United States Patent 11,260,064 (budesonide + ascorbic acid/ascorbate antioxidant) claim scope, coverage map, and US patent landscape
Executive summary: US Patent 11,260,064 claims an oral budesonide pharmaceutical composition formulated with a defined oxidation-control antioxidant system: 0.05% to 0.5% w/w of ascorbic acid + a pharmaceutically acceptable ascorbate salt, optionally with flavoring and/or sweetener, and meeting a tight quality constraint of <0.3% oxidative-degradation impurities (including 21-dehydrobudesonide) and non-discoloration after storage intervals. Dependent claims layer pH (4 to 5.2), preservatives (sodium benzoate/potassium sorbate), post-storage impurity thresholds (down to <0.2% after two months), and a kit embodiment. The strongest competitive risk is for any oral budesonide product (including modified-release or enteric-coated forms) that is marketed or manufactured with the same ascorbic acid/ascorbate antioxidant pairing at the claimed range and that targets the same oxidation/impurity/discoloration performance metrics.
What does US Patent 11,260,064 claim for oral budesonide antioxidant stabilization?
Core independent claim (Claim 1) coverage in plain terms
Claim 1 is directed to an oral budesonide composition that satisfies all of the following simultaneously:
- Drug substance: budesonide (no restriction to a specific polymorph, particle size, or dosage form in Claim 1 language).
- Antioxidant system: an antioxidant amount of about 0.05% to about 0.5% w/w.
- Antioxidant identity: the antioxidant comprises a combination of ascorbic acid and a pharmaceutically acceptable salt of ascorbate.
- Palatability excipients: includes a flavoring agent and/or a sweetener (not necessarily both).
- Oxidative-degradation impurity limit: the composition has <0.3% impurities formed by oxidative degradation.
- Intended route: oral administration.
Key enforceability levers
- The claim is performance-linked (“less than 0.3% impurities formed by oxidative degradation”) rather than purely compositional.
- The antioxidant system is chemically specific (ascorbic acid + ascorbate salt) and quantitatively bounded (0.05% to 0.5% w/w).
- The composition includes flavoring/sweetener, narrowing the claim away from some strictly taste-masked or purely capsule-coating-only oral embodiments.
- There is no explicit restriction to a particular budesonide formulation technology (capsule, tablet, suspension, granules), but in practice the oxidative impurity and discoloration metrics typically implicate the final dosage form and packaging/stability context.
How do dependent claims narrow the claim 1 stabilization performance over time?
Claims 2 through 7 add storage-duration and impurity/discoloration constraints:
- Claim 2: after one month storage, oxidative degradation impurities remain <0.3%.
- Claim 3: after one month, the composition does not discolor.
- Claim 4: after two months, <0.3% oxidative-degradation impurities and no discoloration.
- Claim 5: after three months, <0.3% oxidative-degradation impurities.
- Claim 6: after two months, impurities formed by oxidative degradation are <0.2%.
- Claim 7: impurities are specified to include 21-dehydrobudesonide.
Practical scope implication
Any competitor product designed to keep budesonide below a particular oxidative impurity threshold and avoid discoloration can fall within the claim if it also uses the ascorbic acid/ascorbate antioxidant pairing at the claimed range and meets the performance metrics at the claimed storage points.
What pH window is protected under US 11,260,064?
- Claim 8: composition pH between about 4 and about 5.2.
This is a substantive formulation limiter. Many oral budesonide dosage forms use acidic microenvironments or buffering systems to improve stability. If a competitor operates outside 4–5.2 (or argues that the measured pH is outside the “about” range), it may design around.
What preservative system is explicitly covered?
- Claim 9: composition further comprises a preservative.
- Claim 10: preservative is sodium benzoate and/or potassium sorbate.
Because these are optional dependent elements, they matter in two ways:
- If a competitor includes these preservatives alongside the antioxidant system, risk increases.
