高效液相色谱法测定天麻头风灵胶囊中天麻素含量

目的采用高效液相色谱法测定天麻头风灵胶囊中天麻素的含量。方法色谱柱为Diamonsil C18柱(250 mm×4.6 mm,5μm),流动相为乙腈-0.3%磷酸(2∶98),流速为0.7 mL/min,柱温为30℃,检测波长为221 nm。结果天麻素进样量在0.2～1.8μg范围内与峰面积呈良好的线性关系(r=0.999 9);平均加样回收率为98.90%,RSD为1.11%(n=6)。结论该方法简便易行、结果可靠,可有效控制天麻头风灵胶囊的质量。     

高效液相色谱法测定天麻头风灵片中天麻素的含量

目的建立天麻头风灵片中天麻素含量的测定方法。方法用十八烷基硅烷键合硅胶（4．6×250mm，5μm）为填充剂，以甲醇：水（5：95）为流动相，检测波长为220nm，理论塔板数按天麻素峰计算不得低于2000。结果平均回收率为99．04％，相对标准偏差（RSD）为0．18％；10批样品测定结果：天麻素平均含量为0．095mg／片。结论高效液相色谱法简便、快速、结果准确，可用于天麻头风灵片的质量控制。     

HPLC法测定天麻胶囊中天麻素的含量

目的:建立天麻胶囊中天麻素的HPLC测定方法。方法:色谱柱为Hypersil BDS C_(18)柱(250mm×4.6mm,5μm),流动相为乙腈-0.03%磷酸溶液(2:100),流速为1.0 ml·min~(-1),检测波长为221nm。结果:天麻素在进样量0.21～2.12μg范围内呈良好的线性关系,r=0.9999;平均回收率为97.9%,RSD=2.2%(n=6)。结论:本方法简便、准确、灵敏。可用于天麻胶囊的质量控制。     

HPLC法测定天麻降压胶囊中天麻素的含量

目的 测定天麻降压胶囊中天麻素的含量。方法 采用HPLC法测定了天麻降压胶囊中天 麻素的含量,色谱柱为C18,流动相为乙腈-水-磷酸(3:97:0.2),检测波长为221 nm。结果 天 麻素的平均回收率为99.0％,RSD为1.39%。结论 本法简便、稳定、重现性好,且制剂中其它组 分对测定无干扰,可有效地控制该制剂的质量。     

阿魏酸钠大鼠体内药物动力学研究

用反相ＨＰＬＣ法测定大鼠全血中阿魏酸的含量，并用此法对大鼠股静脉给药后体内药物动力学进行了研究。结果表明本法快速、灵敏、准确可靠，回收率为９５．１２％±１．３２％。阿魏酸在大鼠体内过程归属开放式单空模型，体内消除迅速。Ｔ１／２＝９．８６ｍｉｎ。     

11批天麻胶囊中天麻素的含量考察

目的考察11批不同厂家天麻胶囊的天麻素含量。方法采用HPLC法测定天麻胶囊中的天麻素。结果 11批天麻胶囊中天麻素的含量为26.4~235.1μg.粒-1。结论应增加天麻素的含量测定项目,以保证临床用药安全有效。     

HPLC测定天麻头风灵软胶囊中天麻素的含量

目的测定天麻头风灵软胶囊中天麻素的含量。方法采用HPLC法,D iamonsilTMC18色谱柱(250 mm×4.6 mm,5μm),甲醇-水(2:98)为流动相,流速1.0 m l.m in-1,检测波长221 nm,柱温30℃,进样量5μl。结果天麻素峰与其相邻杂质峰能完全分离,在0.21~1.73 mg.m l-1浓度范围内线性关系良好(r=0.9994)。结论该法简便、准确、专属性好,可作为天麻头风灵软胶囊中天麻素含量的测定方法。     

高效液相色谱法测定天麻胶囊中天麻素的含量

目的 建立天麻胶囊中天麻素的含量测定方法.方法 采用C18反相色谱柱,以甲醇-0.05％磷酸(8∶92)为流动相,柱温30℃,流速1.0mL·min-1,在221nm测定.结果 天麻素在0.00133μg ～0.665μg的范围内时,进样量与峰面积呈良好线性关系,回归方程为y=26693x-1138.5,r=0.9999,平均回收率为107.9％ (n =6),RSD=3.9％.结论 本法简便、准确、重复性好,可用于天麻胶囊中天麻素的含量测定.     

水苏碱在家兔体内的药物动力学研究

目的：研究水苏碱在家兔体内的药物动力学。方法：采用HPLC法测定从家兔耳静脉注射盐酸水苏碱溶液后不同时间的血浓度。用3P97药动学程序对血药浓度-时间数据进行拟合。结果：主要药动学参数为AUC=1712．50min·μg·ml^-1,Vc=11．80L·kg^-1,t1／2α=32．46（min）,t1／2β=189．61min,K21=3．97×10^-3min^-1,K10=1．97×10^-2min^-1,K12=1．36×10^-7min^-1,CLs=0．23L·kg^-1·min^-1。结论：水苏碱在家兔体内呈二室模型.     

