塔斯品碱在Caco－2细胞模型中的吸收机制研究

目的研究塔斯品碱在Caco-2细胞模型中的吸收机制。方法用Caco-2细胞单层模型研究塔斯品碱的双向转运,考察时间、药物质量浓度对塔斯品碱吸收的影响。采用高效液相色谱法检测塔斯品碱的质量浓度,计算其表观渗透系数（Papp）。结果塔斯品碱在Caco-2细胞模型中,从单层细胞层顶端到基底端的转运与基底端到顶端的转运大致相同。结论塔斯品碱在Caco-2细胞模型中的吸收主要是被动转运。     

不同辅料对芒果苷在Caco-2细胞模型吸收转运的影响

[目的]研究不同的制剂辅料对芒果苷口服吸收的影响。[方法]采用人源结肠腺癌细胞系Caco-2细胞模型,考察制剂辅料(羟丙基-β-环糊精,聚乙二醇4000,聚乙二醇6000)对芒果苷在Caco-2细胞模型中吸收转运的影响。[结果]随着辅料浓度的增加,羟丙基-β-环糊精和聚乙二醇4000能改变芒果苷在Caco-2细胞模型中的渗透方向率PDR;而聚乙二醇6000则使芒果苷的渗透方向率PDR增大。[结论]羟丙基-β-环糊精和聚乙二醇4000能促进芒果苷的口服吸收;而聚乙二醇6000则无此作用。     

Caco-2 细胞单层模型中熊果酸摄取转运机制的研究

目的 研究熊果酸在 Caco-2 细胞单层模型中的吸收转运机制。方法 利用人源结肠腺癌细胞系 Caco-2 细胞单层模型研究熊果酸在有或无 P-糖蛋白专属性抑制维拉帕米存在时,评价其双向转运特征,并考察时间、药物浓度、体系温度以及培养介质 pH 值对 Caco-2 细胞摄取熊果酸的影响。采用高效液相色谱-紫外检测法对熊果酸进行定量分析,计算其表现渗透系数 (Papp)。结果 浓度在 10～40 μmol/L 内,Caco-2 细胞对熊果酸摄取量呈线性增加。双向转运研究发现加入 P糖蛋白专属性抑制剂维拉帕米后,其 Papp 发生显著改变,表观渗透率由 3.445 下降至 1.386。结论 熊果酸在 Caco2 细胞模型的吸收转运机制以被动转运为主,P-糖蛋白参与主动转运的过程。     

高效液相色谱-质谱联用法研究芍药苷的大鼠小肠吸收

目的 研究芍药苷的大鼠小肠吸收,探讨芍药苷的吸收机制及其影响因素.方法 使用高效液相色谱-质谱联用技术,采用肠外翻模型,测定不同质量浓度芍药苷溶液在大鼠空肠和回肠的吸收,同时观察加入聚山梨醇酯-80和P-糖蛋白抑制剂维拉帕米对芍药苷吸收的影响.结果 在20～120 mg·L-1内,芍药苷吸收未饱和,呈线性吸收,在低质量浓度下空肠与回肠吸收速率无明显差异,中、高质量浓度时回肠吸收速率要高于空肠,2 g·L-1的聚山梨醇-80对空肠吸收有促进作用,维拉帕米对芍药苷吸收有显著促进作用.结论 芍药苷在小肠外翻模型中吸收遵循一级动力学,芍药苷在不同肠段的吸收有差异,芍药苷是p-糖蛋白的底物,聚山梨醇-80有利于提高芍药苷的吸收.     

