تفاعل #1483116

معادلة التفاعل

Oxytocin acetate

→

Oxytocin

المردود 71.5%

المذيبات

EtOAc

MeOH

EtOAc

ظروف التفاعل

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 10 mM sodium phosphate (pH 8, 0° C., 150 mL) solvent extraction solution
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 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.

المصدر