The Influence of Temperature and Viscosity of Polyethylene Glycol on the Rate of Microwave-Induced In Situ Amorphization of Celecoxib

Microwaved-induced in situ amorphization of a drug in a polymer has been suggested to follow a dissolution process, with the drug dissolving into the mobile polymer at temperatures above the glass transition temperature (T_g) of the polymer. Thus, based on the Noyes–Whitney and the Stoke–Einstein equations, the temperature and the viscosity are expected to directly impact the rate and degree of drug amorphization. By investigating two different viscosity grades of polyethylene glycol (PEG), i.e., PEG 3000 and PEG 4000, and controlling the temperature of the microwave oven, it was possible to study the influence of both, temperature and viscosity, on the in situ amorphization of the model drug celecoxib (CCX) during exposure to microwave radiation. In this study, compacts containing 30 wt% CCX, 69 wt% PEG 3000 or PEG 4000 and 1 wt% lubricant (magnesium stearate) were exposed to microwave radiation at (i) a target temperature, or (ii) a target viscosity. It was found that at the target temperature, compacts containing PEG 3000 displayed a faster rate of amorphization as compared to compacts containing PEG 4000, due to the lower viscosity of PEG 3000 compared to PEG 4000. Furthermore, at the target viscosity, which was achieved by setting different temperatures for compacts containing PEG 3000 and PEG 4000, respectively, the compacts containing PEG 3000 displayed a slower rate of amorphization, due to a lower target temperature, than compacts containing PEG 4000. In conclusion, with lower viscosity of the polymer, at temperatures above its T_g, and with higher temperatures, both increasing the diffusion coefficient of the drug into the polymer, the rate of amorphization was increased allowing a faster in situ amorphization during exposure to microwave radiation. Hereby, the theory that the microwave-induced in situ amorphization process can be described as a dissolution process of the drug into the polymer, at temperatures above the T_g, is further strengthened.     

Development and Validation of an Automated Zone Fluidics-Based Sensor for In Vitro Dissolution Studies of Captopril Using Total Error Concept

In the present research, a zone fluidics-based automated sensor for the analysis of captopril in in vitro dissolution samples is reported. Captopril is reacted under flow conditions with Ni(II) (10 mmol L⁻¹) in alkaline medium (0.15% v/v NH₃) to form a stable derivate, which is monitored spectrophotometrically at 340 nm. The chemical and instrumental parameters were carefully investigated and optimized. The validation of the developed method was performed in the range of 5 to 120% of the expected maximum concentration using the accuracy profiles as a graphical decision-making tool. The β-expectation tolerance intervals did not exceed the acceptance criteria of ±10%, which means that 95% of future results will be encompassed in the defined bias limits. The variation of the relative bias ranged between −2.3% and 3.5% and the RSD values for repeatability and intermediate precision were lower than 2.3% in all cases. The limit of detection (LOD), and the lower and the upper limit of quantification (LLOQ, ULOQ) were satisfactory and found to be 1%, 5% and 120% (corresponding to 0.6, 2.78 and 66.67 μg mL⁻¹ in dissolution medium). The developed method was successfully applied for the analysis of captopril in dissolution tests of two commercially available batches.     

铝制炊具溶出铝量及影响因素的研究

采用分光光度法对铝制炊具溶出铝量及影响因素展开了研究。结果表明,铝制炊具溶出的铝量随温度升高明显增加;且在一定温度下,使用家用调味品也会增加铝制品溶出的铝量。     

纤维素在离子液体中的溶解性能及机理研究进展

综述了纤维素在离子液体中的溶解性能和机理的研究进展,总结了纤维素在离子液体中发生溶胀、溶解的物化特性;指出纤维素在离子液体中的溶解属于直接溶解,溶解温度、溶解时间、加热方式、离子液体结构及是否含水等均可影响纤维素的溶解性能;分析了离子液体体系中纤维素应用方面存在的问题,即用于溶解纤维素的离子液体种类有限,溶解机理尚无成熟和完整的理论模型,有待于进一步研究.     

