| Budget Amount *help |
¥1,000,000 (Direct Cost: ¥1,000,000)
Fiscal Year 1996: ¥1,000,000 (Direct Cost: ¥1,000,000)
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| Research Abstract |
In this study, we selected the w/o/w multiple emulsion as a carrier of water-soluble drugs and studied on preparation, evaluation of pharmaceutical properties and applications for drug delivery system (DDS). For the oily phase of multiple emulsion, an oil mixture of Lipiodol and vegetable oil or isopropyl myristate were used to minimize the difference in specific gravity between oily phase and aqueous phase. HCO-40 or HCO-50 and Pluronic F-88 were used as hydrophobic and hydrophilic surfactants, respectively. For entrapping water-soluble drugs, vancomycin, cytarabine, doxorubicin and ACNU were used. Multiple emulsions were prepared with stirring or membrane emulsification methods.
Multiple emulsions prepared by both methods were stable during storage at 4ﾟC.Particle size of the multiple emulsion was controlled by both methods. Especially, particle distribution of multiple emulsion prepared with membrane method showed homogeneousness. It however took too much time to prepare much multipl
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e emulsion in this method. Although the entrapment efficiency and the release property of drug were different among products, they could be controlled by formulations and preparations of the multiple emulsion.
When the multiple emulsion (particle size being 3 mum) entrapping vancomycin was injected intravenously, the serum concentration of the drug was prolonged. When the multiple emulsions entrapping cytarabine whose particle sizes were 3 and 30 mum injected intraperitoneally, these emulsions were useful for treatments of lymphatic metastasis of cancer and peritoneal carcinomatosis, respectively. When the multiple emulsion entrapping doxorubicin, whose particle size was 30 mum, was injected into hepatic artery of rat bearing Waker 256, and when the emulsion whose particle size was 3 mum, was injected into the portal vein of rat bearing AH109A,survival times of the treated groups were prolonged. When the multiple emulsion entrapping ACNU was injected intrathecally to the meningeal gliomatosis, the survival time of the treated group was prolonged.
The results of this study showed that the multiple emulsion was useful for a carrier of water-soluble drugs and sustained release of drugs. Therefore it can be applied to DDS by controlling the particle size of the emulsion. Less
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