CN117205209A - 含有阿托品的水性组合物 - Google Patents
含有阿托品的水性组合物 Download PDFInfo
- Publication number
- CN117205209A CN117205209A CN202311238651.XA CN202311238651A CN117205209A CN 117205209 A CN117205209 A CN 117205209A CN 202311238651 A CN202311238651 A CN 202311238651A CN 117205209 A CN117205209 A CN 117205209A
- Authority
- CN
- China
- Prior art keywords
- aqueous composition
- buffer
- composition according
- group
- atropine
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 245
- 229930003347 Atropine Natural products 0.000 title claims abstract description 77
- RKUNBYITZUJHSG-UHFFFAOYSA-N Hyosciamin-hydrochlorid Natural products CN1C(C2)CCC1CC2OC(=O)C(CO)C1=CC=CC=C1 RKUNBYITZUJHSG-UHFFFAOYSA-N 0.000 title claims abstract description 77
- 229960000396 atropine Drugs 0.000 title claims abstract description 77
- RKUNBYITZUJHSG-SPUOUPEWSA-N atropine Chemical compound O([C@H]1C[C@H]2CC[C@@H](C1)N2C)C(=O)C(CO)C1=CC=CC=C1 RKUNBYITZUJHSG-SPUOUPEWSA-N 0.000 title claims abstract description 77
- 239000000872 buffer Substances 0.000 claims abstract description 129
- 229920003169 water-soluble polymer Polymers 0.000 claims abstract description 50
- 150000003839 salts Chemical class 0.000 claims abstract description 49
- 239000008363 phosphate buffer Substances 0.000 claims abstract description 41
- 239000008351 acetate buffer Substances 0.000 claims abstract description 20
- BVKZGUZCCUSVTD-UHFFFAOYSA-L Carbonate Chemical compound [O-]C([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-L 0.000 claims abstract description 18
- KXDHJXZQYSOELW-UHFFFAOYSA-N Carbamic acid Chemical compound NC(O)=O KXDHJXZQYSOELW-UHFFFAOYSA-N 0.000 claims abstract description 17
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims abstract description 16
- BTBUEUYNUDRHOZ-UHFFFAOYSA-N Borate Chemical compound [O-]B([O-])[O-] BTBUEUYNUDRHOZ-UHFFFAOYSA-N 0.000 claims abstract description 15
- 229940095064 tartrate Drugs 0.000 claims abstract description 15
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 claims abstract description 8
- 229960000281 trometamol Drugs 0.000 claims abstract description 8
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 52
- 239000012929 tonicity agent Substances 0.000 claims description 42
- 239000007979 citrate buffer Substances 0.000 claims description 33
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 claims description 27
- 239000004354 Hydroxyethyl cellulose Substances 0.000 claims description 26
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 claims description 26
- 229940071826 hydroxyethyl cellulose Drugs 0.000 claims description 26
- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical compound [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 claims description 25
- 229960000686 benzalkonium chloride Drugs 0.000 claims description 24
- 235000011187 glycerol Nutrition 0.000 claims description 22
- 238000000034 method Methods 0.000 claims description 20
- 230000002401 inhibitory effect Effects 0.000 claims description 18
- 239000003889 eye drop Substances 0.000 claims description 17
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 16
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 16
- 230000004515 progressive myopia Effects 0.000 claims description 16
- 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 description 15
- 229930195725 Mannitol Natural products 0.000 claims description 15
