缬沙坦大鼠在体肠吸收动力学

通过大鼠在体单向肠灌流模型(SPIP),采用反相高效液相色谱法测定大鼠肠液中缬沙坦的浓度,研究缬沙坦的肠吸收动力学与P-糖蛋白(P-gp)和有机阴离子转运多肽(OATP)对缬沙坦肠吸收的影响。结果表明,缬沙坦为全肠段吸收,吸收速率与灌流液的pH和肠段部位有关,吸收速率按十二指肠、空肠、结肠和回肠顺序下降。缬沙坦在十二指肠的非线性吸收动力学参数为Ka=0.328 h-1;Vm=72.652μmol/(L.h);Km=10.968μmol/L;Vms=69.115μmol/(L.h);Kms=0μmol/L。空肠、结肠和回肠的吸收速率常数分别为(0.595±0.091),(0.586±0.153)和(0.551±0.030)h-1。与原药组相比,含P-gp抑制剂药物组Papp显著增加,含OATP抑制剂药物组Papp显著减少(P<0.05)。缬沙坦的肠吸收机制为主动转运-被动扩散混合吸收,符合非线性动力学过程。     

蟾毒灵胃肠道吸收动力学研究

目的 :研究蟾毒灵在大鼠胃、肠以及各肠段吸收动力学特征及吸收机制,为蟾毒灵的进一步开发提供依据。方法 :应用大鼠在体灌流技术,研究蟾毒灵大鼠胃肠道的吸收特征,以高效液相色谱法测定蟾毒灵的浓度。结果:蟾毒灵不同质量浓度(10.0,20.0,30.0μg·m L-1)在胃灌流3 h均能较好地吸收,累积吸收率均为90%左右,且与药物的浓度无关;在小肠全肠段的吸收表现为一级动力学特征,三种浓度吸收速率常数分别0.017,0.017,0.019/cm·h-1;蟾毒灵在各肠段均能吸收均呈一级动力学模式,十二指肠、空肠、回肠和结肠的吸收速率常数依次为0.024,0.027,0.022,0.021/cm·h-1。结论 :蟾毒灵在胃、全肠道及全肠各段均能吸收;吸收呈一级动力学模式,吸收机制为被动扩散。     

水飞蓟宾磷脂复合物大鼠肠吸收特性

目的:考察水飞蓟宾磷脂复合物在大鼠全小肠段及各分肠段的吸收。方法:运用大鼠在体肠灌流实验,采用高效液相色谱法测定肠灌流液中药物和酚红的浓度,以吸收百分率和肠壁通透系数为指标,考察水飞蓟宾磷脂复合物的肠吸收特性和肠壁通透性。结果:水飞蓟宾磷脂复合物在小肠中的吸收呈一级动力学特征,6 h时在肠道中约有70%被吸收,吸收速率常数Ka值为(0.193±0.012)h-1;分肠段实验中,各肠段(十二指肠、空肠、回肠、结肠)的吸收百分率和肠壁通透系数均无显著性差异(P>0.05)。结论:水飞蓟宾磷脂复合物在全肠道均有吸收。     

药物AB0315大鼠在体肠吸收中的动力学研究

目的研究药物AB0315在大鼠各肠段吸收的药代动力学特征。方法采用大鼠在体肠段灌流实验装置,利用高效液相色谱法和紫外分光光度法分别测定肠循环液中药物AB0315和酚红的含量。结果药物AB0315在十二指肠、空肠、回肠、结肠的吸收速率常数分别为0．7902,0．6253、0．6812,0．8324h^-1;在不同药物浓度40、80、250μg／mL小肠的吸收速率常数分别为0．5754,0．7191、0．8455h^-1;在不同pH值（4．0、6．5、7．4）时的吸收速率常数分别为0．7422、0．6127、0．5628h^-1。结论药物AB0315在大鼠小肠全肠段均有吸收,并且药物的吸收呈一级动力学,吸收机制为被动转运。     

四妙勇安汤中绿原酸在大鼠肠的吸收动力学研究

目的：考察四妙勇安汤中绿原酸在大鼠肠的吸收动力学特征。方法采用大鼠在体肠灌流模型,结合高效液相色谱法和紫外分光光度法分别测定绿原酸和酚红的质量浓度。结果绿原酸在十二指肠、回肠、空肠的吸收速率常数分别为0.0816、0.0912、0.0748 h-1,回肠与十二指肠、空肠比较,差异均有统计学意义(P<0.01);绿原酸吸收动力学方程为Y=-0.0886X+2.8993(r=0.9932),吸收速率常数为0．0886 h-1。结论绿原酸在回肠段的吸收优于十二指肠段和空肠段,药物吸收呈一级动力学过程。     

