KR20240136358A - 펙소페나딘을 함유하는 조성물 - Google Patents
펙소페나딘을 함유하는 조성물 Download PDFInfo
- Publication number
- KR20240136358A KR20240136358A KR1020247025570A KR20247025570A KR20240136358A KR 20240136358 A KR20240136358 A KR 20240136358A KR 1020247025570 A KR1020247025570 A KR 1020247025570A KR 20247025570 A KR20247025570 A KR 20247025570A KR 20240136358 A KR20240136358 A KR 20240136358A
- Authority
- KR
- South Korea
- Prior art keywords
- sodium
- diluent
- spray
- disintegrant
- dried formulation
- 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
- RWTNPBWLLIMQHL-UHFFFAOYSA-N fexofenadine Chemical compound C1=CC(C(C)(C(O)=O)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 RWTNPBWLLIMQHL-UHFFFAOYSA-N 0.000 title claims abstract description 137
- 229960003592 fexofenadine Drugs 0.000 title claims abstract description 132
- 238000009472 formulation Methods 0.000 claims abstract description 187
- 150000004683 dihydrates Chemical class 0.000 claims abstract description 107
- 238000000034 method Methods 0.000 claims abstract description 63
- 208000024891 symptom Diseases 0.000 claims abstract description 43
- 206010020751 Hypersensitivity Diseases 0.000 claims abstract description 35
- 230000007815 allergy Effects 0.000 claims abstract description 35
- 208000026935 allergic disease Diseases 0.000 claims abstract description 28
- 239000011159 matrix material Substances 0.000 claims abstract description 20
- 239000003085 diluting agent Substances 0.000 claims description 269
- 239000007884 disintegrant Substances 0.000 claims description 136
- 239000007921 spray Substances 0.000 claims description 127
- 239000000314 lubricant Substances 0.000 claims description 120
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims description 96
- 239000011230 binding agent Substances 0.000 claims description 90
- 235000003599 food sweetener Nutrition 0.000 claims description 80
- 239000003765 sweetening agent Substances 0.000 claims description 80
- 239000003795 chemical substances by application Substances 0.000 claims description 69
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 67
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 67
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims description 67
- 230000003113 alkalizing effect Effects 0.000 claims description 65
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical class [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims description 64
- 239000006172 buffering agent Substances 0.000 claims description 61
- BNIILDVGGAEEIG-UHFFFAOYSA-L disodium hydrogen phosphate Chemical group [Na+].[Na+].OP([O-])([O-])=O BNIILDVGGAEEIG-UHFFFAOYSA-L 0.000 claims description 59
- 239000008187 granular material Substances 0.000 claims description 55
- 239000003906 humectant Substances 0.000 claims description 49
- 229920002472 Starch Polymers 0.000 claims description 44
- 229940032147 starch Drugs 0.000 claims description 44
- 239000008107 starch Substances 0.000 claims description 44
- 235000019698 starch Nutrition 0.000 claims description 44
- 229910000397 disodium phosphate Inorganic materials 0.000 claims description 43
- 235000019800 disodium phosphate Nutrition 0.000 claims description 43
- 239000000796 flavoring agent Substances 0.000 claims description 43
- 235000013355 food flavoring agent Nutrition 0.000 claims description 43
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 41
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 41
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 41
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical group 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 41
- 229930006000 Sucrose Natural products 0.000 claims description 38
- 229960004793 sucrose Drugs 0.000 claims description 38
- 239000005720 sucrose Substances 0.000 claims description 38
- RRJFVPUCXDGFJB-UHFFFAOYSA-N Fexofenadine hydrochloride Chemical compound Cl.C1=CC(C(C)(C(O)=O)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 RRJFVPUCXDGFJB-UHFFFAOYSA-N 0.000 claims description 33
- 229960000354 fexofenadine hydrochloride Drugs 0.000 claims description 33
- 229910000019 calcium carbonate Inorganic materials 0.000 claims description 32
- 229920002678 cellulose Chemical class 0.000 claims description 32
- 239000001913 cellulose Chemical class 0.000 claims description 32
- 235000010980 cellulose Nutrition 0.000 claims description 32
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 32
- 239000004386 Erythritol Substances 0.000 claims description 31
- UNXHWFMMPAWVPI-UHFFFAOYSA-N Erythritol Natural products OCC(O)C(O)CO UNXHWFMMPAWVPI-UHFFFAOYSA-N 0.000 claims description 31
- 235000019414 erythritol Nutrition 0.000 claims description 31
- UNXHWFMMPAWVPI-ZXZARUISSA-N erythritol Chemical compound OC[C@H](O)[C@H](O)CO UNXHWFMMPAWVPI-ZXZARUISSA-N 0.000 claims description 31
- 229940009714 erythritol Drugs 0.000 claims description 31
- 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 description 30
- AJPJDKMHJJGVTQ-UHFFFAOYSA-M sodium dihydrogen phosphate Chemical compound [Na+].OP(O)([O-])=O AJPJDKMHJJGVTQ-UHFFFAOYSA-M 0.000 claims description 30
- ZPWVASYFFYYZEW-UHFFFAOYSA-L dipotassium hydrogen phosphate Chemical compound [K+].[K+].OP([O-])([O-])=O ZPWVASYFFYYZEW-UHFFFAOYSA-L 0.000 claims description 29
- 235000019797 dipotassium phosphate Nutrition 0.000 claims description 29
