JP2013533241A5 - - Google Patents
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- JP2013533241A5 JP2013533241A5 JP2013516682A JP2013516682A JP2013533241A5 JP 2013533241 A5 JP2013533241 A5 JP 2013533241A5 JP 2013516682 A JP2013516682 A JP 2013516682A JP 2013516682 A JP2013516682 A JP 2013516682A JP 2013533241 A5 JP2013533241 A5 JP 2013533241A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutical composition
- controlled release
- active agent
- release pharmaceutical
- composition according
- 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.)
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- 238000013270 controlled release Methods 0.000 claims 40
- 239000008194 pharmaceutical composition Substances 0.000 claims 34
- 239000013543 active substance Substances 0.000 claims 21
- 238000013268 sustained release Methods 0.000 claims 20
- 239000012730 sustained-release form Substances 0.000 claims 20
- 230000009246 food effect Effects 0.000 claims 16
- 235000021471 food effect Nutrition 0.000 claims 16
- 239000000203 mixture Substances 0.000 claims 16
- XZWYZXLIPXDOLR-UHFFFAOYSA-N metformin Chemical group CN(C)C(=N)NC(N)=N XZWYZXLIPXDOLR-UHFFFAOYSA-N 0.000 claims 13
- 239000012729 immediate-release (IR) formulation Substances 0.000 claims 12
- 229960003105 metformin Drugs 0.000 claims 11
- 239000003795 chemical substances by application Substances 0.000 claims 9
- 238000000034 method Methods 0.000 claims 7
- 239000002552 dosage form Substances 0.000 claims 6
- 239000003607 modifier Substances 0.000 claims 6
- 239000003472 antidiabetic agent Substances 0.000 claims 5
- 229940126904 hypoglycaemic agent Drugs 0.000 claims 5
- -1 glipiride Chemical compound 0.000 claims 4
- 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 4
- 238000010521 absorption reaction Methods 0.000 claims 3
- 239000003112 inhibitor Substances 0.000 claims 3
- OETHQSJEHLVLGH-UHFFFAOYSA-N metformin hydrochloride Chemical compound Cl.CN(C)C(=N)N=C(N)N OETHQSJEHLVLGH-UHFFFAOYSA-N 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 102000004862 Gastrin releasing peptide Human genes 0.000 claims 2
- 108090001053 Gastrin releasing peptide Proteins 0.000 claims 2
- DTHNMHAUYICORS-KTKZVXAJSA-N Glucagon-like peptide 1 Chemical class C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1N=CNC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 DTHNMHAUYICORS-KTKZVXAJSA-N 0.000 claims 2
- 102100033839 Glucose-dependent insulinotropic receptor Human genes 0.000 claims 2
- 101710163236 Glucose-dependent insulinotropic receptor Proteins 0.000 claims 2
- 102000004877 Insulin Human genes 0.000 claims 2
- 108090001061 Insulin Proteins 0.000 claims 2
- YASAKCUCGLMORW-UHFFFAOYSA-N Rosiglitazone Chemical compound C=1C=CC=NC=1N(C)CCOC(C=C1)=CC=C1CC1SC(=O)NC1=O YASAKCUCGLMORW-UHFFFAOYSA-N 0.000 claims 2
- 108091006269 SLC5A2 Proteins 0.000 claims 2
- 102000058081 Sodium-Glucose Transporter 2 Human genes 0.000 claims 2
- 229940123464 Thiazolidinedione Drugs 0.000 claims 2
- 102000008233 Toll-Like Receptor 4 Human genes 0.000 claims 2
