5'-デオキシフルオロウリジン軟膏の開発と吸収促進剤の効果

概要

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5'_Deoxy-5-Fluorouridine (5'_DFUR) ointment was prepared for local chemotherapy application to inoperable breast cancer. Polyethyleneglycol-4000, ammoniumpolyacrylate and hydroxy-propylcellulose-H were employed to prepare the ointment base. 1-Dodecylazacycloheptan-2-one (Azone) was added to 5'_DFUR ointment as an absorption promoter. The spreadability of the ointment was only slightly changed by Azone addition. Azone was dispersed well in the ointment when the concentration was l%. 5'_DFUR in mouse skin and intestine were analyzed after the application of ointment and oral administration of 5'_DFUR solution. The AUC_<0-6> value observed with 5'_DFUR ointment containing 1.010 Azone was seven times greater than without Azone. Application of Azone-5'_DFUR ointment significantly lowered the levels. of 5'_DFUR in plasma and intestinal tissues over those of the oral administration of 5'_DFUR solution. Furthermore, no change occurred in histopathological findings of mouse skin following ointment application. These results suggest that the addition of Azone in 5'_DFUR ointment may provide a better therapeutic effect in the local chemotherapy treatment of breast cancer.
日本医療薬学会の論文
1994-08-20