JP2005525308A5 - - Google Patents
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- Publication number
- JP2005525308A5 JP2005525308A5 JP2003557529A JP2003557529A JP2005525308A5 JP 2005525308 A5 JP2005525308 A5 JP 2005525308A5 JP 2003557529 A JP2003557529 A JP 2003557529A JP 2003557529 A JP2003557529 A JP 2003557529A JP 2005525308 A5 JP2005525308 A5 JP 2005525308A5
- Authority
- JP
- Japan
- Prior art keywords
- insulin
- dosage form
- oral
- concentration
- blood glucose
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims 158
- 102000004877 Insulin Human genes 0.000 claims 74
- 108090001061 Insulin Proteins 0.000 claims 74
- 229940125396 insulin Drugs 0.000 claims 74
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 34
- 239000008103 glucose Substances 0.000 claims 34
- 210000004369 blood Anatomy 0.000 claims 32
- 239000008280 blood Substances 0.000 claims 32
- 206010012601 diabetes mellitus Diseases 0.000 claims 31
- 238000011282 treatment Methods 0.000 claims 20
- 239000006186 oral dosage form Substances 0.000 claims 17
- 239000008184 oral solid dosage form Substances 0.000 claims 17
- 230000001684 chronic effect Effects 0.000 claims 14
- 239000000126 substance Substances 0.000 claims 14
- 239000003814 drug Substances 0.000 claims 11
- 108090000623 proteins and genes Proteins 0.000 claims 11
- 238000010521 absorption reaction Methods 0.000 claims 9
- 238000000034 method Methods 0.000 claims 9
- 210000001035 gastrointestinal tract Anatomy 0.000 claims 8
- 238000010254 subcutaneous injection Methods 0.000 claims 8
- 239000007929 subcutaneous injection Substances 0.000 claims 8
- 230000014509 gene expression Effects 0.000 claims 7
- 239000002552 dosage form Substances 0.000 claims 6
- 210000002966 serum Anatomy 0.000 claims 6
- 229940125395 oral insulin Drugs 0.000 claims 5
- 229910052736 halogen Chemical group 0.000 claims 4
- 150000002367 halogens Chemical group 0.000 claims 4
- 238000004519 manufacturing process Methods 0.000 claims 4
- 208000019553 vascular disease Diseases 0.000 claims 4
- 108090000695 Cytokines Proteins 0.000 claims 3
- 102000004127 Cytokines Human genes 0.000 claims 3
- 241001465754 Metazoa Species 0.000 claims 3
- 238000002347 injection Methods 0.000 claims 3
- 239000007924 injection Substances 0.000 claims 3
- -1 jun B Proteins 0.000 claims 3
- 238000007726 management method Methods 0.000 claims 3
- 235000012054 meals Nutrition 0.000 claims 3
- 230000007170 pathology Effects 0.000 claims 3
- 210000005259 peripheral blood Anatomy 0.000 claims 3
- 239000011886 peripheral blood Substances 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 238000007920 subcutaneous administration Methods 0.000 claims 3
- 206010060378 Hyperinsulinaemia Diseases 0.000 claims 2
- 101710135898 Myc proto-oncogene protein Proteins 0.000 claims 2
- 102100038895 Myc proto-oncogene protein Human genes 0.000 claims 2
- 102000010752 Plasminogen Inactivators Human genes 0.000 claims 2
- 108010077971 Plasminogen Inactivators Proteins 0.000 claims 2
- 101710150448 Transcriptional regulator Myc Proteins 0.000 claims 2
- 208000024248 Vascular System injury Diseases 0.000 claims 2
- 208000012339 Vascular injury Diseases 0.000 claims 2
- 125000002947 alkylene group Chemical group 0.000 claims 2
- 235000005911 diet Nutrition 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 230000003451 hyperinsulinaemic effect Effects 0.000 claims 2
- 201000008980 hyperinsulinism Diseases 0.000 claims 2
- 108020004999 messenger RNA Proteins 0.000 claims 2
- 230000001575 pathological effect Effects 0.000 claims 2
- 239000002797 plasminogen activator inhibitor Substances 0.000 claims 2
- 230000000770 proinflammatory effect Effects 0.000 claims 2
- 238000011084 recovery Methods 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000007787 solid Substances 0.000 claims 2
- 230000009885 systemic effect Effects 0.000 claims 2
- 230000001225 therapeutic effect Effects 0.000 claims 2
- GCVGCXMTCJMBHY-UHFFFAOYSA-N 4-[(4-chloro-2-hydroxybenzoyl)amino]butanoic acid Chemical group OC(=O)CCCNC(=O)C1=CC=C(Cl)C=C1O GCVGCXMTCJMBHY-UHFFFAOYSA-N 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 101001011741 Bos taurus Insulin Proteins 0.000 claims 1
- 108010075254 C-Peptide Proteins 0.000 claims 1
- 206010007559 Cardiac failure congestive Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
- 101150031329 Ets1 gene Proteins 0.000 claims 1
- 208000002705 Glucose Intolerance Diseases 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- 101000976075 Homo sapiens Insulin Proteins 0.000 claims 1
- 206010058222 Hypertensive cardiomyopathy Diseases 0.000 claims 1
- 101100444898 Mus musculus Egr1 gene Proteins 0.000 claims 1
- 101100445499 Neurospora crassa (strain ATCC 24698 / 74-OR23-1A / CBS 708.71 / DSM 1257 / FGSC 987) erg-1 gene Proteins 0.000 claims 1
- 108010005991 Pork Regular Insulin Proteins 0.000 claims 1
- 102000007568 Proto-Oncogene Proteins c-fos Human genes 0.000 claims 1
- 108010071563 Proto-Oncogene Proteins c-fos Proteins 0.000 claims 1
- 208000017442 Retinal disease Diseases 0.000 claims 1
- 206010038923 Retinopathy Diseases 0.000 claims 1
- 208000007536 Thrombosis Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 125000004450 alkenylene group Chemical group 0.000 claims 1
