尼莫地平在健康人体内的药动学和相对生物利用度

目的 :研究尼莫地平在健康人体内的药动学和相对生物利用度。方法 :8名健康受试者单剂量随机交叉口服尼莫地平标准参比制剂和待测制剂 1 2 0mg,采用HPLC法测定用药后不同时间的血药浓度。结果 :2种制剂的体内过程均符合一房室开放模型 ,AUC分别为 (1 4 3.1± 9.9) μg·h·L-1 和 (1 37.0± 7.3) μg·h·L-1 ,Cmax分别为 (83.1±7.4 ) μg·L-1 和 (80 .8± 4 .6 ) μg·L-1 ,Tmax分别为 (1 .0 0± 0 .0 0 )h和 (1 .0 6± 0 .1 7)h。待测制剂的相对生物利用度为 (96 .0± 5 .9) %。经双向单侧t检验证明 ,2种制剂的AUC、Cmax相比 ,差异均无统计学意义。结论 :2种制剂具有生物等效性。     

三七总皂苷脂质体的药剂学性质及大鼠肺部给药药动学研究

目的　制备三七总皂苷 ( Panax notoginseng saponins,PNS)脂质体 ,研究其药剂学性质及在大鼠体内药动学行为。方法　采用薄膜分散法制备 PNS脂质体 ,考察其形态、粒径、包封率及稳定性 ,采用肺部滴注给药考察脂质体在大鼠体内的药动学行为。结果　 PNS脂质体包封率为 78.5 0 % ,平均粒径为 1.5 μm,外形圆整 ,体外泄漏慢 ,需低温保存。 PNS脂质体经大鼠肺部滴注给药后 ,体内人参皂苷 Rb1的药动学参数分别为 T1 /2 α=7.0 0 h,T1 /2 β=2 7.72 h,AU C=2 2 18.9μg· h/m L,绝对生物利用度为 70 .14 %。结论　 PNS脂质体包封率高 ,性质稳定 ,延长PNS在血循环的时间 ,提高了经血管外给药途径的 PNS生物利用度。     

盐酸曲马多片剂人体相对生物利用度

目的:研究盐酸曲马多片剂在人体内的相对生物利用度。方法:采用HPLC法测定 18名男性健康受试者单剂量交叉口服 100mg2种盐酸曲马多片剂后不同时间血浆中的药物浓度。结果: 2制剂药 时曲线均符合一房室模型,Cmax分别为(410. 0±71. 1)μg·L-1和 (427. 0±57. 1)μg·L-1,Tmax分别为 (2. 20±0. 49)h和 (2. 20±0. 55)h;T1 /2ke分别为(7. 13±0. 83 )h和 ( 7. 08±0. 74 )h;AUCt0 分别为 ( 4 376±855 )μg·h·L-1和 ( 4 514±1 068)μg·h·L-1,AUC∞0 分别为(5 184±1 112)μg·h·L-1和(5 241±1 330)μg·h·L-1。与参比制剂相比,被试制剂的Ft0 为(98. 94±16. 04)%,F∞0 为(1 101. 90±21. 92)%。结论: 2种制剂具有生物等效性。     

格列吡嗪片在健康人体内的药物动力学及相对生物利用度

目的 :研究格列吡嗪片在健康人体的药物动力学及相对生物利用度。方法 :9名健康受试者单剂量随机交叉口服格列吡嗪片参比制剂和被试制剂 5mg ,采用HPLC法测定用药后不同时间的血药浓度。 结果 :2种制剂的体内过程均符合一房室开放模型 ,Tmax分别为 (3 .67± 0 .50 )h和 (3 .33± 0 .50 )h。Cmax分别为 (391± 37) μg·L- 1和 (40 0± 35) μg·L- 1 ,AUC分别为 (2 .46± 0 .39) μg·h·L- 1 和 (2 .2 3± 0 .88) μg·h·L- 1 ,被试制剂的相对生物利用度为 (1 0 2 .9± 1 5 .7) %。结论 :用NDST软件对两种制剂的AUC、Cmax、Tmax进行双单侧t检验 ,证明两种制剂具有生物等效性。     