莲心碱在大鼠体内的药物动力学研究

用反向HPLC法 ,以己酮可可碱为内标 ,建立了血浆中莲心碱的测定方法 ,血浆标准曲线为A1/A2 =0 3188C - 0 0 6 77,相关系数r =0 9999,回收率及日内、日间精密度均符合要求。根据大鼠颈静脉给药 (8 5 4mg/kg)后测得的血药浓度 ,用 3P87处理后求得的莲心碱的主要药动学参数为 :t1/ 2 (α) =2 5 14min ,t1/ 2 ( β) =49 5 2 2min ,AUC =114 878min·μg/mL ,CL =0 0 743L/ (kg·min) -1,V(c) =0 76 6L/kg。     

Distribution and metabolism of gastrodin in rat brain

Gastrodin is the major and bioactive component in Tianma (Gastrodia elata Bl.) and has sedative, anticonvulsive and neuroprotective effects. Since little is known about its neuropharmacokinetics and brain metabolism, this study was undertaken to investigate the kinetic inter-relationship of gastrodin in rat plasma, cerebrospinal fluid (CSF) and brain microdialysate (frontal cortex, hippocampus, thalamus and cerebellum). Gastrodin was administered via the femoral vein at a dose of 200mg/kg, and blood, CSF and brain microdialysate were collected at timed intervals for the measurement of gastrodin concentrations by high-performance liquid chromatography. The samples were analyzed on a Diamonsil C18 column (5 microm, 250 mm x 4.6mm i.d.) with a mobile phase consisting of acetonitrile-water (5% acetonitrile for brain microdialysate, 2.5% acetonitrile for plasma and CSF), and detected with a UV detector at 221 nm. The distribution of gastrodin in rat showed that levels of gastrodin declined rapidly after drug administration, and the entry of gastrodin into the brain was rapid. However, the ratios of AUC(brain)/AUC(plasma) were not high. The individual ratios of the AUC in the CSF, frontal cortex, hippocampus, thalamus and cerebellum to the AUC in the plasma were 4.8+/-2.4%, 3.3+/-1.2%, 3.0+/-0.7%, 3.3+/-1.3% and 6.1+/-1.9%, respectively. The AUC in the cerebellum was significantly higher than that in other brain regions (P<0.05). The concentrations of p-hydroxybenzyl alcohol, the main metabolite of gastrodin, were very low both in the CSF and plasma.     

天麻素经十二指肠给药后的大鼠脑药动学特征（英文）

目的研究天麻素在大鼠十二指肠给药后的脑药动学和不同脑区的分布。方法将大鼠麻醉后,通过其十二指肠给天麻素,剂量为200 mg·kg^-1。在规定时间点收集血浆、脑脊液和4个不同脑区（皮质、海马、丘脑、小脑）的脑微透析液。采用HPLC法测定所收集液体中的药物浓度,采用DAS 2.0药动学软件计算药动学参数。结果天麻素给药后能迅速进入脑部,4个不同脑区和脑脊液的t_max分别为（40.0±6.1）、（42.5±7.7）、（37.5±9.5）、（42.5±7.7）和（55.8±16.0）min,其AUC与血浆AUC的比值分别为（2.6±1.0）%、（2.6±0.9）%、（3.0±0.9）%、（5.3±2.1）%和（6.0±2.6）%。天麻素在小脑的AUC明显大于在其他3个脑区的AUC（P<0.05）。结论天麻素经十二指肠给药后能迅速入脑部,但是入脑量低,所有AUC_脑/AUC_血浆均<6%。     

HPLC法测定天麻素葡萄糖注射液中天麻素的含量

目的建立高效液相色谱法测定天麻素葡萄糖注射液中天麻素（C13H18O7）含量的方法。方法采用Diamonsil-C18色谱柱（4.6 mm×250 mm,5μm）;以甲醇-乙腈-磷酸盐缓冲液-水（10∶45∶25∶920）为流动相,流速为1 ml·min^-1;检测波长为220nm。结果天麻素在21.6～64.8 mg·L^-1浓度范围内有良好的线性关系（r=0.999 9）,平均回收率为99.59%,RSD为1.0%。结论此法简便、快速、准确、专属性强,适用于天麻素葡萄糖注射液中天麻素（C13H18O7）的含量测定。     

Protective effects of gastrodin on hypoxia-induced toxicity in primary cultures of rat cortical neurons

