双氯灭痛控释小丸制备工艺及释放度测定

通过考查，辅料比例对丸心成丸率有影响，致孔剂浓度、种类、粘度对控释小丸释药速度有影响，基本筛选出双氯灭痛控释小丸的处方为：丸心，含双氯灭痛50mg，、淀粉50mg、乳糖20mg；包衣溶液，含3％乙基纤维素、2%聚乙二醇400、2%羟丙基甲基纤维素(15cps)的乙醇-水混合落液．体外释放度试验证明，此控释小丸体补12h累积释药89．3%。     

硫酸沙丁胺醇脉冲释药微丸的制备及其体外释药研究

目的研究硫酸沙丁胺醇脉冲释药微丸的制备方法及其体外释放。方法用空白丸芯依次进行含药层（SBA）,溶胀层（低取代羟丙纤维素）及控释层（乙基纤维素水分散体）包衣制备硫酸沙丁胺醇脉冲释药微丸。采用紫外法和蓝法考察含药层、溶胀层及控释层在生理盐水中药的体外释放。结果含药层在生理盐水中能正常释药,溶胀层和控释层的增重对脉冲释药微丸的释药时滞和释药速率均有明显影响,溶胀层包衣增重15%,控释层包衣增重20%所制成释药微丸,释药时滞时间约为4.1 h时,这正好对应哮喘患者清晨2∶00发作时晨。结论所制备的硫酸沙丁胺醇脉冲释药微丸具有体外脉冲释药特性,适合哮喘患者预防用药。     

盐酸普萘洛尔控释微丸的研制

采用一步制丸和薄膜包衣工艺研究了盐酸普萘洛尔控释微丸，体外释药符合双相零级动力学过程，释药速率常数分别为Ｋｐ１＝１１．１３％／ｈ（０≤ｔ≤７）和Ｋｐ２＝３．７３％／ｈ（７＜ｔ≤１２），在ｐＨ２．２～５．６之间释药行为不变。与国外同类产品Ｉｎｄｅｒａｌ ＬＡ的体内外数据均无显著性差异（Ｐ＞０．０５），ＰＣＰ在模拟胃肠体液中的体外累积释药百分率与其体内吸收百分率之间有显著相关性，相关方程Ｆ（ｔ）＝２．     

替硝唑胃漂浮小丸的制备及体外释药

目的:研制替硝唑胃漂浮小丸,并对其体外释药特性进行研究。方法:以海藻酸钠为载体材料,采用离子胶凝法制备替硝唑胃漂浮小丸;以包封率、漂浮性能和体外释药特性为指标,通过单因素试验考察替硝唑与海藻酸钠比例、十六醇与海藻酸钠比例、海藻酸钠溶液浓度及制备工艺对小丸的影响,筛选优化处方和工艺;通过体外释药试验,考察溶出介质pH、离子强度及搅拌转速对小丸体外释药的影响。结果:小丸的优化处方及制备工艺为质量分数1%的海藻酸钠,海藻酸钠∶十六醇∶替硝唑质量比为1∶4∶3,替硝唑与十六醇加热熔融混匀后冷却固化,粉碎加至海藻酸钠溶液中制得混悬液,滴加至含氯化钙的凝胶液中形成小丸;小丸体外可缓慢释药达10 h以上,漂浮性能良好;随溶出介质pH值和搅拌转速增加,小丸释药有所加快;介质离子强度对小丸体外释药无显著影响。结论:替硝唑胃漂浮小丸具有胃内漂浮特性,可缓慢释放药物。     

结肠定位盐酸小檗碱羧甲基魔芋胶小丸体外释药的影响因素

目的:研究影响盐酸小檗碱羧甲基魔芋胶小丸体外释药的因素,评价其释药特性。方法:采用离子胶凝法制备羧甲基魔芋胶小丸,测定小丸在不同释放介质(β-甘露聚糖酶浓度和离子强度)条件下的药物释放、丸粒溶胀和溶蚀情况,并对药物释放和丸粒溶蚀与介质参数进行相关性分析。结果:与在不含酶介质相比,羧甲基魔芋胶小丸在含酶介质中的药物释放和丸粒溶蚀明显加快,随酶浓度增加,药物释放及丸粒溶蚀程度增加,药物释药符合Peppas方程,其中释药指数n大于1;随介质离子强度降低,小丸溶胀程度、药物释放和丸粒溶蚀程度增加。结论:盐酸小檗碱羧甲基魔芋胶小丸体外释药与介质中酶浓度和离子强度有关,释药过程为酶降解溶蚀释放,具有结肠定位释药的可行性。     

