Scope of U.S. Patent 8,802,142 (Levetiracetam Tablet Formulation): Claim Coverage, Formulation Bounds, Process Limits, and US Patent-Landscape Implications
United States Patent 8,802,142 is directed to a specific levetiracetam pharmaceutical composition (predominantly tablets) defined by: (i) excipient classes and quantitative ranges, (ii) optionality with numeric upper/lower bounds, (iii) specific “species” embodiments for key excipients, and (iv) a manufacturing sequence that includes compacting and grinding before final compression. The independent claim is formulation-by-parameter; the method claim is formulation-by-process. The most infringement-sensitive elements are the levetiracetam/excipient ratios, the allowed disintegrant/gliding/binder/lubricant selections, and the “sum of excipients” cap in claim 9.
What is U.S. Patent 8,802,142 really claiming for levetiracetam compositions?
Short answer: A levetiracetam solid oral formulation with defined excipient-type and percent ranges, optionally including a coating, and optionally exemplified by tablet strengths (250 mg and 500 mg) with named excipients. Claim 23 adds a manufacturing process with step order: mix (APIs + select excipients), add lubricant, re-mix, compact, grind, then compress.
Independent claim 1: formulation definition by excipient classes + numeric ranges
Claim 1 requires:
- Active ingredient: levetiracetam
- Disintegrant: 2.0 to 9.0 wt%, selected from:
- polyvinylpolypyrrolidone
- sodium croscarmellose
- Gliding agent: 0.0 to 3.0 wt%
- Binder: 0.5 to 6.0 wt%, selected from:
- macrogol
- microcrystalline cellulose
- saccharose
- mannitol
- sorbitol
- Lubricant: 0.0 to 1.0 wt%
- All wt% are based on total composition weight
Claim 9 adds a quantitative constraint on totals:
- Sum of disintegrant + gliding agent + binder + lubricant ≤ 20 wt% (by total weight)
This means even if each component falls within its own range, infringement can be blocked if the combined excipient fractions exceed 20%.
“Species” dependent claims narrow key excipients
These convert the broad class claims into specific embodiment anchors:
- Claim 10: disintegrant is sodium croscarmellose
- Claim 11: gliding agent is anhydrous colloidal silica
- Claim 12: binder is polyethylene glycol 6000 (listed as “macrogol” in claim 1; PEG 6000 is a species)
- Claim 13: lubricant is magnesium stearate
So a product using sodium croscarmellose + colloidal silica + PEG 6000 + magnesium stearate with the specified ranges maps tightly to the “core” formulation profile.
Numeric “refinement” dependent claims (range sub-sets)
Several dependents refine sub-ranges inside the independent claim:
- Claim 2: disintegrant 3.0 to 7.0 wt%
- Claim 3: gliding agent 0.5 to 2.5 wt%
- Claim 4: binder 0.5 to 4.0 wt%
- Claim 5: binder 0.8 to 1.6 wt%
- Claim 6: lubricant 0.0 to 0.75 wt%
- Claim 7: lubricant 0.0 to 0.50 wt%
- Claim 8: lubricant 0.08 to 0.15 wt%
- Claim 14: disintegrant is sodium croscarmellose and 2.0 to 9.0 wt% (mirrors claim 1 but makes sodium croscarmellose explicit)
- Claim 15: gliding agent is anhydrous colloidal silica and 0.0 to 3.0 wt%
- Claim 16: binder is PEG 6000 and 0.5 to 6.0 wt%
- Claim 17: lubricant is magnesium stearate and 0.0 to 1.0 wt%
Formulation “amount” dependent claims: fixed compositions at named strengths
Claim 24/25 provide explicit example formulations at different strengths (by mg per tablet, consistent with wt% mapping to composition mass).
Additional dependent claims restate those example compositions (claims 33 and 34) under the process-based composition.
Claim 18 provides a high API fraction bound:
- levetiracetam 80% to 95 wt% of total composition
That is important because it narrows formulations where excipient loading is too high. It also pairs with claim 9 (sum of excipients ≤ 20%) and makes many low-API/high-excipient designs non-infringing.
Dosage form and coating coverage
- Claim 22: the composition is a tablet
- Claim 19/20/21: coating optional and specific coating agent species:
- coating agent present (claim 19)
- coating agent comprises polyvinyl alcohol (claim 20)
- coating agent is hydroxypropylmethylcellulose aqueous dispersions (claim 21)
This is a typical “composition” claim strategy: cover the core blend and leave room for standard coating operations while keeping the excipient core fixed.
What does claim 23 cover: manufacturing process steps and how they map to infringement risk?
Short answer: The manufacturing claim is a step-sequence process for making the claimed formulation. It will be implicated where a manufacturer performs the exact ordered operations including compacting, grinding, and compressing, using the same formulation parameters.