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 15
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 15
- 239000000594 mannitol Substances 0.000 claims description 15
- 235000010355 mannitol Nutrition 0.000 claims description 15
- 235000010980 cellulose Nutrition 0.000 claims description 14
- 229920002678 cellulose Polymers 0.000 claims description 14
- 239000001913 cellulose Substances 0.000 claims description 14
- 229940012356 eye drops Drugs 0.000 claims description 13
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims description 12
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims description 12
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 claims description 11
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims description 11
- 229920002125 Sokalan® Polymers 0.000 claims description 11
- 238000002360 preparation method Methods 0.000 claims description 10
- KGBXLFKZBHKPEV-UHFFFAOYSA-N boric acid Chemical compound OB(O)O KGBXLFKZBHKPEV-UHFFFAOYSA-N 0.000 claims description 9
- 239000004327 boric acid Substances 0.000 claims description 9
- 230000007423 decrease Effects 0.000 claims description 9
- 229910000403 monosodium phosphate Inorganic materials 0.000 claims description 9
- 235000019799 monosodium phosphate Nutrition 0.000 claims description 9
- AJPJDKMHJJGVTQ-UHFFFAOYSA-M sodium dihydrogen phosphate Chemical compound [Na+].OP(O)([O-])=O AJPJDKMHJJGVTQ-UHFFFAOYSA-M 0.000 claims description 9
- IXPNQXFRVYWDDI-UHFFFAOYSA-N 1-methyl-2,4-dioxo-1,3-diazinane-5-carboximidamide Chemical compound CN1CC(C(N)=N)C(=O)NC1=O IXPNQXFRVYWDDI-UHFFFAOYSA-N 0.000 claims description 8
- 229940009098 aspartate Drugs 0.000 claims description 8
- -1 carboxymethyl ethyl Chemical group 0.000 claims description 8
- 229940049906 glutamate Drugs 0.000 claims description 8
- 229930195712 glutamate Natural products 0.000 claims description 8
- 235000010413 sodium alginate Nutrition 0.000 claims description 8
- 239000000661 sodium alginate Substances 0.000 claims description 8
- 229940005550 sodium alginate Drugs 0.000 claims description 8
- 229910021538 borax Inorganic materials 0.000 claims description 7
- 239000001768 carboxy methyl cellulose Substances 0.000 claims description 7
- 239000003814 drug Substances 0.000 claims description 7
- 239000001488 sodium phosphate Substances 0.000 claims description 7
- 235000010339 sodium tetraborate Nutrition 0.000 claims description 7
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims description 6
- 239000002202 Polyethylene glycol Substances 0.000 claims description 6
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 claims description 6
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical group OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 6
- 229920001223 polyethylene glycol Polymers 0.000 claims description 6
- SCVFZCLFOSHCOH-UHFFFAOYSA-M potassium acetate Chemical compound [K+].CC([O-])=O SCVFZCLFOSHCOH-UHFFFAOYSA-M 0.000 claims description 6
- BWHMMNNQKKPAPP-UHFFFAOYSA-L potassium carbonate Chemical compound [K+].[K+].[O-]C([O-])=O BWHMMNNQKKPAPP-UHFFFAOYSA-L 0.000 claims description 6
- 239000001856 Ethyl cellulose Substances 0.000 claims description 5
- 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 description 4
- 229920002134 Carboxymethyl cellulose Polymers 0.000 claims description 4
- 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 description 4
