반응 #1483114

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Leuprolide acetate

disodium pamoate

→

Leuprolide

수율 78.5%

용매

CH2Cl2

BnOH

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후처리

1. 1
   workup.ADDITIONadded to the polymer solution
2. 2
   기타yielding a homogeneous organic phase
3. 3
   기타to provide an emulsion
4. 4
   기타The 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
   여과Hardened microparticles were collected by filtration
8. 8
   세척washed with water, air
9. 9
   기타dried
10. 10
    기타stored at 4° C

실험 절차

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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