Oh I, Kang Y G, Lee Y B, Shin S C, Kim C K
College of Pharmacy, Chonnam National University, Kwangju, Korea.
Drug Dev Ind Pharm. 1998 Oct;24(10):889-94. doi: 10.3109/03639049809097268.
To develop a prolonged and sustained release preparation, we prepared an albumin microsphere-in-oil-in-water emulsion (S/O/W) and examined sustained release from it in comparison with other control preparations such as water-in-oil (W/O) emulsions and microspheres in vitro and in vivo, respectively. Tegafur was used as a model drug. A microsphere-in-oil emulsion was prepared by adding albumin microspheres to soybean oil containing 20% Span 80. To prepare an S/O/W emulsion, the microsphere-in-oil emulsion was added into an aqueous solution of hydroxypropyl methylcellulose containing Pluronic F68. The mean particle size of the albumin microspheres was 3 microns, and the ratio of entrapment of tegafur into albumin microspheres was about 25%. In an in vitro release test, the t75 of the S/O/W emulsion was fourfold greater and in an in vivo release test the mean residence time of tegafur from the S/O/W emulsion was more than twofold that from a W/O emulsion or microsphere system. The mean residence time of 5-fluorouracil (5-FU) from an S/O/W emulsion was also greater than with other dosage forms. These results suggest the possible usefulness of an S/O/W emulsion for the sustained and prolonged release of tegafur.
为开发一种长效缓释制剂，我们制备了一种水包油包白蛋白微球乳液（S/O/W），并分别在体外和体内将其与其他对照制剂（如水包油（W/O）乳液和微球）进行比较，研究其缓释性能。替加氟用作模型药物。通过将白蛋白微球加入含有20%司盘80的大豆油中制备油包微球乳液。为制备S/O/W乳液，将油包微球乳液加入含有普朗尼克F68的羟丙基甲基纤维素水溶液中。白蛋白微球的平均粒径为3微米，替加氟在白蛋白微球中的包封率约为25%。在体外释放试验中，S/O/W乳液的t75大四倍，在体内释放试验中，替加氟从S/O/W乳液中的平均驻留时间是从W/O乳液或微球系统中的两倍多。5-氟尿嘧啶（5-FU）从S/O/W乳液中的平均驻留时间也比其他剂型长。这些结果表明S/O/W乳液对于替加氟的持续长效释放可能有用。
