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

我们研究了等离子体辐照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具有重要意义。利用电子自旋共振（ESR）技术结合计算机模拟，详细研究了单碳水化合物（α-和β-葡萄糖）、二碳水化合物（麦芽糖和纤维二糖）和多碳水化合物（纤维素及其衍生物）等离子体诱导的表面自由基。等离子体辐照纤维素衍生物的ESR研究表明，等离子体诱导的自由基形成的变化与取代基的性质在一个敏感的方式。这些结果为进一步应用于制备新的药用材料提供了基础。我们还研究了葡萄糖基多糖如纤维素和直链淀粉基的机械诱导自由基的形成 ...更多信息 d在ESR上与等离子体诱导的自由基进行比较。最有趣的事实之一是，组分自由基都是葡萄糖衍生的中链烷基自由基，如在等离子体照射的情况下，尽管已知机械自由基是由聚合物主链断裂产生的。因此，可以合理地假设，主要由聚碳水化合物在室温下的1，4-糖苷键断裂形成的机械自由基经历了从葡萄糖单元的氢提取，以产生葡萄糖衍生的中链烷基自由基。由于指定等离子体的每个参数最终影响等离子体的强度，"等离子体功率"，以产生表面自由基，我们已经研究开发了用于等离子体处理的实验和实际设计的估计等离子体功率的方法。结果表明，肌醇自由基的形成可以作为等离子体有效功率的一个指标。即使等离子体工作条件的参数如实际放电瓦数、系统压力、等离子体装置的几何形状或材料的位置发生变化，等离子体功率也将通过测量肌醇自由基的量来推断。根据对等离子体诱导自由基在各种聚合物上形成的性质的一系列研究结果，我们能够开发出几种新型的药物递送系统（DDS）制剂，包括（1）适用于缓释和延迟释放的阿托伐他汀型DDS的多层片剂的制备，和（2）通过等离子体辐照的粉末聚合物的机械应用制造适用于基质型DDS的功能化复合粉末。本发明制备DDS的方法的优点是（1）完全干法，（2）易于控制药物释放速率，（3）避免直接等离子体暴露于药物，和（4）聚合物改性而不影响本体性质。因此，希望在目前正在进行的尝试过程中开发出更多的实际应用。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