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Linear drug release donut-shaped tablets prepared using 3DP

机译:使用3DP制备的线性药物释放甜甜圈形片剂

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Three dimensional printing (3DP) is a solid freeform fabrication technique which employs powder processing and liquid binder materials in the construction of parts in a layer-wise manner. 3DP has drawn increasing attentions because of its outstanding capability, easy process and flexibility. 3DP is able to provide new strategies for the research and development of novel drug delivery devices due to its ability in controlling three-dimensional position of drugs and functional materials, microstructure, and local composition and surface texture in a single tablet accurately ande producibly.In this study, a kind of donut-shaped tablets conceived to furnish zero-order drug release characteristics are prepared using 3DP. The tablet consists of three sections. Both the top and the bottom sections without drug in them represent an inert and impermeable obstacle to water penetration and drug diffusion. Hydrophilic polymer HPMC with low viscosity is employed as drug carrier matrix to keep the tablets dissolution in erosion mechanism. The middle drug-loaded region is dividednto two parts: the peripheral annulus part has a high concentration of release-retardant materials, while the inner annulus part has a high concentration of drug. Thus, the erosion of the tablet surface is retarded and slower at the beginning of dissolution than the late dissolution process. Combined with the relatively lower concentration of drug in the outer region, the initial burst effect caused by imbibing of water and gelling of HPMC can be eliminated. Later, as the outer releasing surface area of cylindrical matrix decreases with time, the inner releasing surface area of the holes increases synchronously. As the height of the tablets remains stable, hence the erodible volume of the tablets in unitary time can keep comparatively constant, resulting in zero-order release profiles within the whole release period.To realize the designs features of special surface texture, non-uniform drug distributions and local variations of the release-retardant materials, the drug incorporated into the tablets both by dispensing the binder solution and by premixing with the excipients powders. The local variations of both the drug and the release-retardant materials are achieved by dispensing different binder solutions into different regions during the 3DP processes.In vitro dissolutions tests demonstrated that up to 95% of the drug acetaminophen is released from the prepared tablets at constant rates. The coating top and bottom layers had good adhesion strength with the drug-contained sections and offered consistent release retardation for the whole duration of dissolution process. The total release time periods of the drug could be modulated independently by the annulus thicknesses of tablets or by dispensing different passes of binder solution containing release-retardant material EC. The dose of acetaminophen could be modulated independently by the heights of tablets. Morphology and the erosion studies showed that the drug released from the tablets by simultaneous erosion of the outer tablet surface and inner cylindrical surface, keeping a comparatively constant releasing surface area to furnish constant release rate.It can be concluded that 3DP has utility, good flexibility and efficacy in fabricating tablets with complex design features for desired release profiles.
机译:三维印刷(3DP)是一种固体自由成形制造技术,该技术采用了粉末处理和液体粘合剂材料在部件中的层式的方式构造。 3DP已引起,因为其出色的性能,易加工性和灵活性越来越多的关注。 3DP是能够提供新颖的药物递送设备的研究和开发的新策略由于其在控制药物和功能材料,微结构的三维位置准确ANDE producibly.In能力,和局部组成和表面纹理在单一片剂这项研究中,一种环形的片剂的设想为配料零级的药物释放特征使用3DP制备。该平板电脑由三个部分组成。顶部和在它们不含药物的底部部分表示惰性和不渗透的障碍水渗透和药物扩散。具有低粘度的亲水性聚合物HPMC用作药物载体基质,以保持片的溶出在侵蚀机制。中间载药区域是dividednto两个部分:外围环形部分具有释放阻燃材料的高浓度,而内环形部具有的药物的高浓度。因此,片剂表面的侵蚀是在溶解比后期溶出过程的开始延迟和慢。与药物在外部区域中的相对较低的浓度相结合,引起的水吸液和HPMC的胶凝的初始突释效应可以消除。后来,随着圆筒状基体的外释放表面积随时间减小,孔的内释放表面积同步增加。作为片剂的高度保持稳定,因此,在单一时间片剂的可侵蚀的体积可保持恒定相对,导致零级释放曲线的整个释放内period.To实现设计特殊的表面纹理,非均匀的功能药物分布和释放性材料的局部变化,将药物掺入到片剂二者通过分配粘合剂溶液,并通过与赋形剂的粉末预混合。药物和释放阻燃材料两者的局部变化是通过在3DP processes.In体外溶出试验分配不同的粘合剂溶液为不同的区域实现证实,直到药物对乙酰氨基酚的95%是从以恒定的制备的片剂释放率。涂层的顶层和底层曾与含药部分良好的粘合强度,并提供一致的释放延迟对于溶解过程的整个持续时间。药物的总释放时间段可以独立地通过片剂的环形厚度或通过分配的含有释放性材料EC粘合剂溶液不同行程来调制。对乙酰氨基酚的剂量可以独立地由药片的高度来调节。形态,并表明,由外片剂表面和圆柱形内表面的同时侵蚀从片剂释放的药物,保持相对恒定的释放表面面积以得到恒定的释放rate.It可以得出结论,3DP具有实用性的侵蚀研究,良好的柔韧性和功效在制造具有复杂的设计特征为期望的释放曲线的片剂。

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