반응 #1483116

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Oxytocin acetate

→

Oxytocin

수율 71.5%

용매

EtOAc

MeOH

EtOAc

반응 조건

후처리

1. 1
   workup.ADDITIONadded to the polymer solution
2. 2
   기타yielding a milky suspension as the organic phase
3. 3
   기타to provide an emulsion
4. 4
   기타The emulsion was collected directly into a 10 mM sodium phosphate (pH 8, 0° C., 150 mL) solvent extraction solution
5. 5
   추출to extract EtOAc
6. 6
   여과Hardened microparticles were collected by filtration
7. 7
   세척washed with water, air
8. 8
   기타dried
9. 9
   기타stored at 4° C

실험 절차

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.

출처