Effects of β- and Dimethyl β-Cyclodextrins on Release and Percutaneous Absorption Behaviors of Prednisolone from Some Ointment Bases

UEKAMA KANETO, MASAKI KATSUHIRO, ARIMORI KAZUHIKO, IRIE TETSUMI, HIRAYAMA FUMITOSHI

doi:10.1248/yakushi1947.107.6_449

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Other Title

プレドニゾロンの各種軟膏基剤からの放出及び経皮吸収に対するβ-及びジメチルβ-シクロデキストリンの影響
プレドニゾロンノカクシュナンコウキザイカラノホウシュツオヨビ
Effects of β- and Dimethyl β-Cyclodextrins on Release and Percutaneous Absorption Behaviors of Prednisolone from Some Ointment Bases

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Abstract

The fast dissolving form of the inclusion complexes of prednisolone (PD) with β-cyclodextrin (β-CyD) and dimethyl β-cyclodextrin (DM-β-CyD) in a molar ratio of 1 : 2 was prepared to examine the in vitro/in vivo relation of percutaneous drug absorption from various ointments containing β-CyDs complexes. The release rate of PD from the ointments containing water (hydrophilic ointment, absorptive ointment and aqueous polyacrylic acid gel) and white petrolatum was significantly increased by both β-CyDs, while retarded in the cases of FAPG and macrogol ointments. The enhanced release of PD seemed to be due to the increase in apparent solubility and/or diffusibility of the drug in the ointment bases by means of water soluble inclusion complex formation. The percutaneous absorption experiments in vivo revealed that the disappearance of PD from the hydrophilic ointment and the appearance of PD in the skin after application to dorsal skin of rabbits were signiflcantly enhanced by both β-CyDs. The in vitro and in vivo data suggested that DM-β-CyD may be particularly useful to improve the topical bioavailability of PD, when an ointment base containing water was used.

Journal

YAKUGAKU ZASSHI

YAKUGAKU ZASSHI 107 (6), 449-456, 1987

The Pharmaceutical Society of Japan

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