- 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 description 4
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 claims description 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 description 4
- 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 description 4
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims description 4
- 229960000583 acetic acid Drugs 0.000 claims description 4
- 235000011054 acetic acid Nutrition 0.000 claims description 4
- 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 description 4
- 229960002028 atropine sulfate Drugs 0.000 claims description 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 description 4
- BVKZGUZCCUSVTD-UHFFFAOYSA-N carbonic acid Chemical compound OC(O)=O BVKZGUZCCUSVTD-UHFFFAOYSA-N 0.000 claims description 4
- 235000010948 carboxy methyl cellulose Nutrition 0.000 claims description 4
- 239000008112 carboxymethyl-cellulose Substances 0.000 claims description 4
- 229920001249 ethyl cellulose Polymers 0.000 claims description 4
- 235000019325 ethyl cellulose Nutrition 0.000 claims description 4
- 239000008103 glucose Substances 0.000 claims description 4
- 229920003063 hydroxymethyl cellulose Polymers 0.000 claims description 4
- 229940031574 hydroxymethyl cellulose Drugs 0.000 claims description 4
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 claims description 4
- 229910000402 monopotassium phosphate Inorganic materials 0.000 claims description 4
- 235000019796 monopotassium phosphate Nutrition 0.000 claims description 4
- LWIHDJKSTIGBAC-UHFFFAOYSA-K potassium phosphate Substances [K+].[K+].[K+].[O-]P([O-])([O-])=O LWIHDJKSTIGBAC-UHFFFAOYSA-K 0.000 claims description 4
- 235000013772 propylene glycol Nutrition 0.000 claims description 4
- 239000001509 sodium citrate Substances 0.000 claims description 4
- 239000004328 sodium tetraborate Substances 0.000 claims description 4
- 239000000600 sorbitol Substances 0.000 claims description 4
- 239000000811 xylitol Substances 0.000 claims description 4
- 235000010447 xylitol Nutrition 0.000 claims description 4
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 claims description 4
- 229960002675 xylitol Drugs 0.000 claims description 4
- LNAZSHAWQACDHT-XIYTZBAFSA-N (2r,3r,4s,5r,6s)-4,5-dimethoxy-2-(methoxymethyl)-3-[(2s,3r,4s,5r,6r)-3,4,5-trimethoxy-6-(methoxymethyl)oxan-2-yl]oxy-6-[(2r,3r,4s,5r,6r)-4,5,6-trimethoxy-2-(methoxymethyl)oxan-3-yl]oxyoxane Chemical compound CO[C@@H]1[C@@H](OC)[C@H](OC)[C@@H](COC)O[C@H]1O[C@H]1[C@H](OC)[C@@H](OC)[C@H](O[C@H]2[C@@H]([C@@H](OC)[C@H](OC)O[C@@H]2COC)OC)O[C@@H]1COC LNAZSHAWQACDHT-XIYTZBAFSA-N 0.000 claims description 3
- OOSZCNKVJAVHJI-UHFFFAOYSA-N 1-[(4-fluorophenyl)methyl]piperazine Chemical compound C1=CC(F)=CC=C1CN1CCNCC1 OOSZCNKVJAVHJI-UHFFFAOYSA-N 0.000 claims description 3
- SLXKOJJOQWFEFD-UHFFFAOYSA-N 6-aminohexanoic acid Chemical group NCCCCCC(O)=O SLXKOJJOQWFEFD-UHFFFAOYSA-N 0.000 claims description 3
- USFZMSVCRYTOJT-UHFFFAOYSA-N Ammonium acetate Chemical compound N.CC(O)=O USFZMSVCRYTOJT-UHFFFAOYSA-N 0.000 claims description 3
- 239000005695 Ammonium acetate Substances 0.000 claims description 3
- ATRRKUHOCOJYRX-UHFFFAOYSA-N Ammonium bicarbonate Chemical compound [NH4+].OC([O-])=O ATRRKUHOCOJYRX-UHFFFAOYSA-N 0.000 claims description 3
- 229920000623 Cellulose acetate phthalate Polymers 0.000 claims description 3
