牛磺酸在大鼠体内的药代动力学

目的:建立牛磺酸(TAU)在血浆和组织中HPLC的测定方法,进行TAU在大鼠体内的药代动力学研究.方法:Wistar大鼠在清醒状态下以60 mg/kg尾静脉注射TAU,分别于给药前和给药后1、3、5、10、15、20、30、45 min,l、1.5、2h,从內眦静脉取血0.5mL,分离血浆后,以乙腈沉淀蛋白,2,4-二硝基氟苯(DNFB)进行柱前衍生化处理后,采用RP-HPLC法,以A:乙酸钠溶液(pH7.0),B:乙腈-水(40∶60,v/v)为二元流动相,经Venusil C18(250 mm×4.6 mm,5μm)色谱柱分离,紫外检测器于波长360 nm处测定血浆中TAU含量,根据测定结果绘制TAU血药浓度-时间曲线并计算其药代动力学参数.结果:TAU以40 mg/kg、80 mg/kg、160 mg/kg尾静脉注射给药后,血中能迅速检测到TAU,其在大鼠体内药时过程符合非线性动力学,在房室模型的拟合上,符合一房室模型,其药代动力学参数T1/2分别为20.61、37.36和77.55 min,C0分别为317.28、477.63和818.02μg/mL,AUC(0-t)分别为10 132.0、18 305.5和59 508.6μg/(mL· min);3个剂量之间T1/2相比有统计学差异(P＜0.01),随剂量增加而延长,AUC(0-1)明显随剂量增加而增大,并且与剂量不成比例;统计矩参数MRT(0-t)分别为28.579、42.549和49.701 min.结论:建立了HPLC法测定大鼠血浆中TAU的方法,能满足研究药物在大鼠体内的药代动力学过程,其动力学行为符合一房室非线性动力学模型.     

Study on Pharmacokinetic Properties of Curcumin Derivative FM0807 in Mice under Different Drug Administration Manners

目的 研究姜黄素衍生物FM0807在不同给药方式的小鼠体内药代动力学特征. 方法 用HPLC法测定FM0807经静脉注射、灌胃给药后的小鼠血浆中FM0807及其代谢产物姜黄素的浓度,计算药代动力学参数. 结果 姜黄素在小鼠体内的代谢过程符合二室开放模型;静脉给药后的药代动力学参数为t1/2β 13.58 min、AUC 620.66 μg/(mL/min)、Vd 2.59 L/kg、Cmax 62.11μg/mL,灌胃给药后t1/2β 79.86 min、AUC 59.81 μg/(mL/min)、Vd 317.35 L/kg、Cmax 0.50 μg/mL. 结论 FM0807静脉给药迅速代谢为姜黄素,维持有效血药浓度50 min,FM0807灌胃后,姜黄素药-时曲线呈双峰,可能存在肝肠循环.     

甲巯咪唑大鼠经皮给药的药代动力学

目的:研究甲巯咪唑在大鼠体内经皮吸收的药代动力学,并与口服吸收动力学进行比较.方法:采用HPLC法测定大鼠口服(2 mg/kg)或经皮(1,2,4 mg/kg)给药后血清和甲状腺组织中的甲巯咪唑浓度.色谱柱为Lichrospher C18柱,流动相为甲醇-水(10:90),流速1.0 min,柱温30℃,检测波长UV 254 nm.结果:口服或经皮(2 mg/kg)给药后,甲巯咪唑的tmax分别为1.5 h和2.5 h,cmax分别为1 716.6和817.2ng/mL,AUC分别为4 606.2和3 739.6 ng·h/mL,t1/2分别为2.64 h和2.70 h,甲状腺组织中的药物浓度分别于给药后2 h和1 h达到峰值,其峰浓度分别为307.7和320.9 ng/50 mg.经皮给予高、中和低3个剂量甲巯咪唑后,其AUC与剂量呈现线性相关性.结论:甲巯咪唑口服给药的血药浓度明显高于经皮给药的血药浓度,但甲状腺组织中的药物浓度无显著性差异,提示经皮给药的全身不良反应小于口服给药.     

