CN103211779B - 包含弱碱性选择性5-羟色胺5-ht3阻断剂和有机酸的药物递送系统 - Google Patents
包含弱碱性选择性5-羟色胺5-ht3阻断剂和有机酸的药物递送系统 Download PDFInfo
- Publication number
- CN103211779B CN103211779B CN201310113926.7A CN201310113926A CN103211779B CN 103211779 B CN103211779 B CN 103211779B CN 201310113926 A CN201310113926 A CN 201310113926A CN 103211779 B CN103211779 B CN 103211779B
- Authority
- CN
- China
- Prior art keywords
- pearl
- coating
- organic acid
- acid
- dosage form
- 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.)
- Expired - Fee Related
Links
- 239000003814 drug Substances 0.000 title claims abstract description 175
- 150000007524 organic acids Chemical class 0.000 title claims abstract description 117
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 title claims abstract description 112
- 238000012377 drug delivery Methods 0.000 title description 10
- 238000000576 coating method Methods 0.000 claims abstract description 230
- 238000013268 sustained release Methods 0.000 claims abstract description 164
- 239000012730 sustained-release form Substances 0.000 claims abstract description 164
- 229940079593 drug Drugs 0.000 claims abstract description 88
- 239000002552 dosage form Substances 0.000 claims abstract description 80
- 238000000034 method Methods 0.000 claims abstract description 47
- 239000006191 orally-disintegrating tablet Substances 0.000 claims abstract description 37
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims abstract description 23
- 239000008187 granular material Substances 0.000 claims abstract description 21
- 230000000968 intestinal effect Effects 0.000 claims abstract description 12
- 238000013270 controlled release Methods 0.000 claims abstract description 11
- 150000001875 compounds Chemical group 0.000 claims abstract description 7
- 230000008569 process Effects 0.000 claims abstract description 7
- 239000000654 additive Substances 0.000 claims abstract description 6
- 230000000996 additive effect Effects 0.000 claims abstract description 6
- 238000003860 storage Methods 0.000 claims abstract description 3
- 239000011248 coating agent Substances 0.000 claims description 217
- 229920000642 polymer Polymers 0.000 claims description 112
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims description 100
- 239000002245 particle Substances 0.000 claims description 58
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims description 48
- 239000000203 mixture Substances 0.000 claims description 45
- 239000001530 fumaric acid Substances 0.000 claims description 44
- 238000009826 distribution Methods 0.000 claims description 35
- 229960005343 ondansetron Drugs 0.000 claims description 31
- 239000013078 crystal Substances 0.000 claims description 28
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 27
- 239000004531 microgranule Substances 0.000 claims description 21
- FELGMEQIXOGIFQ-CYBMUJFWSA-N (3r)-9-methyl-3-[(2-methylimidazol-1-yl)methyl]-2,3-dihydro-1h-carbazol-4-one Chemical compound CC1=NC=CN1C[C@@H]1C(=O)C(C=2C(=CC=CC=2)N2C)=C2CC1 FELGMEQIXOGIFQ-CYBMUJFWSA-N 0.000 claims description 20
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 20
- 239000007771 core particle Substances 0.000 claims description 19
- 239000007787 solid Substances 0.000 claims description 19
- 238000002360 preparation method Methods 0.000 claims description 17
- 150000003839 salts Chemical class 0.000 claims description 16
- 238000012360 testing method Methods 0.000 claims description 16
- 239000002904 solvent Substances 0.000 claims description 15
- 239000003795 chemical substances by application Substances 0.000 claims description 14
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 claims description 12
- 230000008859 change Effects 0.000 claims description 12
- 210000000214 mouth Anatomy 0.000 claims description 11
- 239000000872 buffer Substances 0.000 claims description 10
- 238000004090 dissolution Methods 0.000 claims description 10
- 239000003085 diluting agent Substances 0.000 claims description 9
- 239000000945 filler Substances 0.000 claims description 9
- 150000005846 sugar alcohols Chemical class 0.000 claims description 9
- 239000000853 adhesive Substances 0.000 claims description 8
- 230000001070 adhesive effect Effects 0.000 claims description 8
- 210000003296 saliva Anatomy 0.000 claims description 8
- 239000012738 dissolution medium Substances 0.000 claims description 6
- 239000011148 porous material Substances 0.000 claims description 6
- 238000005096 rolling process Methods 0.000 claims description 6
- KDYFGRWQOYBRFD-UHFFFAOYSA-N Succinic acid Natural products OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 claims description 5
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 claims description 4
- OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 claims description 4
- 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 description 4
- 235000003704 aspartic acid Nutrition 0.000 claims description 4
- 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 4
- KDYFGRWQOYBRFD-NUQCWPJISA-N butanedioic acid Chemical compound O[14C](=O)CC[14C](O)=O KDYFGRWQOYBRFD-NUQCWPJISA-N 0.000 claims description 4
- 238000002512 chemotherapy Methods 0.000 claims description 4
- 230000000694 effects Effects 0.000 claims description 4
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 claims description 4
- 239000011976 maleic acid Substances 0.000 claims description 4
- 235000006408 oxalic acid Nutrition 0.000 claims description 4
- 235000002906 tartaric acid Nutrition 0.000 claims description 4
- 239000011975 tartaric acid Substances 0.000 claims description 4
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 claims description 3