- 108010060804 Toll-Like Receptor 4 Proteins 0.000 claims 2
- 239000000556 agonist Substances 0.000 claims 2
- 239000005557 antagonist Substances 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- PUBCCFNQJQKCNC-XKNFJVFFSA-N gastrin-releasingpeptide Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(N)=O)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H](CC(N)=O)NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)CNC(=O)CNC(=O)[C@H](C)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CC(C)C)NC(=O)[C@H]1N(CCC1)C(=O)[C@@H](N)C(C)C)[C@@H](C)O)C(C)C)[C@@H](C)O)C(C)C)C1=CNC=N1 PUBCCFNQJQKCNC-XKNFJVFFSA-N 0.000 claims 2
- JYGXADMDTFJGBT-VWUMJDOOSA-N hydrocortisone Chemical compound O=C1CC[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 JYGXADMDTFJGBT-VWUMJDOOSA-N 0.000 claims 2
- 229940125396 insulin Drugs 0.000 claims 2
- 238000011835 investigation Methods 0.000 claims 2
- 229960004329 metformin hydrochloride Drugs 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- HYAFETHFCAUJAY-UHFFFAOYSA-N pioglitazone Chemical compound N1=CC(CC)=CC=C1CCOC(C=C1)=CC=C1CC1C(=O)NC(=O)S1 HYAFETHFCAUJAY-UHFFFAOYSA-N 0.000 claims 2
- 150000001467 thiazolidinediones Chemical class 0.000 claims 2
- XUFXOAAUWZOOIT-SXARVLRPSA-N (2R,3R,4R,5S,6R)-5-[[(2R,3R,4R,5S,6R)-5-[[(2R,3R,4S,5S,6R)-3,4-dihydroxy-6-methyl-5-[[(1S,4R,5S,6S)-4,5,6-trihydroxy-3-(hydroxymethyl)-1-cyclohex-2-enyl]amino]-2-oxanyl]oxy]-3,4-dihydroxy-6-(hydroxymethyl)-2-oxanyl]oxy]-6-(hydroxymethyl)oxane-2,3,4-triol Chemical compound O([C@H]1O[C@H](CO)[C@H]([C@@H]([C@H]1O)O)O[C@H]1O[C@@H]([C@H]([C@H](O)[C@H]1O)N[C@@H]1[C@@H]([C@@H](O)[C@H](O)C(CO)=C1)O)C)[C@@H]1[C@@H](CO)O[C@@H](O)[C@H](O)[C@H]1O XUFXOAAUWZOOIT-SXARVLRPSA-N 0.000 claims 1
- BOVGTQGAOIONJV-BETUJISGSA-N 1-[(3ar,6as)-3,3a,4,5,6,6a-hexahydro-1h-cyclopenta[c]pyrrol-2-yl]-3-(4-methylphenyl)sulfonylurea Chemical compound C1=CC(C)=CC=C1S(=O)(=O)NC(=O)NN1C[C@H]2CCC[C@H]2C1 BOVGTQGAOIONJV-BETUJISGSA-N 0.000 claims 1
- TYNLGDBUJLVSMA-UHFFFAOYSA-N 4,5-diacetyloxy-9,10-dioxo-2-anthracenecarboxylic acid Chemical compound O=C1C2=CC(C(O)=O)=CC(OC(C)=O)=C2C(=O)C2=C1C=CC=C2OC(=O)C TYNLGDBUJLVSMA-UHFFFAOYSA-N 0.000 claims 1
- SWLAMJPTOQZTAE-UHFFFAOYSA-N 4-[2-[(5-chloro-2-methoxybenzoyl)amino]ethyl]benzoic acid Chemical compound COC1=CC=C(Cl)C=C1C(=O)NCCC1=CC=C(C(O)=O)C=C1 SWLAMJPTOQZTAE-UHFFFAOYSA-N 0.000 claims 1
- 229940077274 Alpha glucosidase inhibitor Drugs 0.000 claims 1
- 229940123208 Biguanide Drugs 0.000 claims 1
- 102100031151 C-C chemokine receptor type 2 Human genes 0.000 claims 1
- 101710149815 C-C chemokine receptor type 2 Proteins 0.000 claims 1
- RKWGIWYCVPQPMF-UHFFFAOYSA-N Chloropropamide Chemical compound CCCNC(=O)NS(=O)(=O)C1=CC=C(Cl)C=C1 RKWGIWYCVPQPMF-UHFFFAOYSA-N 0.000 claims 1
- JVHXJTBJCFBINQ-ADAARDCZSA-N Dapagliflozin Chemical compound C1=CC(OCC)=CC=C1CC1=CC([C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)O)=CC=C1Cl JVHXJTBJCFBINQ-ADAARDCZSA-N 0.000 claims 1
- 101710088194 Dehydrogenase Proteins 0.000 claims 1
- 229940124213 Dipeptidyl peptidase 4 (DPP IV) inhibitor Drugs 0.000 claims 1
