United States Patent 5,288,480 (Oral plaque-bonding antibacterial compositions): Scope, claim map, and US patent landscape

U.S. Patent 5,288,480 protects an oral, water-humectant-based composition designed to deposit a “plaque-inhibiting” antibacterial agent onto tooth and gum surfaces using a dedicated “antibacterial-enhancing agent” that includes (i) at least one delivery-enhancing functional group and (ii) at least one organic retention-enhancing group, while excluding polyphosphate anticalculus agents (in effective amounts) and excluding a polyethylene glycol (PEG) vehicle that would reduce antibacterial activity.

What patents protect oral plaque-inhibiting antibacterial agents with delivery- and retention-enhancing functional groups?

Answer (scope in one line). US 5,288,480 covers a specific combination: (1) a humectant aqueous vehicle, (2) 5–30 wt% siliceous polishing agent, (3) 0.25–0.35 wt% of a substantially water-insoluble noncationic antibacterial agent (with enumerated chemical classes and a specific preferred example), and (4) 0.05–4 wt% of an antibacterial-enhancing agent having both a delivery-enhancing group and a retention-enhancing group, with explicit negative limitations on polyphosphates and PEG.

Core claim 1 claim elements (practical claim chart)

Below is the “must-include” structure of claim 1 mapped to likely formulation design decisions.

Claim 1 element	Exact claim requirement	Formulation implication / design constraint
Dosage form type	“oral composition” for attaching/ adhering/ bonding a plaque-inhibiting agent to oral tooth and gum surface	Requires surface deposition/bonding purpose; typical toothpaste-gel/mouth formulation positioning
Vehicle	“orally acceptable aqueous humectant vehicle” and “vehicle is other than polyethylene glycol”	PEG-containing vehicles are outside claim; humectants must be other than PEG (at least for the vehicle as recited)
Polishing system	“about 5-30% by weight of a siliceous polishing agent”	Must include silica polishing abrasive in that range
Antibacterial agent	“about 0.25%-0.35% by weight” of “substantially water insoluble noncationic antibacterial agent”	Must use a poorly water-soluble non-cationic antibacterial at narrow wt% band
Antibacterial-enhancing agent	“about 0.05-4% by weight” antibacterial-enhancing agent with delivery-enhancing functional group AND retention-enhancing functional group	This is the distinguishing “deposition technology” layer
Delivery enhancement group	delivery-enhancing group “enhances delivery” to tooth/gum surfaces	Often acidic/phosphonic/phosphoric/sulfonic motif; claim 8–14 narrow examples
Retention enhancement group	retention-enhancing group “enhances attachment/adherence/bonding”	Requires organic retention motif, structurally defined by the claim formula
Surface active + flavor	at least one surface active agent and/or flavoring oil	Not limiting to both, but at least one of those categories
Anticalculus exclusion	“free of polyphosphate anticalculus agent in an effective anticalculus amount”	Polyphosphate anticalculus actives excluded if present at effective anticalculus level
Functional constraints	delivery-enhancing group + retention-enhancing group are part of the antibacterial-enhancing agent	Enhancer must be a multifunctional delivery/retention material, not separate additives (per claim structure)

Claim 1’s functional “delivery/retention enhancer” is the key differentiator

The patent’s claim language requires that the antibacterial-enhancing agent contains:

A delivery-enhancing functional group (delivery-to-surface role), and
An organic retention-enhancing group (attachment/bonding role).

Claim 9 then defines retention-enhancing group more structurally.

Claim 2–4: the antibacterial agent is a constrained chemical set

Claim 2 restricts the antibacterial agent to one of these classes:

Halogenated diphenyl ethers
Halogenated salicylanilides
Benzoic esters
Halogenated carbanilides
Phenolic compounds

Claim 3 narrows to halogenated diphenyl ether.

Claim 4 narrows further to 2,4,4’-trichloro-2’-hydroxyphenyl ether (a specific, enumerated antibacterial).

Practical implication: if a competitor formulates with an antibacterial outside these classes, it avoids the narrowed claim path. If it uses one inside the class but at a concentration outside 0.25–0.35 wt%, it also misses claim 1’s concentration limitation.

Claim 5–6: typical formulation ranges for surfactant and flavor

Claim 5: surface active agent 0.5–5 wt%
Claim 6: flavoring oil 0.1–5 wt%

These are common toothpaste design parameters; the patent’s non-obviousness is likely carried by the antibacterial-enhancer functional architecture and the excluded PEG/polyanionic exclusions.

Claim 7–14: enhancer chemistry is defined broadly then narrowed

Claim 7 sets enhancer molecular weight range: ~100 to ~1,000,000.

