克拉霉素胶囊的人体相对生物利用度研究

目的：研究健康中国青年志愿者单剂量口服克拉霉素后的药代动力学和相对生物利用度。方法：采用微生物法测定,血药浓度—时间数据用３Ｐ９７ 程序拟合计算药动学参数与生物利用度。结果：国产克拉霉素胶囊试验品与进口克拉霉素片剂对照品的Ｔｍ ａｘ分别为（１．２６±０．３６） ｈ 和（１．３２±０．３５） ｈ,Ｃｍａｘ分别为（２．４５６±０．４３０） ｍ ｇ／Ｌ和（２．２４６±０．３３８） ｍ ｇ／Ｌ,ＡＵＣ０－ ２４ｈ分别为（１５．１８９±２．７１８） ｍ ｇ／（Ｌ·ｈ）和（１５．６５１±２．５５７） ｍ ｇ／（Ｌ·ｈ）。经配对ｔ检验、方差分析检验差异无显著性（Ｐ＞ ０．０５）。结论：国产克拉霉素胶囊和进口克拉霉素片剂具有生物等效性。     

RP-HPLC测定血浆中奥美拉唑及其相对生物利用度研究

建立了ＲＰ－ＨＰＬＣ快速测定血浆中奥美拉唑的方法，应用该法测定了１０名健康志愿受试者随机交叉单剂量口服奥美拉唑受试片和进口胶囊后的血药浓度，结果表明：两种制剂在人体内的药动学行为均符合一级吸收的开放一室模型，其达峰时间（ｔｍａｘ）分别为（２．６０±０．９４）ｈ和（３．３０±．８２）ｈ；峰浓度（Ｃｍａｘ）分别为（１１７１．０±５５３．２）ｎｇ／ｍｌ和（１２１４．９±５９０．２）ｎｇ／ｍｌ；生物半衰期（ｔ１／２）分别为（０．９５±０．４４）ｈ和（１．０６±０．７３）ｈ；血浓经时曲线下面积（ＡＵＣ）分别为（３６９１．８±２６６５．２）ｎｇ·ｈ／ｍｌ和（３３８７．２±２４０８．７）ｎｇ·ｈ／ｍｌ，配对ｔ检验结果表明，差异均无显著性（Ｐ＞０．０５）。经双单侧ｔ检验，结果显示两者在生物利用度方面属于等效，相对生物利用度为１０８．２３％。     

头孢克洛分散片在健康人体的药物动力学及相对生物利用度研究

研究头孢克洛分散片在健康人体内的药物动力学及相对生物利用度。采用高效液相色谱法测定８ 名志愿者单剂量口服５００ ｍ ｇ 头孢克洛分散片和胶囊后的血液浓度。药动学参数经３Ｐ８７ 软件处理计算。头孢克洛分散片的主要药动学参数：Ｃｍ ａｘ（１５３２±２４２） ｍ ｇ／Ｌ,Ｔｐｅａｋ（０５７±０１５） ｈ,Ｔ１／２ｋｅ（０７６±０２５） ｈ,ＡＵＣ（２４０７±４４７） ｍ ｇ／（ｈ·Ｌ）;头孢克洛胶囊的主要药动学参数：Ｃｍ ａｘ（１５．６３±２．３２） ｍ ｇ／Ｌ,Ｔｐｅａｋ（０．６０±０．１３） ｈ,Ｔ１／２ｋｅ（０６７±０１８） ｈ,ＡＵＣ（２３１３±３３７）ｍ ｇ／（ｈ·Ｌ）。经统计学处理,两种剂型的药动学参数之间差异均无显著性（Ｐ＞ ００５）。头孢克洛分散片的相对生物利用度为（１０３７５±１１３６）％ ,双单测ｔ检验（ＮＤＳＴ程序）的结果表明,两种制剂生物等效。     

国产替硝唑胶囊剂人体药物动力学及其相对生物利用度

１０名健康志愿者随机交叉一次口服１ｇ受试替耠唑胶囊或参比片剂。用高效液相－紫外（ＨＰＬＣ－ＵＶ）检测法测定其血药浓度经时过程。胶囊和片剂的主要药动力参数分别为：ｔ１／２ｋ（１４．４８±１．３８）ｈ和（１５．１０±０．８３）ｈ,Ｃｍａｘ（２０．５７±２．１３）ｍｇ．Ｌ＾－１和（１９．３６±２．３１）ｍｇ．Ｌ＾－１,ＡＵＣ（４９７．６２±５０．６２）ｍｇ．ｈ．Ｌ＾－１和（４７７．３９±４４．１５）ｍｇ     

