阿苯达唑脂质体及主要代谢产物的HPLC法和药代动力学研究(摘要)

阿苯达唑(Albendazole,ABZ)是一种广谱抗寄生虫药,它在宿主体内极易被代谢为阿苯达唑亚砜(Albendazole suLfoxide,SX)和阿苯达唑砜(Albenda-zole sulphone,SN),且前者经过体内试验证明有抗细粒棘球蚴病的作用.为了使药物具有定向性和在靶区(肝脏包虫组织)具有滞留性以及达到缓释的目的,我们将ABZ制成脂质体,建立了动物(鼠)口服ABZ脂质体后测定血浆、肝脏、包虫囊液及囊组织中的ABZ及主要代谢产物SX和SN的反相HPLC法。同时进行了药代动力学研究以及并用西咪替丁后对血、肝药物浓度的影响。采用Neceleosil C_(13)柱,以甲醇:乙腈:水(5:37:58)为流动相,292 nm为检测波长,甲苯达唑为内标,样品提取溶剂为醋酸乙酯。结     

阿苯达唑脂质体的包封率测定及形态观察(摘要)

阿苯达唑(Albendazole,ABZ)是一种广谱抗寄生虫药,尤其对抗肝包虫是较有效的药物.为了提高其生物利用度,延缓它在体内的代谢,进一步改善疗效,我们将ABZ制成药物新剂型——脂质体.经动物药代动力学实验证明,该脂质体增加了药物的溶解性和稳定性,达到了缓释和靶向给药的目的。本实验对阿苯达唑脂质体采用葡聚糖凝胶Sephadex G-50     

史克肠虫清——中小学生集体驱虫的理想驱虫药

史克肠虫清是一种广谱抗蠕虫新药,由美国史克公司于1975年研制合成,目前已在非洲、拉丁美洲、中东及亚洲等70多个国家应用于各种蠕虫病,均取得了良好的疗效。本药难溶于水,故只有5％在肠道内吸收,而被吸收的95％主要在肠道内直接发挥杀虫作用,吸收的部分经肝脏迅速代谢为阿苯哒唑——砜和阿苯哒唑——亚砜,其中阿苯哒唑亚砜是本品的活性代谢产物,对组织内寄生虫有良好的杀灭作用;400毫克肠虫清服后2.5～3小时达血浓峰值,血浆半衰期为8.5～10.5小时,未吸收部分24小时内由粪便排出,而吸收部分48小时内主要通过肾脏排出,体内无积蓄作用。     

Logistic回归方程对阿苯达唑两种剂型药物治疗囊性包虫病的临床疗效评价

目的应用Logistic回归的方法评价阿苯达唑两种剂型药物治疗囊性包虫病的临床疗效。方法回顾性分析我院自1998~2008年十年收治的阿苯达唑脂质体和阿苯达唑片治疗的共269例囊性包虫病患者的临床随访资料,通过一定的纳入及排除标准,入组病例218例。依据随访记录的可能对临床疗效产生影响的各项指标,应用SPSS13.0及PEMS3.1医学统计软件包对各项指标进行分析并建立Logistic回归方程深入分析。结果影像学疗效结果评价显示阿苯达唑脂质体组与阿苯达唑片剂组比较,3个月总有效率差异有显著统计学意义(χ2=19.581,P=0.00001),将两个治疗组作为疗效的影响因素引入Logistic回归方程分析结果也显示,两个治疗组比较总有效率差异有统计学意义(χ2=20.806,P<0.001,OR<1,95%CI:0.119~0.428)。结论阿苯达唑脂质体及阿苯达唑片剂均是有效的抗包虫药物,Logistic回归方程的结果结合影像学疗效评价显示阿苯达唑脂质体疗效优于阿苯达唑片剂。     

阿苯达唑脂质体口服液的临床疗效及药物副作用

目的探讨阿苯达唑脂质体口服液的临床疗效及药物副作用。方法收集我院100例包虫病患者,随机分为观察组和对照组,均为50例。对照组实施阿苯达唑片治疗,观察组实施阿苯达唑脂质体口服液的治疗,观察临床疗效和药物副作用。结果观察组患者的治疗显效率和总有效率均明显高于对照组,并发症发生率明显低于对照组。结论阿苯达唑脂质体口服液能够明显提升临床治疗效果,同时药物副作用明显低于常规阿苯达唑片,值得推广应用。     