- DVJAMEIQRSHVKC-BDAKNGLRSA-N Dutogliptin Chemical compound OB(O)[C@@H]1CCCN1C(=O)CN[C@H]1CNCC1 DVJAMEIQRSHVKC-BDAKNGLRSA-N 0.000 claims 1
- 108010011459 Exenatide Proteins 0.000 claims 1
- HTQBXNHDCUEHJF-XWLPCZSASA-N Exenatide Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CO)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)CNC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 HTQBXNHDCUEHJF-XWLPCZSASA-N 0.000 claims 1
- 102000012195 Fructose-1,6-bisphosphatases Human genes 0.000 claims 1
- 108010017464 Fructose-Bisphosphatase Proteins 0.000 claims 1
- 101710198884 GATA-type zinc finger protein 1 Proteins 0.000 claims 1
- 108010063919 Glucagon Receptors Proteins 0.000 claims 1
- 102100040890 Glucagon receptor Human genes 0.000 claims 1
- FAEKWTJYAYMJKF-QHCPKHFHSA-N GlucoNorm Chemical compound C1=C(C(O)=O)C(OCC)=CC(CC(=O)N[C@@H](CC(C)C)C=2C(=CC=CC=2)N2CCCCC2)=C1 FAEKWTJYAYMJKF-QHCPKHFHSA-N 0.000 claims 1
- 108010002352 Interleukin-1 Proteins 0.000 claims 1
- LTXREWYXXSTFRX-QGZVFWFLSA-N Linagliptin Chemical compound N=1C=2N(C)C(=O)N(CC=3N=C4C=CC=CC4=C(C)N=3)C(=O)C=2N(CC#CC)C=1N1CCC[C@@H](N)C1 LTXREWYXXSTFRX-QGZVFWFLSA-N 0.000 claims 1
- 108010019598 Liraglutide Proteins 0.000 claims 1
- YSDQQAXHVYUZIW-QCIJIYAXSA-N Liraglutide Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCC)C(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=C(O)C=C1 YSDQQAXHVYUZIW-QCIJIYAXSA-N 0.000 claims 1
- IBAQFPQHRJAVAV-ULAWRXDQSA-N Miglitol Chemical compound OCCN1C[C@H](O)[C@@H](O)[C@H](O)[C@H]1CO IBAQFPQHRJAVAV-ULAWRXDQSA-N 0.000 claims 1
- 229910019142 PO4 Inorganic materials 0.000 claims 1
- 102000003728 Peroxisome Proliferator-Activated Receptors Human genes 0.000 claims 1
- 108090000029 Peroxisome Proliferator-Activated Receptors Proteins 0.000 claims 1
- 102100040918 Pro-glucagon Human genes 0.000 claims 1
- GSINGUMRKGRYJP-VZWAGXQNSA-N Remogliflozin Chemical compound C1=CC(OC(C)C)=CC=C1CC1=C(C)N(C(C)C)N=C1O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 GSINGUMRKGRYJP-VZWAGXQNSA-N 0.000 claims 1
- 229940124639 Selective inhibitor Drugs 0.000 claims 1
- 229940100389 Sulfonylurea Drugs 0.000 claims 1
- 229960002632 acarbose Drugs 0.000 claims 1
- XUFXOAAUWZOOIT-UHFFFAOYSA-N acarviostatin I01 Natural products OC1C(O)C(NC2C(C(O)C(O)C(CO)=C2)O)C(C)OC1OC(C(C1O)O)C(CO)OC1OC1C(CO)OC(O)C(O)C1O XUFXOAAUWZOOIT-UHFFFAOYSA-N 0.000 claims 1
- 229960004733 albiglutide Drugs 0.000 claims 1
- OGWAVGNOAMXIIM-UHFFFAOYSA-N albiglutide Chemical compound O=C(O)C(NC(=O)CNC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)CNC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)CNC(=O)C(NC(=O)CNC(=O)C(N)CC=1(N=CNC=1))CCC(=O)O)C(O)C)CC2(=CC=CC=C2))C(O)C)CO)CC(=O)O)C(C)C)CO)CO)CC3(=CC=C(O)C=C3))CC(C)C)CCC(=O)O)CCC(=O)N)C)C)CCCCN)CCC(=O)O)CC4(=CC=CC=C4))C(CC)C)C)CC=6(C5(=C(C=CC=C5)NC=6)))CC(C)C)C(C)C)CCCCN)CCCNC(=N)N OGWAVGNOAMXIIM-UHFFFAOYSA-N 0.000 claims 1
- 229960001667 alogliptin Drugs 0.000 claims 1
- ZSBOMTDTBDDKMP-OAHLLOKOSA-N alogliptin Chemical compound C=1C=CC=C(C#N)C=1CN1C(=O)N(C)C(=O)C=C1N1CCC[C@@H](N)C1 ZSBOMTDTBDDKMP-OAHLLOKOSA-N 0.000 claims 1
