采用原研制剂制备米诺膦酸片及体外溶出度的一致性考察

制备米诺膦酸片,并以原研制剂为参比制剂,采用f2相似因子法对两者体外溶出度的一致性进行考察.建立合适的体外溶出度测定方法,研究参比制剂的溶出情况,通过单因素试验对辅料的用量进行筛选,制备出米诺磷酸片.比较自制品与原研制剂在不同溶出介质中的溶出行为,评价两者体外溶出行为的相似性.结果表明:制备的米诺膦酸片剂与原研制剂在4种不同pH值溶出介质中的溶出相似因子f2均大于50;制备的米诺膦酸片剂与原研制剂体外溶出行为相似.国家自然科学基金资助项目(81302652);;福建省自然科学基金资助项目(2015J01342

半富马酸替诺福韦艾拉酚胺的合成工艺优化

对最新抗乙肝药物半富马酸替诺福韦艾拉酚胺（TAF）的合成工艺进行优化研究.以腺嘌呤（1）为原料,与（R）-碳酸丙烯酯反应得到（R）-9-（2-羟丙基）腺嘌呤.然后,将产物经磷叶立德取代,水解反应得到（R）-9-（（2-磷酸单苯酯基）甲氧基）丙基)-腺嘌呤.最后,将所得产物经取代、酰化、缩合、成盐反应得到目标产物TAF,并对各步反应条件进行优化.结果表明:总收率达32.1%（以腺嘌呤计）,较原工艺提高23.1%,目标化合物及主要中间体经电子轰击质谱（EI-MS）、核磁共振氢谱（1H-NMR）、核磁共振碳谱(13C-NMR)确证结构;与现有文献报道的TAF合成工艺相比,优化后的工艺总收率大幅提高,反应成本降低,反应时间缩短,可避免生产过程中的安全隐患,适合工业化生产.国家重点研发计划项目(2016YFE0101700

Preparation of pDNA-Loaded Thiolated Chitosan Nanoparticles and Optimization by Using Box-Behnken Design and Response Surface Method

以巯基壳聚糖（TCS）为基因载体,采用离子交联法制备能用于基因口服研究的质粒DNA-巯基壳聚糖纳米粒（pDNA-TCS-NPs）.分别以TCS质量浓度、三聚磷酸钠（TPP）质量浓度、pH值和转速为考察对象,以pDNA-TCS-NPs粒径和Zeta电位为评价指标,采用4因素3水平Box-Behnken效应面法筛选最佳制备工艺,并对其外观形态,包封率等体外性质进行考察.结果表明：TCS质量浓度为0.80mg·mL（-1）,TPP质量浓度为0.65mg·mL（-1）,pH=5.3,转速为2 000r·min（-1）是最优制备工艺,可制得粒径为（134.21±1.34）nm,Zeta电位为（24.36±0.29）mV,包封率在（80.26±0.56）%,形状规则且分散良好的pDNA-巯基壳聚糖纳米粒;Box-Behnken实验设计可用于预测和优化pDNA-TCS-NP制备工艺优化筛选.Preliminary exploration to prepare plasmid DNA-loaded thiolated chitosan nanoparticles（pDNATCS-NPs）which can be used for gene oral administration was investigated.Using TCS as gene carriers,the pDNA-TCS-NPs were prepared by the ionic cross-linking method.The effects of the concentrations of TCS and TPP,pH value and stirring speed were investigated on the particle diameter and zeta potential of the pDNA-TCS-NPs.In addition,the formula was optimized by Box-Behnken design and response surface method with four factors and three levels,and the physic-chemical properties such as the shape and encapsulation efficiency were also studied.The results showed that the optimal formula was as follows：TCS concentration 0.80mg·mL（-1）,TPP concentration 0.65mg·mL（-1）,pH 5.3,and stirring speed 2 000r·min（-1）.Particle diameter was（134.21±1.34）nm,zeta potential was（24.36±0.29）mV,and efficiency was（80.26±0.56）%.under the optimal conditions.The pDNA-TCS-NPs showed uniform spherical solid particles with regular shape and ideal uniformly dispersion.It′s also confirmed that the Box-Behnken experimental design and response surface method could be used to predict and optimize the pDNA-loaded TCS nanoparticles.国家自然科学基金资助项目（81302652）;福建省自然科学基金资助项目（2015J01342

