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PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
9
pubmed:dateCreated
1999-11-30
pubmed:abstractText
We developed a "pH-jump method" to obtain transparent solutions of E5531, a synthetic lipid A analog, at neutral pH for pharmaceutical injection. E5531 has two pKa: pKa1 = 6.0 and pKa2 = 9.3. At pH 11.0, E5531 was dispersed as a dissociated form, and the phase transition temperature Tc of E5531 was determined to be 30 degrees C using differential scanning calorimetry (DSC). Based on these results, the pH-jump method procedure involves dispersing E5531 at pH 11.0 (above pKa2) at 50 degrees C (above Tc) and mixing with a phosphate buffer to neutralize the pH. No degradated products of E5531 were observed at 50 degrees C for 3 hr during dispersing in the alkaline solution. The turbidity of samples prepared with the pH-jump method was similar to that of water and superior to the samples dispersed directly in neutral pH. This method does not need mechanical power and is suitable for large-scale production.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Sep
pubmed:issn
0363-9045
pubmed:author
pubmed:issnType
Print
pubmed:volume
25
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
975-82
pubmed:dateRevised
2004-11-17
pubmed:meshHeading
pubmed:year
1999
pubmed:articleTitle
Preparation of transparent injectable formulation for lipid A analog E5531.
pubmed:affiliation
Formulation Research Laboratory, Kawashima, Eisai Company, Limited, Gifu, Japan.
pubmed:publicationType
Journal Article