- 229910000396 dipotassium phosphate Inorganic materials 0.000 claims description 29
- 239000000080 wetting agent Substances 0.000 claims description 29
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims description 28
- OSGAYBCDTDRGGQ-UHFFFAOYSA-L calcium sulfate Chemical compound [Ca+2].[O-]S([O-])(=O)=O OSGAYBCDTDRGGQ-UHFFFAOYSA-L 0.000 claims description 28
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 claims description 28
- KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 claims description 27
- 239000008184 oral solid dosage form Substances 0.000 claims description 26
- 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 25
- 229930195725 Mannitol Natural products 0.000 claims description 25
- 235000010355 mannitol Nutrition 0.000 claims description 25
- 239000000594 mannitol Substances 0.000 claims description 25
- 229960001855 mannitol Drugs 0.000 claims description 25
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 24
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 24
- 239000002202 Polyethylene glycol Substances 0.000 claims description 24
- 229960000913 crospovidone Drugs 0.000 claims description 24
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 24
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 24
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 24
- 229920001223 polyethylene glycol Polymers 0.000 claims description 24
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims description 24
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims description 24
- 229920003109 sodium starch glycolate Polymers 0.000 claims description 24
- 239000008109 sodium starch glycolate Substances 0.000 claims description 24
- 229940079832 sodium starch glycolate Drugs 0.000 claims description 24
- 239000000872 buffer Substances 0.000 claims description 23
- 229920000881 Modified starch Polymers 0.000 claims description 22
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims description 22
- 229920000053 polysorbate 80 Polymers 0.000 claims description 22
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 21
- DMBUODUULYCPAK-UHFFFAOYSA-N 1,3-bis(docosanoyloxy)propan-2-yl docosanoate Chemical compound CCCCCCCCCCCCCCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCCCCCCCCCCCCCC)COC(=O)CCCCCCCCCCCCCCCCCCCCC DMBUODUULYCPAK-UHFFFAOYSA-N 0.000 claims description 20
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 claims description 20
- 239000004354 Hydroxyethyl cellulose Substances 0.000 claims description 20
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 claims description 20
- 229920001479 Hydroxyethyl methyl cellulose Polymers 0.000 claims description 20
- 235000010216 calcium carbonate Nutrition 0.000 claims description 20
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 claims description 20
- 229920001983 poloxamer Polymers 0.000 claims description 20
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 20
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims description 20
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 20
- 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 18
- 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 18
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Chemical class OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims description 18
- 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 description 18
- 239000005913 Maltodextrin Substances 0.000 claims description 18
- 229920002774 Maltodextrin Polymers 0.000 claims description 18
- 239000008103 glucose Chemical class 0.000 claims description 18
- 229960001031 glucose Drugs 0.000 claims description 18
- 239000000832 lactitol Chemical class 0.000 claims description 18
- 235000010448 lactitol Nutrition 0.000 claims description 18
- VQHSOMBJVWLPSR-JVCRWLNRSA-N lactitol Chemical class 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 description 18
- 229960003451 lactitol Drugs 0.000 claims description 18
- 239000000845 maltitol Substances 0.000 claims description 18
- 235000010449 maltitol Nutrition 0.000 claims description 18
- 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 description 18
- 229940035436 maltitol Drugs 0.000 claims description 18
- 229940035034 maltodextrin Drugs 0.000 claims description 18
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 claims description 18
- 229940068968 polysorbate 80 Drugs 0.000 claims description 18
- 239000000600 sorbitol Substances 0.000 claims description 18
- 229960002920 sorbitol Drugs 0.000 claims description 18
- -1 sterotex Chemical compound 0.000 claims description 18
- 239000013566 allergen Substances 0.000 claims description 16
- 229940071676 hydroxypropylcellulose Drugs 0.000 claims description 16
- 235000019359 magnesium stearate Nutrition 0.000 claims description 16
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 16
- 239000000725 suspension Substances 0.000 claims description 16
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 16
- 235000019658 bitter taste Nutrition 0.000 claims description 15
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims description 15
- SERLAGPUMNYUCK-DCUALPFSSA-N 1-O-alpha-D-glucopyranosyl-D-mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O SERLAGPUMNYUCK-DCUALPFSSA-N 0.000 claims description 14