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 claims description 3
- 229920001479 Hydroxyethyl methyl cellulose Polymers 0.000 claims description 3
- VMHLLURERBWHNL-UHFFFAOYSA-M Sodium acetate Chemical compound [Na+].CC([O-])=O VMHLLURERBWHNL-UHFFFAOYSA-M 0.000 claims description 3
- UIIMBOGNXHQVGW-DEQYMQKBSA-M Sodium bicarbonate-14C Chemical compound [Na+].O[14C]([O-])=O UIIMBOGNXHQVGW-DEQYMQKBSA-M 0.000 claims description 3
- FZQSLXQPHPOTHG-UHFFFAOYSA-N [K+].[K+].O1B([O-])OB2OB([O-])OB1O2 Chemical compound [K+].[K+].O1B([O-])OB2OB([O-])OB1O2 FZQSLXQPHPOTHG-UHFFFAOYSA-N 0.000 claims description 3
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims description 3
- ZUAAPNNKRHMPKG-UHFFFAOYSA-N acetic acid;butanedioic acid;methanol;propane-1,2-diol Chemical compound OC.CC(O)=O.CC(O)CO.OC(=O)CCC(O)=O ZUAAPNNKRHMPKG-UHFFFAOYSA-N 0.000 claims description 3
- 229960002684 aminocaproic acid Drugs 0.000 claims description 3
- 229940043376 ammonium acetate Drugs 0.000 claims description 3
- 235000019257 ammonium acetate Nutrition 0.000 claims description 3
- 239000001099 ammonium carbonate Substances 0.000 claims description 3
- 235000012501 ammonium carbonate Nutrition 0.000 claims description 3
- 235000003704 aspartic acid Nutrition 0.000 claims description 3
- OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 claims description 3
- VSGNNIFQASZAOI-UHFFFAOYSA-L calcium acetate Chemical compound [Ca+2].CC([O-])=O.CC([O-])=O VSGNNIFQASZAOI-UHFFFAOYSA-L 0.000 claims description 3
- 239000001639 calcium acetate Substances 0.000 claims description 3
- 235000011092 calcium acetate Nutrition 0.000 claims description 3
- 229960005147 calcium acetate Drugs 0.000 claims description 3
- 229910000019 calcium carbonate Inorganic materials 0.000 claims description 3
- 235000010216 calcium carbonate Nutrition 0.000 claims description 3
- FNAQSUUGMSOBHW-UHFFFAOYSA-H calcium citrate Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O.[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O FNAQSUUGMSOBHW-UHFFFAOYSA-H 0.000 claims description 3
- 239000001354 calcium citrate Substances 0.000 claims description 3
- 229940081734 cellulose acetate phthalate Drugs 0.000 claims description 3
- 150000001875 compounds Chemical class 0.000 claims description 3
- ZPWVASYFFYYZEW-UHFFFAOYSA-L dipotassium hydrogen phosphate Chemical compound [K+].[K+].OP([O-])([O-])=O ZPWVASYFFYYZEW-UHFFFAOYSA-L 0.000 claims description 3
- 235000019797 dipotassium phosphate Nutrition 0.000 claims description 3
- 229910000396 dipotassium phosphate Inorganic materials 0.000 claims description 3
- WDRWZVWLVBXVOI-QTNFYWBSSA-L dipotassium;(2s)-2-aminopentanedioate Chemical compound [K+].[K+].[O-]C(=O)[C@@H](N)CCC([O-])=O WDRWZVWLVBXVOI-QTNFYWBSSA-L 0.000 claims description 3
- PXEDJBXQKAGXNJ-QTNFYWBSSA-L disodium L-glutamate Chemical compound [Na+].[Na+].[O-]C(=O)[C@@H](N)CCC([O-])=O PXEDJBXQKAGXNJ-QTNFYWBSSA-L 0.000 claims description 3
- PYLIXCKOHOHGKQ-UHFFFAOYSA-L disodium;hydrogen phosphate;heptahydrate Chemical compound O.O.O.O.O.O.O.[Na+].[Na+].OP([O-])([O-])=O PYLIXCKOHOHGKQ-UHFFFAOYSA-L 0.000 claims description 3
- 235000013922 glutamic acid Nutrition 0.000 claims description 3
- 239000004220 glutamic acid Substances 0.000 claims description 3
- 229960003943 hypromellose Drugs 0.000 claims description 3
- 229960001983 magnesium aspartate Drugs 0.000 claims description 3
- ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 claims description 3
- 239000001095 magnesium carbonate Substances 0.000 claims description 3
- 229910000021 magnesium carbonate Inorganic materials 0.000 claims description 3
- 235000014380 magnesium carbonate Nutrition 0.000 claims description 3
- RXMQCXCANMAVIO-CEOVSRFSSA-L magnesium;(2s)-2-amino-4-hydroxy-4-oxobutanoate Chemical compound [H+].[H+].[Mg+2].[O-]C(=O)[C@@H](N)CC([O-])=O.[O-]C(=O)[C@@H](N)CC([O-])=O RXMQCXCANMAVIO-CEOVSRFSSA-L 0.000 claims description 3
- 229920000609 methyl cellulose Polymers 0.000 claims description 3
- 235000010981 methylcellulose Nutrition 0.000 claims description 3
- 239000001923 methylcellulose Substances 0.000 claims description 3
- 235000013919 monopotassium glutamate Nutrition 0.000 claims description 3
- 235000013923 monosodium glutamate Nutrition 0.000 claims description 3
- PJNZPQUBCPKICU-UHFFFAOYSA-N phosphoric acid;potassium Chemical compound [K].OP(O)(O)=O PJNZPQUBCPKICU-UHFFFAOYSA-N 0.000 claims description 3
- XNGIFLGASWRNHJ-UHFFFAOYSA-L phthalate(2-) Chemical compound [O-]C(=O)C1=CC=CC=C1C([O-])=O XNGIFLGASWRNHJ-UHFFFAOYSA-L 0.000 claims description 3
- AVTYONGGKAJVTE-OLXYHTOASA-L potassium L-tartrate Chemical compound [K+].[K+].[O-]C(=O)[C@H](O)[C@@H](O)C([O-])=O AVTYONGGKAJVTE-OLXYHTOASA-L 0.000 claims description 3
- 235000011056 potassium acetate Nutrition 0.000 claims description 3
- 229960004109 potassium acetate Drugs 0.000 claims description 3
- 239000011736 potassium bicarbonate Substances 0.000 claims description 3
- 235000015497 potassium bicarbonate Nutrition 0.000 claims description 3
- 229910000028 potassium bicarbonate Inorganic materials 0.000 claims description 3
- 229910000027 potassium carbonate Inorganic materials 0.000 claims description 3
- 235000011181 potassium carbonates Nutrition 0.000 claims description 3
- 239000001508 potassium citrate Substances 0.000 claims description 3
- 229960002635 potassium citrate Drugs 0.000 claims description 3
- QEEAPRPFLLJWCF-UHFFFAOYSA-K potassium citrate (anhydrous) Chemical compound [K+].[K+].[K+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O QEEAPRPFLLJWCF-UHFFFAOYSA-K 0.000 claims description 3
- 235000011082 potassium citrates Nutrition 0.000 claims description 3
- TYJJADVDDVDEDZ-UHFFFAOYSA-M potassium hydrogencarbonate Chemical compound [K+].OC([O-])=O TYJJADVDDVDEDZ-UHFFFAOYSA-M 0.000 claims description 3
- 229940111695 potassium tartrate Drugs 0.000 claims description 3
- JVUYWILPYBCNNG-UHFFFAOYSA-N potassium;oxido(oxo)borane Chemical compound [K+].[O-]B=O JVUYWILPYBCNNG-UHFFFAOYSA-N 0.000 claims description 3
- HELHAJAZNSDZJO-OLXYHTOASA-L sodium L-tartrate Chemical compound [Na+].[Na+].[O-]C(=O)[C@H](O)[C@@H](O)C([O-])=O HELHAJAZNSDZJO-OLXYHTOASA-L 0.000 claims description 3
- 239000001632 sodium acetate Substances 0.000 claims description 3
- 235000017281 sodium acetate Nutrition 0.000 claims description 3
- 229960004249 sodium acetate Drugs 0.000 claims description 3
- 229910000029 sodium carbonate Inorganic materials 0.000 claims description 3
- 235000017550 sodium carbonate Nutrition 0.000 claims description 3
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims description 3
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 claims description 3
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 claims description 3
