JP2004189753A5 - - Google Patents

Info

Publication number

JP2004189753A5

JP2004189753A5 JP2004062679A JP2004062679A JP2004189753A5 JP 2004189753 A5 JP2004189753 A5 JP 2004189753A5 JP 2004062679 A JP2004062679 A JP 2004062679A JP 2004062679 A JP2004062679 A JP 2004062679A JP 2004189753 A5 JP2004189753 A5 JP 2004189753A5

Authority

JP

Japan

Prior art keywords

composition

fatty acid

acid esters

mono

component

Prior art date

2004-03-05

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.)

Pending

Links

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• 239000000203 mixture Substances 0.000 claims 49
• 235000014113 dietary fatty acids Nutrition 0.000 claims 26
• 239000000194 fatty acid Substances 0.000 claims 26
• 229930195729 fatty acid Natural products 0.000 claims 26
• DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims 24
• -1 fatty acid esters Chemical class 0.000 claims 22
• PMATZTZNYRCHOR-CGLBZJNRSA-N Cyclosporin A Chemical compound CC[C@@H]1NC(=O)[C@H]([C@H](O)[C@H](C)C\C=C\C)N(C)C(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C1=O PMATZTZNYRCHOR-CGLBZJNRSA-N 0.000 claims 17
• 108010036949 Cyclosporine Proteins 0.000 claims 17
• 229960001265 ciclosporin Drugs 0.000 claims 17
• 229930182912 cyclosporin Natural products 0.000 claims 16
• 239000003120 macrolide antibiotic agent Substances 0.000 claims 14
• URAYPUMNDPQOKB-UHFFFAOYSA-N triacetin Chemical compound CC(=O)OCC(OC(C)=O)COC(C)=O URAYPUMNDPQOKB-UHFFFAOYSA-N 0.000 claims 14
• DOOTYTYQINUNNV-UHFFFAOYSA-N Triethyl citrate Chemical compound CCOC(=O)CC(O)(C(=O)OCC)CC(=O)OCC DOOTYTYQINUNNV-UHFFFAOYSA-N 0.000 claims 12
• 239000001069 triethyl citrate Substances 0.000 claims 12
• VMYFZRTXGLUXMZ-UHFFFAOYSA-N triethyl citrate Natural products CCOC(=O)C(O)(C(=O)OCC)C(=O)OCC VMYFZRTXGLUXMZ-UHFFFAOYSA-N 0.000 claims 12
• 235000013769 triethyl citrate Nutrition 0.000 claims 12
• 150000004665 fatty acids Chemical class 0.000 claims 11
• 125000003976 glyceryl group Chemical group [H]C([*])([H])C(O[H])([H])C(O[H])([H])[H] 0.000 claims 11
• 239000004094 surface-active agent Substances 0.000 claims 11
• LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 10
• 229930105110 Cyclosporin A Natural products 0.000 claims 8
• 235000013773 glyceryl triacetate Nutrition 0.000 claims 7
• 239000004615 ingredient Substances 0.000 claims 7
• 229960002622 triacetin Drugs 0.000 claims 7
• WEAPVABOECTMGR-UHFFFAOYSA-N triethyl 2-acetyloxypropane-1,2,3-tricarboxylate Chemical compound CCOC(=O)CC(C(=O)OCC)(OC(C)=O)CC(=O)OCC WEAPVABOECTMGR-UHFFFAOYSA-N 0.000 claims 7
• SECXISVLQFMRJM-UHFFFAOYSA-N N-Methylpyrrolidone Chemical compound CN1CCCC1=O SECXISVLQFMRJM-UHFFFAOYSA-N 0.000 claims 6
• 239000002202 Polyethylene glycol Substances 0.000 claims 6
• 239000000839 emulsion Substances 0.000 claims 6
• 239000004530 micro-emulsion Substances 0.000 claims 6
• WVDDGKGOMKODPV-ZQBYOMGUSA-N phenyl(114C)methanol Chemical compound O[14CH2]C1=CC=CC=C1 WVDDGKGOMKODPV-ZQBYOMGUSA-N 0.000 claims 6
• 229920001223 polyethylene glycol Polymers 0.000 claims 6
• 150000001298 alcohols Chemical class 0.000 claims 5
• 239000003814 drug Substances 0.000 claims 5
• 229920005862 polyol Polymers 0.000 claims 5