新型β-二酮配位剂用于制备高分子量速溶型聚丙烯酰胺

文章采用均聚共水解的方法,以丙烯酰胺为单体、Na2CO3为水解剂,β-二酮为配位剂,复合引发体剂体系下,制备了高分子量速溶型聚丙烯酰胺,研究了单体、引发剂、配位剂、pH值以及引发温度对反应速率和产物分子量的影响。结果表明,当单体、引发剂、配位剂的质量分数分别为25%、0.005%、0.05%,pH值为10.5,引发温度为15℃时,得到水解度为25%左右,重均分子量为1 900×104以上的高分子量速溶型阴离子部分水解聚丙烯酰胺。     

PAN纤维径向结构及其表征方法的研究

以湿法纺丝制备的聚丙烯腈（PAN）纤维为研究对象,将纤维在二甲基亚砜（DMSO）水溶液中进行溶解,通过其溶解特征探讨了纤维的溶解机理,进而对纤维的径向结构进行分析表征,并结合红外测试分析了其径向结构对预氧化进程的影响。结果表明：PAN纤维的溶解机理为自内向外进行;通过纤维的溶解特征可分析出纤维径向结构,且与红外测试所得结论相同;凝固浴温度在45℃时与25℃相比,所得纤维径向上皮层及芯层更致密,过渡区域更疏松;预氧化进程初期,氧气更易在致密程度更低更疏松的纤维径向上发生扩散。     

论“入户抢劫”的认定

"入户抢劫"作为抢劫罪法定加重情节,其认定对刑罚至关重要.然而,"入户抢劫"的认定在理论和实务中仍存在一些争议和分歧.本文欲根据法律及相关解释,对"入户抢劫"的理解和认定进行简单论述,以期益于司法实践.     

审判质量管理的“满意”与“公正”之间

公众对案件的"满意度"与"司法公正"的内涵本身存在的原理性冲突,当事人对事件结果公正的不同理解、媒体对社会舆论的导向,直接影响着公众对司法案件的认识和评价。一旦舆情被某种因素引导,社会舆论就容易发展趋向于一种或几种极端的论调,产生"群体极化"现象。其中非理性的部分社会舆情将产生巨大的力量,可能引发"满意"与司法公正的较量。"河北王朝案"就是发生在审判质量管理背景下舆情与司法的一次激烈冲突。因此,应弱化以"满意度"作为案件质量评估的指标,从而回归司法独立、司法公正的本质。     

控压钻井气侵流动分析模型研究与应用

控压钻井(managed pressure drilling,MPD)发生气侵时,可通过实时动态压力控制在保持井底压力恒定的情况下实现气侵有效控制与安全排溢,气侵安全控制的关键是实时准确地井筒流动分析。通过理论分析建立了考虑侵入流体在不同类型钻井液中溶解析出影响的井筒气液两相流模型,考虑动态回压影响,给出了不同控压钻井模式下模型求解的初始及边界条件。基于有限差分法充分考虑不同控压模式下的压力动态调节对气体滑脱、相态变化的综合影响,给出了该模型的求解流程。运用全尺寸模拟井筒气侵测试数据对模型进行了验证分析,运用该模型对页岩气水平井控压钻井气侵控制进行了计算分析。结果表明,该模型具有较高的精度,能够很好地为控压钻井气侵控制与分析提供技术支持。     

Study of mechanics of physically transient electronics: A step toward controlled transiency

Transient electronics is a class of electronic devices designed to maintain stable operation for a desired and preset amount of time; and, undergo fast and complete degradation and deconstruction once transiency is triggered. Controlled and programmed transiency in solvent‐triggered devices is strongly dependent on chemical and physical interactions between the solvent and the device, as well as those within the device itself, among its constituent components. Mechanics of transiency of prototypical transient circuits demonstrate strong dependence of the transiency characteristics on that of the substrate. In the present study, we demonstrate the control of transiency through the dissolution behavior of a substrate for the devices with electronic parts composed of colloidal units. It is observed that the physical circuit–substrate interactions are the dominating factors in defining the overall transiency behavior of the device. © 2015 Wiley Periodicals, Inc. J. Polym. Sci., Part B: Polym. Phys. 2016 , 54, 517–524