- 235000011083 sodium citrates Nutrition 0.000 claims description 3
- 229940074545 sodium dihydrogen phosphate dihydrate Drugs 0.000 claims description 3
- 229940073490 sodium glutamate Drugs 0.000 claims description 3
- 239000001476 sodium potassium tartrate Substances 0.000 claims description 3
- 235000011006 sodium potassium tartrate Nutrition 0.000 claims description 3
- 239000001433 sodium tartrate Substances 0.000 claims description 3
- 229960002167 sodium tartrate Drugs 0.000 claims description 3
- 235000011004 sodium tartrates Nutrition 0.000 claims description 3
- WTWSHHITWMVLBX-DKWTVANSSA-M sodium;(2s)-2-aminobutanedioate;hydron Chemical compound [Na+].[O-]C(=O)[C@@H](N)CC(O)=O WTWSHHITWMVLBX-DKWTVANSSA-M 0.000 claims description 3
- WYXIGTJNYDDFFH-UHFFFAOYSA-Q triazanium;borate Chemical compound [NH4+].[NH4+].[NH4+].[O-]B([O-])[O-] WYXIGTJNYDDFFH-UHFFFAOYSA-Q 0.000 claims description 3
- 235000013337 tricalcium citrate Nutrition 0.000 claims description 3
- WUUHFRRPHJEEKV-UHFFFAOYSA-N tripotassium borate Chemical compound [K+].[K+].[K+].[O-]B([O-])[O-] WUUHFRRPHJEEKV-UHFFFAOYSA-N 0.000 claims description 3
- BSVBQGMMJUBVOD-UHFFFAOYSA-N trisodium borate Chemical compound [Na+].[Na+].[Na+].[O-]B([O-])[O-] BSVBQGMMJUBVOD-UHFFFAOYSA-N 0.000 claims description 3
- HRXKRNGNAMMEHJ-UHFFFAOYSA-K trisodium citrate Chemical compound [Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O HRXKRNGNAMMEHJ-UHFFFAOYSA-K 0.000 claims description 3
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 claims description 3
- 229910000406 trisodium phosphate Inorganic materials 0.000 claims description 3
- 235000019801 trisodium phosphate Nutrition 0.000 claims description 3
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 2
- 239000006172 buffering agent Substances 0.000 claims description 2
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- Organic Chemistry (AREA)
- Inorganic Chemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Emergency Medicine (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Materials For Photolithography (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Compositions Of Macromolecular Compounds (AREA)
Applications Claiming Priority (4)
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| CN201780031738.6A CN109310687B (zh) | 2016-05-25 | 2017-05-24 | 含有阿托品的水性组合物 |
| PCT/JP2017/019423 WO2017204262A1 (en) | 2016-05-25 | 2017-05-24 | Atropine-containing aqueous composition |
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| CN201780031738.6A Division CN109310687B (zh) | 2016-05-25 | 2017-05-24 | 含有阿托品的水性组合物 |
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| CN117205209A true CN117205209A (zh) | 2023-12-12 |
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| CN201780031738.6A Active CN109310687B (zh) | 2016-05-25 | 2017-05-24 | 含有阿托品的水性组合物 |
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| CN202311240197.1A Pending CN117205210A (zh) | 2016-05-25 | 2017-05-24 | 含有阿托品的水性组合物 |
| CN201780031738.6A Active CN109310687B (zh) | 2016-05-25 | 2017-05-24 | 含有阿托品的水性组合物 |
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| EP (2) | EP4112055A1 (enExample) |
| JP (6) | JP6590860B2 (enExample) |
| KR (4) | KR20250067951A (enExample) |
| CN (3) | CN117205209A (enExample) |
| AR (1) | AR108591A1 (enExample) |
| CA (1) | CA3023149C (enExample) |
| EA (1) | EA201892703A1 (enExample) |
| ES (1) | ES2929368T3 (enExample) |
