聚吡咯／聚合物固体电解质双层复合膜研究

在聚合物固体电解质（聚乙二醇不饱和聚酯网络－LiClO4)中进行吡咯聚合原位制得了聚吡咯／聚合物固体电解质双层复合膜。用扫描电镜观察复合膜的界面结构,用循环伏安和交流阻抗法研究了复合膜的电化学杂脱掺杂性能。结果表明,聚吡咯／聚合物固体电解质双层复合膜具有相互穿插渗透的固／固密接界面结构,这种界面结构改善了聚吡咯和聚俣物固体电解质间的界面接触,提高了聚吡咯在聚俣物固体电解质中的电化学掺杂脱掺杂性能。     

Role of shear wave elastography measured in the flaccid state in predicting arteriogenic erectile dysfunction

The gold-standard method for diagnosing arteriogenic erectile dysfunction (AED) is the penile Doppler ultrasonography. We proposed a novel method for predicting AED using ultrasonic shear wave elastography (SWE) considering that the former was invasive and variable. A total of 98 male patients were enrolled in our study, referred for ED between December 2018 and October 2020. For comparison, we also included 42 volunteers from the Healthy Physical Examination Center of our hospital. The Penile Doppler Ultrasonography (PDU) and SWE were performed for all patients with the intracavernosal injection (ICI). We named three groups as AED group, nonvascular ED group and healthy controls group. No statistically significant differences were found among the three groups in terms of demographic and clinical characteristics. There were no significant differences in IIEF-5 between AED and nonvascular ED. A significant (r = 0.642, p < 0.0001) positive correlation between flaccid and erectile SWE was observed. With a cut-off value of 13.45 KPa, the area under curve, specificity, and sensitivity of the SWE values under the flaccid state in distinguishing AED from healthy subjects were 0.867, 0.786 and 0.896 respectively. The SWE value in the flaccid state can distinguish the AED from healthy subjects.     

有机溶液环境下中药成分的纳滤分离机制及适用性研究策略

随着有机溶液在中药制药领域应用的逐渐普遍,涉及到提取、醇沉、树脂洗脱剂成分制备等环节,从而衍生出衔接性的热处理精制引起中药成分转化、溶剂污染等问题。纳滤具有常温化分离优势,但适用于水溶液的分离模型在有机溶液中存在明显的局限性。通过综述纳滤分离机制,结合复杂溶液体系下中药成分的真实状态和传质行为,以期发现适用于有机溶液环境的中药成分纳滤分离研究策略,提升纳滤技术在中药制药领域的适用性,推动中药资源的合理化利用。     

择业期间大学生焦虑水平及其影响因素

目的 :对择业期间大学生焦虑水平及其影响因素进行调查 ,为高校心理卫生工作提供科学依据。方法 :采用“状态—特质焦虑量表”对 5 2 2名大学生择业期间焦虑水平进行测查 ,采用问卷调查法及访谈法探讨影响择业期间大学生焦虑水平的因素。结果 :择业情境导致大学生焦虑水平普遍升高 ,部分学生呈过度焦虑状态。择业期间大学生焦虑水平受自身条件、个人理想、社会环境、学校教育、家庭期望等因素的综合影响 ,其中自身条件、个人理想为首要因素。结论 :择业期间大学生产生焦虑的根本原因在于职业理想与实现可能的矛盾冲突     

Ca2+ channel actions of the non-dihydropyridine Ca2+ channel antagonist Ro 40-5967 in vascular muscle cells cultured from dog coronary and saphenous arteries

Summary We studied the membrane effects of (1S,2S)-2-(2-[[3-2(benzimidazolyl) propyllmethylamino]ethyl)-6-fluoro-1,2,3,4-tetrahydro-l-isopropyl-2-naphthyl-methoxy-acetate dihydrochloride, Ro 40-5967, a new non-dihydropyridine (DHP) Ca²⁺ channel antagonist, on dog coronary and saphenous arterial vascular muscle cells using the whole-cell patch-clamp method. Long-lasting (L-type) inward currents in 20 mM Ba²⁺ were measured over a range of test potentials (300 ms) from –50 mV to + 90 mV from a holding potential of –80 mV in the presence of 1 M Bay k8644 (a DHP Ca²⁺ agonist). Ro 40-5967 caused a concentration-dependent suppression of Ca²⁺ channel currents in muscle cells from both arteries, with greater potency on coronary than saphenous arterial cells. The concentration of Ro 40-5967 which inhibited the magnitude of peak inward currents by 50% (IC₅₀) was estimated to be 1 M (n = 5) in muscle cells from coronary artery and 10 M (n = 4) in saphenous artery. Ro 40-5967 (1 M) decreased the amplitude of the activation current-voltage relationship for coronary L-type Ca²⁺ channel currents over a wider range of membrane potentials than verapamil, diltiazem, or nifedipine. In contrast, block of Ca²⁺ channel currents in saphenous artery cells by 1 M Ro 40-5967 was only observed at command potentials positive to 0 mV. Ro 40-5967 (1 M) significantly shifted the voltage-inactivation curve downward by 40% in coronary (n = 4), but only by 18% in saphenous arterial muscle cells (n = 3). The non-parallel shift of the coronary artery inactivation curve suggests that pronounced resting channel block is a notable feature of Ro 40-5967. The marked inhibition of Ba²⁺ current by 1 M Ro 40-5967 in the inactivation protocol in coronary arterial muscle cells was found over the entire range of membrane holding potentials tested, while inhibition in the saphenous artery inactivation curve occurred only from holding potentials more positive than –40 mV. Therefore, Ro 40-5967 is unique: 1) in acting over a wider range of voltages, on both instantaneous and resting Ca²⁺ currents, than other Ca²⁺ antagonists; 2) in producing more significant resting state block; and 3) in acting with selectivity for coronary over saphenous arteries.This research was supported by National Institutes of Health grants HL38537, HL38645, and by F. Hoffmann-La Roche, Basel, Switzerland     

