格列吡嗪胶囊人体药动学的研究

目的研究格列吡嗪胶囊人体药物代谢动力学及相对生物利用度。方法用I-IPLC法测定10例受试者单剂量交叉口服5.0 mg格列吡嗪胶囊和片剂后的血药浓度,MC-RKP药动学程序拟合,得药动学参数,计算胶囊剂的相对生物利用度(F)。结果胶囊剂的Cmax为(456±60)ng/mL、Tmax为(2.95±0.6)h、AUC为(2 335±180)ng/(mL.h)。以上参数经双单侧t检验等统计学分析,与片剂比无显著差异。F值为(103±4)%。结论格列吡嗪(2.95±0.6)h血药浓度达高峰,峰浓度为(456±60)ng/mL,且胶囊与片剂为生物等效制剂。     

丹参注射液对格列喹酮在糖尿病大鼠体内药物代谢动力学参数和肠吸收特性的影响

目的 考察丹参注射液对格列喹酮在糖尿病大鼠体内药物代谢动力学参数的影响,为两药的临床合用提供依据。方法 链脲佐菌素腹腔注射建立糖尿病大鼠模型,考察丹参注射液对格列喹酮药物代谢动力学参数的影响;建立原位在体肠循环模型,研究丹参注射液对格列喹酮肠吸收特性的影响。结果 糖尿病大鼠的药物代谢动力学研究结果表明,两药合用能够显著缩短格列喹酮的达峰时间,增加最大药物浓度、药时曲线下面积,并且可以显著减少清除率。肠吸收特性实验结果显示,丹参注射液可以显著增加格列喹酮在糖尿病大鼠体内吸收速率和表观渗透系数。结论 丹参注射液和格列喹酮合用可以显著提高糖尿病大鼠格列喹酮的血药浓度和生物利用度,其原因可能与丹参注射液促进格列喹酮的小肠吸收相关。     

雷公藤内酯醇联用甘草次酸的药代动力学研究

目的 探讨甘草次酸对雷公藤内酯醇在大鼠体内的药代动力学行为的影响. 方法 将SD大鼠随机分为雷公藤内酯醇单独给药组和雷公藤内酯醇与甘草次酸联合给药组,分别通过尾静脉注射雷公藤内酯醇0.2 mg/kg,采用液相色谱-质谱法(LC-MS),选择离子检测(SIM)的方式测定2组大鼠不同时间血浆中的雷公藤内酯醇浓度,比较2组在大鼠体内的药代动力学行为. 结果 在0.2～250 ng/mL质量浓度范围内,血浆中雷公藤内酯醇线性良好.定量下限为0.2 ng/mL,日内和日间精密度RSD均<12.0％,准确度为90％～105％,绝对回收率>80％,基质效应>90％,血浆样品的稳定性良好.药代动力学数据显示,联合给药组的最大血药浓度(cmax)、消除半衰期(t1/2)、平均滞留时间(MRT0～180 min)、血药浓度|时间曲线下面积(AUC0～180 min)分别是单独给药组的0.75,2.51,1.15及1.39倍,其中t1/2、MRT0～180 min在2组间的差别有统计学意义(P<0.05). 结论 甘草次酸与雷公藤内酯醇联用可降低雷公藤内酯醇的峰浓度,延长其体内滞留时间,从而提高其大鼠体内的生物利用度;该测定方法简便、效率高、重复性好,符合生物样品分析的基本要求.     

HPLC-MS/MS法测定依卡倍特钠原料药中潜在遗传毒性杂质

为了定量测定依卡倍特钠中潜在遗传毒性杂质依卡倍特磺酸乙酯(杂质Ⅰ),参考文献方法合成依卡倍特磺酸乙酯。采用高分辨质谱、结合二级质谱与核磁共振确定其相对分子质量及化学结构。采用Thermo C₁₈色谱柱,以5 mmol/L乙酸铵溶液(甲酸调pH至3.0)为流动相A;乙腈为流动相B,按照梯度:0 min 50%B,4 min 50%B,12 min 80%B,16 min 80%B,16.1 min 50%B,20 min 50%B进行洗脱,柱温40 ℃;采用电喷雾负离子化-MS/MS选择反应监测。杂质Ⅰ的线性质量浓度范围为4~150 ng/mL,且线性关系良好(r=0.999);最低定量限为4 ng/mL;杂质Ⅰ的进样精密度、重复性和加标回收率良好,耐用性良好。方法操作简便,灵敏度高,可用于依卡倍特钠原料药中潜在遗传毒性杂质依卡倍特磺酸乙酯的含量测定。     

