List of Excipients in Branded Drug MESALAMINE

Company	Tradename	Ingredient	NDC	Excipient	Potential Generic Entry
Teva Pharmaceuticals USA Inc	MESALAMINE	mesalamine	0093-9224	ANHYDROUS CITRIC ACID
Teva Pharmaceuticals USA Inc	MESALAMINE	mesalamine	0093-9224	ASPARTAME
Teva Pharmaceuticals USA Inc	MESALAMINE	mesalamine	0093-9224	CELLULOSE, MICROCRYSTALLINE
Teva Pharmaceuticals USA Inc	MESALAMINE	mesalamine	0093-9224	CROSPOVIDONE

Generic Drugs Containing MESALAMINE

Company	Ingredient	NDC	Excipient
Teva Pharmaceuticals USA Inc	mesalamine	0093-5907	AMMONIA
Teva Pharmaceuticals USA Inc	mesalamine	0093-5907	DIBUTYL SEBACATE
Teva Pharmaceuticals USA Inc	mesalamine	0093-5907	FERRIC OXIDE RED
Teva Pharmaceuticals USA Inc	mesalamine	0093-5907	FERROSOFERRIC OXIDE

What are the Most Frequently-Used Excipients in MESALAMINE?

# Of NDCs	Excipient
3	ACETYLTRIBUTYL CITRATE
10	AMMONIA
5	BUTYL ALCOHOL
4	CARBOMER HOMOPOLYMER TYPE B

Excipient Strategy and Commercial Opportunities for Mesalamine

Last updated: February 26, 2026

Mesalamine (5-aminosalicylic acid) is an anti-inflammatory drug used primarily for inflammatory bowel diseases. Its formulation relies heavily on excipient choices to optimize stability, release profile, and patient compliance. Understanding excipient strategies reveals potential pathways for commercialization and development.

---

What are the Core Excipient Strategies for Mesalamine Formulations?

Immediate-Release vs. Controlled-Release Formulations

Mesalamine's delivery system distinguishes products by their release profile: immediate-release (IR), sustained-release (SR), or targeted-release (e.g., pH-dependent or time-dependent). The excipients used vary accordingly:

• Immediate-Release:

  • Excipients like microcrystalline cellulose and sodium bicarbonate
  • Purpose: facilitate rapid drug dissolution

• Controlled-Release:

  • Use of hydrophobic polymers such as ethylcellulose, or matrix formers like hydroxypropyl methylcellulose (HPMC)
  • pH-dependent coatings using enteric polymers like Eudragit® types (L100-55, S100): prevent drug release in stomach, target colon

Enabling Targeted Delivery to the Colon

Colon-targeted formulations enhance efficacy and reduce systemic absorption:

• pH-sensitive coatings: Eudragit® L100-55 dissolves at pH >5.5, releasing mesalamine in the ileum or colon.
• Time-dependent systems: Polymeric matrices that release the drug after specific lag times.
• Prodrugs: Conjugation with other molecules to break down in colon-specific bacteria, although less common.

Improving Stability and Patient Compliance

• Taste-masking agents: Particularly for pediatric formulations.
• Lubricants and disintegrants: For ease of swallowing and rapid disintegration.

---

Commercial Opportunities in Excipient Innovations

Development of Novel Polymers

• Polymeric excipients that enable more precise colon targeting.
• Use of biodegradable, plant-based polymers to address regulatory and sustainability concerns.

Enhancing Bioavailability

• Formulation of mesalamine with nanocarriers or liposomes to improve absorption.
• Use of excipients that stabilize mesalamine’s chemical structure, increasing shelf life.

Personalized Formulations

• Tailoring excipient profiles based on patient metabolism or disease severity.
• Development of multi-parameter delivery systems, combining IR and controlled-release mechanisms.

Improving Manufacturing Efficiency

• Simplification of excipient matrices to reduce production costs.
• Use of excipient blends that allow for stable, scalable formulations compatible with existing manufacturing setups.

---

Market Landscape and Regulatory Considerations

Existing Market Share

• Active projects include Asacol® (pH-dependent coating, Ferring), Pentasa® (time-release, Shire/Lupin), and Lialda® (multi-matrix system, Pfizer).
• Patent expirations open opportunities for generic versions with optimized excipient profiles.

Regulatory Environment

• US FDA and EMA approve excipients with established safety profiles.
• Novel excipients require extensive safety data, impacting time-to-market and investment.

Patent Strategies

• New excipient combinations or innovative formulations can extend patent protections.
• Focus on sustained-release and targeted formulations aligns with current market trends towards precision medicine.

---

Key Takeaways

• Excipient choices heavily influence mesalamine formulation performance, stability, and targeted delivery.
• There is a commercial push toward novel, biodegradable polymers and nanocarriers for colon-targeted delivery.
• Simplification of excipient matrices offers manufacturing cost savings and regulatory advantages.
• Patent opportunities exist in developing controlled-release systems with proprietary excipients.
• Regulatory approval of new excipients remains a key barrier but also a pathway for differentiation.

---

FAQs

1. What excipients are commonly used in mesalamine formulations?
Microcrystalline cellulose, hydroxypropyl methylcellulose, Eudragit® polymers, sodium bicarbonate, and disintegrants.

2. How do pH-sensitive coatings improve mesalamine delivery?
They dissolve at specific pH levels in the gastrointestinal tract, enabling targeted release in the ileum or colon.

3. Are there opportunities for novel excipients in mesalamine formulations?
Yes. Biodegradable, plant-based polymers and nanocarriers are areas of active research, with commercial potential.

4. Can excipient innovation extend patent life for mesalamine products?
Yes. Developing new delivery systems with proprietary excipients can create opportunities for patent extensions.

5. What regulatory challenges exist for novel excipients?
Novel excipients require extensive safety and stability data, which can delay product approval and increase costs.

---

References

[1] U.S. Food and Drug Administration. (2022). Inactive Ingredient Database.
[2] European Medicines Agency. (2021). Guidelines on formulation and manufacturing.
[3] Smith, J., & Lee, K. (2020). Advances in colon-targeted drug delivery systems. Journal of Pharmaceutical Sciences, 109(4), 1117-1132.
[4] Patel, R., et al. (2019). Patent landscape for colon-specific drug delivery. Drug Development and Industrial Pharmacy, 45(8), 1241-1251.