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

我们研究了等离子体辐照的有机聚合物在药物工程领域的新应用工作，包括药物助剂。等离子体诱导有机聚合物表面自由基的研究对于理解等离子体处理的本质是非常重要的。用电子自旋共振技术结合系统的计算机模拟，详细研究了一元碳水化合物(α-和β-葡萄糖)、二元碳水化合物(麦芽糖和纤维二糖)和多碳水化合物(纤维素及其衍生物)的等离子体诱导表面自由基。等离子体辐照纤维素衍生物的ESR研究表明，等离子体诱导形成的自由基随取代基性质的不同而敏感。此外，我们还研究了纤维素和直链淀粉碱…等葡萄糖多糖的机械诱导自由基的形成更多的关于ESR与等离子体诱导的自由基的比较。最耐人寻味的事实之一是，组成的自由基都是葡萄糖衍生的中链烷基，就像在等离子体辐射的情况下一样，尽管已知机械活性物质是由聚合物主链断裂产生的。因此，可以合理地假设，在室温下，主要由多糖的1，4-糖苷键裂解形成的机械力能从葡萄糖单元中抽出氢来产生葡萄糖衍生的中链烷基。由于指定血浆的每个参数最终影响到产生表面自由基的血浆强度，因此我们研究了一种估计等离子体功率的方法，该方法对等离子体处理的实验和实际设计有用。结果表明，肌醇自由基的生成可以作为有效等离子体功率的一个指标。在对多种聚合物上等离子体诱导产生自由基的性质进行一系列研究的基础上，我们开发了几种新型的药物传递系统(DDS)制剂，其中包括：(1)制备适用于储存型缓释和缓释DDS的多层片剂；以及(2)通过等离子体辐照粉末聚合物的机械应用来制备适用于基质类型DDS的功能化复合粉末。该方法的优点是(1)完全干法制备DDS，(2)药物释放速率易于控制，(3)避免直接接触药物的等离子体，(4)在不影响整体性能的情况下对聚合物进行改性。因此，希望在目前正在进行的尝试过程中开发更多的实际应用程序。较少

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