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Study on the interaction between diphenhydramine and erythrosin by absorption,fluorescence and resonance Rayleigh scattering spectra

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Science China Chemistry 2007年第1期50卷 54-62页

作者： TANG XiaoLing LIU ZhongFang LIU ShaoPu HU XiaoLi School of Chemistry and Chemical Engineering Southwest China UniversityChongqing 400715China

In pH 4.5 Britton-Robinson(BR)buffer solution,erythrosin(ET)can react with diphenhydramine(DP)to form a 1:1 ion-association complex,which not only results in the change of the absorption spectra,but also results in the great enhancement of resonance Rayleigh scattering(RRS)and the quenching of ***,a new RRS spectrum will appear,and the maximum RRS wavelength was located at about 580 *** this work,the spectral characteristics of the absorption,fluorescence and RRS,the optimum conditions of the reaction and the properties of an analytical chemistry were inves- tigated.A sensitive,simple and new method for the determination of DP by using erythrosin as a probe has been *** detection limits for DP were 0.0020μg/mL for RRS method,0.088μg/mL for absorption method and 0.094μg/mL for *** was a linear relationship between the absorbance,RRS and fluorescence intensities and the drug concentration in the range of 0.0067-2.0, 0.29-6.4 and 0.31-3.2μg/mL,*** effects of the interaction of diphenhydramine and erythrosin on the absorption,fluorescence and resonance Rayleigh scattering spectra were discussed. In light polarization experiment,the polarization of RRS at maximum wavelength was measured to be P =0.9779,and it revealed that the RRS spectrum of DP-ET complex consists mostly of resonance scat- tering and few resonance *** this study,enthalpy of formation and mean polarizability were calculated by AM1 quantum chemistry *** addition,the reaction mechanism and the rea- sons for the enhancement of scattering spectra and the energy transfer between absorption,fluores- cence and RRS were discussed.

关键词： resonance Rayleigh scattering spectrophotometry fluorescence quenching method diphenhydramine erythrosin

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Preparation and Characterization of Orally Fast-Disintegrating Mini-Tablets Containing diphenhydramine Hydrochloride and Aspartic or Glutamic Acid as an Umami Amino Acid

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Pharmacology & Pharmacy 2021年第12期12卷 283-292页

作者： Kyoko Ohkawa Haruka Nishikawa Honami Kojima Takayoshi Okuno Rio Uno Miyako Yoshida Takahiro Uchida Faculty of Pharmaceutical Sciences Mukogawa Women’s University Nishinomiya Japan

The aim of this study was to prepare diphenhydramine hydrochloride (DPH)-loaded orally fast-disintegrating mini-tablets (OFDMTs) containing either L-aspartic acid (Asp) or L-glutamic acid (Glu) as bitterness-suppressant, to characterize the prepared tablets and to evaluate their bitterness under conditions mimicking those of the oral cavity. The preparation of five formulation batches of the OFDMTs involved mixing DPH, with or without two different concentrations of Asp or Glu, and a premix containing a disintegrating agent. When all ingredients were well mixed, the mixture was directly compacted to form small (4 mm diameter) DPH-loaded OFDMTs. There were only small differences between the tablets with respect to mass, diameter, width and hardness. The disintegration times of the five formulation batches of DPH-loaded OFDMTs were measured using the OD-mate, a disintegration test apparatus in which conditions resemble those of the oral cavity. The disintegration times were all within 10 s of exposure to a medium representing the inside of the oral cavity. Rapid release profiles were observed for DPH, Asp and Glu in these dissolution tests. The taste sensor outputs of samples taken at different times (5 - 30 s) from the dissolution test solutions of the four DPH-loaded OFDMTs containing Asp or Glu were significantly inhibited compared with those of control DPH-loaded OFDMT. These results suggest that the inclusion of Asp or Glu in DPH-loaded OFDMTs is sufficient to mask bitterness in the oral cavity for the first 30 s after the tablet is placed in the mouth. It is anticipated that swallowing will have taken place within 30 s.

关键词： Orally Fast Disintegrating Mini-Tablets diphenhydramine Aspartic Acid Glutamic Acid OD-Mate

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Antihistamines mepyramine and diphenhydramine inhibit KCNQ/M currents and lead to depolarization of neuron membrane potential

Antihistamines mepyramine and diphenhydramine inhibit KCNQ/M...

