SK9132000A3 - Pharmaceutical compositions containing micronized bicyclic drugs - Google Patents

Pharmaceutical compositions containing micronized bicyclic drugs Download PDF

Info

Publication number: SK9132000A3
Authority: SK; Slovakia
Prior art keywords: alkyl; hydrogen; composition; formula; alkoxy
Prior art date: 1997-12-16

Application number

SK913-2000A

Other languages

English (en)

Slovak (sk)

Inventor

David Robert Dumpleton

Simon Joseph Holland

Wendy Anne Knight

Graham Stanley Leonard

Original Assignee

Smithkline Beecham Plc

Priority date (The priority date 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 date listed.)

1997-12-16

Filing date

1998-12-14

Publication date

2001-01-18

1998-12-14 Application filed by Smithkline Beecham Plc filed Critical Smithkline Beecham Plc

2001-01-18 Publication of SK9132000A3 publication Critical patent/SK9132000A3/sk

Links

239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 6
239000003814 drug Substances 0.000 title claims description 17
229940079593 drug Drugs 0.000 title description 11
125000002619 bicyclic group Chemical group 0.000 title 1
239000000203 mixture Substances 0.000 claims abstract description 65
239000002245 particle Substances 0.000 claims abstract description 37
150000001875 compounds Chemical class 0.000 claims abstract description 33
238000009826 distribution Methods 0.000 claims abstract description 9
125000000217 alkyl group Chemical group 0.000 claims description 59
239000001257 hydrogen Substances 0.000 claims description 38
229910052739 hydrogen Inorganic materials 0.000 claims description 38
238000000034 method Methods 0.000 claims description 29
239000000725 suspension Substances 0.000 claims description 29
UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 28
-1 -C 1-6 Chemical group 0.000 claims description 23
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 23
238000000227 grinding Methods 0.000 claims description 23
239000011324 bead Substances 0.000 claims description 18
125000004093 cyano group Chemical group *C#N 0.000 claims description 16
125000003545 alkoxy group Chemical group 0.000 claims description 14
208000035475 disorder Diseases 0.000 claims description 14
125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 12
239000006185 dispersion Substances 0.000 claims description 11
125000003118 aryl group Chemical group 0.000 claims description 10
QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 10
230000000694 effects Effects 0.000 claims description 10
150000002431 hydrogen Chemical class 0.000 claims description 10
125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 10
208000004296 neuralgia Diseases 0.000 claims description 10
229910052760 oxygen Inorganic materials 0.000 claims description 10
239000001301 oxygen Substances 0.000 claims description 10
201000010099 disease Diseases 0.000 claims description 9
125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 9
238000001694 spray drying Methods 0.000 claims description 9
238000001238 wet grinding Methods 0.000 claims description 9
XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims description 8
208000021384 Obsessive-Compulsive disease Diseases 0.000 claims description 8
206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims description 8
125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 8
ZPUCINDJVBIVPJ-LJISPDSOSA-N cocaine Chemical compound O([C@H]1C[C@@H]2CC[C@@H](N2C)[C@H]1C(=O)OC)C(=O)C1=CC=CC=C1 ZPUCINDJVBIVPJ-LJISPDSOSA-N 0.000 claims description 8
125000001072 heteroaryl group Chemical group 0.000 claims description 8
239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 8
235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 8
229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 8
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 8
201000006417 multiple sclerosis Diseases 0.000 claims description 8
230000001537 neural effect Effects 0.000 claims description 8
235000019333 sodium laurylsulphate Nutrition 0.000 claims description 8
DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical group [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims description 7
239000008186 active pharmaceutical agent Substances 0.000 claims description 7
125000004448 alkyl carbonyl group Chemical group 0.000 claims description 7
239000003795 chemical substances by application Substances 0.000 claims description 7
229940088679 drug related substance Drugs 0.000 claims description 7
239000004094 surface-active agent Substances 0.000 claims description 7
LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 6
125000005196 alkyl carbonyloxy group Chemical group 0.000 claims description 6
125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims description 6
238000004519 manufacturing process Methods 0.000 claims description 6
230000035939 shock Effects 0.000 claims description 6
229910052717 sulfur Inorganic materials 0.000 claims description 6
125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims description 6
125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 6
FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical group OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 5
229930195725 Mannitol Natural products 0.000 claims description 5
239000001961 anticonvulsive agent Substances 0.000 claims description 5
125000001589 carboacyl group Chemical group 0.000 claims description 5
239000000594 mannitol Substances 0.000 claims description 5
235000010355 mannitol Nutrition 0.000 claims description 5
208000021722 neuropathic pain Diseases 0.000 claims description 5
SNICXCGAKADSCV-JTQLQIEISA-N (-)-Nicotine Chemical compound CN1CCC[C@H]1C1=CC=CN=C1 SNICXCGAKADSCV-JTQLQIEISA-N 0.000 claims description 4
208000030507 AIDS Diseases 0.000 claims description 4
