Hagiwara A, Takahashi T, Ueda T, Iwamoto A, Torii T
Department of Surgery, Red Cross Hospital of Maizuru, Kyoto, Japan.
Anticancer Drug Des. 1987 Apr;1(4):313-21.
The effect of a new dosage form for anti-cancer agents was studied on tissue distribution and compared with the aqueous solution form. The new dosage form, developed in order to distribute a greater amount of the agent to regional lymph nodes, comprises polyvinylpyrrolidone and small activated carbon particles adsorbing pepleomycin (PEP-CH) or mitomycin C (MMC-CH) in saline. Pepleomycin at 500 micrograms/kg or mitomycin C at 250 micrograms/kg were injected into the gastric wall of dogs in the new dosage form or the aqueous solution form. The activity level of the agents in tissues was bioassayed within 24 h after injection by the thin agar plate method. Statistically, the new dosage form maintained an activity level in lymph nodes that was significantly higher than the aqueous solution form (ratio of PEP-CH to solution form, 6-32 times in 24 h; MMC-CH, 100-1000 times in 6 h; p less than 0.05-0.01), and a concentration in blood that was significantly lower (PEP-CH, about 1/2 times in 2 h; MMC-CH, 1/10-1/5 times in 1 h; p less than 0.05).
研究了一种抗癌药物新剂型对组织分布的影响，并与水溶液剂型进行了比较。为了使更多药物分布到局部淋巴结而开发的新剂型，是由聚乙烯吡咯烷酮和在盐水中吸附平阳霉素（PEP-CH）或丝裂霉素C（MMC-CH）的小活性炭颗粒组成。以新剂型或水溶液剂型将500微克/千克的平阳霉素或250微克/千克的丝裂霉素C注入犬的胃壁。注射后24小时内，采用薄琼脂平板法对组织中药物的活性水平进行生物测定。统计学分析表明，新剂型在淋巴结中的活性水平显著高于水溶液剂型（PEP-CH与溶液剂型的比值，24小时内为6至32倍；MMC-CH，6小时内为100至1000倍；p<0.05至0.01），而在血液中的浓度显著较低（PEP-CH，2小时内约为1/2倍；MMC-CH，1小时内为1/10至1/5倍；p<0.05）。