- 229930091371 Fructose Chemical class 0.000 claims description 14
- 239000005715 Fructose Chemical class 0.000 claims description 14
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims description 14
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims description 14
- XAAHAAMILDNBPS-UHFFFAOYSA-L calcium hydrogenphosphate dihydrate Chemical compound O.O.[Ca+2].OP([O-])([O-])=O XAAHAAMILDNBPS-UHFFFAOYSA-L 0.000 claims description 14
- MKJXYGKVIBWPFZ-UHFFFAOYSA-L calcium lactate Chemical compound [Ca+2].CC(O)C([O-])=O.CC(O)C([O-])=O MKJXYGKVIBWPFZ-UHFFFAOYSA-L 0.000 claims description 14
- 239000001527 calcium lactate Substances 0.000 claims description 14
- 235000011086 calcium lactate Nutrition 0.000 claims description 14
- 229960002401 calcium lactate Drugs 0.000 claims description 14
- 239000001506 calcium phosphate Substances 0.000 claims description 14
- 229910000389 calcium phosphate Inorganic materials 0.000 claims description 14
- 235000011010 calcium phosphates Nutrition 0.000 claims description 14
- 235000019700 dicalcium phosphate Nutrition 0.000 claims description 14
- 229940095079 dicalcium phosphate anhydrous Drugs 0.000 claims description 14
- 229960002737 fructose Drugs 0.000 claims description 14
- 239000000905 isomalt Substances 0.000 claims description 14
- 235000010439 isomalt Nutrition 0.000 claims description 14
- HPIGCVXMBGOWTF-UHFFFAOYSA-N isomaltol Natural products CC(=O)C=1OC=CC=1O HPIGCVXMBGOWTF-UHFFFAOYSA-N 0.000 claims description 14
- 229960001375 lactose Drugs 0.000 claims description 14
- 239000008101 lactose Substances 0.000 claims description 14
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 claims description 14
- BBMHARZCALWXSL-UHFFFAOYSA-M sodium dihydrogenphosphate monohydrate Chemical compound O.[Na+].OP(O)([O-])=O BBMHARZCALWXSL-UHFFFAOYSA-M 0.000 claims description 14
- KDYFGRWQOYBRFD-UHFFFAOYSA-N succinic acid Chemical compound OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 claims description 14
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims description 14
- 235000019731 tricalcium phosphate Nutrition 0.000 claims description 14
- 239000000811 xylitol Substances 0.000 claims description 14
- 235000010447 xylitol Nutrition 0.000 claims description 14
- 229960002675 xylitol Drugs 0.000 claims description 14
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 claims description 14
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims description 13
- 229920000136 polysorbate Polymers 0.000 claims description 13
- 229920002134 Carboxymethyl cellulose Polymers 0.000 claims description 12
- 238000002360 preparation method Methods 0.000 claims description 12
- 239000000454 talc Substances 0.000 claims description 12
- 229910052623 talc Inorganic materials 0.000 claims description 12
- 235000012222 talc Nutrition 0.000 claims description 12
- 229920002785 Croscarmellose sodium Polymers 0.000 claims description 11
- 241001465754 Metazoa Species 0.000 claims description 11
- 239000004376 Sucralose Substances 0.000 claims description 11
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical group [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims description 11
- 229960001681 croscarmellose sodium Drugs 0.000 claims description 11
- 235000019408 sucralose Nutrition 0.000 claims description 11
- BAQAVOSOZGMPRM-QBMZZYIRSA-N sucralose Chemical group O[C@@H]1[C@@H](O)[C@@H](Cl)[C@@H](CO)O[C@@H]1O[C@@]1(CCl)[C@@H](O)[C@H](O)[C@@H](CCl)O1 BAQAVOSOZGMPRM-QBMZZYIRSA-N 0.000 claims description 11
- YTKBWWKAVMSYHE-OALUTQOASA-N (3s)-3-[3-(3-hydroxy-4-methoxyphenyl)propylamino]-4-[[(2s)-1-methoxy-1-oxo-3-phenylpropan-2-yl]amino]-4-oxobutanoic acid Chemical compound C([C@@H](C(=O)OC)NC(=O)[C@H](CC(O)=O)NCCCC=1C=C(O)C(OC)=CC=1)C1=CC=CC=C1 YTKBWWKAVMSYHE-OALUTQOASA-N 0.000 claims description 10
- WBZFUFAFFUEMEI-UHFFFAOYSA-M Acesulfame k Chemical compound [K+].CC1=CC(=O)[N-]S(=O)(=O)O1 WBZFUFAFFUEMEI-UHFFFAOYSA-M 0.000 claims description 10
- 239000004394 Advantame Substances 0.000 claims description 10
- 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 description 10
- 108010011485 Aspartame Proteins 0.000 claims description 10
- UDIPTWFVPPPURJ-UHFFFAOYSA-M Cyclamate Chemical compound [Na+].[O-]S(=O)(=O)NC1CCCCC1 UDIPTWFVPPPURJ-UHFFFAOYSA-M 0.000 claims description 10
- RFSUNEUAIZKAJO-ARQDHWQXSA-N Fructose Chemical class OC[C@H]1O[C@](O)(CO)[C@@H](O)[C@@H]1O RFSUNEUAIZKAJO-ARQDHWQXSA-N 0.000 claims description 10
- 108010093901 N-(N-(3-(3-hydroxy-4-methoxyphenyl) propyl)-alpha-aspartyl)-L-phenylalanine 1-methyl ester Proteins 0.000 claims description 10
- 239000004384 Neotame Substances 0.000 claims description 10
- 229920002675 Polyoxyl Polymers 0.000 claims description 10
- VMHLLURERBWHNL-UHFFFAOYSA-M Sodium acetate Chemical compound [Na+].CC([O-])=O VMHLLURERBWHNL-UHFFFAOYSA-M 0.000 claims description 10
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims description 10
- BCKXLBQYZLBQEK-KVVVOXFISA-M Sodium oleate Chemical compound [Na+].CCCCCCCC\C=C/CCCCCCCC([O-])=O BCKXLBQYZLBQEK-KVVVOXFISA-M 0.000 claims description 10
- 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 description 10
- 235000021355 Stearic acid Nutrition 0.000 claims description 10
- 239000004383 Steviol glycoside Substances 0.000 claims description 10
