Development of novel "patient-tailored DDS"by plasma technique

虽然口服给药方便且患者可接受，但治疗效果通常取决于每个患者的胃肠（GI）环境。因此，“患者定制的药物输送系统（DDS）”应根据每个患者的胃肠道环境的诊断开发和管理。我们研究了等离子体辅助制备时间控制DDS和胃内漂浮DDS（FDDS），从而实现靶向胃肠道的“患者定制DDS”。以药物片剂为芯材，聚合物粉末为壁材，制备了双层压片，制备了时间控制型DDS和胃内给药型FDDS。氩等离子体辐照将导致抑制EudragitL 100 -55的溶解度，即使在可溶的pH值溶液中，由于表面交联反应的发生。 ...更多信息 以Eudragit L100-55为壁材制成双层压片，可使药物在一定时间内完全缓释。延迟时间可通过等离子体操作条件来控制，我们利用外层捕获释放的二氧化碳制备双层压片，通过等离子体照射获得胃内FDDS。使用甲基乙烯基醚-马来酸酐共聚物（VEMA）和VEMA与邻苯二甲酸羟丙基甲基纤维素的混合物作为外层，制备双层压片。结果发现，等离子体辐照的片剂在模拟胃液中保持浮力很长一段时间，并且药物释放受到相当大的抑制。通过选择合适的等离子体操作条件，可以控制药物从片剂中以所需的速率释放。本研究结果清楚地表明，如果选择合适的聚合物作为双层压片的壁材以及等离子体操作条件，可以制备出各种所需的DDS装置。少

Although oral delivery is convenient to administration and acceptable for patients, the therapeutic effects often depend on the each patient's gastrointenstinal (GI) environment. Therefore, the "Patient-Tailored Drug Delivery System (DDS)" should be developed and administered based on the diagnosis of each patient's GI environment. We have studied plasma-assisted preparation of time-controlled DDS and intragastric floating DDS (FDDS) leading to the "Patient-Tailored DDS" targeting the GI tract. Double-compressed tablets composed of drug tablet as a core material and polymer powder, which was used as pharmaceutical aids, as a wall material was prepared to fabricate time-controlled DDS and inttragastric FDDS.Since plasma-crosslinkable acrylic monomers are one of the component polymers in Eudragits L100-55, argon plasma-irradiation would lead to the suppression of Eudragit L100-55 solubility even in a dissoluble pH-value solution due to the occurrence of the surface cross-link reactions. … More When Eudragit L100-55 is used as a wall material of the double-compressed tablet, the initial drug release could be completely sustained for a certain period of time. The lag-time could be controlled by plasma operational conditions.We have obtained the intragastric FDDS by plasma-irradiation when the double-compressed tablet was prepared using the outer layer to trap evolved carbon dioxide. The double-compressed tablet was prepared using methyl vinyl ether-maleic anhydride copolymer (VEMA), and a mixture of VEMA and hydroxypropyl methylcellulose phthalate as an outer layer. It was found that the tablet plasma-irradiated remains buoyant in the simulated gastric fluids for a prolonged period of time, and the drug release is considerably suppressed. The drug release can be controlled at a desired rate from the tablets by selecting the plasma operational tunings.The present results have clearly shown that one can prepare a variety of desired DDS devices, if one selects the tailored-polymers for wall materials of double-compressed tablets as well as plasma operational conditions. Less