维生素E聚乙二醇1000琥珀酸酯对Caco-2细胞模型转运宝藿苷I的影响

目的 考察非离子表面活性剂维生素E聚乙二醇1000琥珀酸酯（TPGS）对宝藿苷I在Caco-2细胞模型转运的影响。方法 采用Caco-2细胞模型研究不同浓度的TPGS对宝藿苷I细胞转运行为的影响,以超高压液相色谱（UPLC）法测定细胞样品溶液中宝藿苷I的浓度,计算表观渗透系数（P_app）。结果 在应用TPGS后,宝藿苷I从细胞绒毛面供给侧（AP）→基底面外侧（BL）的跨膜转运量明显增高（P＜0.05）,外排比率显著下降（P＜0.05）。当宝藿苷I与TPGS比例分别为1∶1、1∶3、1∶9时,宝藿苷I的外排比率分别为1.978 8、1.779 8、1.609 0,与仅用宝藿苷I相比分别下降了73%、76%、78%。结论 在Caco-2细胞模型上,TPGS可显著促进宝藿苷I的吸收。     

羌活中二氢呋喃类香豆素在人源肠 Caco-2 细胞单层模型的吸收转运研究

目的 研究紫花前胡苷元 (NANI)、紫花前胡苷 (ND)、前胡苷 V (DEV) 和羌活苷 (FDE) 4个线型二氢呋喃香豆素类化合物在人源肠 Caco-2 细胞单层模型中的吸收特性。方法 利用人源结肠腺癌细胞系 Caco-2 细胞单层模型测试4个香豆素类化合物从绒毛面 (AP 端) 到基底面 (BL 端)、BL 端 到 AP 端2个方向的转运过程。应用偶联紫外检测器的高效液相色谱法对上述4个香豆素进行定量分析,计算转运参数和表观渗透系数(P_app),并与阳性对照药普萘洛尔和阿替洛尔进行比较。结果 NANI 双向转运的 P_app 值在 1×10^-6 cm/s 数量级,介于在 Caco-2 细胞单层模型上呈良好吸收的普萘洛尔和难吸收的阿替洛尔的 P_app 值之间。ND、DEV 和 FDE 的P_app 值与阿替洛尔的P_app 值皆在 1×10^- cm/s 数量级。4个香豆素在 25～400 μmol/L 的转运效率与浓度呈正相关。结论 4个线型二氢呋喃类香豆素可以通过小肠上皮细胞被动吸收进入体内,NANI 属于中等吸收的化合物;ND、DEV 和 FDE 属于难吸收的化合物。     

中药化学成分肠吸收研究中Caco-2细胞模型和标准操作规程的建立

目的:建立人结肠腺癌细胞系(human colon adenocarcinoma cell line,Caco-2)细胞模型和标准操作规程,用于研究和评价中药化学成分的肠吸收。方法:通过电镜扫描和倒置显微镜观察Caco-2细胞单层细胞形态学特点,并通过测定跨Caco-2细胞单层细胞膜电阻、碱性磷酸酶活性以及易吸收阳性对照药普萘洛尔和难吸收阳性对照药阿替洛尔的转运特性等指标对Caco-2细胞模型进行评价。结果:建立的Caco-2细胞模型完整性、紧密性和通透性等良好,各项指标的测定值与文献值一致。结论:建立的Caco-2细胞单昙模型符合各项指标的要求,可用于研究口服中药化学成分的肠吸收及其转运的吸收机制。     

钩藤碱在Caco-2细胞模型中吸收规律研究

目的 建立体外模拟体内肠道细胞——人结肠癌上皮细胞（the human colon adenocarcinoma cell line,Caco-2）的Transwell模型,以此研究钩藤碱在Caco-2细胞模型上的跨膜转运特征。方法 采用聚酯碳酸酯膜连续培养Caco-2细胞21 d,形成致密的单层细胞模型。然后对影响钩藤碱在Caco-2细胞模型上转运特征的因素(包括浓度、时间及跨膜转运蛋白P-糖蛋白)进行考察;同时采用液相色谱-质谱法对溶液中钩藤碱的含量进行测定。结果 钩藤碱在Millicell系统上的转运量具有一定的浓度-时间依赖性,主要以主动转运的方式进行吸收,且随着时间和药物浓度的增加,转运量明显增加。不同浓度钩藤碱从细胞基底侧（basolateral, BL）到细胞刷状缘侧（apical,AP）的表观渗透系数（apparent permeability coefficient, Papp）与AP侧到BL侧的Papp比值均在1.5以上,且钩藤碱从BL侧到AP侧的外排速率明显高于从AP侧到BL侧的吸收速率。当加入P-糖蛋白抑制剂后,药物由BL侧向AP侧的转运量显著减少,而由AP侧到BL侧的转运量显著增加。结论 钩藤碱在Caco-2细胞上转运存在一定的浓度及时间依赖性,且P-糖蛋白介导钩藤碱在Caco-2细胞上转运。     

