反应 #1483110

ord-362ac787d9b2419e8b184b5e68b65f9f

反应方程式

C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccccc2)CSSC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC1=O.O=C(O)c1cc2ccccc2c(Cc2c(O)c(C(=O)O)cc3ccccc23)c1O
Octreotide pamoate
O=C(O)c1cc2ccccc2c(Cc2c(O)c(C(=O)O)cc3ccccc23)c1O
Pamoic Acid

试剂

反应条件

详细条件
See reaction.notes.procedure_details.

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

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.

来源

DOI: 10.6084/m9.figshare.5104873.v1专利: US08900636B2uspto-grants-2014_12