基于串联读出电路的探测器位置识别方法研究

核辐射成像依赖于位置灵敏探测器，其所需的读出电子学通道数一般较多。而传统采用电阻矩阵网络对电荷进行分流的信号读出方法，虽然大幅度减少了电子学通道的数量，但能量分辨率也显著变差。本文设计了一种串联读出电路来减少读出电子学的通道数量，并保证较好的能量分辨能力。探测器选用4×4阵列排布的CsI（Tl）闪烁体，并耦合了阵列SiPM来产生电流信号。电流信号经过串联电阻网络后，在两端通过电荷灵敏前放转化为电压信号。因此，单个探头模组的串联读出电路所需的读出电子学的通道数量仅为两路，而探测器的位置则是利用两端信号幅度比进行识别。针对662 keV能量的实验结果表明，探测器的相对位置分辨率为0.54%，其测得能量分辨率可达6.51%

Determination of the number of ψ(3686) events taken at BESIII

The number of ψ(3686) events collected by the BESIII detector during the 2021 run period is determined to be (2259.3±11.1)×106 by counting inclusive ψ(3686) hadronic events. The uncertainty is systematic and the statistical uncertainty is negligible. Meanwhile, the numbers of ψ(3686) events collected during the 2009 and 2012 run periods are updated to be (107.7±0.6)×106 and (345.4±2.6)×106, respectively. Both numbers are consistent with the previous measurements within one standard deviation. The total number of ψ(3686) events in the three data samples is (2712.4±14.3)×10^

Prediction of Energy Resolution in the JUNO Experiment

International audienceThis paper presents the energy resolution study in the JUNO experiment, incorporating the latest knowledge acquired during the detector construction phase. The determination of neutrino mass ordering in JUNO requires an exceptional energy resolution better than 3% at 1 MeV. To achieve this ambitious goal, significant efforts have been undertaken in the design and production of the key components of the JUNO detector. Various factors affecting the detection of inverse beta decay signals have an impact on the energy resolution, extending beyond the statistical fluctuations of the detected number of photons, such as the properties of liquid scintillator, performance of photomultiplier tubes, and the energy reconstruction algorithm. To account for these effects, a full JUNO simulation and reconstruction approach is employed. This enables the modeling of all relevant effects and the evaluation of associated inputs to accurately estimate the energy resolution. The study reveals an energy resolution of 2.95% at 1 MeV. Furthermore, the study assesses the contribution of major effects to the overall energy resolution budget. This analysis serves as a reference for interpreting future measurements of energy resolution during JUNO data taking. Moreover, it provides a guideline in comprehending the energy resolution characteristics of liquid scintillator-based detectors

JUNO Sensitivity on Proton Decay p→νˉK+p\to \bar\nu K^+ Searches

The Jiangmen Underground Neutrino Observatory (JUNO) is a large liquid scintillator detector designed to explore many topics in fundamental physics. In this paper, the potential on searching for proton decay in $p\to \bar\nu K^+$ mode with JUNO is investigated.The kaon and its decay particles feature a clear three-fold coincidence signature that results in a high efficiency for identification. Moreover, the excellent energy resolution of JUNO permits to suppress the sizable background caused by other delayed signals. Based on these advantages, the detection efficiency for the proton decay via $p\to \bar\nu K^+$ is 36.9% with a background level of 0.2 events after 10 years of data taking. The estimated sensitivity based on 200 kton-years exposure is $9.6 \times 10^{33}$ years, competitive with the current best limits on the proton lifetime in this channel

JUNO sensitivity on proton decay p → ν K + searches*

The Jiangmen Underground Neutrino Observatory (JUNO) is a large liquid scintillator detector designed to explore many topics in fundamental physics. In this study, the potential of searching for proton decay in the $p\to \bar{\nu} K^+$ mode with JUNO is investigated. The kaon and its decay particles feature a clear three-fold coincidence signature that results in a high efficiency for identification. Moreover, the excellent energy resolution of JUNO permits suppression of the sizable background caused by other delayed signals. Based on these advantages, the detection efficiency for the proton decay via $p\to \bar{\nu} K^+$ is 36.9% ± 4.9% with a background level of $0.2\pm 0.05({\rm syst})\pm$$0.2({\rm stat})$ events after 10 years of data collection. The estimated sensitivity based on 200 kton-years of exposure is $9.6 \times 10^{33}$ years, which is competitive with the current best limits on the proton lifetime in this channel and complements the use of different detection technologies