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 role as a metabolic modulator within the field of biochemical and pharmacological research. Structurally, it functions as an inhibitor of fatty acid β-oxidation, promoting a shift toward increased glucose oxidation in cells under metabolic stress. This compound is of significant interest for its ability to influence cellular energy homeostasis, particularly in tissues with high energetic demands such as cardiac and neural cells. Its distinctive mechanism of modulating energy substrate utilization has made it a valuable tool in the study of metabolic adaptation, mitochondrial function, and cellular response to ischemic conditions.
Metabolic modulation studies: Trimetazidine Dihydrochloride is widely applied in research focused on the regulation of cellular metabolism, especially concerning the balance between fatty acid and glucose oxidation. By selectively inhibiting mitochondrial long-chain 3-ketoacyl-CoA thiolase, it enables investigators to dissect the impact of altered substrate preference on cellular energetics and viability. This property is particularly valuable in experimental models designed to simulate metabolic stress, such as hypoxia or nutrient deprivation, providing insights into adaptive mechanisms that maintain ATP production under compromised conditions.
Ischemia and reperfusion research: In cellular and tissue models of ischemia-reperfusion injury, Trimetazidine Dihydrochloride is employed to evaluate the protective effects of metabolic modulation on organ function and cell survival. Its ability to enhance glucose utilization over fatty acid oxidation helps reduce the accumulation of deleterious metabolites and supports maintenance of ionic homeostasis during periods of oxygen deprivation. Researchers utilize this compound to investigate the molecular pathways involved in ischemic tolerance and to identify potential targets for mitigating oxidative stress and tissue damage.
Mitochondrial function analysis: The compound serves as a critical probe in studies examining mitochondrial dynamics, bioenergetics, and oxidative phosphorylation. By modulating the substrate input into mitochondria, Trimetazidine Dihydrochloride allows for the assessment of mitochondrial efficiency and the interplay between different metabolic pathways. Its use in isolated mitochondria, cell cultures, or tissue slices facilitates a deeper understanding of how shifts in substrate utilization affect mitochondrial membrane potential, reactive oxygen species production, and overall cellular health.
Neuroprotection mechanism exploration: Researchers investigating neuroprotection frequently incorporate Trimetazidine Dihydrochloride into experimental models of neuronal injury or neurodegenerative disease. Its metabolic effects are leveraged to study the preservation of neuronal integrity under stress conditions, such as oxidative insult or excitotoxicity. By promoting efficient ATP generation and minimizing metabolic disturbances, the compound aids in elucidating cellular strategies that counteract neuronal dysfunction and degeneration.
Cardiac metabolism research: The use of Trimetazidine Dihydrochloride is instrumental in exploring the metabolic flexibility of cardiac tissue under various physiological and pathophysiological states. It enables detailed investigations into how shifting substrate preference from fatty acids to glucose can influence myocardial efficiency, contractility, and resistance to metabolic stress. These studies contribute to a broader understanding of cardiac bioenergetics and inform the development of novel strategies for protecting cardiac cells during periods of high demand or limited oxygen supply.
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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