US Patent 12,311,057: What Is Covered, How Broad the Claims Are, and Where the Landscape Stacks Up
United States Patent 12,311,057 is directed to an oral budesonide dosage form and regimen for treating IgA nephropathy. The core of the claimed technology is (1) budesonide encapsulated within enteric-coated capsules, and (2) an extended-release polymeric blend on “plurality of cores” that is defined by specific polymer identities, composition ranges, and dissolution performance thresholds in pH 1.2 and pH ~6.5 to 6.8 media using USP<711> Apparatus 2 at 100 rpm. Claims then narrow further to specific polymer species, polymer blend ratios, enteric-coating mass, capsule size, budesonide payload, administration timing, and daily dose.
What is the invention in the independent claim?
Claim 1 defines a “pharmaceutical composition” comprising these elements, in combination:
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Drug and physical architecture
- Budesonide “encapsulated within a capsule comprising an enteric coating.”
- “Plurality of cores” inside the capsule.
- Each core is coated with an “extended release pharmaceutically-acceptable polymeric blend.”
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Polymeric blend defined by two polymer classes and exact solubility cutoffs
- Water-insoluble polymer:
- Solubility in water at 25°C: < about 0.1 mg/mL
- Present at 47 wt.% to 56 wt.% of the extended-release polymeric blend.
- Pore-forming polymer:
- Solubility in water at 25°C: ≥ about 10 mg/mL
- Present at 32 wt.% to 22 wt.% of the extended-release polymeric blend.
- The wording uses ranges that appear inverted on the face of the claim (32 wt.% to 22 wt.%). Practically, this still defines a narrow blend window between those limits.
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Amount of polymeric blend relative to the coated core weight
- The extended-release polymeric blend is present at 5 wt.% to 18 wt.% of the total coated core weight.
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Dissolution performance requirements (USP<711> Apparatus 2, 100 rpm)
- Acid stage (pH ~1.2), 120 minutes:
- “No more than about 10%” budesonide released.
- Intestinal stage (fasted simulated intestinal fluid Level 1 at pH ~6.5, or phosphate buffer pH ~6.8), 30 minutes:
- “No more than about 10%” released.
- Intestinal stage, 120 minutes:
- “At least about 70%” released into the pharmaceutically-relevant medium by 120 minutes.
This makes the claim functional in the sense that polymer selection alone is not enough; the polymer blend must achieve a two-stage release profile: strong early retention, then robust release in pH ~6.5 to 6.8 conditions by 2 hours.
What are the dependent claims narrowing (scope cutters)?
Claims 2-5 and 19-22 specify polymer identities, which materially narrow interpretive scope:
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Claim 2: water-insoluble polymer is alkyl cellulose
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Claim 3: alkyl cellulose is ethyl cellulose
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Claim 4: pore-forming polymer selected from PEG, HPMC, HPC
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Claim 5: combination: ethyl cellulose + (PEG/HPMC/HPC)
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Claim 6: extended-release polymeric blend at 6 wt.% to 13 wt.% of total coated core weight
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Claim 7: polymer blend formed by “coalesced” (coalesced by curing) coated cores:
- curing temperature 55°C to 75°C
- curing time 1 hour to 10 hours
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Claims 8-13: pharmaceutically-relevant medium specifics
- Claim 8: Level 1 fasted simulated intestinal fluid at pH 6.5
- Claim 9: includes added surfactant
- Claims 10: surfactant amount 0.5 mg/mL
- Claims 11-13: phosphate buffer at pH 6.8, with surfactant (again 0.5 mg/mL)
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Enteric coating and capsule specifications
- Claim 14: enteric coating mass 34 mg to 46 mg per capsule
- Claim 15: enteric coating mass 36 mg to 40 mg per capsule
- Claim 16: capsule size size 1
- Claim 17: budesonide amount about 4 mg per capsule
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Method claims
- Claim 18: treatment of IgA nephropathy by oral administration of claim 1 composition, daily dose about 16 mg budesonide
- Claims 25-27: administration timing:
- at least one hour before a meal
- once daily
- in the morning at least one hour before first meal
- Claims 28-30: enteric coating mass ranges and capsule size mirror composition claim limitations.
How narrow is the claim scope? (practical coverage)
Claim 1 requires all of the following simultaneously:
- Enteric coated capsule format for an oral budesonide drug product.
