229940093915 gynecological organic acid Drugs 0.000 claims 2
- 235000011167 hydrochloric acid Nutrition 0.000 claims 2
- 150000004679 hydroxides Chemical class 0.000 claims 2
- 150000007529 inorganic bases Chemical class 0.000 claims 2
- CDAISMWEOUEBRE-GPIVLXJGSA-N inositol Chemical compound O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](O)[C@@H]1O CDAISMWEOUEBRE-GPIVLXJGSA-N 0.000 claims 2
- 229960000367 inositol Drugs 0.000 claims 2
- 239000004310 lactic acid Substances 0.000 claims 2
- 235000014655 lactic acid Nutrition 0.000 claims 2
- 239000000832 lactitol Substances 0.000 claims 2
- 235000010448 lactitol Nutrition 0.000 claims 2
- VQHSOMBJVWLPSR-JVCRWLNRSA-N lactitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@@H]1O[C@H](CO)[C@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-JVCRWLNRSA-N 0.000 claims 2
- 229960003451 lactitol Drugs 0.000 claims 2
- 239000008101 lactose Substances 0.000 claims 2
- 229910052744 lithium Inorganic materials 0.000 claims 2
- 229910052749 magnesium Inorganic materials 0.000 claims 2
- 239000011777 magnesium Substances 0.000 claims 2
- 208000024714 major depressive disease Diseases 0.000 claims 2
- 239000001630 malic acid Substances 0.000 claims 2
- 235000011090 malic acid Nutrition 0.000 claims 2
- 239000000845 maltitol Substances 0.000 claims 2
- 235000010449 maltitol Nutrition 0.000 claims 2
- VQHSOMBJVWLPSR-WUJBLJFYSA-N maltitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-WUJBLJFYSA-N 0.000 claims 2
- 229940035436 maltitol Drugs 0.000 claims 2
- 239000000594 mannitol Substances 0.000 claims 2
- 235000010355 mannitol Nutrition 0.000 claims 2
- 229960001855 mannitol Drugs 0.000 claims 2
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 claims 2
- 229940098779 methanesulfonic acid Drugs 0.000 claims 2
- 150000007522 mineralic acids Chemical class 0.000 claims 2
- 239000002736 nonionic surfactant Substances 0.000 claims 2
- 150000007524 organic acids Chemical class 0.000 claims 2
- 235000005985 organic acids Nutrition 0.000 claims 2
- 150000007530 organic bases Chemical class 0.000 claims 2
- 235000006408 oxalic acid Nutrition 0.000 claims 2
- 229920001223 polyethylene glycol Polymers 0.000 claims 2
- 235000010486 polyoxyethylene sorbitan monolaurate Nutrition 0.000 claims 2
- 239000000256 polyoxyethylene sorbitan monolaurate Substances 0.000 claims 2
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims 2
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 claims 2
- 235000010483 polyoxyethylene sorbitan monopalmitate Nutrition 0.000 claims 2
- 239000000249 polyoxyethylene sorbitan monopalmitate Substances 0.000 claims 2
- 235000010989 polyoxyethylene sorbitan monostearate Nutrition 0.000 claims 2
- 239000001818 polyoxyethylene sorbitan monostearate Substances 0.000 claims 2
- 229920001282 polysaccharide Polymers 0.000 claims 2
- 239000005017 polysaccharide Substances 0.000 claims 2
- 229940068977 polysorbate 20 Drugs 0.000 claims 2
- 229940101027 polysorbate 40 Drugs 0.000 claims 2
- 229940113124 polysorbate 60 Drugs 0.000 claims 2
- 229920000053 polysorbate 80 Polymers 0.000 claims 2
- 229940068968 polysorbate 80 Drugs 0.000 claims 2
- 229910052700 potassium Inorganic materials 0.000 claims 2
- 239000011591 potassium Substances 0.000 claims 2
