Eplerenone API

Eplerenone API

Product Name:Eplerenone Powder
Synonyms:Inspra,SC-66110, Epoxymexrenone, 9,11α-Epoxy-17-hydroxy-3-oxo-17α-pregn-4-ene-7α,21-dicarboxylic acid γ-lactone methyl ester
CAS Number:107724-20-9
Purity:≥99% (HPLC)
Certificate:ISO22000/GMP

Product Introduction
Product Name Eplerenone Powder
Synonyms Inspra, SC-66110, Epoxymexrenone, 9,11α-Epoxy-17-hydroxy-3-oxo-17α-pregn-4-ene-7α,21-dicarboxylic acid γ-lactone methyl ester
Appearance White to light yellow solid powder
CAS Number 107724-20-9
Molecular Formula C₂₄H₃₀O₆
Molecular Weight 414.49–414.50 g/mol
Purity ≥99% (HPLC)
Sample Free Provided
Certificate KOSHER/HACCP/ISO22000/GMP
Solubility Soluble in ethanol, chloroform, ethyl acetate; sparingly soluble in DMSO; insoluble in water
Storage −20 °C, under inert atmosphere, protected from light
 

Products Description

 

What is Eplerenone Powder?

Eplerenone Powder is a high-purity active pharmaceutical ingredient (API) widely recognized in official pharmacopeias as a bulk substance used to manufacture finished drug products. Its primary role in procurement is as a quality-controlled raw material for generic pharmaceutical formulations.

As an API, its physical form, such as particle size, is a critical quality attribute. Nanoparticulate formulations (with a D90 particle size of less than 15 µm) are a known approach to enhance the bioavailability of oral solid preparations, as unformulated eplerenone is not well absorbed in the gastrointestinal tract.

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Applications Of Eplerenone Powder

1. Statutory clinical applications approved by FDA
1.1 Treatment of hypertension Eplerenone is approved by the FDA for the treatment of hypertension alone or in combination with other drugs. The mechanism of action is to lower blood pressure to reduce the risk of cardiovascular events (mainly stroke and myocardial infarction). Eplerenone is not a first-line initial treatment for conventional hypertension, but is particularly suitable for patients with primary aldosteronism (Conn syndrome) or refractory hypertension.
1.2 Post-myocardial infarction heart failure The second approved indication of eplerenone is to improve the survival rate of stable patients with left ventricular systolic dysfunction (ejection fraction ≤40%) and symptoms of heart failure after acute myocardial infarction.
2. Off-label applications in clinical practice Primary aldosteronism (PA/Conn syndrome), which is the most established off-label use of eplerenone, is found in clinical practice guidelines in many countries.

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Benefits Of Eplerenone Powder

1.Clinical Outcomes: Mortality and Cardiac Function Benefits

1.1All-Cause Mortality Reduction

A 2024 systematic review and meta-analysis of 10 studies comprising 21,930 heart failure patients demonstrated that eplerenone is associated with a 1.2lower risk of all-cause mortality compared to spironolactone (HR = 0.78, 95% CI [0.64–0.94], P = 0.009)-5-6. This finding is supported by a separate AHA 2024 meta-analysis covering 1,296 participants, which reported a relative risk of 0.70 (95% CI: 0.52–0.93)-7.

1.3Cardiovascular Mortality

The same analysis showed eplerenone significantly reduced cardiovascular mortality risk (HR = 0.54, 95% CI [0.39–0.74], P = 0.0001)-5-6. A network meta-analysis of 32 randomized trials (15,685 patients) ranked eplerenone above spironolactone for all-cause mortality outcomes

2.Safety and Tolerability Benefits

2.1Gynecomastia Risk Reduction

The 2024 BMC meta-analysis showed eplerenone significantly reduces the risk of gynecomastia compared to spironolactone (RR = 0.07, 95% CI [0.02–0.31], P = 0.0001)-5-6. This is attributed to eplerenone's lower affinity for progesterone, androgen, and glucocorticoid receptors-1. The AHA meta-analysis reported a relative risk of 0.18, though statistical significance was limited by sample size (p=0.13)-7.

2.2Lower Treatment Withdrawal

Eplerenone patients showed a lower risk of treatment discontinuation compared to spironolactone (RR = 0.69, 95% CI [0.62–0.78], P = 0.0001)-5-6. This suggests better overall tolerability and adherence.

2.3Hyperkalemia Risk

Although not statistically significant in all analyses, eplerenone showed a trend toward lower hyperkalemia risk (RR = 0.70, 95% CI [0.45–1.09], p=0.12)-7. Multiple studies confirmed no preference for either agent regarding hyperkalemia, renal failure, or hypotension-5-8.

2.4Pharmacokinetic Advantages

Eplerenone has a short half-life of 3–6 hours and no active metabolites-3-1. This contrasts with spironolactone's longer half-life (>20 hours), providing more predictable drug behavior and faster clearance, which is clinically relevant for dose adjustment in patients with renal impairment.

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Packing & Shipping

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CONTACT PAGE

1.Inquiry methods:
Email:alice@xaheshun.com
Whatspp:+8618509260106

Online instant messaging

2.Contact Information:
Name:Alice

Telephone :+8618509260106
Email:alice@xaheshun.com

FAQ

Q: Does Eplerenone require cold-chain shipping?

A: No – powder can be shipped at room temperature for short transit periods. However, upon receipt, the product should be stored under refrigerated conditions (2–8°C) for long-term stability-2-6. It is classified as heat sensitive, so prolonged exposure to elevated temperatures should be avoided.

Q: What is the difference between research-grade and pharmacopoeial reference standard grades?

A: Research-grade (≥98–99% HPLC) is suitable for laboratory studies, cell assays, and formulation development-2-6. EP Reference Standards (European Pharmacopoeia) are pharmaceutical primary standards intended specifically for system suitability testing and analytical method validation in regulated environments, as prescribed by the issuing Pharmacopoeia.

Q: How does Eplerenone differ from Spironolactone?

A: Eplerenone is a more selective mineralocorticoid receptor antagonist than spironolactone, with lower affinity for progesterone, androgen, and glucocorticoid receptors-2-9-11. This means eplerenone has fewer antiandrogenic side effects (such as gynecomastia) compared to spironolactone.

Q: What purity grades are available for Eplerenone Powder?

A: Research-grade eplerenone is typically available at ≥98% purity by HPLC-2-7, with premium grades reaching 99% for higher-end applications-6. For pharmacopoeial reference standards, the European Pharmacopoeia (EDQM) offers pharmaceutical primary standard grades for system suitability testing.

Q: What is the recommended storage condition and shelf life?

A: Store powder at 2–8°C (refrigerated)-2-6-7. The compound is heat sensitive-7. For long-term storage, 2–8°C is recommended; room temperature shipping is acceptable for short transit periods but transfer to refrigerated storage upon receipt.

 

 

 

 

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