Octreotide pamoate → Pamoic Acid

HRID 539412

反応式

HRID 539412 の反応式
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

参加物

4

反応物 1

HCID 44194024Octreotide pamoate

生成物 1

HCID 8546Pamoic Acid

試薬・触媒・溶媒 2

HCID 244Benzyl Alcohol溶媒HCID 8857Ethyl Acetate溶媒

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.

後処理

  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.

出典と根拠

ORDレコード
ord-d2ee98b6fde74ca58ae5ef1ef994f1fc
出典データセット
uspto-grants-2014_10
特許番号
US08871269B2

関連ノート

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