愈美分散片的HPLC测定

建立了HPLC法测定愈美分散片中愈创木酚甘油醚和氢溴酸右美沙芬的含量.采用ODS柱,流动相为乙腈-甲醇-0.01%三乙胺溶液(18:15:67,pH3.5),流速1.0ml/min,检测波长276nm.愈创木酚甘油醚和氢溴酸右美沙芬的线性范围分别为6～72μg/ml和4.2～51μg/ml,平均回收率分别为99.0%和102.6%,RSD分别为1.2%和1.5%.     

HPLC法测定硝苯地平阿替洛尔缓释双层片中2组分含量

目的测定硝苯地平阿替洛尔缓释双层片中 2组分含量。方法采用ODS(Hypersil,5 μm,4 6mm× 2 0 0mm)为填充剂 ,甲醇 水 磷酸 ( 70∶30∶0 1 )流动相的高效液相色谱法。结果硝苯地平和阿替洛尔线性分别为 0 4 0～ 1 2 0 μg ,0 80～ 2 38μg;回收率分别为 99 8%(RSD =1 0 %) ,99 9%(RSD =0 5 %)。结论该方法为评价该制剂的质量提供了可靠的方法     

复方美佐含片的HPLC测定

建立了复方美佐含片含量和有关物质测定的HPLC方法,采用C8色谱柱,乙腈-0.07mol/L磷酸二氢钾缓冲液(pH3.0)(25:75)为流动相,检测波长220nm.氢溴酸右美沙芬与苯佐卡因分别在7～35μg/ml和2.8～14μg/ml浓度范围内线性关系良好(r均为0.9999),平均回收率分别为99.9%(RSD 0.43%)和98.8%(RSD 0.74%).     

骨炎1号聚乳酸微球中补骨脂素和异补骨脂素的HPLC测定

建立了HPLC法测定骨炎1号聚乳酸微球中补骨脂素和异补骨脂素的含量.采用DiamonsidTM C18柱,甲醇-1%乙酸(60:40)为流动相,流速0.8ml/min,检测波长245nm.补骨脂素和异补骨脂素分别在7.4～55.8μg/mi和6.5～48.9μg/ml范围内线性关系良好(r均为0.9997),平均回收率分别为102.3%(RSD=1.45%)和102.7%(RSD=0.64%).     

高效液相色谱法同时测定复方对乙酰氨基酚片中3组分的含量

目的:建立以高效液相色谱法同时测定复方对乙酰氨基酚片中对乙酰氨基酚、咖啡因、阿司匹林含量的方法。方法:色谱柱为ODS,流动相为甲醇-4.2%的冰醋酸溶液(3∶7),流速为1.0ml/min,检测波长为275nm,进样量为20μl,柱温为25℃。结果:对乙酰氨基酚、咖啡因、阿司匹林的线性范围分别为16.08～428.80μg/ml(r=0.9981)、3.42～91.20μg/ml(r=0.9988)、23.87～769.92μg/ml(r=0.9999),平均回收率分别为99.2%(RSD=0.23%)、100.4%(RSD=0.63%)、99.3%(RSD=0.11%)。结论:本方法简便、快速、准确,可用于复方对乙酰氨基酚片的含量测定。     

硝苯地平光解动力学的研究

目的研究硝苯地平在紫外线灯及日光色荧光灯下的光解动力学.方法用反相高效液相色谱法对4μg/ml～12μg/ml浓度范围硝苯地平甲醇溶液的光解动力学进行了研究.结果硝苯地平甲醇溶液在4μg/ml～12μg/ml浓度范围时,不论是在紫外线灯照射下还是在荧光灯照射下光解均呈线性降解.浓度分别为4μg/ml、8μg/ml、12μg/ml硝苯地平甲醇溶液在相同光照度下(15×100Lux),其在紫外灯下的k分别为113.54×10-3min-1、87.26×10-3min-1、52.21×10-3min-1.在荧光灯下的k分别为22.57×10-3min-1、、21.61×10-3min-1、18.08×10-3min-1.结论不论是在紫外线灯照射下还是在荧光灯照射下硝苯地平甲醇溶液都极易光解,且浓度越大光解速度越慢.在相同光照度下荧光灯对硝苯地平甲醇溶液光解速度的影响比紫外线灯小.     

