反応 #1483110

反応方程式

Octreotide pamoate

→

Pamoic Acid

溶媒

EtOAc

benzyl alcohol

—

in-water

反応条件

後処理

1. 1
   workup.ADDITIONadded to the polymer solution
2. 2
   その他yielding a homogeneous organic phase
3. 3
   その他to provide an emulsion
4. 4
   その他The emulsion was collected directly into a 0.3% PVA solvent extraction solution (150 mL)
5. 5
   抽出to extract EtOAc
6. 6
   ろ過Hardened microparticles were collected by filtration
7. 7
   洗浄washed with water, air
8. 8
   その他dried
9. 9
   その他stored at 4° C.

実験手順

Microparticle formulations (Table 5, Q-W) were prepared by an oil-in-water emulsion/solvent extraction method. PLGA polymer (MW 24,000, 180 mg) was dissolved in EtOAc (1000 μL). Octreotide pamoate (20 or 40 mg) was dissolved in benzyl alcohol (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 in a ratio of 1:2 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.

出典