Perindopril Erbumine

Inquiry

Cat Number

API0231634

CAS Number

107133-36-8

If you have any other questions, please contact our experts.

Product Detail Description Scientific Support Customer Q&A

CAS Number

107133-36-8

EINECS

600-798-6

Storage

Store at room temperature

Synonyms

ACEON; Perindopril tert-butylamine; McN-A-2833-109; S-9490-3; NSC-758929; DTXSID1044198

Molecular Formula

C23H43N3O5

Molecular Weight

441.6

Smiles

CCC[C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1[C@H]2CCCC[C@H]2C[C@H]1C(=O)O.CC(C)(C)N

Appearance

White to off-white crystalline powder

Melting Point

126-128℃

Boiling Point

537.4℃ at 760 mmHg

Relative Density

1.15

General Description

Perindopril erbumine is a long‑acting angiotensin‑converting enzyme (ACE) inhibitor formulated as the tert‑butylamine salt for improved stability and absorption. It is a prodrug that requires hepatic hydrolysis to its active diacid metabolite, perindoprilat.

Mechanism of Action

Perindoprilat inhibits ACE, preventing conversion of angiotensin I to angiotensin II, a potent vasoconstrictor. Reduced angiotensin II leads to vasodilation, decreased aldosterone secretion, and increased bradykinin levels. The drug has high tissue affinity, particularly for vascular and renal ACE, resulting in sustained blood pressure reduction. The increased bradykinin contributes to vasodilation but also causes dry cough.

Application

Perindopril is indicated for essential hypertension, stable coronary artery disease (reducing cardiovascular events), and heart failure. In the EUROPA trial, perindopril reduced major adverse cardiac events in patients with stable coronary artery disease. It is also used for diabetic nephropathy to slow renal progression.

Perindopril erbumine, an antihypertensive agent, was studied for its thermal behavior and decomposition kinetics using ATR‑FTIR, thermogravimetry, and model‑free kinetic methods. As a pure active pharmaceutical ingredient, its main thermal degradation step showed activation energy of 59–69 kJ/mol. However, in the solid tablet formulation containing colloidal silica, microcrystalline cellulose, lactose, and magnesium stearate, the activation energy rose to approximately 170 kJ/mol, indicating substantially improved thermal stability. The authors conclude that these excipients not only are compatible with perindopril erbumine but also contribute positively to its stability under thermal stress, supporting their use in generic formulations.

Fig. 1 Linear plotting of Kissinger-Akahira-Sunose method at selected heating rates for PERas (a) and PERpf (b). (Buda V, et al., 2017)

References

Buda V, et al. Comparative Solid-State Stability of Perindopril Active Substance vs. Pharmaceutical Formulation. Int J Mol Sci. 2017;18(1):164.

Does Perindopril Erbumine require protection from moisture during storage?

Yes, it is highly susceptible to hydrolysis, forming perindoprilat and diketopiperazine derivatives. Store in tightly sealed, moisture-proof containers with desiccant.

What is the recommended storage temperature for Perindopril Erbumine?

Store at controlled room temperature (15-25°C). Avoid temperatures above 30°C, which accelerate cyclization and hydrolysis.

Is Perindopril Erbumine stable in tablet formulations with common excipients?

Yes, when formulated with moisture-protective packaging (e.g., blisters with desiccant). We provide compatibility data for direct compression processes.

How is the impurity perindopril diketopiperazine (DKP) monitored?

This key degradation product is quantified using a stability-indicating HPLC method, ensuring it remains well below pharmacopoeial limits.