硝苯吡啶在家兔体内的时辰药代动力学

目的:观察硝苯吡啶(NF)在家兔体内不同给药时间药代动力学特征。方法:用HPLC法测定不同时间单剂量给药后NF在家兔体内药代动力学。结果:NF在8:00给药AUC,tmax,Cmax分别为974.69μg/(L·h),0.91h,162.15μg/L。在20:00给药分别为536.29μg/(L·h),1.35h,93.61μg/L。2个时间给药的药动学参数差异有统计学意义(P<0.01)。家兔体内NF的药代动力学规律均符合血管外给药一级吸收单室模型,并呈现明显的时间依赖性变化。结论:清晨给药可提高NF的生物利用度。     

福多司坦片在健康志愿者中的药代动力学研究

目的:研究福多司坦的人体药代动力学。方法:36名健康受试者随机分为600,400,200 mg 3个剂量组,每组12人,口服福多司坦片600,400,200 mg后,用高效液相色谱-荧光检测法测定血浆中福多司坦浓度。结果:单次口服福多司坦高、中、低剂量组的cmax分别为(22.44±7.61),(12.91±2.93),(6.53±1.61)μg/mL;tmax分别为(0.52±0.37),(0.44±0.15),(0.40±0.21)h。中剂量组多次口服福多司坦后所测cmax和tmax分别为(13.64±4.39)μg/mL(、0.55±0.50)h,平均稳态血药浓度为(3.67±0.95)μg/mL。低剂量组饮食后口服福多司坦后所测cmax和tmax分别为(3.37±0.68)μg/mL、(1.40±0.78)h。结论:健康受试者单次口服高、中、低3个剂量的福多司坦后,药代动力学参数tmax、Kt、1/2、MRT相近,cmax、AUC0-τ与剂量呈依赖性。对3个剂量的AUC0-τ进行方差分析,结果表明消除体重因素后,男性和女性健康受试者的AUC0-τ之间没有显著性差异(P>0.05),多次给药后福多司坦的人体药动学参数与单次给药的药代动力学参数基本一致,饮食组与空腹组的cmax及tmax差异有极显著性意义(P<0.01)。     

对乙酰氨基酚在大鼠体内药动学研究

目的应用反相高效液相色谱法（RP-HPLC）测定大鼠血浆中对乙酰氨基酚浓度,研究单剂量口服不同剂量对乙酰氨基酚片在大鼠体内的药代动力学。方法3组SD大鼠分别按体重单剂量口服对乙酰氨基酚片300 mg/kg、600 mg/kg、1 200 mg/kg后,采用RP-HPLC测定血浆中药物的浓度,绘制血药浓度-时间曲线,计算其药代动力学参数。结果3个剂量组的对乙酰氨基酚药-时曲线均符合口服吸收的一级动力学二室模型,主要药代动力学参数：Tmax分别为（0.78±0.17）h、（1.07±0.12）h、（1.19±0.12）h;Cmax分别为（158.99±26.08）μg/ml、（226.26±20.38）μg/ml、（402.95±86.46）μg/ml;T1/2kα分别为（0.24±0.09）h、（0.39±0.11）h、（0.43±0.14）h;T1/2ke分别为（3.78±0.33）h、（3.66±0.32）h、（4.33±0.47）h;AUC0→24分别为（718.71±143.03）μg·h^-1·ml^-1（1 578.53±246.76）μg·h^-1·ml^-1（3 734.67±665.58）μg·h^-1·ml^-1AUC0→∞分别为（757.16±155.29）μg·h^-1·ml^-1（1 594.61±247.11）μg·h^-1·ml^-1（3 847.99±692.03）μg·h^-1·ml^-1结论所建立RP-HPLC法能够准确地测定对乙酰氨基酚血药浓度,能满足药代动力学的研究需求;低剂量组和中剂量组的药代动力学过程基本相似,但高剂量组则与上述两组则有所不同,这可能与其剂量过高有关。     

HPLC法测定清热解毒颗粒中大黄素在大鼠体内的药代动力学

目的研究清热解毒颗粒中大黄素在大鼠体内的药代动力学。方法 20只成年大鼠,随机分为0.1g/kg和0.2g/kg清热解毒颗粒组,每组10只,采用HPLC法测定血药浓度,计算药代动力学参数。结果 0.1g/kg组与0.2g/kg组的主要药代动力学参数分别为：Cmax（μg/mL）为（10.14±0.39）与（11.42±0.64）,tmax（h）为（4.08±0.37）与（4.11±0.45）,AΜCto（μg·h·/mL）为（4307±142）与（4632±167）,AΜC0∞（μg·h·/mL）为（4784±183）与（4836±201）。结论 HPLC法适用于清热解毒颗粒中大黄素的药代动力学研究。     

