JP2003535893A5 - - Google Patents

Info

Publication number

JP2003535893A5

JP2003535893A5 JP2002503273A JP2002503273A JP2003535893A5 JP 2003535893 A5 JP2003535893 A5 JP 2003535893A5 JP 2002503273 A JP2002503273 A JP 2002503273A JP 2002503273 A JP2002503273 A JP 2002503273A JP 2003535893 A5 JP2003535893 A5 JP 2003535893A5

Authority

JP

Japan

Prior art keywords

propofol

pharmaceutical composition

parenteral administration

aqueous pharmaceutical

administration according

Prior art date

2000-12-14

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

• Espacenet
• Global Dossier
• Discuss

• OLBCVFGFOZPWHH-UHFFFAOYSA-N propofol Chemical compound CC(C)C1=CC=CC(C(C)C)=C1O OLBCVFGFOZPWHH-UHFFFAOYSA-N 0.000 description 55
• 229960004134 propofol Drugs 0.000 description 55
• 238000007911 parenteral administration Methods 0.000 description 30
• 239000008194 pharmaceutical composition Substances 0.000 description 30
• ODLHGICHYURWBS-LKONHMLTSA-N trappsol cyclo Chemical compound CC(O)COC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)COCC(O)C)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1COCC(C)O ODLHGICHYURWBS-LKONHMLTSA-N 0.000 description 20
• 229920000858 Cyclodextrin Polymers 0.000 description 18
• LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 18
• 238000004519 manufacturing process Methods 0.000 description 13
• 239000000203 mixture Substances 0.000 description 13
• OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 12
• 239000000243 solution Substances 0.000 description 12
• 238000000034 method Methods 0.000 description 10
• 239000000872 buffer Substances 0.000 description 9
• XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 7
• KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 6
• DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 6
• CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 4
• PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 4
• DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 description 4
• FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 4
• 239000003963 antioxidant agent Substances 0.000 description 4
• 235000006708 antioxidants Nutrition 0.000 description 4
• 150000001875 compounds Chemical class 0.000 description 4
• 239000003085 diluting agent Substances 0.000 description 4
• 239000003960 organic solvent Substances 0.000 description 4
• 239000006201 parenteral dosage form Substances 0.000 description 4
• 239000000546 pharmaceutical excipient Substances 0.000 description 4
• 238000002360 preparation method Methods 0.000 description 4
• 239000002904 solvent Substances 0.000 description 4
• 239000003795 chemical substances by application Substances 0.000 description 3
• IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
• KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 description 2
• 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 2
• 239000004471 Glycine Substances 0.000 description 2
• PWKSKIMOESPYIA-BYPYZUCNSA-N L-N-acetyl-Cysteine Chemical compound CC(=O)N[C@@H](CS)C(O)=O PWKSKIMOESPYIA-BYPYZUCNSA-N 0.000 description 2
• 239000002202 Polyethylene glycol Substances 0.000 description 2
• 229960004308 acetylcysteine Drugs 0.000 description 2
• 239000000654 additive Substances 0.000 description 2
• 230000003078 antioxidant effect Effects 0.000 description 2
• 239000011668 ascorbic acid Substances 0.000 description 2
• 235000010323 ascorbic acid Nutrition 0.000 description 2
• 229960005070 ascorbic acid Drugs 0.000 description 2
• 239000000706 filtrate Substances 0.000 description 2
• 238000001914 filtration Methods 0.000 description 2
• 239000008103 glucose Substances 0.000 description 2
• 235000011187 glycerol Nutrition 0.000 description 2
• 239000008363 phosphate buffer Substances 0.000 description 2
• 239000007981 phosphate-citrate buffer Substances 0.000 description 2
• 229920001223 polyethylene glycol Polymers 0.000 description 2
• 150000003839 salts Chemical class 0.000 description 2
• 239000011780 sodium chloride Substances 0.000 description 2
• HRZFUMHJMZEROT-UHFFFAOYSA-L sodium disulfite Chemical compound [Na+].[Na+].[O-]S(=O)S([O-])(=O)=O HRZFUMHJMZEROT-UHFFFAOYSA-L 0.000 description 2
• 229940001584 sodium metabisulfite Drugs 0.000 description 2
• 235000010262 sodium metabisulphite Nutrition 0.000 description 2
• 239000003708 ampul Substances 0.000 description 1
• 239000008364 bulk solution Substances 0.000 description 1
• 239000000084 colloidal system Substances 0.000 description 1
• 230000009918 complex formation Effects 0.000 description 1
• 238000002425 crystallisation Methods 0.000 description 1
• 229940079593 drug Drugs 0.000 description 1
• 239000003814 drug Substances 0.000 description 1
• 238000011049 filling Methods 0.000 description 1
• 229910052757 nitrogen Inorganic materials 0.000 description 1
• 239000000825 pharmaceutical preparation Substances 0.000 description 1
• 238000010926 purge Methods 0.000 description 1
• 238000007789 sealing Methods 0.000 description 1
• 230000006641 stabilisation Effects 0.000 description 1
• 238000011105 stabilization Methods 0.000 description 1
• 238000003756 stirring Methods 0.000 description 1
• 230000001502 supplementing effect Effects 0.000 description 1