共查询到20条相似文献,搜索用时 62 毫秒
1.
目的 :比较国产与进口头孢泊肟酯片在正常人体内的药动学与相对生物利用度。方法 :2 4名男性健康志愿者随机交叉单次口服国产或进口头孢泊肟酯片 2 0 0mg后 ,采用反相高效液相色谱法测定血药浓度 ,用 3P97软件包计算两者的药动学参数与相对生物利用度。结果 :国产片和进口片口服吸收的药 时曲线符合一室模型。Tmax分别为 (2 .5±s0 .6 )h和 (2 .3± 0 .5 )h ,Cmax为 (3.5± 0 .6 )mg·L- 1和 (3.6± 0 .5 )mg·L- 1,AUC0 t分别为 (18± 3)mg·L- 1和 (18.0± 2 .8)mg·L- 1,AUC0 ∞ 分别为(19± 3)mg·L- 1和 (19± 3)mg·L- 1,T12 Ke分别为(2 .0± 0 .3)h和 (2 .2± 0 .4 )h。国产片相对于进口片的相对生物利用度为 (10 2± 15 ) %。经方差分析及双单侧t检验 ,各药动学参数无显著差异 (P >0 .0 5 )。结论 :国产片与进口片生物等效。 相似文献
2.
目的 :比较健康志愿者国产与进口美洛昔康片的人体药动学和相对生物利用度。方法 :采用单次给药 2周期交叉设计 ,HPLC法测定 12名健康男性志愿者口服 15mg美洛昔康后血药浓度 ,计算药动学参数和国产片的相对生物利用度。结果 :2种制剂的药时曲线符合一级吸收的一室开放模型。国产与进口片的药动学参数分别是AUC0 - 96 为 (6 7±s 14 )mg·h·L- 1和 (6 4± 15 )mg·h·L- 1;AUC0 -∞ 为 (73± 19)mg·h·L- 1和 (70± 18)mg·h·L- 1;Cmax为 (2 .3± 0 .5 )mg·L- 1和 (1.6± 0 .3)mg·L- 1;Tmax为 (2 .0± 1.6 )h和 (6± 3)h ;T12 ke为 (2 5± 6 )h和 (2 4± 5 )h ;MRT为 (4 0± 13)hand (39±8)h。方差分析表明两者AUC之间无显著差异 (P>0 .0 5 ) ,但两者的Cmax和Tmax之间有显著差异 (P<0 .0 5 )。结论 :国产片的释药速率比进口片快 ,其相对生物利用度为 (10 5± 13) %。 相似文献
3.
合用盐酸黄连素前后环孢素A的健康人体药动学研究 总被引:7,自引:0,他引:7
目的 :研究健康受试者合用盐酸黄连素 (Ber)前后环孢素A(CsA)的动力学过程 ,以分析两药相互作用发生的部位。方法 :6名健康男性志愿者在单剂口服CsA (6mg·kg-1)后开始连续服用Ber 13d(30 0mg·bid-1) ,然后再单剂口服CsA (6mg·kg-1) ,每次口服CsA后即按时采血 ,并用FPIA法测定全血CsA浓度 ,并计算出药动学参数。结果 :合用Ber前后CsA的主要药动学参数Ka 分别为 0 .91± 0 .30h-1和 1.0 9± 0 .35h-1;T1 2 β分别为 6.18± 0 .94h和6.86± 1.2 7h ;AUC0 -2 4 分别为 11.0± 1.6和 10 .6±1.6mg·h-1·L-1;CL(s)分别为 34.3± 6.7L·h-1和36.6± 9.3L·h-1;Tpeak均为 1.5± 0 .6h ;Cmax分别为1.8± 0 .4mg·L-1和 1.9± 0 .3mg·L-1。结论 :在健康志愿者合用Ber前后CsA的药动学参数没有显著差异 ,推测Ber对CsA的影响部位可能主要在肠道。 相似文献
4.
目的 :研究葡甘聚糖对大鼠口服荧光素钠药动学的影响。方法 :利用荧光素钠作为示踪药物 ,HPLC反相柱色谱分离原药 ,荧光高效液相法定量分析血清荧光素钠含量。结果 :大鼠灌胃荧光素钠溶液T12 α为 (5 .0± 0 .9)min ,T12 β为 (43± 9)min ,Tmax为 (7.5± 0 )min ,Cmax为 (192± 7)mg·L- 1,AUC为 (83± 17) μg·h- 1·L- 1。以 0 .4 %或 0 .8%的葡甘聚糖为制剂时T12 α分别为 (2 0± 6 )min和 (38± 13)min ,T12 β为 (6± 3)h和 (2 5± 12 )h ,Tmax为(19± 9)min和 (40± 16 )min ,Cmax为 (92 .3± 2 .0 )mg·L- 1和 (5 2± 3)mg·L- 1,AUC为 (6 14± 10 5 ) μg·h- 1·L- 1和 (30 1± 2 2 ) μg·h- 1·L- 1。结论 :葡甘聚糖能明显改变口服药物的药动学参数 ,如降低血药峰值浓度 ,提高AUC。 相似文献
5.