- XZAGBDSOKNXTDT-UHFFFAOYSA-N Sucrose monopalmitate Chemical compound CCCCCCCCCCCCCCCC(O)=O.OC1C(O)C(CO)OC1(CO)OC1C(O)C(O)C(O)C(CO)O1 XZAGBDSOKNXTDT-UHFFFAOYSA-N 0.000 claims description 10
- 235000010358 acesulfame potassium Nutrition 0.000 claims description 10
- 229960004998 acesulfame potassium Drugs 0.000 claims description 10
- 239000000619 acesulfame-K Substances 0.000 claims description 10
- 235000019453 advantame Nutrition 0.000 claims description 10
- 239000000605 aspartame Substances 0.000 claims description 10
- 235000010357 aspartame Nutrition 0.000 claims description 10
- IAOZJIPTCAWIRG-QWRGUYRKSA-N aspartame Chemical compound OC(=O)C[C@H](N)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 IAOZJIPTCAWIRG-QWRGUYRKSA-N 0.000 claims description 10
- 229960003438 aspartame Drugs 0.000 claims description 10
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical class OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims description 10
- 229960003563 calcium carbonate Drugs 0.000 claims description 10
- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 claims description 10
- 239000008116 calcium stearate Substances 0.000 claims description 10
- 235000013539 calcium stearate Nutrition 0.000 claims description 10
- 235000011132 calcium sulphate Nutrition 0.000 claims description 10
- 239000004359 castor oil Substances 0.000 claims description 10
- 235000019438 castor oil Nutrition 0.000 claims description 10
- 239000000625 cyclamic acid and its Na and Ca salt Substances 0.000 claims description 10
- MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical compound CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 0.000 claims description 10
- 235000001727 glucose Nutrition 0.000 claims description 10
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 claims description 10
- 229940075507 glyceryl monostearate Drugs 0.000 claims description 10
- 229940037627 magnesium lauryl sulfate Drugs 0.000 claims description 10
- HBNDBUATLJAUQM-UHFFFAOYSA-L magnesium;dodecyl sulfate Chemical compound [Mg+2].CCCCCCCCCCCCOS([O-])(=O)=O.CCCCCCCCCCCCOS([O-])(=O)=O HBNDBUATLJAUQM-UHFFFAOYSA-L 0.000 claims description 10
- 239000001788 mono and diglycerides of fatty acids Substances 0.000 claims description 10
- 235000019412 neotame Nutrition 0.000 claims description 10
- HLIAVLHNDJUHFG-HOTGVXAUSA-N neotame Chemical compound CC(C)(C)CCN[C@@H](CC(O)=O)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 HLIAVLHNDJUHFG-HOTGVXAUSA-N 0.000 claims description 10
- 108010070257 neotame Proteins 0.000 claims description 10
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims description 10
- 150000003013 phosphoric acid derivatives Chemical class 0.000 claims description 10
- 229960000502 poloxamer Drugs 0.000 claims description 10
- 229920001992 poloxamer 407 Polymers 0.000 claims description 10
- 229940044476 poloxamer 407 Drugs 0.000 claims description 10
- CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical compound C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 claims description 10
- 235000019204 saccharin Nutrition 0.000 claims description 10
- 229940081974 saccharin Drugs 0.000 claims description 10
- 239000000901 saccharin and its Na,K and Ca salt Substances 0.000 claims description 10
- 239000001632 sodium acetate Substances 0.000 claims description 10
- 235000017281 sodium acetate Nutrition 0.000 claims description 10
- WXMKPNITSTVMEF-UHFFFAOYSA-M sodium benzoate Chemical compound [Na+].[O-]C(=O)C1=CC=CC=C1 WXMKPNITSTVMEF-UHFFFAOYSA-M 0.000 claims description 10
- 239000004299 sodium benzoate Substances 0.000 claims description 10
- 235000010234 sodium benzoate Nutrition 0.000 claims description 10
- 229960001462 sodium cyclamate Drugs 0.000 claims description 10
- 235000019333 sodium laurylsulphate Nutrition 0.000 claims description 10
- 229940045902 sodium stearyl fumarate Drugs 0.000 claims description 10
- 235000011076 sorbitan monostearate Nutrition 0.000 claims description 10
- 239000001587 sorbitan monostearate Substances 0.000 claims description 10
- 229940035048 sorbitan monostearate Drugs 0.000 claims description 10
- 239000008117 stearic acid Substances 0.000 claims description 10
- 235000019411 steviol glycoside Nutrition 0.000 claims description 10
- 229930182488 steviol glycoside Natural products 0.000 claims description 10
- 150000008144 steviol glycosides Chemical class 0.000 claims description 10
- 235000019202 steviosides Nutrition 0.000 claims description 10
- 150000003445 sucroses Chemical class 0.000 claims description 10
- XOOUIPVCVHRTMJ-UHFFFAOYSA-L zinc stearate Chemical compound [Zn+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O XOOUIPVCVHRTMJ-UHFFFAOYSA-L 0.000 claims description 10
- ILRKKHJEINIICQ-OOFFSTKBSA-N Monoammonium glycyrrhizinate Chemical compound N.O([C@@H]1[C@@H](O)[C@H](O)[C@H](O[C@@H]1O[C@H]1CC[C@]2(C)[C@H]3C(=O)C=C4[C@@H]5C[C@](C)(CC[C@@]5(CC[C@@]4(C)[C@]3(C)CC[C@H]2C1(C)C)C)C(O)=O)C(O)=O)[C@@H]1O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]1O ILRKKHJEINIICQ-OOFFSTKBSA-N 0.000 claims description 9
- RQPZNWPYLFFXCP-UHFFFAOYSA-L barium dihydroxide Chemical compound [OH-].[OH-].[Ba+2] RQPZNWPYLFFXCP-UHFFFAOYSA-L 0.000 claims description 9
- 229910001863 barium hydroxide Inorganic materials 0.000 claims description 9
- AXCZMVOFGPJBDE-UHFFFAOYSA-L calcium dihydroxide Chemical compound [OH-].[OH-].[Ca+2] AXCZMVOFGPJBDE-UHFFFAOYSA-L 0.000 claims description 9
