计算机辅助褶合曲线分析法测定茶苯海明含量

本文采用计算机辅助褶合曲线分析法不经分离分别测定了茶苯海明原料中8-氯茶碱和苯海拉明以及片剂中8-氯茶碱与苯海拉明复盐的含量,平均回收率和变异系数分别为100.1,0.04%(8-氯茶碱)和102.4,1.34%(苯海拉明)。五批商品测定值与中国药典(1985年版)结果一致。     

茶苯海明片溶出度的实验研究

本实验参照美国药典21版规定标准考察了国产八批茶苯海明片的溶出度,对其溶出参数T_(?)、T_(?)值进行了方差分析,经实验认为T_(50)、T_d值与崩解时限间具有高度相关性(P<0.01),同时对国内同类产品的溶出度提出了参考标准。     

The effects of diazepam or diphenhydramine on healthy human subjects

The immediate effects on the mood and some mental and physical functions of a single oral dose of diazepam (10 mg) and diphenhydramine (50 mg) compared with placebo were studied in healthy human subjects. The material comprised 270 students divided into three similar groups. The mood was tested by the Nowlis adjective check list. The digit symbol test and number series were used to test the mental condition.The major significant results of the study were: diazepam decreased activity both in men and women and sociability in women. It increased euphoria in men and depressivity and withdrawing in women. It impaired the results in the digit symbol test and the ability to repeat the number series in both men and women. Diphenhydramine also decreased activity in men and women. It caused some euphoria in men. It had a slighter depressing effect than diazepam on the mental functions.The many different effects in women as compared with men did not seem to be caused only by larger dose per kg given to the former. This was confirmed by an additional study in which a smaller group of men was given the same dose/kg of the drugs as the women in the main study, and vice versa.     

Pharmacokinetic aspects of the sublingual administration of vincamine

The sublingual absorption of vincamine used as tracer occurs in two successive absorption steps: true sublingual absorption and absorption in the gastrointestinal tract of the drug dissolved in the saliva and not absorbed through the buccal mucosa. This is confirmed by a pharmacokinetic study and simulation. These two successive absorptions can explain the increase in the amounts of drug absorbed.     

苯海拉明软膏中盐酸苯海拉明的含量测定

目的：建立苯海拉明软膏中盐酸苯海拉明的含量测定方法。方法比较铬酸钾指示剂法和酸碱滴定法的线性、精密度和回收率。结果铬酸钾指示剂法中,盐酸苯海拉明在3.99~19.94 mg/ml范围内有良好的线性关系, r=0.9999;平均回收率为97.15%, RSD为1.59%。酸碱滴定法中盐酸苯海拉明在4.06~20.32 mg/ml范围呈现良好的线性关系, r=0.9993;平均回收率为98.90%, RSD=0.84%。结论酸碱滴定法准确、可靠,可用于苯海拉明软膏中盐酸苯海拉明的含量测定。     

茶苯海明口腔崩解片及其普通片在恒河猴体内的药代动力学比较

目的：比较茶苯海明口腔崩解片及其普通片在恒河猴体内的药代动力学特征。方法：采用随机、自身对照方法考察两制剂在恒河猴体内的药代动力学特点;采用HPLC-UV法测定分别口服给予相应剂量的药物（均为茶苯海明50 mg）后恒河猴体内血药浓度;并采用DAS2.0对药代动力学参数进行统计分析。结果：茶苯海明口腔崩解片相对生物利用度（F0-12h,F0-∞）分别为（154±42）%和（150±53）%。两制剂间的血药浓度时间-曲线下面积（AUC0-∞）差异无统计学意义（P〉0.05）,而Cmax和AUC0-12差异有统计学意义（P〈0.05）。此外,茶苯海明口腔崩解片tmax与普通片比较明显缩短,但差异无统计学意义（P〉0.05）。茶苯海明在恒河猴空白血浆中10～2000 ng/mL浓度范围内线性良好（r=0.99995）,最低检测限（LLOQ）10 ng/mL。其他确证数据如准确度、精密度等均在要求范围内。结论：茶苯海明口腔崩解片在体内吸收比普通片快。     

