利多卡因和输液部位对丙泊酚注射痛的影响

目的 观察利多卡因和不同输液部位对丙泊酚注射痛的影响.方法 120例妇产科日间手术患者随机分为二组,每组60例,每组内再根据患者的输液部位分成手背静脉和桡静脉两组.1组推注2ml乳酸林格液后和2组推注40mg利多卡因后缓慢推注丙泊酚.观察推注丙泊酚时患者的疼痛情况.结果 1组的桡静脉的注射痛优于手背静脉(P<0.05),2组的桡静脉和手背静脉的注射痛没有明显区别(P>0.05);2组注射痛的发生率45%,1组注射痛的发生率是78%(P<0.05),药物对注射痛的影响因子大于输液部位对静脉痛的影响因子.结论 利多卡因可以缓解丙泊酚的注射痛,在不复合利多卡因的情况下,选择桡静脉要优于选择手背静脉.     

高龄糖尿病患者的健康知识需求状况调查

目的了解糖尿病患者的健康知识需求状况,采取合理的护理对策。方法自行设计问卷,对糖尿病患者进行访谈问卷调查。结果大学及以上文化程度者学习积极性高,患者对治疗效果的需求为100%,反映出求生欲望强烈。而对自我护理技能和自我护理知识的需求仅为71.2%,说明患者自我保健意识不强,不同住院次数患者健康知识掌握有统计学意义（P〈0.05）,首次住院及住院次数少的患者存在严重的健康知识缺乏。结论护士了解了糖尿病患者健康知识需求状况,开展有针对性的健康教育,可提高患者的健康知识水平和自我保健能力。     

妇科腔镜手术麻醉期间二氧化碳气腹气体栓塞8例临床分析

目的:分析二氧化碳(CO2)气腹妇科腔镜手术发生气体栓塞的临床特点、可能原因和救治.方法:回顾性总结8例CO2气腹下妇科腔镜手术麻醉期间气体栓塞,并与胆囊腔镜手术比较,分析其可能原因、临床特点、诊治经过和预后.结果:本组8例气栓病例发生率为0.148%.6例CO2气栓的发生与气腹开始阶段的高流量和麻醉管理有关;除一例心脏骤停后植物生存状态外,其余病例特征为:(1)主要表现为肺栓塞,且术毕才出现低氧血症或当自主呼吸恢复时SpO2多进行性下降,典型的呼吸因难和发绀;而术中未出现明显异常,尤其是监测PFTCO2变化不明显;(2)肺部听珍早期一侧肺局限性明显湿性啰音,后期非对称性啰音;(3)X线明显片状阴影:右下肺叶和中下肺叶大部片状影(5例)、左下肺叶(3例);(4)右下肺叶和中下肺叶大部片状影(5例):均CVP>12cmH2O;心电图出现有意义的心电图改变:S ⅠQⅢTⅢ,电轴右偏;(5)诊断性治疗明显有效.结论:CO2气栓的发生可能与气腹建立、麻醉及妇科手术体位和手术部位有关;早期及时诊断和治疗能有效改善预后.     

大鼠灌胃四逆散提取物后血浆、尿液、粪便、胆汁中主要代谢产物的鉴定

采用UPLC-Q-TOF/MS研究四逆散提取物在大鼠体内的代谢产物,利用碰撞能量梯度(MSE)和质量亏损过滤(MDF)技术进行分析,鉴定大鼠灌胃四逆散提取物后血浆、尿液、粪便、胆汁中的代谢产物。四逆散提取物中柚皮苷、柚皮素、橙皮苷、新橙皮苷、甘草苷、甘草素、甘草酸、甘草次酸、柴胡皂苷a、柴胡皂苷d在大鼠不同代谢途径中推测出原形、羟基化、葡糖醛酸化、硫酸化、葡糖醛酸化与硫酸化结合、羟化葡糖醛酸化等共41个代谢产物。     

In Vivo Bioequivalence and In Vitro Similarity Factor (f2) for Dissolution Profile Comparisons of Extended Release Formulations: How and When Do They Match?

Purpose

To investigate how likely two extended release formulations are to be bioequivalent when they demonstrate f2 similarity.

Method

Dissolution profiles were simulated using the Weibull model and varying model parameters around those of a reference profile. The f2 values were calculated for the comparisons of each simulation with the reference profile. The in vivo inputs obtained from an in vitro-in vivo correlation model were convolved with a unit impulse response function. The AUC, Cmax, and Tmax from each simulated in vivo concentration profile were compared to the reference profile. The AUCR (AUC ratio) and CmaxR (Cmax ratio) were determined. The consistency between f2 and bioequivalence was investigated.

Results

The relationships between AUCR, CmaxR, f2 and the Weibull model parameters demonstrate that the bioequivalence regions enclosed by the contour lines of 80% and 125% of AUCR and CmaxR were generally close to the regions enclosed by the f2?=?50 contour line, but did not exactly match, especially when Dmax and B deviated from the reference values.

Conclusions

When f2 is used for in vitro dissolution profile comparison, the completeness of the dissolution profiles should not differ more than 10%, and the shapes of the dissolution profiles should not be significantly different.     

