List of Excipients in Branded Drug GUAIFENESIN

Company	Tradename	Ingredient	NDC	Excipient	Potential Generic Entry
KROGER COMPANY	GUAIFENESIN	guaifenesin	30142-703	CARBOMER HOMOPOLYMER TYPE B
KROGER COMPANY	GUAIFENESIN	guaifenesin	30142-703	CELLULOSE, MICROCRYSTALLINE
KROGER COMPANY	GUAIFENESIN	guaifenesin	30142-703	HYPROMELLOSE
KROGER COMPANY	GUAIFENESIN	guaifenesin	30142-703	MAGNESIUM STEARATE
KROGER COMPANY	GUAIFENESIN	guaifenesin	30142-703	SODIUM STARCH GLYCOLATE TYPE A POTATO
WALMART STORES INC	GUAIFENESIN	guaifenesin	49035-074	CARBOMER HOMOPOLYMER TYPE B

Generic Drugs Containing GUAIFENESIN

Company	Ingredient	NDC	Excipient
WALGREEN CO	guaifenesin	0363-0028	HYPROMELLOSE 2208
WALGREEN CO	guaifenesin	0363-0028	HYPROMELLOSE 2910
WALGREEN CO	guaifenesin	0363-0028	MAGNESIUM STEARATE
WALGREEN CO	guaifenesin	0363-0028	MICROCRYSTALLINE CELLULOSE 101
WALGREEN CO	guaifenesin	0363-0028	MICROCRYSTALLINE CELLULOSE 102
WALGREEN CO	guaifenesin	0363-0028	POVIDONE K25

What are the Most Frequently-Used Excipients in GUAIFENESIN?

# Of NDCs	Excipient
1	CARBOMER COPOLYMER TYPE A
1	CARBOMER HOMOPOLYMER TYPE
15	CARBOMER HOMOPOLYMER TYPE B
17	CELLULOSE, MICROCRYSTALLINE
1	FD&C BLUE NO. 1
8	FD&C BLUE NO. 2

Last updated: September 3, 2026

ecutive summary: Guaifenesin is a mature, low-cost expectorant with limited active-ingredient patent protection and broad over-the-counter access in the United States. Commercial value depends on formulation engineering, combination products, dosage convenience, taste masking, pediatric usability, supply reliability, and brand execution. The strongest opportunities are extended-release tablets, liquid and orally disintegrating formats, alcohol-free and sugar-free liquids, private-label products, and regulated-market expansion. Patent risk is concentrated in formulation and process claims rather than guaifenesin itself.

Guaifenesin Excipient Strategy, Patent Position, and Commercial Opportunities

What is guaifenesin and how is it regulated?

Guaifenesin is an oral expectorant used to loosen phlegm and thin bronchial secretions associated with the common cold and related respiratory conditions. In the United States, it is regulated primarily through the FDA over-the-counter monograph system rather than through new-drug exclusivity for most products.

The FDA monograph permits guaifenesin in several oral dosage formats, including immediate-release tablets, extended-release tablets, capsules, liquid preparations, and combination products. The applicable monograph specifies permitted labeling, indications, dosage ranges, and conditions of use.[1]

Parameter	Typical U.S. OTC position
Active ingredient	Guaifenesin
Therapeutic category	Expectorant
Common immediate-release dose	200 to 400 mg every four hours
Common adult daily maximum	2,400 mg
Common extended-release dose	600 to 1,200 mg every 12 hours
Typical extended-release daily maximum	2,400 mg
Prescription requirement	Usually no, when compliant with the OTC monograph
Main dosage forms	Tablets, extended-release tablets, capsules, syrups, solutions, powders
Major brands	Mucinex, Robitussin, store brands, regional brands
Biosimilar pathway	Not applicable
Primary commercial barrier	Brand, formulation, distribution, regulatory compliance, and manufacturing cost

The legal framework changed with the CARES Act OTC monograph reforms. FDA now uses an administrative-order process for certain OTC monograph products, although the underlying commercial model remains largely monograph-based.[2]

What patents protect guaifenesin products?

