Doxorubicin Hydrochloride → HCID 86598966, Verbindung

HRID 874086

Reaktionsgleichung

Reaktionsgleichung von HRID 874086
[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.[S:41]([O-:45])([O-:44])(=[O:43])=[O:42].[NH4+].[NH4+]>>[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].[S:41]([O-:45])([O-:44])(=[O:43])=[O:42]

Komponenten

3

Edukt 2

HCID 443939Doxorubicin Hydrochloride3×HCID 6097028Ammonium Sulfate2×

Produkt 1

HCID 86598966HCID 86598966, Verbindung

Versuchsvorschrift

A preferred non-pegylated liposome of the present invention is loaded with doxorubicin hydrochloride and is prepared using methods described above. In one embodiment, when loading doxorubicin hydrochloride using the active loading procedure described above, the drug is dissolved in a suitable buffer solution (as described above) before loading to get a concentration of at least 25 mM. When the active loading process involves an ammonium sulfate gradient, the ammonium sulfate reacts with doxorubicin hydrochloride to form doxorubicin sulfate. Doxorubicin sulfate is insoluble and remains inside the liposomes after loading. Once any unentrapped or free drug is removed from loaded liposomes, the drug loaded liposomes are diluted using aqueous buffer solution to achieve the required drug concentration. The preferred buffer solution used is sucrose-histidine buffer solution as discussed previously.

Aufarbeitung

  1. customis prepared
  2. dissolutionis dissolved in a suitable buffer solution (as described above)
  3. customto get a concentration of at least 25 mM

Quellen und Nachweise

ORD-Eintrag
ord-896d61cbb7894948b4a509a66e7154cd
Quelldatensatz
uspto-grants-2015_03
Patentnummer
US08980310B2

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