HPC法测定爱地清缓释胶囊中硝苯地乎的含量

报导了采用HPLC法测定爱地清缓释胶囊中硝苯地平的含量.采用ODS柱(100mm×4.6mm,5μm)、0.92%辛烷磺酸钠水溶液-冰醋酸-甲醇(542.532.5425)为流动相,用紫外检测器于254波长处检测.平均回收率为99.93%,RSD.64%(n=5),线性范围2μg/ml～6μg/ml.本法具有快速、简便、灵敏、准确等优点.     

注射用赖氨匹林的两种含量测定方法

目的:采用高效液相色谱法和紫外分光光度法同时测定注射用赖氨匹林的含量,为质量控制提供有效的分析手段.方法:高效液相色谱法:Hypersil C18(1500mm×4.6mm,10μm),以甲醇-0.1%三乙胺溶液(1:1.冰醋酸调节pH至3.5)为流动相,检测波长为280nm,按外标法以峰面积计算.紫外分光光度法:检测波长210nm.结果:高效液相色谱法:阿司匹林和水杨酸在60.34～905.10μg/ml和1.20～18.00μg/ml浓度范围内呈良好的线性关系,其线性相关系数分别为0.9999和0.9999;加样回收率分别为98.76%～99.29%(RSD=0.59%～0.93%)和98.49%～99.69%(RSD=0.80%～1.01%).紫外分光光度法:赖氨匹林浓度在4.0～14.0μg/ml范围内与吸收度有良好的线性关系,回归方程为:Y=0.0548X-0.0299,r=0.9998,方法平均回收率为99 8%～100.7%,RSD为1.62%～1.81%.结论:两种方法均可用作注射用赖氨匹林的质量控制.     

高效液相色谱法同时测定降脂饮中3组分的含量

目的:建立以高效液相色谱法同时测定降脂饮中大黄酸、大黄素及大黄酚含量的方法。方法:色谱柱为VP-ODS,流动相为甲醇-0.2%磷酸溶液(80∶20),流速为1ml/min,检测波长为225nm,柱温为室温。结果:大黄酸、大黄素、大黄酚检测浓度分别在0.015～0.15μg/ml(r=0.9996)、0.014～0.14μg/ml(r=0.9998)、0.0085～0.085μg/ml(r=0.9993)范围内线性关系良好;平均回收率分别为99.26%(RSD=2.00%)、98.72%(RSD=1.80%)、99.76%(RSD=2.3%)。结论:本方法稳定、准确、可行,可用于降脂饮的质量控制。     

复方双嘧达莫片的HPLC测定

建立高效液相色谱法测定复方双嘧达莫片中双嘧达莫及阿司匹林的含量.采用Ci8色谱柱,流动相为甲醇-水-磷酸-二乙胺(275:225:0.3:0.1),检测波长225nm.阿司匹林和双嘧达莫分别在6～14μg/mi和48～112ug/ml浓度范围内线性关系良好(r＞0.9995).平均回收率分别为98.0%(RSD=1.91%)和100.6%(RSD=1.50%).     

