Scope and claims of US Patent 8,828,430: what’s actually protected
US Patent 8,828,430 is a US-listed patent centered on a specific small-molecule API salt form plus a tightly constrained immediate-release tablet architecture. The claims are written to capture (1) the composition of a tablet containing a defined amount and particle-size distribution of the active and (2) manufacturing steps for that tablet, with (3) an additional method-of-use claim for treating thrombocytopenia using the claimed tablet.
Active ingredient identity (core limitation):
All composition, process, and use claims are anchored to:
3′-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2′-hydroxy-[1,1′-biphenyl]-3-carboxylic acid bis-(monoethanolamine)
Tablet particle-size distribution (hard limitation):
Each tablet requires that about 90% of the compound particles have a particle size >10 micron and <90 micron.
Tablet excipient loading range (hard limitation):
The tablet must contain 25% to 89% by weight of one or more excipients chosen from:
- microcrystalline cellulose
- powdered cellulose
- pregelatinized starch
- starch
- lactitol
- mannitol
- sorbitol
- maltodextrin
Disintegrant requirement (hard limitation):
A disintegrant is required at ≥4% by weight.
Film-coating requirement (hard limitation):
The tablet is film coated.
Optional components with caps (soft limitation):
- binder: optional, up to ~8% by weight
- lubricant: optional, up to ~2% by weight
These limitations define the protected product: not just the API salt, but the specific particle sizing, the excipient system and load, and the standard compression plus film-coat workflow.
What is the claim breadth for the tablet composition (claims 1–2)?
Featured snippet answer: Claim 1 protects a film-coated tablet containing the specified API bis-(monoethanolamine) salt with a defined particle-size distribution, a specified excipient system/load, and a minimum disintegrant level; it permits limited optional binder and lubricant.
Claim 1 (composition product): what’s “essentially” covered
Claim 1 is “a pharmaceutical tablet consisting essentially of” the defined API salt plus the listed formulation constraints. The phrase “consisting essentially of” gives modest flexibility for unlisted ingredients only if they do not materially change the basic and novel characteristics. The claim language still hard-codes:
- particle-size distribution: ~90% between 10 and 90 micron
- excipient selection list and loading: 25% to 89%
- required disintegrant: ≥4%
- film coating
- optional binder (≤8%) and lubricant (≤2%)
Claim 2 (narrow embodiment)
Claim 2 narrows Claim 1 by restricting the excipient component(s) to:
- microcrystalline cellulose + mannitol only
and keeping the same excipient loading range (25% to 89% by weight).
Practical scope effect: Claim 1 covers multi-excipient or different single-excipient selections from the broader list. Claim 2 is a specific sub-range within Claim 1’s formulation universe.
How broad are the manufacturing method claims (claims 3–4)?
Featured snippet answer: Claims 3–4 protect a compression + film-coating process using the same particle-size-qualified API and the same formulation constraints, including disintegrant level and excipient loading.
Claim 3 (process)
Claim 3 recites:
- admixture of:
- the specified API bis-(monoethanolamine) salt having the defined particle size distribution (~90% between 10 and 90 micron)
- excipients from the defined list
- further excipients (as long as they fit the “provided” formulation constraints)
- compressing into tablets
- applying a film coating
The claim is bounded by a “provided” clause requiring that each resulting tablet meets:
- excipient loading 25% to 89% (from the defined excipient list)
- disintegrant ≥4%
- binder optional ≤8%
- lubricant optional ≤2%
Claim 4 (narrower embodiment)
Claim 4 narrows Claim 3 by limiting excipients to:
- microcrystalline cellulose + mannitol only
Practical scope effect: If a commercial process uses the same API salt and particle sizing and yields tablets that meet the same excipient/disintegrant/coat constraints, Claim 3 is the main infringement pathway even if process equipment differs.
What method-of-use coverage exists for thrombocytopenia (claims 5–6, 11–12)?
Featured snippet answer: The use claims protect administering a therapeutically effective amount of the claimed tablet for treating thrombocytopenia in humans, tying infringement to using (or providing) the claimed product.
Claims 5–6
- Claim 5: administer a therapeutically effective amount of a tablet of Claim 1
- Claim 6: administer a therapeutically effective amount of a tablet of Claim 2
Claims 11–12 (same use idea, different tablet dependency)
- Claim 11: administer a therapeutically effective amount of a tablet of Claim 7
- Claim 12: administer a therapeutically effective amount of a tablet of Claim 8
These depend on the “scale” and additional production requirements in Claims 7–8.
Scope implication: The use claims do not stand alone. Their enforceability tracks the availability and use of the covered tablet formulation.
What extra limitations expand coverage to “scale” production (claims 7–8, 9–10)
Featured snippet answer: Claims 7–10 add a production-scale constraint of at least ~50,000 tablets to the composition and process, plus preserve the same core API, particle sizing, excipient load, disintegrant, and film-coating requirements.
Claim 7 (composition with scale)
Claim 7 protects a tablet containing the same API and formulation constraints as Claim 1, plus:
- tablet is produced on a scale suitable to prepare at least about 50,000 tablets
It also contains the same excipient, disintegrant, optional binder/lubricant, and film-coating limitations.
