List of Excipients in Branded Drug CETIRIZINE

Company	Tradename	Ingredient	NDC	Excipient	Potential Generic Entry
WALGREEN COMPANY	CETIRIZINE HCL	cetirizine hcl	0363-6341	GELATIN
WALGREEN COMPANY	CETIRIZINE HCL	cetirizine hcl	0363-6341	GLYCERIN
WALGREEN COMPANY	CETIRIZINE HCL	cetirizine hcl	0363-6341	MANNITOL
WALGREEN COMPANY	CETIRIZINE HCL	cetirizine hcl	0363-6341	POLYETHYLENE GLYCOL
WALGREEN COMPANY	CETIRIZINE HCL	cetirizine hcl	0363-6341	SODIUM HYDROXIDE

Generic Drugs Containing CETIRIZINE

Company	Ingredient	NDC	Excipient
Walgreens	cetirizine	0363-1040	1,4-SORBITAN
Walgreens	cetirizine	0363-1040	BUTYLATED HYDROXYTOLUENE
Walgreens	cetirizine	0363-1040	GELATIN
Walgreens	cetirizine	0363-1040	GLYCERIN
Walgreens	cetirizine	0363-1040	MANNITOL

What are the Most Frequently-Used Excipients in CETIRIZINE?

# Of NDCs	Excipient
4	1,4-SORBITAN
1	ACETIC ACID
1	AMMONIA N-13
1	BLUE 1
1	BUTYL ALCOHOL

Last updated: September 24, 2026

Executive summary: Cetirizine is a mature, low-cost antihistamine with limited active-ingredient patent protection and substantial formulation-driven commercial opportunity. The strongest opportunities are pediatric liquid products, sugar-free and alcohol-free formulations, orally disintegrating tablets, taste-masked chewables, combination allergy products, and differentiated packaging. Excipient selection should focus on palatability, aqueous stability, moisture control, manufacturability, and regulatory simplicity rather than novel drug delivery.

Cetirizine Excipient Strategy and Commercial Opportunities

What is the commercial position of cetirizine?

Cetirizine hydrochloride is a second-generation H1 antihistamine used for allergic rhinitis, urticaria, and related allergy symptoms. It is marketed in prescription and over-the-counter products, most prominently under the Zyrtec brand and through numerous generic products.

The molecule is mature. Commercial differentiation depends on dosage form, patient segment, flavor, convenience, combination therapy, packaging, and channel execution. New chemical-entity exclusivity is no longer relevant for cetirizine products in the United States.

Attribute	Cetirizine profile
Active ingredient	Cetirizine hydrochloride
Common strengths	5 mg and 10 mg
Primary dosage forms	Tablets, chewable tablets, oral solutions, orally disintegrating tablets
Therapeutic class	Second-generation H1 antihistamine
Main indications	Allergic rhinitis and chronic urticaria
U.S. market status	Prescription and OTC
Major brand	Zyrtec
Generic availability	Extensive
Biosimilar relevance	None; cetirizine is a small molecule
Key formulation issues	Taste, moisture sensitivity, pediatric acceptability, rapid disintegration, dose flexibility
Primary commercial levers	Convenience, taste, sugar-free composition, combination products, private-label supply

Cetirizine is generally less sedating than first-generation antihistamines such as diphenhydramine, although somnolence remains a labeled adverse reaction for some patients. Its broad consumer recognition supports private-label, pharmacy-brand, and retailer-exclusive products.

What excipients are used in cetirizine tablets and liquids?

Cetirizine products use conventional pharmaceutical excipients. The exact composition differs by manufacturer, dosage form, market, and regulatory filing.

Typical tablet excipients

Immediate-release cetirizine tablets commonly use:

• Lactose or microcrystalline cellulose as diluents
• Povidone or copovidone as binders
• Croscarmellose sodium, sodium starch glycolate, or crospovidone as disintegrants
• Magnesium stearate or stearic acid as lubricants
• Colloidal silicon dioxide as a glidant
• Hypromellose, titanium dioxide, polyethylene glycol, and colorants in film coatings

A simple direct-compression platform can support low-cost generic production if powder flow, segregation, and content uniformity are controlled. A wet-granulation platform may improve flow and compression but adds processing steps and moisture exposure.