Claim 23: process with ordered unit operations
Claim 23 recites:
- Mixing levetiracetam + gliding agent + disintegrant + binder
- Adding lubricant
- Mixing the full blend (levetiracetam + gliding + disintegrant + binder + lubricant)
- Compacting the mixture obtained in (3)
- Grinding the mixture obtained in (4)
- Compressing the mixture obtained in (5)
Key infringement sensitivities:
- If a competitor blends lubricant at the start (rather than stepwise) the process may fall outside the literal sequence depending on how the steps are interpreted.
- If compacting is absent or replaced (for example, direct compression without slugging) the process claim can be avoided.
- If grinding is skipped or replaced with milling at different stage points, there is a plausible non-literal path, but the literal claim is directed to grinding after compacting.
- Even if a competitor makes a “similar” tablet, process claim 23 hinges on performing these unit operations in this order.
Process-dependent compositions (claims 26–36)
- Claim 26: pharmaceutical composition made according to process claim 23.
- Claims 27–29 specify excipient species used in the process-made composition.
- Claims 33–36 mirror the fixed example tablet compositions under the process anchor.
So the “fixed composition” is doubly tethered: to claim 1 parameters and to claim 23 manufacturing sequence.
How broad is the excipient scope: what substitutions still fall inside the claims?
Disintegrant scope
In claim 1, disintegrant is restricted to only two choices:
- polyvinylpolypyrrolidone
- sodium croscarmellose
and must be 2.0 to 9.0 wt%.
Switching to other disintegrants (crospovidone, croscarmellose calcium, starches, etc.) is an immediate route around at the formulation level, as long as the product does not literally substitute within these defined choices.
Binder scope
Binder is restricted to:
- macrogol (including but not limited to PEG families)
- microcrystalline cellulose
- saccharose
- mannitol
- sorbitol
with 0.5 to 6.0 wt%.
A product using a different binder (PVP, HPMC, povidone copolymers, pregelatinized starch) can avoid claim 1.
Gliding agent and lubricant scope
- Gliding agent has a numeric range (0.0 to 3.0 wt%) but claim 1 does not list candidate gliding agent types in the text you provided. However, claim 11 constrains one embodiment to “anhydrous colloidal silica.”
- Lubricant likewise has a numeric range (0.0 to 1.0 wt%) but type restriction appears via claim 13 (magnesium stearate species).
Practically, if a product uses a gliding agent outside “anhydrous colloidal silica,” it may avoid dependent claim 11 while still potentially falling inside claim 1 unless the gliding agent type is restricted elsewhere in the full patent text. Based on only the claim text you provided, type for gliding agent and lubricant is not explicitly limited in claim 1.
Combined excipient cap and API fraction cap
Two independent quantitative “off-ramps”:
- Claim 18: levetiracetam must be 80–95 wt%.
- Claim 9: disintegrant + gliding + binder + lubricant ≤ 20 wt%.
These work together. If a formulation includes additional excipients beyond those four classes, claim 9 does not directly limit them, but the API fraction cap (80–95) will indirectly constrain total excipient mass. A design that pushes levetiracetam below 80 wt% will miss claim 18.
Where are the clearest design-around options?
1) Swap disintegrant type
Not allowed under claim 1: use disintegrants other than polyvinylpolypyrrolidone or sodium croscarmellose.
2) Swap binder type
Not allowed under claim 1: use binders other than macrogol (PEG), microcrystalline cellulose, saccharose, mannitol, or sorbitol.
3) Push levetiracetam below the claim’s API fraction
Avoid claim 18 by using excipient-heavy tablets so levetiracetam drops below 80 wt%. Combined with claim 9, excipient loading must be controlled relative to those four component classes.
4) Avoid the claimed process sequence
If manufacturing omits compacting and the subsequent grinding step, or adds lubricant in a different sequence than claim 23, the method claim may be avoided while formulation claims remain in play.
5) Use alternative species that dodge dependent claims
Even if the composition remains within claim 1’s ranges, dependent claims 10/11/12/13 can be avoided by changing those specific excipient species. That affects dependent claim coverage but not claim 1 if the broad claim does not require species identity for gliding agent and lubricant.
How do claims 24–36 affect generic/tablet replication strategies?
The fixed numeric compositions create an “example anchor” that is often used to interpret the intended formulation space. If a competitor’s ANDA product matches those exact ratios, infringement risk rises sharply because those dependents track both the composition parameters and the process anchor (claims 26 and later).
A key feature is proportional scaling between the 250 mg and 500 mg examples:
- sodium croscarmellose is 10.75 mg at 250 mg and 21.50 mg at 500 mg (2x)
- colloidal silica is 5.188 mg and 10.375 mg (2x)
- PEG 6000 is 2.50 mg and 5.00 mg (2x)
- magnesium stearate is 0.313 mg and 0.625 mg (2x)
So the design looks internally consistent and likely intended to be strength-scaled rather than strength-specific.
What is the “claims coverage map” by product features (composition vs process vs tablet vs coating)?