茯苓酸在人源肠Caco-2细胞单层模型的吸收和转运

目的：研究中药茯苓中茯苓酸（pachymic acid，PA）在人肠的吸收和转运。 方法：人源肠Caco－2细胞单层作为药物的肠吸收转运模型，测定PA从绒毛面（AP）到基底面（BL）的渗透性；反相高效液相色谱法测定PA在AP和BL的浓度，紫外检测波长为210nm；计算转运参数和表观渗透系数（Papp），并与在Caco-2细胞单层模型呈良好吸收转运的阳性对照药普萘洛尔和不良吸收转运的阳性对照药阿替洛尔进行比较。 结果：PA由AP到BL方向的Papp值为（9．50±2．20）×10^-7cm／s，由BL到AP方向的Papp值为（11．30±5．90）×10^-7cm／s。在本项研究条件下，普萘洛尔和阿替洛尔的Papp值分别为1．45×10^-5cm／s和4．22×10^-7cm／s。 结论：PA在Caco-2细胞单层馍型的吸收转运呈浓度依赖性，与转运时间呈线性关系；由AP到BL和BL到AP两个方向的转运不良，其Papp值与阿替洛尔的接近；除被动扩散机制外，ATP部分地参与了PA的转运。     

穿心莲内酯在Caco-2细胞单层模型中的吸收机制

目的 研究穿心莲内酯在Caco-2细胞单层模型中的吸收机制。方法 观察穿心莲内酯在Caco-2细胞模型中的双向转运,考察时间、药物浓度、温度和抑制剂对穿心莲内酯吸收的影响。用LC/MS/MS检测药物浓度,计算其表观渗透系数（P_app）。结果 穿心莲内酯在Caco-2细胞模型中,随时间和浓度的增加,药物吸收呈饱和趋势,且受温度和碘乙酰胺影响,但不受外排抑制剂维拉帕米和MK-571的影响。结论 穿心莲内酯在Caco-2细胞中的吸收主要是由载体介导的主动转运。     

Value of D-Dimers in patients with acute aortic dissection

Objective: To evaluatel the value of D-dimers in patients with acute aortic dissection (AAD). Methods: This study consisted of 16 patients with AAD and 27 non-AAD patients. Serum D-dimets were measured by Sta-Liatest D-DI immunoturbidimetric assay. Results: D-dimer level was higher (P ＜ 0.001) in patients with AAD(7.91 ± 5.52 μg/ml) than that in non- AAD group(1.57±1.24 μg/ml). D-dimer was positive (＞0.4 μg/ml) in all patients with AAD and in 10 control group patients (37%). Among patients with acute AAD, D-dimers tended to be higher in Stanford A than in Stanford B (8.67 ± 4.31 μg/ml vs. 3.24±1.27 μg/ml, P ＜0.01). D-dimer values tended to be higher in more extended disease(3.84 ± 1.65 μg/ml, 8.57 ± 3.58 μg/ml and 11.87 ± 5.69 μg/ml in thoracic aorta, thoracic and abdominal aorta, thoracic and abdominal aorta and iliacal arteries, respectively, P ＜ 0.05 for both 8.57 ± 3.58 and 11.87 ± 5.69 vs. 3.84 ± 1.65 ). Including the control group into the analysis, we found a sensitivity of 100%, a negative predictive value of 100%, and a specificity of 66% and a positive predictive value of 64% for D-dimer in diagnosis of AAD in our patients with suspected AAD. Conclusion: D-dimer was elevated in patients with AAD. A negative D-dimer test result could be useful in excluding AAD.     

