反応 #1483117

反応方程式

Oxytocin acetate

disodium pamoate

→

Oxytocin

収率 79.0%

溶媒

EtOAc

MeOH

反応条件

後処理

1. 1
   workup.ADDITIONadded to the polymer solution
2. 2
   その他yielding a milky suspension as the organic phase
3. 3
   その他to provide an emulsion
4. 4
   その他The emulsion was collected directly into a 0.3% PVA solvent extraction solution (150 mL)
5. 5
   抽出to extract EtOAc
6. 6
   ろ過Hardened microparticles were collected by filtration
7. 7
   洗浄washed with water, air
8. 8
   その他dried
9. 9
   その他stored at 4° C

実験手順

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.

出典