褪黑素载药纳米粒的优化设计及研制

目的：探讨采用复合乳液-溶剂挥发法制备褪黑素载药纳米粒的最佳工艺条件。方法：以聚乳酸、壳聚糖可降解生物材料为载体,明胶为分散剂,span-80和tween-80混合液为微乳液,根据微粒的表面形态、粒径大小、分布、包封率、载药量选择最佳工艺条件,制备褪黑素载药纳米粒。结果与结论：原子力显微镜下可见纳米粒表面圆滑,分布均匀。正交设计效应曲线图直观分析和方差分析结果显示,搅拌速度、溶剂挥发温度、聚乳酸与褪黑素投药比、壳聚糖浓度是影响制备工艺的主要因素。在30℃,1000r／min搅拌速度,搅拌时间45min,m(褪黑素)：m(聚乳酸)为1：5,V(Tween-80)：V(Span-80)为5：1,壳聚糖质量浓度为1％条件下,可制备成平均粒径为45．84nm,包封率为38．33％,载药量为8．35％的褪黑素载药纳米粒。     

O-羧甲基乳糖酰化壳聚糖-聚乳酸阿霉素纳米粒的制备及其物理化学性质的测定

目的制备具有肝靶向性的O-羧甲基乳糖酰化壳聚糖-聚乳酸阿霉素纳米粒,并对纳米粒药物含量、包封率和粒径大小进行检测。方法制备出O-羧甲基乳糖酰化壳聚糖-聚乳酸阿霉素纳米粒,并通过紫外分光光度计测定纳米粒的载药量以及包封率,激光粒度分析仪及电镜测量粒径大小。结果电镜及激光粒度分析仪检测证实纳米粒大小均匀,粒径(197±32)nm,载药量为(44.79±4.27)μg/mg,包封率(67.34±3.32)%。结论该实验制备的纳米粒其粒径小,载药量及包封率高。     

恩诺沙星纳米粒的制备及其药剂学性质研究

目的:研制一种新型的恩诺沙星纳米粒制剂。方法:以聚乳酸为载体材料,采用溶剂挥发法制备了恩诺沙星聚乳酸纳米粒,对其形态学、载药量、包封率以及粒径分布等性质进行了研究,并对其进行相关的质量评价。结果:制备的恩诺沙星聚乳酸纳米粒的包封率平均为71.0%,载药量平均为11.3%,平均粒径为66.8 nm,粒径范围为30.0 nm~117.5 nm,电子透射显微镜下观察纳米粒,基本呈较光滑圆整的球形,大小较均匀,且粒径分布较窄。结论:制备工艺可行且制备的恩诺沙星聚乳酸纳米粒包封率相对较高,质量稳定,重现性好。     

荆芥内酯聚乳酸乙醇酸纳米粒的制备及其稳定性研究

目的制备荆芥内酯聚乳酸乙醇酸纳米粒,并优化其制备工艺。方法以粒径、分散度、包封率和载药量为指标,对溶剂挥发法、溶剂扩散法和溶剂-非溶剂法制备荆芥内酯纳米粒进行比较。在单因素考察基础上,采用正交设计法对纳米粒的处方和溶剂-非溶剂法制备工艺进行优化,并考察了4℃和25℃条件下纳米粒溶液的稳定性。结果溶剂-非溶剂法制备的荆芥内酯纳米粒形态圆整,大小均匀,平均粒径(80.3±1.75)nm,分散度0.0144±0.00625,包封率可达52.53%±0.97%,载药量27.56%±0.91%,显著优于溶剂挥发法和溶剂扩散法,且具有良好的稳定性。结论溶剂-非溶剂法制备荆芥内酯纳米粒具有工艺简便,粒径和分散度小,包封率和载药量高,重复性好,质量稳定的优点。     

重组人血管内皮抑素壳聚糖纳米粒的制备及体外评价

采用离子凝胶法制备重组人血管内皮抑素(商品名:Endostar)壳聚糖纳米粒,并对纳米粒的载药量、包封率、粒径、形态、体外释放、体外活性及Endostar结构的完整性进行考察。制得的Endostar壳聚糖纳米粒载药量为(10.5±1.1)%,包封率为(81.3±1.8)%;平均粒径为137 nm,为球形结构;体外释放10 d累积释放达到80%。凝胶电泳实验说明Endostar结构完整,制备与释放过程结构均未被破坏;人脐静脉内皮细胞增殖实验说明Endostar纳米粒仍保留原有的生物活性。结果表明壳聚糖作Endostar的载体,制得的纳米粒具有合适的粒径及包封率,并能达到缓释作用,不会破坏Endostar的结构,同时保留原有的生物活性。     

紫杉醇聚乳酸纳米粒的制备及特性考察

目的制备紫杉醇聚乳酸纳米粒并考察其特性。方法采用超声乳化法制备紫杉醇聚乳酸纳米粒,动态光散射粒径仪测定粒径大小,透射电镜表征表面形态,HPLC测定包封率及载药量。结果紫杉醇聚乳酸纳米粒的平均粒径为(230.00±1.08)nm,包封率为(93.57±0.50)%,载药量为(3.01±0.03)μg/mg。结论该方法制备紫杉醇纳米粒工艺简单,方法可行。     

