List of Excipients in Branded Drug GRISEOFULVIN

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Generic Drugs Containing GRISEOFULVIN

Company	Ingredient	NDC	Excipient
Actavis Pharma Inc	griseofulvin	0472-0013	ALCOHOL
Actavis Pharma Inc	griseofulvin	0472-0013	DOCUSATE SODIUM
Actavis Pharma Inc	griseofulvin	0472-0013	FD&C RED NO. 40
Actavis Pharma Inc	griseofulvin	0472-0013	FD&C YELLOW NO. 6
Actavis Pharma Inc	griseofulvin	0472-0013	MAGNESIUM ALUMINUM SILICATE

What are the Most Frequently-Used Excipients in GRISEOFULVIN?

# Of NDCs	Excipient
4	ALCOHOL
1	ANHYDROUS DIBASIC CALCIUM PHOSPHATE
1	ANHYDROUS LACTOSE
1	CALCIUM STEARATE
1	CARBOXYMETHYLCELLULOSE SODIUM

Last updated: August 23, 2026

Griseofulvin is a mature, off-patent oral antifungal with limited molecule-level exclusivity but continuing formulation opportunities. The strongest commercial opportunities are pediatric oral suspensions, higher-bioavailability ultramicrosize products, taste-masked multiparticulates, and differentiated products that reduce administration burden. Regulatory risk is lower for conventional generic tablets and capsules, but formulation changes must address dissolution, food effects, dose uniformity, stability, and bioequivalence.

Griseofulvin Excipient Strategy, Formulation Patents, and Commercial Opportunities

What is the commercial position of griseofulvin?

Griseofulvin is an oral antifungal used primarily for dermatophyte infections, including tinea capitis, tinea corporis, tinea pedis, and tinea unguium. It is available in microsize and ultramicrosize forms and is administered as tablets, capsules, and oral suspension products.

The product is commercially mature. The original branded products are no longer protected by meaningful composition-of-matter exclusivity, and generic competition has reduced pricing power. Commercial value therefore depends on formulation performance, supply reliability, pediatric usability, and channel access rather than on molecule-level patent protection.

Commercial attribute	Assessment
Active ingredient	Griseofulvin
Therapeutic class	Oral antifungal
Main dosage forms	Tablets, capsules, oral suspension
Particle-size variants	Microsize and ultramicrosize
Primary formulation issue	Poor aqueous solubility and variable absorption
Main clinical population	Pediatric and adult patients with dermatophyte infections
Patent position	Mature, generally off-patent active ingredient
Generic pathway	Abbreviated New Drug Application, subject to product-specific requirements
Key differentiation levers	Bioavailability, taste, dose flexibility, stability, packaging, and supply

The principal formulation constraint is poor water solubility. Griseofulvin absorption is improved when administered with a fatty meal, creating a commercial opening for formulations that produce more consistent exposure with ordinary meals or without meal-dependent dosing [1][2].

What excipient strategy is most suitable for griseofulvin?

The optimal excipient strategy depends on whether the product uses microsize or ultramicrosize griseofulvin and whether the target is an immediate-release tablet, capsule, suspension, or pediatric multiparticulate.

Solubility and dissolution enhancement

Griseofulvin is practically insoluble in water. Excipients should improve wetting, dispersion, particle deagglomeration, and dissolution without creating unacceptable stability or manufacturing risks.

Relevant excipient classes include:

• Surfactants and wetting agents, such as sodium lauryl sulfate, polysorbates, poloxamers, and selected nonionic surfactants.
• Hydrophilic polymers, including povidone, copovidone, hydroxypropyl cellulose, and hydroxypropyl methylcellulose.
• Water-soluble carriers, such as polyethylene glycol and selected sugar alcohols.
• Lipid-based excipients, including medium-chain triglycerides, long-chain triglycerides, mono- and diglycerides, and self-emulsifying systems.
• Disintegrants, including crospovidone, croscarmellose sodium, and sodium starch glycolate.
• Colloidal silicon dioxide to improve powder flow and reduce agglomeration.

A conventional solid dosage form may use a wetting agent, superdisintegrant, and hydrophilic binder. A more differentiated formulation could use amorphous solid dispersion technology or lipid-based delivery. The latter approach is commercially more distinctive but carries greater development complexity because of physical stability, capsule compatibility, and scale-up requirements.