- 239000003888 alpha glucosidase inhibitor Substances 0.000 claims 1
- 230000000692 anti-sense effect Effects 0.000 claims 1
- 229940093265 berberine Drugs 0.000 claims 1
- YBHILYKTIRIUTE-UHFFFAOYSA-N berberine Chemical compound C1=C2CC[N+]3=CC4=C(OC)C(OC)=CC=C4C=C3C2=CC2=C1OCO2 YBHILYKTIRIUTE-UHFFFAOYSA-N 0.000 claims 1
- QISXPYZVZJBNDM-UHFFFAOYSA-N berberine Natural products COc1ccc2C=C3N(Cc2c1OC)C=Cc4cc5OCOc5cc34 QISXPYZVZJBNDM-UHFFFAOYSA-N 0.000 claims 1
- 150000004283 biguanides Chemical class 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 229960001713 canagliflozin Drugs 0.000 claims 1
- VHOFTEAWFCUTOS-TUGBYPPCSA-N canagliflozin hydrate Chemical compound O.CC1=CC=C([C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)O)C=C1CC(S1)=CC=C1C1=CC=C(F)C=C1.CC1=CC=C([C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)O)C=C1CC(S1)=CC=C1C1=CC=C(F)C=C1 VHOFTEAWFCUTOS-TUGBYPPCSA-N 0.000 claims 1
- 229960001761 chlorpropamide Drugs 0.000 claims 1
- 229960003834 dapagliflozin Drugs 0.000 claims 1
- 229960004590 diacerein Drugs 0.000 claims 1
- 229940090124 dipeptidyl peptidase 4 (dpp-4) inhibitors for blood glucose lowering Drugs 0.000 claims 1
- 239000003603 dipeptidyl peptidase IV inhibitor Substances 0.000 claims 1
- 230000009977 dual effect Effects 0.000 claims 1
- 229950003693 dutogliptin Drugs 0.000 claims 1
- 229960001519 exenatide Drugs 0.000 claims 1
- 229940027775 fortamet Drugs 0.000 claims 1
- 229960004580 glibenclamide Drugs 0.000 claims 1
- 229960000346 gliclazide Drugs 0.000 claims 1
- 229960004346 glimepiride Drugs 0.000 claims 1
- WIGIZIANZCJQQY-RUCARUNLSA-N glimepiride Chemical compound O=C1C(CC)=C(C)CN1C(=O)NCCC1=CC=C(S(=O)(=O)NC(=O)N[C@@H]2CC[C@@H](C)CC2)C=C1 WIGIZIANZCJQQY-RUCARUNLSA-N 0.000 claims 1
- ZJJXGWJIGJFDTL-UHFFFAOYSA-N glipizide Chemical compound C1=NC(C)=CN=C1C(=O)NCCC1=CC=C(S(=O)(=O)NC(=O)NC2CCCCC2)C=C1 ZJJXGWJIGJFDTL-UHFFFAOYSA-N 0.000 claims 1
- 229960001381 glipizide Drugs 0.000 claims 1
- ZNNLBTZKUZBEKO-UHFFFAOYSA-N glyburide Chemical compound COC1=CC=C(Cl)C=C1C(=O)NCCC1=CC=C(S(=O)(=O)NC(=O)NC2CCCCC2)C=C1 ZNNLBTZKUZBEKO-UHFFFAOYSA-N 0.000 claims 1
- 229960000890 hydrocortisone Drugs 0.000 claims 1
- 229920001477 hydrophilic polymer Polymers 0.000 claims 1
- 229920001600 hydrophobic polymer Polymers 0.000 claims 1
- 229960002397 linagliptin Drugs 0.000 claims 1
- 229960002701 liraglutide Drugs 0.000 claims 1
- 239000011159 matrix material Substances 0.000 claims 1
- 229950004994 meglitinide Drugs 0.000 claims 1
- 229960001110 miglitol Drugs 0.000 claims 1
- 229960000698 nateglinide Drugs 0.000 claims 1
- OELFLUMRDSZNSF-BRWVUGGUSA-N nateglinide Chemical compound C1C[C@@H](C(C)C)CC[C@@H]1C(=O)N[C@@H](C(O)=O)CC1=CC=CC=C1 OELFLUMRDSZNSF-BRWVUGGUSA-N 0.000 claims 1
- PKWDZWYVIHVNKS-UHFFFAOYSA-N netoglitazone Chemical compound FC1=CC=CC=C1COC1=CC=C(C=C(CC2C(NC(=O)S2)=O)C=C2)C2=C1 PKWDZWYVIHVNKS-UHFFFAOYSA-N 0.000 claims 1
- 239000010452 phosphate Substances 0.000 claims 1