Guaifenesin itself is a mature small molecule and does not provide a meaningful new-molecule patent moat. Commercial protection historically has come from dosage-form patents, controlled-release systems, manufacturing processes, combination products, trademarks, and trade dress.

Active-ingredient patent position

A company launching a conventional guaifenesin product generally cannot rely on composition-of-matter exclusivity for the active ingredient. The practical freedom-to-operate analysis instead focuses on:

• Extended-release matrix design
• Bilayer or multilayer tablet architecture
• Coated-particle technology
• Taste masking
• Liquid suspension stability
• Combination products
• Manufacturing processes
• Tablet tooling and production controls
• Trademark and packaging rights

Historical guaifenesin extended-release patents associated with branded products have generally reached their statutory terms. The presence of an old patent number in product literature does not establish current enforceability. A launch decision requires a current search of U.S. Patent and Trademark Office records, FDA Orange Book listings, court dockets, and continuation or terminal-disclaimer records.

Orange Book status

The Orange Book is most relevant to approved prescription and certain NDA products. Many guaifenesin products are OTC monograph products and do not depend on Orange Book-listed patents. Some branded extended-release products have been approved under NDAs, creating a more conventional patent-listing and exclusivity analysis.

A buyer should distinguish among:

1. A monograph-compliant OTC product.
2. An NDA product with FDA-approved labeling.
3. A private-label product manufactured under an OTC monograph.
4. A branded product using formulation know-how that may not be disclosed in a patent.

The absence of an Orange Book-listed patent does not eliminate all intellectual-property risk. It shifts the analysis toward non-Orange-Book patents, trade secrets, trademarks, unfair-competition claims, and manufacturing know-how.

When does guaifenesin lose exclusivity?

Guaifenesin has already lost active-ingredient exclusivity in practical commercial terms. Generic and private-label competition is established across tablets, liquids, capsules, and combination products.

The relevant exclusivity dates are therefore product-specific:

Protection type	Commercial status
Guaifenesin active ingredient	Mature; no meaningful new-molecule exclusivity
Conventional immediate-release tablets	Broadly commoditized
Standard oral liquids	Broadly commoditized
Extended-release products	Formulation and manufacturing claims may remain relevant, but historical core patents are generally expired
Combination products	Possible protection through formulation, labeling, trademark, or later-added ingredients
Brand names and trade dress	Potentially ongoing if maintained and enforceable
OTC monograph status	Regulatory pathway, not market exclusivity

The commercial question is not whether competitors can enter the guaifenesin market. They can. The question is whether a new product offers lower total cost, better adherence, improved sensory performance, or a differentiated regulatory and distribution position.

What excipients are used in guaifenesin tablets?

Immediate-release guaifenesin tablets typically use conventional fillers, binders, disintegrants, lubricants, and film-coating systems. Excipients should be selected around guaifenesin's high dose, powder flow, compactability, dissolution target, and tablet size.

Excipient function	Candidate materials	Development purpose
Diluent	Microcrystalline cellulose, dibasic calcium phosphate, lactose, mannitol	Controls tablet weight, flow, and compression
Binder	Povidone, copovidone, pregelatinized starch, hydroxypropyl cellulose	Improves granule and tablet strength
Disintegrant	Crospovidone, croscarmellose sodium, sodium starch glycolate	Supports rapid breakup and dissolution
Lubricant	Magnesium stearate, sodium stearyl fumarate	Reduces ejection force and sticking
Glidant	Colloidal silicon dioxide	Improves flow and die filling
Film former	Hypromellose, polyvinyl alcohol	Protects tablet and supports branding
Plasticizer	Polyethylene glycol, propylene glycol	Improves coating flexibility
Opacifier or colorant	Titanium dioxide alternatives, iron oxides, approved color systems	Product identification and appearance
Sweetener	Sucralose, acesulfame potassium, saccharin, steviol glycosides	Liquid and chewable palatability
Suspending agent	Xanthan gum, sodium carboxymethylcellulose, microcrystalline cellulose blends	Maintains liquid uniformity
Preservative	Sodium benzoate, potassium sorbate, parabens where permitted	Microbial control in aqueous products
Buffer	Citrate, phosphate, acetate systems	pH control and preservative performance

Guaifenesin has a relatively high dose compared with many modern active pharmaceutical ingredients. Excipients that improve manufacturability can materially reduce tablet size, compression failures, weight variability, and production cost.

