Development of Novel Drug Engineering Utilizing the Electronic Property on the Solid Surface

利用固体表面电子特性开发新药物工程

基本信息

批准号：
11672147
负责人：
KUZUYA Masayuki
金额：
$ 2.3万
依托单位：
Gifu Pharmaceutical University
依托单位国家：
日本
项目类别：
Grant-in-Aid for Scientific Research (C)
财政年份：
1999
资助国家：
日本
起止时间：
1999 至 2000
项目状态：
已结题

来源：
https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-11672147/
关键词：
plasma treatment mechanolysis radical drug delivery system (DDS)delayed-release tablet dry process crosslinking reaction monolithic DDS 乾式DDS 低温プラズマ表面ラジカル ESR DDS メカノケミカル反応ラジカル再結合セルロース誘導体イノシトール

项目摘要

We have studied novel application works in the field of drug engineering using plasma-irradiated organic polymers including pharmaceutical aids. The study of the plasma-induced surface radicals of organic polymers is very important for understanding of the nature of plasma treatment. Plasma-induced surface radicals of monocarbohydrates (α-and β-glucose), dicarbohydrates (maltose and cellobiose), and polycarbohydrates (cellulose and its derivatives) were studied in detail by electron spin resonance (ESR) coupled with the systematic computer simulations. The ESR study on plasma-irradiated cellulose derivatives revealed that the plasma-induced radicals formed vary with the nature of substituents in a sensitive manner. These findings provide a basis for further application works in the preparation of new pharma-ceutically useful materials.We also studied on the mechanically induced free radical (mechanoradical) formation of glucose-based polycarbohydrates such as cellulose and amylose base … More d on ESR on its comparison with plasma-induced radicals. One of the most intriguing facts is that the component radicals are all glucose-derived mid-chain alkyl radicals as in the case of plasma irradiation, although it is known that mechanoradicals are produced by the polymer main-chain scission. It can be reasonably assumed, therefore, that the mechanoradicals primarily formed by 1, 4-glucosidic bond cleavage of polycarbohydrates at room temperature underwent a hydrogen abstraction from the glucose units to give rise to the glucose-derived mid-chain alkyl radicals.Since each parameter to specify the plasma eventually affects the intensity of plasma, "plasma power", to generate the surface radicals, we have examined to develop the method to estimate the plasma power useful for experimental and practical designs of plasma treatment. It was shown that the formation of myo-inositol radical could be able to use as an index of the effective plasma power. Even if the parameters of plasma operational conditions such as actual discharge wattage, system pressure, the geometry of plasma apparatus or the location of materials are changed, the plasma power will be deduced by measuring the quantity of myo-inositol radicals.On the basis of findings from a series of studies on the nature of plasma-induced radicals formation on a variety of polymers, we were able to develop several novel drug delivery systems (DDS) preparation, which include (1) preparation of multilayered tablets applicable for reservoir-type DDS of sustained- and delayed- release, and (2) fabrication of functionalized composite powders applicable for matrix-type DDS by mechanical applications of plasma-irradiated powder polymers. The advantages of the present approach for preparation of DDS are (1) totally dry process, (2) facile control of drug release rates, (3) avoidance of direct plasma-exposure to drugs, and (4) polymer modification without affecting the bulk properties. Thus, it is hoped that more practical applications will be developed in the course of attempt now in progress. Less

我们研究了包括药物的有机聚合物在包括血浆诱导的有机聚合物表面自由基的药物工程领域，这对于了解血浆治疗的性质很重要。葡萄糖），通过电子自旋共振（ESR）以及系统的计算机模拟详细研究了dicarbohydrates（Maltose和bobobiose）。 SE的敏感方式为新的药物的诱发基于葡萄糖的多碳水化合物（例如细胞糖基碱）的自由基（机械自由基）提供了应用最有趣的事实是，成分是葡萄糖衍生的中链烷基自由基，因为血浆辐照，allthooth已知机械自由基是由聚合物主巧克力BE产生的。，多碳水化合物室温的4-葡萄糖苷键裂解，从葡萄糖到葡萄糖衍生的中链烷基自由基进行了抽象。为了产生表面自由基，我们已经检查了质量处理的实验和实践设计。，血浆设备的几何形状或材料的位置是敏感的，血浆功率将通过肌醇自由基的数量来推导。从一系列关于等离子体诱导的自由基在A上形成本质的研究的发现的基础。多种聚合物赔偿，其中包括（1）制备持续和延迟释放的适用于储层的多层片剂DDS，以及（2）适用于矩阵型DDS的功能化复合粉末的制造辐射聚合物希望更多