高效液相色谱法测定阿替洛尔片中阿替洛尔的含量

目的建立阿替洛尔片中阿替洛尔的含量测定方法。方法采用HPLC法，色谱柱为Dinamonsil-C18柱，以甲醇-水（550：470）1000mL，加庚烷磺酸钠960mg与无水醋酸钠82mg使溶解，加冰醋酸0．57mL为流动相；流速为1．0mL·min^-1；检测波长为276nm,柱温为28℃。结果阿替洛尔进样量在0．1800～1．8000μg呈良好线性关系；其回归方程为Y=0．0781X（r=0．9999）；平均回收率为97．08％；RSD为1．33％（n=9）。结论本方法操作简单，准确，可用于测定阿替洛尔片的含量。     

Bioavailability of atenolol formulations

In this comparative bioavailability study two tablet formulations of atenolol (sales and clinical trial) were compared with an oral solution. Twelve healthy adult male volunteers received, on a cross-over basis, on three separate occasions, 100 mg oral dose of the three formulations of atenolol. Bioavailability was based on concentrations of atenolol in whole blood and urine. The atenolol blood levels peaked at approximately 3 h after dosing, with individual values ranging from 0·21 to 0·92 μg ml^?1 (a four-fold difference), with all three formulations. Three-fold variations among subjects occurred in the areas under the curve (AUC) and urinary recoveries. The average elimination half-life of atenolol was between 6 and 7 h for all three formulations. Some statistically significant differences were observed between the tablets and the aqueous solution: the AUC (∞) and mean peak blood concentrations were significantly greater with the U.K. sales tablet than the solution, and the mean concentrations in the blood at certain specified times after administration were significantly greater with the two tablet formulations than the solution. The profiles of absorption and excretion of the two tablet formulations were similar. No adverse reactions were encountered in this study and all subjects completed the study without incident.     

Tissue atenolol levels following chronic beta-adrenoceptor blockade using oral atenolol in dogs

Tissue atenolol concentrations are high following chronic continuous beta-adrenoceptor blockade in dogs. Furthermore, significant concentrations of this poorly lipid soluble drug are found within the central nervous system after chronic dosing. It is suggested that all beta-adrenoceptor blocking agents may enter the central nervous system in significant and sufficient quantities to account for a central antihypertensive action of this group of compounds. Sequestration of beta-adrenoceptor agents in the CNS or other tissues may account for other clinically observed effects including adaptive effects.     

高效液相色谱法测定阿替洛尔片中阿替洛尔含量及其有关物质

目的:高效液相色谱法测定阿替洛尔片中阿替洛尔含量及其有关物质.方法:Inertsil ODS-3 C18 (5 μm,4.6 mm×150 mm)色谱柱,磷酸盐缓冲液-甲醇-辛烷磺酸钠(700∶300∶1.70)为流动相,检测波长:275 nm,流速:1.0 mL·min-1,柱温:36 ℃.结果:该方法能分离片剂中的阿替洛尔及其相关杂质,阿替洛尔在54.1～270.5 mg·L-1浓度范围内,线性良好,r=0.999 9;最低检测限21.6 ng.结论:HPLC法可作为阿替洛尔片的质量控制方法,简便快速,稳定可靠.     

Pharmacokinetic profile of atenolol aspirinate

We report microwave-assisted synthetic routes, the pharmacokinetic profile along with results from ulcerogenicity and mutagenicity studies of atenolol aspirinate, and an already described derivative, in which acetyl salicylic acid (aspirin) was connected to atenolol by an ester linkage. Atenolol aspirinate was stable towards aqueous hydrolysis but rapidly hydrolyzed in plasma (t(1/2) = 7.6 min). The results showed that the rapid and complete hydrolysis generates atenolol salicylate, which assumes a conformation stabilized by two intramolecular H-bonds, avoiding its further hydrolysis to salicylic acid and atenolol.     

Severe atenolol and diltiazem overdose

CASE REPORT: A case of combined, massive overdose of both atenolol and diltiazem in an adult male is reported. Cardiac arrest ensued which was responsive to cardiopulmonary resuscitation. Bradycardia, hypotension, and oliguria followed which were resistant to intravenous pacing and multiple pharmacologic interventions, including intravenous fluids, calcium, dopamine, dobutamine, epinephrine, prenalterol, and glucagon. Adequate mean arterial pressure and urine output were restored only after addition of phenylephrine to therapy with multiple agents and transvenous pacing. The patient survived until discharge after a hospital course complicated by nontransmural myocardial infarct on hospital day 4 and pneumonia. Laboratory testing subsequently revealed high serum levels of both atenolol and diltiazem. The atenolol level of 35 microg/mL in this patient is the highest reported associated with survival. CONCLUSION: This case illustrates severe cardiovascular toxicity after overdose of both atenolol and diltiazem. Oliguria, which has previously been reported in severe atenolol overdose, was successfully treated without hemodialysis by the addition of phenylephrine to aggressive therapy with pacing, inotropic, and pressor support.     