Particle-size control

Particle size is central to griseofulvin performance. Microsize and ultramicrosize products differ in surface area, dissolution behavior, dose requirements, and excipient demand.

A formulation program should control:

• D90 and D50 particle size.
• Particle-size distribution after blending.
• Agglomeration during granulation.
• Segregation during compression or capsule filling.
• Wetting behavior in the finished dosage form.
• Dissolution under fed and fasted conditions.

Particle-size reduction alone may not provide a durable commercial advantage. A formulation with improved wetting, dispersion, or supersaturation maintenance has a stronger technical basis than one that relies only on smaller particles.

Lipid-based excipients

Lipid-based systems can address the drug’s food-associated absorption profile. Possible formats include:

• Soft gelatin capsules containing a lipid solution or suspension.
• Self-emulsifying drug delivery systems.
• Solid lipid or adsorbed lipid formulations.
• Lipid-coated multiparticulates.
• Lipid-containing oral suspensions.

The principal development risks are oxidation, precipitation after dilution into gastrointestinal fluid, capsule-shell interactions, and variable performance across fed and fasted states. Antioxidants, chelating agents, and appropriate packaging may be required, but each excipient adds regulatory and stability work.

Amorphous solid dispersions

Amorphous solid dispersions can increase apparent solubility and dissolution. Povidone, copovidone, hypromellose acetate succinate, and related polymers are potential carriers.

The commercial case is strongest when the dispersion produces:

• Faster dissolution than a conventional micronized product.
• Less dependence on dietary fat.
• A lower dose or smaller dosage form.
• More consistent exposure.
• A clinically relevant improvement in treatment completion.

The primary risks are recrystallization, moisture sensitivity, thermal degradation, and the need for advanced solid-state characterization. Differential scanning calorimetry, powder X-ray diffraction, hot-stage microscopy, and long-term stability testing are important development tools.

What formulations are protected by griseofulvin patents?

Legacy griseofulvin patent protection historically focused on particle-size reduction, dosage forms, dispersions, suspensions, and manufacturing processes. Most basic patent rights associated with the original products have expired or become commercially weak because of age.

Current formulation protection, if available for a particular product, would more likely arise from:

• A narrowly claimed excipient combination.
• A defined particle-size distribution.
• A specific dissolution profile.
• A solid dispersion or lipid system.
• A pediatric suspension with a defined preservative and taste-masking system.
• A manufacturing process that produces a distinct solid state.
• A fixed-dose combination or novel delivery system.

Patentability requires more than substituting one routine excipient for another. A defensible formulation patent should link the composition to an unexpected technical result, such as reduced food dependence, improved dose uniformity, increased physical stability, or a clinically relevant reduction in treatment duration.

Patent claims should be reviewed in the United States, European Union, Japan, China, India, and other target markets. Geographic coverage is likely to be more valuable for a differentiated formulation than for a conventional generic tablet, because routine products face direct price competition.

What is the Orange Book status of griseofulvin?

The FDA Orange Book lists approved prescription drug products and associated patent and exclusivity information. Griseofulvin products are generally treated as mature products with generic availability, including microsize and ultramicrosize presentations [3].

A company evaluating an ANDA should confirm:

• The applicable reference listed drug.
• Whether the proposed product is microsize or ultramicrosize.
• Dosage-form and strength matching requirements.
• Any listed patents or exclusivity entries associated with the selected reference product.
• FDA product-specific guidance, if published.
• Bioequivalence requirements for the proposed formulation.

The practical regulatory issue is usually not basic molecule exclusivity. It is whether the proposed product matches the reference product’s active ingredient form, dosage form, strength, and performance characteristics.

When does griseofulvin lose exclusivity?

Griseofulvin’s original small-molecule exclusivity has expired. The product is not a biologic and does not create a biosimilar pathway. Competition occurs through conventional generic-drug pathways rather than biosimilar interchangeability.

