Improvement of Stability and Dissolution of Prostaglandin E_1 by Maltosyl-β-cyclodextrin in Lyophilized Formulation

概要

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To improve undesirable pharmaceutical properties of prostaglandin E_1 (PGE_1) in lyophilized formulation, potential use of highly water-soluble maltosyl-β-cyclodextrin (G_2-β-CyD) was examined, comparing it with parent β-cyclodextrin (β-CyD). Inclusion complexation of PGE_1 with G_2-β-CyD in an aqueous solution was estimated by the solubility method, circular dichroism and carbon-13 nuclear magnetic resonance spectroscopies. PGE_1 was freeze-dried with various additives and subjected to stability and dissolution testd. When the amorphous products were stored at 60℃, decomposition of PGE_1 was significantly decelerated by both G_2-β-CyD and β-CyD, while it was accelerated by mannitol as an inert ingredient. During storage, the rapid dissolving property of PGE_1 was maintained by complexation with G_2-β-CyD, while it tended to decrease by β-CyD, depending on the moisture-adsorbing and wetting properties along with crystallinity change of the additives. The limited data obtained here suggests that G_2-β-CyD may be preferable to β-CyD for the improvement of chemical instability and poor dissolution properties of PGE_1 in dry solids for injections.
公益社団法人日本薬学会の論文
1992-03-25