Typical oral-solution excipients

Cetirizine oral solutions may contain:

• Purified water
• Glycerin or propylene glycol
• Sorbitol solution
• Sodium citrate or citric acid
• Sodium benzoate or another preservative
• Flavoring agents
• Sweeteners such as sucralose, saccharin sodium, or sucrose
• pH-adjusting agents

The commercial target determines the excipient choice. A pediatric product generally benefits from a low-viscosity, sugar-free, alcohol-free formulation with strong taste masking. A product for diabetic or calorie-conscious consumers should avoid sucrose and may reduce polyol loading if gastrointestinal tolerance is a concern.

Typical chewable and orally disintegrating tablet excipients

Chewable cetirizine products may use:

• Mannitol
• Sorbitol
• Compressible sugars
• Microcrystalline cellulose
• Crospovidone
• Aspartame, sucralose, or acesulfame potassium
• Flavors
• Magnesium stearate
• Colloidal silicon dioxide

Orally disintegrating tablets require a balance between rapid wetting, mechanical strength, mouthfeel, and low friability. Crospovidone and porous mannitol-based systems can provide rapid dispersion without creating an excessively chalky texture.

Which excipient strategy is best for cetirizine?

The best platform depends on the commercial objective.

Commercial objective	Preferred excipient strategy	Main trade-off
Lowest-cost generic tablet	Microcrystalline cellulose, conventional disintegrant, magnesium stearate	Limited differentiation
Pediatric liquid	Sorbitol or glycerin, citrate buffer, strong flavor system, preservative	Taste and preservative compatibility
Sugar-free product	Sucralose or saccharin with polyol base	Aftertaste and gastrointestinal tolerance
Chewable tablet	Mannitol, flavor, high-efficiency disintegrant, taste-masking system	Compression and mouthfeel
Orally disintegrating tablet	Porous mannitol, crospovidone, low lubricant level	Fragility and moisture sensitivity
Premium fast-onset product	Rapid-wetting tablet architecture or ODT platform	More complex packaging and manufacturing
Pediatric dose flexibility	Oral solution or scored tablet	Stability, dosing-device, and child-resistant packaging requirements
Combination allergy product	Excipient system compatible with multiple actives	Greater interaction and stability burden

Cetirizine hydrochloride is water soluble enough to support liquid products, but solubility alone does not solve bitterness. A commercial liquid requires taste masking, suitable pH, preservative control, and a dosing device that supports accurate administration.

What are the main formulation barriers for cetirizine?

Taste masking

Bitterness is the most important barrier for pediatric and orally disintegrating products. Flavor-only masking may be inadequate at 5 mg or 10 mg doses if the drug is released rapidly in the mouth.

Useful approaches include:

• High-intensity sweetener combinations rather than a single sweetener
• Fruit or berry flavors with acidic top notes
• Ion-exchange resin complexes
• Polymer coating of drug particles
• Lipid or multiparticulate barriers
• Mannitol-based fast-dissolving matrices that reduce residence time

Taste-masking excipients must not materially delay dissolution after swallowing. A coating that performs well in a sensory panel but causes a dissolution failure is commercially unusable.

Moisture management

ODTs and chewable tablets can be moisture sensitive because of porous structures, hygroscopic polyols, and high surface area. Suitable controls include:

• Low-moisture excipient grades
• Desiccant-containing bottles
• High-barrier blister packaging
• Aluminum-aluminum blister systems for premium ODT products
• Tight control of residual water during granulation and compression

Preservative selection

Liquid formulations need a preservative system that remains effective across the finished-product pH range. Sodium benzoate and parabens are established options, but compatibility with flavors, sweeteners, bottle materials, and pediatric-use expectations must be verified.

A preservative-free multidose liquid can be commercially attractive but generally requires a more demanding microbial-control strategy, validated packaging, or a unit-dose presentation.

Mouthfeel and residual sensation

Mannitol often provides a cleaner mouthfeel than some high-sorbitol systems. Crospovidone can improve breakup but may increase a gritty or powdery perception if used at excessive levels. Lubricant concentration also affects wetting and oral dispersion.

Dose uniformity

Cetirizine tablets contain a relatively low drug load. Direct compression requires control of powder segregation and blend uniformity. Ordered mixing, granulation, or engineered excipient grades may be needed for robust content uniformity at commercial scale.

