Disodium methylenebis(2-hydroxy-3-naphthoate) → Oxytocin

HRID 1395935

Reaktionsgleichung

Reaktionsgleichung von HRID 1395935
[CH3:1][CH2:2][C@@H:3]([C@@H:5]1[NH:29][C:27](=[O:28])[C@H:26]([CH2:30][C:31]2[CH:36]=[CH:35][C:34]([OH:37])=[CH:33][CH:32]=2)[NH:25][C:23](=[O:24])[C@@H:22]([NH2:38])[CH2:21][S:20][S:19][CH2:18][C@@H:17]([C:39]([N:41]2[C@H:45]([C:46]([NH:48][C@H:49]([C:54]([NH:56][CH2:57][C:58]([NH2:60])=[O:59])=[O:55])[CH2:50][CH:51]([CH3:53])[CH3:52])=[O:47])[CH2:44][CH2:43][CH2:42]2)=[O:40])[NH:16][C:14](=[O:15])[C@H:13]([CH2:61][C:62]([NH2:64])=[O:63])[NH:12][C:10](=[O:11])[C@H:9]([CH2:65][CH2:66][C:67]([NH2:69])=[O:68])[NH:8][C:6]1=[O:7])[CH3:4].CC(O)=O.C1C=C2C=C(C(O)=O)C(O)=C(CC3C4C(=CC=CC=4)C=C(C(O)=O)C=3O)C2=CC=1.[Na+]>CCOC(C)=O.CO>[CH3:1][CH2:2][C@@H:3]([C@@H:5]1[NH:29][C:27](=[O:28])[C@H:26]([CH2:30][C:31]2[CH:36]=[CH:35][C:34]([OH:37])=[CH:33][CH:32]=2)[NH:25][C:23](=[O:24])[C@@H:22]([NH2:38])[CH2:21][S:20][S:19][CH2:18][C@@H:17]([C:39]([N:41]2[C@H:45]([C:46]([NH:48][C@H:49]([C:54]([NH:56][CH2:57][C:58]([NH2:60])=[O:59])=[O:55])[CH2:50][CH:51]([CH3:53])[CH3:52])=[O:47])[CH2:44][CH2:43][CH2:42]2)=[O:40])[NH:16][C:14](=[O:15])[C@H:13]([CH2:61][C:62]([NH2:64])=[O:63])[NH:12][C:10](=[O:11])[C@H:9]([CH2:65][CH2:66][C:67]([NH2:69])=[O:68])[NH:8][C:6]1=[O:7])[CH3:4]

Komponenten

5

Edukt 2

HCID 10179807Disodium methylenebis(2-hydroxy-3-naphthoate)HCID 12004215Oxytocin acetate

Produkt 1

HCID 439302OxytocinAusbeute 79 %

Reagenzien, Katalysatoren, Lösungsmittel 2

HCID 887MethanolLösungsmittelHCID 8857Ethyl AcetateLösungsmittel

Versuchsvorschrift

PLGA polymer (MW 24,000, 180 mg) was dissolved in EtOAc (1800 μL). Oxytocin acetate (40 mg) was dissolved in MeOH (200 μL) and added to the polymer solution yielding a milky suspension as the organic phase. The resulting organic phase was combined with a 1% PVA aqueous phase containing 10 mM disodium pamoate to provide an emulsion. The emulsion was collected directly into a 0.3% PVA solvent extraction solution (150 mL) and stirred for four hours to extract EtOAc. Hardened microparticles were collected by filtration, washed with water, air dried and stored at 4° C. This provided formulation BM (158 mg, 79.0% yield) with a median particle size 144 μm. The core load (8.9%), encapsulation efficiency (44.5%) and in vitro burst (21.1%) were determined by RP-HPLC assay.

Aufarbeitung

  1. additionadded to the polymer solution
  2. customyielding a milky suspension as the organic phase
  3. customto provide an emulsion
  4. customThe emulsion was collected directly into a 0.3% PVA solvent extraction solution (150 mL)
  5. extractionto extract EtOAc
  6. filtrationHardened microparticles were collected by filtration
  7. washwashed with water, air
  8. customdried
  9. customstored at 4° C

Quellen und Nachweise

ORD-Eintrag
ord-75d558ae9381413bafa6cd500e091d1b
Quelldatensatz
uspto-grants-2014_12
Patentnummer
US08900636B2

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