Doxorubicin Hydrochloride → Doxorubicin

HRID 1034377Notizen

Reaktionsgleichung

Reaktionsgleichung von HRID 1034377
[CH3:1][C@@H:2]1[O:7][C@@H:6]([O:8][C@@H:9]2[C:14]3=[C:15]([OH:32])[C:16]4[C:28](=[O:29])[C:27]5[C:22](=[CH:23][CH:24]=[CH:25][C:26]=5[O:30][CH3:31])[C:20](=[O:21])[C:17]=4[C:18]([OH:19])=[C:13]3[CH2:12][C@@:11]([OH:37])([C:33]([CH2:35][OH:36])=[O:34])[CH2:10]2)[CH2:5][C@H:4]([NH2:38])[C@@H:3]1[OH:39].Cl>CC(N(O)CCCCCNC(CCC(N(O)CCCCCNC(CCC(N(O)CCCCCN)=O)=O)=O)=O)=O.CS(O)(=O)=O>[CH3:1][C@@H:2]1[O:7][C@@H:6]([O:8][C@@H:9]2[C:14]3=[C:15]([OH:32])[C:16]4[C:28](=[O:29])[C:27]5[C:22](=[CH:23][CH:24]=[CH:25][C:26]=5[O:30][CH3:31])[C:20](=[O:21])[C:17]=4[C:18]([OH:19])=[C:13]3[CH2:12][C@@:11]([OH:37])([C:33]([CH2:35][OH:36])=[O:34])[CH2:10]2)[CH2:5][C@H:4]([NH2:38])[C@@H:3]1[OH:39]

Komponenten

3

Edukt 1

HCID 443939Doxorubicin Hydrochloride

Produkt 1

HCID 31703Doxorubicin

Reagenzien, Katalysatoren, Lösungsmittel 1

HCID 62881Deferoxamine MesylateLösungsmittel

Versuchsvorschrift

1 ml of a 10 mg/ml solution of doxorubicin HCl dissolved in saline-desferal was added to 1 ml of the liposome dispersion after the liposomes were gel filtrated on a Sephadex G-50 column. The mixture was incubated at room temperature for approximately 24 hours. At the end of incubation period, the mixture was passed through a Dowex 50 WX-4 (Serva) column to adsorb the free unincorporated drug. As small amount as 60 mg of the resin is able to adsorb as much as 1 mg of free doxorubicin in a time shorter than less than 15 minutes while liposome incorporated doxorubicin does not adsorb to the dowex resin at all and remains with the liposomes. A column containing 1-2 g dry weight of the resin was sufficient to adsorb all unincorporated drug. To determine the ratio of incorporated drug to liposomal lipid, the phospholipid and doxorubicin concentration were determined as described in Example 1.

Aufarbeitung

  1. additionwas added to 1 ml of the liposome dispersion after the liposomes
  2. filtrationfiltrated on a Sephadex G-50 column
  3. customshorter than less than 15 minutes
  4. additionA column containing 1-2 g
  5. customdry weight of the resin
  6. concentrationthe phospholipid and doxorubicin concentration

Quellen und Nachweise

ORD-Eintrag
ord-a5aaa78b2ead45beb277129f459d2e08
Quelldatensatz
uspto-grants-1994_05
Patentnummer
US05316771

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