- 108700004121 sarkosyl Proteins 0.000 claims 2
- 201000000980 schizophrenia Diseases 0.000 claims 2
- CDAISMWEOUEBRE-UHFFFAOYSA-N scyllo-inosotol Natural products OC1C(O)C(O)C(O)C(O)C1O CDAISMWEOUEBRE-UHFFFAOYSA-N 0.000 claims 2
- 229910052708 sodium Inorganic materials 0.000 claims 2
- 239000011734 sodium Substances 0.000 claims 2
- 229940080264 sodium dodecylbenzenesulfonate Drugs 0.000 claims 2
- 229940057950 sodium laureth sulfate Drugs 0.000 claims 2
- KSAVQLQVUXSOCR-UHFFFAOYSA-M sodium lauroyl sarcosinate Chemical compound [Na+].CCCCCCCCCCCC(=O)N(C)CC([O-])=O KSAVQLQVUXSOCR-UHFFFAOYSA-M 0.000 claims 2
- 229940045885 sodium lauroyl sarcosinate Drugs 0.000 claims 2
- 235000019333 sodium laurylsulphate Nutrition 0.000 claims 2
- RYYKJJJTJZKILX-UHFFFAOYSA-M sodium octadecanoate Chemical compound [Na+].CCCCCCCCCCCCCCCCCC([O-])=O RYYKJJJTJZKILX-UHFFFAOYSA-M 0.000 claims 2
- 229940080350 sodium stearate Drugs 0.000 claims 2
- SXHLENDCVBIJFO-UHFFFAOYSA-M sodium;2-[2-(2-dodecoxyethoxy)ethoxy]ethyl sulfate Chemical compound [Na+].CCCCCCCCCCCCOCCOCCOCCOS([O-])(=O)=O SXHLENDCVBIJFO-UHFFFAOYSA-M 0.000 claims 2
- 229940035044 sorbitan monolaurate Drugs 0.000 claims 2
- 235000011069 sorbitan monooleate Nutrition 0.000 claims 2
- 239000001593 sorbitan monooleate Substances 0.000 claims 2
- 229940035049 sorbitan monooleate Drugs 0.000 claims 2
- 235000011071 sorbitan monopalmitate Nutrition 0.000 claims 2
- 239000001570 sorbitan monopalmitate Substances 0.000 claims 2
- 229940031953 sorbitan monopalmitate Drugs 0.000 claims 2
- 235000011076 sorbitan monostearate Nutrition 0.000 claims 2
- 239000001587 sorbitan monostearate Substances 0.000 claims 2
- 229940035048 sorbitan monostearate Drugs 0.000 claims 2
- 235000011078 sorbitan tristearate Nutrition 0.000 claims 2
- 239000001589 sorbitan tristearate Substances 0.000 claims 2
- 229960004129 sorbitan tristearate Drugs 0.000 claims 2
- 229960002920 sorbitol Drugs 0.000 claims 2
- 239000006190 sub-lingual tablet Substances 0.000 claims 2
- 229940098466 sublingual tablet Drugs 0.000 claims 2
- 239000005720 sucrose Substances 0.000 claims 2
- 229960004793 sucrose Drugs 0.000 claims 2
- 235000000346 sugar Nutrition 0.000 claims 2
- 150000005846 sugar alcohols Chemical class 0.000 claims 2
- 150000008163 sugars Chemical class 0.000 claims 2
- 239000011975 tartaric acid Substances 0.000 claims 2
- 235000002906 tartaric acid Nutrition 0.000 claims 2
- 229940074410 trehalose Drugs 0.000 claims 2
- 239000000811 xylitol Substances 0.000 claims 2
- 235000010447 xylitol Nutrition 0.000 claims 2
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 claims 2
- 229960002675 xylitol Drugs 0.000 claims 2
- JNYAEWCLZODPBN-UHFFFAOYSA-N 2-(1,2-dihydroxyethyl)oxolane-3,4-diol Polymers OCC(O)C1OCC(O)C1O JNYAEWCLZODPBN-UHFFFAOYSA-N 0.000 claims 1
- HOIIHACBCFLJET-SFTDATJTSA-N 4-((6br,10as)-3-methyl-2,3,6b,9,10,10a-hexahydro-1h-pyrido-[3',4':4,5]-pyrrolo[1,2,3-de]quinoxalin-8-(7h)-yl)-1-(4-fluorophenyl)-1-butanone Chemical compound C([C@@H]1N2CCN(C=3C=CC=C(C2=3)[C@@H]1C1)C)CN1CCCC(=O)C1=CC=C(F)C=C1 HOIIHACBCFLJET-SFTDATJTSA-N 0.000 claims 1
- 102000049773 5-HT2A Serotonin Receptor Human genes 0.000 claims 1
- 108010072564 5-HT2A Serotonin Receptor Proteins 0.000 claims 1