What excipients are best for extended-release guaifenesin?

Extended-release guaifenesin is the most important formulation segment because dosing convenience supports brand differentiation. The target is usually delivery over approximately 12 hours, with acceptable initial release and no dose dumping.

Hydrophilic matrix systems

Hydrophilic polymers such as hypromellose are practical candidates for a sustained-release matrix. Polymer grade, viscosity, particle size, compression force, and tablet geometry control the release profile.

Key development variables include:

• Polymer concentration
• Polymer viscosity grade
• Guaifenesin particle size
• Tablet porosity
• Compression force
• Coating weight
• Dissolution medium and agitation
• Food effect
• Alcohol sensitivity

Hydrophilic matrices can be cost-effective and scalable. They also expose the product to formulation-performance risk because small changes in granulation moisture, compression, or polymer distribution can affect dissolution.

Hydrophobic matrix systems

Hydrophobic excipients such as ethylcellulose, stearic acid, glyceryl behenate, and waxes can reduce water penetration and sustain release. These systems may improve robustness but can create manufacturing and dissolution challenges.

Hydrophobic matrices are attractive when the developer seeks:

• Lower sensitivity to processing moisture
• Better resistance to rapid hydration
• More durable release control
• A differentiated process or formulation platform

Coated-particle and multiparticulate systems

Pellets, granules, or coated particles can deliver more consistent release and support capsules, sachets, and sprinkle products. They also allow separation of incompatible ingredients in combination products.

Potential benefits include:

• Lower risk of tablet-size escalation
• Better flexibility for pediatric and geriatric administration
• Improved combination-product design
• Reduced dependence on a single tablet matrix
• Opportunities for taste masking

The main tradeoff is higher process complexity and greater coating-control requirements.

What formulation opportunities exist for guaifenesin?

Extended-release tablets

Extended-release 600 mg and 1,200 mg products have the clearest consumer value proposition: fewer daily doses. Opportunities include smaller tablets, easier swallowing, lower friability, and improved food-effect performance.

Alcohol-free and sugar-free liquids

Alcohol-free, sugar-free, and dye-free formulations address pediatric, geriatric, diabetic, and family-care segments. These products require close control of preservative efficacy, viscosity, sedimentation, redispersibility, and flavor persistence.

Pediatric products

The main constraints are taste, dose flexibility, swallowability, and age-appropriate labeling. Suitable formats include:

• Oral solutions
• Suspensions
• Unit-dose cups
• Sachets for reconstitution
• Low-volume concentrated liquids
• Orally disintegrating or chewable tablets

The FDA's pediatric labeling framework and OTC monograph requirements limit what can be claimed. A formulation can be commercially differentiated without supporting a new therapeutic claim.

Orally disintegrating and chewable tablets

These formats can improve convenience but create a difficult sensory problem. Guaifenesin's taste and high dose can require intense flavor systems, sweeteners, cooling agents, taste-masking polymers, or coated granules.

Commercial feasibility depends on keeping the tablet small enough for acceptable mouthfeel. A 600 mg orally disintegrating tablet may be materially more difficult than a conventional swallowable tablet.

Combination products

Guaifenesin is frequently combined with dextromethorphan, pseudoephedrine, phenylephrine, acetaminophen, or antihistamines. Combination products can increase basket size and brand visibility, but they create regulatory and safety constraints.

Key risks include:

• Duplicate active ingredients across products
• Inappropriate use in children
• Drug-interaction labeling
• Ingredient-specific contraindications
• Greater dissolution complexity
• Higher stability burden
• More complicated supply chains

The strongest combination opportunity is not necessarily the largest number of active ingredients. Products with clear symptom segmentation, simple labeling, and low duplication risk are easier to commercialize.

How should an excipient strategy be designed for guaifenesin?

A practical development strategy should separate the product into three tiers.

Tier 1: Cost-optimized immediate release

Use a conventional direct-compression or wet-granulation platform. Priorities are:

• Low-cost excipients
• High-dose loading
• Robust flow
• Fast disintegration
• Stable supply
• Simple manufacturing

Microcrystalline cellulose, a superdisintegrant, magnesium stearate, and a film coat may be sufficient, subject to formulation development and regulatory testing.

