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

我们使用包括药物艾滋病在内的血浆辐射有机聚合物研究了药物工程领域的新型应用作品。对有机聚合物的血浆诱导的表面自由基的研究对于理解血浆处理性质非常重要。血浆诱导的单碳水化合物（α-和β-葡萄糖），二碳水化合物（麦芽糖和纤维纤维）以及多碳水化合物（纤维素及其衍生物）的表面自由基通过与系统的计算机仿真一起详细研究了电子旋转（ESR）。 ESR对等离子体辐射的纤维素衍生物的研究表明，血浆诱导的自由基以敏感方式随着微接的性质而变化。这些发现为进一步应用的工作提供了基础，以制备新的药物 - 头为有用的材料。我们还研究了机械诱导的自由基自由基（机械自由）形成的基于葡萄糖的多碳水化合物（例如纤维素和淀粉酶基础），例如纤维素和淀粉糖基碱基…在与血浆诱导的自由基的比较上，在ESR上更多的D。最有趣的事实之一是，分量自由基都是葡萄糖衍生的中链烷基自由基，就像在血浆照射的情况下一样，尽管已知机械是由聚合物主链分割产生的。因此，可以合理地假定，由1、4-葡萄糖糖苷键裂解在室温下的多碳水化合物形成的机械型，从葡萄糖单位进行了氢抽象，从而引起葡萄糖衍生的中链烷基激进的质量，以最终影响普拉斯的质量，以指定质量的质量，以构成plas的强度。激进分子，我们已经检查了为估计血浆治疗实验和实用设计的血浆功率的方法。结果表明，肌醇自由基的形成可以用作有效等离子体功率的索引。即使等离子体操作条件的参数，例如实际排放瓦数，系统压力，血浆仪器的几何形状或材料的位置发生了变化，也将通过测量肌醇自由基的数量来推导血浆功率，从而从一系列关于等离子体诱导的plos to pron to to Protimation to Protimation to Protimation的研究的基础，从准备工作包括（1）制备可用于持续和延迟释放的Reserver-type DDS的多层片剂，以及（2）通过机械施用的矩阵型DDS制造适用于矩阵型DDS的功能化复合粉末，该粉末是通过机械应用的，可用于矩阵型DDS。当前制备DDS的方法的优点是（1）完全干燥的过程，（2）轻松控制药物释放率，（3）避免直接血浆暴露于药物，以及（4）聚合物修饰而不会影响块状特性。这是希望在正在进行的尝试过程中开发更实际的应用程序。较少的