Claim 8 narrows delivery-enhancing group to “acidic.”

Claim 9 defines delivery and retention groups and provides the retention formula:

Delivery group types: carboxylic, phosphoric, phosphinic, sulfonic acids and salts.
Retention-enhancing group comprises formula: --(X)n--R
- X can be O, N, S, SO, SO2, P, PO, or Si
- R is hydrophobic or inert-substituted moiety types
- n can be 0 or 1+

Claim 9 also defines the antibacterial-enhancing agent as a natural or synthetic monomer/polymer selection:

oligomers, homopolymers, copolymers, ionomers
block/graft copolymers
cross-linked polymers

Claim 10: “anionic polymer containing a plurality of” both delivery and retention groups.

Claim 13–14: further narrows the delivery group to phosphonic, and gives specific polymer exemplars:

poly(β-styrenephosphonic acid)
poly(α-styrenephosphonic acid)
copolymers of styrenephosphonic acid with other ethylenically unsaturated polymerizable monomers

Practical implication: a product using a phosphonic acid polymer architecture for enhancer delivery/retention fits tightly with claims 8, 9, 10, 13, 14.

Claim 15: fluoride-providing source inclusion

Claim 15 adds compatibility with fluoride-providing source, but it does not remove other constraints; therefore, fluoride addition does not create a workaround if the other claim limitations remain.

How does US 5,288,480 compare with common plaque-control and antiplaque polymer deposition technologies?

Answer (comparative positioning). US 5,288,480 is an “engineered deposition” formulation: it relies on an antibacterial that is substantially water-insoluble plus a polymeric, multifunctional acidic delivery/organic retention enhancer, coupled with silica polishing and strict excipients exclusions (polyphosphate anticalculus at effective amounts; PEG vehicle).

Design-around levers implied by the claim structure

The claim’s negative limitations and narrow quantitative bands create identifiable “escape hatches”:

PEG vehicle exclusion (claim 1):
- A formulation using PEG as the vehicle (or with the vehicle being PEG) risks falling outside claim 1 because the vehicle must be “other than polyethylene glycol.”
Siliceous polishing agent range (5–30 wt%):
- Changing the abrasive system and/or concentration may avoid the claim if outside range or not “siliceous polishing agent.”
Antibacterial concentration band (0.25–0.35 wt%):
- Even within the same antibacterial class, concentration changes can reduce literal coverage.
Polyphosphate anticalculus exclusion:
- A product using polyphosphate anticalculus agents at effective levels may fall outside claim 1 because claim 1 requires the composition be “free” of such agents.
Antibacterial chemical class:
- If the antibacterial is not within the listed classes (or not within halogenated diphenyl ether if targeting claims 3–4), narrower dependent claims do not read.

Note: these are claim-language levers rather than an assurance of non-infringement; the literal scope is driven by exact composition and functional enhancer structure.

When does US 5,288,480 lose exclusivity for generic or reformulated tooth/gum antibacterials?

Answer. Not computable from the provided information. Patent expiration depends on the application filing/priority date and maintenance status; exclusivity for generic entry also depends on FDA listing and any Hatch-Waxman litigation posture tied to the specific NDA/ANDA/BLA holder and Orange Book listing. No filing, priority, or FDA listing data is included in the prompt, so expiration and generic timing cannot be stated accurately.

What Orange Book status applies to US 5,288,480?

Answer. Not computable from the provided information. Orange Book status requires the specific reference product/NDA-ANDA link and listing details; none are provided.

What patent estate exists around the same antibacterial deposition concept (delivery/retention enhancers)?

Answer. Not computable from the provided information. A landscape requires bibliographic data for US 5,288,480 (assignee, filing date, continuation families, related patents/citations, and subsequent prosecutions) and/or a claim- and assignee-linked search. None of that metadata is supplied in the prompt.

What formulations are protected by the claim’s siliceous polishing and water-insoluble antibacterial constraints?

Answer (protected formulation archetypes). The claim covers an oral aqueous-humectant-based plaque-inhibiting antibacterial composition with:

silica polishing at 5–30 wt%
water-insoluble noncationic antibacterial at 0.25–0.35 wt%
multifunctional acidic delivery/organic retention polymer enhancer at 0.05–4 wt%
at least one surfactant and/or flavor oil
no polyphosphate anticalculus agent at effective anticalculus amounts
a vehicle that is not polyethylene glycol
optional fluoride source

Example fit-for-claim pathways (by claim narrowing)

The “most constrained” fit is:

Antibacterial: halogenated diphenyl ether, specifically 2,4,4’-trichloro-2’-hydroxyphenyl ether
Enhancer: anionic phosphonic acid polymer such as poly(β-styrenephosphonic acid) or poly(α-styrenephosphonic acid) or related copolymers

That combination aligns with dependent claim pathways (2 → 3 → 4 and 7 → 8 → 9 → 10 → 13 → 14).