- Multiple cores, each with extended-release polymeric blend.
- Two-polymer blend meeting:
- water-insoluble polymer solubility < 0.1 mg/mL (25°C),
- pore-forming polymer solubility ≥ 10 mg/mL (25°C),
- narrow wt.% windows within the blend.
- Polymer blend present at 5-18 wt.% of coated core weight.
- Release thresholds in two dissolution conditions:
- <=10% release at pH 1.2 by 120 min,
- <=10% release at intestinal pH by 30 min,
-
=70% release into intestinal pH by 120 min.
- USP<711 Apparatus 2 at 100 rpm is baked into the performance requirement.
That combination is more specific than many general extended-release formulations. In landscape terms, it is the kind of claim set that typically blocks “design-around” variants that alter polymer identity, polymer ratios, blend loading, or dissolution behavior, even if they keep the overall concept of enteric coating plus extended release.
What does the dissolution profile imply for design-around risk?
The dissolution requirements impose a stringent constraint set:
Acid stage
- Media: pH about 1.2
- Requirement: <=10% released by 120 minutes
This is consistent with enteric protection and/or diffusion resistance during gastric transit.
Early intestinal stage
- Media: Level 1 fasted simulated intestinal fluid (pH about 6.5) or phosphate buffer (pH about 6.8)
- Requirement: <=10% released by 30 minutes
This is a second gating point that reduces the chance of burst release after pH upshift.
By 120 minutes
- Requirement: >=70% released by 120 minutes in intestinal media
So the system must be both:
- stable under acidic conditions and initially stable in intestinal conditions,
- then capable of release within a 2-hour window after the intestinal transition.
This is exactly the sort of multi-point functional language that courts and examiners treat as a meaningful limiting feature when an accused product’s dissolution curve differs.
Claim-by-claim landscape structure (coverage grid)
Below is a “coverage grid” mapping the independent claim elements to dependent claim narrowing.
| Element in Claim 1 |
Dependent claims that narrow it |
What gets locked in |
| Water-insoluble polymer defined by solubility <0.1 mg/mL |
2, 3, 19, 20 |
alkyl cellulose; then ethyl cellulose |
| Pore-forming polymer defined by solubility >=10 mg/mL |
4, 21, 22 |
PEG/HPMC/HPC |
| Blend ratios (47-56 wt.% insoluble; 32-22 wt.% pore-former) |
6, 23 |
narrower loading and blend amount (6-13 wt.% of total coated core weight) |
| Polymer blend loading on core (5-18 wt.% of coated core weight) |
6, 23 |
tight window 6-13 wt.% |
| Coalescing/cure conditions |
7, 24 |
55-75°C, 1-10 hours |
| Dissolution: pH 1.2 <=10% by 120 min |
built into claim 1 |
functional performance gate |
| Dissolution: pH 6.5 or 6.8 <=10% by 30 min |
8-13 |
medium identity and surfactant at 0.5 mg/mL |
| Dissolution: >=70% by 120 min |
built into claim 1 |
functional performance gate |
| Enteric coating mass 34-46 mg |
14 |
enteric coat mass window |
| Enteric coating mass 36-40 mg |
15 and 28-29 |
tighter enteric mass window |
| Capsule size |
16, 30 |
size 1 |
| Budesonide payload |
17 |
about 4 mg per capsule |
| IgA nephropathy method |
18 |
specific indication and regimen |
| Daily dose and regimen |
18, 25-27 |
about 16 mg/day; once daily morning before food |
How does this sit in the broader US oral budesonide patent landscape?
The meaningful landscape risk for competitors is less about “budesonide patents” generally and more about patents that claim:
- enteric protection for budesonide,
- extended-release multipart cores,
- polymer blends defined by solubility and composition windows, and
- multi-point dissolution curves tied to USP<711 Apparatus 2 at 100 rpm.
In US practice, this level of specificity usually creates two outcomes:
- Fencing off close formulations: if a competitor matches the dissolution curve but uses different polymer classes outside the solubility cutoffs or changes blend ratio/loading outside 5-18 wt.% or 47-56 wt.% / 22-32 wt.% windows, it may fall outside the claim.
- Enabling enforcement on functional mismatch: if a product’s dissolution profile does not match the “<=10% at pH 1.2 by 120 min” and “<=10% at intestinal pH by 30 min” gates while also meeting “>=70% by 120 min,” it can avoid the independent claim even if it uses similar polymers.