- If a competitor uses different preservatives (or none), it does not automatically exit Claim 1 because Claims 9–10 are dependent; however, prosecution history and written description can affect how strictly a court reads the “further comprising” language.
How is the antioxidant ratio/amount quantified in the claims?
- Claim 11: the ascorbic acid + ascorbate salt combination is present 0.1% to 0.5% w/w.
Compared with Claim 1’s broader 0.05% to 0.5%, Claim 11 tightens a minimum of 0.1%. A product with antioxidant at ~0.06%–0.09% could still theoretically satisfy Claim 1 but would miss Claim 11. In litigation, claim-dependent distinctions are often used to allocate infringement proof for particular compositions.
What does the “kit” claim cover?
- Claim 12: a kit for treating/inflammation associated with gastrointestinal inflammatory diseases/conditions, comprising:
- an oral pharmaceutical composition with the antioxidant system and oxidative impurity/discoloration constraints of Claim 1.
The kit claim is a secondary coverage angle: it can capture marketing and distribution structures that bundle the same protected composition into a patient kit. Kit claims can matter if the commercial unit is sold as a bundled system rather than a standalone dosage form.
Where is the real boundary of infringement: composition vs. performance vs. impurity identity?
US 11,260,064 mixes:
- Compositional limitations (ascorbic acid + ascorbate salt; defined w/w ranges; optional flavor/sweetener; pH; preservatives),
- with stability/performance limitations (oxidative-degradation impurities below a threshold; non-discoloration after storage),
- and impurity identity specificity (Claim 7 calling out 21-dehydrobudesonide).
Impurity marker: why 21-dehydrobudesonide matters
Claim 7 specifies that oxidative degradation impurities comprise 21-dehydrobudesonide. For infringement:
- If oxidative degradation products measured by the competitor include 21-dehydrobudesonide above assay thresholds, it supports meeting the Claim 7 impurity characterization.
- The presence of 21-dehydrobudesonide does not by itself prove infringement; it must align with the rest of Claim 1 limitations (including antioxidant system identity and levels).
Performance data: how to think about the “<0.3% impurities formed by oxidative degradation” metric
This is typically measured via a stability protocol and analytically defined impurities. In litigation, infringement proof can hinge on:
- the competitor’s stability data and test conditions,
- whether the measured impurities are attributable to oxidative degradation under the same analytical definitions,
- and whether discoloration was observed under comparable conditions.
Claim 2–6 create time checkpoints (1, 2, 3 months) and two thresholds (<0.3% and <0.2% at two months) that can be used to show or contest infringement.
What is the likely formulation and product category scope (oral budesonide)?
While the claim language does not name a dosage form type, it does constrain the product to:
- oral administration
- with flavoring/sweetener present (or at least optionally included).
That pattern aligns most naturally with:
- oral suspensions,
- oral solutions,
- chewable or taste-masked formulations,
- and possibly flavored immediate-release forms where budesonide stability is engineered in a patient-friendly matrix.
If a competitor’s budesonide is in a format that does not include flavor/sweetener (for example, some standard tablets/capsules designed to avoid taste-masking), it may argue it does not meet Claim 1’s “flavoring agent, sweetener, or combination thereof” limitation. Conversely, a competitor can include taste-modifying excipients and still argue the amount and presence are not in the tested composition, depending on how the claim reads on inclusion.
How does US 11,260,064 fit into the broader US budesonide patent landscape?
Adjacent patent themes for budesonide oral products
In the US, budesonide IP around oral products typically clusters into:
- drug substance stability (oxidation pathways, impurity control),
- formulation compositions (buffers, antioxidants, chelators),
- delivery technology (controlled release, enteric or pH-dependent coatings),
- formulation process (mixing/handling conditions to control impurity formation),
- methods of treatment/use (GI inflammatory indications, dosing regimens),
- and device/kit packaging.