What cetirizine dosage forms offer the strongest commercial opportunities?

Pediatric oral solution

Pediatric allergy treatment remains a practical differentiation segment. A strong product profile includes:

• 1 mg/mL or another convenient concentration
• Sugar-free composition
• Alcohol-free formulation
• Pleasant fruit flavor
• Low viscosity
• Dosing syringe rather than a cup alone
• Child-resistant packaging
• Clear label directions for age and dose

The principal opportunity is not a new pharmacology claim. It is a better use experience for parents and children.

Chewable tablets

Chewables can compete with liquids where portability and mess reduction matter. The formulation must minimize bitterness, chalkiness, and tablet size. A 5 mg pediatric chewable and a 10 mg adult chewable can support age-segmented merchandising.

Orally disintegrating tablets

ODTs offer a differentiated platform for consumers who have difficulty swallowing tablets or want dosing without water. The commercial case is strongest when the product has:

• Rapid in-mouth dispersion
• Low tablet mass
• Strong taste masking
• Robust unit-dose packaging
• Clear differentiation from standard tablets

ODTs often carry higher packaging and manufacturing costs than conventional tablets. Their price premium must compensate for those costs.

Combination products

Cetirizine combinations can target congestion, ocular symptoms, or other allergy complaints. Potential categories include combinations with pseudoephedrine or other established allergy ingredients, subject to local regulatory requirements.

Combination products introduce several risks:

• More complex labeling
• Greater contraindication burden
• Additional stability studies
• Potential limits on pediatric use
• Consumer confusion around duplicate active ingredients

The commercial opportunity is strongest when the combination addresses a clear unmet convenience need rather than simply increasing the number of actives.

What patents protect cetirizine products?

Core cetirizine composition-of-matter protection has expired. Current commercial barriers are primarily regulatory, manufacturing, trademark, formulation know-how, and distribution barriers.

IP category	Cetirizine relevance
Composition-of-matter patent	Expired
Basic oral tablet claims	Generally weak or expired
Method-of-use patents	Historical relevance; unlikely to block ordinary generic allergy use
Formulation patents	Possible for specific taste-masking, ODT, liquid, or combination compositions
Manufacturing patents	Possible for specialized particle engineering or coating processes
Trademark rights	Important for Zyrtec and other branded products
Trade secrets	Relevant to flavors, coating processes, excipient grades, and scale-up
Regulatory exclusivity	No meaningful new-drug exclusivity for ordinary cetirizine products

A formulation patent can protect a particular excipient combination or manufacturing process without protecting cetirizine itself. The claim must be tested for novelty, obviousness, enablement, written description, and practical design-around risk.

When did cetirizine lose exclusivity?

Cetirizine lost meaningful U.S. small-molecule exclusivity before its OTC launch. FDA approved Zyrtec in the 1990s, and the product moved to OTC status in the United States in 2007. Generic cetirizine products have been widely available for years.

The market therefore has no conventional branded-generic cliff comparable to a newly launched prescription product. Revenue is distributed across branded OTC, store-brand OTC, generic prescription, combination products, and international products.

What is the Orange Book status of cetirizine?

The FDA Orange Book is relevant to approved prescription cetirizine products and historical patent information. Cetirizine is not protected by a currently meaningful, molecule-wide U.S. patent barrier. Ordinary generic cetirizine tablets and solutions face a low patent-entry risk relative to newer prescription drugs.

Paragraph IV activity is not a central current risk category for standard cetirizine products. Any applicant challenging a listed patent would need to evaluate the specific NDA, patent listing, dosage form, and claim scope in the Orange Book at the time of filing. Historical cetirizine patents do not prevent routine generic manufacturing today.

What is the FDA regulatory status of cetirizine?

Cetirizine is FDA-approved in prescription and OTC products. The relevant regulatory paths include:

• Abbreviated New Drug Application for qualifying prescription generic products
• OTC monograph or applicable OTC pathway for eligible products
• NDA or supplemental NDA for products with nonstandard claims, combinations, or novel delivery systems
• Drug Facts labeling for OTC products
• Pediatric safety and dosing requirements for products intended for children

An excipient change can trigger different regulatory treatment depending on whether it affects inactive ingredients, product performance, labeling, safety, or dosage form. A new ODT, chewable, or complex taste-masked system may require more than a simple generic formulation approach.

