Trimetazidine Dihydrochloride is a 3-ketoacyl-coenzyme, a thiolase inhibitor. It is a cellular antiischemic agent indicated in the management and prophylaxis of angina pectoris.
CAT No: 10-101-126
CAS No:5011-34-7 (net), 13171-25-0 (dihydrochloride)
Synonyms/Alias:1-(2,3,4-Trimethoxybenzyl)piperazine · 2 HCl
Trimetazidine Dihydrochloride is a synthetic piperazine derivative recognized for its unique modulation of cellular energy metabolism, particularly under conditions of ischemic stress. With a well-characterized molecular structure, this compound is widely utilized in research settings to investigate its effects on metabolic pathways within various cell types. Trimetazidine Dihydrochloride is distinguished by its ability to selectively inhibit fatty acid oxidation, thereby promoting a shift toward glucose utilization, which can be advantageous in settings where energy efficiency and cell survival are critically challenged. Researchers value its stability, solubility, and reproducibility, making it a reliable tool for laboratory studies focused on cellular energetics and metabolic adaptation. Its compatibility with a range of in vitro and in vivo models further enhances its versatility for scientific investigation.
Cellular Metabolism Research: Trimetazidine Dihydrochloride is extensively applied in studies aimed at deciphering the intricacies of cellular energy metabolism. By modulating the balance between fatty acid and glucose oxidation, it enables researchers to probe the adaptive responses of cells to metabolic stress, such as hypoxia or nutrient deprivation. This property is particularly valuable in the exploration of mitochondrial function, ATP production, and overall energy efficiency in both normal and pathological states. Utilizing Trimetazidine Dihydrochloride in metabolic assays allows scientists to delineate the molecular mechanisms underlying energy substrate preference, mitochondrial resilience, and the preservation of cell viability under adverse conditions.
Cardiac Ischemia Modeling: In preclinical research focused on cardiovascular health, Trimetazidine Dihydrochloride serves as a key agent for simulating and studying the metabolic alterations associated with ischemic heart conditions. By shifting cardiac energy metabolism from fatty acid oxidation to glucose utilization, it helps to mimic the metabolic environment observed during episodes of reduced oxygen supply. This application aids in the investigation of myocardial cell survival, contractile function, and the identification of potential therapeutic targets for protecting cardiac tissue during ischemic insults. Its use in ex vivo heart perfusion systems and cellular models of ischemia provides valuable insights into the metabolic flexibility and resilience of cardiac tissue.
Neuroprotection Studies: The protective effects of Trimetazidine Dihydrochloride on neuronal cells under metabolic stress have made it a useful compound in neurobiology research. By optimizing energy substrate utilization and reducing oxidative stress, it allows researchers to investigate mechanisms that support neuronal survival during hypoxic or ischemic episodes. Studies employing this compound often focus on mitochondrial function, synaptic integrity, and the modulation of apoptotic pathways in cultured neurons or brain tissue preparations. Such research contributes to a deeper understanding of neuroprotective strategies and the maintenance of central nervous system function under adverse metabolic conditions.
Organ Preservation Research: Trimetazidine Dihydrochloride is also utilized in experimental protocols aimed at enhancing the preservation of organs and tissues destined for transplantation or extended storage. Its ability to maintain cellular energy balance and reduce metabolic stress during hypothermic or ischemic storage conditions is of particular interest. Researchers employ this compound in perfusion solutions and preservation media to assess its impact on tissue viability, mitochondrial function, and recovery following reperfusion. These studies are essential for developing improved strategies for organ preservation and transplantation science.
Pharmacological Mechanism Exploration: Scientists leverage Trimetazidine Dihydrochloride to dissect the pharmacological pathways involved in metabolic modulation and cytoprotection. By acting as a model compound, it facilitates the identification of signaling cascades, enzyme targets, and regulatory networks that govern cell survival under metabolic duress. This application is integral to drug discovery efforts aimed at designing new agents with similar or enhanced metabolic effects. Through detailed mechanistic studies, Trimetazidine Dihydrochloride continues to advance our understanding of cellular adaptation and resilience in the face of metabolic challenges, thereby supporting the development of innovative research tools and therapeutic concepts.
Trimetazidine dihydrochloride is an effective anti-anginal agent; however, it is freely soluble in water and suffers from a relatively short half-life. To solve this encumbrance, it is a prospective candidate for fabricating trimetazidine extended-release formulations. Trimetazidine extended-release floating tablets were prepared using different hydrophilic matrix forming polymers including HPMC 4000 cps, carbopol 971P, polycarbophil, and guar gum. The tablets were fabricated by dry coating technique. In vitro evaluation of the prepared tablets was performed by the determination of the hardness, friability, content uniformity, and weight variation. The floating lag time and floating duration were also evaluated. Release profile of the prepared tablets was performed and analyzed. Furthermore, a stability study of the floating tablets was carried out at three different temperatures over 12 weeks. Finally, in vivo bioavailability study was done on human volunteers. All tablet formulas achieved <0.5 min of floating lag time, more than 12 h of floating duration, and extended t1/2. The drug release in all formulas followed zero-order kinetics. T4 and T8 tablets contained the least polymer concentration and complied with the dissolution requirements for controlled-release dosage forms. These two formulas were selected for further stability studies. T8 exhibited longer expiration date and was chosen for in vivo studies. T8 floating tablets showed an improvement in the drug bioavailability compared to immediate-release tablets (Vastrel® 20 mg).
Abdelbary, A., El-Gazayerly, O. N., El-Gendy, N. A., & Ali, A. A. (2010). Floating tablet of trimetazidine dihydrochloride: an approach for extended release with zero-order kinetics. Aaps Pharmscitech, 11(3), 1058-1067.
Three methods are presented for the determination of trimetazidine dihydrochloride in the presence of its acid-induced degradation products. The first method was based on measurement of first-derivative D1 value of trimetazidine dihydrochloride at 282 nm over a concentration range of 8.00-56.00 microg/mL with mean percentage accuracy of 99.80+/-1.17. The second method was based on first derivative of the ratio spectra DD1 at 282 nm over the same concentration range with the percentage accuracy of 99.14+/-0.68. The third method was based on separation of trimetazidine dihydrochloride from its acid-induced degradation products followed by densitometric measurement of the spots at 215 nm. The separation was performed on silica gel 60 F254 using methanol-ammonia (100+/-1.5, v/v) as mobile phase. This method was applicable for determination of the intact drug in the presence of its degradation products over a concentration range of 2.00-9.00 microg/spot with mean percentage accuracy of 99.86+/-0.92. The proposed methods were successfully applied for the determination of trimetazidine dihydrochloride in bulk powder, laboratory-prepared mixtures containing different percentages of degradation products, and pharmaceutical dosage forms. The validity of results was assessed by applying the standard addition technique. The results obtained agreed statistically with those obtained by the reported method.
Bebawy, L. I., El Tarras, M. F., & El Sabour, S. A. (2004). Determination of trimetazidine dihydrochloride in the presence of its acid-induced degradation products. Journal of AOAC International, 87(4), 827-833.
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