The phenolic glucoside gastrodin is the main component extracted from the rhizome of Gastrodia elata (Orchidaceae), a Chinese herbal medicine, which has long been used for treating dizziness, epilepsy, stroke and dementia. The present study aims to investigate the effect of gastrodin on hypoxia-induced neurotoxicity in cultured rat cortical neurons. Neuron survival and extracellular glutamate level were measured after an insult by hypoxia. Glutamate concentrations were determined by an HPLC-ECD system. The results demonstrated that neurons were significantly damaged by hypoxia for 24 h. When pretreated with gastrodin (100, 200 microg/mL) in hypoxia, neuron survival was significantly increased compared with no gastrodin treatment. Moreover, the enhancement of extracellular glutamate level stimulated by hypoxia was inhibited by pretreatment with gastrodin (100 microg/mL). Further studies demonstrated that gastrodin prevented glutamate- and NMDA-induced neurotoxicity. In addition, gastrodin also inhibited the extracellular glutamate level induced by NMDA insult. These findings suggest that gastrodin has a neuroprotective action against hypoxia in the cultured cortical neuron, and the mechanism may involve a decreasing of the extracellular glutamate level.     

Pharmacokinetic study of tolmetin in the rat.

The pharmacokinetics of tolmetin (CAS 26171-23-3) was studied in male Wistar rats after intravenous and oral administration of 32.95 mg/kg. After intravenous administration of the drug, it was shown that the most probable model was the two-compartment-open model with Michaelis-Menten elimination. After oral administration, the drug was absorbed rapidly (K01 = 0.1304 min-1). The bioavailability was 96.94% and the drug was mostly excreted as 1-methyl-5-(4-carboxybenzoyl)-1H-pyrrole-2-acetic acid, while the excretion of the unchanged drug was 6.12%.     

Pharmacokinetic characterization of dehydroevodiamine in the rat brain

The objective of this study was to examine the kinetics of the distribution of dehydroevodiamine (DHED) in the rat brain. After an intravenous infusion of 15 min (dose of 1-10 mg/kg), the temporal profiles of the plasma levels of DHED declined in a multiexponential manner. Moment analysis indicated that the clearance and steady-state volume of distribution for DHED were not statistically different with the dose, indicating that the pharmacokinetics for DHED is linear in the range examined. Nonlinear regression analysis of DHED concentrations in the plasma and the brain revealed that the linear kinetics into and out from the brain reasonably described the data and that the clearances for influx into and efflux from the brain were comparable. Transport clearances for DHED across MBEC4 monolayers, an in vitro model of the blood-brain barrier, were also comparable for influx and efflux, and were independent of the medium concentration. The concentration of DHED in cerebrospinal fluid was negligible compared with that found in plasma, indicating that the drug is not primarily distributed to the brain via the blood-cerebrospinal fluid barrier. These observations indicate that DHED is transported from the systemic circulation to the brain via the blood-brain barrier by linear kinetics.     

厄贝沙坦和吡格列酮在大鼠体内的药动学相互作用

目的:建立同时测定大鼠血浆中厄贝沙坦、吡格列酮的HPLC法,探讨厄贝沙坦与吡格列酮联用时有无显著的药动学相互作用。方法:大鼠分为A、B、C3组,A组按30mg.kg-1服用厄贝沙坦,B组按4.5mg.kg-1服用吡格列酮,C组为联合给药组,按30mg.kg-1服用厄贝沙坦,按4.5mg.kg-1服用吡格列酮,采用HPLC法同时测定不同时间点厄贝沙坦和吡格列酮的血药浓度,计算药动学参数。结果:与2种药物分别使用的情况相比,厄贝沙坦组在联用时的ρmax、AUC存在有显著性差异。结论:厄贝沙坦与吡格列酮在联用时,存在显著的药动学相互作用。     

Pharmacokinetic study of iodine-labeled silibinins in rat.

The very low bioavailability of silibinin (silybin, SB), the main antioxidant flavonolignan of silymarin from Silybum marianum L. (Asteraceae), requires sensitive methods to study the modulation of silibinin bioavailability. To evaluate the potential for use of radiolabeled silibinin, two silibinin derivatives, separated by HPLC after iodination ((125)I-SB(1) and (125)I-SB(2)) and their complexes 1 : 1 with phosphatidylcholine ((125)I-SPC(1) and (125)I-SPC(2)) were administered concurrently with a single intragastric dose of 5.0 mg or 50 mg of unlabeled silibinin (alone or as a constituent of the complex) per kg of body weight in a comparative study of bioavailability in the rat. Pharmacokinetic parameters as well as organ uptake of (125)I-SB(1)-derived radioactivity showed a dose-response pattern. The parameters of bioavailability after (125)I-SPC(1) intake were not influenced by unlabeled silibinin (complexed with phosphatidylcholine), since maximal levels were achieved by the lower dose of unlabeled compound. The superior bioavailability of (125)I-SPC(1) was obvious at the lower dose of unlabeled compound as elevated AUC and RA(max) (maximal percentage of administered radioactivity), and increased radioactivity in liver, kidney, spleen and heart. An absence of these characteristics with (125)I-SB(2) and (125)I-SPC(2) suggests the use of(125)I-SB(1) for studies of modulation of its bioavailability in vivo in rat.