Research of combined liver-kidney transplantation model in rats

Objective： To set up a simple and reliable rat model of combined liver-kidney transplantation. Methods： SD rats served as both donors and recipients. 4℃ sodium lactate Ringer＇s was infused from portal veins to donated livers,and from abdominal aorta to donated kidneys, respectively. Anastomosis of the portal vein and the inferior vena cava （IVC） inferior to the right kidney between the graft and the recipient was performed by a double cuff method, then the superior hepatic vena cava with suture. A patch of donated renal artery was anastomosed to the recipient abdominal aorta. The urethra and bile duct were reconstructed with a simple inside bracket. Results： Among 65 cases of combined liver-kidney transplantation, the success rate in the late 40 cases was 77.5%. The function of the grafted liver and kidney remained normal. Conclusion： This rat model of combined liver-kidney transplantation can be established in common laboratory conditions with high success rate and meet the needs of renal transplantation experiment.     

APPLICATION OF LORNOXICAM TO PATIENT-CONTROLLED ANALGESIA IN PATIENTS UNDERGOING ABDOMINAL SURGERIES

FOR anesthesiologis s ,treatingpostoperativepainhas alwaysbeen a problem.Althoughopioidshave been provedtobe effective,theirsideeffectscouldnotbeignored.With thedevelopmentofscienceand pharmacology,many drugs with aspectsof satisfactoryanalgesicefficacyand couldbe welltoleratedby patientshave been developed.And lornoxicamisone of them, which isa non-steroidalanti-inflammatorydrug (NSAID ), with analgesic, anti-infl-ammatory,andantipyreticproperties.Itseliminationhalf-time(3 to 5 hours) isle…     

Acupuncture Combined with Spinal Tui Na for Treatment of Primary Dysmenorrhea in 30 Cases

Objective: To observe the therapeutic effects in acupunture treatment of primary dysmenorrhea combined with spinal Tui Na, and study its mechanism. Methods: Thirty cases of the treatment group were treated by acupuncture combined with spinal Tui Na, and thirty cases in the control group were treated by routine acupuncture. Results: The total effective rate was 93.3% in the treatment group, and 73.3% in the control group, with a significant difference between the two groups (P<0.05). Conclusions: Acupuncture combined with spinal Tui Na has good prospects for treatment of primary dysmenorrhea.     

Luo Lingjie's Experience in Treating Chronic Nephropathy

In treating chronic nephropathy,Luo Lingjie,a chief physician,pays attention to regulating the balance between yin and yang,treating infection if present,and removing pathogenic factors.He prescribes gentle drugs and uses carefully strongly warming-tonifying ones,emphasizes the importance of persuading the patient to persist in treatment with medication and nurse one's health for recuperation,and is good at combined use of TCM and western medicine therapy and brings the merits of various therapies into full play,with obvious theraoeutic effects.     

Dr.Zhang Ren's Experience in the Acupuncture Treatment of Different Diseases with the Same Therapeutic Principle

Dr.Zhang Ren,the chief physician,is the chairman of Shanghai Acupuncture and Moxibustion Association.Having been engaged in medicine for about 40 years,he is experienced in treating various intractable diseases.In his long years of clinical practice,he advocates taking the TCM differentiation as the basis to seek for the acupuncture method for treatment of modern intractable diseases.The author of this essay had the fortune to follow Dr.Zhang in study.The following is a summary of Dr.Zhang's experience in the acupuncture treatment for different intractable diseases with the same therapeutic principle.     