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 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
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims description 3
- 206010047700 Vomiting Diseases 0.000 claims description 3
- BJEPYKJPYRNKOW-UHFFFAOYSA-N alpha-hydroxysuccinic acid Natural products OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 claims description 3
- 238000007906 compression Methods 0.000 claims description 3
- 238000011978 dissolution method Methods 0.000 claims description 3
- 235000013922 glutamic acid Nutrition 0.000 claims description 3
- 239000004220 glutamic acid Substances 0.000 claims description 3
- 239000001630 malic acid Substances 0.000 claims description 3
- 235000011090 malic acid Nutrition 0.000 claims description 3
- 208000031649 Postoperative Nausea and Vomiting Diseases 0.000 claims description 2
- 238000005469 granulation Methods 0.000 claims description 2
- 230000003179 granulation Effects 0.000 claims description 2
- 239000002464 receptor antagonist Substances 0.000 claims description 2
- 239000002253 acid Substances 0.000 abstract description 41
- 239000003826 tablet Substances 0.000 abstract description 30
- 239000002775 capsule Substances 0.000 abstract description 12
- 238000013461 design Methods 0.000 abstract description 2
- 238000007599 discharging Methods 0.000 abstract description 2
- 238000012545 processing Methods 0.000 abstract description 2
- 239000011049 pearl Substances 0.000 description 252
- MKBLHFILKIKSQM-UHFFFAOYSA-N 9-methyl-3-[(2-methyl-1h-imidazol-3-ium-3-yl)methyl]-2,3-dihydro-1h-carbazol-4-one;chloride Chemical compound Cl.CC1=NC=CN1CC1C(=O)C(C=2C(=CC=CC=2)N2C)=C2CC1 MKBLHFILKIKSQM-UHFFFAOYSA-N 0.000 description 45
- 229960000770 ondansetron hydrochloride Drugs 0.000 description 45
- 239000000243 solution Substances 0.000 description 42
- 230000004888 barrier function Effects 0.000 description 37
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 36
- 239000011324 bead Substances 0.000 description 32
- DOOTYTYQINUNNV-UHFFFAOYSA-N Triethyl citrate Chemical compound CCOC(=O)CC(O)(C(=O)OCC)CC(=O)OCC DOOTYTYQINUNNV-UHFFFAOYSA-N 0.000 description 27
- 239000001069 triethyl citrate Substances 0.000 description 27
- VMYFZRTXGLUXMZ-UHFFFAOYSA-N triethyl citrate Natural products CCOC(=O)C(O)(C(=O)OCC)C(=O)OCC VMYFZRTXGLUXMZ-UHFFFAOYSA-N 0.000 description 27
- 235000013769 triethyl citrate Nutrition 0.000 description 27
- 239000010408 film Substances 0.000 description 26
- 239000002202 Polyethylene glycol Substances 0.000 description 25
- 229920001223 polyethylene glycol Polymers 0.000 description 25
- 239000001856 Ethyl cellulose Substances 0.000 description 24
- 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 description 24
- 229920001249 ethyl cellulose Polymers 0.000 description 24
- 235000019325 ethyl cellulose Nutrition 0.000 description 24
- 229920003169 water-soluble polymer Polymers 0.000 description 23
- 239000006185 dispersion Substances 0.000 description 21
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 20
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 20
- 230000000873 masking effect Effects 0.000 description 18
- FELGMEQIXOGIFQ-UHFFFAOYSA-N Ondansetron Chemical compound CC1=NC=CN1CC1C(=O)C(C=2C(=CC=CC=2)N2C)=C2CC1 FELGMEQIXOGIFQ-UHFFFAOYSA-N 0.000 description 17
- 238000010521 absorption reaction Methods 0.000 description 16
- 239000011230 binding agent Substances 0.000 description 15
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 14
- 230000002496 gastric effect Effects 0.000 description 13
- 239000012528 membrane Substances 0.000 description 13
- 230000036470 plasma concentration Effects 0.000 description 13
- -1 particulate Substances 0.000 description 12
- 229920003132 hydroxypropyl methylcellulose phthalate Polymers 0.000 description 11
- 229920005596 polymer binder Polymers 0.000 description 11
- 239000002491 polymer binding agent Substances 0.000 description 11
- 230000001681 protective effect Effects 0.000 description 11
- 239000013557 residual solvent Substances 0.000 description 10
- 210000001035 gastrointestinal tract Anatomy 0.000 description 9
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 8
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 8
- 230000008878 coupling Effects 0.000 description 8
- 238000010168 coupling process Methods 0.000 description 8
- 238000005859 coupling reaction Methods 0.000 description 8
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 8
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 8
- 239000004014 plasticizer Substances 0.000 description 8
- 239000008186 active pharmaceutical agent Substances 0.000 description 7
- 238000001035 drying Methods 0.000 description 7
- 229920001002 functional polymer Polymers 0.000 description 7
- 239000008194 pharmaceutical composition Substances 0.000 description 7
- 239000000725 suspension Substances 0.000 description 7
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 6
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 6
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 6
- 230000003203 everyday effect Effects 0.000 description 6
- 238000009472 formulation Methods 0.000 description 6
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 6
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 6
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 6
- 239000000546 pharmaceutical excipient Substances 0.000 description 6
- 210000002381 plasma Anatomy 0.000 description 6
- 238000005507 spraying Methods 0.000 description 6
- 210000002784 stomach Anatomy 0.000 description 6
- 230000001360 synchronised effect Effects 0.000 description 6