• NLZUEZXRPGMBCV-UHFFFAOYSA-N Butylhydroxytoluene Chemical compound CC1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1 NLZUEZXRPGMBCV-UHFFFAOYSA-N 0.000 claims 4
• CZBZUDVBLSSABA-UHFFFAOYSA-N butylated hydroxyanisole Chemical compound COC1=CC=C(O)C(C(C)(C)C)=C1.COC1=CC=C(O)C=C1C(C)(C)C CZBZUDVBLSSABA-UHFFFAOYSA-N 0.000 claims 4
• 150000002148 esters Chemical class 0.000 claims 4
• 238000004519 manufacturing process Methods 0.000 claims 4
• 230000002265 prevention Effects 0.000 claims 4
• 239000003963 antioxidant agent Substances 0.000 claims 3
• 235000006708 antioxidants Nutrition 0.000 claims 3
• 239000004064 cosurfactant Substances 0.000 claims 3
• 239000011732 tocopherol Substances 0.000 claims 3
• XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 3
• IAYPIBMASNFSPL-UHFFFAOYSA-N Ethylene oxide Chemical compound C1CO1 IAYPIBMASNFSPL-UHFFFAOYSA-N 0.000 claims 2
• QAQJMLQRFWZOBN-LAUBAEHRSA-N L-ascorbyl-6-palmitate Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](O)[C@H]1OC(=O)C(O)=C1O QAQJMLQRFWZOBN-LAUBAEHRSA-N 0.000 claims 2
• 239000011786 L-ascorbyl-6-palmitate Substances 0.000 claims 2
• 229920001214 Polysorbate 60 Polymers 0.000 claims 2
• 206010052779 Transplant rejections Diseases 0.000 claims 2
• 230000003078 antioxidant effect Effects 0.000 claims 2
• 235000010385 ascorbyl palmitate Nutrition 0.000 claims 2
• 230000001363 autoimmune Effects 0.000 claims 2
• 239000007795 chemical reaction product Substances 0.000 claims 2
• 150000001875 compounds Chemical class 0.000 claims 2
• 239000008172 hydrogenated vegetable oil Substances 0.000 claims 2
• 230000004968 inflammatory condition Effects 0.000 claims 2
• 239000008203 oral pharmaceutical composition Substances 0.000 claims 2
• 150000003138 primary alcohols Chemical class 0.000 claims 2
• 238000002560 therapeutic procedure Methods 0.000 claims 2
• 229960001295 tocopherol Drugs 0.000 claims 2
• 229930003799 tocopherol Natural products 0.000 claims 2
• 150000003626 triacylglycerols Chemical class 0.000 claims 2
• 235000015112 vegetable and seed oil Nutrition 0.000 claims 2
• 239000008158 vegetable oil Substances 0.000 claims 2
• 208000009329 Graft vs Host Disease Diseases 0.000 claims 1
• 229920001400 block copolymer Polymers 0.000 claims 1
• GVJHHUAWPYXKBD-UHFFFAOYSA-N d-alpha-tocopherol Natural products OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 claims 1
• 239000002552 dosage form Substances 0.000 claims 1
• 150000002191 fatty alcohols Chemical class 0.000 claims 1
• 239000007903 gelatin capsule Substances 0.000 claims 1
• 208000024908 graft versus host disease Diseases 0.000 claims 1
• 210000003734 kidney Anatomy 0.000 claims 1
• 230000036457 multidrug resistance Effects 0.000 claims 1
• 210000000056 organ Anatomy 0.000 claims 1
• 239000002245 particle Substances 0.000 claims 1
• 229920002503 polyoxyethylene-polyoxypropylene Polymers 0.000 claims 1
• 235000010384 tocopherol Nutrition 0.000 claims 1
• 235000019149 tocopherols Nutrition 0.000 claims 1
• 238000002054 transplantation Methods 0.000 claims 1
• GVJHHUAWPYXKBD-IEOSBIPESA-N α-tocopherol Chemical compound OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-N 0.000 claims 1
• QUEDXNHFTDJVIY-UHFFFAOYSA-N γ-tocopherol Chemical class OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1 QUEDXNHFTDJVIY-UHFFFAOYSA-N 0.000 claims 1