UA73101C2 - Antagonist of serotonin receptor encapsulated by biodegradable polymer and method for its manufacture - Google Patents
Antagonist of serotonin receptor encapsulated by biodegradable polymer and method for its manufacture Download PDFInfo
- Publication number
- UA73101C2 UA73101C2 UA2001064165A UA2001064165A UA73101C2 UA 73101 C2 UA73101 C2 UA 73101C2 UA 2001064165 A UA2001064165 A UA 2001064165A UA 2001064165 A UA2001064165 A UA 2001064165A UA 73101 C2 UA73101 C2 UA 73101C2
- Authority
- UA
- Ukraine
- Prior art keywords
- specified
- indicated
- polymer
- pharmaceutically active
- active molecule
- Prior art date
Links
- 238000000034 method Methods 0.000 title claims abstract description 99
- 229920002988 biodegradable polymer Polymers 0.000 title claims abstract description 28
- 239000004621 biodegradable polymer Substances 0.000 title claims abstract description 28
- 239000005557 antagonist Substances 0.000 title claims abstract description 6
- 102000040125 5-hydroxytryptamine receptor family Human genes 0.000 title claims 3
- 108091032151 5-hydroxytryptamine receptor family Proteins 0.000 title claims 3
- 238000004519 manufacturing process Methods 0.000 title abstract description 7
- 229920000642 polymer Polymers 0.000 claims abstract description 109
- 239000000203 mixture Substances 0.000 claims abstract description 85
- 239000011859 microparticle Substances 0.000 claims abstract description 51
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 45
- 229920001577 copolymer Polymers 0.000 claims abstract description 18
- 239000002552 dosage form Substances 0.000 claims abstract description 13
- 239000006104 solid solution Substances 0.000 claims abstract description 13
- 208000020925 Bipolar disease Diseases 0.000 claims abstract description 10
- 208000028017 Psychotic disease Diseases 0.000 claims abstract description 10
- 206010013663 drug dependence Diseases 0.000 claims abstract description 8
- 208000011117 substance-related disease Diseases 0.000 claims abstract description 8
- 238000002156 mixing Methods 0.000 claims description 51
- 150000001875 compounds Chemical class 0.000 claims description 40
- 229940125904 compound 1 Drugs 0.000 claims description 31
- 230000000694 effects Effects 0.000 claims description 28
- 230000015572 biosynthetic process Effects 0.000 claims description 25
- 239000000243 solution Substances 0.000 claims description 22
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 claims description 18
- 238000009826 distribution Methods 0.000 claims description 16
- 238000013268 sustained release Methods 0.000 claims description 15
- 239000012730 sustained-release form Substances 0.000 claims description 15
- 230000009477 glass transition Effects 0.000 claims description 13
- 239000008187 granular material Substances 0.000 claims description 12
- 229920000728 polyester Polymers 0.000 claims description 12
- 150000003839 salts Chemical class 0.000 claims description 12
- 229940076279 serotonin Drugs 0.000 claims description 10
- 208000020401 Depressive disease Diseases 0.000 claims description 8
- 239000003420 antiserotonin agent Substances 0.000 claims description 8
- 102000005962 receptors Human genes 0.000 claims description 8
- 108020003175 receptors Proteins 0.000 claims description 8
- 239000000725 suspension Substances 0.000 claims description 8
- 208000019901 Anxiety disease Diseases 0.000 claims description 7
- 230000036506 anxiety Effects 0.000 claims description 7
- 208000021384 Obsessive-Compulsive disease Diseases 0.000 claims description 6
- 229940121356 serotonin receptor antagonist Drugs 0.000 claims description 6
- 238000005469 granulation Methods 0.000 claims description 5
- 230000003179 granulation Effects 0.000 claims description 5
- 239000008240 homogeneous mixture Substances 0.000 claims description 5
- 208000019116 sleep disease Diseases 0.000 claims description 5
- RKDVKSZUMVYZHH-UHFFFAOYSA-N 1,4-dioxane-2,5-dione Chemical group O=C1COC(=O)CO1 RKDVKSZUMVYZHH-UHFFFAOYSA-N 0.000 claims description 4
- 230000005764 inhibitory process Effects 0.000 claims description 4
- JJTUDXZGHPGLLC-UHFFFAOYSA-N lactide Chemical group CC1OC(=O)C(C)OC1=O JJTUDXZGHPGLLC-UHFFFAOYSA-N 0.000 claims description 4
- 208000003890 Coronary Vasospasm Diseases 0.000 claims description 3
- 208000007536 Thrombosis Diseases 0.000 claims description 3
- 206010002383 Angina Pectoris Diseases 0.000 claims description 2
- AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Polymers OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 claims description 2
- 239000004952 Polyamide Substances 0.000 claims description 2
- 229920002732 Polyanhydride Polymers 0.000 claims description 2
- 229920000954 Polyglycolide Polymers 0.000 claims description 2
- 229920000331 Polyhydroxybutyrate Polymers 0.000 claims description 2
- 229920001710 Polyorthoester Polymers 0.000 claims description 2
- 239000005015 poly(hydroxybutyrate) Substances 0.000 claims description 2
- 229920000747 poly(lactic acid) Polymers 0.000 claims description 2
- 229920002627 poly(phosphazenes) Polymers 0.000 claims description 2
- 229920002647 polyamide Polymers 0.000 claims description 2