208000024827 Alzheimer disease Diseases 0.000 claims description 4
208000019901 Anxiety disease Diseases 0.000 claims description 4
206010003591 Ataxia Diseases 0.000 claims description 4
201000006474 Brain Ischemia Diseases 0.000 claims description 4
206010058019 Cancer Pain Diseases 0.000 claims description 4
206010008120 Cerebral ischaemia Diseases 0.000 claims description 4
206010026749 Mania Diseases 0.000 claims description 4
208000019695 Migraine disease Diseases 0.000 claims description 4
206010052904 Musculoskeletal stiffness Diseases 0.000 claims description 4
208000018737 Parkinson disease Diseases 0.000 claims description 4
206010036312 Post-traumatic epilepsy Diseases 0.000 claims description 4
208000028017 Psychotic disease Diseases 0.000 claims description 4
208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 claims description 4
208000030886 Traumatic Brain injury Diseases 0.000 claims description 4
230000016571 aggressive behavior Effects 0.000 claims description 4
125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 4
125000004685 alkoxythiocarbonyl group Chemical group 0.000 claims description 4
125000004691 alkyl thio carbonyl group Chemical group 0.000 claims description 4
239000003006 anti-agglomeration agent Substances 0.000 claims description 4
229940125681 anticonvulsant agent Drugs 0.000 claims description 4
230000036506 anxiety Effects 0.000 claims description 4
125000005129 aryl carbonyl group Chemical group 0.000 claims description 4
125000004391 aryl sulfonyl group Chemical group 0.000 claims description 4
229940049706 benzodiazepine Drugs 0.000 claims description 4
150000001557 benzodiazepines Chemical class 0.000 claims description 4
125000001231 benzoyloxy group Chemical group C(C1=CC=CC=C1)(=O)O* 0.000 claims description 4
239000000919 ceramic Substances 0.000 claims description 4
206010008118 cerebral infarction Diseases 0.000 claims description 4
229960003920 cocaine Drugs 0.000 claims description 4
206010012601 diabetes mellitus Diseases 0.000 claims description 4
206010015037 epilepsy Diseases 0.000 claims description 4
125000005469 ethylenyl group Chemical group 0.000 claims description 4
125000005223 heteroarylcarbonyl group Chemical group 0.000 claims description 4
206010022437 insomnia Diseases 0.000 claims description 4
125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 4
206010027599 migraine Diseases 0.000 claims description 4
201000003631 narcolepsy Diseases 0.000 claims description 4
210000005036 nerve Anatomy 0.000 claims description 4
208000015122 neurodegenerative disease Diseases 0.000 claims description 4
230000007971 neurological deficit Effects 0.000 claims description 4
229960002715 nicotine Drugs 0.000 claims description 4
SNICXCGAKADSCV-UHFFFAOYSA-N nicotine Natural products CN1CCCC1C1=CC=CN=C1 SNICXCGAKADSCV-UHFFFAOYSA-N 0.000 claims description 4
208000019906 panic disease Diseases 0.000 claims description 4
230000033764 rhythmic process Effects 0.000 claims description 4
208000019116 sleep disease Diseases 0.000 claims description 4
230000009529 traumatic brain injury Effects 0.000 claims description 4
206010044652 trigeminal neuralgia Diseases 0.000 claims description 4
208000023105 Huntington disease Diseases 0.000 claims description 3
208000032851 Subarachnoid Hemorrhage Diseases 0.000 claims description 3
208000000323 Tourette Syndrome Diseases 0.000 claims description 3
208000016620 Tourette disease Diseases 0.000 claims description 3
125000005138 alkoxysulfonyl group Chemical group 0.000 claims description 3
125000003806 alkyl carbonyl amino group Chemical group 0.000 claims description 3
125000005135 aryl sulfinyl group Chemical group 0.000 claims description 3
230000004064 dysfunction Effects 0.000 claims description 3
210000005069 ears Anatomy 0.000 claims description 3
CHNUOJQWGUIOLD-NFZZJPOKSA-N epalrestat Chemical compound C=1C=CC=CC=1\C=C(/C)\C=C1/SC(=S)N(CC(O)=O)C1=O CHNUOJQWGUIOLD-NFZZJPOKSA-N 0.000 claims description 3
229910052736 halogen Inorganic materials 0.000 claims description 3
150000002367 halogens Chemical class 0.000 claims description 3
125000005150 heteroarylsulfinyl group Chemical group 0.000 claims description 3
125000005143 heteroarylsulfonyl group Chemical group 0.000 claims description 3
230000002265 prevention Effects 0.000 claims description 3
201000000980 schizophrenia Diseases 0.000 claims description 3
230000002123 temporal effect Effects 0.000 claims description 3
208000004371 toothache Diseases 0.000 claims description 3
125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims description 2
125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 2
WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims description 2
ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims description 2
PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 2
201000004311 Gilles de la Tourette syndrome Diseases 0.000 claims description 2
NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 2
125000004656 alkyl sulfonylamino group Chemical group 0.000 claims description 2
125000003435 aroyl group Chemical group 0.000 claims description 2
125000005199 aryl carbonyloxy group Chemical group 0.000 claims description 2
125000004429 atom Chemical group 0.000 claims description 2
125000000852 azido group Chemical group *N=[N+]=[N-] 0.000 claims description 2
GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims description 2
229910052794 bromium Inorganic materials 0.000 claims description 2
125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims description 2
239000000460 chlorine Substances 0.000 claims description 2
229910052801 chlorine Inorganic materials 0.000 claims description 2
229910052731 fluorine Inorganic materials 0.000 claims description 2
239000011737 fluorine Substances 0.000 claims description 2