阿魏酸在大鼠体内肠吸收动力学的研究

目的研究阿魏酸在大鼠各肠各段的吸收动力学特征。方法采用大鼠在体肠回流实验装置,采用UV法和HPLC法分别测定肠循环液中酚红和阿魏酸的量。结果阿魏酸在大鼠小肠各段的吸收速率常数(ka)于阿魏酸不同质量浓度(20、50、100、200μg/mL)时分别为0.433 4、0.469 7、0.452 1、0.430 2-h 1;不同pH值7.8、6.8、5.4时分别为0.254 1、0.602 1、1.200 6-h 1;在不同肠段十二指肠、空肠、回肠、结肠时分别为0.151 2、0.178 4、0.168 7、0.066 9 h-1。结论药物质量浓度对ka无影响;在pH值为5.4~7.8,随药物溶液pH值的减小,药物ka显著增加;药物在十二指肠、空肠和回肠的吸收较好,在结肠的吸收较差;阿魏酸在肠道的吸收呈一级动力学过程,吸收机制为被动扩散。     

A771726在大鼠体内的药代动力学

目的研究A771726在大鼠体内的药代动力学过程。方法单剂量口服给药3个剂量的A771726,根据大鼠体内血药浓度经时过程,计算相应的药代动力学参数。结果A771726(3、6、12mg/kg)的血药经时过程均符合一级吸收的一房室模型,其主要药动学参数T1/2Ka(h)3.91±3.43、5.63±2.07、6.73±1.67;T1/2Ke(h)17.45±10.79、9.68±4.65、7.63±1.39;AUC(0~tn)(mg/L.h-1)163.83±17.88、447.88±148.60、843.72±175.41;Cmax(mg/L)7.05±1.17、24.00±1.87、39.93±3.90;Tmax(h)8.00±0.00、6.67±2.06、8.00±0.00;MRT(0~tn)(h)19.87±4.25、19.54±1.11、19.29±2.47。结论单剂量口服A7717263个剂量组的药物代谢均成线性关系,其血药浓度-时间曲线符合一级吸收的一房室模型。     

喷雾干燥乳剂提高一氧化氮供体药物ZLR-8大鼠在体肠吸收的研究

目的： 考察难溶性一氧化氮供体药物ZLR-8大鼠在体肠吸收特征及喷雾干燥乳剂对ZLR-8肠吸收的促进作用。方法： 采用大鼠在体小肠回流装置,以UV法和HPLC法分别测定酚红和ZLR-8的含量,计算ZLR-8在各肠段的吸收速率常数,考察ZLR-8浓度、肠循环液pH对肠吸收的影响,并对ZLR-8混悬液与ZLR-8喷雾干燥乳剂的肠吸收进行比较。结果： 以喷雾干燥乳剂给药,大鼠十二指肠﹑空肠﹑回肠﹑结肠1 h后对ZLR-8的吸收百分率分别为(23.54±1.40)%,(15.95±0.09)%,(12.30±0.74)%,(3.98±0.12)%,吸收速率常数分别为（0.248 6±0.046 0）,（0.143 7±0.036 0）,（0.069 2±0.001 3）,（0.020 8±0.000 4） h^-1,各肠段吸收特性有极显著性差异。ZLR-8浓度对吸收速率常数无显著影响,但吸收量与浓度线性相关;肠循环液pH显著影响肠吸收,ZLR-8在pH 5.4～7.4时有较好吸收;与混悬液相比,喷雾干燥乳剂极显著性增加大鼠肠吸收。结论： ZLR-8混悬液仅在小肠有微弱吸收,在其他肠段无明显吸收;喷雾干燥乳剂在各肠段均有明显吸收,吸收机制为被动扩散,极显著性地提高了ZLR-8的肠吸收。     

阿西美辛固体分散体大鼠在体肠道吸收动力学的研究

目的：考察阿西美辛固体分散体在大鼠不同肠段的吸收动力学特征及不同的药物浓度的影响。并与阿西美辛混悬液进行比较。方法：采用大鼠在体肠吸收实验方法。结果：阿西美辛固体分散体在十二指肠、回肠的吸收量分别为0．9294，0．5043cm^2／h。不同药物浓度：0．05，0．1，0．5，1．0mg／ml在回肠的吸收速率常数分别为0．4798，0．5025，0．5570，0．6306cm^2／h。结论：阿西美辛固体分散体比阿西美辛混悬液在肠道中的吸收量大；药物浓度对吸收速率常数无影响；吸收机制为被动扩散。     

A771726在大鼠体内肝肠循环的研究

目的 研究A771726在大鼠体内肝肠循环情况.方法 运用配对大鼠肝肠循环模型研究A771726在大鼠体内从胆汁重吸收的药动学过程,采用HPLC法测定血浆中A771726浓度,药动学参数用DAS软件统计矩法计算.结果 配对大鼠肝肠循环模型表明,胆汁供体大鼠和胆汁受体大鼠的AUC分别为(1352.85±184.51)mg/(L·h)、(314.94 ± 21.15)mg/(L ·h).结论 A771726静脉注射后存在肝肠循环现象,约有静脉注射给药量的23.8%进入肝肠循环.     

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…