반응 #1483110

ord-362ac787d9b2419e8b184b5e68b65f9f

반응 방정식

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

시약

없음

반응 조건

상세 조건
See reaction.notes.procedure_details.

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 (150 mL)
  5. 5
    추출to extract EtOAc
  6. 6
    여과Hardened microparticles were collected by filtration
  7. 7
    세척washed with water, air
  8. 8
    기타dried
  9. 9
    기타stored at 4° C.

실험 절차

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.

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US08900636B2uspto-grants-2014_12