- 229920001610 polycaprolactone Polymers 0.000 claims description 2
- 239000004632 polycaprolactone Substances 0.000 claims description 2
- 229920000515 polycarbonate Polymers 0.000 claims description 2
- 239000004417 polycarbonate Substances 0.000 claims description 2
- 229940102213 injectable suspension Drugs 0.000 claims 2
- 238000003801 milling Methods 0.000 claims 1
- 238000012876 topography Methods 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract description 19
- 238000000227 grinding Methods 0.000 abstract description 18
- 239000004480 active ingredient Substances 0.000 abstract description 15
- 238000001125 extrusion Methods 0.000 abstract description 12
- 201000000980 schizophrenia Diseases 0.000 abstract description 11
- 238000007580 dry-mixing Methods 0.000 abstract description 7
- 239000013543 active substance Substances 0.000 abstract description 6
- 238000002347 injection Methods 0.000 abstract description 5
- 239000007924 injection Substances 0.000 abstract description 5
- 230000008569 process Effects 0.000 abstract description 4
- 208000022531 anorexia Diseases 0.000 abstract description 3
- 206010061428 decreased appetite Diseases 0.000 abstract description 3
- 238000013270 controlled release Methods 0.000 abstract description 2
- 102000049773 5-HT2A Serotonin Receptor Human genes 0.000 abstract 1
- 108010072564 5-HT2A Serotonin Receptor Proteins 0.000 abstract 1
- 229940079593 drug Drugs 0.000 description 34
- 239000003814 drug Substances 0.000 description 34
- 241001465754 Metazoa Species 0.000 description 30
- 239000011159 matrix material Substances 0.000 description 28
- 229930006000 Sucrose Natural products 0.000 description 24
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 24
- 239000005720 sucrose Substances 0.000 description 24
- 238000002474 experimental method Methods 0.000 description 22
- 239000000463 material Substances 0.000 description 22
- 239000002245 particle Substances 0.000 description 19
- 230000008901 benefit Effects 0.000 description 16
- 210000003169 central nervous system Anatomy 0.000 description 11
- 208000035475 disorder Diseases 0.000 description 11
- 238000002844 melting Methods 0.000 description 11
- 239000002904 solvent Substances 0.000 description 11
- 239000000155 melt Substances 0.000 description 10
- 230000008018 melting Effects 0.000 description 10
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 10
- 238000000113 differential scanning calorimetry Methods 0.000 description 9
- VYFYYTLLBUKUHU-UHFFFAOYSA-N dopamine Chemical compound NCCC1=CC=C(O)C(O)=C1 VYFYYTLLBUKUHU-UHFFFAOYSA-N 0.000 description 9
- 230000002035 prolonged effect Effects 0.000 description 9
- 238000005809 transesterification reaction Methods 0.000 description 9
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 8
- 238000005481 NMR spectroscopy Methods 0.000 description 8
- 239000000523 sample Substances 0.000 description 8
- 238000004626 scanning electron microscopy Methods 0.000 description 8
- 238000012360 testing method Methods 0.000 description 8
- 208000024891 symptom Diseases 0.000 description 7
- 206010026749 Mania Diseases 0.000 description 6
- 201000010099 disease Diseases 0.000 description 6
- 238000004090 dissolution Methods 0.000 description 6
- 235000013305 food Nutrition 0.000 description 6
- 239000011521 glass Substances 0.000 description 6
- 238000004128 high performance liquid chromatography Methods 0.000 description 6
- 208000024714 major depressive disease Diseases 0.000 description 6
- 238000004458 analytical method Methods 0.000 description 5
- 230000001684 chronic effect Effects 0.000 description 5
- 238000000354 decomposition reaction Methods 0.000 description 5
- 239000003937 drug carrier Substances 0.000 description 5
- 238000001035 drying Methods 0.000 description 5
- 239000000945 filler Substances 0.000 description 5
- 238000009472 formulation Methods 0.000 description 5
- 238000010438 heat treatment Methods 0.000 description 5
- 229960004801 imipramine Drugs 0.000 description 5
- BCGWQEUPMDMJNV-UHFFFAOYSA-N imipramine Chemical compound C1CC2=CC=CC=C2N(CCCN(C)C)C2=CC=CC=C21 BCGWQEUPMDMJNV-UHFFFAOYSA-N 0.000 description 5
- 230000003993 interaction Effects 0.000 description 5
- 239000003921 oil Substances 0.000 description 5
- 235000019198 oils Nutrition 0.000 description 5
- 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 5
- 239000000843 powder Substances 0.000 description 5
- 238000002360 preparation method Methods 0.000 description 5
- 239000000126 substance Substances 0.000 description 5
- 206010012374 Depressed mood Diseases 0.000 description 4
- 230000001154 acute effect Effects 0.000 description 4
- 239000003795 chemical substances by application Substances 0.000 description 4
- 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 description 4
- 238000013329 compounding Methods 0.000 description 4
- 230000007423 decrease Effects 0.000 description 4
- 229960003638 dopamine Drugs 0.000 description 4
- 238000005227 gel permeation chromatography Methods 0.000 description 4
- 239000003094 microcapsule Substances 0.000 description 4
- 229910052757 nitrogen Inorganic materials 0.000 description 4
- 238000007911 parenteral administration Methods 0.000 description 4