苯海拉明软膏微生物限度检查方法的验证

目的：建立苯海拉明软膏微生物限度检查方法。方法采用常规法进行细菌、霉菌及酵母菌计数方法的验证和控制菌检查的验证。结果采用常规法,细菌、霉菌及酵母菌的回收率均〉70%,并可检出铜绿假单胞菌和金黄色葡萄球菌。结论经方法学验证,结果符合现行《中国药典》2010年版的要求。     

Effects of desloratadine,diphenhydramine, and placebo on driving performance and psychomotor performance measurements

Introduction First-generation antihistamines taken for relief of allergic rhinitis are sedating and pose potential risks for those driving a car or operating machinery. Desloratadine is a potent, selective, histamine H₁-receptor antagonist that does not easily cross the blood–brain barrier. It is nonsedating at therapeutic doses and should not affect driving or psychomotor performance.Objective This study compared the acute effects of desloratadine with diphenhydramine (active control) and placebo on the performance of healthy subjects evaluated with standard over-the-road driving tests (primary objective). The subjects performances were also evaluated (secondary objective) with the use of conventional performance tests.Methods Eighteen men and women received a single dose of desloratadine 5 mg, diphenhydramine 50 mg, or placebo during each period of this randomized, double-blind, three-way, crossover study. Two hours post-dosing, subjects operated a specially instrumented vehicle in a 90-min test designed to measure their ability (1) to maintain constant speed and lateral position while following another vehicle at a constant distance and (2) to respond to brake signals. Additionally, a full battery of performance tests was administered.Results No significant differences were noted between desloratadine and placebo in standard deviation of lateral position (SDLP), whereas diphenhydramine treatment significantly increased SDLP (P<0.001 for both comparisons). Brake reaction time was significantly faster following treatment with desloratadine than diphenhydramine (473.72 ms vs 541.22 ms; P<0.001) or placebo (512.06 ms; P=0.033). No differences were seen among treatments in deviation of speed or distance to the lead car. The majority of performance tests showed no significant differences among groups.Conclusion Desloratadine at a therapeutic dose does not impair driving performance.     

复方利巴韦林滴鼻剂中主药的含量测定

目的建立复方利巴韦林滴鼻剂中主药的含量测定方法。方法以ZORBAX SB-CN(250mm×4.6mm,5μm)色谱柱,乙腈-水-磷酸(38∶62∶0.1)为流动相测定利巴韦林和盐酸苯海拉明的含量。检测波长为224nm,流速为1.0mL.m in-1。结果利巴韦林在0.1~1.0 mg.mL-1浓度范围有良好的线性关系,r=0.9990;平均回收率为100.3%,RSD=0.62%(n=9);盐酸苯海拉明回收率为100.8%,RSD=0.54%(n=9)。结论含量测定方法简单、准确和有效。     

Side effects of anti-emetics: results of a class experiment

A number of standard anti-emetic drugs (perphenazine, promethazine, propiomazine, thiethylperazine, hyoscine, cyclizine, dimenhydrinate, metoclopramide) and a placebo were given by intramuscular injection to students in a clinical pharmacology class to allow them to study side effects. Students proved to be sensitive detectors of the subjective side effects and the placebo response rate was low. Drowsiness was the commonest and most marked side effect; the extra-pyramidal effects were confined to the phenothiaziness, and dizziness and dryness of mouth were frequent only after hyoscine. Cardiovascular effects were trivial and only slight bradycardia was noted with all substances administered. The undesired actions of the phenothiazines lasted longer than those of cyclizine and hyoscine. The frequency of side-effects of anti-emetic drugs is so high that they must be balanced against efficacy in choosing an anti-emetic for a particular situation.     

Novel Use of Dexmedetomidine for the Treatment of Anticholinergic Toxidrome

Introduction

We report the case of an adolescent with anticholinergic toxidrome from diphenhydramine overdose, whose symptoms were treated with a novel application of dexmedetomidine.

