To improve undesirable pharmaceutical properties of prostaglandin E1 (PGE1) in lyophilized formulation, potential use of highly water-soluble maltosyl-β-cyclodextrin (G2-β-CyD) was examined, comparing it with parent β-cyclodextrin (β-CyD). Inclusion complexation of PGE1 with G2-β-CyD in an aqueous solution was estimated by the solubility method, circular dichroism and carbon-13 nuclear magnetic resonance spectroscopies. PGE1 was freeze-dried with various additives and subjected to stability and dissolution testd. When the amorphous products were stored at 60°C, decomposition of PGE1 was significantly decelerated by both G2-β-CyD and β-CyD, while it was accelerated by mannitol as an inert ingredient. During storage, the rapid dissolving property of PGE1 was maintained by complexation with G2-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 G2-β-CyD may be preferable to β-CyD for the improvement of chemical instability and poor dissolution properties of PGE1 in dry solids for injections.
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Yamamoto et al. (1992) studied this question.
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