高效液相色谱法同时测定血浆中艾司唑仑、三唑仑和阿普唑仑浓度

目的 :建立同时测定血浆中艾司唑仑、三唑仑和阿普唑仑浓度的方法。方法 :采用HPLC法 ,选用ZORBAXRP C18柱(15 0mm× 4 .6mm ,5 μm) ;甲醇 2 5mmol·L-1醋酸铵溶液 (5 7∶4 3)作流动相 ;检测波长为 2 30nm。结果 :本法对三唑仑、阿普唑仑和艾司唑仑的最低检测限浓度均为 4 μg·L-1;回收率接近 10 0 % ;日内、日间精密度 <5 % ;线性范围均为 2 0～ 10 0 0 μg·L-1。结论 :本法能同时测定血浆中三唑仑、阿普唑仑和艾司唑仑 ,此法重现性好 ,灵敏 ,可靠 ,可用于临床药物中毒监测。     

LC-MS/MS法同时测定人血浆中咪达唑仑和 1-羟基咪达唑仑的浓度

目的:建立同时测定人血浆样本中咪达唑仑和1-羟基咪达唑仑浓度的LC-MS/MS方法.方法:以d4-咪达唑仑为内标,血浆样本加入含内标的乙腈处理后进样分析.色谱柱为Kinetex C18(2.1mm×50 mm,2.6μm),流动相为乙腈-1 mmol· L-1甲酸铵溶液(含0.1％甲酸),梯度洗脱,流速为0.3 mL·min-1,进样量为3.0 μL.质谱条件采用电喷雾正离子源,扫描方式为多重反应监测,用于定量分析的检测离子分别为m/z 325.9→291.0(咪达唑仑)、m/z 342.0→324.1(1-羟基咪达唑仑)、m/z 329.9→295.0(d4-咪达唑仑).结果:咪达唑仑和1-羟基咪达唑仑分别在0.300～200 ng· mL-1和0.150～100 ng·mL-1线性关系良好,定量下限分别为0.300 ng· mL-1和0.150ng·mL-1,批内和批间精密度均小于15％,准确度在-4.7％～9.9％,基质效应为95.5％～101.4％,提取回收率为100.6％～102.4％.血浆样本室温放置12h、3次冻融循环及-40℃冰冻12个月稳定性良好,待测溶液进样器放置24h稳定.结论:本研究建立的分析方法灵敏、准确,样本前处理简便、快捷,可用于人血浆样本中咪达唑仑和1-羟基咪达唑仑浓度的测定.     

HPLC法测定大鼠血浆中1’-羟基咪达唑仑及咪达唑仑的浓度

目的:建立大鼠血浆中咪达唑仑及其代谢产物1’-羟基咪达唑仑测定的高效液相色谱（HPLC）方法。方法:血浆样品以地西泮为内标,经碳酸盐缓冲液碱化后,由混合有机溶剂（正己烷:二氯甲烷=7:3,v/v）提取。采用Hypersil BDS C₁₈（250mm×4.6 mm,5μm）柱,以KH₂PO₄(0.02 mol·L^-1)缓冲液-乙腈-甲醇（38:20:42）为流动相,柱温40℃,流速1.0 ml·min^-1,于紫外230 nm处检测1’-羟基咪达唑仑及咪达唑仑浓度。结果:在该试验条件下,血浆中1’-羟基咪达唑仑的线性范围为8.32～832 ng·ml^-1,最低检测限为8.32 ng·ml^-1;咪达唑仑的线性范围为25～2 500 ng·ml^-1,最低检测限为25 ng·ml^-1。其日间和日内精密度均小于8%,提取回收率为84～90%。结论:本方法专属性强、灵敏度高、重复性好,适用于实验室评价药物间相互作用研究。     

RP-HPLC同时测定血浆中8种苯二氮(艹卓)类药物

目的 采用HPLC法建立同时测定血浆中8种苯二氮(艹卓)类药物(氯硝西泮、艾司唑仑、阿普唑仑、三唑仑、澳沙西泮、替马西泮、氯氮(艹卓)和地西泮)的方法.方法 血浆样品经正己烷-二氯甲烷(5:3)提取.选用Diamonsil Rp-C18柱(250 mm×4.6mm,5μm);甲醇-25 mmol.L-1醋酸铵溶液(63:37)作流动相,流速1.0 mL·min-1,检测波长230 nm.结果 氯硝西泮、三唑仑、澳沙西泮、氯氮(艹卓)、地西泮的最低检测浓度为8μg·L-1,艾司唑仑、阿普唑仑、替马西泮的最低检测浓度为5μg·L-1;方法回收率接近100%;提取回收率大于70%,日内、日间精密度小于6%;艾司唑仑、阿普唑仑和替马西泮10～1.5×103μg·L-1的线性关系良好,其余5种药物的线性范围为20～1.5×103μg·L-1(r＞0.999).结论 所建方法操作简便、快速、准确、灵敏度高、重复性好,适用于临床上人血浆中8种苯二氮(艹卓)类药物的同时定性、定量检测.     