- 125000002467 phosphate group Chemical group [H]OP(=O)(O[H])O[*] 0.000 claims 1
- 229960005095 pioglitazone Drugs 0.000 claims 1
- 108700027806 rGLP-1 Proteins 0.000 claims 1
- 239000000018 receptor agonist Substances 0.000 claims 1
- 229940044601 receptor agonist Drugs 0.000 claims 1
- 229940126844 remogliflozin Drugs 0.000 claims 1
- 229960002354 repaglinide Drugs 0.000 claims 1
- 229960004586 rosiglitazone Drugs 0.000 claims 1
- 229960004937 saxagliptin Drugs 0.000 claims 1
- QGJUIPDUBHWZPV-SGTAVMJGSA-N saxagliptin Chemical compound C1C(C2)CC(C3)CC2(O)CC13[C@H](N)C(=O)N1[C@H](C#N)C[C@@H]2C[C@@H]21 QGJUIPDUBHWZPV-SGTAVMJGSA-N 0.000 claims 1
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- MFFMDFFZMYYVKS-SECBINFHSA-N sitagliptin Chemical compound C([C@H](CC(=O)N1CC=2N(C(=NN=2)C(F)(F)F)CC1)N)C1=CC(F)=C(F)C=C1F MFFMDFFZMYYVKS-SECBINFHSA-N 0.000 claims 1
- 239000004094 surface-active agent Substances 0.000 claims 1
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- 229960001641 troglitazone Drugs 0.000 claims 1
- GXPHKUHSUJUWKP-UHFFFAOYSA-N troglitazone Chemical compound C1CC=2C(C)=C(O)C(C)=C(C)C=2OC1(C)COC(C=C1)=CC=C1CC1SC(=O)NC1=O GXPHKUHSUJUWKP-UHFFFAOYSA-N 0.000 claims 1
- GXPHKUHSUJUWKP-NTKDMRAZSA-N troglitazone Natural products C([C@@]1(OC=2C(C)=C(C(=C(C)C=2CC1)O)C)C)OC(C=C1)=CC=C1C[C@H]1SC(=O)NC1=O GXPHKUHSUJUWKP-NTKDMRAZSA-N 0.000 claims 1
- 229960001254 vildagliptin Drugs 0.000 claims 1
- SYOKIDBDQMKNDQ-XWTIBIIYSA-N vildagliptin Chemical compound C1C(O)(C2)CC(C3)CC1CC32NCC(=O)N1CCC[C@H]1C#N SYOKIDBDQMKNDQ-XWTIBIIYSA-N 0.000 claims 1
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| US7407955B2 (en) | 2002-08-21 | 2008-08-05 | Boehringer Ingelheim Pharma Gmbh & Co., Kg | 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions |
| DE102004054054A1 (de) | 2004-11-05 | 2006-05-11 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Verfahren zur Herstellung chiraler 8-(3-Amino-piperidin-1-yl)-xanthine |
| PE20080251A1 (es) | 2006-05-04 | 2008-04-25 | Boehringer Ingelheim Int | Usos de inhibidores de dpp iv |
| EP1852108A1 (en) | 2006-05-04 | 2007-11-07 | Boehringer Ingelheim Pharma GmbH & Co.KG | DPP IV inhibitor formulations |
| CN102838599A (zh) | 2006-05-04 | 2012-12-26 | 贝林格尔.英格海姆国际有限公司 | 多晶型 |
| PE20091730A1 (es) | 2008-04-03 | 2009-12-10 | Boehringer Ingelheim Int | Formulaciones que comprenden un inhibidor de dpp4 |
| KR20200118243A (ko) | 2008-08-06 | 2020-10-14 | 베링거 인겔하임 인터내셔날 게엠베하 | 메트포르민 요법이 부적합한 환자에서의 당뇨병 치료 |
| US20200155558A1 (en) | 2018-11-20 | 2020-05-21 | Boehringer Ingelheim International Gmbh | Treatment for diabetes in patients with insufficient glycemic control despite therapy with an oral antidiabetic drug |
| PL2395983T3 (pl) | 2009-02-13 | 2020-09-07 | Boehringer Ingelheim International Gmbh | Kompozycja farmaceutyczna zawierająca inhibitor sglt2, inhibitor dpp-iv i ewentualnie dalszy środek przeciwcukrzycowy oraz jej zastosowania |
| NZ599298A (en) | 2009-11-27 | 2014-11-28 | Boehringer Ingelheim Int | Treatment of genotyped diabetic patients with dpp-iv inhibitors such as linagliptin |