单硝酸异山梨酯缓释片的释放度及相对生物利用度

对试制的单硝酸异山梨酯缓释片与德国麦克乐制药公司（ Ｍｅｒｃｋｌｅ Ｇｍｂ Ｈ） 缓释胶囊剂进行体外释放度、体内血浓测定比较;体外含量测定采用 Ｈ Ｐ Ｌ Ｃ 法,体内采用 Ｇ Ｃ 法。体内数据按口服单室模型,经计算机处理求得药动学参数：缓释胶囊： Ｋａ ＝ ０ ．２５０ ｈ － １ , Ｋｅ ＝ ０ ．１３７９ ｈ － １ , Ｔｍ ａｘ ＝ ５ ．３６ ｈ , Ｃｍ ａ ｘ ＝ ３５１ ．９８ ｎｇｍｌ, Ａ Ｕ Ｃ０ →∞ ＝５３８２ ．７９ ｈ·ｎｇｍｌ , Ｆ Ｉ＝ １ ．８６ 。缓释片： Ｋａ ＝ ０ ．２４７９ ｈ － １ , Ｋｅ ＝ ０ ．１４０３ ｈ － １ , Ｔｍ ａｘ ＝ ５ ．３５ ｈ , Ｃｍａ ｘ ＝ ３７７ ．０９ ｎｇｍｌ , Ａ Ｕ Ｃ０ →∞ ＝ ５７２８ ．５１ ｈ·ｎｇｍｌ , Ｆ Ｉ＝ １ ．９７ 。研制的单硝酸异山梨酯缓释片对德国麦克乐制药公司缓释胶囊相对生物利用度为（１０６ ．２８ ±３ ．４３） ％ 。     

石楠藤提取物对急性出血坏死性胰腺炎大鼠治疗作用的实验研究

作者报道中药石楠藤提取物对急性出血坏死性胰腺炎（ＡＨＮＰ）大鼠治疗作用的实验研究。将１００只ＳＤ大鼠随机分为三组：①假手术组（ＳＯ组）；②ＡＨＮＰ组（ＡＰ组），该组动物在ＡＨＮＰ诱发后，不做特殊治疗；③石楠藤提取物治疗组（ＳＮ组）。该组动物在ＡＨＮＰ诱发后１０分钟经腹腔内注射石楠藤提取物（１％石楠藤提取物５ｍｌ／ｋｇ体重）。结果表明：ＳＮ组血清淀粉酶值明显下降（ＳＮ组１６１３０±５０３０Ｕ／Ｌ６ｈ、１９２９０±５３８０Ｕ／Ｌ１２ｈｖｓＡＰ组２３７８０±３９６０Ｕ／Ｌ、２８４７０±４１５０Ｕ／Ｌ，Ｐ＜０．０１）。血中ＰＡＦ含量明显降低（ＳＮ组１．３±０．３０ｎｇ／ｍｌ１ｈ、２．０±０．３４ｎｇ／ｍｌ６ｈ、２．１±０．３２ｎｇ／ｍｌ１２ｈｖｓＡＰ组２．２±０．２５ｎｇ／ｍｌ、６．１±０．４２ｎｇ／ｍｌ、１０．１±０．５３ｎｇ／ｍｌ，ｐ＜０．０１）。血浆内毒素含量明显下降（ＳＮ组６９．９±７．２ＥＵ／Ｌ、６ｈ、９１．１±８．４ＥＵ／Ｌ、１２ｈｖｓＡＰ组９８．４±６．９ＥＵ／Ｌ、１５１．７±９．１ＥＵ／Ｌ，Ｐ＜０．０１）。石楠藤提取物治疗组术后平均存活时间明显长于ＡＰ组（ＳＮ组：４３．５ｈ，ＡＰ组１１．５ｈ，ｐ＜０     

依那普利对高血压左心室肥厚患者血浆P物质和肾素—血管紧张素…

观察２７例高血压病伴左心室肥厚患依那普利治疗１２周前后左心室质量指数，血浆肾素活性及血浆Ｐ物质血管紧张素Ⅱ和醛固酮水平的变化。结果：血浆ＳＰ水平由治疗前（１２．６２±５．１１）ｎｇ．Ｌ＾－１升高至（３７．２１±１１．０６）ｎｇ．１０＾－１ＬＶＭＩ由治疗前（１３９．２９±１７．９８）ｇ．ｍ＾－２降低（１０７．７７±１０．９４）ｇ．ｍ＾－２；ＰＲＡ由治疗前（２．３３±５３．３９）μｇ．Ｌ＾－１．ｈ＾     

