Some Physicochemical Properties of FK906: Glass Transition and Relaxation

Jouhn-Wern Jang; Satoshi Kitamura; J. Keith Guillory

Abstract

FK906, a tripeptide antihypertensive agent, was used as a model compound to study some physicochemical properties of peptides and peptide-related compounds. Our results indicate that lyophilization, grinding and melting or storing the samples under conditions of high relative humidity affect chemical stability and crystallinity of FK906. In a preliminary study of lyophilization process design, an extended phase diagram for FK906 in aqueous solution was constructed, and the effects of cooling rate and heating rate on the glass transition temperatures of lyophilized FK906 and the FK906 solution were investigated. Following lyophilization, the DSC thermogram of FK906 exhibits an endothermic peak whose area is storage temperature- and time-dependent. The endothermic peak shifts to higher temperatures as the heating rate is increased. Our results indicate that the endothermic peak is related to structural change during incubation of lyophilized FK906.

Received May 3, 1994.
Accepted August 31, 1994.

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