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| NZ603319A (en) | 2010-06-24 | 2015-04-24 | Boehringer Ingelheim Int | Diabetes therapy |
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| AR083878A1 (es) | 2010-11-15 | 2013-03-27 | Boehringer Ingelheim Int | Terapia antidiabetica vasoprotectora y cardioprotectora, linagliptina, metodo de tratamiento |
| UY33937A (es) * | 2011-03-07 | 2012-09-28 | Boehringer Ingelheim Int | Composiciones farmacéuticas que contienen inhibidores de dpp-4 y/o sglt-2 y metformina |
| CA2841552C (en) | 2011-07-15 | 2020-06-23 | Boehringer Ingelheim International Gmbh | Substituted quinazolines, the preparation thereof and the use thereof in pharmaceutical compositions |
| CN104136004B (zh) * | 2012-02-22 | 2018-03-06 | 达切斯内公司 | 多西拉敏和吡哆醇和/或其代谢物或盐的制剂 |
| US9555001B2 (en) | 2012-03-07 | 2017-01-31 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition and uses thereof |
| EP3685839A1 (en) | 2012-05-14 | 2020-07-29 | Boehringer Ingelheim International GmbH | Linagliptin for use in the treatment of albuminuria and kidney related diseases |
| US20130303554A1 (en) | 2012-05-14 | 2013-11-14 | Boehringer Ingelheim International Gmbh | Use of a dpp-4 inhibitor in sirs and/or sepsis |
| WO2013174767A1 (en) | 2012-05-24 | 2013-11-28 | Boehringer Ingelheim International Gmbh | A xanthine derivative as dpp -4 inhibitor for use in modifying food intake and regulating food preference |
| UY34856A (es) * | 2012-07-03 | 2013-12-31 | Bayer Pharma AG | Formas de presentación farmacéuticas que contienen 5-cloro-n-({(5s)-2-oxo-3-[4-(3-oxo-4- morfolinil)-fenil]-1,3-oxazolidin-5-il}-metil)-2-tiofencarboxamida |
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| ES2670619T3 (es) | 2013-07-22 | 2018-05-31 | Duchesnay Inc. | Composición para la gestión de náuseas y vómitos |
| CN103655570B (zh) * | 2013-12-11 | 2016-07-06 | 深圳翰宇药业股份有限公司 | 西格列汀与二甲双胍复方缓释制剂及其制备方法 |
| CN104739835A (zh) * | 2013-12-30 | 2015-07-01 | 中美华世通生物医药科技（武汉）有限公司 | 一种治疗糖尿病的新型药物组合物 |
| WO2015101916A1 (en) | 2013-12-30 | 2015-07-09 | Mylan Laboratories Ltd. | Process for the preparation of empagliflozin |
| KR101633292B1 (ko) * | 2014-02-25 | 2016-06-24 | 동아에스티 주식회사 | 용법이 개선된 엔테카비어를 함유하는 약학적 조성물 |
| WO2015130083A1 (ko) * | 2014-02-25 | 2015-09-03 | 동아에스티 주식회사 | 용법이 개선된 엔테카비어를 함유하는 약학적 조성물 |
| ES2950384T3 (es) | 2014-02-28 | 2023-10-09 | Boehringer Ingelheim Int | Uso médico de un inhibidor de DPP-4 |
| US10689460B2 (en) | 2014-05-15 | 2020-06-23 | Incube Labs, Llc | PCSK9 antibody preparations for delivery into a lumen of the intestinal tract using a swallowable drug delivery device |
| CA2949236C (en) | 2014-05-15 | 2023-06-13 | Incube Labs, Llc | Pharmaceutical compositions and methods for fabrication of solid masses comprising polypeptides and/or proteins |
| CN105287581A (zh) * | 2014-07-15 | 2016-02-03 | 上海星泰医药科技有限公司 | 阿格列汀二甲双胍缓释片及其制备方法 |
| TWI595874B (zh) | 2014-08-29 | 2017-08-21 | 達契斯奈股份有限公司 | 多西拉敏及吡哆醇及／或其代謝產物或鹽之多模式釋放調配物 |