HPLC法同时测定鲜鱼腥草不同部位8个活性成分的含量

目的:同时测定鲜鱼腥草不同药用部位8个活性成分的含量。方法:Alltima C18柱(7.5 mm×4.6 mm,5μm),流动相:0.2%的冰乙酸溶液(A),乙腈(B),梯度洗脱:0~20 min,5%~20%B;20~40 min,20%~20.5%B;40~50 min,20.5%~35%B;50~90 min,35%~90%B;流速:0.6 mL/min;检测波长:280 nm。结果:表明不同药用部位含量不同。结论:该法简便、准确、分离效果好,适用于鱼腥草的质量控制。     

抗HIV化学成分DB02在大鼠体内的初步药代动力学研究

目的建立大鼠血浆中DB02的高效液相色谱质谱联用（HPLC-MS/MS）检测方法,并进行DB02的大鼠尾静脉注射给药药代动力学研究。方法6只Sprague Dawley（SD）大鼠,雌雄各半,尾静脉注射DB02增溶溶液1.004mg/kg·bw,分别于不同时间点眼底静脉丛取血,HPLC-MS/MS测定各时间点大鼠血药浓度,应用DAS2.0计算药代参数。结果所建立的检测方法在4.60~930ng/mL浓度范围内,线性关系良好,定量下限为4.60ng/mL（S/N≥10）,对13.6,123,923ng/mL 3个浓度的DB02大鼠血浆质控样品进行回收率、精密度与准确度考察,各浓度回收率均在90%以上,日内与日间精密度均小于15%,准确度为93.34%~102.51%,符合《药物非临床药代动力学研究技术指导原则》要求。大鼠尾静脉注射DB02后药代参数如下：C max=（513±69）μg/L;t 1/2=（33.4±5.3）min;AUC （0-t）=（8.15±0.06）mg/L*min。结论实验所建立的HPLC-MS/MS分析方法简单、快速、准确,能够满足DB02在大鼠体内的药代动力学的研究要求。按照1.004mg/kg单剂量单次静脉给药后,DB02在大鼠体内的血药浓度－时间曲线呈一房室模型。     

HPLC法同时测定半枝莲中黄酮和生物碱类成分

目的 建立同时测定半枝莲饮片中木犀草素、芹菜素、汉黄芩素、半枝莲生物碱A和半枝莲生物碱B的HPLC法。方法 采用高效液相色谱法,色谱柱为Phenomenon C₁₈柱(250 mm×4.60 mm,5 μm),以乙腈-水溶液为流动相,梯度洗脱;流速为1.0 mL/min,柱温为30 ℃;木犀草素、芹菜素检测波长为355 nm,汉黄芩素、半枝莲生物碱A和生物碱B检测波长为264 nm。结果 木犀草素、芹菜素、汉黄芩素、半枝莲生物碱A和生物碱B分别在0.0374~2.40 μg、0.0312~2.00 μg、0.0312~2.00 μg、0.0062~0.40 μg和0.0062~0.40 μg内线性关系良好。精密度,重复性及加样回收均符合要求。结论 此方法快速简便,重现性好,可用于半枝莲饮片的质量控制。     

枳壳和枳实化学成分的HPLC-ESI-MS分析

目的分析比较枳壳、枳实的化学成分。方法采用HPLC-ESI-MS法,SymmetryShieldTMRP18色谱柱(150mm×3.9mm,5μm)(Waters,Milford,MA,USA)。流动相:A为0.6%醋酸水溶液,pH=2.5;B为甲醇。采用梯度洗脱:20%~40%B(0~48min),40%B(48~54min),40%~55%B(54~60min),55%~95%B(60~75min),95%B(75~85min),95%~20%B(85~90min)。体积流量:0.7mL/min。温度为室温,检测波长为283nm。Surveg质谱检测器。结果鉴定了柚皮苷、柚皮苷元、新橙皮苷、橙皮苷、辛弗林等成分,并测定了它们在枳壳、枳实中的含量。枳壳、枳实药材的主要化学成分种类相同,但含量不同。结论HPLC-ESI-MS法可用于枳壳和枳实的研究。     

格列吡嗪胶囊人体药动学及相对生物利用度的研究

目的研究格列吡嗪胶囊人体药物代谢动力学及相对生物利用度.方法用HPLC法测定10名受试者单剂量交叉口服5mg格列吡嗪胶囊和片剂后的血药浓度,MC-PKP药动学程序拟合,得药动学参数,计算胶囊剂的相对生物利用度(F).结果胶囊剂的Cmax为(456±60)ng/ml、Tmax为(2.9 5±0.6)h、AUC为(2335±180)h*ng/ml.以上参数经双单侧t检验等统计分析,与片剂比无显著差异.F值为(103±4)%.结论格列吡嗪(2.95±0.6)h血药浓度达高峰,峰浓度为(456±60 )ng/ml.且胶囊与片剂为生物等效制剂.     

