AIMTo establish an HPLC-fluorescent spectrometric method for the determination of mexiletine hydrochloride in plasma after derivatization with fluram.

METHODSFluram acetone solution was added to the deproteinized plasma with acetone to obtain the derivative of mexiletine. The HPLC method was performed on a column of Allitima C18 (150 mm x 4.6 mm, 5 microns) with the mobile phase of methanol-water-diethylamine-phosphoric acid buffer (2.4 mol.L-1, pH 4.0) (70:28:2), and the detective wavelength were set at Ex 392 nm and Em 480 nm.

RESULTSMexiletine has a liner range over the concentration range from 0.100-6.400 mg.L-1. The lowest detectable concentration of this method was 5 micrograms.L-1 (S/N > or = 4). The intra-day and inter-day RSDs were 1.34%-5.31%, respectively.

CONCLUSIONThis method is simple, selective and can be used for therapeutic drug monitoring (TDM) and pharmacokinetic studies of mexiletine.

Anti-Arrhythmia Agents ; blood ; pharmacokinetics ; Chromatography, High Pressure Liquid ; methods ; Fluorescamine ; chemistry ; Humans ; Mexiletine ; blood ; pharmacokinetics

This paper reviewed the advances on effective constituents and biological activities of coumarins in recent ten years. Coumarins are a group of important natural compounds, and have been found to have multi-biological activities such as anti-HIV, anti-tumor, anti-hypertension, anti-arrhythmia, anti-osteoporosis, assuaging pain, preventing asthma and antisepsis. Therefore, further investigation should emphasize on improving techniques for extraction and separation, searching the effective precursory compound, and synthesizing and screening out courmarin derivatives with high activity and low toxicity.
Animals ; Anti-Arrhythmia Agents ; pharmacology ; Anti-HIV Agents ; pharmacology ; Antihypertensive Agents ; pharmacology ; Antineoplastic Agents, Phytogenic ; pharmacology ; Coumarins ; isolation & purification ; pharmacology ; Humans ; Plants, Medicinal ; chemistry

To further understand sinomenine, this paper has introduced the abstract technology, assaying, pharmaceutical chemistry, pharmacological action, pharmacotoxicology, pharmacokinetics and clinical application of sinomenine based on the important and significant contents of reference which have been consulted in the past ten years. Sinomenine is a kind of non-steroidal anti-inflammatory drugs with very effective and little side effect and expected it as a good new drug withdrawal medicine in the future.
Animals ; Anti-Arrhythmia Agents ; pharmacology ; Anti-Inflammatory Agents, Non-Steroidal ; pharmacology ; Antirheumatic Agents ; pharmacology ; Humans ; Morphinans ; isolation & purification ; pharmacokinetics ; pharmacology ; toxicity ; Plant Roots ; chemistry ; Plants, Medicinal ; chemistry ; Sinomenium ; chemistry ; Technology, Pharmaceutical ; methods

OBJECTIVE: To establish a liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for detection of mexiletine by liquid chromatography tandem mass spectrometry. METHODS: After simple protein precipitation of the blood sample with acetonitrile, the organic solvent layer diluted with LC mobile solvent was separated by Allure PFP Propyl column, confirmed and quantified by MS/MS in the multi-reaction monitoring (MRM) mode via positive electrospray ionization. RESULTS: Mexiletine and naloxone (internal standard) got ideal resolution under the selected analytical condition. The correlation coeficient of linear calibration curve was over 0.9999 within the mexiletine concentration range 0.02-10 microg/mL. The relative standard deviations were under 10% for intra-day and under 15% for inter-day, and the detection limit was 0.01 microg/mL. CONCLUSION The established LC-MS/MS method is simple, rapid, sensitive, unaffected by matrix effect and appropriate for detection of mexiletine in blood in the field of therapeutic drug monitoring and forensic toxicology.
Anti-Arrhythmia Agents/chemistry* ; Forensic Medicine ; Humans ; Mexiletine/poisoning* ; Molecular Structure ; Naloxone/chemistry* ; Reproducibility of Results ; Sensitivity and Specificity ; Spectrometry, Mass, Electrospray Ionization/methods* ; Tandem Mass Spectrometry/methods*

OBJECTIVEThe progress in the research on matrine was involved to provide references for the exploitation and utilization of the matrine.

METHODPharmacological functions and mechanism were reviewed according to related experimental studies.

RESULTMatrine has various pharmacological activities.

CONCLUSIONMatrine has extensive applied prospect and will be developed further.

