反应 #1483113

反应方程式

Leuprolide acetate

→

Leuprolide

收率 70.0%

溶剂

CH2Cl2

BnOH

反应条件

后处理

1. 1
   workup.ADDITIONadded to the polymer solution
2. 2
   其他yielding a homogeneous organic phase
3. 3
   其他to provide an emulsion
4. 4
   其他The emulsion was collected directly into a 0.3% PVA solvent extraction solution (150 mL)
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 24,000, 160 mg) was dissolved in CH2Cl2 (1000 μL). Leuprolide acetate (40 mg) was dissolved in BnOH (1000 μL) and added to the polymer solution yielding a homogeneous organic phase. The resulting organic phase was combined with a 1% PVA aqueous phase 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 BI (140 mg, 70.0% yield) with a median particle size 50.1 μm. The core load (1.99%), encapsulation efficiency (9.95%) and in vitro burst (1.63%) were determined by RP-HPLC assay.

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