- 229940124277 aminobutyric acid Drugs 0.000 claims 1
- 238000004458 analytical method Methods 0.000 claims 1
- 125000000732 arylene group Chemical group 0.000 claims 1
- 230000017531 blood circulation Effects 0.000 claims 1
- IXIBAKNTJSCKJM-BUBXBXGNSA-N bovine insulin Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@H]1CSSC[C@H]2C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@H](C(N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC=3C=CC(O)=CC=3)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=3C=CC(O)=CC=3)C(=O)N[C@@H](CSSC[C@H](NC(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=3C=CC(O)=CC=3)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=3NC=NC=3)NC(=O)[C@H](CO)NC(=O)CNC1=O)C(=O)NCC(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(O)=O)C(=O)N[C@@H](CC(N)=O)C(O)=O)=O)CSSC[C@@H](C(N2)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](NC(=O)CN)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H](N)CC=1C=CC=CC=1)C(C)C)C1=CN=CN1 IXIBAKNTJSCKJM-BUBXBXGNSA-N 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 239000000460 chlorine Substances 0.000 claims 1
- 230000004087 circulation Effects 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 208000029078 coronary artery disease Diseases 0.000 claims 1
- 230000037213 diet Effects 0.000 claims 1
- 230000000378 dietary effect Effects 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 238000001647 drug administration Methods 0.000 claims 1
- 238000007877 drug screening Methods 0.000 claims 1
- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical compound NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 claims 1
- 210000001156 gastric mucosa Anatomy 0.000 claims 1
- 230000014101 glucose homeostasis Effects 0.000 claims 1
- 238000011221 initial treatment Methods 0.000 claims 1
- PBGKTOXHQIOBKM-FHFVDXKLSA-N insulin (human) Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@H]1CSSC[C@H]2C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@H](C(N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC=3C=CC(O)=CC=3)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=3C=CC(O)=CC=3)C(=O)N[C@@H](CSSC[C@H](NC(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=3C=CC(O)=CC=3)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=3NC=NC=3)NC(=O)[C@H](CO)NC(=O)CNC1=O)C(=O)NCC(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)C(=O)N[C@@H](CC(N)=O)C(O)=O)=O)CSSC[C@@H](C(N2)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](NC(=O)CN)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H](N)CC=1C=CC=CC=1)C(C)C)C1=CN=CN1 PBGKTOXHQIOBKM-FHFVDXKLSA-N 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 230000003859 lipid peroxidation Effects 0.000 claims 1
- 230000009525 mild injury Effects 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 230000007823 neuropathy Effects 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 201000009104 prediabetes syndrome Diseases 0.000 claims 1
- 238000009101 premedication Methods 0.000 claims 1
- 239000007909 solid dosage form Substances 0.000 claims 1
- 210000005166 vasculature Anatomy 0.000 claims 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US34674602P | 2002-01-07 | 2002-01-07 | |
| US34731202P | 2002-01-09 | 2002-01-09 | |
| US36861702P | 2002-03-29 | 2002-03-29 | |
| US37497902P | 2002-04-23 | 2002-04-23 | |
| US38936402P | 2002-06-17 | 2002-06-17 | |
| US10/237,138 US20030198666A1 (en) | 2002-01-07 | 2002-09-06 | Oral insulin therapy |
| PCT/US2003/000337 WO2003057170A2 (en) | 2002-01-07 | 2003-01-07 | Oral insulin therapy |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2005525308A JP2005525308A (ja) | 2005-08-25 |
| JP2005525308A5 true JP2005525308A5 (https=) | 2006-03-02 |
| JP4659358B2 JP4659358B2 (ja) | 2011-03-30 |
Family
ID=27559275
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003557529A Expired - Fee Related JP4659358B2 (ja) | 2002-01-07 | 2003-01-07 | 経口インスリン療法 |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US20030198666A1 (https=) |
| EP (1) | EP1469812B1 (https=) |
| JP (1) | JP4659358B2 (https=) |
| AU (1) | AU2003226436B2 (https=) |
| CA (1) | CA2471769C (https=) |
| WO (1) | WO2003057170A2 (https=) |
Families Citing this family (103)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
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| US9006175B2 (en) | 1999-06-29 | 2015-04-14 | Mannkind Corporation | Potentiation of glucose elimination |
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| CA2511530C (en) * | 2003-01-06 | 2013-07-09 | Emisphere Technologies, Inc. | Night-time oral insulin therapy |
| EP1605895A4 (en) * | 2003-03-06 | 2011-08-24 | Emisphere Tech Inc | ORAL INSULIN THERAPIES AND PROTOCOL |
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| EA014685B1 (ru) | 2003-04-25 | 2010-12-30 | Джилид Сайэнс, Инк. | Фосфонатсодержащие антивирусные соединения (варианты) и фармацевтическая композиция на их основе |
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| US20110046053A1 (en) | 2008-05-05 | 2011-02-24 | Oramed Ltd. | Methods and compositions for oral administration of exenatide |
| ES2929343T3 (es) | 2008-06-13 | 2022-11-28 | Mannkind Corp | Inhalador de polvo seco accionado por aspiración para la administración de fármacos |
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