Tier 2: Differentiated extended release

Use a hydrophilic matrix, multiparticulate system, or coated-particle platform. Priorities are:

• Twelve-hour release
• Low tablet weight
• Reproducible dissolution
• Food-effect control
• Alcohol-dose-dumping assessment
• Scalable manufacturing

The formulation should be designed around the final commercial claim. A product marketed as long-lasting must have dissolution and clinical-support data consistent with that positioning.

Tier 3: Sensory and access differentiation

Use taste masking, sugar-free systems, alcohol-free liquids, chewables, or orally disintegrating dosage forms. Priorities are:

• Human palatability
• Dose accuracy
• Microbial quality
• Shelf stability
• Packaging usability
• Pediatric and caregiver acceptance

Excipient selection should use a Quality by Design framework. Critical material attributes include polymer viscosity, particle-size distribution, moisture, density, lubricant surface area, and flavor volatility.

What manufacturing and IP barriers affect guaifenesin products?

Manufacturing barriers are more important than active-ingredient patent barriers.

Manufacturing barriers

A developer may face:

• High tablet weight from the guaifenesin dose
• Poor powder flow
• Sticking and picking during compression
• Variable extended-release dissolution
• Coating defects
• Flavor loss or interaction with packaging
• Sedimentation in liquid products
• Preservative failure
• Supply concentration among qualified excipient vendors
• Inconsistent guaifenesin particle size

A low-cost product can lose its margin through yield loss, slow compression, excessive coating time, or failed stability batches.

Intellectual-property barriers

Potentially relevant claims may cover:

• Polymer ratios
• Coated particles
• Layered tablets
• Release-control coatings
• Taste-masking compositions
• Specific guaifenesin combinations
• Manufacturing sequences
• Packaging and dosing systems

Trade secrets may protect process parameters that are not obvious from a patent. An acquirer should evaluate whether the product depends on a proprietary granulation endpoint, coating profile, particle-size specification, or supplier-specific raw material.

Which companies compete in guaifenesin?

The market includes branded consumer-health companies, private-label manufacturers, contract manufacturers, and regional OTC producers.

Segment	Representative participants	Competitive basis
Branded expectorants	Reckitt, Haleon, regional consumer-health companies	Brand awareness, pharmacy placement, combination portfolios
Private label	Retail pharmacy and mass-merchandise chains	Price, availability, retailer control
Generic OTC manufacturers	Multiple U.S. and international manufacturers	Cost, regulatory compliance, supply reliability
Contract manufacturers	CMO and CDMO suppliers	Scale, packaging, formulation capability
Ingredient suppliers	API and excipient manufacturers	Quality, capacity, particle-size control, price

Mucinex is associated with Reckitt's consumer-health portfolio. Robitussin products are associated with Haleon's consumer-health portfolio. Brand ownership, product authorization, and distribution arrangements should be verified against current company filings and product labels because portfolios change.[3][4]

What is the FDA regulatory status of guaifenesin?

Guaifenesin is an established FDA OTC active ingredient when used under the applicable monograph conditions. A monograph-compliant product typically avoids the full NDA development burden, but the manufacturer remains responsible for:

• Active and inactive ingredient compliance
• Current good manufacturing practice
• Stability
• Finished-product testing
• Labeling
• Tamper-evident packaging where applicable
• Adverse-event reporting
• Facility registration and listing
• Foreign and domestic manufacturing controls

A formulation that departs from monograph conditions, introduces a nonpermitted claim, or relies on a novel combination may require a different regulatory pathway.

Are Paragraph IV challenges relevant to guaifenesin?

Paragraph IV litigation is generally relevant only when a product relies on an abbreviated new drug application and references an NDA with listed patents. It is less central for ordinary OTC monograph guaifenesin products.