125000001153 fluoro group Chemical group F* 0.000 claims description 2
125000001207 fluorophenyl group Chemical group 0.000 claims description 2
125000005204 heteroarylcarbonyloxy group Chemical group 0.000 claims description 2
WCPAKWJPBJAGKN-UHFFFAOYSA-N oxadiazole Chemical class C1=CON=N1 WCPAKWJPBJAGKN-UHFFFAOYSA-N 0.000 claims description 2
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 2
125000001476 phosphono group Chemical group [H]OP(*)(=O)O[H] 0.000 claims description 2
229910001404 rare earth metal oxide Inorganic materials 0.000 claims description 2
208000011117 substance-related disease Diseases 0.000 claims description 2
239000011593 sulfur Substances 0.000 claims description 2
230000017105 transposition Effects 0.000 claims description 2
150000003852 triazoles Chemical class 0.000 claims description 2
125000006624 (C1-C6) alkoxycarbonylamino group Chemical group 0.000 claims 2
125000004738 (C1-C6) alkyl sulfinyl group Chemical group 0.000 claims 2
125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 claims 2
125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims 2
125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 2
125000001091 aminosulfinyl group Chemical group [H]N([H])S(*)=O 0.000 claims 2
125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 2
125000004845 (C1-C6) alkylsulfonylamino group Chemical group 0.000 claims 1
241001233887 Ania Species 0.000 claims 1
206010013654 Drug abuse Diseases 0.000 claims 1
125000004390 alkyl sulfonyl group Chemical group 0.000 claims 1
125000003277 amino group Chemical group 0.000 claims 1
125000006620 amino-(C1-C6) alkyl group Chemical group 0.000 claims 1
238000002360 preparation method Methods 0.000 description 24
239000003826 tablet Substances 0.000 description 18
238000009472 formulation Methods 0.000 description 16
239000000843 powder Substances 0.000 description 15
239000000126 substance Substances 0.000 description 14
238000006243 chemical reaction Methods 0.000 description 13
239000003981 vehicle Substances 0.000 description 10
239000007921 spray Substances 0.000 description 9
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 9
238000003801 milling Methods 0.000 description 8
206010010904 Convulsion Diseases 0.000 description 7
229940125904 compound 1 Drugs 0.000 description 7
239000000463 material Substances 0.000 description 7
239000002002 slurry Substances 0.000 description 7
238000012360 testing method Methods 0.000 description 6
238000002156 mixing Methods 0.000 description 5
241000700159 Rattus Species 0.000 description 4
QCWXUUIWCKQGHC-UHFFFAOYSA-N Zirconium Chemical compound [Zr] QCWXUUIWCKQGHC-UHFFFAOYSA-N 0.000 description 4
239000012736 aqueous medium Substances 0.000 description 4
239000002775 capsule Substances 0.000 description 4
235000019441 ethanol Nutrition 0.000 description 4
239000007788 liquid Substances 0.000 description 4
HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 4
238000012545 processing Methods 0.000 description 4
239000008213 purified water Substances 0.000 description 4
239000004677 Nylon Substances 0.000 description 3
DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
230000001773 anti-convulsant effect Effects 0.000 description 3
150000001562 benzopyrans Chemical class 0.000 description 3
239000007884 disintegrant Substances 0.000 description 3
238000001035 drying Methods 0.000 description 3
239000000945 filler Substances 0.000 description 3
239000000314 lubricant Substances 0.000 description 3
229920001778 nylon Polymers 0.000 description 3
230000036470 plasma concentration Effects 0.000 description 3
230000002685 pulmonary effect Effects 0.000 description 3
RUDFQVOCFDJEEF-UHFFFAOYSA-N yttrium(III) oxide Inorganic materials [O-2].[O-2].[O-2].[Y+3].[Y+3] RUDFQVOCFDJEEF-UHFFFAOYSA-N 0.000 description 3
FEAVXMPFTQROEI-UHFFFAOYSA-N 2h-pyrano[3,2-b]pyridine Chemical class C1=CN=C2C=CCOC2=C1 FEAVXMPFTQROEI-UHFFFAOYSA-N 0.000 description 2
GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 2
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 description 2
239000004354 Hydroxyethyl cellulose Substances 0.000 description 2
229920000663 Hydroxyethyl cellulose Polymers 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
241000124008 Mammalia Species 0.000 description 2
229920002472 Starch Polymers 0.000 description 2
MCMNRKCIXSYSNV-UHFFFAOYSA-N Zirconium dioxide Chemical compound O=[Zr]=O MCMNRKCIXSYSNV-UHFFFAOYSA-N 0.000 description 2
239000004480 active ingredient Substances 0.000 description 2
239000013543 active substance Substances 0.000 description 2
125000004466 alkoxycarbonylamino group Chemical group 0.000 description 2
239000003086 colorant Substances 0.000 description 2
229940125782 compound 2 Drugs 0.000 description 2
230000036461 convulsion Effects 0.000 description 2
125000000753 cycloalkyl group Chemical group 0.000 description 2
238000007907 direct compression Methods 0.000 description 2
239000000796 flavoring agent Substances 0.000 description 2
239000008187 granular material Substances 0.000 description 2
235000019447 hydroxyethyl cellulose Nutrition 0.000 description 2
239000008101 lactose Substances 0.000 description 2
210000003141 lower extremity Anatomy 0.000 description 2
235000019359 magnesium stearate Nutrition 0.000 description 2
229920000609 methyl cellulose Polymers 0.000 description 2
239000001923 methylcellulose Substances 0.000 description 2
235000010981 methylcellulose Nutrition 0.000 description 2
AICOOMRHRUFYCM-ZRRPKQBOSA-N oxazine, 1 Chemical compound C([C@@H]1[C@H](C(C[C@]2(C)[C@@H]([C@H](C)N(C)C)[C@H](O)C[C@]21C)=O)CC1=CC2)C[C@H]1[C@@]1(C)[C@H]2N=C(C(C)C)OC1 AICOOMRHRUFYCM-ZRRPKQBOSA-N 0.000 description 2
239000001267 polyvinylpyrrolidone Substances 0.000 description 2
229920000036 polyvinylpyrrolidone Polymers 0.000 description 2
