Octreotide pamoate → Pamoic Acid

HRID 539412

반응식

HRID 539412 반응식
C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC2C3C=CC=CC=3NC=2)NC(=O)[C@H](CC2C=CC=CC=2)NC(=O)[C@@H](NC([C@H](N)CC2C=CC=CC=2)=O)CSSC[C@@H](C(N[C@@H]([C@H](O)C)CO)=O)NC1=O.[CH:72]1[CH:73]=[CH:74][C:75]2[C:76](=[CH:78][C:79]([C:98]([OH:100])=[O:99])=[C:80]([OH:97])[C:81]=2[CH2:82][C:83]2[C:92]([OH:93])=[C:91]([C:94]([OH:96])=[O:95])[CH:90]=[C:89]3[C:84]=2[CH:85]=[CH:86][CH:87]=[CH:88]3)[CH:77]=1>CCOC(C)=O.C(O)C1C=CC=CC=1>[CH:72]1[CH:73]=[CH:74][C:75]2[C:76](=[CH:78][C:79]([C:98]([OH:100])=[O:99])=[C:80]([OH:97])[C:81]=2[CH2:82][C:83]2[C:92]([OH:93])=[C:91]([C:94]([OH:96])=[O:95])[CH:90]=[C:89]3[C:84]=2[CH:85]=[CH:86][CH:87]=[CH:88]3)[CH:77]=1

참가 물질

4

반응물 1

HCID 44194024Octreotide pamoate

생성물 1

HCID 8546Pamoic Acid

시약·촉매·용매 2

HCID 244Benzyl Alcohol용매HCID 8857Ethyl Acetate용매

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.

후처리

  1. additionadded to the polymer solution
  2. customyielding a homogeneous organic phase
  3. customto provide an emulsion
  4. customThe emulsion was collected directly into a 0.3% PVA solvent extraction solution (150 mL)
  5. extractionto extract EtOAc
  6. filtrationHardened microparticles were collected by filtration
  7. washwashed with water, air
  8. customdried
  9. customstored at 4° C.

출처 및 근거

ORD 기록
ord-d2ee98b6fde74ca58ae5ef1ef994f1fc
출처 데이터셋
uspto-grants-2014_10
특허 번호
US08871269B2

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