- 239000000920 calcium hydroxide Substances 0.000 claims description 9
- 229910001861 calcium hydroxide Inorganic materials 0.000 claims description 9
- 239000001685 glycyrrhizic acid Substances 0.000 claims description 9
- 229940057948 magnesium stearate Drugs 0.000 claims description 9
- AYGJDUHQRFKLBG-UHFFFAOYSA-M sodium;1,1-dioxo-1,2-benzothiazol-3-olate;dihydrate Chemical compound O.O.[Na+].C1=CC=C2C(=O)[N-]S(=O)(=O)C2=C1 AYGJDUHQRFKLBG-UHFFFAOYSA-M 0.000 claims description 9
- 229910019142 PO4 Inorganic materials 0.000 claims description 8
- 229920002511 Poloxamer 237 Polymers 0.000 claims description 8
- 229920002517 Poloxamer 338 Polymers 0.000 claims description 8
- 235000021317 phosphate Nutrition 0.000 claims description 8
- 229920001993 poloxamer 188 Polymers 0.000 claims description 8
- 229940044519 poloxamer 188 Drugs 0.000 claims description 8
- 238000001694 spray drying Methods 0.000 claims description 8
- OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 claims description 7
- 239000007910 chewable tablet Substances 0.000 claims description 7
- 229940069078 citric acid / sodium citrate Drugs 0.000 claims description 7
- 239000001530 fumaric acid Substances 0.000 claims description 7
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 claims description 7
- 239000011976 maleic acid Substances 0.000 claims description 7
- 229950008882 polysorbate Drugs 0.000 claims description 7
- 239000001508 potassium citrate Substances 0.000 claims description 7
- 229960002635 potassium citrate Drugs 0.000 claims description 7
- 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 7
- 235000011082 potassium citrates Nutrition 0.000 claims description 7
- 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 7
- 239000002904 solvent Substances 0.000 claims description 7
- 229960004274 stearic acid Drugs 0.000 claims description 7
- 239000001384 succinic acid Substances 0.000 claims description 7
- 239000008118 PEG 6000 Substances 0.000 claims description 6
- 229920002584 Polyethylene Glycol 6000 Polymers 0.000 claims description 6
- 210000002345 respiratory system Anatomy 0.000 claims description 6
- 229940068682 chewable tablet Drugs 0.000 claims description 5
- 239000003826 tablet Substances 0.000 claims description 5
- 241000238876 Acari Species 0.000 claims description 4
- 208000035285 Allergic Seasonal Rhinitis Diseases 0.000 claims description 4
- 206010013911 Dysgeusia Diseases 0.000 claims description 4
- 239000005434 MCC/mannitol excipient Substances 0.000 claims description 4
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 claims description 4
- BPQQTUXANYXVAA-UHFFFAOYSA-N Orthosilicate Chemical compound [O-][Si]([O-])([O-])[O-] BPQQTUXANYXVAA-UHFFFAOYSA-N 0.000 claims description 4
- 239000011247 coating layer Substances 0.000 claims description 4
- 239000000428 dust Substances 0.000 claims description 4
- 239000011777 magnesium Substances 0.000 claims description 4
- 229910052749 magnesium Inorganic materials 0.000 claims description 4
- 230000000873 masking effect Effects 0.000 claims description 4
- 239000006191 orally-disintegrating tablet Substances 0.000 claims description 4
- 229940093429 polyethylene glycol 6000 Drugs 0.000 claims description 4
- 241000196324 Embryophyta Species 0.000 claims description 3
- 239000000391 magnesium silicate Substances 0.000 claims description 3
- 229910052919 magnesium silicate Inorganic materials 0.000 claims description 3
- 235000019792 magnesium silicate Nutrition 0.000 claims description 3
- 229920000642 polymer Polymers 0.000 claims description 3
- 210000003296 saliva Anatomy 0.000 claims description 3
- 239000007909 solid dosage form Substances 0.000 claims description 3
- 210000002700 urine Anatomy 0.000 claims description 3
- 241000209504 Poaceae Species 0.000 claims description 2
- 239000008297 liquid dosage form Substances 0.000 claims description 2
- HCWCAKKEBCNQJP-UHFFFAOYSA-N magnesium orthosilicate Chemical compound [Mg+2].[Mg+2].[O-][Si]([O-])([O-])[O-] HCWCAKKEBCNQJP-UHFFFAOYSA-N 0.000 claims 1
- 239000006186 oral dosage form Substances 0.000 abstract description 9
- 239000007787 solid Substances 0.000 abstract description 6
- 238000004519 manufacturing process Methods 0.000 abstract description 3
- 125000000185 sucrose group Chemical group 0.000 description 12
- 239000000047 product Substances 0.000 description 11
- 235000010486 polyoxyethylene sorbitan monolaurate Nutrition 0.000 description 9
- 229920001213 Polysorbate 20 Polymers 0.000 description 8
- 229920001219 Polysorbate 40 Polymers 0.000 description 8
- 229920001214 Polysorbate 60 Polymers 0.000 description 8
- 230000003247 decreasing effect Effects 0.000 description 8
- 125000002791 glucosyl group Chemical group C1([C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO)* 0.000 description 8
- 208000003251 Pruritus Diseases 0.000 description 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 7
- 239000002552 dosage form Substances 0.000 description 7
- 206010011224 Cough Diseases 0.000 description 6
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 6
- 208000036071 Rhinorrhea Diseases 0.000 description 5
- 206010039101 Rhinorrhoea Diseases 0.000 description 5
- 206010043521 Throat irritation Diseases 0.000 description 5