| JP2018513203A (ja) * | 2015-04-20 | 2018-05-24 | ティダブリューアイ・バイオテクノロジー・インコーポレイテッドＴＷＩ Ｂｉｏｔｅｃｈｎｏｌｏｇｙ， Ｉｎｃ． | ジアセレインを含有する製剤及びそれを用いて尿酸の血中濃度を低下させる方法 |
| TWI684465B (zh) * | 2015-04-22 | 2020-02-11 | 安成生物科技股份有限公司 | 含雙醋瑞因之製劑及使用其於降低尿酸血中濃度的方法 |
| CN105055413A (zh) * | 2015-07-23 | 2015-11-18 | 上海市第六人民医院 | 一种小檗碱和瑞格列奈的药物组合物 |
| CN105496970A (zh) * | 2015-12-18 | 2016-04-20 | 北京华禧联合科技发展有限公司 | 含有利格列汀的组合物及其制备方法 |
| CN106924208A (zh) * | 2015-12-30 | 2017-07-07 | 深圳翰宇药业股份有限公司 | 一种复方达格列净二甲双胍缓释片及其制备方法 |
| WO2017153939A1 (en) * | 2016-03-10 | 2017-09-14 | Aurobindo Pharma Limited | Pharmaceutical composition comprising canagliflozin, process of preparation and use thereof |
| WO2017211979A1 (en) | 2016-06-10 | 2017-12-14 | Boehringer Ingelheim International Gmbh | Combinations of linagliptin and metformin |
| WO2019195766A1 (en) * | 2018-04-06 | 2019-10-10 | AMMA Therapeutics, Inc. | Composition for controlled release of therapeutic agents |
| IT201800011119A1 (it) | 2018-12-14 | 2020-06-14 | Dpl Pharma S P A | Composizioni farmaceutiche orali solide per la somministrazione cronotropica di sitagliptin |
| TR201916829A2 (tr) * | 2019-10-31 | 2021-05-21 | Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi | Dapagli̇flozi̇n ve metformi̇n i̇çeren çi̇ft katmanli tablet formülasyonlari |
| CN110974792A (zh) * | 2019-12-26 | 2020-04-10 | 南京亿华药业有限公司 | 一种结晶性药物片剂及其制备方法 |
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| US6360257B1 (en) * | 1998-01-30 | 2002-03-19 | Telefonaktiebolaget L M Ericsson (Publ) | Managing group IP addresses in mobile end stations |
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| US20030187074A1 (en) * | 2002-03-04 | 2003-10-02 | Javed Hussain | Oral compositions for treatment of diabetes |
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| KR20120034211A (ko) * | 2002-09-20 | 2012-04-10 | 안드렉스 랩스 엘엘씨 | 약제학적 정제 |
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| PT1558220E (pt) * | 2003-07-24 | 2010-03-12 | Rasendrakumar Jha | Composições orais para tratamento da diabetes |
| WO2005041925A2 (en) * | 2003-10-31 | 2005-05-12 | Alza Corporation | Compositions and dosage forms for enhanced absorption |
| CN1901879A (zh) * | 2003-10-31 | 2007-01-24 | 阿尔扎公司 | 左旋多巴和卡比多巴的给药 |
| WO2010045656A2 (en) * | 2008-10-17 | 2010-04-22 | Nectid, Inc. | Novel sglt2 inhibitor dosage forms |
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- 2011-06-21 AU AU2011271124A patent/AU2011271124A1/en not_active Abandoned
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- 2011-06-21 MX MX2012015188A patent/MX2012015188A/es active IP Right Grant
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- 2011-06-21 CN CN201180031366XA patent/CN103037849A/zh active Pending
- 2011-06-21 CA CA2802335A patent/CA2802335A1/en not_active Abandoned
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- 2011-06-21 RU RU2012155890/15A patent/RU2012155890A/ru not_active Application Discontinuation
- 2011-06-21 JP JP2013516682A patent/JP2013533241A/ja active Pending
- 2011-06-22 TW TW100121863A patent/TW201206503A/zh unknown
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