235000013855 polyvinylpyrrolidone Nutrition 0.000 description 2
230000005855 radiation Effects 0.000 description 2
229920003109 sodium starch glycolate Polymers 0.000 description 2
239000008109 sodium starch glycolate Substances 0.000 description 2
229940079832 sodium starch glycolate Drugs 0.000 description 2
239000007787 solid Substances 0.000 description 2
239000000600 sorbitol Substances 0.000 description 2
235000010356 sorbitol Nutrition 0.000 description 2
239000008107 starch Substances 0.000 description 2
229940032147 starch Drugs 0.000 description 2
235000019698 starch Nutrition 0.000 description 2
230000001954 sterilising effect Effects 0.000 description 2
239000006188 syrup Substances 0.000 description 2
235000020357 syrup Nutrition 0.000 description 2
239000007916 tablet composition Substances 0.000 description 2
230000001225 therapeutic effect Effects 0.000 description 2
238000002560 therapeutic procedure Methods 0.000 description 2
239000000080 wetting agent Substances 0.000 description 2
229910052726 zirconium Inorganic materials 0.000 description 2
125000004768 (C1-C4) alkylsulfinyl group Chemical group 0.000 description 1
125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 description 1
ZORQXIQZAOLNGE-UHFFFAOYSA-N 1,1-difluorocyclohexane Chemical compound FC1(F)CCCCC1 ZORQXIQZAOLNGE-UHFFFAOYSA-N 0.000 description 1
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
235000019489 Almond oil Nutrition 0.000 description 1
WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.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 WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 description 1
KYNSBQPICQTCGU-UHFFFAOYSA-N Benzopyrane Chemical compound C1=CC=C2C=CCOC2=C1 KYNSBQPICQTCGU-UHFFFAOYSA-N 0.000 description 1
125000003830 C1- C4 alkylcarbonylamino group Chemical group 0.000 description 1
229920002134 Carboxymethyl cellulose Polymers 0.000 description 1
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 description 1
IAYPIBMASNFSPL-UHFFFAOYSA-N Ethylene oxide Chemical compound C1CO1 IAYPIBMASNFSPL-UHFFFAOYSA-N 0.000 description 1
108010010803 Gelatin Proteins 0.000 description 1
208000032843 Hemorrhage Diseases 0.000 description 1
101001126084 Homo sapiens Piwi-like protein 2 Proteins 0.000 description 1
235000010643 Leucaena leucocephala Nutrition 0.000 description 1
240000007472 Leucaena leucocephala Species 0.000 description 1
241001465754 Metazoa Species 0.000 description 1
229920000168 Microcrystalline cellulose Polymers 0.000 description 1
229920000881 Modified starch Polymers 0.000 description 1
208000007101 Muscle Cramp Diseases 0.000 description 1
208000002193 Pain Diseases 0.000 description 1
102100029365 Piwi-like protein 2 Human genes 0.000 description 1
208000005392 Spasm Diseases 0.000 description 1
206010043220 Temporomandibular joint syndrome Diseases 0.000 description 1
206010043994 Tonic convulsion Diseases 0.000 description 1
GYMWQLRSSDFGEQ-ADRAWKNSSA-N [(3e,8r,9s,10r,13s,14s,17r)-13-ethyl-17-ethynyl-3-hydroxyimino-1,2,6,7,8,9,10,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-17-yl] acetate;(8r,9s,13s,14s,17r)-17-ethynyl-13-methyl-7,8,9,11,12,14,15,16-octahydro-6h-cyclopenta[a]phenanthrene-3,17-diol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1.O/N=C/1CC[C@@H]2[C@H]3CC[C@](CC)([C@](CC4)(OC(C)=O)C#C)[C@@H]4[C@@H]3CCC2=C\1 GYMWQLRSSDFGEQ-ADRAWKNSSA-N 0.000 description 1
238000005299 abrasion Methods 0.000 description 1
239000000654 additive Substances 0.000 description 1
125000003282 alkyl amino group Chemical group 0.000 description 1
125000004644 alkyl sulfinyl group Chemical group 0.000 description 1
239000008168 almond oil Substances 0.000 description 1
CEGOLXSVJUTHNZ-UHFFFAOYSA-K aluminium tristearate Chemical compound [Al+3].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CEGOLXSVJUTHNZ-UHFFFAOYSA-K 0.000 description 1
229940063655 aluminum stearate Drugs 0.000 description 1
238000004458 analytical method Methods 0.000 description 1
230000003276 anti-hypertensive effect Effects 0.000 description 1
229960003965 antiepileptics Drugs 0.000 description 1
239000002249 anxiolytic agent Substances 0.000 description 1
230000000949 anxiolytic effect Effects 0.000 description 1
239000008365 aqueous carrier Substances 0.000 description 1
230000001580 bacterial effect Effects 0.000 description 1
238000000498 ball milling Methods 0.000 description 1
238000010296 bead milling Methods 0.000 description 1
239000011230 binding agent Substances 0.000 description 1
239000008280 blood Substances 0.000 description 1
210000004369 blood Anatomy 0.000 description 1
235000021152 breakfast Nutrition 0.000 description 1
235000014633 carbohydrates Nutrition 0.000 description 1
150000001720 carbohydrates Chemical class 0.000 description 1
239000001768 carboxy methyl cellulose Substances 0.000 description 1
235000010948 carboxy methyl cellulose Nutrition 0.000 description 1
239000008112 carboxymethyl-cellulose Substances 0.000 description 1
239000000969 carrier Substances 0.000 description 1
229920002678 cellulose Polymers 0.000 description 1
239000001913 cellulose Substances 0.000 description 1
235000010980 cellulose Nutrition 0.000 description 1
239000003240 coconut oil Substances 0.000 description 1
235000019864 coconut oil Nutrition 0.000 description 1
238000011109 contamination Methods 0.000 description 1
238000013270 controlled release Methods 0.000 description 1
238000007796 conventional method Methods 0.000 description 1
238000001816 cooling Methods 0.000 description 1
238000013461 design Methods 0.000 description 1
239000003085 diluting agent Substances 0.000 description 1
239000008157 edible vegetable oil Substances 0.000 description 1
238000004945 emulsification Methods 0.000 description 1
239000003995 emulsifying agent Substances 0.000 description 1