| MY (1) | MY189774A (enExample) |
| PH (1) | PH12018502421A1 (enExample) |
| SG (1) | SG11201809822SA (enExample) |
| TW (3) | TWI849355B (enExample) |
| UA (1) | UA126195C2 (enExample) |
| WO (1) | WO2017204262A1 (enExample) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| US9421199B2 (en) | 2014-06-24 | 2016-08-23 | Sydnexis, Inc. | Ophthalmic composition |
| WO2016172712A2 (en) * | 2015-04-23 | 2016-10-27 | Sydnexis, Inc. | Ophthalmic composition |
| US11052094B2 (en) | 2015-05-29 | 2021-07-06 | Sydnexis, Inc. | D2O stabilized pharmaceutical formulations |
| WO2018154440A1 (en) * | 2017-02-21 | 2018-08-30 | Singapore Health Services Pte Ltd | Composition and method for preventing or delaying onset of myopia comprising atropine |
| MX392558B (es) | 2017-05-11 | 2025-03-24 | Vyluma Inc | Composición oftálmica líquida estable, que comprende una solución acuosa con un tampón, un agente de tonicidad, un quelante, un modificador de la viscosidad y atropina; y el uso de la misma para el tratamiento de la miopía. |
| CN109157503B (zh) * | 2018-09-25 | 2019-08-16 | 沈阳兴齐眼药股份有限公司 | 防治nitm的药物组合物及其医药用途 |
| CN110934816B (zh) * | 2018-09-25 | 2022-04-08 | 沈阳兴齐眼科医院有限公司 | 一种提高低浓度阿托品眼用制剂稳定性的方法 |
| EP3701938B8 (en) | 2019-03-01 | 2024-02-21 | Medivis S.R.L. | Ophthalmic formulations based on atropine |
| CN114302726A (zh) * | 2020-08-04 | 2022-04-08 | 参天制药株式会社 | 用于治疗近视、预防近视及/或抑制近视发展的药剂 |
| AU2021362374A1 (en) * | 2020-10-14 | 2023-05-25 | Santen Pharmaceutical Co., Ltd. | Stable pharmaceutical composition |
| AU2021368138A1 (en) | 2020-11-02 | 2023-06-22 | Trethera Corporation | Crystalline forms of a deoxycytidine kinase inhibitor and uses thereof |
| WO2022130337A1 (en) * | 2020-12-17 | 2022-06-23 | Sun Pharmaceutical Industries Limited | An aqueous sterile solution of atropine for ophthalmic use |
| EP4088714A1 (en) | 2021-05-10 | 2022-11-16 | Warszawskie Zaklady Farmaceutyczne Polfa S.A. | Ophthalmic pharmaceutical composition comprising atropine |
| EP4088713A1 (en) | 2021-05-10 | 2022-11-16 | Warszawskie Zaklady Farmaceutyczne Polfa S.A. | Ophthalmic pharmaceutical composition comprising atropine |
| US20230120997A1 (en) * | 2021-10-18 | 2023-04-20 | Ocular Science, Inc. | Compositions and methods for myopia control and orthokeratology lenses treatment |
| CN114129511A (zh) * | 2021-12-07 | 2022-03-04 | 河南润弘制药股份有限公司 | 一种具有改进稳定性的硫酸阿托品注射液 |
| AU2023337098A1 (en) * | 2022-09-11 | 2024-10-03 | Alcon Inc. | Aqueous pharmaceutical compositions comprising benzyl atropine and uses thereof |
| JP7665073B1 (ja) | 2024-04-05 | 2025-04-18 | ロート製薬株式会社 | 容器に収容してなる眼科用組成物 |
| JP7723851B1 (ja) * | 2024-11-22 | 2025-08-14 | 参天製薬株式会社 | アトロピン含有水性医薬組成物 |
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| JP2617508B2 (ja) * | 1988-02-05 | 1997-06-04 | エーザイ株式会社 | 安定なジフェンヒドラミン含有水溶液 |
| JP3166002B2 (ja) * | 1997-01-27 | 2001-05-14 | 日本車輌製造株式会社 | 自動車の洗浄装置 |
| US20030096831A1 (en) | 2000-01-18 | 2003-05-22 | Stone Richard A. | Ocular growth and nicotinic antagonists |
| EP1397132A4 (en) * | 2001-05-25 | 2006-12-13 | Valley Forge Pharmaceuticals I | OPHTHALMIC PIRENZEPINE GEL |
| US20070254914A1 (en) * | 2006-05-01 | 2007-11-01 | Non-Profit Organization Chang Gung Memorial Hospital | Low-concentration atropine solution for preventing myopia progression and preparing method thereof |
| JP2007308398A (ja) * | 2006-05-17 | 2007-11-29 | Chang Gung Memorial Hospital | 目薬、及びその製造方法 |