Operational implications for product developers and litigators
Key “hard stops” for design-arounds
Claim 1 is most difficult to avoid if any of the following remain unchanged:
- Enteric-coated capsule format with plurality of cores
- A two-polymer extended-release blend meeting the solubility thresholds
- Blend ratios and loadings within stated ranges
- Dissolution curve meeting the three-point matrix (pH 1.2, pH 6.5/6.8 at 30 min, pH 6.5/6.8 at 120 min)
Where competitors can carve space
The most plausible carve points, based on the claim text itself, are:
- Switch polymer systems so the water-insoluble polymer does not meet <0.1 mg/mL solubility at 25°C, or the pore-forming polymer does not meet ≥10 mg/mL at 25°C.
- Move outside blend ratio windows inside the polymer blend.
- Alter extended-release blend loading on coated core outside 5-18 wt.%.
- Shift dissolution profile so the product fails one of the three dissolution thresholds in the specified media and apparatus conditions.
The dependent claims also add additional fencing by specifying medium surfactant at 0.5 mg/mL and cure conditions. Those narrower claims can matter for infringement if a product matches claim 1 broadly and then also matches the narrower conditions.
Method-of-treatment scope: IgA nephropathy and regimen specificity
Claim 18 turns the dosage form claim into a treatment claim with:
- oral administration
- daily dose about 16 mg budesonide
- subject: IgA nephropathy
Claim 25-27 further narrow administration schedule:
- at least one hour before a meal,
- once daily,
- morning at least one hour before the first meal.
Competitors that match the dosage form but alter administration timing may still face claim 1 infringement if they use the composition, but method claims can be harder to trigger if the regimen differs.
What is the likely claim enforcement posture
With the structure present in claim 1, enforcement often pivots on dissolution testing and formulation composition evidence:
- polymer identity and weight fractions within the blend,
- polymer solubility at 25°C,
- extent and distribution of extended-release polymeric blend on cores,
- dissolution testing in USP<711 Apparatus 2 at 100 rpm under the specified media conditions (pH 1.2, Level 1 fasted simulated intestinal fluid pH 6.5, or phosphate buffer pH 6.8, including surfactant where required by dependent claims),
- enteric coating mass and capsule size/payload.
Key Takeaways
- Claim 12,311,057 is not a generic “enteric + extended-release budesonide” patent. Claim 1 requires a multipart core design, a two-polymer blend defined by solubility thresholds and specific wt.% windows, and a three-point dissolution performance profile under USP<711 Apparatus 2 at 100 rpm.
- Dependent claims materially narrow polymer identities and test media. Alkyl cellulose then ethyl cellulose, pore-formers limited to PEG/HPMC/HPC, and surfactant content fixed at 0.5 mg/mL in specified intestinal media.
- Method coverage targets IgA nephropathy with a regimen. About 16 mg/day budesonide, once daily in the morning at least one hour before the first meal.
- Design-around risk is highest when a competitor preserves both polymer chemistry and dissolution curve shape. The claim is structured to block variants that miss any of the key dissolution gates or polymer composition/solubility thresholds.
FAQs
1) Does claim 1 require specific polymer names?
No. Claim 1 defines polymers by solubility cutoffs and wt.% ranges. Polymer names appear in dependent claims (ethyl cellulose; PEG/HPMC/HPC).
2) What dissolution test controls infringement risk?
Claim 1 specifies USP<711 dissolution, Apparatus 2 (paddle), 100 rpm, with performance thresholds at pH 1.2 (120 min) and intestinal media (pH ~6.5 or ~6.8) at 30 min and 120 min.
3) Are enteric coating mass and capsule size required in the independent claim?
No. Those are in dependent claims (enteric coating mass in mg per capsule; capsule size size 1; budesonide payload about 4 mg).
4) Can a different dosing schedule avoid method claims?
It can, because dependent method claims specify timing (once daily, morning, at least one hour before first meal). Composition infringement can still remain if the product matches claim 1.
5) What is the most likely “escape hatch” for competitors?
Alter one or more of the claim-critical boundaries: polymer solubility thresholds, polymer blend ratios and loadings, cure conditions (for dependent claims), or the dissolution profile across the three specified time/media points.
References
[1] United States Patent No. 12,311,057.
