应用PHYCON 6600实现抗肿瘤药物(carmofur)的缓释。

Drug design and delivery Pub Date : 1989-12-01
K Imasaka, H Ueda, T Azuma, T Nagai
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引用次数: 0

摘要

本研究试图开发基于PHYCON 6600(一种新型硅凝胶)的可植入缓释剂型。将两种基本组分(PHYCON A和PHYCON B溶液)在室温下聚合约1小时制备固体凝胶。我们探索的应用是将可植入的PHYCON-药物复合材料用于肿瘤治疗。选择Carmofur(1-己基氨基甲酰-5-氟尿嘧啶,HCFU)作为一种实用的抗肿瘤药物。通过体外溶出试验,在约35天的时间内观察到接近零级释放率。发现“爆裂现象”释放的药物量小于HCFU的毒性剂量。通过测量淋巴瘤接种小鼠(ILS)的寿命,进行了抗肿瘤活性的体内研究。腹腔注射PHYCON制剂后的寿命增加(38.5%)与单独注射5天后的寿命增加(36.4%)相似。我们的研究结果表明,PHYCON抗肿瘤药物的可注射和可植入缓释制剂可能适合肿瘤化疗。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Application of PHYCON 6600 to achieve sustained release of an antitumor drug (carmofur).

This study attempted to develop sustained release implantable dosage forms based on PHYCON 6600, a new silicone gel. The solid gel is prepared at ambient temperature by polymerization of two basic components (PHYCON A and PHYCON B solutions) for about 1 h. The application we explored was the use of implantable PHYCON-drug composites in tumor therapy. Carmofur (1-hexylcarbamoyl-5-fluorouracil, HCFU) was chosen as a practical antitumor drug. Using an in vitro dissolution test, near zero-order release rate was observed over a period of about 35 days. The amount of drug released by the 'burst phenomenon' was found to be less than the HCFU toxic dose. In vivo studies of antitumor activity were carried out by measuring the lifespan of lymphoma-inoculated mice (ILS). The increase in lifespan (38.5%) following intraperitoneal administration of the PHYCON formulations was similar to that (36.4%) following injection of the drug alone for 5 days. Our results suggest that the injectable and implantable sustained release formulations of the antitumor drug in PHYCON might be suitable for tumor chemotherapy.

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