US 11,260,064 is strongly positioned in the stability-and-oxidation control segment because it is anchored on:
- antioxidant identity (ascorbic acid + ascorbate),
- dosage range (w/w),
- oxidative-degradation impurity limits,
- and discoloration outcomes.
Competitive risk profile
- Highest risk: competitor oral budesonide formulations using ascorbic acid/ascorbate at similar levels and that maintain oxidative impurities below the same thresholds during stability.
- Medium risk: products that use the same antioxidant chemistry but with antioxidant outside the claimed ranges or rely on different stability strategies that do not meet the specific impurity/discoloration performance targets.
- Lower risk: products that use alternative antioxidant systems (eg, vitamin E derivatives, NAC, BHA/BHT where permissible, or other redox/chelation approaches) or omit taste excipients entirely, depending on how Claim 1 is construed.
What about generic or biosimilar risk under Hatch-Waxman (Paragraph IV) for this kind of formulation patent?
For a formulation-specific composition patent like US 11,260,064, generic entry risk is typically addressed via:
- Hatch-Waxman Paragraph IV certifications challenging validity and/or non-infringement of formulation patents.
- Settlement agreements that can delay launch until patent expiry or until a court resolves infringement/validity.
Because Claim 1 is both chemically defined (ascorbic acid + ascorbate) and performance constrained (oxidative impurity and discoloration), typical generic design-arounds may involve:
- replacing the antioxidant system entirely,
- using the antioxidant but outside 0.05%–0.5% and/or 0.1%–0.5% ranges,
- adjusting pH outside 4–5.2,
- changing preservative package,
- or ensuring the stability profile does not match the claimed impurity/discoloration thresholds under relevant test conditions.
How strong is the patent estate for this technology based on claim structure?
Strength indicators embedded in the claims
- Narrow chemical identity of the antioxidant system (ascorbic acid + ascorbate salt).
- Quantitative range constraints (0.05%–0.5%; 0.1%–0.5% in dependent claim).
- Stability outcome constraints (impurity % thresholds and discoloration).
- Specific impurity marker (21-dehydrobudesonide) at the dependent level.
- Additional formulation constraints (pH range and preservative identity).
These features collectively increase the chance that:
- a direct-copy formulation would infringe,
- but a generic or competitor can design around by changing the antioxidant chemistry or moving pH/preservative systems.
Where strength can weaken
Performance-based claims can also be harder for the patentee to enforce because competing data sets, packaging configurations, and analytical definitions can create factual disputes over:
- whether oxidative-degradation impurities were measured as defined in the patent,
- whether discoloration is assessed under the same storage conditions,
- and whether “about” ranges include the competitor’s measured values.
Claim-by-claim coverage map for infringement and design-around
| Claim |
Key elements |
Infringement trigger |
Main design-around vector |
| 1 |
Oral budesonide; antioxidant 0.05%–0.5% w/w; antioxidant is ascorbic acid + ascorbate salt; flavoring/sweetener present; <0.3% oxidative-degradation impurities |
A competitor composition that matches antioxidant system + ranges and meets oxidative impurity limit with storage-relevant evidence |
Change antioxidant chemistry; move outside w/w range; omit flavor/sweetener; reformulate to shift oxidative impurity profile |
| 2 |
Claim 1 + <0.3% oxidative impurities after 1 month |
Stability shows <0.3% at 1 month |
Alter formulation to exceed threshold or ensure oxidative impurities are not “formed by oxidative degradation” as defined |
| 3 |
Claim 2 + no discoloration after 1 month |
Visual stability criteria met |
Allow discoloration under test window (or argue conditions/assay differ) |
| 4 |
Claim 1 + <0.3% after 2 months and no discoloration |
Stability meets both criteria at 2 months |
Decrease effectiveness to >0.3% or induce discoloration |
| 5 |
Claim 1 + <0.3% after 3 months |
Stability meets threshold at 3 months |