Effect of hepatic cirrhosis on the pharmacokinetics of theophylline in rats

The experimental hepatic cirrhosis was induced either by bile duct ligation (BDL) or by pretreatment with dimethylnitrosamine (DMNA). The pharmacokinetics of theophylline were studied after a single intravenous or a single oral administration. Using the ultrafiltration method, protein-drug binding experiments were also carried out. The bilirubin level was several-fold increased by BDL, but not by DMNA treatment. The albumin content was decreased in both cirrhotic groups. The total clearance (Clt, ml/kg/hr) of theophylline in both hepatic cirrhosis groups significantly decreased and the terminal half-life (t_1/2) in the cirrhotic rats was increased about two-fold after intravenous and oral administration. The volume of distribution at steady state (Vdss, ml/kg) was increased slightly in the cirrhotic groups. Protein binding in BDL (8.67±4.85%) decreased about four-folds, but in DMNA (73.00±9.85%) similar result, was observed as compared with the control. Increased free fraction of theophylline did not increase the volume of distribution in BDL. Therefore decreased total body clearance of theophylline was mainly due to decreased intrinsic clearance of theophylline in the liver. The absolute bioavailability of theophylline in these experiments was between 63.8 and 72.8%(66.1% in BDL, 63.8% in Sham operated and Control, 72.8% in DMNA). These results suggest that in the experimental hepatic cirrhosis model, administration route does not affect the disposition of theophylline.     

Crystal Structure of 2-Debenzoyl, 2-Acetoxy Paclitaxel (Taxol®): Conformation of the Paclitaxel Side-Chain

Crystals of the C2-acetate analog of paclitaxel, grown from a mixture of isopropyl alcohol and methanol, belong to the space group P2_l with a = 9.058(3), b = 18.306(5), c = 15.043(1) , = 97.09(1)°, Z = 2, V = 2475.1(9)³, D _calc = 1.269 gcm^–3 and µ = 0.75 cm^–1. The structure was determined by direct methods and refined to R(F) = 0.054 and wR(F) = 0.057 for 605 variables and 3496 observed reflections. The paclitaxel side chain possesses a conformation similar to that observed in the crystal structure of docetaxel (Taxotere^®). A three dimensional network of hydrogen bonds is formed through solvent molecules and stabilizes the crystal lattice.     

Effect of probenecid on the formation and elimination kinetics of the sulphate and glucuronide conjugates of diflunisal

The effect of probenecid on the pharmacokinetics of diflunisal and its glucuronide and sulphate conjugates was studied in 8 healthy volunteers. Diflunisal 250 mg b. d. was administered p. o. for 15 days and its steady state pharmacokinetics was evaluated on Day 16 after the last dose (control phase). Probenecid 500 mg b. d. was co-administered throughout the entire study period in the treatment phase of the study.The steady state plasma concentration of diflunisal was significantly higher during the probenecid treatment phase as compared to the control phase (104.0 vs. 63.1 g·ml^–1). This was the result of a significant decrease in the plasma clearance of diflunisal from 5.8 (control) to 3.4 ml·min^–1 (probenecid co-administration). The metabolite formation clearances of both glucuronides were significantly decreased by probenecid, -45 % and -54 % for the phenolic and acyl glucuronide, respectively. The metabolite formation clearance of the sulphate conjugate was not affected by probenecid co-administration.Steady state plasma concentrations of the sulphate and glucuronide conjugates of diflunisal were 2.5- to 3.1-fold higher during probenecid co-administration, due to a significant reduction in the renal clearance of the three diflunisal conjugates. Probenecid also reduced the plasma protein binding of diflunisal, but only to a minor extent; the unbound plasma fraction of diflunisal at steady state averaged between 5 and 30 % higher during probenecid co-administration.     

闭角型青光眼凝血指标的变化

目的:探讨闭角型青光眼患者凝血指标变化与临床的关系。方法:对50例闭角型青光眼患者及43例正常对照组进行了凝血指标(PT、TT、Fbg、APTT)检测。结果:闭角型青光眼患者与对照组比较PT、TT无显著变化(P<0.05),Fbg含量升高有极显著性差异(P<0.01),APTT时间缩短有极显著性差异(P<0.01)。结论:闭角型青年眼患者体内血液是高凝状态,而这种高凝状态在闭角青光眼病的发生、发展中起着重要的作用。