- 108090000765 processed proteins & peptides Proteins 0.000 description 4
- 239000000047 product Substances 0.000 description 4
- 230000001105 regulatory effect Effects 0.000 description 4
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 3
- 206010012239 Delusion Diseases 0.000 description 3
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 3
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 description 3
- 238000001816 cooling Methods 0.000 description 3
- 231100000868 delusion Toxicity 0.000 description 3
- 238000012377 drug delivery Methods 0.000 description 3
- 235000019441 ethanol Nutrition 0.000 description 3
- 230000001747 exhibiting effect Effects 0.000 description 3
- 206010022437 insomnia Diseases 0.000 description 3
- 239000004005 microsphere Substances 0.000 description 3
- 239000012299 nitrogen atmosphere Substances 0.000 description 3
- 230000006977 prepulse inhibition Effects 0.000 description 3
- 239000000651 prodrug Substances 0.000 description 3
- 229940002612 prodrug Drugs 0.000 description 3
- 239000007962 solid dispersion Substances 0.000 description 3
- 239000007858 starting material Substances 0.000 description 3
- 230000001225 therapeutic effect Effects 0.000 description 3
- 210000001519 tissue Anatomy 0.000 description 3
- 208000007415 Anhedonia Diseases 0.000 description 2
- 208000000103 Anorexia Nervosa Diseases 0.000 description 2
- 235000017060 Arachis glabrata Nutrition 0.000 description 2
- 244000105624 Arachis hypogaea Species 0.000 description 2
- 235000010777 Arachis hypogaea Nutrition 0.000 description 2
- 235000018262 Arachis monticola Nutrition 0.000 description 2
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 description 2
- 208000007590 Disorders of Excessive Somnolence Diseases 0.000 description 2
- 208000001640 Fibromyalgia Diseases 0.000 description 2
- 208000004547 Hallucinations Diseases 0.000 description 2
- 206010052904 Musculoskeletal stiffness Diseases 0.000 description 2
- UFWIBTONFRDIAS-UHFFFAOYSA-N Naphthalene Chemical compound C1=CC=CC2=CC=CC=C21 UFWIBTONFRDIAS-UHFFFAOYSA-N 0.000 description 2
- 208000002193 Pain Diseases 0.000 description 2
- 208000001431 Psychomotor Agitation Diseases 0.000 description 2
- 208000003782 Raynaud disease Diseases 0.000 description 2
- 208000012322 Raynaud phenomenon Diseases 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- 238000010171 animal model Methods 0.000 description 2
- 239000012867 bioactive agent Substances 0.000 description 2
- 230000015556 catabolic process Effects 0.000 description 2
- 208000015114 central nervous system disease Diseases 0.000 description 2
- 229960003920 cocaine Drugs 0.000 description 2
- 230000000052 comparative effect Effects 0.000 description 2
- 230000006735 deficit Effects 0.000 description 2
- 238000006731 degradation reaction Methods 0.000 description 2
- 239000003085 diluting agent Substances 0.000 description 2
- 208000024732 dysthymic disease Diseases 0.000 description 2
- 230000007613 environmental effect Effects 0.000 description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 2
- 230000006870 function Effects 0.000 description 2
- 206010020765 hypersomnia Diseases 0.000 description 2
- 230000001771 impaired effect Effects 0.000 description 2
- 239000012907 medicinal substance Substances 0.000 description 2
- 239000012803 melt mixture Substances 0.000 description 2
- 230000036651 mood Effects 0.000 description 2
- 210000001577 neostriatum Anatomy 0.000 description 2
- 239000002858 neurotransmitter agent Substances 0.000 description 2
- 239000003960 organic solvent Substances 0.000 description 2
- 235000020232 peanut Nutrition 0.000 description 2
- 239000000312 peanut oil Substances 0.000 description 2
- 239000008363 phosphate buffer Substances 0.000 description 2
- 102000004196 processed proteins & peptides Human genes 0.000 description 2
- 208000020016 psychiatric disease Diseases 0.000 description 2
- 230000009467 reduction Effects 0.000 description 2
- 238000001878 scanning electron micrograph Methods 0.000 description 2
- 239000008159 sesame oil Substances 0.000 description 2
- 239000011780 sodium chloride Substances 0.000 description 2
- 239000007787 solid Substances 0.000 description 2
- 230000010512 thermal transition Effects 0.000 description 2
- 230000009466 transformation Effects 0.000 description 2
- 239000003981 vehicle Substances 0.000 description 2
- SNICXCGAKADSCV-JTQLQIEISA-N (-)-Nicotine Chemical compound CN1CCC[C@H]1C1=CC=CN=C1 SNICXCGAKADSCV-JTQLQIEISA-N 0.000 description 1
- SFLSHLFXELFNJZ-QMMMGPOBSA-N (-)-norepinephrine Chemical compound NC[C@H](O)C1=CC=C(O)C(O)=C1 SFLSHLFXELFNJZ-QMMMGPOBSA-N 0.000 description 1
- 229930182837 (R)-adrenaline Natural products 0.000 description 1
- UCTWMZQNUQWSLP-VIFPVBQESA-N (R)-adrenaline Chemical compound CNC[C@H](O)C1=CC=C(O)C(O)=C1 UCTWMZQNUQWSLP-VIFPVBQESA-N 0.000 description 1
- KWTSXDURSIMDCE-QMMMGPOBSA-N (S)-amphetamine Chemical compound C[C@H](N)CC1=CC=CC=C1 KWTSXDURSIMDCE-QMMMGPOBSA-N 0.000 description 1
- 238000005160 1H NMR spectroscopy Methods 0.000 description 1
- 206010001540 Akathisia Diseases 0.000 description 1
- 244000144725 Amygdalus communis Species 0.000 description 1