Reduce stability performance relative to claim window |
| 6 |
Claim 1 + <0.2% after 2 months |
Stability meets tighter threshold at 2 months |
Reformulate to keep impurities between 0.2% and 0.3% |
| 7 |
Claim 1 + oxidative impurities comprise 21-dehydrobudesonide |
Analytical impurity profile includes 21-dehydrobudesonide |
Use alternative oxidation pathway management or shift impurity distribution |
| 8 |
Claim 1 + pH 4 to 5.2 |
Measured pH falls in range |
Adjust buffer system to outside range |
| 9 |
Claim 1 + preservative present |
Preservative included |
Omit preservatives or use others (if written description supports) |
| 10 |
Claim 9 + preservative is sodium benzoate and/or potassium sorbate |
Specific preservative identity |
Replace with different preservative system |
| 11 |
Claim 1 + ascorbic acid + ascorbate present 0.1%–0.5% |
Antioxidant amount in range |
Use 0.05%–0.1% or >0.5% (if allowed) |
| 12 |
Kit for GI inflammatory disease containing Claim 1 composition |
Kit includes protected composition |
Sell same composition without kit structure (not always effective if composition still infringes) |
What to monitor in FDA/Orange Book style freedom-to-operate for this patent type
For a composition formulation patent like this one, the critical FTO inputs are:
- whether US 11,260,064 is listed for a relevant NDA (or ANDA-relevant product) in the Orange Book,
- whether there are related formulation patents in the same family listed for the same reference product,
- and whether any generic applicant has asserted non-infringement based on antioxidant chemistry, antioxidant concentration, pH, or oxidative impurity/stability profiles.
Because the claim is performance-driven, the most litigated disputes typically revolve around:
- stability study design and analytical definitions,
- matching antioxidant system identity,
- and whether the competitor’s formulation includes the claimed flavoring/sweetener limitation.
Key Takeaways
- US 11,260,064 is a narrow but enforceable formulation patent that protects an oral budesonide composition using a specific antioxidant system: ascorbic acid + ascorbate salt at 0.05%–0.5% w/w, combined with flavoring/sweetener and demonstrated oxidative stability (<0.3% oxidative-degradation impurities) and non-discoloration at defined storage timepoints.
- Dependent claims add tightening layers: <0.2% after two months, explicit inclusion of 21-dehydrobudesonide, a pH window (4–5.2), and optional preservative identity (sodium benzoate/potassium sorbate).
- Competitive design-around is most likely to succeed by changing antioxidant chemistry, moving outside concentration and pH ranges, or ensuring stability metrics do not meet the claimed oxidative impurity and discoloration thresholds under comparable test conditions.
- The kit claim extends protection to distribution formats, but infringement still depends on the kit containing the covered composition.
FAQs
1) Does Claim 1 require a specific budesonide dosage form (tablet vs suspension)?
The claim text mandates only oral administration; it does not specify a dosage form, but it does require inclusion of flavoring agent and/or sweetener and meeting the oxidative impurity/discoloration performance requirements.
2) If a competitor uses ascorbic acid without an ascorbate salt, is it covered?
Claim 1 requires an antioxidant comprising a combination of ascorbic acid and a pharmaceutically acceptable ascorbate salt, so omission of the salt would typically avoid this specific antioxidant system limitation.
3) What is the tightest impurity limit in the claims?
The tightest is <0.2% oxidative-degradation impurities after two months (Claim 6). The baseline limit across multiple claims is <0.3%.
4) Is pH a required element for infringement of Claim 1?
No. pH between 4 and 5.2 is in dependent Claim 8. Claim 1 does not include a pH limitation.
5) Can a kit infringe even if the exact same composition is sold separately?
Yes, if the kit contains the composition that meets the limitations of Claim 1; Claim 12 is directed to the kit structure but is anchored to the protected composition.
References
- US Patent 11,260,064, Claims 1-12 (as provided in user prompt).
