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一种新开发的使用活性炭细颗粒进行靶向化疗的药物递送系统。

A newly developed drug delivery system using fine particles of activated charcoal for targeting chemotherapy.

作者信息

Ito K, Kiriyama K, Watanabe T, Yamauchi M, Akiyama S, Kondou K, Takagi H

机构信息

Department of Surgery II, Nagoya University School of Medicine, Japan.

出版信息

ASAIO Trans. 1990 Jul-Sep;36(3):M199-202.

PMID:2123633
Abstract

Targeting chemotherapy to the metastatic lesions of the lymph nodes after surgical removal of the main tumor, a drug delivery system using ultrafine particles of activated charcoal was developed and examined for its ability to adsorb mitomycin C (MMC) and to transport MMC to the lymph system. Satisfactory results were obtained. In animal experiments, serial sampling of thoracic duct lymph by cannulation and serial samplings of peripheral vein blood after injection of MMC-charcoal solution into the subserosal space of the intestinal wall were made to study the pharmacodynamics of the lymph-blood system through analysis of MMC regression curves. Clearance (K) and half-life (t1/2) are calculated from the formula; C(t) = C(t0) X e-kt, and compared with that of MMC-saline. Activated charcoal has a proven ability to transport MMC to the lymphatic system. With activated charcoal, MMC is retained for much longer in the lymph nodes than with saline. Congestion of the lymph system was produced by ligation of the thoracic duct in CH-40, with 25% prolongation of t1/2. In conclusion, these drug delivery systems are suitable for targeting chemotherapy at lymph node metastases, and it is proven that 1500 AA Mitsubishi ultrafine charcoal is a good carrier of drug and a slow drug-release material in the lymphatics. Minimal side effects are expected because of the constant low concentrations in the general circulation.

摘要

在手术切除主要肿瘤后,针对淋巴结转移病灶进行化疗,研发了一种使用活性炭超细颗粒的药物递送系统,并对其吸附丝裂霉素C(MMC)以及将MMC转运至淋巴系统的能力进行了研究,获得了满意的结果。在动物实验中,通过插管对胸导管淋巴进行连续采样,并在将MMC-活性炭溶液注入肠壁浆膜下间隙后对外周静脉血进行连续采样,通过分析MMC消退曲线来研究淋巴-血液系统的药效学。清除率(K)和半衰期(t1/2)根据公式C(t) = C(t0) X e-kt计算得出,并与MMC-生理盐水的清除率和半衰期进行比较。活性炭已被证实具有将MMC转运至淋巴系统的能力。与生理盐水相比,使用活性炭时MMC在淋巴结中的保留时间长得多。在CH-40中通过结扎胸导管导致淋巴系统充血,t1/2延长了25%。总之,这些药物递送系统适用于针对淋巴结转移进行化疗,并且已证实1500 AA三菱超细活性炭是一种良好的药物载体以及淋巴管中的缓释材料。由于在体循环中浓度持续较低,预计副作用最小。

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