- 235000011437 Amygdalus communis Nutrition 0.000 description 1
- 206010003225 Arteriospasm coronary Diseases 0.000 description 1
- 208000021465 Brief psychotic disease Diseases 0.000 description 1
- COVZYZSDYWQREU-UHFFFAOYSA-N Busulfan Chemical compound CS(=O)(=O)OCCCCOS(C)(=O)=O COVZYZSDYWQREU-UHFFFAOYSA-N 0.000 description 1
- 241000700199 Cavia porcellus Species 0.000 description 1
- 208000000094 Chronic Pain Diseases 0.000 description 1
- 206010010144 Completed suicide Diseases 0.000 description 1
- RYGMFSIKBFXOCR-UHFFFAOYSA-N Copper Chemical compound [Cu] RYGMFSIKBFXOCR-UHFFFAOYSA-N 0.000 description 1
- 206010011091 Coronary artery thrombosis Diseases 0.000 description 1
- 206010011971 Decreased interest Diseases 0.000 description 1
- 208000024254 Delusional disease Diseases 0.000 description 1
- 101100421425 Drosophila melanogaster Sply gene Proteins 0.000 description 1
- 206010016374 Feelings of worthlessness Diseases 0.000 description 1
- 241000282326 Felis catus Species 0.000 description 1
- 239000005715 Fructose Substances 0.000 description 1
- RFSUNEUAIZKAJO-ARQDHWQXSA-N Fructose Chemical compound OC[C@H]1O[C@](O)(CO)[C@@H](O)[C@@H]1O RFSUNEUAIZKAJO-ARQDHWQXSA-N 0.000 description 1
- 229930091371 Fructose Natural products 0.000 description 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- 241000282412 Homo Species 0.000 description 1
- 206010020710 Hyperphagia Diseases 0.000 description 1
- 206010022562 Intermittent claudication Diseases 0.000 description 1
- 206010022998 Irritability Diseases 0.000 description 1
- 241000840267 Moma Species 0.000 description 1
- 241000699666 Mus <mouse, genus> Species 0.000 description 1
- 206010028391 Musculoskeletal Pain Diseases 0.000 description 1
- PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical compound OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 description 1
- 240000007817 Olea europaea Species 0.000 description 1
- 206010034010 Parkinsonism Diseases 0.000 description 1
- 241000009328 Perro Species 0.000 description 1
- 241000288906 Primates Species 0.000 description 1
- 206010037211 Psychomotor hyperactivity Diseases 0.000 description 1
- 241000700159 Rattus Species 0.000 description 1
- 241000700157 Rattus norvegicus Species 0.000 description 1
- 241000283984 Rodentia Species 0.000 description 1
- 244000000231 Sesamum indicum Species 0.000 description 1
- 235000003434 Sesamum indicum Nutrition 0.000 description 1
- 102000005157 Somatostatin Human genes 0.000 description 1
- 108010056088 Somatostatin Proteins 0.000 description 1
- 208000011963 Substance-induced psychotic disease Diseases 0.000 description 1
- 231100000393 Substance-induced psychotic disorder Toxicity 0.000 description 1
- 206010042458 Suicidal ideation Diseases 0.000 description 1
- 206010044565 Tremor Diseases 0.000 description 1
- 229940123445 Tricyclic antidepressant Drugs 0.000 description 1
- 240000008042 Zea mays Species 0.000 description 1
- 235000005824 Zea mays ssp. parviglumis Nutrition 0.000 description 1
- 235000002017 Zea mays subsp mays Nutrition 0.000 description 1
- 231100000230 acceptable toxicity Toxicity 0.000 description 1
- 238000009825 accumulation Methods 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 150000007513 acids Chemical class 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 239000000556 agonist Substances 0.000 description 1
- 150000001298 alcohols Chemical class 0.000 description 1
- 235000020224 almond Nutrition 0.000 description 1
- 239000008168 almond oil Substances 0.000 description 1
- 150000001413 amino acids Chemical class 0.000 description 1
- 229940025084 amphetamine Drugs 0.000 description 1
- 230000003042 antagnostic effect Effects 0.000 description 1
- 230000003288 anthiarrhythmic effect Effects 0.000 description 1
- 230000001430 anti-depressive effect Effects 0.000 description 1
- 230000000561 anti-psychotic effect Effects 0.000 description 1
- 239000000935 antidepressant agent Substances 0.000 description 1
- 229940005513 antidepressants Drugs 0.000 description 1
- 230000036528 appetite Effects 0.000 description 1
- 235000019789 appetite Nutrition 0.000 description 1
- 239000007900 aqueous suspension Substances 0.000 description 1
- 230000006793 arrhythmia Effects 0.000 description 1
- 206010003119 arrhythmia Diseases 0.000 description 1
- 239000012298 atmosphere Substances 0.000 description 1
- 239000003693 atypical antipsychotic agent Substances 0.000 description 1
- 229940127236 atypical antipsychotics Drugs 0.000 description 1
- 230000004888 barrier function Effects 0.000 description 1
- 230000003542 behavioural effect Effects 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid group Chemical group C(C1=CC=CC=C1)(=O)O WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 229920000229 biodegradable polyester Polymers 0.000 description 1
- 239000004622 biodegradable polyester Substances 0.000 description 1
- 238000006065 biodegradation reaction Methods 0.000 description 1
- 230000008499 blood brain barrier function Effects 0.000 description 1
- 210000001218 blood-brain barrier Anatomy 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- 239000000872 buffer Substances 0.000 description 1