自发性高血压大鼠心肌纤维化与醛固酮和血管紧张素Ⅱ的关系

目的采用动物实验和细胞培养方法探讨自发性高血压大鼠（ＳＨＲ）心肌纤维化与醛固酮（Ａｌｄ）和血管紧张素Ⅱ（ＡｎｇⅡ）的关系。方法和结果（１）动物实验部分利用２０ｍｇ·ｋｇ－１·ｄ－１剂量的安体舒通治疗２４周龄ＳＨＲ（ｎ＝１０），持续１６周，借助计算机辅助图像分析技术，形态学观察其对心肌间质和血管旁纤维化的疗效。发现ＳＨＲ不但在左室而且右室心肌胶原容积分数（ＣＶＦ）都有明显升高；安体舒通治疗对血压和左室肥厚无明显影响，但能降低左右心室的ＣＶＦ（左室心内膜下１０．１１％±２．０７％，ｖｓ６．０６％±１．１９％，心外膜下６．４１％±１．５２％ｖｓ４．１８％±１．８６％，右室８．０６％±１．５１％５．０１％±１．２１％，Ｐ＜０．０１～０．０５）；减轻血管旁胶原面积（ＰＶＣＡ）（３．８４±０．４０ｖｓ２．８８±０．８３，Ｐ＜０．０５），但均未能降低到ＷＫＹ水平。（２）细胞培养部分通过离体培养的ＳＨＲ和ＷＫＹ两种心肌成纤维细胞，观察对血管紧张素Ⅱ（ＡｎｇⅡ）和醛固酮（Ａｌｄ）及相应拮抗剂Ｄｕｐ７５３和安体舒通的反应。发现在无血清状态下，ＳＨＲ心肌成纤维细胞的３Ｈ－ｐｒｏｌｉｎｅ参入量高出ＷＫＹ６８％，ＡｎｇⅡ和Ａｌｄ呈浓     

盐酸曲马多缓释片的制备及药动学研究

研制了盐酸曲马多缓释片，其体外溶出符合一级动力学过程，释药常数Ｋｒ＝０．１９８ｈ＾－１。盐酸曲马多体内吸收符合一室模型，药动学参数为Ｋａ＝０．５７０２ｈ＾－１，Ｋ＝０．０８５６ｈ＾－１，Ｃｍａｘ＝２１９．５７ｎｇ／ｍｌ、Ｔｍａｘ＝４．６２ｈ，ＡＵＣ０→∞＝３７２１．０９ｎｇ／ｍｌ．ｈ。经双单侧ｔ检测，结果表明普通胶囊与缓释片的Ｃｍａｘ、Ｔｍａｘ具有显著性差异，而ＡＵＣ０→∞无差异，表明两制剂生物等     

环孢素胶丸的药代动力学和相对生物利用度

采用高效液相色谱法进行环孢素胶丸的药代动力学和生物利用度研究，１０名健康志愿者随机交叉单剂量ｐｏ温州第二制药厂和瑞士Ｓａｎｄｏｚ公司的环孢胶丸（２００ｍｇ），其血药浓度－时间曲线均符合一级吸收的双室模型，温州产环孢素胶丸的主要药动学参数ｔ１／２Ｋｄ＝１．０９±０．４６ｈ，ｔ１／２α＝０．３４±０．１５ｈ，ｔ１／２β＝５．１３±１．４１ｈ，ｔｍａｘ＝１．１９±０．１９ｈ，Ｃｍａｘ＝８７８．２±１６７．２ｎｇ／ｍｌ，ＡＵＣ＝４１２７．７±８５４．１ｎｇ·ｈ·ｍｌ－１，其相对生物利用度为（１０４．２±１１．９）％     

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.     

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.     

