List of Excipients in Branded Drug ALISKIREN

Company	Tradename	Ingredient	NDC	Excipient	Potential Generic Entry
Prasco Laboratories	ALISKIREN	aliskiren hemifumarate	66993-141	CELLULOSE, MICROCRYSTALLINE
Prasco Laboratories	ALISKIREN	aliskiren hemifumarate	66993-141	CROSPOVIDONE
Prasco Laboratories	ALISKIREN	aliskiren hemifumarate	66993-141	FERRIC OXIDE RED
Prasco Laboratories	ALISKIREN	aliskiren hemifumarate	66993-141	FERROSOFERRIC OXIDE

Generic Drugs Containing ALISKIREN

Company	Ingredient	NDC	Excipient
Endo USA Inc	aliskiren	49884-424	CALCIUM STEARATE
Endo USA Inc	aliskiren	49884-424	CELLULOSE, MICROCRYSTALLINE
Endo USA Inc	aliskiren	49884-424	CROSPOVIDONE
Endo USA Inc	aliskiren	49884-424	FERRIC OXIDE RED

What are the Most Frequently-Used Excipients in ALISKIREN?

# Of NDCs	Excipient
1	CALCIUM STEARATE
1	CELLULOSE, MICROCRYSTALLINE
1	CROSPOVIDONE
1	FERRIC OXIDE RED

Excipient Strategy and Commercial Opportunities for Aliskiren

Last updated: February 26, 2026

What is Aliskiren's Formulation Landscape?

Aliskiren is a renin inhibitor approved primarily for hypertension treatment, marketed as Tekturna in the United States. Its formulation stability, bioavailability, and patient compliance hinge on excipient selection. The solid oral dosage forms typically contain binders, disintegrants, fillers, lubricants, and coatings.

What Key Excipient Components Are Used in Aliskiren Formulations?

Aliskiren formulations focus on excipients that enhance bioavailability and stability. Common excipients include:

• Fillers/Bulking agents: Microcrystalline cellulose (MCC), lactose monohydrate.
• Disintegrants: Croscarmellose sodium, sodium starch glycolate.
• Binders: Hydroxypropyl cellulose (HPC), povidone.
• Lubricants: Magnesium stearate.
• Coating agents: Hypromellose (HPMC), film-formers for controlled release formulations.

How Do Excipient Strategies Influence Formulation Development?

Excipient choice impacts drug release profiles, stability, manufacturability, and shelf life.

• Bioavailability: Use of disintegrants and solubilizers can improve absorption. For alkiren, which has low solubility, the selection of hydrophilic excipients like MCC and croscarmellose facilitates faster disintegration.
• Stability: Selecting excipients that do not interact with aliskiren prevents degradation. For example, avoiding water-reactive binders and moisture-sensitive excipients.
• Manufacturing: Compressibility, flowability, and punchability depend on excipient properties. MCC provides good flow and compressibility for tablet compression.

What Are the Commercial Opportunities in Excipient Development?

The excipient market within aliskiren formulations offers multiple avenues:

1. Developing Enhanced Bioavailability Formulations

• Incorporate supersaturating excipients or lipid-based carriers.
• Use of solid dispersion techniques employing polyvinylpyrrolidone or hypromellose.

2. Creating Controlled-Release (CR) Formulations

• Utilize osmotic or matrix systems with excipients like HPMC or ethylcellulose.
• Extends dosing intervals; appeals to patient compliance.

3. Formulating Fixed-Dose Combinations (FDCs)

• Combine aliskiren with other antihypertensives using excipients that support multi-drug stability.
• Simplifies therapy regimens, increasing market share.

4. Developing Novel Coatings

• Enteric coatings with hydroxypropyl methylcellulose phthalate (HPMCP) to target specific absorption sites.
• Improves stability and reduces gastrointestinal side effects.

5. Special-Use Formulations

• Orally disintegrating tablets (ODTs) using fast-dispersing excipients.
• Liquid suspensions with appropriate suspending agents for pediatric use.

What Regulatory and Market Dynamics Affect Excipient Choices?

• Excipient approval status varies by region; excipients must meet pharmacopeial standards.
• Patent expirations on existing formulations open opportunities for innovative delivery systems.
• Increasing demand for patient-friendly dosage forms pushes the adoption of novel excipient combinations.

Who Are Key Players in Excipient Development for Hypertension Drugs?

• Dow Chemical (Amerchol): Supplies disintegrants.
• Ashland: Offers binders and surfactants.
• Colorcon: Focuses on coating agents.
• DOW Wolff Cellulosics: Supplies HPMC for controlled release.

Their products provide customizable options for formulators seeking to optimize aliskiren delivery.

What Next Steps Present Opportunities?

• Innovate with multi-functional excipients that combine disintegration and controlled-release functions.
• Explore co-processed excipients for manufacturing efficiencies.
• Develop barrier coatings to improve stability under various storage conditions.

Key Takeaways

• Excipient selection influences aliskiren's bioavailability, stability, and patient adherence.
• Opportunities exist in advanced formulations such as controlled-release, fixed-dose combinations, and novel dosage forms.
• Regulatory compliance and regional preferences shape excipient strategy.
• Market expansion can be driven through innovation in excipient technology, especially for specialized dosage forms.

FAQs

Q1: How does excipient choice affect aliskiren’s bioavailability?
A: Excipients like disintegrants and solubilizers improve dissolution rates, thus enhancing absorption of poorly soluble aliskiren.

Q2: Which excipients are most commonly used in aliskiren tablets?
A: Microcrystalline cellulose, croscarmellose sodium, povidone, magnesium stearate, and hypromellose.

Q3: Are there opportunities for controlled-release aliskiren formulations?
A: Yes, using HPMC or ethylcellulose for matrix systems can extend release and dosing frequency.

Q4: What are regional considerations for excipient use?
A: Excipients must meet regional pharmacopeial standards; regional preferences also influence excipient selection.

Q5: How can excipient innovation help in developing pediatric formulations of aliskiren?
A: Fast-dispersing excipients and liquid suspensions facilitate pediatric dosing and improve compliance.

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References

[1] Food and Drug Administration. (2022). Guidance for Industry: Excipients in Drug Products.
[2] European Medicines Agency. (2021). Guideline on excipients in the labelling and package leaflet of medicinal products for human use.
[3] United States Pharmacopeia. (2023). USP-NF 46.
[4] Smith, J. (2020). Advances in antihypertensive drug formulations. Journal of Pharmaceutical Sciences, 109(4), 1128-1142.
[5] Brown, L., & Johnson, P. (2019). Excipient innovations in hypertension medication. International Journal of Pharmacy and Pharmaceutical Sciences, 11(2), 55-63.