- URAYPUMNDPQOKB-UHFFFAOYSA-N triacetin Chemical compound CC(=O)OCC(OC(C)=O)COC(C)=O URAYPUMNDPQOKB-UHFFFAOYSA-N 0.000 description 6
- 229940072018 zofran Drugs 0.000 description 6
- 229950010118 cellacefate Drugs 0.000 description 5
- 229920002678 cellulose Polymers 0.000 description 5
- 239000001913 cellulose Substances 0.000 description 5
- 238000006471 dimerization reaction Methods 0.000 description 5
- 230000008030 elimination Effects 0.000 description 5
- 238000003379 elimination reaction Methods 0.000 description 5
- 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 description 5
- 238000005461 lubrication Methods 0.000 description 5
- 238000004519 manufacturing process Methods 0.000 description 5
- 239000000463 material Substances 0.000 description 5
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 description 5
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 description 5
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 4
- 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 description 4
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 description 4
- ZFOZVQLOBQUTQQ-UHFFFAOYSA-N Tributyl citrate Chemical compound CCCCOC(=O)CC(O)(C(=O)OCCCC)CC(=O)OCCCC ZFOZVQLOBQUTQQ-UHFFFAOYSA-N 0.000 description 4
- 230000015572 biosynthetic process Effects 0.000 description 4
- NPAKNKYSJIDKMW-UHFFFAOYSA-N carvedilol Chemical compound COC1=CC=CC=C1OCCNCC(O)COC1=CC=CC2=NC3=CC=C[CH]C3=C12 NPAKNKYSJIDKMW-UHFFFAOYSA-N 0.000 description 4
- 229960004195 carvedilol Drugs 0.000 description 4
- DGBIGWXXNGSACT-UHFFFAOYSA-N clonazepam Chemical compound C12=CC([N+](=O)[O-])=CC=C2NC(=O)CN=C1C1=CC=CC=C1Cl DGBIGWXXNGSACT-UHFFFAOYSA-N 0.000 description 4
- 229960003120 clonazepam Drugs 0.000 description 4
- 229960000913 crospovidone Drugs 0.000 description 4
- 239000011928 denatured alcohol Substances 0.000 description 4
- FLKPEMZONWLCSK-UHFFFAOYSA-N diethyl phthalate Chemical compound CCOC(=O)C1=CC=CC=C1C(=O)OCC FLKPEMZONWLCSK-UHFFFAOYSA-N 0.000 description 4
- IZEKFCXSFNUWAM-UHFFFAOYSA-N dipyridamole Chemical compound C=12N=C(N(CCO)CCO)N=C(N3CCCCC3)C2=NC(N(CCO)CCO)=NC=1N1CCCCC1 IZEKFCXSFNUWAM-UHFFFAOYSA-N 0.000 description 4
- 229960002768 dipyridamole Drugs 0.000 description 4
- 239000007888 film coating Substances 0.000 description 4
- 238000009501 film coating Methods 0.000 description 4
- 239000000796 flavoring agent Substances 0.000 description 4
- 239000007903 gelatin capsule Substances 0.000 description 4
- 238000000338 in vitro Methods 0.000 description 4
- 239000002609 medium Substances 0.000 description 4
- 239000007921 spray Substances 0.000 description 4
- 238000005303 weighing Methods 0.000 description 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- 229920003119 EUDRAGIT E PO Polymers 0.000 description 3
- 229920003139 Eudragit® L 100 Polymers 0.000 description 3
- 229930195725 Mannitol Natural products 0.000 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 description 3
- 230000002378 acidificating effect Effects 0.000 description 3
- NEDGUIRITORSKL-UHFFFAOYSA-N butyl 2-methylprop-2-enoate;2-(dimethylamino)ethyl 2-methylprop-2-enoate;methyl 2-methylprop-2-enoate Chemical compound COC(=O)C(C)=C.CCCCOC(=O)C(C)=C.CN(C)CCOC(=O)C(C)=C NEDGUIRITORSKL-UHFFFAOYSA-N 0.000 description 3
- 229920001577 copolymer Polymers 0.000 description 3
- 238000007922 dissolution test Methods 0.000 description 3
- 150000002148 esters Chemical class 0.000 description 3
- 239000012530 fluid Substances 0.000 description 3
- 235000013355 food flavoring agent Nutrition 0.000 description 3
- 239000001087 glyceryl triacetate Substances 0.000 description 3
- 235000013773 glyceryl triacetate Nutrition 0.000 description 3
- 229920000639 hydroxypropylmethylcellulose acetate succinate Polymers 0.000 description 3
- 239000007788 liquid Substances 0.000 description 3
- 239000000594 mannitol Substances 0.000 description 3
- 235000010355 mannitol Nutrition 0.000 description 3
- 230000007935 neutral effect Effects 0.000 description 3
- 239000000047 product Substances 0.000 description 3
- 230000000717 retained effect Effects 0.000 description 3
- 239000000377 silicon dioxide Substances 0.000 description 3
- 238000003756 stirring Methods 0.000 description 3
- 238000002560 therapeutic procedure Methods 0.000 description 3
- 229960002622 triacetin Drugs 0.000 description 3
- ZEMPKEQAKRGZGQ-AAKVHIHISA-N 2,3-bis[[(z)-12-hydroxyoctadec-9-enoyl]oxy]propyl (z)-12-hydroxyoctadec-9-enoate Chemical compound CCCCCCC(O)C\C=C/CCCCCCCC(=O)OCC(OC(=O)CCCCCCC\C=C/CC(O)CCCCCC)COC(=O)CCCCCCC\C=C/CC(O)CCCCCC ZEMPKEQAKRGZGQ-AAKVHIHISA-N 0.000 description 2
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 2
- PYGXAGIECVVIOZ-UHFFFAOYSA-N Dibutyl decanedioate Chemical compound CCCCOC(=O)CCCCCCCCC(=O)OCCCC PYGXAGIECVVIOZ-UHFFFAOYSA-N 0.000 description 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 description 2
- 241001597008 Nomeidae Species 0.000 description 2
- 229920002565 Polyethylene Glycol 400 Polymers 0.000 description 2
- 239000012736 aqueous medium Substances 0.000 description 2
- 239000007864 aqueous solution Substances 0.000 description 2
- 239000002585 base Substances 0.000 description 2
- 210000004369 blood Anatomy 0.000 description 2
- 239000008280 blood Substances 0.000 description 2
- 239000007853 buffer solution Substances 0.000 description 2
- 230000003139 buffering effect Effects 0.000 description 2
- 229910000019 calcium carbonate Inorganic materials 0.000 description 2
- 229920002301 cellulose acetate Polymers 0.000 description 2
- 229920006217 cellulose acetate butyrate Polymers 0.000 description 2
- 238000005354 coacervation Methods 0.000 description 2
- 239000003086 colorant Substances 0.000 description 2