格列吡嗪片健康人体生物等效性研究

目的　研究格列吡嗪片在健康人体内的生物等效性。方法　 9名健康受试者单剂量随机交叉口服格列吡嗪片参比制剂和被试制剂 5mg,采用HPLC法测定用药后不同时间的血药浓度。结果　二制剂健康人体的体内过程均符合一房室开放模型 ,Tmax分别为 (3 0± 0 )h和 (3 0± 0 )h ,Cmax分别为 (30 5± 2 2 ) μg·L-1和 (2 99± 13) μg·L-1;T1/2 分别 (3 2 4± 0 37)h和 (3 2 2± 0 4 0 )h ;AUC分别为 (14 90± 70 ) μg·h·L-1和 (14 90± 70 ) μg·h·L-1。被试制剂的相对生物利用度为 (10 0 4± 7 8) %。结论　方差分析和单双侧t检验证明 ,两种制剂具有生物等效性     

头孢克洛在健康人体的药代动力学和相对生物利用度

目的:研究头孢克洛在健康人体的药动学及相对生物利用度。方法:18名健康受试者随机交叉单剂量口服头孢克洛片标准参比制剂和被试制剂500mg,采用微生物法测定不同时间血清中药物浓度。结果:两制剂的体内过程均符合一房室开放模型,其主要药动学参数Cmax分别为(13.94±1.55)mg·L-1和(14.10±1.45)mg·L-1,Tmax为(0.72±0.15)h和(0.75±0.12)h,T1/2ke为(0.65±0.05)h和(0.69±0.06)h,AUCt0为(15.78±2.75)mg·h·L-1和(14.86±2.98)mg·h·L-1,AUC∞0为(15.96±2.74)mg·h·L-1和(15.10±3.04)mg·h·L-1。被试制剂的相对生物利用度为(107.99±17.82)%。结论:2种制剂具有生物等效性。     

紫杉醇透明质酸冻干制剂的制备和药动学研究

目的以透明质酸为载体材料制备紫杉醇透明质酸冻干制剂,并考察冻干制剂在大鼠体内的药动学。方法采用乳匀-冻干法制备冻干制剂;以透射电子显微镜观察其粒子形态;建立冻干制剂及其在血浆中紫杉醇的HPLC分析方法;以紫杉醇注射剂为对照,测定冻干制剂10mg/kgiv给药后,大鼠体内的药动学参数。结果在冻干制剂中,紫杉醇以球形包覆于透明质酸基质中;在溶液中,分散成平均粒径为80nm的包覆微球;大鼠iv冻干制剂和紫杉醇注射剂的药物浓度-时间曲线符合二室模型,其药动学参数AUC分别为(37.68±6.36μg·h/mL和(27.54±5.88)μg·h/mL;CL分别为(0.26±0.04)h-1和(0.38±0.07)h-1。结论透明质酸可能成为一种新的抗癌药物载体。     

汉黄芩素脂质体的制备及大鼠体内药代动力学

目的:制备包封率高且粒径适宜的汉黄芩素脂质体,考察其体外释放及大鼠体内药代动力学。方法:用薄膜分散法制备汉黄芩素脂质体,用葡聚糖凝胶色谱法测定脂质体的包封率,考察脂质体在等渗磷酸盐缓冲液(pH 7.4)中的释放规律及血浆存在对其释放的影响,并研究其在大鼠体内的药代动力学。结果:制备的汉黄芩素脂质体包封率为(81.2±4.2)%,粒径为(157±22)nm。在磷酸盐缓冲液中24 h仅释放约40%,血浆的存在会导致释放有所增加。脂质体在大鼠体内具有明显的缓释效果,生物利用度是溶液剂的3.48倍。结论:制备的汉黄芩素脂质体包封率较高,粒径符合要求,体内外研究均表明脂质体具有缓释效果。     

