小剂量阿司匹林缓释微丸药代动力学及生物等效性研究

用荧光分光光度法测定了口服小剂量阿司匹林缓释微丸在人体内的血药浓度,10名健康志愿受试者体内药代动力学结果显示,缓释微丸的相对生物利用度为Ka=0.4869 h~(-1),K=0.1097 h~(-1),t_(1/2)=6.69 h,C_(mx)=4.47μg/ml,t_(max)=4.52 h。方差分析表明阿司匹林缓释微丸与普通片具有生物等效性。     

用高效液相色谱法测定消炎痛的血浓度

本文报道用高效液相色谱法测定消炎痛(Indomethacin)血浓度的方法和结果。高效液相色谱仪填以反相YWG-C_(18)(10μm),并带有254nm UV检测器。流动相为甲醇∶水∶乙腈∶冰醋酸(63∶27∶10∶0.1ml,V/V),流速为1ml/min。内标物选用炔诺酮。消炎痛的保留时间t_R=9min,内标物t_R=6min10s。线性范围为0.1～5.0μg/ml血清,检测限为0.05μg消炎痛。应用本法测定7名健康受试者的消炎痛血清浓度,其药代动力学参数平均值为:K=0.1677h~(-1),K_α=2.4597h~(-1),t_(1/2)=4.44h,C_(max)=2.3924μg/ml,t_(max)=1.65h,AUC_(0～12h)=6.7525μg.h/ml。结果表明,本法简便快速,适于临床进行消炎痛血清浓度的监测。     

布洛芬缓释微丸的制备及其药物动力学研究

采用膜控法制备布洛芬缓释微丸,应用转篮法(50r/min,37±1℃)比较了缓释微丸和普通片剂的体外药物溶出速率,采用HPLC法测定了制剂的血药浓度,并研究了制剂在人体内的药物动力学。缓释微丸的体外药物溶出符合一级动力学过程(K_r=0.4505h~(-1));体内动力学过程符合一级吸收和一级消除的单室模型,k_a=0.27h~(-1),K=0.27h~(-1),V_d=7.54L,t_(max)=3.97h,C_(max)=19.52μg/ml。多剂量给药血药浓度测定及计算表明:缓释微丸具有维持有效血药浓度(8.5μg/ml)时间长,血药浓度波动范围小的特点。此外,缓释微丸的体内外数据具有显著的相关性(p<0.01)。     

盐酸雷尼替丁胃内滞留漂浮型缓释片的制备及药物动力学研究

本文研制了盐酸雷尼替丁胃内滞留漂浮型缓释片剂(RSRT)。本品的体外溶出符合一级动力学过程:RSRT在胃内滞留时间5-6h,明显比普通对照片(2h内)长;RSRT体内以单室模型描述较适宜,RSRT体内为一级释药。药动学参数为:Ka=0.2550h~(-1),K=0.2765h~(-1),Vd=84.38L,t_(max)=3.77h,C_(max)=627.7ng/ml。本品的体内外数据具有显著相关性。     

盐酸雷尼替丁胃内滞留漂浮型缓释片的制备及药物动力学研究

本文研制了盐酸雷尼替丁胃内滞留漂浮型缓释片剂(RSRT)。本品的体外溶出符合一级动力学过程:RSRT在胃内滞留时间5-6h,明显比普通对照片(2h内)长;RSRT体内以单室模型描述较适宜,RSRT体内为一级释药。药动学参数为:Ka=0.2550h~(-1),K=0.2765h~(-1),Vd=84.38L,t_(max)=3.77h,C_(max)=627.7ng/ml。本品的体内外数据具有显著相关性。     

乙酰水杨酸肠溶微丸的研制

采用薄膜包衣法制备乙酰水杨酸肠溶微丸,以转篮法(100 r/min,37 0.5℃)测定了体外溶出速率。实验结果表明:本制剂2 h在人工胃液中的释放量不超过15%,转入人工肠液后在40min内完全释放(Kr=2.975 h~(-1))。体内试验选择了六名健康受试者(平行法单剂量给药900 mg)服用乙酰水杨酸普通片及肠溶微丸,测定了二种制剂在体内的经时过程。药动学参数的求算表明:普通片:Ka=0.309 h~(-1),K=0.309 h~(-1),Cls=1.598 L/h,AUC=563.30 h·μg/ml;肠溶微丸:Ka=0.415h~(-1),K=0.134 h~(-1),Cls=1.235 L/h,AUC=728.66 h·μg/ml。     

补骨脂素混合结晶在S_(180)小鼠腹水和癌细胞内的浓度测定及药代动力学研究

补骨脂素混合结晶中补骨脂素在S_(180)小鼠腹水内属单室模型中呈双峰吸收。其动力学参数如下■l/2(h)为22.19;K_a(h~(-1))为12.3580;K(h-1)为0.0312;tlag(h)为0.0718;C_(max)(μg/ml)为6.3967;t_(max)(h)为0.5570;AUC(μg·h/ml)为175.0300。2亿S_(180)癌细胞内在0.25h时,其补骨脂素含量高达10.97μg/ml,腹水内补骨脂素含量既高且久,有利于肿瘤的冶疗。     

