Hagiwara A, Takahashi T, Kondoh S, Iwamoto A, Sawai K
1st Dept. of Surgery, Kyoto Prefectural University of Medicine.
Gan To Kagaku Ryoho. 1988 Apr;15(4 Pt 2-1):1038-42.
A new drug delivery system comprising activated carbon particles adsorbing anticancer drugs was developed. Activated carbon particles have affinity to the regional lymph-nodes and the tumor surface. When activated carbon particles adsorbing anticancer drug were administered into the tissues or serosal cavity, they remained for a long time at the site of application, and released the drug slowly. Activated carbon particles adsorbing mitomycin C (MMC-CH) were prepared for the use of an intracavitary administration. In animal experiment tissues, MMC-CH distributed a large amount of mitomycin C to the intraperitoneal tissues, while there was a low level of mitomycin C in the whole body. The LD50 value of MMC-CH was 5.3 times as high as that of mitomycin C aqueous solution. The therapeutic index (LD50/ED50) of the MMC-CH therapy was 3.1 times higher than that of the mitomycin C aqueous solution in Yoshida sarcoma ascites. Clinical trials of MMC-CH were performed in 81 patients with malignant effusion. Fifty-one of the 81 patients responded well. Activated carbon particles adsorbing peplomycin (PEP-CH) were prepared for chemotherapy against lymphatic metastasis. A high level of peplomycin was distributed to regional lymph nodes for a long time, when it was injected into the gastric wall of dogs. In animal experiments using MH 134 tumor, the therapeutic efficacy of PEP-CH on the lymphatic metastasis was greater than that of peplomycin aqueous solution. Clinical trials were carried out in 7 patients with esophageal cancer who did not undergo surgery. The local response rate was 85% and the survival time was 9.4 months in average including 5 survivors.
开发了一种包含吸附抗癌药物的活性炭颗粒的新型药物递送系统。活性炭颗粒对区域淋巴结和肿瘤表面具有亲和力。当将吸附有抗癌药物的活性炭颗粒施用于组织或浆膜腔时，它们会在应用部位长时间停留，并缓慢释放药物。制备了吸附丝裂霉素C（MMC-CH）的活性炭颗粒用于腔内给药。在动物实验组织中，MMC-CH将大量丝裂霉素C分布到腹膜内组织，而全身丝裂霉素C水平较低。MMC-CH的半数致死剂量（LD50）值是丝裂霉素C水溶液的5.3倍。在吉田肉瘤腹水模型中，MMC-CH疗法的治疗指数（LD50/ED50）比丝裂霉素C水溶液高3.1倍。对81例恶性积液患者进行了MMC-CH的临床试验。81例患者中有51例反应良好。制备了吸附培普利霉素（PEP-CH）的活性炭颗粒用于抗淋巴转移化疗。当将其注入犬胃壁时，高水平的培普利霉素会在区域淋巴结中长时间分布。在使用MH 134肿瘤的动物实验中，PEP-CH对淋巴转移的治疗效果大于培普利霉素水溶液。对7例未接受手术的食管癌患者进行了临床试验。局部缓解率为85%，平均生存时间为9.4个月，其中5例存活。
