United States Patent 12,551,448: Scope, Claim Architecture, and Practical Patent-Landscape Read
United States Drug Patent 12,551,448 is directed to high-load immediate-release-style tablet formulations of ibrutinib using a defined high ibrutinib loading threshold (≥50% w/w) plus a specific excipient set. The claim set is structured as a broad formulation genus with nested fallback versions that fix (i) the ibrutinib loading window (about 60% to about 80% w/w) and (ii) key excipient exemplars including lactose as diluent (8% to 14% w/w), croscarmellose as disintegrant, hydroxypropyl cellulose or polyvinylpyrrolidone as binder, sodium lauryl sulfate as surfactant, silica as glidant, and (in certain dependent claim groupings) magnesium stearate as lubricant.
What is the claim scope in plain, enforceable terms?
1) Core independent claim coverage (high-load ibrutinib tablets with a constrained excipient system)
Claim 1 is the broadest stated scope and defines the invention by three layers:
Layer A: Active identity
- The tablet formulation comprises ibrutinib
- Ibrutinib is “a compound with the structure of Compound 1”
Layer B: Loading threshold
- Formulation comprises at least 50% w/w of ibrutinib
Layer C: Excipients are drawn from a set with defined functional classes
- Excipients selected from:
- diluents
- binders
- disintegrating agents
- lubricants
- glidants
- surfactants
- Then the claim locks particular exemplars for key functional categories:
- diluent: selected from a long list including lactose, cellulose, microcrystalline cellulose, etc.
- disintegrating agent: selected from a long list including croscarmellose / croscarmellose sodium and multiple other cross-linked polymers and starch-based materials
- binder: hydroxypropyl cellulose or polyvinylpyrrolidone
- surfactant: sodium lauryl sulfate
- glidant: silica
Claims 8, 15, and 22 broaden the same concept through slightly different dependent structuring, including an explicit addition of magnesium stearate as lubricant in claim 8/22 groupings.
2) Loading window narrowing (fallback)
Across the dependent claim set, the formulation range is tightened:
- Dependent claims cover formulations comprising about 60% w/w to about 80% w/w of ibrutinib (e.g., Claims 2, 9, 16, 23).
This creates a clear “infringement zone” that is narrower than the genus (≥50%) but more operationally concrete for formulation teams.
3) Diluent-specific fallback (lactose fixed and quantified)
Several dependent claims select lactose as the diluent and quantify it:
- Diluent is selected from lactose, cellulose, or microcrystalline cellulose (Claims 4, 11, 18, 25)
- Diluent is lactose with lactose present from about 8% w/w to about 14% w/w (Claims 5, 12, 19, 26)
This is a high-value limitation because it pins both the material identity and a quantitative band.
4) Disintegrant-specific fallback (croscarmellose fixed)
Multiple dependent claims pin the disintegrant:
- Disintegrating agent is croscarmellose (Claims 7, 14, 21, 27, 28 depending on the claim group)
This provides another concrete non-generic element.
5) Lubricant inclusion (magnesium stearate)
In the claim groupings that explicitly add a lubricant category exemplar:
- Claim 8 includes lubricant is magnesium stearate
- Claim 22 includes “a glidant … silica; and a lubricant” (but the provided claim text does not explicitly identify the lubricant exemplar in claim 22 in the excerpt you provided; claim 8 does)
6) Compound 1 definition is central but not disclosed in the excerpt
All claims tie to “Compound 1” structure. The excerpt does not reproduce the chemical structure or IUPAC description, so the enforceable scope depends on that reference definition within the patent specification.
How is the excipient system constrained (and where are the enforceable choke points)?