- 238000000113 differential scanning calorimetry Methods 0.000 description 5
- 239000002245 particle Substances 0.000 description 5
- 229940068965 polysorbates Drugs 0.000 description 5
- 206010041232 sneezing Diseases 0.000 description 5
- 229920002690 Polyoxyl 40 HydrogenatedCastorOil Polymers 0.000 description 4
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 4
- 208000027418 Wounds and injury Diseases 0.000 description 4
- 229940008201 allegra Drugs 0.000 description 4
- HZVVJJIYJKGMFL-UHFFFAOYSA-N almasilate Chemical compound O.[Mg+2].[Al+3].[Al+3].O[Si](O)=O.O[Si](O)=O HZVVJJIYJKGMFL-UHFFFAOYSA-N 0.000 description 4
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 4
- 239000001768 carboxy methyl cellulose Substances 0.000 description 4
- 239000008112 carboxymethyl-cellulose Substances 0.000 description 4
- JAUGGEIKQIHSMF-UHFFFAOYSA-N dialuminum;dimagnesium;dioxido(oxo)silane;oxygen(2-);hydrate Chemical compound O.[O-2].[O-2].[Mg+2].[Mg+2].[Al+3].[Al+3].[O-][Si]([O-])=O.[O-][Si]([O-])=O.[O-][Si]([O-])=O JAUGGEIKQIHSMF-UHFFFAOYSA-N 0.000 description 4
- 238000001938 differential scanning calorimetry curve Methods 0.000 description 4
- 201000010099 disease Diseases 0.000 description 4
- DGLRDKLJZLEJCY-UHFFFAOYSA-L disodium hydrogenphosphate dodecahydrate Chemical compound O.O.O.O.O.O.O.O.O.O.O.O.[Na+].[Na+].OP([O-])([O-])=O DGLRDKLJZLEJCY-UHFFFAOYSA-L 0.000 description 4
- 239000008298 dragée Substances 0.000 description 4
- BJHIKXHVCXFQLS-UYFOZJQFSA-N fructose group Chemical group OCC(=O)[C@@H](O)[C@H](O)[C@H](O)CO BJHIKXHVCXFQLS-UYFOZJQFSA-N 0.000 description 4
- 239000000463 material Substances 0.000 description 4
- 229940045641 monobasic sodium phosphate Drugs 0.000 description 4
- 229910000403 monosodium phosphate Inorganic materials 0.000 description 4
- 235000019799 monosodium phosphate Nutrition 0.000 description 4
- 239000000825 pharmaceutical preparation Substances 0.000 description 4
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 4
- 239000010452 phosphate Substances 0.000 description 4
- 239000000256 polyoxyethylene sorbitan monolaurate Substances 0.000 description 4
- 235000010483 polyoxyethylene sorbitan monopalmitate Nutrition 0.000 description 4
- 239000000249 polyoxyethylene sorbitan monopalmitate Substances 0.000 description 4
- 235000010989 polyoxyethylene sorbitan monostearate Nutrition 0.000 description 4
- 239000001818 polyoxyethylene sorbitan monostearate Substances 0.000 description 4
- 229940068977 polysorbate 20 Drugs 0.000 description 4
- 229940101027 polysorbate 40 Drugs 0.000 description 4
- 229940113124 polysorbate 60 Drugs 0.000 description 4
- 235000019600 saltiness Nutrition 0.000 description 4
- 235000019640 taste Nutrition 0.000 description 4
- 206010008469 Chest discomfort Diseases 0.000 description 3
- 206010013786 Dry skin Diseases 0.000 description 3
- 208000000059 Dyspnea Diseases 0.000 description 3
- 206010013975 Dyspnoeas Diseases 0.000 description 3
- 208000010201 Exanthema Diseases 0.000 description 3
- 206010052140 Eye pruritus Diseases 0.000 description 3
- 206010016059 Facial pain Diseases 0.000 description 3
- 206010028735 Nasal congestion Diseases 0.000 description 3
- 208000037656 Respiratory Sounds Diseases 0.000 description 3
- 206010040744 Sinus headache Diseases 0.000 description 3
- 206010070488 Upper-airway cough syndrome Diseases 0.000 description 3
- 208000024780 Urticaria Diseases 0.000 description 3
- 206010047924 Wheezing Diseases 0.000 description 3
- DGVMNQYBHPSIJS-UHFFFAOYSA-N dimagnesium;2,2,6,6-tetraoxido-1,3,5,7-tetraoxa-2,4,6-trisilaspiro[3.3]heptane;hydrate Chemical group O.[Mg+2].[Mg+2].O1[Si]([O-])([O-])O[Si]21O[Si]([O-])([O-])O2 DGVMNQYBHPSIJS-UHFFFAOYSA-N 0.000 description 3
- 208000035475 disorder Diseases 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- 239000003814 drug Substances 0.000 description 3
- 229940126534 drug product Drugs 0.000 description 3
- 230000037336 dry skin Effects 0.000 description 3
- 238000001035 drying Methods 0.000 description 3
- 201000005884 exanthem Diseases 0.000 description 3
- 239000012467 final product Substances 0.000 description 3
- 239000004615 ingredient Substances 0.000 description 3
- 206010037844 rash Diseases 0.000 description 3
- 230000008786 sensory perception of smell Effects 0.000 description 3
- 230000014860 sensory perception of taste Effects 0.000 description 3
- 208000013220 shortness of breath Diseases 0.000 description 3
- 239000011780 sodium chloride Substances 0.000 description 3
- 238000005507 spraying Methods 0.000 description 3
- 239000000126 substance Substances 0.000 description 3
- 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 description 2
- LOUPRKONTZGTKE-WZBLMQSHSA-N Quinine Chemical compound C([C@H]([C@H](C1)C=C)C2)C[N@@]1[C@@H]2[C@H](O)C1=CC=NC2=CC=C(OC)C=C21 LOUPRKONTZGTKE-WZBLMQSHSA-N 0.000 description 2
- 238000010521 absorption reaction Methods 0.000 description 2
- 235000015111 chews Nutrition 0.000 description 2
- 229940061607 dibasic sodium phosphate Drugs 0.000 description 2
- 238000005469 granulation Methods 0.000 description 2
- 230000003179 granulation Effects 0.000 description 2
- 208000014674 injury Diseases 0.000 description 2
- 230000007803 itching Effects 0.000 description 2
- ZADYMNAVLSWLEQ-UHFFFAOYSA-N magnesium;oxygen(2-);silicon(4+) Chemical compound [O-2].[O-2].[O-2].[Mg+2].[Si+4] ZADYMNAVLSWLEQ-UHFFFAOYSA-N 0.000 description 2