The current exclusivity analysis should distinguish among:

Protection type	Relevance to griseofulvin
Composition-of-matter patent	Generally expired for the historic molecule
Basic formulation patent	Generally expired for legacy products
Method-of-use patent	Historic claims are generally old; product-specific review remains necessary
Pediatric exclusivity	Not a general current barrier to generic development
New formulation patent	Possible for a newly developed delivery system
Orphan exclusivity	Not generally applicable to conventional griseofulvin products
Biosimilar exclusivity	Not applicable
Regulatory exclusivity	Depends on any newly approved formulation or indication

A new formulation could obtain patent protection even though griseofulvin itself is old. The claim scope would need to focus on the formulation, process, use, or performance limitation rather than the active ingredient in the abstract.

Which companies are challenging griseofulvin products?

Griseofulvin is supplied through a fragmented generic and specialty-pharmaceutical market rather than a single active branded franchise. Depending on jurisdiction and product form, manufacturers and label holders have included companies such as Ortho Dermatologics, manufacturers of Gris-PEG products, and multiple generic suppliers.

Generic competition typically focuses on:

• Microsize tablets.
• Ultramicrosize tablets or capsules.
• Oral suspensions.
• Contract-manufactured products.
• Institutional and pediatric channels.

Paragraph IV litigation is less likely to be commercially significant for legacy griseofulvin products than for newly launched high-value medicines. A Paragraph IV challenge could still arise against a newly patented formulation, but litigation would concern the formulation patent rather than the underlying antifungal molecule.

What generic entry risks exist for griseofulvin?

Generic entry risk is high for conventional immediate-release products. A basic tablet or capsule with standard excipients has limited protection against substitution and price competition.

The main risks are:

1. Price erosion. Multiple suppliers can compete on a mature active ingredient.
2. Reference-product mismatch. Microsize and ultramicrosize products may not be treated as interchangeable from a formulation-development perspective.
3. Supply volatility. Low-volume products can experience API, packaging, or manufacturing interruptions.
4. Pediatric substitution pressure. Hospitals and pharmacies may favor the lowest-cost liquid or tablet.
5. Limited prescriber loyalty. Griseofulvin is usually selected by clinical need, not brand preference.
6. Label and administration constraints. Suspension products must maintain uniformity throughout use and support accurate dosing.

A differentiated formulation can reduce direct price competition, but the product must create a visible benefit for prescribers, pharmacists, caregivers, or payers.

What commercial opportunities exist for griseofulvin excipients?

Pediatric oral suspension

Pediatric tinea capitis remains the strongest formulation opportunity because children may have difficulty swallowing tablets and treatment courses can be prolonged.

A competitive suspension should address:

• Palatability and bitterness.
• Sedimentation and redispersibility.
• Dose uniformity at the beginning and end of the bottle.
• Low viscosity sufficient for accurate dosing.
• Compatibility with oral syringes.
• Preservative robustness.
• Short preparation and administration time.
• Storage requirements after opening.

Taste masking may combine polymer coating, ion exchange, lipid barriers, sweeteners, flavors, and bitterness suppressors. The strategy should avoid excessive sweetness, high sugar load, and excipient levels that complicate pediatric use.

Sprinkle capsules and multiparticulates

Multiparticulates can provide flexible administration for children who cannot swallow tablets. The product could be opened and sprinkled onto a small amount of soft food, provided the labeling and stability data support that use.

Potential technical advantages include:

• Dose flexibility.
• Reduced dependence on swallowing ability.
• Improved taste masking.
• Less sedimentation than a liquid.
• Better portability.
• Use in pharmacies and outpatient settings without reconstitution.

The development program must demonstrate content uniformity among particles and reliable release after administration with the selected food vehicle.

High-bioavailability capsules

A softgel or lipid-based capsule could target adult patients who have inconsistent meal patterns or difficulty taking the medicine with a high-fat meal. A successful product would need evidence that exposure is more predictable and that the formulation does not increase adverse effects.

This segment is more commercially attractive where the product can support a smaller dose, fewer daily administrations, or a more convenient treatment schedule.

Ready-to-use and reconstituted liquids

A ready-to-use suspension avoids reconstitution errors but carries higher shipping and stability burdens. A powder for reconstitution improves transport and shelf life but shifts complexity to the pharmacy or caregiver.

Excipient opportunities include:

• Stable suspending systems.
• Low-sugar or sugar-free vehicles.
• Preservative systems suitable for multidose use.
• pH-controlled formulations.
• Packaging that limits oxygen and moisture exposure.
• Dosing devices calibrated to the labeled strength.