Alkaloids ; isolation & purification ; pharmacology ; Animals ; Anti-Arrhythmia Agents ; pharmacology ; Anti-Inflammatory Agents, Non-Steroidal ; pharmacology ; Antineoplastic Agents, Phytogenic ; pharmacology ; Drugs, Chinese Herbal ; isolation & purification ; pharmacology ; Plants, Medicinal ; chemistry ; Quinolizines ; Sophora ; chemistry

OBJECTIVETo study the plasma concentration-time curve, pharmacokinetic parameters and bioavilability of oxymatrine-phospholipid complex and to compare with oxymatrine in rats.

METHODRats were given oxymatrine-phospholipid 100 mg x kg(-1). Blood samples were collected at different times after oral administration. The internal standard was cimetidine. Protein in plasma was precipitated with merhanol and centrifuged at high speed. The supernatant was directly injected and assayed by CE method. The running buffer was 0.04 mol x L(-1) Tris-10 mmol x L(-1) sodium phosphate monobasic-40% isopropanol pH to 7.6 with phosphoric acid. The wavelength of detection was 205 nm.

RESULTThe AUC of oxymatrine and oxymatrine-phospholipid complex were 4.52 mg x mL(-1) x h(-1) and 6.21 mg x mL(-1) x h(-1), respectively. The oxymatrine-phospholipid bioavailability enhanced 1.4 times.

CONCLUSIONIt is concluded that after oral administration of oxymatrine-phospholipid complex in rats the bioavailability of oxymatrine is increased greatly. This is mainly due to an obvious improvement of the lipophilic property of oxymatrine-phospholipid complex compared with oxymatrine material and an increase in gastrointestinal absorption.

Administration, Oral ; Alkaloids ; administration & dosage ; chemistry ; pharmacokinetics ; Animals ; Anti-Arrhythmia Agents ; administration & dosage ; chemistry ; pharmacokinetics ; Area Under Curve ; Biological Availability ; Male ; Phospholipids ; chemistry ; Plants, Medicinal ; chemistry ; Quinolizines ; administration & dosage ; chemistry ; pharmacokinetics ; Rats ; Rats, Wistar ; Sophora ; chemistry

To summarize the new progress of the study about volatile oil of the angelica, including the distillable methods, the analysis of the chemical components, the pharmacological effects and the clinical applications. We tracked and searched the correlative references and study reports about volatile oil of the angelica in CNKI data base(1994-2004) and Medline data base (1997-2004). We summarized and compared the different distillable methods of volatile oil of the angelica, meanwhile we summarized many study reports about the analysis of the chemical components of volatile oil of the angelica and it's pharmacological effects, including the toxicity of the volatile oil and it's effects on the uterus smooth muscle, cardiovascular system, respiratory system, central nerve system and immune system. Finally we summarized the clinical application of the volatile oil of the angelica. There are three distillable methods of volatile oil of the angelica . The harvest efficiency of volatile oil is different with different distillable methods. The chemical components are very complicated and the new chemical components are separated and identified. The volatile oil has bidirectional effects on the uterus smooth muscle. It can inhibit the contraction of the uterus smooth muscle induced by different mechanisms. Meanwhile it can depress the blood pressure and ameliorate the cardiac ischemia. The volatile oil can resist the arrhythmia and asthma, restrain the central system, improve the immune function. Nowadays the volatile oil of the angelica is applied to therapy the dysmenorrhea and disorder of the catamenia. The chemical components of the volatile oil of the angelica are very complicated, moreover the pharmacological effects of the volatile oil are comprehensive. People make the new progress of the study about volatile oil of the angelica.
4-Butyrolactone ; analogs & derivatives ; isolation & purification ; pharmacology ; Angelica ; chemistry ; Animals ; Anti-Arrhythmia Agents ; pharmacology ; Anti-Asthmatic Agents ; pharmacology ; Anti-Inflammatory Agents, Non-Steroidal ; pharmacology ; Blood Pressure ; drug effects ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; pharmacology ; Dysmenorrhea ; drug therapy ; Female ; Humans ; Male ; Muscle Contraction ; drug effects ; Muscle, Smooth ; drug effects ; Oils, Volatile ; chemistry ; isolation & purification ; pharmacology ; Plants, Medicinal ; chemistry ; Uterus ; drug effects

OBJECTIVETo observe the effect of Puerarin on L-type calcium channel in isolated rat ventricular myocytes.

METHODThe cardiac ventricular myocytes were isolated enzymatically by Langendorff perfusion techniques at constant flow rate. Whole-cell recording of patch-clamp techniques was used to observe the current of L-type calcium channel.

