Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
Physical Properties of Pyrimidine and Purine Antimetabolites. II. Permeation of 5-Fluorouracil and 1-(2-Tetrahydrofuryl)-5-fluorouracil through Cellophane, Collagen, and Silicone Membranes
中野 眞汎荒川 佳子井上 博之有田 隆一
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1976 年 24 巻 11 号 p. 2716-2722

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5-Fluorouracil and its derivative, 1-(2-tetrahydrofuryl)-5-fluorouracil (THFFU) were studied as to their permeability through cellophane, collagen, and silicone membranes. 5-Fluorouracil permeated through cellophane and collagen membranes slightly faster than THFFU. 5-Fluorouracil, however, permeated through the silicone membrane much more slowly than THFFU. Although the solubility of THFFU in silicone oil was much smaller than that in water, propylene glycol, or macrogol 400, its permeation rates through the silicone membrane from suspensions in these media were similar. The permeation rate of 5-fluorouracil through the silicone membrane from suspension in water was slightly greater than that in macrogol 400 in spite of smaller solubility in water. The permeation rate of THFFU from aqueous solutions through the silicone membrane was accelerated by the presence of sodium chloride and sodium sulfate whereas it was decelerated by sodium iodide. Permeation studies of THFFU through the silicone membrane at various pH values revealed that only the unionized form of the drug permeated through the membrane. The effect of temperature on permeability and flux of THFFU through the silicone membrane was also studied.
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© The Pharmaceutical Society of Japan
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