高效液相色谱法测定阿苯达唑前体胶束药物含量

目的:建立阿苯达唑前体胶束药物含量测定的高效液相色谱法。方法:色谱条件:Symmetry ShieldTM RP18色谱柱(3.9 mm×150 mm,5μm),流动相为甲醇∶乙腈∶三乙胺-磷酸缓冲液(24∶20∶56);检测波长295nm,流速1.0 ml/min,柱温30℃,进样量20μl。结果:阿苯达唑与辅料及溶剂峰均得到良好分离。阿苯达唑在4~20μg/ml浓度范围内线性良好(r=0.999 8,n=5),平均回收率97.16%,日内及日间平均RSD分别为1.06%、2.19%(n=5)。结论:高效液相色谱法灵敏、准确,可靠性好,可用于阿苯达唑前体胶束药物含量的测定。     

阿苯达唑脂质体对泡状棘球蚴作用的病理形态学观察

目的：试图通过阿苯达唑脂质体口服新剂型与阿苯达唑片剂的动物对比实验,对口服和腹腔注射抗泡状棘球蚴作用做出客观评价。方法：采用泡状棘球蚴继发感染小鼠动物模型（２２５只）,经灌胃和腹腔注射（每公斤体重３７．５、７５．０和１５０．０ｍｇ）１０周,观察其病理组织学变化。将用药后病理形态变化分为正常、变性和坏死３级,以便用药组与对照组进行等级资料的统计学比较。结果：阿苯达唑及代谢产物有较强的破坏棘球蚴囊壁结构和抑制原头蚴增殖作用。结论：阿苯达唑脂质体经口灌注或腹腔注射抗泡状棘球蚴作用均优于口服阿苯达唑片剂。     

阿苯达唑脂质体治疗小鼠继发性肝,腹腔泡状棘球蚴病的？…

目的：通过使用新的载体药物阿苯达唑脂质体（Ｌｉｐｏｓｏｍａｌ ａｌｂｅｎｄａｚｏｌｅ,Ｌ－ＡＢＺ）经口服和腹腔注射治疗感染泡状棘球蚴（Ｅｃｈｉｎｏｃｏｃｃｕｓ ｍｕｌｔｉｌｏｃｕｌａｉｓ,Ｅ．ｍ）的小鼠,并与口服阿苯达唑片剂粉末对照,观察阿苯达唑脂质体对动物体内的泡状棘球蚴的治疗作用。感染泡状棘球蚴的小鼠经一定时间阿苯达唑脂质体治疗后,将其泡状棘球蚴组织再种植于健康小鼠体内,观察Ｅ．ｍ的生长情况,     

消炎痛在外科临床中的应用

一、消炎痛的药理及作用机制消炎痛又名吲哚美辛(Indomethacin)。有注射液、片剂、栓剂、贴膏剂、胶囊、缓释胶囊等剂型。口服给药1小时血药浓度达高峰,直肠给药半小时达高峰,有效血浆浓度为0.5～3.0μg/ml。主要在肝脏代谢,口服后血浆药物清除率为1～2.5ml/min/kg,1/2—3小时。栓剂血药浓度为片剂的1.5倍,高峰浓度持续4小时后下降。     

区域性灌注化疗时5-FU的血液和肝脏组织药物浓度分布特征

目的 研究经肝动脉和门静脉等不同途径区域灌注化疗时5-FU在大鼠血液和肝脏组织中的浓度分布和消除过程,为临床肝脏肿瘤化疗提供参考.方法 经颈静脉注射5-FU或分别经肝动脉及门静脉插管区域灌注,剂量为20 mg/kg体重.采用高效液相色谱法测定血浆及肝脏组织中5-FU的含量.进一步计算5-FU在肝脏和血浆中的药动学数据和穿透比率及治疗优势度.结果 外周静脉注射时,肝脏组织的药物峰浓度(Cmax)和药物时量曲线下面积(AUC)分别为13.79±4.56μg/g,342.20±108.20μg·min/g;血浆Cmax和AUC分别为36.85±5.96μg/ml,842.00?58.00μg·min/ml.肝动脉灌注5-FU时,肝脏组织药物Cmax和AUC分别为29.58±4.30μg/g,794.60±15.40 μg·min/g;血浆Cmax和AUC分别为24.39±4.63μg/ml,639.70?33.80μg·min/ml.门静脉灌注时,肝脏组织药物Cmax和AUC分别为2821±4.06μg/g,733.60±18.3μg·min/g;血浆Cmax和AUC分别为21.02±406μg/ml,529.80±111.50μg·min/ml.结论 与外周静脉注射全身化疗比较,区域性肝动脉或门静脉灌注化疗可显著提高肝脏组织中的药物浓度,同时减少化疗药物在外周血中的分布,可作为临床肝癌化疗的较好治疗措施.     