体液中毒物与药物快速定性定量分析方法研究：Ⅷ.RP—HPLC法同时测…

应用高效液相色谱法测定人体血清中艾司唑仑和三唑仑的浓度，用反相Ｃ１８柱，甲醇－水－乙腈－四甲基乙二胺为流动相，冰醋酸调ＰＨ６．５，检测波长２５４ｎｍ，选用安定作内标，样品用无水乙醚在碱性条件下提取。血清中艾司唑仑和三唑仑的最低检测浓度分别为８．３５μｇ／Ｌ，和２０μｇ／Ｌ，平均回收率分别为９２．６％和８９．４％，ＲＳＤ分别为３．２１％和５．５３％，本法简便，快速，灵敏度高，适用于艾司唑仑和三唑仑的     

氟康唑联用咪达唑仑血药浓度测定方法及相互作用

目的:建立可同时进行氟康唑和咪达唑仑生物样品前处理的方法,应用RP-HPLC法分别测定氟康唑、咪达唑仑、1-羟基咪达唑仑的血药浓度;同时考察氟康唑与咪达唑仑联用对咪达唑仑血药浓度的影响.方法:1 mL血清样品加入内标后以5 mL乙酸乙酯提取,有机相用氮气吹干,以100 μL甲醇溶解,分别在不同的色谱条件下以20 μL进样测定.结果:氟康唑、咪达唑仑、1-羟基咪达唑仑及内标能够在同一条件下被提取.氟康唑在0.5～20 μg/mL范围内线性关系良好(r=0.997 0,n=6),咪达唑仑在0.03 ～ 7.29 μg/mL范围内线性关系良好(r=0.998 5,n=16),1-羟基咪达唑仑在0.09 ～ 7.29 μg/mL范围内线性关系良好(r=0.999 3,n=5).联用氟康唑和咪达唑仑组较单用咪达唑仑组中咪达唑仑血药浓度明显增高.结论:该法灵敏、准确、简单、快速,可用于同时测定氟康唑、咪达唑仑及其代谢产物的血药浓度.联用氟康唑和咪达唑仑与单用咪达唑仑比较,咪达唑仑血药浓度明显增高.     

液相色谱-质谱联用法检测体液中三唑仑及其代谢产物

建立了鉴别体液中三唑仑及其主要代谢物的液相色谱 质谱联用法。采用液相色谱 电喷雾离子阱质谱法 ,得到三唑仑和羟基化代谢物及其葡萄糖苷酸型结合物的色谱、质谱信息以及特征碎片离子。三唑仑的最低检测限小于 0 1ng。用本法分析了一例怀疑服用过量三唑仑的麻醉抢劫案例所取证的血样及尿样 ,并与健康受试者服药后尿样及家兔灌胃三唑仑后所取的血样及尿样比较 ,得到了当事人服用三唑仑的可靠数据。该方法可靠、快速、简便 ,尤其适用于需快速响应的法医学和毒理学分析     

高效液相色谱法同时测定血清中咖啡因和氯唑沙宗的浓度

目的:建立同时测定血清中两种探针药物(咖啡因、氯唑沙宗)浓度的高效液相色谱法.方法:采用迪马C18色谱柱(250 mm×4.6 mm,5 μm);流动相:乙腈-0.02 mol·L-1 磷酸二氢钾溶液(1∶3,v/v),含0.01 mol·L-1三乙胺;流速:1.5 mL·min-1;紫外检测波长:280 nm;柱温:30℃.结果: 咖啡因在2.5～12.5 μg·mL-1、氯唑沙宗在2.5～12.5 μg·mL-1的浓度范围内线性关系良好,最低检测限分别为0.1 μg·mL-1、0.4 μg·mL-1,回收率分别为103.70%±4.36%、102.82%±4.39%.结论: 本法操作简便,灵敏度高,快速可靠,可用于血清中咖啡因和氯唑沙宗的浓度测定.     

