Abstract:
:Esmolol hydrochloride degrades in aqueous solutions by the hydrolysis of a labile aliphatic carboxyester group. The products are methanol and ASL-8123. The resulting aliphatic carboxylic acid moiety (ASL-8123) has a pK of 4.80, which is within 1 pH unit of the pH of the formulation. ASL-8123 therefore acts as a "secondary buffer" and minimizes the change in pH due to degradation. Equations are presented to calculate the change in the pH when the primary degradation product acts as a secondary buffer. This information can be used in the development of a parenteral product to predict, a priori, the concentration of buffer necessary for optimal pH maintenance. This knowledge can reduce the number of formulation screens required to determine the necessary buffer capacity for optimal drug stability.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Rosenberg LS,Hostetler CK,Wagenknecht DM,Aunet DAdoi
10.1023/a:1015973425708subject
Has Abstractpub_date
1988-08-01 00:00:00pages
514-7issue
8eissn
0724-8741issn
1573-904Xjournal_volume
5pub_type
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journal_title:Pharmaceutical research
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