替诺昔康片人体生物等效性研究 总被引:1,自引:1,他引:1
目的 以Mobiflex片为参比药物 ,研究替诺昔康片的人体药代动力学和相对生物利用度 ,以判断两种制剂是否具有生物等效性。方法 2 4名健康志愿者随机分组交叉自身对照给药 ,每次服药后 2 4 0h内多点采血 ,HPLC法测定血清中药物浓度。结果 两制剂的血药浓度经时变化基本一致 ,替诺昔康片和Mobiflex片的主要药代动力学参数分别为 :T1/2Ke(6 9 6 8± 12 5 6 )h ,(6 8 75± 13 39)h ;Cmax(2 95±0 5 0 )mg·L-1,(2 82± 0 4 8)mg·L-1;AUC0~t(2 0 9 70±32 4 3)mg·L-1·h-1,(2 0 0 6 5± 18 5 7)mg·L-1·h-1;AUC0~∞(2 2 8 4 5± 36 0 7)mg·L-1 h-1,(2 18 11± 2 1 34)mg·L-1·h-1;Tmax(2 75± 1 0 7)h ,(2 75± 1 11)h ,经配对t检验差异均无显著性。替诺昔康片相对生物利用度为10 5 0 6 %± 16 6 1% (99 2 5 %~ 110 87% )。结论 替诺昔康片与Mobiflex片具有生物等效性 相似文献
6.
目的 :建立依托度酸的血药浓度测定方法 ,研究国产受试制剂与进口参比制剂在健康人体内的药动学特征及其生物等效性。方法 :2 0名健康男性志愿者多剂量交叉口服依托度酸缓释片受试制剂和参比制剂 ,采用HPLC法测定血浆中依托度酸的浓度 ,计算药动学参数和相对生物利用度 ,并对所得参数进行方差分析和双单侧t检验。结果 :依托度酸缓释片受试制剂及参比制剂的主要药动学参数为 :Cssmax分别为 (11.2± 3.7)mg·L-1和 (12 .0± 4 .4 )mg·L-1;Cssmin分别为 (4 .5± 2 .1)mg·L-1和 (4 .4± 1.6 )mg·L-1;稳态平均血药浓度Cav分别为 (5 .9± 2 .4 )mg·L-1和 (6 .2± 1.9)mg·L-1;血药浓度波动系数DF(% )分别为 (12 8.4± 6 7.4 ) %和 (131.2± 5 3.7) % ;Tssmax分别为 (2 .0± 1.5 )h和 (4 .0± 2 .7)h ;t1/ 2 分别为 (14 .1± 2 .1)h和 (13.4±2 .3)h ;稳态条件下AUCss0→ 2 4分别为 (14 1.± 5 7.2 )mg·L-1·h-1和 (14 6 .3± 4 4 .6 )mg·L-1·h-1;稳态条件下的相对生物利用度F(0→ 2 4) 为 (98.8± 32 .1) %。结论 :经统计学分析 ,两制剂具有生物等效性 相似文献
7.
缬沙坦3种制剂的健康人体生物等效性研究 总被引:6,自引:0,他引:6
目的 :研究缬沙坦 3种制剂的人体生物利用度和药动学特征。方法 :2 4名健康男性受试者采用三制剂三周期随机交叉试验设计 ,分别口服单剂量 80mg缬沙坦片剂 (被试制剂T 1)、胶囊 (被试制剂T 2 )和缬沙坦胶囊 (参比制剂R)。采用HPLC 荧光检测法测定血浆样品中的缬沙坦浓度。结果 :T 1,T 2与R的主要药动学参数分别为 :Tmax(2 .4±s 0 .8)h ,(2 .8± 0 .8)h和 (2 .2± 0 .5 )h ;Cmax(2 .2± 0 .8)mg·L- 1,(1.9± 1.0 )mg·L- 1和 (2 .0± 1.0 )mg·L- 1;AUC0 2 4 (12± 4 )mg·h·L- 1,(11± 4 )mg·h·L- 1和 (11± 5 )mg·h·L- 1;T12 β(6 .0± 1.1)h ,(5 .8± 1.0 )h和 (5 .9± 0 .9)h。相对生物利用度 :(117± 37) % (T 1)和 (10 4± 4 4) % (T 2 )。药动学参数经多因素方差分析显示周期间与制剂间差异均无显著意义 (P >0 .0 5 ) ,双单侧t检验表明接受T 1与R和T 2与R生物等效的假设 ,经计算 90 %置信区间均在规定值内。结论 :T 1,T 2与R 3种制剂生物等效 相似文献
8.