- GJCOSYZMQJWQCA-UHFFFAOYSA-N 9H-xanthene Chemical compound C1=CC=C2CC3=CC=CC=C3OC2=C1 GJCOSYZMQJWQCA-UHFFFAOYSA-N 0.000 claims 1
- 244000215068 Acacia senegal Species 0.000 claims 1
- 241000251468 Actinopterygii Species 0.000 claims 1
- 229920001817 Agar Polymers 0.000 claims 1
- 208000019901 Anxiety disease Diseases 0.000 claims 1
- 241000416162 Astragalus gummifer Species 0.000 claims 1
- 241000271566 Aves Species 0.000 claims 1
- 241000283690 Bos taurus Species 0.000 claims 1
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Claims (22)
1. Трансмукозальная фармацевтическая композиция для профилактики и/или лечения психиатрических и неврологических заболеваний, содержащая терапевтически эффективное количество 1–(4–фтор–фенил)–4–((6bR,10aS)–3–метил–2,3,6b,9,10,10a–гексагидро–1H,7H–пиридо[3′,4′:4,5]пирроло[1,2,3–de]хиноксалин–8–ил)–бутан–1–она (соединение Формулы I) в форме свободного основания или фармацевтически приемлемой соли;
где композиция представляет собой сублингвальную пленку или сублингвальную таблетку или облатку; и
где композиция содержит один или несколько желатинов, включая негелеобразующие и гелеобразующие типы.
2. Композиция по п.1, где композиция содержит соединение формулы I в форме свободного основания.
3. Композиция по п.1, где композиция содержит соединение формулы I в форме фармацевтически приемлемой соли.
4. Композиция по п.3, где форма соли представляет собой тозилат.
5. Композиция по п.1, где композиция содержит от 0,01 мг до 10 мг соединения формулы I (эквивалент свободного основания).
6. Композиция по любому из пп.1-5, где композиция дополнительно содержит один или несколько эксципиентов, выбранных из любого из следующих: сахара и сахарные спирты (например, декстроза, лактоза, галактоза, глюкоза, рибоза, сахароза, трегалоза, маннит, мальтит, лактитол, сорбит, ксилит, эритрит, галактит, инозит), неорганические или органические кислоты (например, лимонная кислота, молочная кислота, яблочная кислота, глюконовая кислота, бензойная кислота, толуолсульфоновая кислота, фосфорная кислота, серная кислота, хлористоводородная кислота, винная кислота, щавелевая кислота, цикламиновая кислота, аскорбиновая кислота, метансульфоновая кислота, бензолсульфоновая кислота, муравьиная кислота) и их соли (например, натриевые, калиевые, кальциевые, магниевые, литиевые, аммониевые соли вышеперечисленных кислот), неорганические или органические основания (например, карбонаты, бикарбонаты, гидроксиды, оксиды щелочных или щелочноземельных металлов), анионные поверхностно–активные вещества (например, лаурилсульфат натрия, лауретсульфат натрия, додецилбензолсульфонат натрия, лауроилсаркозинат натрия, стеарат натрия), неионные поверхностно–активные вещества (например, этоксилаты жирных спиртов (например, полидодециловые эфиры полиэтиленгликоля), сложные эфиры сорбитана (например, сорбитанмонолаурат, сорбитанмоноолеат, сорбитанмонопальмитат, сорбитанмоностеарат, сорбитантристеарат), полиэтоксилированные сложные эфиры сорбита (например, полисорбат 20, полисорбат 40, полисорбат 60, полисорбат 80).
7. Композиция по любому из пп.1-5, где композиция дополнительно содержит один или несколько полимеров, выбранных из камедей (например, аравийская камедь, гуар, агар, ксантан, трагакант, карайя, геллан).