| WO2008144065A1 (en) * | 2007-05-21 | 2008-11-27 | Neuroptix Corporation | Ophthalmic formulations of amyloid- contrast agents and methods of use thereof |
| CN101327216A (zh) * | 2007-06-22 | 2008-12-24 | 肖正连 | 一种硫酸阿托品眼用即型凝胶 |
| WO2012161655A1 (en) * | 2011-05-23 | 2012-11-29 | Singapore Health Services Pte Ltd | Composition and/or method for reducing and/or preventing myopia progression comprising atropine |
| US20160009705A1 (en) * | 2014-06-24 | 2016-01-14 | Sydnexis, Inc. | Ophthalmic composition |
| US9421199B2 (en) * | 2014-06-24 | 2016-08-23 | Sydnexis, Inc. | Ophthalmic composition |
| JP2017102939A (ja) * | 2016-12-26 | 2017-06-08 | 株式会社プロフィールド | オーサリング装置、オーサリング方法、およびプログラム |
| MX392558B (es) | 2017-05-11 | 2025-03-24 | Vyluma Inc | Composición oftálmica líquida estable, que comprende una solución acuosa con un tampón, un agente de tonicidad, un quelante, un modificador de la viscosidad y atropina; y el uso de la misma para el tratamiento de la miopía. |
-
2017
- 2017-05-24 SG SG11201809822SA patent/SG11201809822SA/en unknown
- 2017-05-24 CN CN202311238651.XA patent/CN117205209A/zh active Pending
- 2017-05-24 UA UAA201812662A patent/UA126195C2/uk unknown
- 2017-05-24 TW TW110141612A patent/TWI849355B/zh active
- 2017-05-24 TW TW106117194A patent/TWI791438B/zh active
- 2017-05-24 ES ES17802848T patent/ES2929368T3/es active Active
- 2017-05-24 KR KR1020257014231A patent/KR20250067951A/ko active Pending
- 2017-05-24 KR KR1020187037233A patent/KR20190013877A/ko not_active Ceased
- 2017-05-24 JP JP2017102939A patent/JP6590860B2/ja active Active
- 2017-05-24 EA EA201892703A patent/EA201892703A1/ru unknown
- 2017-05-24 US US16/303,686 patent/US20210267885A1/en not_active Abandoned
- 2017-05-24 CA CA3023149A patent/CA3023149C/en active Active
- 2017-05-24 EP EP22189717.6A patent/EP4112055A1/en active Pending
- 2017-05-24 KR KR1020227039104A patent/KR102580933B1/ko active Active
- 2017-05-24 TW TW112102321A patent/TWI874894B/zh active
- 2017-05-24 WO PCT/JP2017/019423 patent/WO2017204262A1/en not_active Ceased
- 2017-05-24 CN CN202311240197.1A patent/CN117205210A/zh active Pending
- 2017-05-24 KR KR1020237031744A patent/KR102804061B1/ko active Active
- 2017-05-24 MY MYPI2018001914A patent/MY189774A/en unknown
- 2017-05-24 AR ARP170101418A patent/AR108591A1/es not_active Application Discontinuation
- 2017-05-24 CN CN201780031738.6A patent/CN109310687B/zh active Active
- 2017-05-24 EP EP17802848.6A patent/EP3463360B1/en active Active
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2018
- 2018-11-16 PH PH12018502421A patent/PH12018502421A1/en unknown
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2019
- 2019-09-17 JP JP2019168569A patent/JP6886502B2/ja active Active
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2021
- 2021-05-14 JP JP2021082578A patent/JP7224390B2/ja active Active
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2023
- 2023-02-07 JP JP2023016850A patent/JP2023058574A/ja not_active Withdrawn
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2024
- 2024-05-28 US US18/676,396 patent/US20240307305A1/en not_active Abandoned
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2025
- 2025-03-03 JP JP2025032538A patent/JP2025084921A/ja active Pending
- 2025-09-16 JP JP2025153045A patent/JP2025176149A/ja active Pending
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