تفاعل #1483117

ord-75d558ae9381413bafa6cd500e091d1b

معادلة التفاعل

CC(=O)O.CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
Oxytocin acetate
O=C(O)c1cc2ccccc2c(Cc2c(O)c(C(=O)O)cc3ccccc23)c1O.[Na+]
disodium pamoate
→
CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
Oxytocin
المردود 79.0%

المتفاعلات

—
PLGA
CC(=O)O.CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
Oxytocin acetate
O=C(O)c1cc2ccccc2c(Cc2c(O)c(C(=O)O)cc3ccccc23)c1O.[Na+]
disodium pamoate

الكواشف

لا شيء

المذيبات

CCOC(C)=O
EtOAc
CO
MeOH

ظروف التفاعل

الظروف التفصيلية
See reaction.notes.procedure_details.

المعالجة

  1. 1
    workup.ADDITIONadded to the polymer solution
  2. 2
    أخرىyielding a milky suspension as the organic phase
  3. 3
    أخرىto provide an emulsion
  4. 4
    أخرىThe emulsion was collected directly into a 0.3% PVA solvent extraction solution (150 mL)
  5. 5
    استخلاصto extract EtOAc
  6. 6
    ترشيحHardened microparticles were collected by filtration
  7. 7
    غسيلwashed with water, air
  8. 8
    أخرىdried
  9. 9
    أخرىstored at 4° C

الإجراء التجريبي

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.

المصدر

DOI: 10.6084/m9.figshare.5104873.v1براءة الاختراع: US08900636B2uspto-grants-2014_12