A prospective entrant should classify the target product before assessing Paragraph IV exposure:

Product type	Paragraph IV relevance
Basic OTC monograph tablet	Usually low
OTC liquid under monograph	Usually low
NDA extended-release product	Potentially relevant
Authorized generic of an NDA product	Potentially relevant
Branded combination NDA	Potentially relevant
Novel delivery system	Potentially relevant

The absence of Paragraph IV litigation does not mean the product has no commercial risk. It may indicate that market entry is governed by monograph compliance and ordinary product competition rather than patent certification.

What patent litigation and settlement risks affect guaifenesin?

Guaifenesin is not generally associated with the level of recurring high-value patent litigation seen in patented oncology, immunology, or specialty drugs. Litigation risk is more likely to involve:

• Trademark infringement
• Trade dress
• False advertising
• OTC labeling
• Product liability
• Contract manufacturing
• Quality failures
• Patent disputes over extended-release or combination formulations

Settlement agreements may arise around branded extended-release products or combination products, but they should not be assumed to exist without a docket-specific review. Any transaction involving a branded guaifenesin product should identify active litigation, consent judgments, licenses, covenant-not-to-sue arrangements, and patent assignments.

What licensing deals create opportunities in guaifenesin?

Licensing value is usually tied to the platform rather than the active ingredient. Attractive targets may include:

• Long-acting oral delivery technology
• Taste-masked high-dose particles
• Pediatric liquid platforms
• Low-volume concentrated suspensions
• Dual-layer tablets
• Stable alcohol-free formulations
• Combination-product know-how
• Regional brand and distribution rights

A license should define ownership of improvements, regulatory files, stability data, supplier qualifications, manufacturing parameters, trademarks, and rights to use clinical or consumer-preference data.

The strongest deal structure may be a regional commercialization license with supply rights, rather than a worldwide composition-of-matter license that cannot generate meaningful exclusivity.

How does guaifenesin compare with competing expectorant and cough products?

Guaifenesin competes within a broader cough, cold, and flu category that includes antitussives, decongestants, antihistamines, analgesics, saline products, and non-drug remedies.

Product category	Primary consumer need	Differentiation potential
Guaifenesin	Loosening mucus	Extended release, taste, format, combination
Dextromethorphan	Cough suppression	Dose, abuse-mitigation, combination simplicity
Phenylephrine and other decongestants	Nasal congestion	Regulatory and efficacy scrutiny
Antihistamines	Allergy and cold symptoms	Sedation profile, duration
Acetaminophen combinations	Pain and fever	Duplicate-ingredient risk
Saline and non-drug products	Moisturization and comfort	Natural positioning and device usability

Guaifenesin has a relatively straightforward regulatory profile but lower protection. Products compete primarily on price, convenience, perceived efficacy, and brand familiarity.

What generic launch scenarios exist for guaifenesin?

Immediate-release launch

This is the lowest-risk and fastest commercial pathway. The entrant can compete through private-label supply, low-cost packaging, and retailer contracts. Gross margins are typically constrained by intense price competition.

Extended-release launch

This offers better differentiation but requires more development work. The entrant must establish reproducible dissolution, manufacturing scale, and a defensible formulation position.

Pediatric liquid launch

This can achieve a stronger niche position through flavor, dosing accuracy, sugar-free claims, and caregiver-focused packaging. Commercial success depends on sensory testing and reliable retail distribution.

Combination-product launch

This can increase revenue per purchase but has higher regulatory and safety complexity. Products should minimize active-ingredient duplication and use clear symptom-specific positioning.

Regional or international launch

Guaifenesin regulatory status varies by jurisdiction. Some markets classify it as OTC, while others apply prescription, pharmacy, or national monograph requirements. Geographic expansion requires country-specific review of claims, permitted excipients, dosage limits, pack sizes, and pharmacovigilance obligations.

How strong is the guaifenesin patent estate?

The estate is weak for the active ingredient and stronger only at the product-design level.

Estate component	Relative strength
Active ingredient	Low
Immediate-release formulation	Low
Extended-release formulation	Moderate if claims remain valid and commercially relevant
Taste masking	Moderate where technically specific
Combination product	Variable
Manufacturing process	Moderate, often difficult to enforce without evidence
Trademark and trade dress	Potentially significant for established brands
Supply and distribution contracts	Commercially significant but not patent rights

Patent strength should be assessed claim by claim. A narrow formulation patent may have little blocking power if a competitor can achieve the same release profile with a different polymer system. A broader claim may face validity challenges based on earlier guaifenesin release technologies.