Does cetirizine face biosimilar risk?

No. Cetirizine is a chemically synthesized small molecule, not a biologic. Biosimilar approval under the Biologics Price Competition and Innovation Act does not apply.

The relevant competitive threats are:

• Generic tablets
• Private-label OTC products
• Store-brand liquids
• Branded combination products
• Alternative antihistamines such as loratadine, fexofenadine, and levocetirizine
• Retailer-specific allergy products

How does cetirizine compare with competing antihistamines?

Product	Common differentiation	Formulation opportunity
Cetirizine	Strong consumer familiarity and broad generic supply	Pediatric liquids, ODTs, taste masking
Loratadine	Low-sedation positioning	Chewables, dissolving tablets, combination products
Fexofenadine	Low-sedation and larger-dose positioning	High-palatability tablets and liquids
Levocetirizine	Single-enantiomer positioning	Premium prescription and OTC formulations
Diphenhydramine	Low cost and broad availability	Lower strategic attractiveness because of sedation concerns

Cetirizine has a strong platform for pediatric and family allergy products. Fexofenadine and loratadine may compete more effectively for consumers prioritizing low sedation. A differentiated cetirizine product should avoid relying solely on claims that are difficult to distinguish from competitor labeling.

Which companies are challenging cetirizine’s market?

Competition is fragmented across:

• Kenvue, through the Zyrtec brand
• Large generic manufacturers
• Private-label OTC suppliers
• Retail pharmacy chains
• Consumer health companies with combination allergy brands
• Contract development and manufacturing organizations supplying retailer brands

No single generic manufacturer controls the category. Manufacturing scale, FDA compliance, packaging capacity, flavor performance, and retailer access are more important than molecule ownership.

What licensing and partnership opportunities exist?

The most practical licensing opportunities are formulation and commercial, not molecule-based. Potential deal structures include:

1. Pediatric formulation licensing: A ready-to-file sugar-free liquid with validated taste masking and stability data.
2. ODT technology licensing: A fast-disintegrating cetirizine platform that can be adapted to other antihistamines.
3. Private-label supply agreements: Multi-year supply to pharmacy, grocery, and mass-retail chains.
4. Combination-product partnerships: Co-development with companies holding complementary OTC brands.
5. Packaging partnerships: Unit-dose blister, child-resistant, or dosing-device systems.
6. International rights deals: Regional commercialization where cetirizine remains prescription-only or where dosage-form competition is less developed.

Royalty value depends on the durability of the formulation claims, regulatory status, cost of goods, and access to retail channels. A broad claim directed only to a conventional cetirizine tablet is likely to have limited licensing value.

What generic launch scenarios exist for cetirizine?

Low-cost standard tablet

This is the easiest launch path and the most exposed to price competition. Success requires reliable supply, high manufacturing utilization, and low packaging costs.

Premium pediatric liquid

This approach can support stronger margins if the product has meaningful taste and dosing advantages. The principal risks are preservative performance, flavor stability, and consumer acceptance.

ODT or chewable

This format can command a price premium but requires stronger protection against moisture, better sensory data, and higher-quality packaging.

Retailer-exclusive private label

Private-label products can achieve significant volume without national advertising. The supplier must meet strict service-level, change-control, and shortage-management requirements.

Combination product

A combination can increase shelf differentiation but carries more regulatory and labeling complexity. It is most attractive when the product solves a clear consumer problem.

How strong is the cetirizine patent estate?

The core estate is weak as a barrier to entry because cetirizine is an established generic active ingredient. A commercial formulation estate can still be valuable if it protects several layers:

• Specific excipient ratios
• Taste-masked drug particles
• Particle-size distributions
• Coating materials and coating levels
• Moisture-barrier packaging
• Rapid-disintegration performance
• Stability across a defined pH range
• Manufacturing process parameters
• Combination-product compositions

The strongest strategy is usually a layered portfolio combining composition claims, process claims, performance data, and trade secrets. Patent value is reduced when competitors can reproduce the same consumer benefit through a different excipient or process route.

What manufacturing and IP barriers remain?

Manufacturing barriers are moderate for standard tablets and higher for differentiated products.