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中国神经科学学会第四次会员代表大会暨第七届全国学术会议

作者： Bo-Yi LIU,Hai-Lin ZHANG Department of Pharmacology,Hebei Medical University Shijiazhuang 050017,China

The first-generation antihistamines are widely prescribed medications to relieve allergic reactions and urticaria by blocking the peripheral histamine H1 *** of these drugs often results in serious neuronal toxic effects, including seizures,convulsions and worsening of epileptic *** now,the molecular mechanism underlying these adverse effects has not been fully ***/M K+ channel plays a crucial role in controlling neuron ***,we demonstrate that mepyramine and diphenhydramine,two structurally related first-generation antihistamines,can act as potent KCNQ/M channel *** application of these drugs quickly and reversibly reduced KCNQ2/Q3 currents heterologously expressed in HEK293 *** current inhibition was concentration and voltage *** estimated IC50(12.5 and 48.1μmol/L,respectively) is within the scope of drug concentrations detected in poisoned patients(30 to 300μmol/L).Both drugs shifted the I-V curve of KCNQ2/Q3 channel to more depolarized potentials,and altered channel gating property by prolonging activation and shortening deactivation kinetics. Mepyramine also inhibited the individual homomeric KCNQ1-3 currents in similar potencies,suggesting little selectivity among KCNQ *** inhibitory effects of mepyramine were not observed when it was applied intracellularly,and were not affected by blocking phospholipase C(PLC) activity,indicating an extracellular and direct channel blocking ***,in cultured rat superior cervical ganglion(SCG) neurons,mepyramine reduced the M type Kcurrent in a concentration dependent manner,and led to a marked and reversible membrane potential depolarization,providing a possible mechanism for the neuroexcitatory adverse effects observed in patients intoxicated with overdose antihistamines.

关键词： mepyramine diphenhydramine patch clamp M-current modulation

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Effects of oral premedication on cognitive status of elderly patients undergoing cardiac catheterization

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Journal of Geriatric Cardiology 2015年第3期12卷 257-262页

作者： Javed M Ashraf Marc Schweigel Neelima Vallurupalli Sandra Bellantonio James R Cook Department of Cardiology Truman Medical Center UMKC School of Medicine Kansas City MO USA Departments of Cardiology Baystate Medical Center Tufts University School of Medicine MA USA Department of Internal Medicine and Geriatrics Baystate Medical Center Tufts University School of Medicine Springfield MA USA

Background Sedatives and analgesics are often administered to achieve conscious sedation for diagnostic and therapeutic procedures. Appropriate concerns have been raised regarding post procedure delirium related to peri-procedural medication in the elderly. The objective of this study was to investigate the effect of premedication on new onset delirium and procedural care in elderly patients. Methods Patients 〉 70 years old and scheduled for elective cardiac catheterization were randomly assigned to receive either oral diphenhydramine and diaze- pam （25 rag/5 mg） or no premedication. All patients underwent a mini mental state exam and delirium assessment using confusion assess- ment method prior to the procedure and repeated at 4 h after the procedure and prior to discharge. Patients＇ cooperation during the procedure and ease of post-procedure were measured using Visual Analog Scale （VAS）. The degree of alertness was assessed immediately on arrival to the floor, and twice hourly afterwards using Observer＇s Assessment of Alermess/Sedation Scale （OAA/S）. Results A total of 93 patients were enrolled. The mean age was 77 years, and 47 patients received premedication prior to the procedure. None of the patients in either group developed delirium. Patients＇ cooperation and the ease of procedure was greater and pain medication requirement less both during and after the procedure in the pre-medicated group （P 〈 0.05 for both）. Nurses reported an improvement with patient management in the pre-medicated group （P = 0.08）. Conclusions In conclusion, prcmedication did not cause delirium in elderly patients undergoing cardiac catheterization. The reduced pain medication requirement, perceived procedural ease and post procedure management favors premedication in elderly patients undergoing cardiac catheterization.

关键词： Cardiac catheterization diphenhydramine Diazepam Delirium The elderly

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A Study on Hypotensive Action of Total Saponin of Ziziphus Jujuba Mill and Its Mechanism

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Journal of Medical Colleges of PLA 1987年第4期 315-318页

作者：古维新刘菊芳张家新刘小明刘胜家陈月蓉 Department of Pharmacology First Medical College of PLA. Guangzhou Department of Pharmacology First Medical College of PLA. Guangzhou Department of Chemistry Xi’an Medical University Xi’an

Total saponin of Ziziphus Jujuba Mill seeds(ZS) produced amarked hvpotensive effect in anesthetized Sprague-Dawley rats(I. V. or I. P. )and cats (I. V. ). ZS showed no effect on the pressor effect of nor-adrenalinein rats. the depressor effect of ZS was not influenced by atropine nor bydiphenhydramine. ZS markedly inhibited the pressor reflex in catsinduced by ocelusion of the common carotid artery. In rats, ZS inhibitedthe spontaneous discharges of the preganglionic fibers of the greatersplanchnic nerve and decreased the plasma renin activity. These resultsshowed that the hypotensive action of ZS was probably central in origin.

关键词： total saponin of Ziziphus Jujuba Mill hypotensive effect atropine noradrenaline diphenhydramine spontaneous discharge plasma renin activity

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