Hospital and institutional packaging

Unit-dose cups, oral syringes, and tamper-evident packaging can create practical value even without new pharmaceutical technology. Institutional purchasers may value reduced preparation time, fewer dosing errors, and simplified inventory management.

How strong is the patent estate for griseofulvin?

The patent estate for conventional griseofulvin products is weak because the active ingredient and historic dosage forms are old. A new entrant should assume that routine excipient selection will not create substantial exclusivity.

Patent strength improves when claims are supported by:

• A non-obvious solubility-enhancement mechanism.
• A defined and reproducible solid-state form.
• A demonstrated reduction in fed-fasted variability.
• A clinically relevant pharmacokinetic benefit.
• A difficult-to-reproduce manufacturing process.
• A pediatric usability advantage supported by human factors or adherence data.
• A combination of composition and performance limitations.

Trade secrets may be more valuable than patents for process parameters, coating conditions, particle engineering, and scale-up know-how. The limitation is that trade secrets do not block independent development or reverse engineering of the finished product.

What FDA regulatory pathway applies to a new griseofulvin product?

A conventional generic product would generally use an ANDA if it can demonstrate pharmaceutical equivalence and bioequivalence to the appropriate reference listed drug [4].

A materially different formulation may require a different regulatory strategy. The pathway depends on the extent of formulation change, dosage form, strength, labeling, and clinical claims. A new drug application could be necessary for a novel delivery system or a product seeking claims that cannot be supported through the generic pathway.

Key development studies may include:

• Comparative dissolution.
• Fed and fasted pharmacokinetic studies.
• Food-effect evaluation.
• Particle-size characterization.
• Content uniformity.
• Microbial limits and preservative effectiveness for liquids.
• In-use stability.
• Container-closure compatibility.
• Reconstitution and redispersibility testing.
• Pediatric dosing-device performance.

For an oral suspension, formulation sameness is not limited to the active ingredient. Vehicle composition, preservative system, viscosity, particle settling, dose uniformity, and administration instructions can affect regulatory risk.

How does griseofulvin compare with newer oral antifungals?

Griseofulvin remains inexpensive and clinically established but requires longer treatment courses than several newer antifungals. Its principal disadvantages are poor solubility, food-dependent absorption, and prolonged administration.

Attribute	Griseofulvin	Terbinafine	Itraconazole
Main use in dermatophyte infections	Established, especially pediatric tinea capitis	Widely used alternative	Used in selected cases
Solubility challenge	High	Lower formulation burden than griseofulvin	Significant
Treatment duration	Often relatively long	Often shorter for some infections	Regimen-dependent
Pediatric liquid opportunity	Strong	Product and indication dependent	Product and indication dependent
Generic competition	High	High	High
Formulation differentiation	Suspension, multiparticulates, lipid systems	Dosing and formulation optimization	Solubilization and absorption control
Patent opportunity	New formulation or delivery claims	Product-specific	Product-specific

Griseofulvin’s commercial opportunity is therefore concentrated in underserved administration formats and reliable exposure, not in premium pricing based solely on the active ingredient.

What patent litigation and settlement issues affect griseofulvin?

There is no broad, current litigation pattern comparable to high-value patented medicines. Legacy griseofulvin products generally face ordinary generic competition rather than active patent settlement markets.

For a newly patented formulation, the relevant litigation risks would include:

• Paragraph IV certification.
• Invalidity challenges based on obviousness and lack of written description.
• Non-infringement claims based on excipient or particle-size differences.
• Product-by-process claim disputes.
• Regulatory exclusivity disputes.
• ANDA launch timing after settlement.

Settlement agreements would need review for launch dates, authorized generic rights, supply obligations, and restrictions on formulation changes. The commercial value of settlement is likely limited unless the new formulation achieves meaningful market share or reimbursement differentiation.

What manufacturing and intellectual-property barriers matter most?

The main barriers are technical execution and consistent supply rather than access to the molecule.

Important manufacturing controls include:

• API particle-size consistency.
• Prevention of agglomeration.
• Uniform distribution at low dose.
• Controlled granulation moisture.
• Compression robustness.
• Suspension sedimentation behavior.
• Coating uniformity for taste-masked particles.
• Protection from humidity and oxidation.
• Reproducible dissolution across batches.