- 239000006227 byproduct Substances 0.000 description 1
- 239000004359 castor oil Substances 0.000 description 1
- 210000003710 cerebral cortex Anatomy 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 150000008280 chlorinated hydrocarbons Chemical class 0.000 description 1
- ZPEIMTDSQAKGNT-UHFFFAOYSA-N chlorpromazine Chemical compound C1=C(Cl)C=C2N(CCCN(C)C)C3=CC=CC=C3SC2=C1 ZPEIMTDSQAKGNT-UHFFFAOYSA-N 0.000 description 1
- 229960001076 chlorpromazine Drugs 0.000 description 1
- 239000011248 coating agent Substances 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 230000001149 cognitive effect Effects 0.000 description 1
- 239000012141 concentrate Substances 0.000 description 1
- 238000013267 controlled drug release Methods 0.000 description 1
- 229910052802 copper Inorganic materials 0.000 description 1
- 239000010949 copper Substances 0.000 description 1
- 235000005822 corn Nutrition 0.000 description 1
- 239000002285 corn oil Substances 0.000 description 1
- 201000011634 coronary artery vasospasm Diseases 0.000 description 1
- 208000002528 coronary thrombosis Diseases 0.000 description 1
- 239000002385 cottonseed oil Substances 0.000 description 1
- 235000012343 cottonseed oil Nutrition 0.000 description 1
- 235000019788 craving Nutrition 0.000 description 1
- 208000026725 cyclothymic disease Diseases 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 230000003111 delayed effect Effects 0.000 description 1
- 230000003001 depressive effect Effects 0.000 description 1
- 230000000994 depressogenic effect Effects 0.000 description 1
- 238000013461 design Methods 0.000 description 1
- 239000008121 dextrose Substances 0.000 description 1
- 235000005911 diet Nutrition 0.000 description 1
- 230000037213 diet Effects 0.000 description 1
- 238000001938 differential scanning calorimetry curve Methods 0.000 description 1
- 239000002270 dispersing agent Substances 0.000 description 1
- 239000006185 dispersion Substances 0.000 description 1
- 239000012153 distilled water Substances 0.000 description 1
- 238000009513 drug distribution Methods 0.000 description 1
- 208000010118 dystonia Diseases 0.000 description 1
- 230000002996 emotional effect Effects 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 230000003511 endothelial effect Effects 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 229960005139 epinephrine Drugs 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 230000005713 exacerbation Effects 0.000 description 1
- 230000002349 favourable effect Effects 0.000 description 1
- 125000000524 functional group Chemical group 0.000 description 1
- 230000004927 fusion Effects 0.000 description 1
- PCHJSUWPFVWCPO-UHFFFAOYSA-N gold Chemical compound [Au] PCHJSUWPFVWCPO-UHFFFAOYSA-N 0.000 description 1
- 229910052737 gold Inorganic materials 0.000 description 1
- 239000010931 gold Substances 0.000 description 1
- 210000005003 heart tissue Anatomy 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- UWYVPFMHMJIBHE-OWOJBTEDSA-N hydroxymaleic acid group Chemical group O/C(/C(=O)O)=C/C(=O)O UWYVPFMHMJIBHE-OWOJBTEDSA-N 0.000 description 1
- 230000001505 hypomanic effect Effects 0.000 description 1
- 239000007972 injectable composition Substances 0.000 description 1
- 238000009434 installation Methods 0.000 description 1
- 230000010354 integration Effects 0.000 description 1
- 208000021156 intermittent vascular claudication Diseases 0.000 description 1
- 238000010255 intramuscular injection Methods 0.000 description 1
- 239000007927 intramuscular injection Substances 0.000 description 1
- 238000010902 jet-milling Methods 0.000 description 1
- 238000009533 lab test Methods 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 229940126601 medicinal product Drugs 0.000 description 1
- 201000003995 melancholia Diseases 0.000 description 1
- 230000002503 metabolic effect Effects 0.000 description 1
- CWWARWOPSKGELM-SARDKLJWSA-N methyl (2s)-2-[[(2s)-2-[[2-[[(2s)-2-[[(2s)-2-[[(2s)-5-amino-2-[[(2s)-5-amino-2-[[(2s)-1-[(2s)-6-amino-2-[[(2s)-1-[(2s)-2-amino-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoyl]amino]-5 Chemical compound C([C@@H](C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)OC)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CCCCN)NC(=O)[C@H]1N(CCC1)C(=O)[C@@H](N)CCCN=C(N)N)C1=CC=CC=C1 CWWARWOPSKGELM-SARDKLJWSA-N 0.000 description 1
- 239000011812 mixed powder Substances 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 239000000178 monomer Substances 0.000 description 1
- 238000000465 moulding Methods 0.000 description 1
- 230000001537 neural effect Effects 0.000 description 1
- 230000001722 neurochemical effect Effects 0.000 description 1
- 239000003176 neuroleptic agent Substances 0.000 description 1
- 239000003076 neurotropic agent Substances 0.000 description 1
- 229960002715 nicotine Drugs 0.000 description 1
- SNICXCGAKADSCV-UHFFFAOYSA-N nicotine Natural products CN1CCCC1C1=CC=CN=C1 SNICXCGAKADSCV-UHFFFAOYSA-N 0.000 description 1
- 229960003512 nicotinic acid Drugs 0.000 description 1
- 235000001968 nicotinic acid Nutrition 0.000 description 1
- 239000011664 nicotinic acid Substances 0.000 description 1
- 231100000252 nontoxic Toxicity 0.000 description 1