- 230000002354 daily effect Effects 0.000 description 2
- LUJQXGBDWAGQHS-UHFFFAOYSA-N ethenyl acetate;phthalic acid Chemical compound CC(=O)OC=C.OC(=O)C1=CC=CC=C1C(O)=O LUJQXGBDWAGQHS-UHFFFAOYSA-N 0.000 description 2
- 239000005002 finish coating Substances 0.000 description 2
- 235000013305 food Nutrition 0.000 description 2
- 238000009478 high shear granulation Methods 0.000 description 2
- 229920001477 hydrophilic polymer Polymers 0.000 description 2
- 239000004615 ingredient Substances 0.000 description 2
- 239000008101 lactose Substances 0.000 description 2
- 238000002156 mixing Methods 0.000 description 2
- 238000006386 neutralization reaction Methods 0.000 description 2
- 239000008188 pellet Substances 0.000 description 2
- 229920002689 polyvinyl acetate Polymers 0.000 description 2
- 239000011118 polyvinyl acetate Substances 0.000 description 2
- 239000000843 powder Substances 0.000 description 2
- 238000011160 research Methods 0.000 description 2
- 230000035945 sensitivity Effects 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- 229920001059 synthetic polymer Polymers 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 description 1
- NGNBDVOYPDDBFK-UHFFFAOYSA-N 2-[2,4-di(pentan-2-yl)phenoxy]acetyl chloride Chemical class CCCC(C)C1=CC=C(OCC(Cl)=O)C(C(C)CCC)=C1 NGNBDVOYPDDBFK-UHFFFAOYSA-N 0.000 description 1
- NIXOWILDQLNWCW-UHFFFAOYSA-M Acrylate Chemical compound [O-]C(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-M 0.000 description 1
- 239000004925 Acrylic resin Substances 0.000 description 1
- 229920000178 Acrylic resin Polymers 0.000 description 1
- 208000024172 Cardiovascular disease Diseases 0.000 description 1
- 229920000623 Cellulose acetate phthalate Polymers 0.000 description 1
- 229920002261 Corn starch Polymers 0.000 description 1
- 206010013786 Dry skin Diseases 0.000 description 1
- 244000024675 Eruca sativa Species 0.000 description 1
- 235000014755 Eruca sativa Nutrition 0.000 description 1
- JIGUQPWFLRLWPJ-UHFFFAOYSA-N Ethyl acrylate Chemical compound CCOC(=O)C=C JIGUQPWFLRLWPJ-UHFFFAOYSA-N 0.000 description 1
- 229920003149 Eudragit® E 100 Polymers 0.000 description 1
- 239000001828 Gelatine Substances 0.000 description 1
- 229920001503 Glucan Polymers 0.000 description 1
- 102220570135 Histone PARylation factor 1_L30D_mutation Human genes 0.000 description 1
- 241000282414 Homo sapiens Species 0.000 description 1
- CERQOIWHTDAKMF-UHFFFAOYSA-M Methacrylate Chemical compound CC(=C)C([O-])=O CERQOIWHTDAKMF-UHFFFAOYSA-M 0.000 description 1
- VVQNEPGJFQJSBK-UHFFFAOYSA-N Methyl methacrylate Chemical compound COC(=O)C(C)=C VVQNEPGJFQJSBK-UHFFFAOYSA-N 0.000 description 1
- VRSLTNZJOUZKLX-UHFFFAOYSA-N Ondansetron hydrochloride Chemical compound O.O.Cl.CC1=NC=CN1CC1C(=O)C(C=2C(=CC=CC=2)N2C)=C2CC1 VRSLTNZJOUZKLX-UHFFFAOYSA-N 0.000 description 1
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 1
- 229920003081 Povidone K 30 Polymers 0.000 description 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 230000002411 adverse Effects 0.000 description 1
- 239000003513 alkali Substances 0.000 description 1
- 150000001412 amines Chemical group 0.000 description 1
- 229940069428 antacid Drugs 0.000 description 1
- 239000003159 antacid agent Substances 0.000 description 1
- 238000000889 atomisation Methods 0.000 description 1
- 230000008901 benefit Effects 0.000 description 1
- 210000000941 bile Anatomy 0.000 description 1
- 239000003833 bile salt Substances 0.000 description 1
- 229940093761 bile salts Drugs 0.000 description 1
- 230000037058 blood plasma level Effects 0.000 description 1
- 125000004181 carboxyalkyl group Chemical group 0.000 description 1
- 229940081734 cellulose acetate phthalate Drugs 0.000 description 1
- 150000005829 chemical entities Chemical class 0.000 description 1
- 239000008199 coating composition Substances 0.000 description 1
- 229940000425 combination drug Drugs 0.000 description 1
- 238000005056 compaction Methods 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- 230000006835 compression Effects 0.000 description 1
- 238000012790 confirmation Methods 0.000 description 1
- 239000008120 corn starch Substances 0.000 description 1
- 230000003111 delayed effect Effects 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- QGBSISYHAICWAH-UHFFFAOYSA-N dicyandiamide Chemical compound NC(N)=NC#N QGBSISYHAICWAH-UHFFFAOYSA-N 0.000 description 1
- 235000018823 dietary intake Nutrition 0.000 description 1
- NSNHWTBQMQIDCF-UHFFFAOYSA-N dihydrate;hydrochloride Chemical compound O.O.Cl NSNHWTBQMQIDCF-UHFFFAOYSA-N 0.000 description 1
- 229940126534 drug product Drugs 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 238000013265 extended release Methods 0.000 description 1
- 238000011049 filling Methods 0.000 description 1
- 239000010419 fine particle Substances 0.000 description 1
- 238000010579 first pass effect Methods 0.000 description 1
- 235000019634 flavors Nutrition 0.000 description 1
- 235000011389 fruit/vegetable juice Nutrition 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 150000004676 glycans Chemical class 0.000 description 1
- 238000004128 high performance liquid chromatography Methods 0.000 description 1
- 229940031704 hydroxypropyl methylcellulose phthalate Drugs 0.000 description 1
- 229960003943 hypromellose Drugs 0.000 description 1
- 239000012729 immediate-release (IR) formulation Substances 0.000 description 1
- 229910052500 inorganic mineral Inorganic materials 0.000 description 1
- 238000007689 inspection Methods 0.000 description 1
- PYZRQGJRPPTADH-UHFFFAOYSA-N lamotrigine Chemical compound NC1=NC(N)=NN=C1C1=CC=CC(Cl)=C1Cl PYZRQGJRPPTADH-UHFFFAOYSA-N 0.000 description 1
