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Trimetazidine Dihydrochloride

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CAT#
10-101-126
Synonyms/Alias
1-(2,3,4-Trimethoxybenzyl)piperazine · 2 HCl
CAS No.
5011-34-7 (net), 13171-25-0 (dihydrochloride)
M.W/Mr.
268.35
Molecular Formula
C14H24N2O3
Source
Synthetic
Application
Trimetazidine is an anti-ischemic (anti-anginal) metabolic agent, which improves myocardial glucose utilization through inhibition of fatty acid metabolism, also known as fatty acid oxidation inhibitor.
Description
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.
Areas of Interest
Ischemic heart disease & Chorioretinal vascular disorders
  • Background
  • Related Products
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Trimetazidine is a cellular acting anti-ischaemic agent. It has 3 main properties by which it acts as a cytoprotective agent. It inhibits the anaerobic glycolysis and fatty acid metabolism, thus allowing only aerobic glycolysis. This action helps to restore the energy balance in the cell. It inhibits acidosis and free radical accumulation in the cell. All these action help the cell to restore the normal ionic and metabolic balance.

CAS: 124584-08-3 (net)
Sequence: H-Ser-Pro-Lys-Met-Val-Gln-Gly-Ser-Gly-Cys-Phe-Gly-Arg-Lys-Met-Asp-Arg-Ile-Ser-Ser-Ser-Ser-Gly-Leu-Gly-Cys-Lys-Val-Leu-Arg-Arg-His-OH Acetate salt (Disulfide bond)
M.W: 3464.09
Molecular Formula: C143H244N50O42S4
CAS: 69-25-0
Sequence: Pyr-Pro-Ser-Lys-Asp-Ala-Phe-Ile-Gly-Leu-Met-NH2
M.W: 1188.4
Molecular Formula: C54H85N13O15S
CAS: 117399-94-7 (net)
Sequence: H-Cys-Ser-Cys-Ser-Ser-Leu-Met-Asp-Lys-Glu-Cys-Val-Tyr-Phe-Cys-His-Leu-Asp-Ile-Ile-Trp-OH acetate salt (Disulfide bonds between Cys1 and Cys15/Cys3 and Cys11)
M.W: 2491.94
Molecular Formula: C109H159N25O32S5
CAS: 138068-37-8 (net)
Sequence: H-Leu-Thr-Tyr-Thr-Asp-Cys-Thr-Glu-Ser-Gly-Gln-Asn-Leu-Cys-Leu-Cys-Glu-Gly-Ser-Asn-Val-Cys-Gly-Gln-Gly-Asn-Lys-Cys-Ile-Leu-Gly-Ser-Asp-Gly-Glu-Lys-Asn-Gln-Cys-Val-Thr-Gly-Glu-Gly-Thr-Pro-Lys-Pro-Gln-Ser-His-Asn-Asp-Gly-Asp-Phe-Glu-Glu-Ile-Pro-Glu-Glu-Tyr-L
M.W: 6979.52
Molecular Formula: C287H440N80O111S6
CAS: 355151-12-1
Sequence: Ac-D-Tyr-D-Pro-D-Hyp-Gly-D-Ala-Gly-NH2
M.W: 617.65
Molecular Formula: C28H39N7O9

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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