Coverage matrix
| Feature |
Claim coverage |
Practical infringement trigger |
| Levetiracetam API present |
Claim 1, 18 |
Always for levetiracetam tablets |
| Disintegrant class |
Claim 1 |
Must be polyvinylpolypyrrolidone or sodium croscarmellose |
| Disintegrant wt% |
Claim 1; dependents |
Must fit 2–9 wt% (or sub-ranges) |
| Gliding agent wt% |
Claim 1 |
0–3 wt% (sub-ranges in claims 3/15) |
| Binder class |
Claim 1 |
Must be macrogol/PEG, MCC, saccharose, mannitol, sorbitol |
| Binder wt% |
Claim 1; dependents |
0.5–6 wt% with tighter dependent options |
| Lubricant wt% |
Claim 1; dependents |
0–1 wt% with tighter dependent options |
| Total excipient cap |
Claim 9 |
Sum (disintegrant+gliding+binder+lubricant) ≤ 20 wt% |
| API fraction cap |
Claim 18 |
80–95 wt% levetiracetam |
| Tablet dosage form |
Claim 22 |
Solid compressed tablet |
| Coating agent |
Claim 19–21 |
If coating uses specified agents/types |
| Manufacturing sequence |
Claim 23 |
Mix order + compact + grind + compress |
| Strength-specific composition amounts |
Claims 24–25; 33–34 |
Exact mg match strongly increases literal risk |
US patent landscape around U.S. Patent 8,802,142: what other IP categories typically coexist for levetiracetam tablets
A complete landscape requires the patent’s family, priority, assignees, prosecution history, and the Orange Book listings for specific NDA/ANDA products. That information is not provided in your prompt, so only claim-scoped landscape implications can be stated from the claim text.
Most relevant adjacent patent categories to test in a diligence program
For levetiracetam solid oral forms, typical competing estates include:
- Other excipient systems (different disintegrants, binders, or lubricants)
- Manufacturing/process claims for direct compression or alternative granulation/slugging sequences
- Coating/process claims for film coating compositions and parameters
- Particle engineering (granule sizing, flow properties) tied to dissolution profiles
- Method-of-use claims are usually less common for an already-established API, but still occur for specific regimens or patient subsets
How to read 8,802,142 within that landscape
This patent is narrowly excipient- and process-sequence anchored, not a novel API. It is therefore most likely to be a “formulation barrier” against generics that use a near-neighbor blend and similar tablet manufacturing.
Key Takeaways
- U.S. Patent 8,802,142 is an excipient-bound levetiracetam tablet patent centered on sodium croscarmellose (or polyvinylpolypyrrolidone), gliding agent (numerically constrained), PEG-family or other enumerated binders, and lubricant (numerically constrained), with additional caps on total excipient fractions and levetiracetam wt%.
- The formulation core is claim 1, tightened by:
- claim 9 (sum of four excipient categories ≤ 20 wt%)
- claim 18 (levetiracetam 80–95 wt%)
- The process claim (claim 23) is the second pillar: mix, add lubricant, mix, compact, grind, compress. Manufacturing that omits compacting or grinding, or reorders lubricant addition, can reduce process-claim exposure.
- Strength-specific fixed examples (claims 24–25, and 33–34) indicate an intended strength scaling and provide high-risk literal match points.
- Design-arounds most plausibly come from swapping the disintegrant or binder to non-enumerated types, adjusting API fraction/excipient loading to breach claim 18 or claim 9, and altering the compaction/grinding/compression process sequence.
FAQs
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Can a levetiracetam tablet avoid U.S. Patent 8,802,142 by changing sodium croscarmellose to another disintegrant?
Yes, if the disintegrant is not polyvinylpolypyrrolidone or sodium croscarmellose or if the formulation falls outside the 2.0–9.0 wt% bound.
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Does claim 9’s “sum of excipients ≤ 20%” matter if each excipient is within its own wt% range?
Yes. A formulation can satisfy individual ranges yet still infringe claim 1 while failing claim 9, depending on the total of disintegrant + gliding agent + binder + lubricant.
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Is the “process” in claim 23 infringement-riskier than the formulation claim 1?
Typically, process is narrower because it requires a specific step sequence including compacting and grinding, but it can still matter if a competitor uses that sequence to make tablets with the claimed blend.
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Do the coating claims expand infringement beyond the tablet core?
They can, if the product includes a coating agent and that coating agent matches the claim’s species (polyvinyl alcohol and/or hydroxypropylmethylcellulose aqueous dispersions).
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If a generic matches the 250 mg or 500 mg example mg amounts exactly, is it automatically within the claims?
Matching the example composition is a high-risk indicator for the dependent claims that recite those exact amounts, and it also tends to fall within claim 1’s numeric structure if the wt% bounds align.
References (APA)
No external sources were used. Only the claim text provided in the prompt was analyzed.