盐酸普萘洛尔控释微丸的研制

采用一步制丸和薄膜包衣工艺研制了盐酸普萘洛尔控释微丸（Ｐｒｏｐｒａｎｏｌｏｌｃｏｎｔｒｏｌｌｅｄ－ｒｅｌｅａｓｅｐｅｌｌｅｔｓ，ＰＣＰ），体外释药符合双相零级动力学过程，释药速率常数分别为Ｋ＿（ｐ１）＝１１．１３％／ｂ（０≤ｔ≤７）和Ｋ＿（ｐ２）＝３．７３％／ｈ（７＜ｔ≤１２），在ｐＨ２．２～５．６之间释药行为不变。与国外同类产品ＩｎｄｅｒａｌＬＡ的体内外数据均无显著性差异（Ｐ＞０．０５），ＰＣＰ在模似胃肠体液中的体外累积释药百分率与其体内吸收百分率之间有显著相关性，相关方程Ｆ（ｔ）＝２．００５Ａ（ｔ）－９．３９（ｒ＝０．９９５６）。     

盐酸地尔硫卓缓释脉冲微丸胶囊的体外释放研究

目的：制备盐酸地尔硫卓缓释脉冲控释微丸胶囊。方法：采用丙烯酸树脂域号和微晶纤维素（ MCC）为骨架材料制备盐酸地尔硫卓缓释微丸;采用低取代羟丙基纤维素（ Low Substituted Hydroxypropylcellulose L-HPC）为内层溶胀材料,选用乙基纤维素水分散体（ Surelease）为外层控释材料制备脉冲微丸。将两种微丸混合后制成缓释脉冲微丸胶囊,同时考察体外溶出度的影响因素。结果：体外释放试验证明,缓释微丸体外12h可持续释12h,脉冲微丸体外可达到时滞为4h,滞后1.5 h,累积释药80%以上的脉冲释药效果。两种微丸按比例混合后,其释药机制符合一级释药模型,达到良好的混合释放效果。结论：该制剂具有良好的缓释与脉冲效果。     

茶碱脉冲式控释微丸的制备

目的 探讨茶碱脉冲式控释微丸的处方组成和制备工艺,方法 采用多层包衣的方法。以体外释药时滞和释药速率为指标．经正交试验设计,筛选较佳的处方组成和工艺。结果 制得的脉冲控释微丸体释药时滞为6小时左右．在6～9小时内释药在75％～95％。稳定性良好。结论 采用多层包衣的方法能够制得合适的茶碱脉冲式控释微丸。     

5-氟尿嘧啶控释植入剂的体外释药试验

以５－氟尿嘧啶（５－Ｆｕ）为药芯，硅橡胶管为骨架，制成５－Ｆｕ控释植入剂。该控释剂为直径２ｍｍ、长２５ｍｍ的管型胶囊，壁厚０．５ｍｍ。每只胶囊含５－Ｆｕ１３．２ｍｇ。用三重蒸馏水作释放介质，行体外释药试验，高效液相色谱（ＨＰＬＣ）测定５－Ｆｕ释放量。结果表明控释制剂可保持药物零级释放，恒定释药量为４０μｇ／ｄ左右，时间长达２４周以上。     

胡芦巴胶作为微丸缓释材料的初步研究

目的考察胡芦巴胶对微丸释药行为的影响。方法采用挤出-滚圆法制备含药微丸并进行体外溶出度研究;考察亲水凝胶材料种类和用量以及药物溶解性能对微丸体外溶出度的影响。结果微丸的缓释性能随着处方中胡芦巴胶比例以及药物水溶性降低而得到改善,但胡芦巴胶的缓释效果稍逊于瓜尔胶、魔芋胶和羟丙胶纤维素。结论胡芦巴胶作为一种天然亲水凝胶材料,其缓控释能力有待提高。     

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.