239000000839 emulsion Substances 0.000 description 1
239000002702 enteric coating Substances 0.000 description 1
238000009505 enteric coating Methods 0.000 description 1
150000002148 esters Chemical class 0.000 description 1
BEFDCLMNVWHSGT-UHFFFAOYSA-N ethenylcyclopentane Chemical compound C=CC1CCCC1 BEFDCLMNVWHSGT-UHFFFAOYSA-N 0.000 description 1
238000002474 experimental method Methods 0.000 description 1
238000000605 extraction Methods 0.000 description 1
239000004744 fabric Substances 0.000 description 1
239000003925 fat Substances 0.000 description 1
235000019197 fats Nutrition 0.000 description 1
238000011049 filling Methods 0.000 description 1
235000019634 flavors Nutrition 0.000 description 1
239000012530 fluid Substances 0.000 description 1
238000003304 gavage Methods 0.000 description 1
239000000499 gel Substances 0.000 description 1
239000008273 gelatin Substances 0.000 description 1
229920000159 gelatin Polymers 0.000 description 1
235000019322 gelatine Nutrition 0.000 description 1
235000011852 gelatine desserts Nutrition 0.000 description 1
150000002314 glycerols Chemical class 0.000 description 1
238000005469 granulation Methods 0.000 description 1
230000003179 granulation Effects 0.000 description 1
125000005843 halogen group Chemical group 0.000 description 1
238000010438 heat treatment Methods 0.000 description 1
150000004677 hydrates Chemical class 0.000 description 1
239000012535 impurity Substances 0.000 description 1
238000010348 incorporation Methods 0.000 description 1
238000009616 inductively coupled plasma Methods 0.000 description 1
230000036512 infertility Effects 0.000 description 1
239000004615 ingredient Substances 0.000 description 1
238000001990 intravenous administration Methods 0.000 description 1
229910052742 iron Inorganic materials 0.000 description 1
238000010902 jet-milling Methods 0.000 description 1
239000000832 lactitol Substances 0.000 description 1
235000010448 lactitol Nutrition 0.000 description 1
VQHSOMBJVWLPSR-JVCRWLNRSA-N lactitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@@H]1O[C@H](CO)[C@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-JVCRWLNRSA-N 0.000 description 1
229960003451 lactitol Drugs 0.000 description 1
235000010445 lecithin Nutrition 0.000 description 1
239000000787 lecithin Substances 0.000 description 1
229940067606 lecithin Drugs 0.000 description 1
239000007937 lozenge Substances 0.000 description 1
210000004072 lung Anatomy 0.000 description 1
239000011777 magnesium Substances 0.000 description 1
238000005259 measurement Methods 0.000 description 1
239000002609 medium Substances 0.000 description 1
239000012528 membrane Substances 0.000 description 1
HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 description 1
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
235000010270 methyl p-hydroxybenzoate Nutrition 0.000 description 1
239000004292 methyl p-hydroxybenzoate Substances 0.000 description 1
229940016286 microcrystalline cellulose Drugs 0.000 description 1
235000019813 microcrystalline cellulose Nutrition 0.000 description 1
239000008108 microcrystalline cellulose Substances 0.000 description 1
235000019426 modified starch Nutrition 0.000 description 1
239000003607 modifier Substances 0.000 description 1
239000002687 nonaqueous vehicle Substances 0.000 description 1
238000007911 parenteral administration Methods 0.000 description 1
238000003921 particle size analysis Methods 0.000 description 1
238000010951 particle size reduction Methods 0.000 description 1
238000005192 partition Methods 0.000 description 1
239000000546 pharmaceutical excipient Substances 0.000 description 1
239000000825 pharmaceutical preparation Substances 0.000 description 1
229920000642 polymer Polymers 0.000 description 1
239000003755 preservative agent Substances 0.000 description 1
230000003449 preventive effect Effects 0.000 description 1
235000010232 propyl p-hydroxybenzoate Nutrition 0.000 description 1
239000004405 propyl p-hydroxybenzoate Substances 0.000 description 1
QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 description 1
238000001953 recrystallisation Methods 0.000 description 1
239000000243 solution Substances 0.000 description 1
239000012453 solvate Substances 0.000 description 1
235000010199 sorbic acid Nutrition 0.000 description 1
239000004334 sorbic acid Substances 0.000 description 1
229940075582 sorbic acid Drugs 0.000 description 1
239000001593 sorbitan monooleate Substances 0.000 description 1
235000011069 sorbitan monooleate Nutrition 0.000 description 1
229940035049 sorbitan monooleate Drugs 0.000 description 1
238000012453 sprague-dawley rat model Methods 0.000 description 1
239000007858 starting material Substances 0.000 description 1
238000004659 sterilization and disinfection Methods 0.000 description 1
238000003756 stirring Methods 0.000 description 1
238000003860 storage Methods 0.000 description 1
125000001424 substituent group Chemical group 0.000 description 1
238000006467 substitution reaction Methods 0.000 description 1
239000000829 suppository Substances 0.000 description 1
239000000375 suspending agent Substances 0.000 description 1
229940124597 therapeutic agent Drugs 0.000 description 1
239000002562 thickening agent Substances 0.000 description 1
238000004448 titration Methods 0.000 description 1
210000003901 trigeminal nerve Anatomy 0.000 description 1
238000009827 uniform distribution Methods 0.000 description 1
235000010447 xylitol Nutrition 0.000 description 1
HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 1
229910001233 yttria-stabilized zirconia Inorganic materials 0.000 description 1
229910052727 yttrium Inorganic materials 0.000 description 1
VWQVUPCCIRVNHF-UHFFFAOYSA-N yttrium atom Chemical compound [Y] VWQVUPCCIRVNHF-UHFFFAOYSA-N 0.000 description 1