What is the revenue exposure and commercial opportunity?

Guaifenesin is a high-volume, low-to-moderate value OTC ingredient. Revenue exposure is greatest for companies with:

• Large respiratory-care portfolios
• Retailer shelf access
• Seasonal forecasting capability
• Combination-product brands
• Efficient tablet and liquid manufacturing
• Strong e-commerce distribution

Public companies commonly report guaifenesin within broader consumer-health categories rather than as a separate line item. SKU-level revenue analysis therefore requires retailer data, syndicated market data, shipment data, or internal sales records. Company filings can establish portfolio ownership and category exposure, but they often do not isolate guaifenesin sales.[3][4]

The most defensible commercial opportunities are:

1. Private-label extended-release tablets.
2. Sugar-free and alcohol-free liquids.
3. Pediatric and caregiver-friendly dosing formats.
4. Retail-exclusive combination products.
5. Contract manufacturing for regional brands.
6. Low-cost international products using qualified local supply.
7. Excipient or delivery platforms that can be licensed across other high-dose OTC actives.

Key Takeaways

• Guaifenesin is a mature OTC expectorant with little practical active-ingredient exclusivity.
• The FDA OTC monograph is the central U.S. regulatory pathway for ordinary products.
• Extended-release formulations provide the clearest opportunity for technical and commercial differentiation.
• Excipient strategy should focus on high-dose tablet manufacturability, dissolution control, taste masking, suspension stability, and sensory performance.
• Orange Book and Paragraph IV analysis is product-specific and more relevant to NDA-based extended-release or combination products than to basic monograph products.
• Patent risk is concentrated in formulation, process, combination, trademark, and trade-dress rights.
• Biosimilar risk is irrelevant because guaifenesin is a small-molecule drug, not a biologic.
• The strongest near-term opportunities are private label, pediatric liquids, sugar-free products, extended-release systems, and regional licensing.
• Manufacturing reliability and retail distribution are usually more important than patent exclusivity.

FAQs about guaifenesin excipients and commercial strategy

Can guaifenesin be formulated without lactose?

Yes. Microcrystalline cellulose, mannitol, dibasic calcium phosphate, starch-based materials, and other suitable diluents can support lactose-free formulations. The selected excipient must meet the target for compression, dissolution, stability, and labeling.

Which polymer is commonly evaluated first for extended-release guaifenesin?

Hypromellose is a common starting point because it is widely used, scalable, and available in multiple viscosity grades. Ethylcellulose and lipid-based systems may be evaluated when greater hydrophobic control or a multiparticulate design is required.

Is guaifenesin suitable for an orally disintegrating tablet?

It is technically possible, but the high dose creates tablet-size and taste challenges. Taste masking and rapid dispersion must be balanced against mouthfeel, compression, and stability.

Can a guaifenesin formulation receive patent protection today?

Potentially, but protection would usually need to arise from a novel and nonobvious formulation, release profile, particle system, combination, manufacturing process, or delivery method. A simple conventional tablet is unlikely to create a strong patent position.

What is the best commercial entry strategy for a new guaifenesin manufacturer?

The lowest-risk strategy is a monograph-compliant product supported by a qualified supply chain and a private-label or regional-brand customer. The higher-value strategy is an extended-release, pediatric, taste-masked, or sugar-free platform with documented manufacturing and sensory advantages.

References

1. U.S. Food and Drug Administration. (2024). 21 C.F.R. Part 341: Cold, cough, allergy, bronchodilator, and antiasthmatic drug products for over-the-counter human use. Electronic Code of Federal Regulations.

2. U.S. Food and Drug Administration. (2024). Over-the-counter monograph drugs. https://www.fda.gov/drugs/over-counter-otc-nonprescription-medicines/over-counter-otc-drug-monograph-system

3. Haleon plc. (2024). Annual report and financial statements 2023. https://www.haleon.com/investors

4. Reckitt Benckiser Group plc. (2024). Annual report and financial statements 2023. https://www.reckitt.com/investors/annual-reports/