For an advanced formulation, the critical intellectual-property assets may include particle engineering, spray drying, hot-melt extrusion, lipid preconcentrate processing, coating technology, and packaging design.

A manufacturer with existing pediatric liquid capacity, analytical expertise, and low-volume commercial infrastructure may have a better competitive position than a company with only conventional tablet manufacturing.

What is the revenue exposure and market-entry outlook?

Public company revenue attributable solely to griseofulvin is generally difficult to isolate because generic manufacturers report broad product portfolios. The market should be assessed through product-level prescription volume, average selling price, wholesaler data, institutional contracts, and label-holder concentration rather than relying on company-wide revenue.

The most viable entry scenarios are:

Conventional generic tablet or capsule

This is the fastest and lowest-cost route but has the highest price and substitution risk. The product requires reliable API sourcing and efficient manufacturing.

Pediatric suspension

This offers stronger differentiation and may support better retention if taste, dosing accuracy, and stability are superior. The market is smaller than the total tablet market but more defensible.

Multiparticulate or sprinkle product

This has potential for pediatric and caregiver convenience. It requires more complex development and may need a clear administration claim to justify commercial investment.

Lipid-based or amorphous formulation

This could create the strongest technical differentiation if it improves exposure or reduces food dependence. It also has the highest formulation, analytical, and regulatory burden.

Key Takeaways

• Griseofulvin is an old, generic oral antifungal with little remaining molecule-level exclusivity.
• Conventional tablets and capsules face high generic-entry and price-erosion risk.
• Poor aqueous solubility and food-dependent absorption are the primary formulation targets.
• Pediatric oral suspension, taste-masked multiparticulates, and sprinkle products offer the clearest commercial opportunities.
• Lipid-based delivery and amorphous solid dispersions may support new formulation patents if they produce measurable performance advantages.
• A new product should differentiate through bioavailability, dose flexibility, stability, or administration convenience.
• The FDA pathway is generally an ANDA for a conventional generic, while materially novel formulations may require a different regulatory strategy.
• Manufacturing know-how, particle-size control, taste masking, and packaging may be more valuable than broad legacy patent rights.
• Biosimilar risk is not relevant because griseofulvin is a small-molecule drug.
• Commercial success depends on product-level execution, not on the age of the active ingredient.

FAQs

Can griseofulvin be reformulated as a once-daily product?

A once-daily product would require pharmacokinetic and clinical support. Excipient changes alone cannot establish a new dosing schedule. A controlled-release or high-exposure formulation could support development, but the regulatory and clinical burden would be higher than for an immediate-release generic.

Which excipients are best for masking griseofulvin bitterness?

Polymer coatings, lipid barriers, ion-exchange systems, sweeteners, flavors, and bitterness suppressors can be used. The best system depends on particle size, dose, release requirements, and pediatric acceptability. A coating that prevents bitterness must still release griseofulvin rapidly after swallowing.

Is a griseofulvin oral suspension easier to approve than a new tablet?

Not necessarily. A suspension introduces additional requirements for sedimentation, redispersibility, preservative effectiveness, viscosity, in-use stability, and dose uniformity. It may offer greater commercial differentiation but also creates more formulation and regulatory variables.

Can a new griseofulvin formulation receive patent protection?

Yes. Patent protection may be available for a novel composition, particle engineering method, solid dispersion, lipid system, manufacturing process, or use supported by unexpected results. The patent would protect the defined formulation or process, not griseofulvin generally.

Does griseofulvin require administration with fatty food?

Food, particularly dietary fat, can improve absorption. A formulation that reduces this dependence could provide a meaningful product advantage, but the benefit must be demonstrated through comparative pharmacokinetic and food-effect studies.

References

1. DailyMed. (n.d.). Gris-PEG: Griseofulvin ultramicrosize tablet prescribing information. U.S. National Library of Medicine.

2. U.S. Food and Drug Administration. (n.d.). Griseofulvin product labeling and prescribing information. FDA.

3. U.S. Food and Drug Administration. (n.d.). Approved drug products with therapeutic equivalence evaluations, Orange Book. FDA.

4. U.S. Food and Drug Administration. (n.d.). ANDA submissions: Pharmaceutical equivalence and bioequivalence requirements. FDA.