肝細胞癌動注化学療法に用いるピラルビシン(THP)・エマルジョンの基礎的検討

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  • The study of pirarubicin-emulsion for hepatic arterial infusion chemotherapy.

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To develop new dosage form of pirarubicin (THP) for hepatic arterial infusion chemotherapy, we investigated constituents of THP-emulsion, stability of THP in emulsions, and release characteristics of THP from emulsions. The THP-emulsion was prepared by high pressure homogenization using three-way cock. Water and non-ionic contrast media (CM), which are Iopamidol, Iohexol and Ioversol, were used as solvents for THP. Sesame oil, soybean oil, and Lipiodol-ultrafluid (LPD) were used as oily phase, and surfactants and saccharides were used as additives to make the emulsion stable. Stable w/o and o/w types of emulsions were obtained only when THP was dissolved in CM and mixed with LPD. Stability of THP in CM was examined and Iopamidol (Iopamiron 300) was selected as the solvent. Release characteristics of THP from the emulsion consisted of Iopamiron 300 and LPD was examined by means of multistoried method using saline. THP was released rapidly from the o/w type of emulsion, but gradually from the w/o type of emulsion. In this study, we could propose o/w and w/o types of THP-emulsions using Iopamiron 300 and LPD as constituents to carry preclinical study for hepatic arterial infusion chemotherapy.

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