富马酸替诺福韦二吡呋酯胶囊在中国人体内的药代动力学

研究富马酸替诺福韦二吡呋酯胶囊在中国人体内的药代动力学特征。12名健康受试者依次进行低剂量(300mg)单、多次给药;高(600 mg)剂量单次给药和低剂量饮食影响单次给药的药代动力学试验,计算药代动力学参数。受试者单次口服300 mg和600 mg受试制剂后,替诺福韦的cmax分别为(305.4±96.4)和(590.0±149.6)ng/mL,AUC0-72 h分别为(2 396±489)和(4 465±1 042)ng.h/mL,t1/2分别为(19.9±2.4)和(21.9±3.0)h。结果显示替诺福韦在300～600 mg剂量范围内呈现线性药代动力学特征,体内过程不受性别差异的影响。与空腹给药相比,高脂餐后给药的tmax延后1.6 h,AUC0-72 h提高约32%。多次给药达稳态后,替诺福韦的稳态血药浓度波动度为2.7±0.6,累积常数Rcmax为1.3±0.3,RAUC为1.7±0.4,在人体内的暴露量增加约70%。     

左旋和右旋奥硝唑在大鼠体内的药代动力学

目的:研究大鼠口服和静注左旋、右旋奥硝唑,比较两者药代动力学行为差异。方法:大鼠分别口服和静注左旋、右旋奥硝唑后,用HPLC法测定血浆中药物的浓度。色谱柱为Lichrospher C18柱,流动相为甲醇-0.4%HOAc(30∶70),流速0.8 mL/min,柱温40℃,紫外检测波长316 nm。结果:口服给药后,左旋、右旋奥硝唑的t1/2分别为2.49和3.42 h,AUC分别为168.21和207.19μg.h/mL,CL/F分别为0.11和0.09 L/h。静脉注射给药后,左旋、右旋奥硝唑的t1/2分别为2.19和3.23h,AUC分别为138.40和203.09μg.h/mL,CL分别为0.08和0.05 L/h。结论:左旋、右旋奥硝唑在大鼠体内的药代动力学行为存在一定的差异。     

HPLC-MS/MS法测定大鼠血浆中紫杉醇含量及其脂质体药代动力学研究

目的:建立一种测定大鼠血浆中紫杉醇浓度的高效液相色谱串联质谱（HPLC-MS/MS）分析方法,并研究其脂质体的药代动力学。方法:对6只SD大鼠静脉注射1 mg/kg的紫杉醇脂质体注射液,分别于给药后0、0.5、1、2、4、8、12、24、48 h自眼眶取血0.2 mL,C18反相色谱柱作为固定相,水（1 mmoL/L甲酸铵-0.05%甲酸）-甲醇作为流动相,ESI+扫描模式,MRM监测模式,药代动力学参数采用DAS 2.0软件进行计算。结果:紫杉醇在1～5 000 ng/mL范围内线性较好（R2 =0.999 7）,定量下限（LLOQ）为1 ng/mL,日内和日间精密度均低于10%,紫杉醇脂质体给药后血药浓度-时间曲线满足二室模型,主要药代动力学参数t1/2、Cmax、AUC0→t分别为（4.79±0.85）h、（49 785.12±1 618.45）μg/L、（38 753.08±6 144.66）μg/L·h。结论:本方法专属性和灵敏度高,结果可靠,能满足测定大鼠血浆中紫杉醇的定量需求。     

Acupuncture Treatment of Vomiting

CASE HISTORY A female patient, 46 years old, head of the foreign affairs department of a certain university in Beijing, paid her first visit on October 9, 2006, with the chief complaint of vomiting for one month. She got vomiting after meals in early September. Before that, she had discomfortable sensation in the stomach due to angry with others, but she didn't pay much attention. Later, it developed into vomiting after eating. After the vomiting, the discomfort would be relieved, but with slight hypodynamia. She was once diagnosed as having 'neurogenic vomiting'. Having taken some western and Chinese drugs, the above symptoms were a little bit improved, but she would have nausea upon eating and with regurgitation. Because of the fear for vomiting, she did not dare to have food intake, with body weight reduction of 6 kilos in one month.     

Qiu Baoguo''''s Experience in Treating Consumptive Syndromes after Radio-Chemotherapies

Radiotherapy and chemotherapy are the important modern medical therapies for malignant tumors,yet they can also bring about serious local and systemic toxic side reactions so to decrease the patient;'s life quality,manifested by a series of consumptive symptoms.Having engaged in the combined work of Chinese and western medicine for nearly 50 years,the research fellow Qiu Baoguo in Henan Provincial Academy of TCM has developed his unique views on the TCM study of consumptive syndromes.The author of this essay had once the fortune tO follow Dr.Qiu in clinic,and specially would like to introduce in the following Dr.Qiu's experience in treating consumptive syndromes after radio-chemotherapies for patients with malignant tumor.     

