Physicochemical properties of two types of adriamycin preparation, suspensions and emulsions prepared for i.a. chemotherapy of hepatocellular carcinoma, were investigated. A suspension was prepared by dispersing adriamycin directly into the lipid contrast medium, Lipiodol, whereas an emulsion was obtained by emulsifying an aqueous solution of adriamycin into Lipiodol. The dispersibility of the drug in each preparation was examined microscopically. The chemical stability of and drug release from the preparation were determined by high-performance liquid chromatography and spectrophotometry, respectively. The suspension was then given to ten patients with primary hepatocellular carcinoma. The suspension maintained good dispersibility without coagulation of drug particles, whereas coalescence of aqueous droplets and the resultant phase separation occurred 4 h after preparation of the emulsion. Both preparations maintained the initial drug content for at least 1 week at room temperature. The release of adriamycin was more prolonged in the suspension than in the emulsion. After i.a. administration of the suspension, a selective accumulation of Lipiodol in the tumor and decrease in serum alpha-fetoprotein (AFP) levels were found in most patients. A significant amount of adriamycin was still detected in hepatic specimens resected from two patients 1 and 2 months after treatment. These findings suggest that the adriamycin-Lipiodol suspension may be a useful preparation for targeting chemotherapy to hepatocellular carcinoma.
Ethanolamine oleate injection containing 30% iopamiron 300 (30% IP 300-E0) has been previously prepared for endoscopic sclerotherapy of esophageal varices on X-ray TV monitor. However,the ability of fluoroscopic visualization of this sclerosing agent was slightly insufficient in clinical use.We prepared ethanolamine oleate injection containing 30% iopamiron 370 (30% IP 370-E0),and measured the physical characteristics such as viscosity and osmotic pressure of this agent.The ability of visualization was observed in patients with esophageal varix by X-ray.The viscosity,which was inversely related to the injectability into varices,of 30% IP 370-E0 was relatively low and its osmotic nressure was almost the same as that of normal saline.30 % IP 370-E0 was easily injected into varices.Better fluoroscopic visualization was obtained by intravariceal injection with 30% IP 370-E0 than with 30% IP 300-E0.These results suggest that 30% 1P370-E0 is more useful agent for endoscopic sclerotherapy of esophageal varices.
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