- 229960001848 lamotrigine Drugs 0.000 description 1
- 230000002045 lasting effect Effects 0.000 description 1
- 239000000787 lecithin Substances 0.000 description 1
- 235000010445 lecithin Nutrition 0.000 description 1
- 229940067606 lecithin Drugs 0.000 description 1
- TWNIBLMWSKIRAT-VFUOTHLCSA-N levoglucosan Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@H]2CO[C@@H]1O2 TWNIBLMWSKIRAT-VFUOTHLCSA-N 0.000 description 1
- 238000011068 loading method Methods 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 229940117841 methacrylic acid copolymer Drugs 0.000 description 1
- 229920003145 methacrylic acid copolymer Polymers 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 239000003094 microcapsule Substances 0.000 description 1
- 239000011707 mineral Substances 0.000 description 1
- 150000004767 nitrides Chemical class 0.000 description 1
- 229940126701 oral medication Drugs 0.000 description 1
- 235000005985 organic acids Nutrition 0.000 description 1
- 238000004806 packaging method and process Methods 0.000 description 1
- 238000005192 partition Methods 0.000 description 1
- 235000010603 pastilles Nutrition 0.000 description 1
- PNJWIWWMYCMZRO-UHFFFAOYSA-N pent‐4‐en‐2‐one Natural products CC(=O)CC=C PNJWIWWMYCMZRO-UHFFFAOYSA-N 0.000 description 1
- 230000035699 permeability Effects 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 239000002897 polymer film coating Substances 0.000 description 1
- 229920001451 polypropylene glycol Polymers 0.000 description 1
- 229920001282 polysaccharide Polymers 0.000 description 1
- 239000005017 polysaccharide Substances 0.000 description 1
- 229920002744 polyvinyl acetate phthalate Polymers 0.000 description 1
- 229940100467 polyvinyl acetate phthalate Drugs 0.000 description 1
- 239000001253 polyvinylpolypyrrolidone Substances 0.000 description 1
- 230000002980 postoperative effect Effects 0.000 description 1
- 239000002244 precipitate Substances 0.000 description 1
- 238000001556 precipitation Methods 0.000 description 1
- 230000000541 pulsatile effect Effects 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 230000002829 reductive effect Effects 0.000 description 1
- 230000003578 releasing effect Effects 0.000 description 1
- 238000007789 sealing Methods 0.000 description 1
- 238000004088 simulation Methods 0.000 description 1
- 239000007909 solid dosage form Substances 0.000 description 1
- 238000005063 solubilization Methods 0.000 description 1
- 230000007928 solubilization Effects 0.000 description 1
- 230000003381 solubilizing effect Effects 0.000 description 1
- 238000005563 spheronization Methods 0.000 description 1
- 239000001384 succinic acid Substances 0.000 description 1
- 239000007916 tablet composition Substances 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 239000010409 thin film Substances 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- LPKHOSYFABZFDZ-UHFFFAOYSA-N tributyl 5-acetyl-7-butyl-6-hydroxyundecane-4,5,6-tricarboxylate Chemical compound C(C)(=O)C(C(C(C(=O)OCCCC)(CCCC)CCCC)(O)C(=O)OCCCC)(C(=O)OCCCC)CCCC LPKHOSYFABZFDZ-UHFFFAOYSA-N 0.000 description 1
- 210000004916 vomit Anatomy 0.000 description 1
- 230000008673 vomiting Effects 0.000 description 1
- 238000004260 weight control Methods 0.000 description 1
- 238000001238 wet grinding Methods 0.000 description 1
Classifications
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
-
- 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
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
-
- 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
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5073—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5084—Mixtures of one or more drugs in different galenical forms, at least one of which being granules, microcapsules or (coated) microparticles according to A61K9/16 or A61K9/50, e.g. for obtaining a specific release pattern or for combining different drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/12—Antidiarrhoeals
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Hospice & Palliative Care (AREA)
- Otolaryngology (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US76275006P | 2006-01-27 | 2006-01-27 | |
| US60/762,750 | 2006-01-27 | ||
| CN2007800114852A CN101410094B (zh) | 2006-01-27 | 2007-01-29 | 包含弱碱性选择性5-羟色胺5-ht3阻断剂和有机酸的药物递送系统 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2007800114852A Division CN101410094B (zh) | 2006-01-27 | 2007-01-29 | 包含弱碱性选择性5-羟色胺5-ht3阻断剂和有机酸的药物递送系统 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103211779A CN103211779A (zh) | 2013-07-24 |
| CN103211779B true CN103211779B (zh) | 2016-03-16 |
Family
ID=38325269
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2007800114852A Expired - Fee Related CN101410094B (zh) | 2006-01-27 | 2007-01-29 | 包含弱碱性选择性5-羟色胺5-ht3阻断剂和有机酸的药物递送系统 |
| CN201310113926.7A Expired - Fee Related CN103211779B (zh) | 2006-01-27 | 2007-01-29 | 包含弱碱性选择性5-羟色胺5-ht3阻断剂和有机酸的药物递送系统 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2007800114852A Expired - Fee Related CN101410094B (zh) | 2006-01-27 | 2007-01-29 | 包含弱碱性选择性5-羟色胺5-ht3阻断剂和有机酸的药物递送系统 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US20070190145A1 (enExample) |
| EP (2) | EP1976491B1 (enExample) |
| JP (3) | JP5433236B2 (enExample) |
| KR (1) | KR101413613B1 (enExample) |
| CN (2) | CN101410094B (enExample) |
| AU (1) | AU2007211091B8 (enExample) |
| BR (1) | BRPI0707324A2 (enExample) |
| CA (1) | CA2640460C (enExample) |
| ES (2) | ES2550035T3 (enExample) |
| IL (1) | IL193020A0 (enExample) |
| NZ (1) | NZ570039A (enExample) |
| RU (1) | RU2490012C2 (enExample) |
| WO (1) | WO2007090082A2 (enExample) |
| ZA (1) | ZA200806497B (enExample) |