血清呋喃氟脲嘧啶的反相高效液相色谱测定法及在大鼠体内的药代动力学研究

本文报道呋喃氟脲嘧啶(FT-207)血清浓度的反相高效液相色谱测定法。固定相为Shim-packCLC-ODS柱(0.15m×6.0φ),流动相为定时程序控制的甲醇溶液,检测波长254nm。样品用甲醇沉淀蛋白,取上清液20ul直接进样。最低检测浓度为0.03μg/ml,标准曲线的线性范围为0.03～132.0μg/ml(r=0.99997)。用本法测定了9只大鼠口服FT-207后的血清浓度,其药时曲线符合一室开放模型。用残数法算得主要药代学参数为k(?)=1.2883±1.0972h~(-1),k_e=0.0767±0.0179h~(-1),tal/2=0.77±0.37h,tel/2=9.42±1.86h,t_p=2.88±1.02h,C_(max)=83.56±11.87μg/ml,AUC=1659.43±258.48μg.h/ml。     

原子吸收分光光度法测定家兔口服碳酸锂的血药浓度和药物动力学参数

采用国产原子吸收分光光度计测定血液中的锂浓度,在0.05～1.50μg/ml浓度范围内吸收度和浓度呈线性,A=0.008+0.289Liμg/ml,γ=0.998,回收率测定为94.0±1.6～97.3±2.3％(加入量为0.25～0.50μg/ml):五只家兔一次口服碳酸锂12mg/kg定时取血测定锂浓度,得到的时间—药浓曲线呈显典型的二室模型,动力学参数为α=0.43h~(-1),β=0.038h~(-1),k_a=2.12h~(-1),t 1/2α=1.60h,t 1/2 β=18.1h,t(?)=1.2h,C_(max)=0.29mmol/L     

盐酸黄连素对环孢素A增效作用的药物动力学研究

目的:研究盐酸黄连素对肾移植受者使用环孢素A增效作用的体内动力学过程。方法:选择肾移植术后1个月以内、连续服用环孢素A2周、肝肾功能稳定的患者6名,环孢素A剂量6mg·kg~(-1)d~(-1),用FPIA方法(单抗)检测合用黄连素前后各时间点环孢素A全血浓度。结果:单服环孢素A的主要药动学参数分别为T_(max)(h):0.93±0.47,C_(max)(μg·L~(-1)):1176.7±405.88,C_(min)(μg·L~(-1)):173.95±78.71,T_(1/2)(h):2.62±1.00,AUC(μg·L~(-1))·h~(-1):5237.7±1776.5,CL/F(L·h~(-1)):35±15;与黄连素合用的主要药动学参数为T_(max)(h):2.26±1.15,C_(max)(μg·L~(-1)):919.17±330.87,C_(min)(μg·L~(-1)):319.22±163.45,T_(1/2)(h):5.33±2.60,AUC(μg·L~(-1))·h~(-1):9213.17±3802.6,CL/F(L·h~(-1)):22±13。结论:盐酸黄连素与环孢素A合用可使后者T_(max)滞后,t_(1/2)延长,清除率减少,AUC增大,生物利用度增加;对肝肾功能没有影响。     

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…     

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.     

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.     

Dr.Zhang Ren's Experience in the Acupuncture Treatment of Different Diseases with the Same Therapeutic Principle

Dr.Zhang Ren,the chief physician,is the chairman of Shanghai Acupuncture and Moxibustion Association.Having been engaged in medicine for about 40 years,he is experienced in treating various intractable diseases.In his long years of clinical practice,he advocates taking the TCM differentiation as the basis to seek for the acupuncture method for treatment of modern intractable diseases.The author of this essay had the fortune to follow Dr.Zhang in study.The following is a summary of Dr.Zhang's experience in the acupuncture treatment for different intractable diseases with the same therapeutic principle.     

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.     

猪肺磷脂注射液联合经鼻持续气道正压通气对呼吸衰竭早产儿的临床疗效及肌酸激酶同工酶活性的影响

目的 探讨猪肺磷脂注射液联合经鼻持续气道正压通气(NCPAP)对呼吸衰竭早产儿的临床疗效及肌酸激酶同工酶活性(CK-MB)的影响.方法 选取呼吸衰竭早产儿80例,分为观察组和对照组各40例.对照组采用NCPAP给氧治疗,观察组给予NCPAP给氧联合猪肺磷脂气管内给药.观察两组患儿治疗前及治疗12h、24 h后PaO2、PaCO2、血氧饱和度(SaO2)、pH的变化情况,检测治疗前及治疗5d后血清CK-MB水平;评估两组患儿的临床治疗效果.结果 两组患儿PaO2、PaCO2、SaO2、pH比较,差异均有统计学意义(P＜0.05),其中观察组治疗后的PaO2、SaO2、pH均高于对照组,PaCO2则低于对照组.两组的PaO2、SaO2、pH均随观察时间延长而升高(P＜0.05),PaCO2均随观察时间的延长而降低(P＜0.05).观察组治疗有效率为87.5％,显著高于对照组的70.0％ (P ＜0.05).治疗5d后两组患儿血清CK-MB水平均较前降低(P＜0.05),且观察组明显低于对照组(P＜0.05).结论 猪肺磷脂注射液气管内给药联合NCPAP可以显著降低呼吸衰竭早产儿CK-MB的含量,提高治疗有效率,起到很好的呼吸循环支持作用.