- 230000003000 nontoxic effect Effects 0.000 description 1
- SFLSHLFXELFNJZ-UHFFFAOYSA-N norepinephrine Natural products NCC(O)C1=CC=C(O)C(O)=C1 SFLSHLFXELFNJZ-UHFFFAOYSA-N 0.000 description 1
- 229960002748 norepinephrine Drugs 0.000 description 1
- 239000012053 oil suspension Substances 0.000 description 1
- 239000004006 olive oil Substances 0.000 description 1
- 238000000879 optical micrograph Methods 0.000 description 1
- 238000000399 optical microscopy Methods 0.000 description 1
- 150000002894 organic compounds Chemical class 0.000 description 1
- 235000020830 overeating Nutrition 0.000 description 1
- 208000002851 paranoid schizophrenia Diseases 0.000 description 1
- 238000003921 particle size analysis Methods 0.000 description 1
- 230000001575 pathological effect Effects 0.000 description 1
- 230000008447 perception Effects 0.000 description 1
- 230000002085 persistent effect Effects 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 229940127557 pharmaceutical product Drugs 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- WVDDGKGOMKODPV-ZQBYOMGUSA-N phenyl(114C)methanol Chemical compound O[14CH2]C1=CC=CC=C1 WVDDGKGOMKODPV-ZQBYOMGUSA-N 0.000 description 1
- 238000012667 polymer degradation Methods 0.000 description 1
- -1 polyphosphoesters Polymers 0.000 description 1
- 230000003334 potential effect Effects 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 238000012545 processing Methods 0.000 description 1
- 230000000541 pulsatile effect Effects 0.000 description 1
- 230000000306 recurrent effect Effects 0.000 description 1
- 238000012552 review Methods 0.000 description 1
- 238000011808 rodent model Methods 0.000 description 1
- 239000012488 sample solution Substances 0.000 description 1
- 208000022610 schizoaffective disease Diseases 0.000 description 1
- 230000001932 seasonal effect Effects 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 210000004911 serous fluid Anatomy 0.000 description 1
- 235000011803 sesame oil Nutrition 0.000 description 1
- 238000007873 sieving Methods 0.000 description 1
- 208000022925 sleep disturbance Diseases 0.000 description 1
- 150000003384 small molecules Chemical class 0.000 description 1
- 239000008247 solid mixture Substances 0.000 description 1
- NHXLMOGPVYXJNR-ATOGVRKGSA-N somatostatin Chemical compound C([C@H]1C(=O)N[C@H](C(N[C@@H](CO)C(=O)N[C@@H](CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CC=2C3=CC=CC=C3NC=2)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(=O)N1)[C@@H](C)O)NC(=O)CNC(=O)[C@H](C)N)C(O)=O)=O)[C@H](O)C)C1=CC=CC=C1 NHXLMOGPVYXJNR-ATOGVRKGSA-N 0.000 description 1
- 229960000553 somatostatin Drugs 0.000 description 1
- 238000001228 spectrum Methods 0.000 description 1
- 239000012798 spherical particle Substances 0.000 description 1
- 229910001220 stainless steel Inorganic materials 0.000 description 1
- 239000010935 stainless steel Substances 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 208000011580 syndromic disease Diseases 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 230000002110 toxicologic effect Effects 0.000 description 1
- 231100000027 toxicology Toxicity 0.000 description 1
- 238000012549 training Methods 0.000 description 1
- 230000007704 transition Effects 0.000 description 1
- 239000003029 tricyclic antidepressant agent Substances 0.000 description 1
- 238000000870 ultraviolet spectroscopy Methods 0.000 description 1
- 210000002700 urine Anatomy 0.000 description 1
- 230000002792 vascular Effects 0.000 description 1
- 235000013311 vegetables Nutrition 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 150000003722 vitamin derivatives Chemical class 0.000 description 1
- 230000003442 weekly effect Effects 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
- 230000004584 weight gain Effects 0.000 description 1
- 235000019786 weight gain Nutrition 0.000 description 1
- 230000004580 weight loss Effects 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1641—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
- A61K9/1647—Polyesters, e.g. poly(lactide-co-glycolide)
-
- 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
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
- A61P25/18—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
- A61P25/30—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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (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)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Heart & Thoracic Surgery (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Cardiology (AREA)
- Pain & Pain Management (AREA)
- Addiction (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Anesthesiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Hydrogenated Pyridines (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Biological Depolymerization Polymers (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US21298698A | 1998-12-16 | 1998-12-16 | |
| PCT/US1999/027705 WO2000035423A1 (fr) | 1998-12-16 | 1999-11-22 | Antagoniste du recepteur de la serotonine, encapsule dans du polymere biodegradable et son procede de preparation |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| UA73101C2 true UA73101C2 (en) | 2005-06-15 |
