反应 #1483115

反应方程式

Leuprolide acetate

disodium pamoate

→

Leuprolide

收率 60.0%

溶剂

—

in-water

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

A microparticle formulation was prepared by an oil-in-water emulsion/solvent extraction method. 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 50 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 BK (120 mg, 60.0% yield) with a median particle size 43.1 μm. The core load (10.6%), encapsulation efficiency (53.0%) and in vitro burst (21.1%) were determined by RP-HPLC assay.

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