US Patent 8,895,064 (Drug) Budesonide Gastro-Resistant Tablet: Claims Scope, Design-Around Risk, and Landscape Implications
What does US 8,895,064 claim, in enforceable terms?
US 8,895,064 claims an oral, human-administered budesonide tablet with a defined core composition and a defined gastro-resistant coating film that produces measurable budesonide lag time (Tlag) and exposure parameters (Cmax, Tmax-Tlag). The core is anchored on a 9 mg budesonide dose and a specific excipient matrix described as macroscopically homogeneous and containing stearic acid (and/or its salt), lecithin, and hydroxypropyl cellulose (HPC), with budesonide dispersed in that matrix.
The coating is anchored on a gastro-resistant film that “consists essentially of” a mixture of two methacrylic acid copolymers, with 8 mg of a first and 8 mg of a second copolymer (total coating polymer mass specified in claim language). The claims then require in vivo performance, expressed through Tlag (and dependent claims add Cmax or Tmax-Tlag).
Independent claim set (core + coat + functional lag-time limits)
The independent-like claim statements in the set are claims 1, 3, 5, 7, 9, 11 (since claims 2, 4, 6, 8, 10, 12 are “further provides Cmax…”).
Below is the enforceable claim structure, reduced to required elements.
| Claim No. |
Tablet form |
Core: budesonide |
Core: excipient matrix (must be macroscopically homogeneous) |
Coating: gastro-resistant film (must “consist essentially of”) |
Performance requirement(s) |
| 1 |
Tablet |
9 mg |
Stearic acid and/or salt + lecithin + hydroxypropyl cellulose; budesonide dispersed in matrix |
Mixture of two methacrylic acid copolymers: 8 mg first + 8 mg second |
Tlag ~ 6.79 ± 3.24 h |
| 3 |
Tablet |
9 mg |
Same as claim 1 |
Same as claim 1 |
(Tmax − Tlag) ~ 7.21 ± 5.49 h |
| 5 |
Tablet (consisting essentially of) |
9 mg |
Same as claim 1 |
Same as claim 1 |
Tlag ~ 6.79 ± 3.24 h |
| 7 |
Tablet (consisting essentially of) |
9 mg |
Same as claim 1 |
Same as claim 1 |
(Tmax − Tlag) ~ 7.21 ± 5.49 h |
| 9 |
Tablet |
9 mg |
Same as claim 1 |
Same as claim 1 |
Tlag from 1 h to 12 h (range) |
| 11 |
Tablet (consisting essentially of) |
9 mg |
Same as claim 1 |
Same as claim 1 |
Tlag from 1 h to 12 h (range) |
Dependent claim performance reinforcement (Cmax)
Claims 2, 4, 6, 8, 10, 12 add the exposure requirement:
- Cmax ~ 1768.7 ± 1499.8 pg/mL after administration to a human.
These are not alternative formulations; they narrow the same composition/performance scaffold to match an exposure window.
How broad is the formulation coverage?
Coverage has two distinct breadth layers: (1) composition specificity and (2) functional/performance windows.
1) Composition specificity: high constraint
The claim set is tight on four parameters:
- Dose: budesonide fixed at 9 mg.
- Core matrix: must include stearic acid (or salt) + lecithin + hydroxypropyl cellulose with budesonide dispersed in that macroscopically homogeneous composition.
- Coating polymer system: must be gastro-resistant film that “consists essentially of” a mixture of two methacrylic acid copolymers.
- Coating polymer quantities: 8 mg + 8 mg (first and second copolymer masses).
From a patent scope standpoint, this is not “any enteric/budesonide oral dosage form.” It is a narrowly defined budesonide tablet design where both quantities and polymer identity class (methacrylic acid copolymers) are specified, and the coating is limited by “consists essentially of,” which constrains additional ingredients in the coating film.
2) Performance windows: moderate breadth, but still claim-anchored
The performance limits create additional enforceability and limit trivial design-arounds.
Two tiers exist:
- Narrow-lag claims: Tlag ~6.79 ± 3.24 hours (claims 1 and 5).
- Range-lag claims: Tlag from about 1 hour to about 12 hours (claims 9 and 11).
That means the patent is written to capture both:
- formulations that land around a mean Tlag of about 6.79 h, and
- formulations that achieve any “acceptable lag” within 1 to 12 h.