Family
ID=22793267
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| UA2001064165A UA73101C2 (en) | 1998-12-16 | 1999-11-22 | Antagonist of serotonin receptor encapsulated by biodegradable polymer and method for its manufacture |
Country Status (35)
| Country | Link |
|---|---|
| EP (1) | EP1140026B1 (fr) |
| JP (1) | JP4759141B2 (fr) |
| KR (1) | KR100707710B1 (fr) |
| CN (1) | CN1195497C (fr) |
| AP (1) | AP1769A (fr) |
| AR (1) | AR021652A1 (fr) |
| AT (1) | ATE303795T1 (fr) |
| AU (1) | AU770673B2 (fr) |
| BG (1) | BG65500B1 (fr) |
| BR (1) | BR9916276A (fr) |
| CA (1) | CA2355077C (fr) |
| CR (1) | CR6424A (fr) |
| CZ (1) | CZ301947B6 (fr) |
| DE (1) | DE69927177T2 (fr) |
| DK (1) | DK1140026T3 (fr) |
| EA (1) | EA004502B1 (fr) |
| EE (1) | EE200100314A (fr) |
| ES (1) | ES2245128T3 (fr) |
| HK (1) | HK1041645B (fr) |
| HR (1) | HRP20010446A2 (fr) |
| HU (1) | HU226586B1 (fr) |
| ID (1) | ID28909A (fr) |
| IL (2) | IL143761A0 (fr) |
| ME (2) | MEP19408A (fr) |
| NO (1) | NO20012981L (fr) |
| NZ (1) | NZ511962A (fr) |
| OA (1) | OA11728A (fr) |
| PL (1) | PL196822B1 (fr) |
| RS (1) | RS50123B (fr) |
| SK (1) | SK285812B6 (fr) |
| TR (1) | TR200101759T2 (fr) |
| TW (1) | TWI221418B (fr) |
| UA (1) | UA73101C2 (fr) |
| WO (1) | WO2000035423A1 (fr) |
| ZA (1) | ZA200104899B (fr) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10061932A1 (de) * | 2000-12-13 | 2002-10-24 | Pharmatech Gmbh | Wirkstoffhaltige Mikropartikel und Verfahren zur Herstellung der Mikropartikel durch Abrasion |
| AU2002256694A1 (en) * | 2001-03-20 | 2002-10-03 | Euroscreen S.A. | Screening, diagnostic and/or dosage method and device of an agonist and/or antagonist for a calcium-coupled receptor |
| PL364054A1 (en) | 2001-05-23 | 2004-12-13 | Hexal Ag | Homogenised product for implants and microparticles |
| US20050215561A1 (en) * | 2004-03-19 | 2005-09-29 | Krishnendu Ghosh | Pharmaceutical dosage forms and compositions |
| KR20070059161A (ko) * | 2004-09-21 | 2007-06-11 | 산동 루예 파마슈티칼 컴파니 리미티드 | 도파민 수용체 효능제를 함유하는 장시간 작용 서방성 제제및 그 제조방법 |
| MX2010009990A (es) | 2008-03-11 | 2010-12-15 | Depomed Inc | Formas de dosificación gástricas retentivas de liberación prolongada que comprenden combinaciones de un analgésico no opioide y un analgésico opioide. |
| US8372432B2 (en) | 2008-03-11 | 2013-02-12 | Depomed, Inc. | Gastric retentive extended-release dosage forms comprising combinations of a non-opioid analgesic and an opioid analgesic |
| CA2737257C (fr) * | 2008-09-18 | 2016-11-15 | Purdue Pharma L.P. | Formes galeniques comprenant de la poly(.epsilon.-caprolactone) |
| US20100291214A1 (en) * | 2008-12-23 | 2010-11-18 | Armark Authentication Technologies, Llc | Three-dimensional microfiber extrudate structure and process for forming three-dimensional microfiber extrudate structure |
| WO2010151746A2 (fr) * | 2009-06-26 | 2010-12-29 | Armark Authentication Technologies, Llc | Structure d'extrudat en microfibres tridimensionnelle et procédé de formation de la structure d'extrudat en microfibre tridimensionnelle |
| US8597681B2 (en) | 2009-12-22 | 2013-12-03 | Mallinckrodt Llc | Methods of producing stabilized solid dosage pharmaceutical compositions containing morphinans |
| US9198861B2 (en) | 2009-12-22 | 2015-12-01 | Mallinckrodt Llc | Methods of producing stabilized solid dosage pharmaceutical compositions containing morphinans |
| US9050335B1 (en) | 2011-05-17 | 2015-06-09 | Mallinckrodt Llc | Pharmaceutical compositions for extended release of oxycodone and acetaminophen resulting in a quick onset and prolonged period of analgesia |
| US8858963B1 (en) | 2011-05-17 | 2014-10-14 | Mallinckrodt Llc | Tamper resistant composition comprising hydrocodone and acetaminophen for rapid onset and extended duration of analgesia |
| US8741885B1 (en) | 2011-05-17 | 2014-06-03 | Mallinckrodt Llc | Gastric retentive extended release pharmaceutical compositions |
| US20160193151A1 (en) * | 2015-01-06 | 2016-07-07 | Maria Del Pilar Noriega Escobar | Dosage form incorporating an amorphous drug solid solution |
| US11672755B2 (en) * | 2019-12-31 | 2023-06-13 | Wanka Tanka Ltd. | Extended release plastic formulation |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4389330A (en) * | 1980-10-06 | 1983-06-21 | Stolle Research And Development Corporation | Microencapsulation process |
| DE3612212A1 (de) * | 1986-04-11 | 1987-10-15 | Basf Ag | Verfahren zur herstellung von festen pharmazeutischen formen |
| CH679207A5 (fr) * | 1989-07-28 | 1992-01-15 | Debiopharm Sa | |
| US5439688A (en) * | 1989-07-28 | 1995-08-08 | Debio Recherche Pharmaceutique S.A. | Process for preparing a pharmaceutical composition |
| DE69133136T2 (de) * | 1990-05-16 | 2003-06-18 | Southern Research Institute, Birmingham | Mikrokapseln mit gesteuerter freigabe sowie deren verwendung zur stimulierung des nervenfaserwachstums |
| AU652759B2 (en) * | 1990-06-01 | 1994-09-08 | Aventisub Ii Inc. | (+)-alpha-(2,3-dimethoxyphenyl)-1-(2-(4-fluorophenyl)ethyl)- 4-piperidinemethanol |
| GB9016885D0 (en) * | 1990-08-01 | 1990-09-12 | Scras | Sustained release pharmaceutical compositions |
| KR0182801B1 (ko) * | 1991-04-16 | 1999-05-01 | 아만 히데아키 | 고체 분산체의 제조방법 |