Transplacental passage of atenolol in man

Summary Maternal and umbilical serum concentrations of atenolol, a hydrophilic, cardioselective beta-adrenoceptor antagonist, were studied at delivery in seven cases of pregnancy hypertension. The drug had been administered to each patient for at least one week. Atenolol was detected in both maternal and umbilical serum in six cases, showing that there is transplacental passage of the drug. In the seventh case, who had stopped taking atenolol more than one day before delivery, neither maternal nor umbilical serum contained a measurable quantity of the drug. Atenolol concentration varied 3- to 6-fold between individuals, but there was no systematic difference between maternal and umbilical levels. It seems reasonable to assume that during steady state conditions the blood level of atenolol in mother and fetus is approximately equal, and that fetal accumulation of the drug does not occur.     

Cardioselectivity of atenolol in asthmatic patients

Summary Eight male patients with compensated congestive cardiomyopathy received single 300-mg doses of intravenous quinidine by 15-min infusion. Left ventricular (LV) performance was evaluated by echocardiography at multiple points in time during the next 24 h. Quinidine kinetics and protein binding were determined from multiple serum samples drawn for up to 36 h after dosage. LV function was not impaired. Instead, quinidine transiently increased ejection fraction (mean: +39%) and rate of circumferential shortening (mean: +46%). Endsystolic and end-diastolic LV internal diameter likewise were decreased (means: −13% and −7%). Blood pressure and ventricular rate were not significantly altered. Compared to 8 healthy controls matched for age, sex, and weight, quinidine volume of distribution among patients was smaller (means: 2.27 vs 1.90 l/kg), as was total quinidine clearance (3.49 vs 2.84 ml/min/kg); however, differences were not statistically significant. Well-controlled, slow intravenous infusion of quinidine does not impair LV performance and is safe for patients with compensated congestive cardiomyopathy. However, such patients may have reduced quinidine clearance and hence require lower doses than expected based on age and weight. Supported in part by Deutsche Forschungsgemeinschaft, Bonn-Bad Godesberg, Federal Republic of Germany, by Sandoz Studienstiftung, Basel, Switzerland, and by Grant MH-12279 from the United States Public Health Service. This work was part of the doctoral thesis of Dr. R. Arendt, Medizinische Universit?tsklinik, Bonn, Federal Republic of Germany     

Phenelzine and atenolol in social phobia

Seventy-four patients meeting DSM-III criteria for social phobia completed 4 or more weeks of double-blind, randomized treatment with the monoamine oxidase inhibitor phenelzine, the cardioselective beta-adrenergic blocker atenolol, or placebo. Sixty-four percent of the patients on phenelzine demonstrated moderate or marked improvement, compared to 30 percent on atenolol and 23 percent on placebo. Phenelzine was significantly more effective than atenolol or placebo, whereas the efficacy of atenolol and placebo did not differ significantly. Patients were also prospectively divided into generalized and discrete subtypes of social phobia. Phenelzine appeared to be a particularly effective treatment for the generalized form of social phobia. Atenolol may be useful for discrete forms of social phobia such as performance anxiety.     

Distribution coefficients of atenolol and sotalol

The distribution coefficient (D) of atenolol is lower than that of sotalol, despite the latter's lower partition coefficient (P). Since D is the relevant quantity under physiological conditions, it is re-established that atenolol is in practice the more hydrophilic. Because of the common confusion between P and D which this case exemplifies, the relation between them is set out.