Families Citing this family (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101489401B1 (ko) * | 2006-01-27 | 2015-02-03 | 앱탈리스 파마테크, 인코포레이티드 | 약 염기성 약물과 유기산을 포함하는 약물 전달 시스템 |
| CN105534936B (zh) * | 2007-08-13 | 2020-07-31 | Ohemo 生命科学股份有限公司 | 抗滥用药物、使用方法和制备方法 |
| WO2009076361A1 (en) * | 2007-12-10 | 2009-06-18 | Eurand, Inc. | Orally disintegrating tablets comprising diphenhydramine |
| WO2009086046A1 (en) * | 2007-12-21 | 2009-07-09 | Eurand, Inc. | Orally disintegrating tablet compositions of temazepam |
| JP5783725B2 (ja) | 2007-12-28 | 2015-09-24 | インパックス ラボラトリーズ、 インコーポレイテッドＩｍｐａｘ Ｌａｂｏｒａｔｏｒｉｅｓ， Ｉｎｃ． | レボドパの放出制御製剤及びその使用 |
| EP2090297A1 (en) * | 2008-02-13 | 2009-08-19 | Boehringer Ingelheim International GmbH | Formulations of flibanserin |
| US8133506B2 (en) * | 2008-03-12 | 2012-03-13 | Aptalis Pharmatech, Inc. | Drug delivery systems comprising weakly basic drugs and organic acids |
| TWI519322B (zh) * | 2008-04-15 | 2016-02-01 | 愛戴爾製藥股份有限公司 | 包含弱鹼性藥物及控制釋放劑型之組合物 |
| WO2010026993A1 (ja) * | 2008-09-03 | 2010-03-11 | 武田薬品工業株式会社 | 製剤における吸収性改善方法および吸収性が改善された製剤 |
| US20120128764A1 (en) * | 2009-02-23 | 2012-05-24 | Aptalis Pharmatech, Inc. | Controlled-release compositions comprising a proton pump inhibitor |
| RU2011145278A (ru) * | 2009-04-09 | 2013-05-20 | Алкермес Фарма Айэленд Лимитед | Композиции клозапина с контролируемым высвобождением |
| US20110003005A1 (en) * | 2009-07-06 | 2011-01-06 | Gopi Venkatesh | Methods of Treating PDNV and PONV with Extended Release Ondansetron Compositions |
| BR112012013011A2 (pt) * | 2009-11-30 | 2015-09-08 | Aptalis Pharmatech Inc | odt; composição de odt; método para a preparação de um tablete de odt multiparticulado, método para tratar ou prevenir náusea e vômito pós operatória ou náusea e vômito pós- alta por até 24 horas após a dosagem, método para tratar pu prevenir náusea por até 24 horas após a dosagem e método para tratar ou prevenir náusea e vômito associados a radioterapia em pacientes que recebem ou irradiação de corpo total, dose alta única ao abdômen, ou frações diárias ao abdômen por até 24 horas após a dosagem |
| MX337603B (es) | 2009-11-30 | 2016-03-10 | Adare Pharmaceuticals Inc | Composiciones y tabletas farmaceuticas con recubrimiento compresible y metodos de fabricacion. |
| KR101143997B1 (ko) * | 2010-03-04 | 2012-05-09 | 한미사이언스 주식회사 | 유산균 제제 및 5-ｈｔ4 수용체 효능제를 함유하는 경구 투여용 복합 제제 및 이의 제조방법 |
| GB201004020D0 (en) | 2010-03-11 | 2010-04-21 | Acacia Pharma Ltd | New therapeutic use |
| US9011912B2 (en) | 2010-10-07 | 2015-04-21 | Abon Pharmaceuticals, Llc | Extended-release oral dosage forms for poorly soluble amine drugs |
| CN107028900A (zh) | 2010-12-02 | 2017-08-11 | 艾戴尔医药公司 | 快速分散颗粒、口腔崩解片以及方法 |
| US10987313B2 (en) | 2013-10-07 | 2021-04-27 | Impax Laboratories, Llc | Muco-adhesive, controlled release formulations of levodopa and/or esters of levodopa and uses thereof |
| EP3782614A1 (en) | 2013-10-07 | 2021-02-24 | Impax Laboratories, LLC | Muco-adhesive, controlled release formulations of levodopa and/or esters of levodopa and uses thereof |
| SG10201808645TA (en) * | 2013-12-16 | 2018-11-29 | Massachusetts Inst Technology | Fortified Micronutrient Salt Formulations |
| CN106456611B (zh) | 2014-03-11 | 2021-07-20 | 红山生物医药有限公司 | 用于治疗恶心、呕吐或腹泻症状的恩丹西酮缓释固体制剂 |
| PL3200764T3 (pl) * | 2014-10-01 | 2020-12-28 | Oxytone Bioscience B.V. | Rozpadająca się w jamie ustnej stała farmaceutyczna jednostka dawkowania zawierająca substancję kontrolującą poród |
| ES2690140T3 (es) * | 2014-10-01 | 2018-11-19 | Oxytone Bioscience B.V. | Unidad de dosificación farmacéutica sólida de desintegración oral que contiene una sustancia de control del parto |
| CN104473895A (zh) * | 2014-11-20 | 2015-04-01 | 美吉斯制药（厦门）有限公司 | 拉莫三嗪口腔崩解缓释片 |
| US10406336B2 (en) * | 2016-08-03 | 2019-09-10 | Neil S. Davey | Adjustable rate drug delivery implantable device |
| GB201702250D0 (en) | 2017-02-10 | 2017-03-29 | Acacia Pharma Ltd | Method |
| CN108624005B (zh) * | 2017-03-24 | 2021-10-29 | 华东理工大学 | 基于poc和介孔纳米微球的双因子缓释系统 |
| EP4167971A1 (en) | 2020-06-18 | 2023-04-26 | XWPharma Ltd. | Controlled release granulations of water-soluble active pharmaceutical ingredients |
| WO2022020621A1 (en) | 2020-07-24 | 2022-01-27 | XWPharma Ltd. | Pharmaceutical compositions and pharmacokinetics of a gamma-hydroxybutyric acid derivative |
| EP4225274A1 (en) | 2020-10-05 | 2023-08-16 | XWPharma Ltd. | Modified release compositions of a gamma-hydroxybutyric acid derivative |
| WO2022140448A1 (en) | 2020-12-22 | 2022-06-30 | Amneal Pharmaceuticals Llc | Levodopa dosing regimen |
| US11986449B2 (en) | 2020-12-22 | 2024-05-21 | Amneal Pharmaceuticals Llc | Levodopa dosing regimen |
| DK4308086T3 (da) | 2021-03-19 | 2025-11-17 | Xwpharma Ltd | Farmakokinetik af formuleringer med kombineret frigivelse af et gamma-hydroxysmørsyrederivat |
| WO2022233885A2 (en) * | 2021-05-03 | 2022-11-10 | Cambridge Glycoscience Ltd | Soluble and insoluble saccharide compositions and related methods |
| US12303604B1 (en) | 2024-10-16 | 2025-05-20 | Currax Pharmaceuticals Llc | Pharmaceutical formulations comprising naltrexone and/or bupropion |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004096182A1 (en) * | 2003-04-30 | 2004-11-11 | Ranbaxy Laboratories Limited | Extended release matrix tablets of carvedilol |
Family Cites Families (55)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3634584A (en) * | 1969-02-13 | 1972-01-11 | American Home Prod | Sustained action dosage form |
| US3954959A (en) * | 1973-03-28 | 1976-05-04 | A/S Alfred Benzon | Oral drug preparations |
| GB1468172A (en) * | 1973-03-28 | 1977-03-23 | Benzon As Alfred | Oral drug preparations |
