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Aryloxypropanolamine is an essential structural scaffold for a variety of β-adrenergic receptor antago-nists such as metoprolol. Molecules with such a structural motif tend to degrade into α, β-hydroxypropanolamine impurities via a radical-initiated oxidation pathway. These impurities are typically polar and nonchromophoric, and are thus often overlooked using traditional reversed phase chromatography and UV detection. In this work, stress testing of metoprolol confirmed the generation of 3-isopropylamino-1,2-propanediol as a degradation product, which is a specified impurity of metoprolol in the European Pharmacopoeia (impurity N). To ensure the safety and quality of metoprolol drug products, hydrophilic interaction chromatography (HILIC) methods using Halo Penta HILIC column (150 mm×4.6 mm, 5 μm) coupled with charged aerosol detection (CAD) were developed and optimized for the separation and quantitation of metoprolol impurity N in metoprolol drug products including metoprolol tartrate injection, metoprolol tartrate tablets, and metoprolol succinate extended-release tablets. These HILIC-CAD methods were validated per USP validation guidelines with respect to speci-ficity, linearity, accuracy, and precision, and have been successfully applied to determine impurity N in metoprolol drug products.
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OBJECTIVE:To establish the method for dissolution determination of Metoprolol tartrate tablets,and to evaluate the similarity of dissolution curves of generics and original drugs. METHODS:The paddle method was adopted with rotational the speed of 50 r/min,using pH 1.2 hydrochloric acid solution,pH 4.5 acetate buffer solution and pH 6.8 phosphate buffer solution as dissolution media. Fiber-optical drug dissolution real-time measurement instrument was used to determine the dissolution curves of generic and original Metoprolol tartrate tablets with optical distance of 10 mm. Similarity factor (f2) method was used to evaluate its similarity. RESULTS:In 3 dissolution mediums,the f2 of generic and original Metoprolon tartrate tablets were 80.5,66.8, 69.4,respectively,which indicated that the dissolution curves showed similarity. CONCLUSIONS:Established real-time dissolution process analysis method is suitabe for the dissolution determination of Metoprolol tartrate tablets. Generic and eriginal show the sim-ilarity in dissolation behavier,so they have good consistency in quality.
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Objective To investigate the therapeutic effect of Danhong injection combined with metoprolol tartrate tablets on cardiac arrhythmia in climacteric women.Methods Retrospective a total of 115 patients with arrhythmia in The First People’s Hospital of Guiyang from May 2014 to May 2016 were divided into the western medicine treatment group and the traditional Chinese and western medicine treatment group.Western medicine treatment group were treated by metoprolol tartrate tablets, the traditional Chinese and western medicine treatment group were treated by Danhong injection combined with metoprolol tartrate tablets.The effect of two groups of patients after two months of treatment were observed,the heart rate variability,heart function index,sleep quality and the incidence of adverse reaction rate were compared between two groups of patients before and after treatment .Results After treatment,the effective rate of the traditional Chinese and western medicine treatment group was 98.33%, higher than the western medicine treatment group (P<0.05);the levels of SDNN,SDANN,RMSSD and PNN50 (%) were significantly higher in the the traditional Chinese and western medicine treatment group than those in the western medicine group (P<0.05);the levels of SV,LVPS and LVEF in the traditional Chinese and western medicine treatment group were higher than that in the western medicine treatment group ( P <0.05 );the sleep quality of the traditional Chinese and western medicine treatment group was significantly improved compared with the western medicine treatment group(P<0.05);the abdominal distension, nausea and vomiting,fatigue and cough incidence were no difference between the two groups.Conclusion Danhong injection combined with metoprolol tartrate tablets arrhythmia in menopausal women has a better therapeutic effect ,can obviously improve the patients with heart rate variability and cardiac function and adverse reactions occurred rate is low.
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Objective To investigate the clinical effects of Metoprolol Tartrate Tablets and Sodium Fructose Diphosphate(FDP) :injection in the early treatment of 48 cases of acute myocardial infarction(AMI) patients with thrombolytic therapy.Methods 84 cases of acute myocardial infarction who were in accordance with the indications for thrombolytic therapy in patients were randomly divided into a treatment group(group A,48 cases,treated with Metoprolol Tartrate Tablets and Sodium Fructose Diphosphate Injection) and a control group(group B,36 cases,treated with the conventional therapy).The occurrence of reperfusion arrhythmias,early sighs and symptms,and retoration of myocardial injury were observed in patients after thrombolytic therapy in order to understand clinical effect on the patients with that treatment.Results In treatment group there were decreased incidence of heart symptoms (chest pain,cardiopalmus) and RA(group A,36.1%;group B,71.4%),improved recovery of cardiac muscde enzymogram as compared to control,which was significantly different with control and between treatment groups (P
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AIM: To study the bioequivalence of domestic and imported Metoprolol Tartrate Tablets in Chinese healthy volunteers.METHODS: According to the rule published by SFDA,the serum concentration of 20 selected volunteers among 18 to 40 years old was determined by HPLC-fluorescence detection after giving domestic and imported Metoprolol Tartrate Tablets 0.1g,and the pharmacokinetic parameters were calculated by DAS software.RESULTS: The method of HPLC-fluorescence detection to study the pharmakokinetics of Metoprolol Tartrate was sensitive,reliable,accurate and reasonable.The main pharmakokinetics parameters of domestic and imported Metoprolol Tartrate Tablets were T_(max):(1.11)?(0.36 h) and(1.39)?(0.65 h) respectively;C_(max):(269.20)?(87.15)(?g?L~(-1)) and(262.03)?(75.52)(?g?L~(-1)) respectively;AUC_(0-12h):(1088.91)?(510.52)(?g?L~(-1)?h) and(1098.29)?5(55.14)(?g?L~(-1)?h) respectively.The relative bioavailability of domestic Metoprolol Tartrate Tablets was(100.09)%.CONCLUSION: The domestic and imported Metoprolol Tartrate Tablets was bioequivalents.