盐酸二甲双胍肠溶片的人体相对生物利用度 总被引:6,自引:0,他引:6
目的 :研究盐酸二甲双胍肠溶片在健康男性志愿者体内的相对生物利用度。方法 :2 0名健康志愿者交叉口服盐酸二甲双胍肠溶片和盐酸二甲双胍肠溶胶囊 ,采用HPLC法测定人血清中盐酸二甲双胍的浓度 ,使用NDST程序对各药动学参数进行方差分析和双单侧t检验。结果 :口服 10 0 0mg盐酸二甲双胍肠溶片和盐酸二甲双胍肠溶胶囊的cmax分别为 :(2 .6 1±0 .85 ) ,(2 .4 1± 0 .84 )mg L-1;tmax分别为 :(3.13± 0 .78) ,(3.4 8± 0 .95 )h ;T1/2 分别为 :(3.80± 0 .99) ,(3.2 9± 0 .5 4 )h ;AUC0→ 16分别为 :(13.95± 3.97) ,(12 .76± 4 .0 2 )mg·h·L-1;AUC0→∞ 分别为 :(14 .78± 3.97) ,(13.4 2± 4 .18)mg·h·L-1。统计学处理结果 ,两剂型的药动学参数间均无显著性差异 ,受试制剂的相对生物利用度为 (113.8± 2 5 9) %。结论 :2种制剂具有生物等效性 相似文献
9.
国产格列齐特片(Ⅱ)在健康人体内的药动学研究 总被引:2,自引:0,他引:2
目的 :研究国产格列齐特片 (Ⅱ )和进口片的药动学。方法 :10名健康男性受试者单剂量随机交叉口服格列齐特片(Ⅱ )受试制剂或参比制剂各 80mg ,采用HPLC法测定血药浓度 ,用 3P87程序对试验数据进行处理。结果 :受试制剂和参比制剂主要药动学参数 :cmax分别为 (5 .78± 1.90 ) ,(5 .93± 1.18)mg·L-1;tmax分别为 (5 .12± 1.6 0 ) ,(5 .2 2± 1.14 )h ;T1/ 2 分别为(11.19± 2 .6 7) ,(10 .94± 2 .6 3)h ;Ka分别为 (1.17± 0 .4 4 ) ,(1.18± 0 .4 3)h-1;Ke分别为 (0 .0 6 5 1± 0 .0 15 ) ,(0 .0 6 70± 0 .0 17)h-1;AUC0→∞ 分别为 (10 0 .85± 16 .87) ,(97.87± 17.81)mg·h·L-1;受试制剂的相对生物利用度为 (10 4 .5 1± 18.86 ) %。AUC经对数转换后的双单侧t检验结果表明无显著差别。结论 :两制剂具有生物等效性 相似文献
10.
罗红霉素缓释胶囊在家犬体内的药动学及相对生物利用度 总被引:16,自引:0,他引:16
目的评价罗红霉素缓释胶囊在家犬体内的药动学、相对生物利用度及体内外相关性。方法6条家犬随机交叉口服罗红霉素普通片和罗红霉素缓释胶囊 3 0 0mg后 ,利用HPLC法测定血药浓度并对其进行药动学和生物利用度研究。结果罗红霉素缓释胶囊和普通片的tmax分别为 (6 40±1 67)h和 (1 60± 0 5 5 )h ,cmax分别为 (6 5 2± 1 44)mg·L-1和 (1 5 5 1± 4 3 8)mg·L-1,AUC0 -52 分别为 (1 5 2 99± 3 3 5 2 )mg·h·L-1和 (1 70 86± 446 43 )mg·h·L-1,MRT0 -52 分别为 (2 0 42± 1 1 5 )h和 (1 3 0 3± 2 80 )h ,相对生物利用度为 90 76% ;其体内吸收与体外释药相关性显著 (r =0 9788)。结论罗红霉素缓释胶囊具有明显的缓释特征 相似文献
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13.