Two additional timing markers are claimed:
- Tmax − Tlag ~ 7.21 ± 5.49 hours (claims 3 and 7).
And exposure is optionally layered via dependent claims:
- Cmax ~1768.7 ±1499.8 pg/mL (claims 2, 4, 6, 8, 10, 12).
Which claim elements are likely to be the real “deal makers” for infringement?
In enforcement, claim terms that are both (a) structurally limiting and (b) measurable are typically the main battlegrounds. In this claim set, those are:
1) The budesonide dose (9 mg)
If a competing tablet uses anything other than 9 mg of budesonide, the claim language is less likely to read directly onto it. Even “close” dosing can be outside literal scope.
2) The core excipient triad and homogeneity
The claim requires a macroscopically homogeneous composition containing:
- stearic acid and/or salt
- lecithin
- hydroxypropyl cellulose
and budesonide dispersed in that matrix. A competitor that swaps out HPC or lecithin (or changes dispersibility/homogeneity approach) reduces literal fit. Changing only process (granulation method) may not avoid if the resulting tablet contains the same composition and is macroscopically homogeneous in the claim sense.
3) The gastro-resistant coating defined by “consists essentially of” two methacrylic acid copolymers
This is a high-value limiter:
- “gastro-resistant film” must be “consisting essentially of” a mixture of two methacrylic acid copolymers.
- and the mixture is defined by 8 mg of each copolymer.
Literal scope is most sensitive to the polymer system:
- If a competitor uses different enteric polymers (e.g., cellulose derivatives, pH-dependent systems not using methacrylic acid copolymers, or includes additional coating polymers such that they are more than “essentially” allowed), infringement risk shifts.
4) Tlag window (and optionally Cmax)
The claims are performance-tethered. Even if a formulation matches composition, infringement could still be contested on whether it produces the required:
- Tlag ~ 6.79 ± 3.24 h, or
- Tlag about 1 h to about 12 h, and/or
- Tmax − Tlag ~ 7.21 ± 5.49 h, and
- Cmax ~ 1768.7 ± 1499.8 pg/mL (dependent).
Because these are human PK outcomes, testing design and study comparability can matter in practice, even if composition is similar.
What claim redundancies exist, and why they matter for landscape and freedom-to-operate?
The claim set has a repeating scaffolding with multiple redundant variants that appear designed to preserve coverage under different measurement emphases.
- Claims 1 and 5 both require Tlag ~6.79 ± 3.24 h, while differing only in the “tablet comprises” versus “tablet consisting essentially of” drafting posture.
- Claims 3 and 7 both require Tmax − Tlag ~7.21 ± 5.49 h with the same core/coating architecture.
- Claims 9 and 11 both cover Tlag from about 1 h to about 12 h with the same core/coating architecture.
- Dependent Cmax claims are layered onto multiple independents, capturing different timing-anchored forms.
Practical effect: if a competitor tries to shift formulation performance to move outside one timing window, the range-based claims may still capture the device unless the shift escapes the 1 to 12 h Tlag range.
How should competitors design around without triggering “consisting essentially of” traps?
A design-around needs to break at least one required element that cannot be traded off while maintaining bioavailability goals.
High-leverage design moves (based strictly on claim text)
-
Change budesonide dose away from 9 mg
This targets the dose-locked element.
-
Change at least one core excipient functionally or compositionally
Replace stearic acid/salt, lecithin, or hydroxypropyl cellulose, or remove the “macroscopically homogeneous” dispersed matrix concept.
-
Change the enteric polymer class or the two-copolymer mixture system
The coating must be “consisting essentially of” a mixture of two methacrylic acid copolymers at specified masses. Using only one copolymer, changing the polymer class, or significantly changing the mass ratio/amount can help.
-
Shift Tlag out of 1 to 12 hours (or out of 6.79 ± 3.24 hours, if that narrower claim set is asserted)
Since claims explicitly require Tlag windows, moving outside them is a direct path to non-infringement.
-
Adjust performance such that dependent Cmax claims are not met
This is only partial protection because independent timing claims still remain. It is most useful as a secondary defense.
“Consisting essentially of” risk
Because the coating film is not simply “includes” but “consists essentially of”, the coating cannot freely add other film-formers or plasticizers that become material to the film’s composition. Competitors must be careful that any additional components do not defeat the “essentially of” limitation as interpreted by claim construction.
What is the likely competitive patent landscape structure for this technology?
