Pamoic Acid → Disodium pamoate

HRID 539411

反応式

HRID 539411 の反応式
[CH:1]1[CH:2]=[CH:3][C:4]2[C:5](=[CH:7][C:8]([C:27]([OH:29])=[O:28])=[C:9]([OH:26])[C:10]=2[CH2:11][C:12]2[C:21]([OH:22])=[C:20]([C:23]([OH:25])=[O:24])[CH:19]=[C:18]3[C:13]=2[CH:14]=[CH:15][CH:16]=[CH:17]3)[CH:6]=1.[OH-].[Na+:31]>O1CCOCC1.O1CCOCC1.O>[CH:16]1[CH:17]=[C:18]2[CH:19]=[C:20]([C:23]([OH:25])=[O:24])[C:21]([O-:22])=[C:12]([CH2:11][C:10]3[C:4]4[C:5](=[CH:6][CH:1]=[CH:2][CH:3]=4)[CH:7]=[C:8]([C:27]([OH:29])=[O:28])[C:9]=3[O-:26])[C:13]2=[CH:14][CH:15]=1.[Na+:31].[Na+:31]

参加物

5

反応物 2

HCID 8546Pamoic AcidHCID 14798Sodium Hydroxide

生成物 1

HCID 54676156Disodium pamoate

試薬・触媒・溶媒 2

HCID 312751,4-Dioxane溶媒HCID 218864351,4-Dioxane--water (1/1)溶媒

実験手順

A second octreotide-pamoate complex was prepared by dissolving pamoic acid (19.4 mg, 0.05 mmol) in 0.4 N NaOH (250 μL) and dioxane (250 μL) to provide a solution of sodium pamoate in dioxane/water (1:1). Octreotide acetate (50 mg, 0.05 mmol) was dissolved in dioxane/water (1:1, 200 μL). The octreotide acetate solution was added drop wise to the sodium pamoate with mixing to provide a light yellow, homogenous solution. This material was lyophilized to dryness providing a light yellow powder (65 mg). The octreotide/pamoate ratio of this preparation was 1.02 as measured by RP-HPLC. These two preparations were used to prepare new PLGA microparticle formulations.

後処理

  1. customA second octreotide-pamoate complex was prepared

出典と根拠

ORDレコード
ord-57af1edf5fcf43abbad924c9ddb766e0
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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