- 238000002483 medication Methods 0.000 description 2
- 238000002844 melting Methods 0.000 description 2
- 230000008018 melting Effects 0.000 description 2
- 230000001953 sensory effect Effects 0.000 description 2
- 239000000377 silicon dioxide Substances 0.000 description 2
- 235000012239 silicon dioxide Nutrition 0.000 description 2
- 239000011734 sodium Substances 0.000 description 2
- 229910052708 sodium Inorganic materials 0.000 description 2
- 230000000087 stabilizing effect Effects 0.000 description 2
- 239000008223 sterile water Substances 0.000 description 2
- 210000001779 taste bud Anatomy 0.000 description 2
- 230000008733 trauma Effects 0.000 description 2
- 229940085254 wal-fex Drugs 0.000 description 2
- FTLYMKDSHNWQKD-UHFFFAOYSA-N (2,4,5-trichlorophenyl)boronic acid Chemical compound OB(O)C1=CC(Cl)=C(Cl)C=C1Cl FTLYMKDSHNWQKD-UHFFFAOYSA-N 0.000 description 1
- 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 description 1
- 239000001096 (4-ethenyl-1-azabicyclo[2.2.2]octan-7-yl)-(6-methoxyquinolin-4-yl)methanol hydrochloride Substances 0.000 description 1
- MPQKYZPYCSTMEI-FLZPLBAKSA-N (r)-[(2s,4s,5r)-5-ethenyl-1-azabicyclo[2.2.2]octan-2-yl]-(6-methoxyquinolin-4-yl)methanol;dihydrate;hydrochloride Chemical compound O.O.Cl.C([C@H]([C@H](C1)C=C)C2)CN1[C@@H]2[C@H](O)C1=CC=NC2=CC=C(OC)C=C21 MPQKYZPYCSTMEI-FLZPLBAKSA-N 0.000 description 1
- 244000025254 Cannabis sativa Species 0.000 description 1
- 235000001258 Cinchona calisaya Nutrition 0.000 description 1
- HSRJKNPTNIJEKV-UHFFFAOYSA-N Guaifenesin Chemical compound COC1=CC=CC=C1OCC(O)CO HSRJKNPTNIJEKV-UHFFFAOYSA-N 0.000 description 1
- 241000167880 Hirundinidae Species 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 229920002538 Polyethylene Glycol 20000 Polymers 0.000 description 1
- 229920002594 Polyethylene Glycol 8000 Polymers 0.000 description 1
- 206010062519 Poor quality sleep Diseases 0.000 description 1
- 235000009754 Vitis X bourquina Nutrition 0.000 description 1
- 235000012333 Vitis X labruscana Nutrition 0.000 description 1
- 240000006365 Vitis vinifera Species 0.000 description 1
- 235000014787 Vitis vinifera Nutrition 0.000 description 1
- 238000005054 agglomeration Methods 0.000 description 1
- 230000002776 aggregation Effects 0.000 description 1
- 238000004458 analytical method Methods 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 238000012512 characterization method Methods 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 239000003153 chemical reaction reagent Substances 0.000 description 1
- 230000001055 chewing effect Effects 0.000 description 1
- LOUPRKONTZGTKE-UHFFFAOYSA-N cinchonine Natural products C1C(C(C2)C=C)CCN2C1C(O)C1=CC=NC2=CC=C(OC)C=C21 LOUPRKONTZGTKE-UHFFFAOYSA-N 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 230000007423 decrease Effects 0.000 description 1
- 235000014113 dietary fatty acids Nutrition 0.000 description 1
- 239000000194 fatty acid Substances 0.000 description 1
- 229930195729 fatty acid Natural products 0.000 description 1
- 150000004665 fatty acids Chemical class 0.000 description 1
- 239000013020 final formulation Substances 0.000 description 1
- 230000002209 hydrophobic effect Effects 0.000 description 1
- 238000011065 in-situ storage Methods 0.000 description 1
- 238000010348 incorporation Methods 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 244000144972 livestock Species 0.000 description 1
- 239000008368 mint flavor Substances 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 229940054194 mucinex Drugs 0.000 description 1
- 229940127557 pharmaceutical product Drugs 0.000 description 1
- 239000008363 phosphate buffer Substances 0.000 description 1
- 229920001451 polypropylene glycol Polymers 0.000 description 1
- 229960000948 quinine Drugs 0.000 description 1
- 229960001811 quinine hydrochloride Drugs 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 229940085605 saccharin sodium Drugs 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 230000003860 sleep quality Effects 0.000 description 1
- 229940075562 sodium phosphate dihydrate Drugs 0.000 description 1
- 229940071117 starch glycolate Drugs 0.000 description 1
- 239000013589 supplement Substances 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 238000001757 thermogravimetry curve Methods 0.000 description 1
- 229920000428 triblock copolymer Polymers 0.000 description 1
- 230000001960 triggered effect Effects 0.000 description 1
- CRKADHVTAQCXRA-UHFFFAOYSA-K trisodium;phosphate;dihydrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]P([O-])([O-])=O CRKADHVTAQCXRA-UHFFFAOYSA-K 0.000 description 1
- YNIRKEZIDLCCMC-UHFFFAOYSA-K trisodium;phosphate;hydrate Chemical group [OH-].[Na+].[Na+].[Na+].OP([O-])([O-])=O YNIRKEZIDLCCMC-UHFFFAOYSA-K 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1611—Inorganic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
- A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1641—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1682—Processes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1682—Processes
- A61K9/1694—Processes resulting in granules or microspheres of the matrix type containing more than 5% of excipient
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Inorganic Chemistry (AREA)
- Pulmonology (AREA)