安心颗粒对急诊经皮冠状动脉介入术后生活质量影响的研究

目的：评价使用安心颗粒对急诊经皮冠状动脉介入术（PPCI）术后生活质量的影响.方法：将160例接受PPCI的急性ST段抬高型心肌梗死患者随机分为安心颗粒组（术前顿服安心颗粒8.8g,术后安心颗粒4.4 g/次,每日2次）和对照组（仅接受基础药物治疗）.所有患者均服用阿司匹林、氯吡格雷和阿托伐他汀.分别在入院时、出院前1d、出院后180 d时,应用心肌梗死多维度量表（MIDAS）、中文版SF-36评价量表对患者生活质量评分.并观察术后30 d以内的出血并发症、血小板减少症发生情况.结果：入院时和出院前1d,两组患者的心肌梗死MIDAS、SF-36量表评分比较无差异（P＞0.05）;出院后180 d时,与对照组比较,安心颗粒组MIDAS、SF-36评分明显减低（P＜0.05）;组内与入院时比较,两组出院前1d、出院后180 d时,MIDAS、SF-36评分均降低（P＜0.05）.两组患者在随访期间均无大量出血、少量出血、重度和极重度血小板减少症发生,安心颗粒组有4例、对照组有7例发生不明显出血（P＞0.05）.两组发生轻度血小板减少症的患者数比较无差异（P＞0.05）.结论：PPCI使用安心颗粒,能改善急性ST段抬高型心肌梗死患者的生活质量,且不增加出血风险.     

The comparative studies of the influences of Urapidil and Nicardipine on sino-atrial node function, atrio-ventricular node function and hemodynamics

Objective:To investigate the influences of urapidil and nicardipine on rabbit sinus function,atrio-ventricular node function and hemodynamics.Methods:Thirty-two Angora's rabbits were selected and randomly divided into four groups.U1 group:urapidil 0.25 mg/kg;U2 group:urapidil 0.5 mg/kg;N1 group:nicardipine 10 μg/kg;N2 group:nicardipine 20 μg/kg.All these medicine were administrated within 30 seconds.Measurements were taken before and after the administration of urapidil or nicardipine for the following data:mean blood pressure(MAP),heart rate(HR),sino-atrial conduction time(SACT),maximal sinoatrial recovery time(SNRTmax)corrected sinus node recovery time(CSNRT),index of sinus node recovery time(SNRTI),Wenckebach A-V conduction frequency (WB),and P-R interval.Results:Significant MAP and HR changes were identified in all of the four groups before and after administration of both urapidil and nicardipine.No significant changes could be found in the rest of the parameters.Intergroup analysis showed that SACT and CSNRT of N1 and N2 groups were shorter than those of the U2 group(P＜0.01);the MAP decreased(P＜0.01)and the HR increased drastically(P＜0.01).Conclusions:Neither urapidil(0.25 mg/kg,0.5 mg/kg)nor nicardipine(10μg/kg,20μg/kg)has any significant influence on rabbit sinus function or rabbit atrio-ventricular node function.Nicardipine could be a better choice than urapidil for parafunctional sinus node patients.     

猪肺磷脂注射液联合经鼻持续气道正压通气对呼吸衰竭早产儿的临床疗效及肌酸激酶同工酶活性的影响

目的 探讨猪肺磷脂注射液联合经鼻持续气道正压通气(NCPAP)对呼吸衰竭早产儿的临床疗效及肌酸激酶同工酶活性(CK-MB)的影响.方法 选取呼吸衰竭早产儿80例,分为观察组和对照组各40例.对照组采用NCPAP给氧治疗,观察组给予NCPAP给氧联合猪肺磷脂气管内给药.观察两组患儿治疗前及治疗12h、24 h后PaO2、PaCO2、血氧饱和度(SaO2)、pH的变化情况,检测治疗前及治疗5d后血清CK-MB水平;评估两组患儿的临床治疗效果.结果 两组患儿PaO2、PaCO2、SaO2、pH比较,差异均有统计学意义(P＜0.05),其中观察组治疗后的PaO2、SaO2、pH均高于对照组,PaCO2则低于对照组.两组的PaO2、SaO2、pH均随观察时间延长而升高(P＜0.05),PaCO2均随观察时间的延长而降低(P＜0.05).观察组治疗有效率为87.5％,显著高于对照组的70.0％ (P ＜0.05).治疗5d后两组患儿血清CK-MB水平均较前降低(P＜0.05),且观察组明显低于对照组(P＜0.05).结论 猪肺磷脂注射液气管内给药联合NCPAP可以显著降低呼吸衰竭早产儿CK-MB的含量,提高治疗有效率,起到很好的呼吸循环支持作用.