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…     

BLOOD PRESSURE CHANGE WITH AGE IN SALT-SENSITIVE TEENAGERS

Objective To observe blood pressure change with age in salt-sensitive teenagers whose salt sensitivity were determined by repeated testing.Methods Salt sensitivity was determined through intravenous infusion of normal saline combined with volume-depletion by oral diuretic furosemide in 55 teenagers. After five years, salt sensitivity was re-examined and subject blood pressure was followed up. Blood pressure changes in salt-sensitive teenagers were compared to that of non-salt sensitive teenagers over five years.Results After 5 years, the repetition rate of salt sensitivity determined by intravenous saline loading is 92.7%. In teenagers with salt sensitivity on the baseline, both the systolic blood pressure increments and increment rates were much higher than non-salt sensitive teenagers (12.7±12.1 mmHg vs. 2.8±5.2 mmHg, P＜ 0.01; 12.2%± 12.0% vs. 2.5% ±4.4%, P＜ 0.001,respectively). There was a similar trend for diastolic blood pressure (8.4 ± 6.4 mmHg vs. 3.7 ± 6.4 mmHg, P = 0.052; 13.2% ±10.6 % vs. 6.8%± 10.1%, P = 0.053, respectively).Conclusions Salt sensitivity determined by intravenous saline loading showed good reproducibility. Blood pressure increments with age were much higher in salt-sensitive teenagers than non-salt sensitive teenagers, especially in terms of systolic blood pressure.     

Development on Adjustable Calibration Marker for Shock Wave Focus

Shock wave lithotripsy （SWL） is a treatment of choice for upper urinary stones. However, this procedure is inappropriate for obese patients because the focus is often unable to reach the target owing to the limited focal distance in shock wave source. Although treating such patients in a blast path may increase the application length of shock wave source, it＇s difficult to find this path on the lithotripter monitor. For this reason, we invented an adjustable calibration marker in order to set an effective focus in the shock wave hath.     

Study on the TCM Pathogenesis of Angiopathic Complications of Type II Diabetes

Excess production of reactive oxygen species(ROS)of mitochondrion mediated by hyperglycemia is the common pathogenesis of angiopathic complications of diabetes.TCM holds that the damp from the dysfunction of spleen.kidney and liver is the causative factor of complications of diabetes.This is similar to the mechanism of Ros resulting in angiopathic complications of diabetes.When the angiopathic complications of type II diabetes mellitus(T2DM)are difierentiated as caused by turbid damp in TCM can be explained as ROS.Since the obstruction of pathogenic damp in channels and collaterals is said to be the main pathogenesis,the treating principle should be dissolving the damp to remove the obstruction.     

Leptin, Ghrelin and TNF-α before and after Hypo-caloric Traditional Chinese Diet and Auricular Acupuncture

INTRODUCTION Obesity is a complex emergent problem, which can be possibly solved not only by the diet but also by the life style and promotion of a constant physical exercise. 1, 2 No doubt careful attentions must be given to the nutritional condition of obese people, the dietary habits, the somatic build (i.e. distribution of fat mass) and the organic functions linked to formation of the fat mass. All the parameters should be constantly monitored before, during and after a diet treatment. 3, 4, 5     

Relationship between Dysglycemia and Carotid Atherosclerosis in Tibetan Population

People with dysglycemia are at high risk for atherosclerotic diseases. This study aims at investigating the atherosclerotic vascular damage in dysglycemia and its metabolic origin in Tibetan population.     

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.