Product type	Manufacturing difficulty	Main barrier
Immediate-release tablet	Low	Blend uniformity and cost
Oral solution	Moderate	Taste, microbial control, preservative system
Chewable tablet	Moderate	Taste, texture, compression
ODT	Moderate to high	Moisture, friability, packaging
Taste-masked multiparticulate	High	Coating uniformity and dissolution
Combination product	Moderate to high	Stability and regulatory complexity

Trade secrets can protect flavor compositions, coating parameters, excipient suppliers, and scale-up controls. They do not replace freedom-to-operate analysis for patented formulation technologies.

What is the revenue exposure for a cetirizine investment?

Cetirizine has low molecule-level pricing power and high category volume potential. Revenue exposure is concentrated in:

• Retail sell-through
• Seasonal allergy demand
• Private-label contracts
• Pediatric and family products
• Product availability during allergy peaks
• Pricing and reimbursement by market
• Brand recognition and shelf placement

Kenvue reports Zyrtec within its consumer health portfolio, but public company reporting does not necessarily provide a complete standalone revenue view for every cetirizine SKU or geography. A product-specific investment case should use channel-level volume, average selling price, retailer margins, and seasonal demand rather than molecule-level patent assumptions.

Key takeaways

• Cetirizine is a mature, widely genericized antihistamine with no meaningful molecule-wide U.S. exclusivity barrier.
• The strongest commercial opportunities are pediatric liquids, chewables, ODTs, sugar-free products, and retailer private-label programs.
• Taste masking is the central formulation challenge, especially for children and orally disintegrating products.
• Liquid products require careful control of pH, preservatives, flavor stability, viscosity, and dosing accuracy.
• ODT products require moisture-resistant packaging and a balance between rapid disintegration and mechanical strength.
• Formulation patents and manufacturing know-how can create value, but conventional tablet claims are vulnerable to design-around.
• Cetirizine has no biosimilar risk because it is a small molecule.
• Licensing value is concentrated in differentiated dosage forms, validated sensory performance, packaging, and commercial supply access.
• The preferred strategy is a layered formulation and trade-secret portfolio supported by private-label or branded distribution.

FAQs

Is cetirizine suitable for a sugar-free pediatric formulation?

Yes. A sugar-free liquid can use sorbitol, glycerin, or a mixed vehicle with high-intensity sweeteners. The formulation must control aftertaste, viscosity, preservative effectiveness, and gastrointestinal tolerance.

Which excipient best improves cetirizine ODT performance?

Mannitol is commonly useful for mouthfeel and compressibility, while crospovidone can support rapid disintegration. The optimal system depends on moisture content, tablet strength, taste-masking method, and packaging.

Can a cetirizine formulation patent support premium pricing?

It can support differentiation if the patent protects a difficult-to-reproduce consumer benefit, such as improved taste, rapid disintegration, or extended stability. A conventional excipient substitution usually provides limited commercial protection.

Is cetirizine suitable for a private-label retail launch?

Yes. The active ingredient is widely available, and the market supports store-brand products. The strongest private-label opportunities are liquid, chewable, ODT, and combination formats with reliable seasonal supply.

Does cetirizine require a novel excipient for commercial differentiation?

No. Commercial differentiation can be achieved with established excipients through improved taste masking, excipient grade selection, dose flexibility, moisture protection, and packaging. A novel excipient would increase regulatory and development complexity.

References

1. European Medicines Agency. (n.d.). Zyrtec and cetirizine product information. European Medicines Agency.

2. U.S. Food and Drug Administration. (n.d.). Approved drug products with therapeutic equivalence evaluations: Orange Book. https://www.accessdata.fda.gov/scripts/cder/ob/

3. U.S. Food and Drug Administration. (n.d.). DailyMed: Cetirizine hydrochloride drug labeling. National Library of Medicine. https://dailymed.nlm.nih.gov/

4. U.S. Food and Drug Administration. (2007). FDA approves over-the-counter Zyrtec. U.S. Department of Health and Human Services.

5. Kenvue Inc. (2024). Annual report for fiscal year 2023. U.S. Securities and Exchange Commission.

6. National Library of Medicine. (n.d.). Cetirizine hydrochloride: PubChem compound summary. https://pubchem.ncbi.nlm.nih.gov/