Insomnia Due to Deficiency of Both the Heart and Spleen Treated by Acupuncture-Moxibustion and Chinese Tuina

OBJECTIVE: To observe therapeutic effects of the comprehensive therapy of acupuncture-moxibustion and Chinese Tuina for treatment of insomnia due to deficiency of both the heart and spleen. METHODS: 92 cases were divided randomly into the treatment group (treated by acupuncture-moxibustion and Chinese Tuina) and the control group (treated by acupuncture-moxibustion). RESULTS: The therapeutic effect of the treatment group was obviously superior to that of the control group (the CHI2 test showed P < 0.01). CONCLUSIONS: The comprehensive therapy of acupuncture-moxibustion and Chinese Tuina can give marked therapeutic effects for treatment of insomnia due to deficiency of both the heart and spleen.     

Analysis of CK-19,PDX-1,Nestin,Ngn3 in different donor islet purity in rats

Objective: To investigate if there are the CK-19, PDX-1, Nestin, Ngn3 positive cells in the donor islets of different purity in rats. Methods: Thirty male adult SD rats were randomly divided into 3 groups. Islets were isolated using digestion by ductal injection of collagenase. Group Ⅰ (n=10): Separating cell preparations were not purified, Group Ⅱ(n=10): Islet sediment was purified with 25% Ficoll400 ,Group Ⅲ (n=10): Islet sediment was purified with 25% and 11% Ficoll-400. The levels of protein of CK-19, PDX-1, Nestin and Ngn3 were detected by immunohistochemistry and the mRNA of CK-19, PDX-1, Nestin, Ngn3 was amplified by RT-PCR. Results: After two different purification methods applied, three islet preparations of different purities were obtained. The difference of islet purity was significant among various groups (P＜0.05). Compared with group Ⅱ and group Ⅲ,the protein and mRNA of CK-19, PDX-1, Nestin,Ngn3 were both higher in group Ⅰ; group Ⅲ was poorly expressed. Conclusions: The three different islet purity donor islet have different CK-19, PDX-1, Nestin, Ngn3 positive cells within them, indicating that there are some islet stem cells in the purified donor islet.     

A preliminary screening study on the associated proteins in human psoriasis vulgaris by serum proteomics technologies

Objective：To investigate the optimum screening conditions of associated proteins in human psoriasis vulgaris by serum proteomics technique, and to screen the different expression proteins related with psoriasis vulgaris. Methods：Serum samples of peripheral blood were collected from newly diagnosed psoriasis vulgaris patients in the clinic, and 20 matched healthy persons. Serum albumin IgG was removed by filtering with ProteoExtract Albumin/IgG. After comparative proteomics analysis the different protein spots were identified using 2-DE and MS. Results ：Electrophoresis figures with high resolution and reproducibility were obtained. Three different expression proteins were found only in the serum from psoriasis vulgaris patients, while nine other different proteins expressing from healthy volunteers. Conclusion：The protein expression was different in the serum between the psoriasis vulgaris patients and healthy volunteers. It was hoped that we could find the biomarkers related to psoriasis vulgaris by using proteomics.     

A CASE OF HUGE GASTRIC DISOPYROBEZOAR

PYTOBEZOARS are common bezoars in gastrontestinal tract, commonly seen in stomach and mall intestine,1but huge disopyrobezoars are     

Acupuncture Treatment of Chest Bi Syndrome

CASE HISTORY A male,a retired officer of 61 years old,paid his first visit on May 12,2006.The patient stated that 2 weeks before he suddenly got paroxysmal precordial choking pain,with irregular attacks.Each attack would last several seconds to several minutes.The attack was accompanied with heavy oppressed sensation in the precordial region,palpitation,lassitude,and in severe cases,sweating,which was once diagnosed by a hospital as'coronary heart disease'.Recalling the case history,the patient said that several days before he got angry with others because of some affairs in work,and he was not so used to the life pattern since he had just retired from his busy working post.At usual times,he was quick tempered and peevish.In recent days,he had poor appetite,and loose stool.     

Instructions to Contributors

The English edition of Chinese Journal of Integrative Medicine is edited and published by the Chinese Journal of Integrated Traditional and Western Medicine Press.Original scientific papers of advanced clinical and experimental medicine in the field of complementary/alternative medicine or integrative medicine are expected.     

Development Is A High Level Inheritance for China Time-honored Brand Products

<正>As culture is the soul of a nation,the three books,"History of Chinese Philosophy,""History of Chinese Culture"and"History of Chinese Science and Technology"have demonstrated the superiority of our great Chinese culture,and its significant impact in the field of international culture.Both core value and practical value of the Chinese culture are very clear,reflected in the views of universe,nature,life,health,disease,and therapy and related considerations,concepts,and technical methods.