Expression of OPGmRNA and ODFmRNA in the patients of hip fracture due to osteoporosis

Objective：To investigate the gene expression of osteoprotegerin（OPG） and osteoclast differentiation factor（ODF） in the bone tissue of patients with hip fracture due to osteoporosis. Methods：OPGmRNA and ODFmRNA in the bone tissue in 50 cases of osteoporosis sufferers（over 50 years old） with hip fracture（Observer Group） and 30 cases of hip facture sufferers with no osteoporosis（Control group） were analyzed with the Semi-Quantitative RT-PCR method. Results：The mRNA expressed of ODF, OPG were both high in the patients with hip fracture. In the control group, the expression of OPG mRNA was observed, while the expression of ODF mRNA was very slight. Conclusion：Aged patients contained all signals including OPG, ODF that are essential for inducing osteoclastogenesis and promoting bone resorption.     

The clinicopathological and immuohistochemical analysis of solid-pseudopapillary tumor of the pancreas： report of 9 cases

Objective：To investigate the clinical features, pathological characteristics and immunophenotype of solid-pseudopapillary tumor of the pancreas（SPTP）. Methods：Nine surgically treated cases of SPTP were retrospectively reviewed. Hematoxylin and Eosin（HE） staining and immunohistochemical staining were used to analyze all cases, and the general clinical data was collected. Results：Six patients were asymptomatic except for a palpable mass. Two patients complained of vague-epigastric pain. One patient appeared jaundice. The tumor was encapsulated and solid tissues alternately with cystic tissues. Histologically, the histological structure of solid portion was pseudopapillary with a fibrovascular core. Tumor cells were uniform and medium-sized which were arranged in sheets ets or nests or pseudopapillary patterns. Immunohistochemical studies demonstrated that SPTP proved positive in vimentin（9/9 cases）, AAT（9/9 cases）, NSE（9/9 cases）, ACT（7/9 cases）, CK20（2/9 cases）, CgA（1/9 cases）, S-100（3/gcases）, PR（4/gcases）, Syn（3/9 cases） and CD56（5/9cases）, negative in CEA and ER. Conclusion：SPTP is a tumor predominantly occurring in young women frequently without special symptoms. This tumor has various characteristical histological patterns with different immunophenotype.     

Dynamic Changes in Serum Estradiol and Progesterone levels in Patients of Premenstrual Syndrome with Adverse Flow of Liver-qi

Objective:To probe into the influence of changes of ovarian hormones on the pathogenesis of the specific sub-type premenstrual syndrome(PMS)and reveal partial microcosmic mechanisms of adverse flow of liver-qi.Methods:Estradiol(E2)and progesterone(P)levels in serum were determined at different phases of menstrual cycle by radioimmunoassay.Results:In the group of PMS with adverse flow of liver-qi.the secretive peak value Of E2 and P at the follicular phase significantly decreased,and the secretive peak value at the luteal phase did not come into being.Conclusions:Low E2 and P secretive peak at the follicular phase and absence of secretive peak at the luteal phase is one of the microcosmic mechanisms of PMS with adverse flow of liver-qi.One of the pathophysiologic mechanisms of specific sub-type PMS is probably the continuous low level of E2and P.     

Real-time Three-dimensional Echocardiography in Assessment of Left Ventricular and Right Ventricular Volumes

Real-time three-dimensional echocardiography (RT3DE)is a new ultrasound technique that enables dynamic threedimensional visualization and quantification of the heart in real time. Investigation of feasibility and methodology of RT3DE in determining left ventricular (LV) and right ventricular (RV) volumes, RT3DE was performed in 35 normal adults using Philips SONOS 7500 system with a 2-4 MHz matrix array transducer. The 60°×60° "pyramid" volume database was obtained and analyzed on a TomTec echo workstation. Both LV and RV volumes were calculated with four 3DE methods (i.e. apical 2, 4, 8, and 16-plane) through manually tracing ventricular endocardial borders in end diastole and end systole. Stroke volumes were then calculated. LV volume was also measured by 2DE Simpson's rule using GE VIVID 7 ultrasound machine.     

SCREENING FOR A 21-CHROMOSOME ABNORMALITY IN PREIMPLANTED EMBRYOS OF ELDERLY WOMEN

Increasing maternal age is the only etiological factor unequivocally linked to Down's syndrome in humans. The occurrence rate of newborns with Down's syndrome is about 1/220 in women over 35 years old. However, the occurrence rate in embryos fertilized in vitro, of the elder woman is unclear. Using FISH we screened the number of chromosome 21 in preimplanted embryos of 5 elderly women (average age, 38.4 years) to study the feasibility and necessity of screening trisomy 21 in embryos in patients over 35 years old at the in vitro fertilization (IVF) center.