Classifications

- B—PERFORMING OPERATIONS; TRANSPORTING
- B02—CRUSHING, PULVERISING, OR DISINTEGRATING; PREPARATORY TREATMENT OF GRAIN FOR MILLING
- B02C—CRUSHING, PULVERISING, OR DISINTEGRATING IN GENERAL; MILLING GRAIN
- B02C17/00—Disintegrating by tumbling mills, i.e. mills having a container charged with the material to be disintegrated with or without special disintegrating members such as pebbles or balls
- B02C17/04—Disintegrating by tumbling mills, i.e. mills having a container charged with the material to be disintegrated with or without special disintegrating members such as pebbles or balls with unperforated container
- B02C17/06—Disintegrating by tumbling mills, i.e. mills having a container charged with the material to be disintegrated with or without special disintegrating members such as pebbles or balls with unperforated container with several compartments
- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- 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
- 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
- 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
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/145—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic 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
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/06—Antimigraine agents
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/20—Hypnotics; Sedatives
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- B—PERFORMING OPERATIONS; TRANSPORTING
- B02—CRUSHING, PULVERISING, OR DISINTEGRATING; PREPARATORY TREATMENT OF GRAIN FOR MILLING
- B02C—CRUSHING, PULVERISING, OR DISINTEGRATING IN GENERAL; MILLING GRAIN
- B02C17/00—Disintegrating by tumbling mills, i.e. mills having a container charged with the material to be disintegrated with or without special disintegrating members such as pebbles or balls
- B02C17/18—Details
- B02C17/20—Disintegrating members
- B—PERFORMING OPERATIONS; TRANSPORTING
- B02—CRUSHING, PULVERISING, OR DISINTEGRATING; PREPARATORY TREATMENT OF GRAIN FOR MILLING
- B02C—CRUSHING, PULVERISING, OR DISINTEGRATING IN GENERAL; MILLING GRAIN
- B02C17/00—Disintegrating by tumbling mills, i.e. mills having a container charged with the material to be disintegrated with or without special disintegrating members such as pebbles or balls
- B02C17/18—Details
- B02C17/22—Lining for containers
- 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
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

Health & Medical Sciences (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Veterinary Medicine (AREA)
Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Pharmacology & Pharmacy (AREA)
Life Sciences & Earth Sciences (AREA)
Animal Behavior & Ethology (AREA)
General Health & Medical Sciences (AREA)
Public Health (AREA)
Organic Chemistry (AREA)
Neurology (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Biomedical Technology (AREA)
Neurosurgery (AREA)
Epidemiology (AREA)
Psychiatry (AREA)
Diabetes (AREA)
Food Science & Technology (AREA)
Pain & Pain Management (AREA)
Psychology (AREA)
Physical Education & Sports Medicine (AREA)
Emergency Medicine (AREA)
Addiction (AREA)
Hospice & Palliative Care (AREA)
Urology & Nephrology (AREA)
Vascular Medicine (AREA)
Cardiology (AREA)
Heart & Thoracic Surgery (AREA)
Anesthesiology (AREA)
Orthopedic Medicine & Surgery (AREA)
Endocrinology (AREA)
Hematology (AREA)
Obesity (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Nitrogen Condensed Heterocyclic Rings (AREA)
Plural Heterocyclic Compounds (AREA)

SK913-2000A 1997-12-16 1998-12-14 Pharmaceutical compositions containing micronized bicyclic drugs SK9132000A3 (en)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
GBGB9726543.3A GB9726543D0 (en)	1997-12-16	1997-12-16	Novel compositions
PCT/EP1998/008156 WO1999030687A1 (fr)	1997-12-16	1998-12-14	Preparations pharmaceutiques contenant des medicaments bicycliques micronises

Publications (1)

Publication Number	Publication Date
SK9132000A3 true SK9132000A3 (en)	2001-01-18

Family

ID=10823680

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
SK913-2000A SK9132000A3 (en)	1997-12-16	1998-12-14	Pharmaceutical compositions containing micronized bicyclic drugs

Country Status (32)