雷公藤甲素聚乳酸纳米粒载药体系的研究

目的:研究聚乳酸包裹雷公藤甲素纳米粒的制备,并探讨其载药性质.方法:采用改良的自乳化溶剂蒸发法制备雷公藤甲素(TP)聚乳酸(PLA)纳米粒,考察各工艺因素对纳米粒粒径、包封率及载药量的影响,并通过透射电子显微镜(TEM)、动态激光粒度分析仪、傅立叶红外光谱(FT-IR)及X-射线粉末衍射(X-ray)初步研究了其载药性质.结果:优选出适合处方的包合工艺为:水相与有机相的比例为40:15(v/v),表面活性剂的浓度为1%,药物的浓度为0.3%,TP与PLA的比例为1:15(w/w),包封率为74.27%,载药量的百分率为1.36%,所得纳米粒形态光滑规整,其粒径分布均匀,FT-IR及X-ray表明TP被有效地包裹在纳米粒中.结论:此方法适合制备脂溶性药物聚合物纳米粒,适合大生产.     

壳聚糖纳米粒作为基因载体的研究:制备,特征和对DNA的保护

目的:制备载基因壳聚糖纳米粒,研究纳米粒药剂学特征以及对DNA的保护作用.方法:复凝聚法制备纳米粒,对纳米粒的形态、粒径及分布、Zeta电位、包封率、载药量和处方影响因素进行了考察,凝胶阻滞法分析壳聚糖和pDNA的聚合方式,pDNA保护性试验考察壳聚糖纳米粒抵抗核酸酶的能力.结果:制备的pDNA/壳聚糖纳米粒为结构较紧密的不规则球形,平均粒径为(240.4±13.2)nm,多分散指数为(0.173±0.05),Zeta电位为(18.4±0.6)mV,包封率为(95.2±1.9)%,载药量为(30.7±0.8)%.凝胶阻滞分析结果表明,纳米粒荷正电,pDNA与壳聚糖之间通过静电作用而完全结合.纳米粒的粒径、Zeta电位受处方中的壳聚糖相对分子质量、N/P(壳聚糖中伯胺基数目/pDNA中磷酸基数目)比、pDNA浓度、Na2SO4浓度和pH值等因素影响.pDNA保护性试验表明,壳聚糖纳米粒对pDNA有保护作用.结论:壳聚糖可以有效凝聚pDNA,采用复凝聚法可制得200～500 nm范围荷正电的纳米粒,有较高的包封率和载药量,可有效保护pDNA免受核酸酶降解.壳聚糖作为黏膜给药的非病毒基因载体具有应用价值.     

聚乳酸-羟基乙酸共聚物载肝细胞生长因子纳米粒的构建及生物学活性评价

目的探究制备聚乳酸-羟基乙酸共聚物（PLGA）纳米粒的优化条件,构建肝细胞生长因子（HGF）纳米粒,评价其包封率、 载药量、回收率、释放度和生物学活性。方法采用复乳溶剂挥发法制备牛血清白蛋白（BSA）PLGA纳米粒,通过正交试验设计, 以粒径较小,包封率、载药量和回收率较高为考察指标,优化纳米粒的制备条件;选取优化条件制备HGF纳米粒,分别采用BCA 试剂盒和HGF-ELISA试剂盒检测BSA纳米粒和HGF纳米粒的包封率、载药量和释放度,通过CCK8增殖实验评价HGF纳米粒 的生物活性。结果优化条件下制备的HGF 纳米粒大小均匀,粒径234.4±4.8 nm,包封率（77.75±3.04）%,回收率（49.33± 9.34）%,体外释放度曲线表现为先突释,后缓释;HGF纳米粒可以促进角质形成细胞的增殖。结论复乳溶剂挥发法-优化条件 下制备的HGF纳米粒具有较高包封率,良好的缓释效果和生物学活性。     

激素类药物醋酸地塞米松纳米粒的研制及其质量控制

目的:探讨研制载药量高,具有缓释效果的醋酸地塞米松纳米粒制剂的制备方法。方法:本次研究以醋酸地塞米松为主药,大豆油和蛋黄卵磷脂为载体材料,采用薄膜-超声法制备醋酸地塞米松纳米粒,并对载体投料比、投药量、表面活性剂种类、有机溶剂的种类以及超声时间进行筛选和体外释放进行研究。结果:载体材料蛋黄卵磷脂(A)和大豆油(B)的投料比为1∶1时,制备纳米粒制剂的粒径、包封率以及载药量都最为理想,5%的泊洛沙姆-188和5%的吐温-80各12 ml,并超声制成初乳,最佳超声时间为6 min。该处方制备所得的醋酸地塞米松纳米粒的球体均匀度较好,载药纳米粒的包封率约为96.71%。结论:本研究制剂具有提高醋酸地塞米松包封率和载药量的优点,可以避免主药的迅速释放,质量容易控制,值得在临床上推广和应用。     

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.     

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.