Abstract:
:The isomerization reactions of ceftibuten and ceftibuten-related compounds in aqueous solution were investigated to estimate the substitution effect on the isomerization reaction and identify the three proximal dissociation constants of ceftibuten kinetically from the pH-rate profiles. The isomerization reaction of ceftibuten-related compounds was influenced by the substituents near the double bond at the C7-side chain, and the electron-withdrawing substituent was found to increase the isomerization rate. Ceftibuten isomerized at the C7-side chain, and the isomerization rate was influenced by the dissociation of the C7-side chain carboxylic acid and aminothiazole in the acidic pH region. The dissociation constants of ceftibuten were assigned by comparing the isomerization rates of ceftibuten with its related compounds at various pH conditions, and the pKas 2.3, 3.2, and 4.5 were attributed to the 4-carboxylic acid, 7-carboxylic acid, and 7-aminothiazole, respectively.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Hashimoto N,Hirano Kdoi
10.1021/js980048zsubject
Has Abstractpub_date
1998-09-01 00:00:00pages
1091-6issue
9eissn
0022-3549issn
1520-6017pii
S0022-3549(15)50637-0journal_volume
87pub_type
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