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

虽然口服给药方便，患者可以接受，但治疗效果往往取决于每个患者的胃肠道(GI)环境。因此，应该根据每个患者的胃肠道环境的诊断来开发和管理“患者定制的药物输送系统(DDS)”。我们已经研究了等离子体辅助制备时间控制的DDS和胃内浮动DDS(FDDS)，从而产生了针对胃肠道的“患者定制DDS”。以药片为芯材，以聚合物粉末为壁材制成双压片，制备了时控型DDS和胃内FDDS。由于等离子体可交联丙烯酸酯单体是Eudradits L100-55的组成聚合物之一，所以即使在可溶的pH溶液中，Ar等离子体辐照也会由于表面交联反应的发生而导致Eudradit L100-55的溶解度受到抑制。…此外，当使用Eudradit L100-55作为双重压片的壁材时，最初的药物释放可以完全持续一段时间。滞留时间可以通过等离子体操作条件来控制。利用外层捕获释放的二氧化碳制备双压片时，我们通过等离子体辐照获得了胃内FDDS。以甲基乙烯基醚-马来酸酐共聚物(VEMA)和邻苯二甲酸羟丙基甲基纤维素的混合物为外层，制备双压片。研究发现，经等离子体辐照后的片剂在模拟胃液中可保持较长时间的浮力，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参数，可以控制药物从片剂中的释放速度。目前的研究结果表明，只要选择合适的聚合物作为二次压片的壁材以及等离子体操作条件，就可以制备出各种所需的DDS装置。较少

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