著者

小川 泰亮

出版者

日本膜学会

雑誌

膜 (ISSN:03851036)

巻号頁・発行日

vol.20, no.2, pp.149-153, 1995-03-01 (Released:2011-03-04)

参考文献数

10

被引用文献数

1

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A monolithic microcapsule-depot form using a biodegradable polymer was designed and developed, which constantly releases a super-active agonist of LH-RH, leuprorelin, at a constant rate for about one month following a single injection. Microcapsules containing the drug were prepared by a new preparation technique, modifying the solvent evaporation method. When copoly (lactic/glycolic) acid of copolymer ratio of 75/25 and average molecular weight of 10, 000 was adopted a biodegradable polymer, leuprorelin was eliminated from the injection site in rats at a pseudo-zero order rate for one month after a single subcutaneous or intramuscular injection of the microcapsules. Serum leuprorelin levels were maintained at a steady level in rats and dogs for 4 weeks after an injection, and serum testosterone levels decreased to below the normal level and were maintained at the suppressed level for more than 6 weeks. The results indicate that the microcapsule dosage form is useful for LH-RH therapy of sex hormone dependent diseases.After extended clinical evaluation, the monthly microcapsule-depot form of leuprorelin for treating prostate cancer, endometriosis, precocious puberty, and other sex hormone dependent diseases was approved by health authorities in U.S.A., Europe, and Japan as Lupron®; Depot, Enantone®; Depot, and Leuprin®;, respectively.