Clinical and in vitro investigations were carried out to test the efficacy of gut lavage, hemodialysis, and hemoperfusion in the treatment of poisoning with paraquat or diquat. In a patient suffering from diquat intoxication 130 times more diquat was removed by gut lavage 30 h after ingestion than was removed by complete aspiration of the gastric contents.Determination of in vitro clearances for paraquat and diquat by hemodialysis showed that, at serum concentrations of 1–2 ppm, such as are frequently encountered in poisoning in man, toxicologically relevant quantities of herbicide cannot be removed from the body. At a concentration of 20 ppm, on the other hand, hemodialysis proved to be effective, the clearance being 70 ml/min at a blood flow rate of 100 ml/min. The efficacy of hemoperfusion with coated activated charcoal was on the whole better. Especially at concentrations around 1–2 ppm, the clearance values for hemoperfusion were some 5–7 times higher than those for hemodialysis.In a patient suffering from paraquat poisoning, both hemodialysis as well as hemoperfusion were carried out. The in vitro results could be confirmed: At serum concentrations of paraquat less than 1 ppm no clearance could be obtained by hemodialysis while by hemoperfusion with activated charcoal quite high clearance values were measured and the serum level dropped down to zero.
Zusammenfassung Klinische Untersuchungen und Laboratoriumsversuche wurden durchgeführt, um die Wirksamkeit von Darmspülung, Hämodialyse und Hämoperfusion bei Paraquat- und Deiquat-Vergiftungen zu prüfen.Bei einem Patienten wurde 30 Std nach Deiquat-Aufnahme durch Darmspülung 130mal mehr Deiquat entfernt als durch vollständige Aspiration des Mageninhaltes. In vitro-Versuche ergaben, daß bei Blutserumkonzentrationen von 1–2 ppm, die bei Vergiftungen oft gemessen werden, durch Hämodialyse keine toxikologisch relevanten Paraquat- oder Deiquat-Mengen entfernt werden können. Dagegen erwies sich die Hämodialyse bei 20 ppm und einer Blutumlaufgeschwindigkeit von 100 ml/min mit einer Clearance von 70 ml/min als wirksam. Die Hämoperfusion mit beschicheter Aktivkohle war in diesen Versuchen aber eindeutig überlegen, denn insbesondere bei Konzentrationen um 1–2 ppm waren die Clearance-Werte 5–7mal höher als bei der Hämodialyse.Die in vitro-Ergebnisse wurden bei einem Patienten mit einer Paraquat-Vergiftung bestätigt: Bei Konzentrationen unter 1 ppm war die Hämodialyse wirkungslos, während durch Hämoperfusion relativ hohe Clearance-Werte erreicht wurden, so daß der Serumspiegel rasch unter die Nachweisgrenze abfiel.相似文献
14.
Petrikovics I McGuinn WD Sylvester D Yuzapavik P Jiang J Way JL Papahadjopoulos D Hong K Yin R Cheng TC DeFrank JJ 《Drug delivery》2000,7(2):83-89
This study describes a new approach for organophosphorous (OP) antidotal treatment by encapsulating an OP hydrolyzing enzyme, OPA anhydrolase (OPAA), within sterically stabilized liposomes. The recombinant OPAA enzyme was derived from Alteromonas strain JD6. It has broad substrate specificity to a wide range of OP compounds: DFP and the nerve agents, soman and sarin. Liposomes encapsulating OPAA (SL)* were made by mechanical dispersion method. Hydrolysis of DFP by (SL)* was measured by following an increase of fluoride ion concentration using a fluoride ion selective electrode. OPAA entrapped in the carrier liposomes rapidly hydrolyze DFP, with the rate of DFP hydrolysis directly proportional to the amount of (SL)* added to the solution. Liposomal carriers containing no enzyme did not hydrolyze DFP. The reaction was linear and the rate of hydrolysis was first order in the substrate. This enzyme carrier system serves as a biodegradable protective environment for the recombinant OP-metabolizing enzyme, OPAA, resulting in prolongation of enzymatic concentration in the body. These studies suggest that the protection of OP intoxication can be strikingly enhanced by adding OPAA encapsulated within (SL)* to pralidoxime and atropine. 相似文献
16.