Case Report

A 13-year-old female developed an anticholinergic toxidrome after intentionally ingesting 9.5 mg/kg of diphenhydramine. Despite routine supportive therapies, to include appropriate doses of lorazepam, she continued to have significant agitation, psychosis, and hallucinations. A dexmedetomidine infusion was started to aid in the treatment of her agitation and psychosis with marked improvement of her symptoms.

Discussion

Using dexmedetomidine for the treatment of anticholinergic toxidrome has not been previously described in the literature, but there are multiple reports of its use in alcohol withdrawal syndrome. We suggest that adding dexmedetomidine as an adjunctive agent in the therapy of anticholinergic toxidrome may relieve the symptoms of agitation, psychosis, tachycardia, and hypertension, without the attendant risk of respiratory depression associated with high doses of benzodiazepines.     

盐酸苯海拉明片在中国健康人体内的药动学研究

目的研究盐酸苯海拉明片在中国健康人体内的药动学。方法采用高效液相色谱-质谱法,以右美沙芬为内标,血样经液-液萃取后进样,电离源为ES+,选择性离子监测(SIR),苯海拉明及内标的M/Z分别为256.0、272.2。结果苯海拉明不受杂质干扰,线性范围浓度为3.33~200.00ng/ml;萃取回收率均大于90%,方法回收率均在80%~120%内,日内、日间精密度均小于15%。单次服用100mg盐酸苯海拉明片的AUC0~34为(770.37±251.64)(ng.h)/ml,AUC0~∞为(870.92±290.50)(ng.h)/ml,Cmax为(72.25±27.47)ng/ml,tmax为(2.99±0.91)h,t1/2为(9.89±2.04)h。结论盐酸苯海拉明片在中国健康人体中口服吸收快,消除较慢。     

光纤药物溶出原位过程监测仪评价茶苯海明片的体外溶出度

目的:使用光纤药物溶出原位过程监测仪实时监测不同厂家及批号的茶苯海明片的体外溶出度,以评价其工艺质量。方法:监测仪设置条件为测定波长278nm、基准校正波长550nm,光纤探头规格为2mm,温度37℃,转速50r·min-1,数据采集间隔时间30s,介质为水900mL;采用桨法测定各样品溶出度,并与《中国药典》法比较。结果:监测仪测定结果表明,茶苯海明片所有样品溶出度均符合《中国药典》的相关规定,但溶出曲线不同,即溶出过程存在差异;同一批号的样品采用监测仪及药典法测定虽然45min时的溶出度结果比较无显著性差异,但溶出曲线有差异。结论:与《中国药典》法比较,光纤药物溶出实时监测仪可准确连续地反映药物的溶出过程,获得的数据更加完整、真实,可用于评价产品的体外溶出过程。     

盐酸苯海拉明乳膏的制备及质量控制

目的：制备盐酸苯海拉明乳膏,并建立质量控制方法。方法：用水包油型基质制备本品,以高效液相色谱法测定盐酸苯海拉明的含量,并建立相关质控指标。结果：盐酸苯海拉明线性范围为0．1—3．2μg,线性关系良好（r=0．9999）,平均回收率为97．83％,RSD为0．84％。结论：处方及制备工艺合理可行。质量标准可靠、全面,可用于本品的质量控制。     

高效液相色谱法同时测定丁苯乳膏中两组分的含量

应用高效液相色谱法同时测定丁苯乳膏中丁酸氢化可的松和盐酸苯海拉明含量.色谱条件为:色谱柱:XTerra RP C18(250 mm×4.6 mm,5 mm);流动相:甲醇-乙腈-0.5％醋酸铵溶液(35∶27∶38);流速:1.0 mL·min-1;检测波长:232 nm.丁酸氢化可的松及盐酸苯海拉明在125～250 μg· mL-1及25～50 μg·mL-1范围内线性关系良好,表明应用HPLC法可同时测定该制剂丁酸氢化可的松及盐酸苯海拉明的含量.     