RESULTPuerarin 2.4 mmol x L(-1) could inhibit the current of L-type calcium channel of rat ventricular myocytes and this inhibition was time-dependent. Purerarin elevated the current-voltage (I-V) curve of calcium current.

CONCLUSIONPuerarin can inhibit L-type calcium current of rat ventricular myocytes. Which implies that puerarin takes part in anti-myocardial ischemia and anti-arrhythmics partly due to the inhibition of L-type calcium channel.

Animals ; Anti-Arrhythmia Agents ; isolation & purification ; pharmacology ; Calcium Channels, L-Type ; drug effects ; Cell Separation ; Heart Ventricles ; cytology ; Isoflavones ; isolation & purification ; pharmacology ; Male ; Myocytes, Cardiac ; metabolism ; Patch-Clamp Techniques ; Plants, Medicinal ; chemistry ; Pueraria ; chemistry ; Rats ; Rats, Sprague-Dawley

OBJECTIVETo investigate the effect of ethyl acetate extract from Chrysanthemum Morifolium Ramat (CME) on experimental arrhythmia induced by ischemia/reperfusion or aconitine in rats and to explore its underlying mechanisms.

METHODSArrhythmia model in intact rat was induced by aconitine (30 microg/kg body weight, i.v.). In isolated Langendorff perfused rat hearts, regional ischemia and reperfusion was induced by ligation and release of left anterior descending artery. The ventricular fibrillation threshold (VFT), effective refractory period (ERP), and diastolic excitation threshold (DET) in the isolated heart were measured. The action potentials of papillary muscle in rat right ventricle were recorded by conventional glass microelectrode technique.

RESULTSCompared with control group CME significantly decreased the number and duration of ventricular tachycardia (VT); delayed the occurrence of ventricular premature beats (VPB) and VT induced by aconitine. Arrhythmia score of the CME group was lower than that in aconitine-treated group. CME markedly prolonged the ERP and increased the VFT in the isolated perfused rat hearts during ischemia and reperfusion. CME prolonged action potential duration at 50% and 90% repolarization of the right ventricular papillary muscles and decreased the maximal rate of rise of the action potential upstroke, but did not affect the resting potential, amplitude of action potential.

CONCLUSIONCME can reduce myocardial vulnerability and exerts its antiarrhythmic effects induced by aconitine or ischemia/reperfusion, which may be related to its prolongation of action potential duration and effective refractory period that enhance the electrophysiological stability of myocardiaium.

Acetates ; chemistry ; Action Potentials ; drug effects ; Animals ; Anti-Arrhythmia Agents ; isolation & purification ; pharmacology ; Arrhythmias, Cardiac ; chemically induced ; physiopathology ; Chrysanthemum ; chemistry ; Drugs, Chinese Herbal ; pharmacology ; In Vitro Techniques ; Male ; Rats ; Rats, Sprague-Dawley ; Refractory Period, Electrophysiological ; drug effects

OBJECTIVETo compare the actions of the three flavone ingredients in choerospondias axillaris on arrhythmias Induced by aconitine.

METHODLangendorff perfuse was applied in the experiment, the antiarrhythmic action was to study by using aconitine on the the isolated heart; The antiarrhythmic action of the three flavone ingredients in choerospondias axillaris was to study by using i.v. aconitine in rat to induce arrhythmias.

RESULTCompared with the NS group, sample 1 and sample 2 both significantly prolonged the beginning time of VF of isolated heart and increased the dosage of aconitine, sample 3 reduced the beginning time of VF of isolated heart and decreased the dosage of aconitine, sample 1 and sample 2 both greatly prolonged the beginning time of VE, VT, VF, HA; sample 3 greatly reduced the beginning time of VT,VF. The actions of the three samples were in a concentration-dependent way.

CONCLUSIONSample 1 and sample 2 both resisted the occurrence of arrhythmias induced by aconitine, sample 3 markedly promoted the occurrence of arrhythmias induced by aconitine.

Aconitine ; Anacardiaceae ; chemistry ; Animals ; Anti-Arrhythmia Agents ; isolation & purification ; therapeutic use ; Arrhythmias, Cardiac ; chemically induced ; prevention & control ; Dose-Response Relationship, Drug ; Female ; Flavones ; isolation & purification ; therapeutic use ; In Vitro Techniques ; Male ; Phytotherapy ; Plants, Medicinal ; chemistry ; Random Allocation ; Rats ; Rats, Wistar