List of Excipients in Branded Drug ITRACONAZOLE

Company	Tradename	Ingredient	NDC	Excipient	Potential Generic Entry
Patriot Pharmaceuticals LLC	ITRACONAZOLE	itraconazole	10147-0150	ADRABETADEX
Patriot Pharmaceuticals LLC	ITRACONAZOLE	itraconazole	10147-0150	CARAMEL
Patriot Pharmaceuticals LLC	ITRACONAZOLE	itraconazole	10147-0150	CHERRY
Patriot Pharmaceuticals LLC	ITRACONAZOLE	itraconazole	10147-0150	HYDROCHLORIC ACID
Patriot Pharmaceuticals LLC	ITRACONAZOLE	itraconazole	10147-0150	PROPYLENE GLYCOL
Patriot Pharmaceuticals LLC	ITRACONAZOLE	itraconazole	10147-0150	SACCHARIN SODIUM

Generic Drugs Containing ITRACONAZOLE

Company	Ingredient	NDC	Excipient
Mylan Pharmaceuticals Inc	itraconazole	0378-5100	FD&C BLUE NO. 2
Mylan Pharmaceuticals Inc	itraconazole	0378-5100	FERRIC OXIDE RED
Mylan Pharmaceuticals Inc	itraconazole	0378-5100	FERRIC OXIDE YELLOW
Mylan Pharmaceuticals Inc	itraconazole	0378-5100	FERROSOFERRIC OXIDE
Mylan Pharmaceuticals Inc	itraconazole	0378-5100	GELATIN
Mylan Pharmaceuticals Inc	itraconazole	0378-5100	HYPROMELLOSE

What are the Most Frequently-Used Excipients in ITRACONAZOLE?

# Of NDCs	Excipient
6	ALCOHOL
10	AMMONIA
1	ASCORBIC ACID
6	BUTYL ALCOHOL
3	CELLULOSE, MICROCRYSTALLINE
3	D&C RED NO. 22

Excipient Strategy and Commercial Opportunities for Itraconazole

Last updated: February 25, 2026

What is the current excipient formulation of Itraconazole?

Itraconazole, an antifungal agent, is commercially available in capsules and oral solutions. The capsule formulation commonly contains excipients such as:

• Hydroxypropyl methylcellulose (HPMC)
• Lactose monohydrate
• Magnesium stearate
• Corn starch

The oral solution typically includes:

• Hydroxypropyl beta-cyclodextrin (HP-β-CD)
• Ethanol
• Glycerin
• Citric acid
• Sodium benzoate

Excipient selection influences solubility, stability, bioavailability, and patient tolerability.

How does excipient selection impact bioavailability and formulation stability?

Itraconazole exhibits poor water solubility, approximately 0.01 mg/mL, complicating oral absorption. The choice of excipients aims to enhance bioavailability:

• Cyclodextrins: Used in solutions to form inclusion complexes that increase solubility.
• Hydrophilic polymers: Such as HPMC, in capsules to modulate disintegration and release.
• Surfactants: Not typically used but can improve solubilization.

Stability concerns center on pH sensitivity and crystallization tendencies. Incorporating stabilizing excipients like lactose or citric acid maintains capsule integrity and prevents polymorphic transformations.

What are recent innovations and potential excipient modifications?

Companies focus on improving oral bioavailability and patient compliance through:

• Nanotechnology-based excipients: Lipid-based formulations and micelles to improve solubility and tissue penetration.
• Amorphous solid dispersions: Using polymers like HPMC or polyvinylpyrrolidone (PVP) to stabilize the amorphous form.
• Cyclodextrin derivatives: Such as methyl-β-cyclodextrin for higher complexation efficiency.

Potential innovations include developing salt forms or new excipient matrices that deliver faster absorption or extended release.

What are the licensing and regulatory implications?

Regulatory pathways center on demonstrating equivalent bioavailability and stability:

• Bioequivalence studies: To support generic formulations with modified excipients.
• Stability testing: According to ICH guidelines, to confirm shelf life with new excipient combinations.

FDA and EMA guidelines allow excipient modifications if they do not affect efficacy and safety profiles.

What commercial opportunities arise from excipient innovations?

Emerging opportunities include:

• Generic version reformulations: Differentiated by improved bioavailability or tolerability through excipient changes.
• Extended-release products: Utilizing novel excipient matrices, capturing patent opportunities.
• Biodegradable and patient-friendly excipients: Targeting populations with food allergies or sensitivities, such as lactose intolerance.

The global antifungal market size was valued at USD 11.2 billion in 2022 (Grand View Research), with increasing demand for improved formulations.

What are the key challenges?

• Ensuring regulatory compliance across markets
• Matching bioavailability of existing products
• Managing costs for surfactant or polymer excipients
• Overcoming patent barriers for innovative excipients

Summary Table: Excipient Strategies and Opportunities

Strategy	Description	Commercial Opportunity	Challenge
Cyclodextrin complexation	Enhance solubility via inclusion complexes	Simplify bioavailability improvements	Regulatory approval for new excipients
Solid dispersions	Use polymers like HPMC for amorphous forms	Extend patent life with innovative release	Stability during manufacturing
Nanotechnology-based formulations	Lipid micelles, nanoparticles	Improved absorption and tissue targeting	Manufacturing complexity
Novel excipient matrices	Modified release systems	Extended-release formulations, new patents	Cost and regulatory hurdles

Key Takeaways

• Excipients in Itraconazole formulations are designed to improve solubility, stability, and bioavailability.
• Innovations focus on cyclodextrins, solid dispersions, and nanocarriers to address poor water solubility challenges.
• Regulatory pathways support excipient modifications if bioequivalence and stability are demonstrated.
• Commercial opportunities include reformulations for generics, extended release, and populations with special tolerances.
• Challenges involve balancing formulation complexity, costs, and regulatory compliance.

FAQs

1. Can excipient modifications extend patent protection for Itraconazole formulations?
Yes, if they demonstrate non-obvious improvements in bioavailability, stability, or patient tolerability.

2. Are cyclodextrins safe for long-term oral use?
Yes, cyclodextrins like HP-β-CD have established safety profiles when used within approved limits.

3. What excipients are most suitable for extended-release Itraconazole products?
Hydrophilic polymers like HPMC and matrix-forming excipients enable controlled release.

4. How does lactose intolerance influence excipient choices?
Products aimed at lactose-intolerant populations avoid lactose as an excipient, favoring alternatives like microcrystalline cellulose.

5. What regulatory considerations are key when introducing new excipients in Itraconazole formulations?
Regulatory agencies require detailed safety, stability, and bioavailability data; changes should follow ICH guidelines.

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References

[1] Grand View Research. (2022). Global antifungal market size, share & trends analysis report.
[2] U.S. Food and Drug Administration. (2017). Guidance for industry: Bioavailability and bioequivalence studies for orally administered drug products.
[3] European Medicines Agency. (2020). Guideline on the requirements for the safety and effectiveness of excipients in medicinal products.

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