| DE2336218C3 (de) * | 1973-07-17 | 1985-11-14 | Byk Gulden Lomberg Chemische Fabrik Gmbh, 7750 Konstanz | Orale Arzneiform |
| DD146547A5 (de) * | 1978-07-15 | 1981-02-18 | Boehringer Sohn Ingelheim | Arzneimittel-retardform mit unloeslichen poroesen diffusionshuellen |
| IE48715B1 (en) * | 1978-12-22 | 1985-05-01 | Elan Corp Plc | New galencial forms for administration of medicaments by oral route,with programmed release and processes for preparing same |
| US4381546A (en) * | 1979-03-02 | 1983-04-26 | Paradyne Corporation | System for the quantitative measurement of impairments in the communication channel of a quadrature amplitude modulation data communication system |
| DE3000979A1 (de) * | 1980-01-12 | 1981-07-23 | Dr. Karl Thomae Gmbh, 7950 Biberach | Neue dipyridamol-retardformen und verfahren zu ihrer herstellung |
| DE3124090A1 (de) * | 1981-06-19 | 1983-01-05 | Dr. Karl Thomae Gmbh, 7950 Biberach | Neue orale dipyridamolformen |
| DE3126703A1 (de) * | 1981-07-07 | 1983-01-27 | Dr. Karl Thomae Gmbh, 7950 Biberach | Bromhexin-retardform und verfahren zu ihrer herstellung |
| DE3237575A1 (de) * | 1982-10-09 | 1984-04-12 | Dr. Karl Thomae Gmbh, 7950 Biberach | Neue orale mopidamolformen |
| IE55745B1 (en) * | 1983-04-06 | 1991-01-02 | Elan Corp Plc | Sustained absorption pharmaceutical composition |
| IE56459B1 (en) * | 1983-12-21 | 1991-08-14 | Elan Corp Ltd | Controlled absorption pharmaceutical formulation |
| US4894240A (en) * | 1983-12-22 | 1990-01-16 | Elan Corporation Plc | Controlled absorption diltiazem formulation for once-daily administration |
| IE56999B1 (en) * | 1983-12-22 | 1992-03-11 | Elan Corp Plc | Pharmaceutical formulation |
| US4826688A (en) * | 1985-11-13 | 1989-05-02 | 501 Elan Corporation PLC. | Controlled absorption pharmaceutical formulation |
| GB2189698A (en) * | 1986-04-30 | 1987-11-04 | Haessle Ab | Coated omeprazole tablets |
| IE58401B1 (en) * | 1986-06-20 | 1993-09-08 | Elan Corp Plc | Controlled absorption pharmaceutical composition |
| DE3627423A1 (de) * | 1986-08-13 | 1988-02-18 | Thomae Gmbh Dr K | Arzneimittel enthaltend dipyridamol oder mopidamol und o-acetylsalicylsaeure bzw. deren physiologisch vertraegliche salze, verfahren zu ihrer herstellung und ihre verwendung zur bekaempfung der thrombusbildung |
| AU2016992A (en) * | 1991-05-20 | 1992-12-30 | Marion Laboratories, Inc. | Multi-layered controlled release formulation |
| US5464632C1 (en) * | 1991-07-22 | 2001-02-20 | Prographarm Lab | Rapidly disintegratable multiparticular tablet |
| JPH0710745A (ja) * | 1993-06-22 | 1995-01-13 | Tanabe Seiyaku Co Ltd | 放出開始時間制御型腸デリバリー経口製剤 |
| JPH08157392A (ja) * | 1994-12-01 | 1996-06-18 | Kanegafuchi Chem Ind Co Ltd | 放出制御型製剤 |
| SI9500173B (sl) * | 1995-05-19 | 2002-02-28 | Lek, | Trofazna farmacevtska oblika s konstantnim in kontroliranim sproščanjem amorfne učinkovine za enkrat dnevno aplikacijo |
| US5837284A (en) * | 1995-12-04 | 1998-11-17 | Mehta; Atul M. | Delivery of multiple doses of medications |
| US5705190A (en) * | 1995-12-19 | 1998-01-06 | Abbott Laboratories | Controlled release formulation for poorly soluble basic drugs |
| US5840329A (en) * | 1997-05-15 | 1998-11-24 | Bioadvances Llc | Pulsatile drug delivery system |
| JP2002505269A (ja) * | 1998-03-06 | 2002-02-19 | エウランド インターナショナル ソシエタ ペル アチオニ | 急速崩壊錠剤 |
| US6602521B1 (en) * | 1998-09-29 | 2003-08-05 | Impax Pharmaceuticals, Inc. | Multiplex drug delivery system suitable for oral administration |
| CA2348871C (en) * | 1998-11-02 | 2009-04-14 | John G. Devane | Multiparticulate modified release composition |
| US6383471B1 (en) * | 1999-04-06 | 2002-05-07 | Lipocine, Inc. | Compositions and methods for improved delivery of ionizable hydrophobic therapeutic agents |
| US6936275B2 (en) * | 1999-12-20 | 2005-08-30 | Scolr, Inc. | Amino acid modulated extended release dosage form |
| CA2395974A1 (en) * | 2000-01-20 | 2001-07-26 | Suggy S. Chrai | Multi-step drug dosage forms |
| US6627223B2 (en) * | 2000-02-11 | 2003-09-30 | Eurand Pharmaceuticals Ltd. | Timed pulsatile drug delivery systems |
| US6500457B1 (en) * | 2000-08-14 | 2002-12-31 | Peirce Management, Llc | Oral pharmaceutical dosage forms for pulsatile delivery of an antiarrhythmic agent |
| US20020107275A1 (en) * | 2000-10-30 | 2002-08-08 | Ramy Lidor-Hadas | Novel crystal and solvate forms of ondansetron hydrochloride and processes for their preparation |
| PT1405621E (pt) * | 2001-06-20 | 2011-05-31 | Takeda Pharmaceutical | Processo de prepara??o de comprimidos |
| US6500454B1 (en) * | 2001-10-04 | 2002-12-31 | Eurand Pharmaceuticals Ltd. | Timed, sustained release systems for propranolol |
| DE10149674A1 (de) * | 2001-10-09 | 2003-04-24 | Apogepha Arzneimittel Gmbh | Orale Darreichungsformen für Propiverin oder seinen pharmazeutisch annehmbaren Salzen mit verlängerter Wirkstoffreisetzung |
| US20040019096A1 (en) * | 2001-10-23 | 2004-01-29 | Vlassios Andronis | Novel formulations of carvedilol |
| US6663888B2 (en) * | 2001-12-14 | 2003-12-16 | Eurand Pharmaceuticals Ltd. | Pulsatile release histamine H2 antagonist dosage form |
| MY139719A (en) * | 2002-02-12 | 2009-10-30 | Glaxo Group Ltd | Oral dosage form for controlled drug release |
| MY143789A (en) * | 2003-02-18 | 2011-07-15 | Helsinn Healthcare Sa | Use of palonosetron treating post- operative nausea and vomiting |
| US20040265375A1 (en) * | 2003-04-16 | 2004-12-30 | Platteeuw Johannes J. | Orally disintegrating tablets |
| DE10353186A1 (de) * | 2003-11-13 | 2005-06-16 | Röhm GmbH & Co. KG | Mehrschichtige Arzneiform, enthaltend eine in Bezug auf die Wirkstoffabgabe modulatorisch wirkende Substanz |