Country	Link
EP (2)	EP1338274A1 (fr)
JP (1)	JP2002508310A (fr)
KR (1)	KR20010033149A (fr)
CN (2)	CN1284865A (fr)
AP (1)	AP2000001837A0 (fr)
AR (1)	AR017212A1 (fr)
AT (1)	ATE260094T1 (fr)
AU (1)	AU743155B2 (fr)
BG (1)	BG104596A (fr)
BR (1)	BR9813602A (fr)
CA (1)	CA2314968A1 (fr)
DE (1)	DE69821978T2 (fr)
DZ (1)	DZ2677A1 (fr)
EA (1)	EA003732B1 (fr)
ES (1)	ES2216350T3 (fr)
GB (1)	GB9726543D0 (fr)
HU (1)	HUP0100384A3 (fr)
ID (1)	ID24930A (fr)
IL (1)	IL136664A0 (fr)
MA (1)	MA24721A1 (fr)
MY (1)	MY132978A (fr)
NO (1)	NO20003073L (fr)
NZ (1)	NZ504991A (fr)
OA (1)	OA11429A (fr)
PE (1)	PE20000114A1 (fr)
PL (1)	PL341339A1 (fr)
SK (1)	SK9132000A3 (fr)
TR (1)	TR200001792T2 (fr)
TW (1)	TW200305442A (fr)
UY (1)	UY25307A1 (fr)
WO (1)	WO1999030687A1 (fr)
ZA (1)	ZA9811502B (fr)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
EP0810853B1 (fr)	1995-02-24	2004-08-25	Elan Pharma International Limited	Aerosols contenant des dispersions de nanoparticules
US7521068B2 (en)	1998-11-12	2009-04-21	Elan Pharma International Ltd.	Dry powder aerosols of nanoparticulate drugs
EP1294358B1 (fr) *	2000-06-28	2004-08-18	Smithkline Beecham Plc	Procede de broyage par voie humide
GB0112497D0 (en) *	2001-05-22	2001-07-11	Smithkline Beecham Plc	Formulation
GB0127805D0 (en)	2001-11-20	2002-01-09	Smithkline Beecham Plc	Pharmaceutical composition
KR20080066977A (ko)	2005-11-10	2008-07-17	더루우브리졸코오포레이션	분산체의 제조방법
EP2307004A1 (fr) *	2008-06-05	2011-04-13	Minster Research Limited	Nouveaux traitements
JP2011522031A (ja) *	2008-06-05	2011-07-28	ミンスター・リサーチ・リミテッド	新規な治療
MX2012006352A (es) *	2009-12-03	2012-06-27	Proximagen Ltd	Tratamiento de alodinia e hiperalgesia.
RU2012124838A (ru) *	2009-12-03	2014-01-10	Проксимэджен ЛТД	Лечение инфекционных заболеваний
EP2471513B1 (fr) *	2010-12-28	2015-06-10	LEK Pharmaceuticals d.d.	Procédé de production d'ingrédients pharmaceutique actif et préparation sous la forme de billes
WO2016157061A1 (fr) *	2015-03-31	2016-10-06	Wockhardt Limited	Procédé de broyage humide aseptique pour le palmitate de palipéridone

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US5065946A (en) *	1988-07-21	1991-11-19	Matsushita Electric Industrial Co., Ltd.	Media agitating mill and method for milling ceramic powder
US5145684A (en) *	1991-01-25	1992-09-08	Sterling Drug Inc.	Surface modified drug nanoparticles
NZ248813A (en) *	1992-11-25	1995-06-27	Eastman Kodak Co	Polymeric grinding media used in grinding pharmaceutical substances
NZ258611A (en) *	1992-12-11	1997-07-27	Smithkline Beecham Plc	4-benzoyl(or heteroarylcarbonyl)amino-3,4-dihydro- 3-hydroxy-2h-benzo[b]pyran derivatives;benzopyrano[4,3-d]oxazole intermediates
HUT76136A (en) *	1994-06-10	1997-06-30	Smithkline Beecham Plc	Benzopyran compounds and their use as therapeutic agents
US5534270A (en) *	1995-02-09	1996-07-09	Nanosystems Llc	Method of preparing stable drug nanoparticles
US5518738A (en) *	1995-02-09	1996-05-21	Nanosystem L.L.C.	Nanoparticulate nsaid compositions
DE19614295A1 (de) *	1995-04-21	1996-10-24	Friedrich Dr Ing Vock	Verfahren und Vorrichtung zum Nassmahlen und Dispergieren von Feststoffpartikeln in Flüssigkeiten