| US5505963A (en) * | 1993-04-07 | 1996-04-09 | Schwartz Pharma Ag | Slow release pharmaceutical preparation |
| US5456917A (en) * | 1993-04-12 | 1995-10-10 | Cambridge Scientific, Inc. | Method for making a bioerodible material for the sustained release of a medicament and the material made from the method |
| BR9509985A (pt) * | 1995-12-12 | 1998-11-03 | Omeros Med Sys Inc | Solução para irrigação e método para inibição de dor inflamação e esparmo |
-
1999
- 1999-11-22 DK DK99960556T patent/DK1140026T3/da active
- 1999-11-22 ES ES99960556T patent/ES2245128T3/es not_active Expired - Lifetime
- 1999-11-22 CZ CZ20012157A patent/CZ301947B6/cs not_active IP Right Cessation
- 1999-11-22 KR KR1020017007561A patent/KR100707710B1/ko not_active IP Right Cessation
- 1999-11-22 NZ NZ511962A patent/NZ511962A/xx not_active IP Right Cessation
- 1999-11-22 EA EA200100551A patent/EA004502B1/ru not_active IP Right Cessation
- 1999-11-22 AT AT99960556T patent/ATE303795T1/de active
- 1999-11-22 AP APAP/P/2001/002198A patent/AP1769A/en active
- 1999-11-22 DE DE69927177T patent/DE69927177T2/de not_active Expired - Lifetime
- 1999-11-22 ME MEP-194/08A patent/MEP19408A/xx unknown
- 1999-11-22 IL IL14376199A patent/IL143761A0/xx active IP Right Grant
- 1999-11-22 ID IDW00200101296A patent/ID28909A/id unknown
- 1999-11-22 HU HU0105048A patent/HU226586B1/hu not_active IP Right Cessation
- 1999-11-22 CN CNB998145831A patent/CN1195497C/zh not_active Expired - Fee Related
- 1999-11-22 CA CA002355077A patent/CA2355077C/fr not_active Expired - Fee Related
- 1999-11-22 UA UA2001064165A patent/UA73101C2/uk unknown
- 1999-11-22 TR TR2001/01759T patent/TR200101759T2/xx unknown
- 1999-11-22 BR BR9916276-8A patent/BR9916276A/pt not_active Application Discontinuation
- 1999-11-22 SK SK828-2001A patent/SK285812B6/sk not_active IP Right Cessation
- 1999-11-22 ME MEP-2008-194A patent/ME00066B/me unknown
- 1999-11-22 RS YUP-414/01A patent/RS50123B/sr unknown
- 1999-11-22 JP JP2000587744A patent/JP4759141B2/ja not_active Expired - Fee Related
- 1999-11-22 EE EEP200100314A patent/EE200100314A/xx unknown
- 1999-11-22 OA OA1200100150A patent/OA11728A/en unknown
- 1999-11-22 EP EP99960556A patent/EP1140026B1/fr not_active Expired - Lifetime
- 1999-11-22 WO PCT/US1999/027705 patent/WO2000035423A1/fr active IP Right Grant
- 1999-11-22 PL PL348233A patent/PL196822B1/pl not_active IP Right Cessation
- 1999-11-22 AU AU17425/00A patent/AU770673B2/en not_active Ceased
- 1999-12-10 TW TW088121702A patent/TWI221418B/zh not_active IP Right Cessation
- 1999-12-14 AR ARP990106345A patent/AR021652A1/es unknown
-
2001
- 2001-06-12 BG BG105591A patent/BG65500B1/bg unknown
- 2001-06-14 HR HR20010446A patent/HRP20010446A2/hr not_active Application Discontinuation
- 2001-06-14 IL IL143761A patent/IL143761A/en not_active IP Right Cessation
- 2001-06-14 ZA ZA200104899A patent/ZA200104899B/en unknown
- 2001-06-15 NO NO20012981A patent/NO20012981L/no not_active Application Discontinuation
- 2001-07-16 CR CR6424A patent/CR6424A/es not_active Application Discontinuation
-
2002
- 2002-05-04 HK HK02103401.5A patent/HK1041645B/zh not_active IP Right Cessation
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| UA73101C2 (en) | Antagonist of serotonin receptor encapsulated by biodegradable polymer and method for its manufacture | |
| EP2968320B1 (fr) | Composés organiques | |
| US6455526B1 (en) | Biodegradable polymer encapsulated pharmaceutical compositions and method for preparing the same | |
| US20150148366A1 (en) | Particulates | |
| HU211845A9 (en) | Orally administrated solvent-free pharmaceutical composition with delayed active-substance release and a method for preparing thereof | |
| Jedinger et al. | Development of an abuse-and alcohol-resistant formulation based on hot-melt extrusion and film coating | |
| Manini et al. | Paliperidone palmitate as model of heat-sensitive drug for long-acting 3D printing application | |
| CA3023795C (fr) | Utilisation de sucre amine comme plastifiant | |
| Xu et al. | Porous core/dense shell PLA microspheres embedded with high drug loading of bupivacaine crystals for injectable prolonged release | |
| US4902516A (en) | Binder-free granules with delayed release of the active compound | |
| Tamaddon et al. | Thermoanalytical characterization of clindamycin-loaded intravitreal implants prepared by hot melt extrusion | |
| DE3701625A1 (de) | Perorale arzneimittelzubereitung mit verzoegerter wirkstofffreigabe | |
| MXPA01005920A (es) | Antagonista del receptor de serotonina encapsulada de polimero biodegradable y metodo para preparar el mismo | |
| JP2003522097A (ja) | 可溶化デリバリーシステムおよび製造方法 | |
| WATER | PHARMACEUTICAL SCIENCES | |
| Kapote | Improving solubility and supersaturation of poorly soluble drugs using solid dispersions based on natural polymers and mixtures thereof | |
| Alqahtani | Controlled release oral dosage forms using functional additives in hot melt extruded pharmaceuticals | |
| Kallakunta | A Novel Dimension of Twin-Screw Technology for Controlled Release and Solubility Enhancement: Study on Effect of Formulation and Process Parameters | |
| GGLLGGGGGG | GGLGLGLGLSS GGGLGG LGGGLGGGGG LGGGGGG SLLLLaaLLL S LLLL STRENGTH |