高效液相色谱法测定血浆中咪达唑仑浓度

目的 :建立测定血浆中咪达唑仑浓度的反相高效液相色谱法。方法 :以地西泮为内标 ,采用C18柱及保护柱 ;流动相为甲醇 -水 (6 0∶4 0 ,V/V) ,含乙腈 1%、二乙胺 0 1%、磷酸 0 0 5 % ;流速为 0 6mL·min-1;提取液为乙醚 ;采用紫外检测 ,检测波长为 2 2 5nm。结果 :咪达唑仑与内标分离良好 ,保留时间分别为 (11 2 1± 0 5 8)min和 (9 4 1± 0 39)min ;咪达唑仑在 0 1～ 2 0 μg·mL-1范围内线性良好 ,回归方程为Y =9× 10 -4X - 9 17× 10 -2 ,r=0 9998;日内及日间变异均 <6 % ;最低检测浓度 0 0 5 μg·mL-1。结论 :本方法适用于咪达唑仑的药动学和药效学研究     

体液中毒物与药物快速定性定量分析方法研究Ⅷ.RP—HPLC法同时测定血清中艾司唑仑和三唑仑的浓度

应用高效液相色谱法测定人体血清中艾司唑仑和三唑仑的浓度。用反相Ｃ１８柱，甲醇—水—乙腈—四甲基乙二胺为流动相，冰醋酸调ｐＨ６．５，检测波长２５４ｎｍ，选用安定作内标，样品用无水乙醚在碱性条件下提取。血清中艾司唑仑和三唑仑的最低检测浓度分别为８．３５μｇ／Ｌ和２０μｇ／Ｌ，平均回收率分别为９２．６％和８９．４％，ＲＳＤ分别为３．２１％和５．５３％。本法简便、快速、灵敏度高，适用于艾司唑仑和三唑仑的治疗药物监测和中毒时的快速筛选。     

Degraded and undegraded carrageenans and experimental gastric and duodenal ulceration

The prevention of histamine-induced gastric and duodenal ulceration in the guinea-pig has been examined using a series of undegraded and degraded carrageenans. Undegraded carrageenans were active at lower doses than degraded carrageenans. The high viscosity of the undegraded carrageenans in solution prevented their use in larger doses. Degradation of carrageenan without serious loss of sulphate, gives a product which allows the dose to be increased to an extent that its effect more than offsets the slight loss in activity caused by the degradation. No single feature of carrageenan structure can be related to anti-ulcer activity although degradation, and hence reduction of molecular size, generally reduces activity. Sulphate contents over 30% have little apparent effect on activity; κ-carrageenans were not consistently different in anti-ulcer activity from Λ-carrageenans. This contrasts with the antipeptic activity of carrageenans where κ-carrageenans are less active than their Λ-counter-parts. As with antipeptic activity, the degree of anti-ulcer activity is probably determined by a combination of structural features which includes molecular size and polyanionic properties.     

Affective and Anxiety Disorders and Alcohol and Drug Dependence:

Depression and anxiety frequently coexist in patients with substance use disorders. This clinically-oriented article examiens the relationship between these conditions and emphasizes data showing that substances of abuse can cause signs and symptoms of both depression and anxiety. These substance-related syndromes appear to have a different course and prognosis than uncomplicated, independent anxiety and major depressive disorders, and clinicians should consider the role of alcohol and other drugs in all patients presenting with these complaints. The authors will also outline an approach for diagnosing and managing patients with the combination of a substance use and depressive or anxiety disorder.     

Alcohol and Substance Use and Abuse in Women and Children

No abstract available for this article.     

Excretion and biotransformation of alfentanil and sufentanil in rats and dogs

The excretion and biotransformation of alfentanil (ALF) and sufentanil (SUF), two recent analogues of the synthetic opioid fentanyl, were studied after single iv administration of the tritium-labeled drugs in male rats and dogs. The drugs were almost completely metabolized in the two species, which resulted in a large number of metabolites. The excretion of the metabolites was rapid and exceeded 95% within 4 days, except for that of ALF metabolites in dogs (about 85%). For ALF, excretion of the radioactivity with the urine (73% in rats, about 76% in dogs) exceeded that with the feces. For SUF, excretion of the radioactivity with the urine amounted to 38 and 60% and that with the feces to 62 and 40%, in rats and dogs, respectively. Bile-cannulated rats excreted 68% with the bile within 24 hr after SUF dosing, and about 22% of this biliary radioactivity was subjected to enterohepatic circulation. After an ALF dose, the biliary excretion amounted to 24%, and the enterohepatic circulation was minimal. The main metabolic pathways of the two drugs were the oxidative N-dealkylation at the piperidine nitrogen and at the amide nitrogen, oxidative O-demethylation, aromatic hydroxylation, and the formation of ether glucuronides. N-[4-(Hydroxymethyl)-4-piperidinyl]-N-phenylpropanamide (M6) was the main metabolite of both ALF and SUF in rats. In dogs, the glucuronide of N-(4-hydroxyphenyl)propanamide (M5) was the main metabolite of ALF. After SUF dosing in dogs, N-[4-(methoxymethyl)-4-piperidinyl]-N-phenylpropanamide was more abundant than M5.