1997
- 1997-12-16 GB GBGB9726543.3A patent/GB9726543D0/en not_active Ceased
1998
- 1998-11-22 TW TW092109280A patent/TW200305442A/zh unknown
- 1998-12-14 HU HU0100384A patent/HUP0100384A3/hu unknown
- 1998-12-14 WO PCT/EP1998/008156 patent/WO1999030687A1/fr not_active Ceased
- 1998-12-14 AT AT98966322T patent/ATE260094T1/de not_active IP Right Cessation
- 1998-12-14 JP JP2000538670A patent/JP2002508310A/ja active Pending
- 1998-12-14 CN CN98813568A patent/CN1284865A/zh active Pending
- 1998-12-14 NZ NZ504991A patent/NZ504991A/xx unknown
- 1998-12-14 EP EP03076016A patent/EP1338274A1/fr not_active Withdrawn
- 1998-12-14 AU AU22724/99A patent/AU743155B2/en not_active Ceased
- 1998-12-14 ES ES98966322T patent/ES2216350T3/es not_active Expired - Lifetime
- 1998-12-14 DE DE69821978T patent/DE69821978T2/de not_active Expired - Fee Related
- 1998-12-14 IL IL13666498A patent/IL136664A0/xx unknown
- 1998-12-14 BR BR9813602-0A patent/BR9813602A/pt not_active IP Right Cessation
- 1998-12-14 CA CA002314968A patent/CA2314968A1/fr not_active Abandoned
- 1998-12-14 TR TR2000/01792T patent/TR200001792T2/xx unknown
- 1998-12-14 ID IDW20001124A patent/ID24930A/id unknown
- 1998-12-14 PL PL98341339A patent/PL341339A1/xx unknown
- 1998-12-14 EA EA200000664A patent/EA003732B1/ru not_active IP Right Cessation
- 1998-12-14 AP APAP/P/2000/001837A patent/AP2000001837A0/en unknown
- 1998-12-14 SK SK913-2000A patent/SK9132000A3/sk unknown
- 1998-12-14 EP EP98966322A patent/EP1037612B1/fr not_active Expired - Lifetime
- 1998-12-14 CN CNA031787088A patent/CN1475206A/zh active Pending
- 1998-12-14 MA MA25390A patent/MA24721A1/fr unknown
- 1998-12-14 KR KR1020007006525A patent/KR20010033149A/ko not_active Ceased
- 1998-12-15 UY UY25307A patent/UY25307A1/es not_active Application Discontinuation
- 1998-12-15 MY MYPI98005667A patent/MY132978A/en unknown
- 1998-12-15 DZ DZ980287A patent/DZ2677A1/fr active
- 1998-12-15 ZA ZA9811502A patent/ZA9811502B/xx unknown
- 1998-12-15 AR ARP980106367A patent/AR017212A1/es not_active Application Discontinuation
- 1998-12-16 PE PE1998001230A patent/PE20000114A1/es not_active Application Discontinuation
2000
- 2000-06-15 NO NO20003073A patent/NO20003073L/no not_active Application Discontinuation
- 2000-06-16 OA OA1200000176A patent/OA11429A/en unknown
- 2000-07-11 BG BG104596A patent/BG104596A/xx unknown

Also Published As

Publication number	Publication date
PL341339A1 (en)	2001-04-09
DZ2677A1 (fr)	2003-03-29
CN1284865A (zh)	2001-02-21
HUP0100384A3 (en)	2002-04-29
EP1338274A1 (fr)	2003-08-27
PE20000114A1 (es)	2000-04-30
KR20010033149A (ko)	2001-04-25
JP2002508310A (ja)	2002-03-19
NO20003073D0 (no)	2000-06-15
EP1037612A1 (fr)	2000-09-27
DE69821978D1 (de)	2004-04-01
EA003732B1 (ru)	2003-08-28
AU2272499A (en)	1999-07-05
BR9813602A (pt)	2002-01-22
MY132978A (en)	2007-10-31
OA11429A (en)	2004-04-26
ES2216350T3 (es)	2004-10-16
AP2000001837A0 (en)	2000-06-30
ATE260094T1 (de)	2004-03-15
MA24721A1 (fr)	1999-07-01
ZA9811502B (en)	2000-06-15
IL136664A0 (en)	2001-06-14
ID24930A (id)	2000-08-31
EP1037612B1 (fr)	2004-02-25
NO20003073L (no)	2000-08-10
TR200001792T2 (tr)	2000-11-21
GB9726543D0 (en)	1998-02-11
UY25307A1 (es)	2001-08-27
CA2314968A1 (fr)	1999-06-24
BG104596A (en)	2001-04-30
CN1475206A (zh)	2004-02-18
NZ504991A (en)	2002-11-26
AU743155B2 (en)	2002-01-17
TW200305442A (en)	2003-11-01
DE69821978T2 (de)	2004-12-23
AR017212A1 (es)	2001-08-22
EA200000664A1 (ru)	2000-12-25
HUP0100384A2 (hu)	2001-12-28
WO1999030687A1 (fr)	1999-06-24

Publication	Publication Date	Title
JP6619386B2 (ja)	2019-12-11	生物学的活性物質の溶解プロファイルを改善するための方法
JP6175464B2 (ja)	2017-08-02	商業的規模での封入ナノ粒子の製造
SK9132000A3 (en)	2001-01-18	Pharmaceutical compositions containing micronized bicyclic drugs
CN1870979A (zh)	2006-11-29	生产基本无溶剂的小颗粒的方法
US20030165570A1 (en)	2003-09-04	Pharmaceutical compositions containing micronized bicyclic drugs
CZ20002207A3 (cs)	2000-11-15	Farmaceutické prostředky obsahující mikronizovaná bicyklická léčiva
NZ518798A (en)	2004-03-26	Preparation of particulate compositions by wet milling a sparingly water-soluble drug substance as an aqueous dispersion in a multi-chamber bead mill, where the aqueous dispersion also comprises a soluble carrier, a surfactant and an anti-agglomeration agent
HK1059211A (en)	2004-06-25	Process for preparing a particulate composition
AU2005231355B2 (en)	2008-09-18	Spray dried pharmaceutical compositions
AU3438102A (en)	2002-09-05	Pharmaceutical compositions containing micronized bicyclic drugs
EP1940358A2 (fr)	2008-07-09	Préparations pharmaceutiques
WO2002094223A2 (fr)	2002-11-28	Formulation
HK1099213B (en)	2009-04-30	Spray dried pharmaceutical compositions
MXPA06010860A (en)	2007-04-20	Spray dried pharmaceutical compositions
HK1225989A1 (zh)	2017-09-22	包封的纳米颗粒在工业规模的制备
HK1095272A (en)	2007-05-04	Process for production of essentially solvent-free small particles
HK1096309A (en)	2007-06-01	Method for preparing submicron particles of paclitaxel