Screening of immunomodulatory components in Yu-ping-feng-san using splenocyte binding and HPLC

Yu-ping-feng-san (YPFS) is a widely used immunomodulatory herbal medication used in traditional Chinese medicine, but the active molecules remain obscure. To screen for bioactive components we combined splenocyte binding with high performance liquid chromatography (SB-HPLC). After enrichment by splenocyte binding, two YPFS components (C1 and C2) were analyzed by HPLC. Compound C2 was identified as linoleic acid (LA) based on UV absorption and mass spectrometry. Silica gel chromatography was used to purify compound C1 from Radix Saposhnikoviae, a major constituent of YPFS. This allowed identification of the molecule as panaxynol (PAN) based on EI-MS and NMR spectrometry. Bioassay in vitro demonstrated that PAN significantly inhibited splenocyte proliferation induced by concanavalin A (ConA) in a concentration-dependent manner, whereas LA had no significant effect on splenocyte proliferation. In vivo, PAN was found to attenuate allergic contact dermatitis in a mouse model of delayed-type hypersensitivity (DTH), a pharmacological activity not previously reported for this molecule. It is suggested that PAN contributes to the anti-DTH effects of YPFS. SB-HPLC provides a rapid and efficient method for the identification of potential immunomodulatory components in traditional Chinese medicines.     

Silibinin activated p53 and induced autophagic death in human fibrosarcoma HT1080 cells via reactive oxygen species-p38 and c-Jun N-terminal kinase pathways

Our previous research demonstrated that hepatic-protectant silibinin induced autophagy in human fibro-sarcoma HT1080 cells through reactive oxygen species (ROS) pathway. Pifithrin-α (PFT-α), a specific inhibitor of p53, reduced autophagy and reversed silibinin's growth-inhibitory effect; besides, PFT-α decreased the activation of caspase-3, a crucial executor of apoptosis. Silibinin upregulated expression of p53/phosphorylated-p53 (p-p53) in a time-dependent manner. Catalase (scavenger of H(2)O(2)), superoxide dismutase (SOD) (scavenger of O(2)(?-)), and SB203580 (inhibitor of p38) attenuated upregulation of p53 expression, suggesting that p53 might be partially regulated by ROS-p38 pathway. On the other hand, c-Jun N-terminal kinase (JNK) increased autophagic death in silibinin-treated cells, and JNK/p-JNK expression was upregulated by silibinin time-dependently. Inhibition of JNK by SP600125 did not influence generation of ROS. Scavengers of H(2)O(2) or O(2)(?-) showed no effect on expression of JNK/p-JNK, indicating that JNK might not correlate with ROS in this process. However, activation of p53 was suppressed by SP600125; therefore the function of p53 was possibly controlled by JNK as well. Western blotting analysis showed that PFT-α reduced activation of extracellular regulated kinase1/2 (ERK1/2) and expression of protein kinase B (PKB, or Akt)/p-Akt. PD98059 (inhibitor of mitogen-activated protein kinase kinase (MEK)/ERK) and wortmannin (inhibitor of phosphoinositide 3-kinase (PI3K)/Akt) enhanced silibinin's cytotoxicity. Wortmannin augmented silibinin-induced autophagy, while PD98059 did not affect autophagic ratio. These results suggest that silibinin might induce p53-mediated autophagic cell death by activating ROS-p38 and JNK pathways, as well as inhibiting MEK/ERK and PI3K/Akt pathways.     

New hope for the treatment of osteoarthritis through selective inhibition of MMP-13

Osteoarthritis (OA) is the leading cause of joint pain and disability in middle-aged and elderly patients, and is characterized by progressive loss of articular cartilage that eventually leads to a complex process involving degradation of various components of the cartilage matrix, chief among them are the cartilage-specific type II collagen (CII) and aggrecan. While the loss of aggrecan is thought to be an early and reversible process, degradation of CII is considered to be irreversible and a key step in the loss of structural and functional integrity of cartilage. Among the various matrix metalloproteinases (MMPs), MMP-13 is specifically expressed in the cartilage of human OA patients and is not present in normal adult cartilage. It is the major collagenase in OA cartilage and has the highest activity against CII. However, the clinical utility of broad-spectrum MMP inhibitors developed for treatment of OA has been restricted by dose- and duration-dependent musculoskeletal side effects in humans. Consequently, selectively inhibiting the MMP-13 would seem to be an attractive therapeutic objective. This review mainly focuses on selective MMP-13 inhibitors development in terms of OA since the late 90s, in terms of synthetic compounds of low molecular mass incorporating specific zinc-binding groups, non-zinc-binding groups. In addition, dual inhibitors of MMP-13 and aggrecanase are also reviewed. Special emphasis is placed on logistic concerns for lead compound search as well as the structure-activity relationship (SAR) in this field. Through these methods, new hope is emerging for the treatment of OA through selective inhibition of MMP-13.     

抗凝清脂口服液的薄层色谱分析方法

目的控制抗凝清脂口服液的质量。方法用薄层色谱法鉴别制剂中党参、丹酚酸B。结果供试品溶液色谱中,在与党参对照药材溶液、丹酚酸B对照品溶液色谱相应位置上显相同颜色的斑点。结论薄层色谱法简便、准确、重现性好,可用于控制抗凝清脂口服液的质量。     

HPLC同时测定大豆磷脂中磷脂酰胆碱和溶血磷脂酰胆碱含量

目的建立同时测定大豆磷脂中磷脂酰胆碱（PC）和溶血磷脂酰胆碱（LPC）含量的方法。方法采用高效液相色谱法,色谱柱为Phenomenex silica柱（4.6 mm×150 mm,5μm）,流动相为正己烷-异丙醇-水（5∶80∶20）,流速：0.7 mL.min-1,检测波长：206 nm,柱温：25℃。结果 PC在0.4~2.4 mg.mL-1内呈良好的线性关系,平均回收率为99.4%,RSD为0.40%（n=6）;LPC在10~60μg.mL-1内呈良好的线性关系,平均回收率为98.0%,RSD为1.65%（n=6）。结论本试验方法简便、重复性好、专属性强,可作为大豆磷脂中PC,LPC的检测方法。