Gamma scintigraphy in the delivery, biodistribution and targeting of therapeutic agents.

A C Perkins, M V Pimm, C G Wilson
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Abstract

The established clinical role of radionuclide imaging includes the diagnosis and monitoring of a wide range of clinical conditions. The therapeutic use of radionuclides has centred on a relatively small number of pathological conditions, particularly within the field of oncology. More recently there has been growing interest in the use of radionuclide imaging in drug evaluation and research (RIDER). Studies have been undertaken in order to increase the understanding of the in in vivo behaviour of pharmaceutical dosage forms in addition to the in vivo behaviour of molecular and cellular anti-tumour agents. The imaging facilities required for such undertakings are available in most nuclear medicine departments, although the expertise for radiolabelling and the requirements for the production of drug conjugates and pharmaceutical formulations are limited to a small number of centres. This paper discusses the application of radionuclide imaging in drug research with particular reference to the role of gamma-scintigraphy in monitoring the biodistribution and pharmacokinetics of immune mediated drug conjugates intended for the treatment of malignant disease. Examples described include the evaluation of oral and inhaled drug delivery systems and the biodistribution and in vivo kinetics of parenteral administrations.

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伽玛闪烁成像在药物传递、生物分布和靶向治疗中的应用。
放射性核素成像已确立的临床作用包括诊断和监测广泛的临床状况。放射性核素的治疗用途集中于相对少数的病理情况,特别是在肿瘤学领域。最近,人们对放射性核素成像在药物评价和研究中的应用越来越感兴趣。除了分子和细胞抗肿瘤剂的体内行为外,还进行了研究,以增加对药物剂型的体内行为的理解。这些工作所需的成像设施在大多数核医学部门都有,虽然放射性标签的专门知识和生产药物偶联物和药物制剂的要求仅限于少数中心。本文讨论了放射性核素成像在药物研究中的应用,特别是伽马显像在监测用于治疗恶性疾病的免疫介导药物偶联物的生物分布和药代动力学中的作用。所描述的例子包括口服和吸入给药系统的评估以及肠外给药的生物分布和体内动力学。
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