Excipients by functional class (as recited)
| Functional excipient class |
Claim recitation |
Enforceable exemplars in your provided claims |
| Diluent |
Must be one or more selected from a list |
lactose, sucrose, dextrose, dextrates, maltodextrin, mannitol, xylitol, sorbitol, cyclodextrins, calcium phosphate, calcium sulfate, starches, modified starches, cellulose, microcrystalline cellulose, microcellulose, talc |
| Disintegrating agent |
Must be one or more selected from a list |
natural starch, pregelatinized starch, sodium starch, methylcrystalline cellulose, methylcellulose, croscarmellose, croscarmellose sodium, cross-linked sodium carboxymethylcellulose, cross-linked carboxymethylcellulose, cross-linked croscarmellose, cross-linked starch (e.g., sodium starch glycolate), crospovidone, cross-linked polyvinylpyrrolidone, sodium alginate, clay, gum |
| Binder |
Must be selected from a limited set |
hydroxypropyl cellulose and polyvinylpyrrolidone |
| Surfactant |
Limited to one exemplar |
sodium lauryl sulfate |
| Glidant |
Limited to one exemplar |
silica |
| Lubricant |
Included in some claim variants; not fully identified in all provided excerpts |
magnesium stearate (in Claim 8; Claim 22 says “a lubricant” without specifying exemplar in the excerpt you provided) |
Three practical “choke points”
- High loading threshold: ≥50% w/w ibrutinib
- Sodium lauryl sulfate + silica: surfactant and glidant identity are fixed (in Claim 1 and its equivalents)
- Fallback quantification for lactose: 8% to 14% w/w lactose
- Fallback identity for disintegrant: croscarmellose
- Secondary fallback range for loading: 60% to 80% w/w
Any formulation that avoids one of these fixed material identities (e.g., swaps sodium lauryl sulfate) or materially alters lactose banding (or targets a loading below 50%) is less likely to land inside the claim set, assuming the remaining excipient classes still satisfy the lists.
Claim-by-claim scope map (what each claim adds)
Claims 1 and 8: Broad independent coverage with fixed surfactant and glidant
Claims 2 and 9: Quantitative loading window
- Adds: about 60% w/w to about 80% w/w.
Claims 3-7: Diluent and disintegrant tightening
- Claim 3: “At least one excipient is a diluent”
- Claim 4: diluent is lactose, cellulose, or microcrystalline cellulose
- Claim 5: diluent is lactose and lactose is 8% to 14% w/w
- Claim 6: at least one disintegrating agent present
- Claim 7: disintegrating agent is croscarmellose
Claims 15-16 and 22-23: Alternate dependent claim sets with excipient-group framing
Your excerpt includes overlapping structure where claims 15 and 22 describe compositions by explicitly listing diluent/disintegrant/binder/surfactant/glidant groups. These do not change the underlying excipient identities but change the claim’s phrasing structure.
What does the patent landscape likely look like around this formulation space?
A formulation patent landscape for a drug like ibrutinib typically clusters into:
- Drug substance and crystalline form patents
- Salt/formulation patents (tablet/capsule, excipient systems, processing)
- High-loading and dose-dense tablet patents (key when doses are large and conventional tablet sizes become impractical)
- Bioavailability / disintegration / dissolution performance patents
- Manufacturing process patents for direct compression vs wet granulation
Within that ecosystem, the distinctive feature in your claim set is the combination of:
- dose-dense / high-load tablet structure (≥50% w/w)
- specific excipient identity constraints (not just “pharmaceutically acceptable”; surfactant and glidant are locked)
- explicit diluent and disintegrant fallbacks (lactose in a quant band; croscarmellose)
Positioning effect
In practical infringement analysis, a high-load tablet patent with fixed excipient identities tends to narrow design-around options relative to a formulation claim that only requires general excipient functionality. Here, surfactant (sodium lauryl sulfate) and glidant (silica) are fixed, and the “easy” design-around paths are:
- Change surfactant away from sodium lauryl sulfate
- Change glidant away from silica
- Change disintegrant away from croscarmellose (if targeting dependent claim infringement)
- Drop loading below the ≥50% w/w floor
- Alter lactose band away from 8% to 14% w/w (for dependent claims tied to lactose amount)
That makes the patent a meaningful constraint if a generic or follow-on developer wants both high loading and these excipient choices.
Freedom-to-operate (FTO) reading: where risk is highest vs lowest
Highest literal risk
A product that matches all of the following is highest risk:
- Ibrutinib loading ≥50% w/w
- Uses sodium lauryl sulfate as the surfactant
- Uses silica as glidant
- Uses binder from hydroxypropyl cellulose or polyvinylpyrrolidone
- Uses diluent and disintegrant within the listed classes
- If matching dependent coverage: lactose at 8% to 14% w/w and disintegrant croscarmellose
Medium risk
- Matching the core high-load and excipient-class framework, but substituting lactose away from 8% to 14% (for dependent claims)
- Substituting disintegrant away from croscarmellose (reduces dependent risk but core Claim 1 still requires disintegrant selected from the list, so risk depends on the specific disintegrant chosen within the allowed list)
Lower risk
- Substituting surfactant away from sodium lauryl sulfate, or glidant away from silica, assuming those swaps stay outside the claim’s “surfactant is sodium lauryl sulfate” and “glidant is silica” limitations.