The claim set suggests a niche but defensible IP cluster at the intersection of:
- budesonide controlled delivery,
- enteric/gastro-resistant film polymer system using methacrylic acid copolymers, and
- excipient matrix using stearic acid (salt) + lecithin + hydroxypropyl cellulose,
- with human PK timing targets (Tlag, Tmax − Tlag) and exposure (Cmax).
Landscape implications for other players
Given the specificity, the most relevant competitive filings tend to be either:
- formulation follow-ons that keep the same enteric polymer system but change excipient amounts or coating build, or
- PK-tuned variants that aim to shift Tlag/Tmax-Tlag while trying to keep total release characteristics.
If other patents claim similar budesonide dose and methacrylic acid copolymer mixtures, they will likely overlap around this same parameter set. If they claim different polymer systems, they may avoid literal overlap but can still face infringement theories under broader or equivalents-type analyses, depending on claim construction and prior art.
Where does the scope sit between “composition patent” and “method/performance patent”?
This patent is written as a composition/product claim (oral tablet formulation), but it is heavily anchored to performance in humans:
- Tlag in hours,
- Tmax − Tlag in hours,
- Cmax in pg/mL.
That makes it closer to a “composition defined by in vivo performance” style claim. As a result, in litigation or design validation, the core argument tends to combine:
- whether the tablet’s ingredients and quantities match the textual requirements, and
- whether the performance measurements for that particular tablet match the numeric windows.
Quantitative claim map: what exactly must match for infringement
Below is a “must-match” checklist distilled from the claim set provided.
| Category |
Must-match items in US 8,895,064 (from claims provided) |
| Product type |
Oral pharmaceutical composition in the form of a tablet administered to a human |
| Drug dose |
9 mg budesonide in the tablet core |
| Core matrix composition |
Macroscopically homogeneous composition containing stearic acid and/or salt + lecithin + hydroxypropyl cellulose (HPC); budesonide dispersed in the matrix |
| Coating type |
Coating on core is gastro-resistant film |
| Coating composition |
Film “consists essentially of” mixture of two methacrylic acid copolymers with 8 mg first + 8 mg second |
| Lag-time performance |
Either: Tlag ~ 6.79 ± 3.24 h or Tlag 1 to 12 h (depending on asserted claim) |
| Timing metric |
Either: Tmax − Tlag ~ 7.21 ± 5.49 h (claims 3 and 7) |
| Exposure metric (dependent) |
Cmax ~1768.7 ±1499.8 pg/mL (dependent claims) |
Key Takeaways
- US 8,895,064 protects a very specific budesonide tablet architecture: 9 mg budesonide in a macroscopically homogeneous core made from stearic acid (or salt) + lecithin + hydroxypropyl cellulose with budesonide dispersed; plus a gastro-resistant coating “consisting essentially of” a two-methacrylic-acid-copolymer film at 8 mg + 8 mg, with human Tlag windows claimed at ~6.79 ± 3.24 h and 1 to 12 h.
- The patent’s scope is not only ingredient-based; it is also performance-tethered through Tlag, Tmax − Tlag, and dependent Cmax windows, increasing enforceability against formulations that match composition but land in the same PK space.
- Design-arounds that rely on minor excipient tweaks but keep the same 9 mg dose, the same core excipient triad, the same two-copolymer methacrylic acid enteric system at 8 mg each, and Tlag within 1 to 12 h remain at high infringement risk.
FAQs
-
Does US 8,895,064 cover non-tablet dosage forms (capsules, suspensions)?
No. The claims are limited to an oral pharmaceutical composition “in the form of a tablet.”
-
Is the budesonide dose fixed or adjustable within claim scope?
The claims explicitly require 9 mg budesonide.
-
What must the gastro-resistant coating film contain?
It must be a gastro-resistant film that consists essentially of a mixture of two methacrylic acid copolymers with 8 mg of each, as stated in the claims.
-
How is the lag-time limitation used to narrow infringement?
The claims require specific Tlag outcomes: either ~6.79 ± 3.24 hours or about 1 to about 12 hours, depending on which claim is asserted.
-
Do the Cmax limitations apply to all claims?
No. Cmax is added only in dependent claims (claims that include “further provides a Cmax…”), while the independent structure is primarily constrained by composition and Tlag (and in some claims Tmax − Tlag).
References
[1] United States Patent No. 8,895,064. (Claims as provided in the prompt).
