反应 #1483116

反应方程式

Oxytocin acetate

→

Oxytocin

收率 71.5%

溶剂

EtOAc

MeOH

EtOAc

反应条件

后处理

1. 1
   workup.ADDITIONadded to the polymer solution
2. 2
   其他yielding a milky suspension as the organic phase
3. 3
   其他to provide an emulsion
4. 4
   其他The emulsion was collected directly into a 10 mM sodium phosphate (pH 8, 0° C., 150 mL) solvent extraction solution
5. 5
   萃取to extract EtOAc
6. 6
   过滤Hardened microparticles were collected by filtration
7. 7
   洗涤washed with water, air
8. 8
   其他dried
9. 9
   其他stored at 4° C

实验过程

PLGA polymer (MW 13,000, 180 mg) was dissolved in EtOAc (900 μL). Oxytocin acetate (20 mg) was dissolved in MeOH (100 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 5% EtOAc to provide an emulsion. The emulsion was collected directly into a 10 mM sodium phosphate (pH 8, 0° C., 150 mL) solvent extraction solution and stirred for four hours while warming to room temperature to extract EtOAc. Hardened microparticles were collected by filtration, washed with water, air dried and stored at 4° C. This provided formulation BL (143 mg, 71.5% yield) with a median particle size 44.0 μm. The core load (1.67%), encapsulation efficiency (16.7%) and in vitro burst (46.3%) were determined by RP-HPLC assay.

来源