- Immunology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Dispersion Chemistry (AREA)
- Zoology (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/IB2021/000916 WO2023126637A1 (en) | 2021-12-29 | 2021-12-29 | Compositions containing fexofenadine |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20240136358A true KR20240136358A (ko) | 2024-09-13 |
Family
ID=80122351
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020247025570A Pending KR20240136358A (ko) | 2021-12-29 | 2021-12-29 | 펙소페나딘을 함유하는 조성물 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US20250082623A1 (https=) |
| EP (1) | EP4456880B1 (https=) |
| JP (1) | JP7826492B2 (https=) |
| KR (1) | KR20240136358A (https=) |
| CN (1) | CN118715004A (https=) |
| AR (1) | AR128113A1 (https=) |
| AU (1) | AU2021480621A1 (https=) |
| CA (1) | CA3242293A1 (https=) |
| CO (1) | CO2024009774A2 (https=) |
| MX (1) | MX2024008242A (https=) |
| PE (1) | PE20242355A1 (https=) |
| WO (1) | WO2023126637A1 (https=) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2026074306A1 (en) | 2024-10-03 | 2026-04-09 | Opella Healthcare Group Sas | Chewable fexofenadine tablets |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6723348B2 (en) * | 2001-11-16 | 2004-04-20 | Ethypharm | Orodispersible tablets containing fexofenadine |
| DOP2006000274A (es) * | 2005-12-14 | 2007-10-15 | Sanofi Aventis Us Llc | Formulación de suspensión de fexofenadina |
| CN102958515A (zh) * | 2009-12-02 | 2013-03-06 | 阿普塔利斯制药有限公司 | 非索非那定微胶囊及含有非索非那定微胶囊的组合物 |
| FR2959130A1 (fr) * | 2010-04-21 | 2011-10-28 | Sanofi Aventis | Procede de preparation de compositions pharmaceutiques destinees a l'administration par voie orale comprenant un ou plusieurs principes actifs et les compositions les comprenant. |
| CN102512389B (zh) * | 2011-12-27 | 2013-08-21 | 天津市嵩锐医药科技有限公司 | 非索非那定盐酸盐口腔崩解药物组合物 |
| KR101761983B1 (ko) * | 2014-08-25 | 2017-08-07 | 아주대학교산학협력단 | 구강내 속붕해 필름 조성물 및 그 제조방법 |
| CN105997910A (zh) * | 2016-06-09 | 2016-10-12 | 北京化工大学 | 一种掩味制剂及其制备方法 |
-
2021
- 2021-12-29 KR KR1020247025570A patent/KR20240136358A/ko active Pending
- 2021-12-29 PE PE2024001517A patent/PE20242355A1/es unknown
- 2021-12-29 CN CN202180105441.6A patent/CN118715004A/zh active Pending
- 2021-12-29 CA CA3242293A patent/CA3242293A1/en active Pending
- 2021-12-29 AU AU2021480621A patent/AU2021480621A1/en active Pending
- 2021-12-29 MX MX2024008242A patent/MX2024008242A/es unknown
- 2021-12-29 EP EP21851701.9A patent/EP4456880B1/en active Active
- 2021-12-29 JP JP2024539614A patent/JP7826492B2/ja active Active
- 2021-12-29 US US18/725,446 patent/US20250082623A1/en active Pending
- 2021-12-29 WO PCT/IB2021/000916 patent/WO2023126637A1/en not_active Ceased
-
2022
- 2022-12-27 AR ARP220103594A patent/AR128113A1/es unknown
-
2024
- 2024-07-23 CO CONC2024/0009774A patent/CO2024009774A2/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA3242293A1 (en) | 2023-07-06 |
| JP7826492B2 (ja) | 2026-03-09 |
| EP4456880B1 (en) | 2026-03-18 |
| AU2021480621A1 (en) | 2024-07-18 |
| CN118715004A (zh) | 2024-09-27 |
| WO2023126637A1 (en) | 2023-07-06 |
| PE20242355A1 (es) | 2024-12-16 |
| MX2024008242A (es) | 2024-07-19 |
| CO2024009774A2 (es) | 2024-08-08 |
| US20250082623A1 (en) | 2025-03-13 |
| AR128113A1 (es) | 2024-03-27 |
| EP4456880A1 (en) | 2024-11-06 |
| JP2024546513A (ja) | 2024-12-24 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US8048449B2 (en) | Mouth dissolving pharmaceutical composition and process for preparing the same | |
| JP4740740B2 (ja) | 薬物含有粒子および該粒子を含む固形製剤 | |
| TWI398273B (zh) | 用於抑制酸分泌之醫藥調配物及其製備及使用之方法 | |
| JP6054940B2 (ja) | １−（３−（２−（１−ベンゾチオフェン−５−イル）エトキシ）プロピル）アゼチジン−３−オールまたはその塩を含有する固形医薬組成物 | |
| CN103547265B (zh) | 口腔内速崩片 | |
| EP3013323A2 (en) | Complex granule formulation having improved stability comprising levocetirizine and montelukast | |
| EP2563340A2 (en) | Water soluble pharmaceutical composition | |
| JP2010270110A (ja) | ネオテームを含有する経口製剤 | |
| JP7826492B2 (ja) | フェキソフェナジン含有組成物 | |
| EP2566449B1 (en) | Pharmaceutical compositions comprising ceftibuten | |
| KR20050035907A (ko) | 암로디핀 유리염기를 함유한 구강 속붕해정 및 그의 조성물 | |
| KR100957731B1 (ko) | 쓴맛이 저감된 프란루카스트 수화물을 함유하는 제제 | |
| JP3899522B2 (ja) | 苦味が低減されたプランルカスト水和物を含有する製剤 | |
| HK40111138A (zh) | 含有非索非那定的组合物 | |
| TWI383809B (zh) | 含有西洛他唑（ｃｉｌｏｓｔａｚｏｌ）之口腔崩解粉末 | |
| EP3505164A1 (en) | An effervescent composition comprising erdosteine | |
| JP2024546513A5 (https=) | ||
| WO2021061066A1 (en) | Effervescent formulations of sapropterin dihydrochloride | |
| WO2019197939A1 (en) | Taste masked mouth dissolving formulation of montelukast sodium and levocetirizine hydrochloride | |
| JP2008094751A (ja) | プランルカスト水和物含有医薬組成物 | |
| WO2026074306A1 (en) | Chewable fexofenadine tablets | |
| JP2010053048A (ja) | 苦味が緩和されたイルベサルタン含有医薬組成物 | |
| KR20160012921A (ko) | 블로난세린을 포함하는 구강 속붕해성 제제 | |
| WO2021123341A1 (en) | Composition comprising diosmin | |
| HK40117367A (zh) | 屈他维林口腔崩解适口制剂及其制备方法 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PA0105 | International application |
Patent event date: 20240729 Patent event code: PA01051R01D Comment text: International Patent Application |
|
| PG1501 | Laying open of application | ||
| A201 | Request for examination | ||
| PA0201 | Request for examination |
Patent event code: PA02012R01D Patent event date: 20241217 Comment text: Request for Examination of Application |