氟康唑胶囊在健康人体中的药动学和相对生物利用度研究

目的　研究氟康唑胶囊对健康人体的药动学和相对生物利用度。方法　采用高效液相色谱法 (HPLC) ,测定 2 0名男性健康受试者单剂量交叉口服 30 0mg两种氟康唑胶囊后 ,不同时间血浆中的药物浓度。结果　两制剂的药时曲线均符合一房室模型 ,被试制剂和参比制剂的主要药动学参数如下 :Cmax分别为 (6 .2 2± 0 .6 9)mg·L-1和(6 .2 6± 0 .6 2 )mg·L-1;Tmax分别为 (1.78± 0 .93)h和 (1.78± 0 .75 )h ;T1/2ke分别 (2 5 .99± 4 .81)h和 (2 6 .2 0± 3.13)h ;AUCt0 分别为 (2 0 2 .2 2± 37.37)mg·h·L-1和 (2 0 9.98± 34.4 1)mg·h·L-1;AUC∞0 分别为 (2 2 1.77± 5 0 .71)mg·h·L-1和(2 2 6 .73± 37.78)mg·h·L-1;对试制剂的相对利用度F10 与F∞0 分别为 (97.74± 17.39) %和 (98.4 2± 19.4 6 ) %。结论　方差分析和双单侧t检验证明 2种制剂具有生物等效性     

洛莫司汀脂质体的制备及其在大鼠体内的药动学

目的 研究洛莫司汀(CCNU)脂质体的制备方法并考察用聚乙二醇单甲醚(2000)胆固醇琥珀酸酯(PEGCHS)修饰前后的2种脂质体静脉给药后在大鼠体内的药动学.方法 用改良逆相蒸发法制备普通和PEGCHS修饰的CCNU脂质体,测定包封率和粒径,静脉注射给药后,以格列苯脲为内标,采用高效液相色谱法测定血液中的药物含量;并采用3P87药动学程序进行数据处理.结果 制备的洛莫司汀脂质体包封率高(＞80%),平均粒径50 nm左右;CCNU PBS溶液、CCNU脂质体和用PEGCHS修饰的CCNU脂质体的t1/2α分别为0.061 8,0.093 1和0.153 l h;t1/2β分别为0.087 9,0.416 2和1.002 1 h;AUC分别为13.520 7,86.9113和166.640 6 mg·h·L-1.结论 制备的CCNU脂质体包封率较高,粒径小;2种CCNU脂质体均可不同程度地增加CCNU的AUC,延长其在血液循环中的时间,并以用PEGCHS修饰的CCNU脂质体效果最好.     

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.     

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.     

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…     

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.     

CLINICAL SIGNIFICANCE OF SERUM CYTOKINES IL-1β,sIL-2R,IL-6,TNF-α,AND IFN-v IN ACUTE CORONARY SYNDROME

Objectives To explore serum cytokines levels (including IL-1 β, sIL-2R, IL-6, TNF-α, and IFN-v) and their significance in patients with acute coronary syndrome (ACS) and the subsequent follow-ups, with attempt to estimate the role of various serum inflammatory markers in the diagnosis and assessment of ACS.Methods The study population include 40 patients with acute myocardial infarction (AMI), 40 patients with unstable angina pectoris (UAP), and 40 controls. Among the 80 patients, 60 patients attended a follow up 4 months later. Serum inflammatory markers including IL-1 β, sIL-2R, IL-6, TNF-α, and IFN-v were measured by enzyme linked immunosorbent assay.Results Serum IL- 1 β, sIL-2R, IL-6, TNF-α were significantly higher in AMI group or UAP group compared to the control group and became significantly lower 4 months later in the follow-up patients. Serum levels of IFN-v shows no significant difference between AMI group or UAP group and controls, also showing no significant change when measured in follow up patients. There was no correlation between serum creatine kinase-MB isoenzyme levels and serum inflammatory markers either in UAP or AMI group. Furthermore, when divided into two subgroups using Wagner's QRS scoring system in the AMI group, there is no difference of each serum inflammatory marker between ≤ 6 scores group and ＞ 6 scores group.Conclusion Serum levels of certain inflammatory markers may have some diagnostic value for ACS, and can be a useful marker reflecting disease stability.