UPLC-MS/MS同时测定大鼠血浆中9种重楼皂苷类成分及其药代动力学研究

目的:建立UPLC-MS/MS同时测定大鼠血浆中9种皂苷类化合物的分析方法,并研究重楼中9种皂苷类成分在大鼠体内药代动力学参数。方法:血浆样品以乙腈沉淀蛋白,采用UPLC-MS/MS以多反应离子监测(MRM)模式,电喷雾离子源(ESI)正、负离子检测;流动相A为0.1%甲酸水溶液,B为0.1%甲酸乙腈溶液;洗脱梯度:0→1 min,5%B→52%B;1→6 min,52%B→56%B;6→7 min;56%B→95%B;7→7.5 min,95%B→95%B;7.5→9min,95%B→5%B;9→10 min,5%B→5%B。建立血浆中重楼皂苷Ⅰ、重楼皂苷Ⅱ、重楼皂苷Ⅲ、重楼皂苷Ⅴ、重楼皂苷Ⅵ、重楼皂苷Ⅶ、重楼皂苷H、纤细薯蓣皂苷和重楼皂苷S的检测方法;将重楼提取物采用尾静脉注射的方式给药,分别在给药后0、0.25、0.5、1、2、4、8、10、24 h眼眶取血,测量不同时间点血浆中的各成分含量,并计算尾静脉注射后药代动力学参数。结果:方法学考察结果显示,该检测方法在大鼠血浆中9种化合物中的线性关系良好(r2>0.99),线性范围适宜(1~260 ng/m L),日内精密度和日间精密度的RSD值均小于15%,提取回收率在85%~110%之间。结论:方法学验证表明,该方法简单、快速、灵敏,重复性好,可以用于9种皂苷类成分在大鼠血浆中的含量测定和药代动力学研究。     

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…     

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.     

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.     

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.     

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.     

Survey and practice of reporting quality of randomized controlled clinical trials on traditional Chinese medicine

Evidence obtained from randomized controlled trials （RCTs） has been generally accepted as the gold standard in the evaluation of clinical effectiveness. Readers need to understand the trial design, implementation, results, analysis and interpretation, so as to fully Jnderstand the results of RCTs. Thus, the investigators of RCTs have to report these items in a complete, accurate and clear manner. Since 1998, we have conducted several evaluations on the reporting quality of RCTs published in Chinese journals on traditional Chinese medicine （TCM） and results have shown that there is an urgent need for higher quality RCTs on TCM.     

TCM Treatment of Ankylosing Spondylitis by Tonifying the Kidney and Strengthening the Governor Vessel

Ankylosing spondylitis is a chronic and progressive disorder with inflammation mainly involving the central axis joints. It mainly affects the cervical spine and the lumbosacral area, with the pathogenesis closely related to the kidney and the Governor Vessel (GV). TCM holds that the syndrome is deficiency in origin and excess in superficiality, which is due to insufficiency of the kidney, deficiency of GV, and blocking of the channels with the invasion of exogenous evil, leading to poor circulation of qi and blood and malnutrition of the bones, muscles and joints. The TCM method of tonifying the kidney and strengthening GV to regulate circulation of qi and blood and check the arthralgia pain should be adopted, with the Kidney-Tonifying and GV Strengthening Decoction (益肾强督汤) prescribed.     

IMPROVING P-gp EXPRESSION IN HUMAN MONONUCLEAR CELLS IN VITRO TRANSFECTED BY MULTIDRUG RESISTANCE-1 mRNA

CHEMOTHERAPY playsa greatrolein the treat- ment of malignanttumors,especiallyingynecolo- gicalones.But inanticancerchemotherapy,leuko-cytopeniaisfrequentlytheprimarydose-limitingsideeffect factor.Moreover,cancersarefrequentlychemoresistantbe-causeof overexpressionof P-glycoprotein(P-gp), which isencodedby multidrugresistancegene (MDR1 ) and detectableinup to50% ofhuman cancersand renderscellsresistancetoanticancerdrugs.The safetyand potentialtherapeuticbenefitof mdr1 gene transferredto h…