| WO2005077341A1 (en) * | 2004-01-19 | 2005-08-25 | Ranbaxy Laboratories Limited | Orally disintegrating pharmaceutical compositions of ondansetron |
| US8545881B2 (en) * | 2004-04-19 | 2013-10-01 | Eurand Pharmaceuticals, Ltd. | Orally disintegrating tablets and methods of manufacture |
| CA2579767A1 (en) * | 2004-04-30 | 2005-11-10 | Astellas Pharma Inc. | Oral pharmaceutical composition in timed-release particle form and fast-disintegrating tablets containing this composition |
| US9884014B2 (en) | 2004-10-12 | 2018-02-06 | Adare Pharmaceuticals, Inc. | Taste-masked pharmaceutical compositions |
| WO2006047493A2 (en) | 2004-10-21 | 2006-05-04 | Eurand Pharmaceuticals Limited | Taste-masked pharmaceutical compositions with gastrosoluble pore-formers |
| US20060105038A1 (en) | 2004-11-12 | 2006-05-18 | Eurand Pharmaceuticals Limited | Taste-masked pharmaceutical compositions prepared by coacervation |
| US20060280795A1 (en) * | 2005-06-08 | 2006-12-14 | Dexcel Pharma Technologies, Ltd. | Specific time-delayed burst profile delivery system |
| ATE489079T1 (de) * | 2005-12-29 | 2010-12-15 | Osmotica Kereskedelmi Es Szolgaltata Kft | Mehrschichtige tablette mit dreifacher freisetzungskombination |
| KR101441459B1 (ko) * | 2006-10-24 | 2014-09-18 | 헬신 헬쓰케어 에스.에이. | 안정성 및 생체이용률이 개선된 염산 팔로노세트론을 포함하는 연질 캡슐 |
| US8133506B2 (en) * | 2008-03-12 | 2012-03-13 | Aptalis Pharmatech, Inc. | Drug delivery systems comprising weakly basic drugs and organic acids |
-
2007
- 2007-01-29 CN CN2007800114852A patent/CN101410094B/zh not_active Expired - Fee Related
- 2007-01-29 EP EP07717465.4A patent/EP1976491B1/en not_active Not-in-force
- 2007-01-29 JP JP2008552611A patent/JP5433236B2/ja not_active Expired - Fee Related
- 2007-01-29 BR BRPI0707324-0A patent/BRPI0707324A2/pt not_active IP Right Cessation
- 2007-01-29 NZ NZ570039A patent/NZ570039A/en not_active IP Right Cessation
- 2007-01-29 RU RU2008134912/15A patent/RU2490012C2/ru not_active IP Right Cessation
- 2007-01-29 WO PCT/US2007/061217 patent/WO2007090082A2/en not_active Ceased
- 2007-01-29 AU AU2007211091A patent/AU2007211091B8/en not_active Ceased
- 2007-01-29 ES ES11001973.4T patent/ES2550035T3/es active Active
- 2007-01-29 KR KR1020087021036A patent/KR101413613B1/ko not_active Expired - Fee Related
- 2007-01-29 CA CA2640460A patent/CA2640460C/en not_active Expired - Fee Related
- 2007-01-29 EP EP11001973.4A patent/EP2363117B1/en not_active Not-in-force
- 2007-01-29 CN CN201310113926.7A patent/CN103211779B/zh not_active Expired - Fee Related
- 2007-01-29 US US11/668,167 patent/US20070190145A1/en not_active Abandoned
- 2007-01-29 ES ES07717465T patent/ES2531215T3/es active Active
-
2008
- 2008-07-24 IL IL193020A patent/IL193020A0/en not_active IP Right Cessation
- 2008-07-25 ZA ZA2008/06497A patent/ZA200806497B/en unknown
-
2013
- 2013-08-08 JP JP2013165542A patent/JP5918179B2/ja not_active Expired - Fee Related
-
2015
- 2015-09-25 JP JP2015188001A patent/JP2016014048A/ja not_active Withdrawn
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004096182A1 (en) * | 2003-04-30 | 2004-11-11 | Ranbaxy Laboratories Limited | Extended release matrix tablets of carvedilol |
Also Published As
| Publication number | Publication date |
|---|---|
| CA2640460A1 (en) | 2007-08-09 |
| EP1976491B1 (en) | 2014-12-17 |
| KR20080098627A (ko) | 2008-11-11 |
| CA2640460C (en) | 2015-05-26 |
| JP2013249305A (ja) | 2013-12-12 |
| RU2490012C2 (ru) | 2013-08-20 |
| NZ570039A (en) | 2011-07-29 |
| EP2363117B1 (en) | 2015-08-19 |
| JP5433236B2 (ja) | 2014-03-05 |
| JP2016014048A (ja) | 2016-01-28 |
| ZA200806497B (en) | 2009-12-30 |
| AU2007211091A8 (en) | 2013-08-29 |
| CN101410094A (zh) | 2009-04-15 |
| JP2009524697A (ja) | 2009-07-02 |
| WO2007090082A2 (en) | 2007-08-09 |
| JP5918179B2 (ja) | 2016-05-18 |
| ES2531215T3 (es) | 2015-03-11 |
| ES2550035T3 (es) | 2015-11-04 |
| AU2007211091A1 (en) | 2007-08-09 |
| AU2007211091B2 (en) | 2013-05-02 |
| RU2008134912A (ru) | 2010-03-10 |
| US20070190145A1 (en) | 2007-08-16 |
| EP2363117A1 (en) | 2011-09-07 |
| CN101410094B (zh) | 2013-04-17 |
| WO2007090082A3 (en) | 2007-12-21 |
| BRPI0707324A2 (pt) | 2011-05-03 |
| EP1976491A2 (en) | 2008-10-08 |
| AU2007211091B8 (en) | 2013-08-29 |
| CN103211779A (zh) | 2013-07-24 |
| KR101413613B1 (ko) | 2014-07-10 |
| IL193020A0 (en) | 2009-09-22 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN103211779B (zh) | 包含弱碱性选择性5-羟色胺5-ht3阻断剂和有机酸的药物递送系统 | |
| CN101410093A (zh) | 包含弱碱性药物和有机酸的药物递送系统 | |
| TWI440480B (zh) | 包含弱鹼性藥物及有機酸之藥物遞送系統 | |
| CN102458117B (zh) | 含有非阿片样和阿片样止痛药的组合的口腔崩解片组合物 | |
| JP2015098477A (ja) | 弱塩基性薬物を含む組成物及び徐放性剤形 | |
| CN100475197C (zh) | 口服的可持续释放的药用组合物 | |
| AU2013204408B2 (en) | Drug delivery systems comprising weakly basic selective serotonin 5-HT3 blocking agent and organic acids | |
| AU2013204400B2 (en) | Drug delivery systems comprising weakly basic drugs and organic acids | |
| MX2008009616A (en) | Drug delivery systems comprising weakly basic selective serotonin 5-ht3 blocking agent and organic acids | |
| MX2008009613A (en) | Drug delivery systems comprising weakly basic drugs and organic acids |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C53 | Correction of patent of invention or patent application | ||
| CB02 | Change of applicant information |
Address after: ohio Applicant after: EURAND INC. Address before: ohio Applicant before: Eurand Inc. |
|
| COR | Change of bibliographic data |
Free format text: CORRECT: APPLICANT; FROM: APTALIS PHARMA LIMITED TO: ADARE PHARMACEUTICALS, INC. Free format text: CORRECT: ADDRESS; FROM: |
|
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20160316 Termination date: 20190129 |
|
| CF01 | Termination of patent right due to non-payment of annual fee |