反应 #1483114

反应方程式

Leuprolide acetate

disodium pamoate

→

Leuprolide

收率 78.5%

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 (100 mL)
5. 5
   workup.ADDITIONwas added
6. 6
   workup.STIRRINGstirred for an additional four hours
7. 7
   过滤Hardened microparticles were collected by filtration
8. 8
   洗涤washed with water, air
9. 9
   其他dried
10. 10
    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 containing 10 mM disodium pamoate to provide an emulsion. The emulsion was collected directly into a 0.3% PVA solvent extraction solution (100 mL) and stirred for 10 minutes. A secondary extraction solution consisting of 2% isopropanol (200 mL) was added and stirred for an additional four hours. Hardened microparticles were collected by filtration, washed with water, air dried and stored at 4° C. This provided formulation BJ (157 mg, 78.5% yield) with a median particle size 54.0 μm. The core load (9.4%), encapsulation efficiency (47.0%) and in vitro burst (5.31%) were determined by RP-HPLC assay.

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