Claim 8 (scale + excipient restriction)
Claim 8 further restricts excipients to:
- microcrystalline cellulose + mannitol
while keeping the same scale requirement and other constraints.
Claim 9 (process with scale)
Claim 9 adds the “at least about 50,000 tablets” scale suitability to Claim 3’s compression + film-coating process.
Claim 10 (process with scale + excipient restriction)
Claim 10 further limits excipients to microcrystalline cellulose + mannitol.
Scope effect: These “50,000 tablet” constraints are unusual for composition patenting. They can matter in disputes where one party argues the commercial activity involved only small batch trials or non-covered scale runs, though enforcement practice varies.
Claim-to-infringement map: which design-arounds are most likely to work
Featured snippet answer: The tightest design-around levers are (1) API particle-size distribution, (2) excipient selection and load range, (3) disintegrant level, and (4) film-coating.
Below are the key “tripwires” implied by the claims:
1) Particle size window (10–90 micron; ~90% in-range)
The claims require about 90% in-range. Moving outside the window for most particles is a direct way to avoid literal coverage. Any infringement analysis would likely focus on:
- whether the product meets “about 90%”
- whether particle-size measurement matches the claim’s definition and methodology
2) Excipients list and loading (25%–89% by weight)
The claim ties both the allowed excipients and the total loading to 25%–89%. Using excipients outside the listed set, or altering total excipient mass outside the range, is another route.
3) Disintegrant ≥4% by weight
Even with the right excipients and loading, failure to meet the disintegrant minimum risks avoiding literal infringement.
4) Film coated tablets
Switching to uncoated tablets or changing the coating concept can reduce risk if the claim is interpreted strictly on “film coated.”
5) Binder and lubricant caps
Optional components have caps. If binder or lubricant exceed the specified upper limits, literal coverage is weakened.
Where this patent typically sits in a portfolio (tablet formulation vs. compound vs. indication)
Within a typical pharmaceutical IP landscape, US 8,828,430 reads as:
- formulation patent (tablet composition + particle sizing + excipients + disintegrant + coating)
- with process-by-formulation coverage (mix, compress, film coat)
- and indication method-of-use coverage (thrombocytopenia administration)
But it does not appear, from the claim text provided, to be a general compound patent covering all solid forms, all particle sizes, or all dosing regimens. Its scope is tied to a very particular solid-state and tablet build.
What patents would likely exist around it (landscape expectations, not listed here)
A complete “patent landscape” for a single US patent normally includes:
- the parent compound patents (API synthesis, salt formation, polymorph/solid-state)
- intermediate process patents (API manufacture, milling/granulation)
- other formulation patents (different excipients, different coatings, different disintegrant systems)
- manufacturing scale/technology transfer patents
- Orange Book registrations and patent litigation tied to generic or biosimilar-like entries (if applicable)
However, no supporting bibliographic data (publication number, filing/priority dates, assignee, continuation status, related family members, or Orange Book listing) was included in the prompt. Without those, a defensible mapping of “how many patents cover what” and “which companies are challenging” cannot be produced from the provided information alone.
Key takeaways
- US 8,828,430 claims are anchored to a specific API salt and a strict tablet specification: particle-size distribution (~90% between 10 and 90 micron), excipient loading (25%–89% from a defined list), disintegrant ≥4%, and film coating.
- Composition coverage is split into broad excipient-list embodiments (Claim 1/3/7) and narrower microcrystalline cellulose + mannitol only embodiments (Claim 2/4/8/10).
- Process claims track the same constraints and add compression + film coating; they are also tied to the same excipient/disintegrant/binder/lubricant caps.
- Thrombocytopenia use claims depend on using the covered tablet and therefore shift infringement risk toward the product used by prescribers and patients.
- “At least about 50,000 tablets” introduces a scale suitability limiter in Claims 7–10 that can become relevant in disputes about batch size and commercial activity.
FAQs
1) Can a generic avoid US 8,828,430 by changing excipients but keeping the same disintegrant level?
Claim scope depends on both the excipient selection list and total excipient loading (25%–89%). Changing excipients can avoid literal coverage if it breaks either element.
2) Does changing film coating to sugar coating avoid the patent?
The claims require the tablet is “film coated.” Moving away from film-coating can be a direct non-infringement lever if the product is not “film coated.”
3) Are binder and lubricant limits enforceable if they are optional?
Yes. Although binder/lubricant are “optional,” the claim still sets maximum amounts (binder up to ~8%, lubricant up to ~2%), so exceeding those limits undermines literal coverage.
4) How important is particle-size testing for infringement?
It is central. The claims require about 90% of particles to be within a specific micron window, so test results against that distribution are likely to be outcome-determinative.
5) Do the thrombocytopenia method claims cover prescribing even if a non-covered tablet is used?
No. The method claims are limited to administering a therapeutically effective amount of the tablets defined in the dependent composition claims.
References
No sources were cited.