微创疗法治疗舌下腺囊肿的临床效果评价

目的 探讨应用平阳霉素联合地塞米松治疗舌下腺囊肿的疗效.方法 应用平阳霉素及地塞米松治疗舌下腺囊肿患者120例,平阳霉素1支(8mg),地塞米松1支(5mg)加入到2%盐酸利多卡因3ml中,混合液终浓度为每1ml溶液中含平阳霉素2mg、地塞米松1.25mg,囊肿腔内注射,酌情给药.7d注射1次,3次为1疗程.囊肿完全消失者为治愈;囊肿缩小,但不能完全消失或需要手术辅助治愈者为好转.结果 治愈109例(90.8%),好转11例(9.2%).结论 应用平阳霉素联合地塞米松局部注射治疗舌下腺囊肿,可作为不能耐受手术治疗患者的首选.     

分光光度法间接测定扑尔敏、盐酸苯海拉明和咳必清

本文制定了扑尔敏、盐酸苯海拉明和咳必清的铜-锌-药物三元络合物的氯仿提取液的分光光度测定法,测定波长615nm,药物浓度在10-50μg/ml范围内呈线性。扑尔敏平均百分回收率100.3%,标准误差0.01。进一步采用连续变化方法确定络合物组成比为1:1:1,同时用薄层层析法加以鉴别。酸性和中性共存药物以及常用赋形剂对本法无干扰,故可用于上述药物在制剂中的测定。     

Abuse liability and stimulant properties of dextromethorphan and diphenhydramine combinations in rats

Rationale The abuse of over-the-counter (OTC) medications has been widely reported. However, there are few preclinical studies examining the behavioral effects of OTC medications at higher, abused doses.Objectives The objectives of the current study were to determine whether the anti-histamine diphenhydramine (DIP) and the antitussive dextromethorphan (DEX), either alone or in combination, would have stimulant properties and be self-administered in animals.Methods For drug self-administration, naive rats with no history of exposure to other drugs were trained to self-administer IV DEX+DIP (0.5+0.5, 1+1 or 2+2 mg/kg per injection), DEX alone (1 mg/kg) or DIP (1 mg/kg) alone under five-response fixed-ratio (FR) schedule with a 30-s time-out after each injection in 2-h sessions 3–5 days a week. Separate groups of rats were tested on locomotor activity. After 8 consecutive days of habituation, naive rats were injected with 3, 10, or 30 mg/kg DEX or DIP alone IP, or in combination of 3+3 mg/kg, 10+10 mg/kg, or 30+30 mg/kg DEX+DIP IP. Saline was injected IP during the intervening days. Locomotor activity was measured for each session.Results DEX+DIP combinations were self-administered, but the drugs alone were not. The acquisition of DEX+DIP self-administration was rapid with a majority of rats reaching the final FR5 schedule in 22–23 sessions. The total IV combination dose for each final scheduled session ranged from 40 mg/kg to 160 mg/kg DEX+DIP. Significant increases in locomotor activity were observed for DIP, an effect that was significantly enhanced when DIP was given in combination with DEX. Significant mortality was also observed for the drug combination at each dose tested when given IV, with the highest mortality following the highest dose (2+2 mg/kg). When given IP, no mortality was observed.Conclusions These results show that combinations of DEX and DIP have stimulant properties and are self-administered by animals. Abuse of this combination in humans would be expected.     

HPLC法测定盐酸苯海拉明乳膏的含量

目的：建立测定盐酸苯海拉明乳膏含量的方法。方法：采用HPLC法,色谱柱：Platisil C18柱（250 mm×4.6 mm,5μm）;流动相：乙腈-水-三乙胺（50∶50∶0.5）;检测波长：258 nm;流速：0.8 m L·min^-1;柱温：40℃。结果：盐酸苯海拉明与其它杂质峰分离良好。盐酸苯海拉明在125.0-1 000.0μg·m L^-1范围内与峰面积呈良好的线性关系（r=1.000 0）;盐酸苯海拉明的平均回收率为98.18%,RSD=0.40%（n=9）。结论：本方法简便、准确、重复性好,可用于盐酸苯海拉明乳膏的含量测定。