- Reducing ibrutinib loading below 50% w/w
- Using different binder(s) if the claim requires binder selected from hydroxypropyl cellulose or polyvinylpyrrolidone
Key design-around levers implied by the claim text
| Lever |
What to change |
Claim language that becomes avoided |
| Surfactant |
Replace sodium lauryl sulfate |
“surfactant is sodium lauryl sulfate” (Claim 1 and equivalents) |
| Glidant |
Replace silica |
“glidant is silica” (Claim 1 and equivalents) |
| Loading |
Reduce ibrutinib loading below 50% w/w |
“comprises at least 50% w/w of ibrutinib” |
| Lactose amount (dependent) |
Move lactose outside 8% to 14% w/w |
“lactose present in an amount from about 8% w/w to about 14% w/w” |
| Disintegrant (dependent) |
Use a disintegrant other than croscarmellose |
“disintegrating agent is croscarmellose” |
| Lubricant (dependent group) |
Replace magnesium stearate |
“lubricant is magnesium stearate” (Claim 8 grouping) |
What is missing for an evidence-grade “full landscape” and how it affects claim-to-portfolio mapping?
A full, citation-backed US landscape normally requires:
- The patent’s bibliographic details (assignee, priority dates, expiration dates, continuations)
- Claim set as issued (including whether any amended claims differ from your excerpt)
- The underlying specification’s “Compound 1” definition
- Identification of related family members and prosecution history
Your prompt provides only the claim text. Without publication identifiers (publication number, filing date, family members) and without access to the patent record, a complete cross-patent landscape with other US patents by number, assignee, and family linkage cannot be built in a way that meets an evidence-grade standard.
Accordingly, the landscape analysis above focuses on scope mechanics and design-around implications derived directly from the claim language you provided.
Key Takeaways
- US 12,551,448 claims dose-dense tablets comprising ibrutinib at ≥50% w/w.
- The independent claim scope is constrained by a defined excipient architecture with fixed identities for surfactant (sodium lauryl sulfate) and glidant (silica) plus binders restricted to hydroxypropyl cellulose or polyvinylpyrrolidone.
- The highest-friction dependent limitations are:
- ibrutinib 60% to 80% w/w
- lactose diluent at 8% to 14% w/w
- croscarmellose as disintegrant
- magnesium stearate in the lubricant-specific claim variant.
- The most direct design-around levers are changing surfactant or glidant, or reducing ibrutinib loading below 50% w/w, or moving off the dependent numeric banding and specific disintegrant/lubricant exemplars.
FAQs
-
Is the patent limited to any specific tablet manufacturing method (direct compression vs granulation)?
The provided claims specify composition elements but do not recite processing steps or manufacturing method limitations.
-
What is the strictest concentration limitation in the claim set?
The strictest quantitative limiter in the excerpt is lactose present at about 8% w/w to about 14% w/w (dependent claims), paired with the high-load ≥50% w/w threshold (independent) and the 60% to 80% w/w window (dependent).
-
Can a formulation infringe even if it does not use croscarmellose?
It may still fall within broader coverage if it satisfies Claim 1’s core structure, because Claim 1 permits disintegrants selected from a list; croscarmellose is required only in dependent claims as recited.
-
Which excipients are “fixed” rather than “selected from a list” in Claim 1?
Sodium lauryl sulfate (surfactant) and silica (glidant) are fixed in Claim 1 as provided.
-
How does the added lubricant limitation change risk?
The presence of magnesium stearate is explicitly included in the Claim 8 grouping as provided; using a different lubricant can reduce risk for that specific dependent framing, while core coverage remains governed by the fixed surfactant and glidant plus the ≥50% loading requirement.
References
No external sources were used or cited because your prompt did not include bibliographic identifiers or patent-record details beyond the claim text.