《Critical reviews in toxicology》2013,43(5-6):327-369
AbstractThe uptake of metals from food and water sources by insects is thought to be additive. For a given metal, the proportions taken up from water and food will depend both on the bioavailable concentration of the metal associated with each source and the mechanism and rate by which the metal enters the insect. Attempts to correlate insect trace metal concentrations with the trophic level of insects should be made with a knowledge of the feeding relationships of the individual taxa concerned. Pathways for the uptake of essential metals, such as copper and zinc, exist at the cellular level, and other nonessential metals, such as cadmium, also appear to enter via these routes. Within cells, trace metals can be bound to proteins or stored in granules. The internal distribution of metals among body tissues is very heterogeneous, and distribution patterns tend to be both metal and taxon specific. Trace metals associated with insects can be both bound on the surface of their chitinous exoskeleton and incorporated into body tissues. The quantities of trace meals accumulated by an individual reflect the net balance between the rate of metal influx from both dissolved and particulate sources and the rate of metal efflux from the organism. The toxicity of metals has been demonstrated at all levels of biological organization: cell, tissue, individual, population, and community. Much of the literature pertaining to the toxic effects of metals on aquatic insects is based on laboratory observations and, as such, it is difficult to extrapolate the data to insects in nature. The few experimental studies in nature suggest that trace metal contaminants can affect both the distribution and the abundance of aquatic insects. Insects have a largely unexploited potential as biomonitors of metal contamination in nature. A better understanding of the physico-chemical and biological mechanisms mediating trace metal bioavailability and exchange will facilitate the development of general predictive models relating trace metal concentrations in insects to those in their environment. Such models will facilitate the use of insects as contaminant biomonitors. 相似文献
17.
Chang Min Kim Kun Ho Son Sung Hwan Kim Hyun Pyo Kim 《Archives of pharmacal research》1991,14(4):305-310
In order to find out the values of the steroid resources for the future use. the compositions and contents of steroidal sapogenins
from 13 domestic plants have been investigated. As a result,Dioscorea nipponica, D. quinqueloba andSmilax china were found to have large amount of diosgenin. And pennogenin inTrillium kamtschaticum andParis verticillata, yuccagenin inAllium fistulosum, hecogenin inAgave americana and neochlorogenin inSolanum nigum were appeared to be major steroidal sapogenins. 相似文献
18.
Alberto García-Lled Javier Gmez-Pavn Juan Gonzlez del Castillo Teresa Hernndez-Sampelayo Mari Cruz Martín-Delgado Francisco Javier Martín Snchez Manuel Martínez-Sells Jos María Molero García Santiago Moreno Guilln Fernando Rodríguez-Artalejo Julin Ruiz-Galiana Rafael Cantn Pilar De Lucas Ramos Alejandra García-Botella Emilio Bouza 《Rev Esp Quimioter》2022,35(2):115
The precocity and efficacy of the vaccines developed so far against COVID-19 has been the most significant and saving advance against the pandemic. The development of vaccines has not prevented, during the whole period of the pandemic, the constant search for therapeutic medicines, both among existing drugs with different indications and in the development of new drugs. The Scientific Committee of the COVID-19 of the Illustrious College of Physicians of Madrid wanted to offer an early, simplified and critical approach to these new drugs, to new developments in immunotherapy and to what has been learned from the immune response modulators already known and which have proven effective against the virus, in order to help understand the current situation. 相似文献
19.
《Expert opinion on investigational drugs》2013,22(1):79-86
Advances in the molecular biological knowledge of neuronal nicotinic acetylcholine receptors (nAChRs) have led to a growing interest by the pharmaceutical industry in the development of novel compounds that selectively modulate nAChR function. The ability of (-)-nicotine, an activator of nAChRs, to enhance attentional aspects of cognition in animals and humans, to exert neuroprotective and anxiolytic-like effects, and presumably to mediate the negative correlation between smoking and Alzheimer's (and Parkinson's) Disease, has focused interest on the potential therapeutic utility of modulators of nAChR function for treatment of some of the deficits associated with these progressive, neurodegenerative conditions. Numerous compounds are known which activate nAChRs and which might serve as lead compounds toward the development of such agents. The pharmacologic diversity of neuronal nAChR subtypes suggests the possibility of developing selective compounds which would have more favourable side-effect profiles than existing agents. This broader class of agents, collectively called cholinergic channel modulators (ChCMs), is anticipated to encompass compounds which would have more favourable side-effect profiles than existing agents, which generally exhibit low selectivity. This selectivity may be achieved by preferentially activating some subtypes of nAChRs (i.e., Cholinergic Channel Activators, ChCAs) or inhibiting the function of other subtypes (Cholinergic Channel Inhibitors, ChCIs). An overview of the biology of nAChRs and the rationale for the use of ChCMs for the treatment of dementia related to neurodegenerative diseases are presented, followed by a discussion of lead compounds and compounds under consideration for clinical evaluation. 相似文献