How strong are the claims for litigation and licensing leverage?

Answer (strength drivers). Strength is built on tight, cumulative compositional limitations that reduce ambiguity:

specific concentration bands for antibacterial and enhancer
specific vehicle exclusion (non-PEG)
specific abrasive type and range (siliceous polishing 5–30%)
explicit structural functional requirements for enhancer (delivery group + retention group), with narrowing examples (acidic/phosphonic; polymer types)

Potential vulnerability driver: the broad polymer definition in claim 9 (retention group formula and polymer class) may still face validity challenges if the field already disclosed similar acidic/phosphonic retention polymers used to deposit actives on oral surfaces. But that is an assertion that requires citation data; none is provided in the prompt.

What are the most likely infringement/validity attack points based on claim wording alone?

Infringement: composition matching

Most infringement disputes in this claim class turn on whether the accused product:

contains the specific antibacterial chemical class at the specified 0.25–0.35 wt% band
uses a vehicle “other than polyethylene glycol”
uses silica polishing in the specified wt% range
includes the enhancer at 0.05–4 wt% and whether the enhancer contains both delivery and retention functional groups in the same antibacterial-enhancing agent
avoids polyphosphate anticalculus agents at effective levels (or contains none)

Validity: breadth of functional polymer architecture

The enhancer is defined by:

acidic delivery group classes and salts
retention group generic formula and its allowable atom types
polymer backbones and macromolecular types

If prior art disclosed multifunctional acidic/phosphonic polymers used in oral antibacterial delivery with retention motifs, claim 1 and its dependent polymer claims could face obviousness/anticipation issues. Resolving that requires a search that is not included in the prompt.

Key Takeaways

US 5,288,480 protects an oral antibacterial formulation engineered for tooth/gum surface deposition using a multifunctional antibacterial-enhancing agent with both delivery and retention functional groups.
Claim 1 is narrowed by cumulative quantitative and compositional constraints: aqueous humectant vehicle (non-PEG), silica polishing 5–30 wt%, water-insoluble noncationic antibacterial 0.25–0.35 wt%, and enhancer 0.05–4 wt%, plus explicit exclusions (polyphosphate anticalculus at effective levels).
Dependent claims tightly narrow antibacterial chemistry to halogenated diphenyl ethers (including the specific 2,4,4’-trichloro-2’-hydroxyphenyl ether) and narrow enhancer chemistry to acidic and especially phosphonic anionic polymers like styrenephosphonic acid polymers.
Expiration timing, Orange Book status, and the wider US patent landscape cannot be determined from the claim text alone because no bibliographic metadata, assignee, family data, or FDA product linkage is provided.

FAQs

1. Does US 5,288,480 require the antibacterial-enhancing agent to contain both delivery and retention groups in the same molecule?
Yes. Claim 1 requires “an antibacterial-enhancing agent which contains at least one delivery-enhancing functional group and at least one organic retention-enhancing group,” and the enhancer’s delivery group enhances delivery while the retention group enhances attachment/bonding.

2. Can a PEG-containing vehicle avoid claim 1?
Claim 1 requires the vehicle be “other than polyethylene glycol.” If the vehicle is PEG, the literal “vehicle is other than” limitation is not met.

3. What antibacterial classes are covered?
Claim 2 limits to halogenated diphenyl ethers, halogenated salicylanilides, benzoic esters, halogenated carbanilides, and phenolic compounds.

4. What are the key concentration limits that define the scope?
Claim 1 sets: antibacterial 0.25–0.35 wt%, siliceous polishing 5–30 wt%, and antibacterial-enhancing agent 0.05–4 wt%, all within the aqueous humectant vehicle composition.

5. Is a fluoride source allowed?
Yes. Claim 15 adds that the oral composition according to claims 1–14 can contain a fluoride-providing source.

References

No sources were cited because no external bibliographic, prosecution, FDA/Orange Book, litigation, or prior-art documents were provided in the prompt.

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	243371	⤷ Start Trial
Argentina	244259	⤷ Start Trial
Austria	119764	⤷ Start Trial
Austria	138557	⤷ Start Trial
Austria	150291	⤷ Start Trial
Austria	157533	⤷ Start Trial
Austria	207731	⤷ Start Trial
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Details for Patent: 5,288,480

Summary for Patent: 5,288,480