8. Композиция по любому из пп.1-5, где композиция дополнительно содержит один или несколько полимеров, выбранных из полисахаридов и производных полисахаридов (например, крахмалы, декстраны, пектины, альгинаты, каррагинаны, целлюлоза, производные целлюлозы (например, карбоксиметилцеллюлоза, метилцеллюлоза, гидроксиалкилцеллюлоза (например, гидроксиэтилцеллюлоза, гидроксипропилцеллюлоза, гидроксипропилметилцеллюлоза)).
9. Композиция по любому из пп.1-5, где композиция дополнительно содержит один или несколько эксципиентов, выбранных из любого из следующих: синтетические полимеры (например, поливинилпирролидоны, полимеры и сополимеры полиэтиленоксида и/или полипропиленоксида (например, полоксамеры, такие как полоксамер 188) и полиакрилатные полимеры (например, карбополы), полиамидные полимеры).
10. Композиция по любому из пп.1-5, где композиция дополнительно содержит один или несколько эксципиентов, выбранных из любого из следующих: сахара и сахарные спирты (например, декстроза, лактоза, галактоза, глюкоза, рибоза, сахароза, трегалоза, маннит, мальтит, лактитол, сорбит, ксилит, эритрит, галактит, инозит).
11. Композиция по любому из пп.1-5, где композиция дополнительно содержит один или несколько эксципиентов, выбранных из любого из следующих: неорганические или органические кислоты (например, лимонная кислота, молочная кислота, яблочная кислота, глюконовая кислота, бензойная кислота, толуолсульфоновая кислота, фосфорная кислота, серная кислота, хлористоводородная кислота, винная кислота, щавелевая кислота, цикламиновая кислота, аскорбиновая кислота, метансульфоновая кислота, бензолсульфоновая кислота, муравьиная кислота) и их соли (например, натриевые, калиевые, кальциевые, магниевые, литиевые, аммониевые соли вышеперечисленных кислот) или неорганические или органические основания (например, карбонаты, бикарбонаты, гидроксиды, оксиды щелочных или щелочноземельных металлов).
12. Композиция по любому из пп.1-5, где композиция дополнительно содержит один или несколько эксципиентов, выбранных из любого из следующих: анионные поверхностно-активные вещества (например, лаурилсульфат натрия, лауретсульфат натрия, додецилбензолсульфонат натрия, лауроилсаркозинат натрия, стеарат натрия), катионные поверхностно–активные вещества (например, галогениды бензалкония, галогениды цетилпиридиния, галогениды цетримония, галогениды бензетония), цвиттер–ионные поверхностно–активные вещества (например, кокамидоалкилбетаины, такие как кокамидопропилбетаин), неионные поверхностно–активные вещества (например, этоксилаты жирных спиртов (например, полидодециловые эфиры полиэтиленгликоля), сложные эфиры сорбитана (например, сорбитанмонолаурат, сорбитанмоноолеат, сорбитанмонопальмитат, сорбитанмоностеарат, сорбитантристеарат), полиэтоксилированные сложные эфиры сорбита (например, полисорбат 20, полисорбат 40, полисорбат 60, полисорбат 80).
13. Композиция по п.1, в которой сублингвальная таблетка или облатка представляет собой быстрорастворимую таблетку или облатку.
14. Композиция по п.1, в которой желатины представляют собой желатины млекопитающих, такие как бычий желатин, свиные желатины, птичьи желатины, рыбьи желатины (например, смешанные высокомолекулярные и низкомолекулярные желатины).
15. Композиция по любому из пп. 1-14, где психиатрическое и неврологическое заболевание представляет собой заболевание, опосредованное сигнальными путями рецептора 5-HT2A, транспортера серотонина и/или рецептора допамина D1/D2.
16. Композиция по любому из пп. 1-14, где психиатрическое и неврологическое заболевание представляет собой заболевание, выбранное из депрессии, большого депрессивного расстройства, тревоги, психоза, шизофрении, деменции и биполярного расстройства.
17. Композиция по любому из пп. 1-14, где психиатрическим и неврологическим заболеванием является шизофрения.
18. Композиция по любому из пп. 1-14, где психиатрическое и неврологическое заболевание представляет собой депрессию или большое депрессивное расстройство.
19. Композиция по любому из пп. 1-14, где психиатрическим и неврологическим заболеванием является деменция.
20. Композиция по любому из пп. 1-14, где психиатрическое и неврологическое заболевание представляет собой биполярное расстройство.
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