United States Patent 12,318,367: Scope, Claim Construction, and U.S. Patent Landscape for a Vitamin E TPGS-Dispersed Hydrogen Sulphate Salt Composition
US 12,318,367 is tightly claim-drafted around one active entity: a hydrogen sulphate salt of 6-(4-bromo-2-chloro-phenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide (“H2SO4 salt of benzimidazole carboxamide”), in fixed weight-ratio ranges with d-alpha-tocopheryl polyethylene glycol 1000 succinate (Vitamin E TPGS, “TPGS”), where the salt is dispersed in TPGS and the composition is semi-solid/solid at ambient temperature. The independent claim scope is primarily a composition-of-matter with functional performance limits that appear as process-adjacent product constraints (particle size; dissolution in USP Apparatus II).
What does US Patent 12,318,367 claim protect? (composition scope and enforceable product boundaries)
Independent claim 1: the core protected composition
Claim 1 protects a pharmaceutical composition defined by:
- Actives
- Hydrogen sulphate salt of 6-(4-bromo-2-chloro-phenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide.
- Carrier / excipient matrix
- d-alpha-tocopheryl polyethylene glycol 1000 succinate (Vitamin E TPGS).
- Weight ratio envelope
- (i) 5 to 10 parts salt
- (ii) 95 to 90 parts TPGS
- (i) + (ii) = 100 parts by weight
- Dispersion requirement
- the hydrogen sulphate salt is dispersed within Vitamin E TPGS.
- Physical state limitation
- composition is semi-solid or solid at ambient temperature.
Enforceable boundary: a solid or semi-solid TPGS dispersion containing the specific H2SO4 salt within the 5–10 wt% range, with dispersion morphology and dispersion state, is within claim 1 even without other excipients being recited (claim language is “consisting of,” so additional components are excluded unless they are part of the claimed two constituents by definition).
Independent claim 11 and claim 20: additional composition ratio bands
Claim 11 mirrors claim 1 with an approximate 10:90 ratio (“approximately 10 parts salt and approximately 90 parts TPGS”), while claim 20 covers an approximate 20:80 ratio.
Practical effect: the patent protects at least three ratio points/bands (near 5–10%, near ~10%, near ~20%), each further constrained by dispersion, ambient physical state, and (in dependent claims) particle size/dissolution.
How broad are the claims? (numerical ranges, “consisting of,” and key limitations)
“Consisting of” narrows infringement design-arounds
The claims use “consisting of” for the composition. That typically excludes:
- other pharmaceutically acceptable excipients (binders, surfactants, fillers, diluents),
- coatings,
- additional solubilizers,
unless the claim construction treats such materials as impurities or unavoidable components of the two specified constituents.
Net result: manufacturing routes that add common capsule fill excipients are at high risk for falling outside the literal claim, but a fuller infringement analysis would require the full spec and claim construction record, which is not provided.
Dose-quantity dependent claims add product specificity but not carrier freedom
Dependent claims 2–6, 12–15, and 21–24 recite mg amounts of salt in the composition (with ±2 mg or “contains X mg” versions). These are narrow to specific loadings, typically matching capsule fill amounts or unit-dose formulations.
Particle size dependent claims are enforceable morphological constraints
Claims 7–8 and 16–17 and 25–26 require:
- particle size about 1 to 20 microns, and/or
- particle size distribution: about 90% particles with diameter < 15 microns.
This gives the patent holder an additional hook against generic/manufacturing variants that keep the same wt% but fail on particle size/distribution.
Dissolution-dependent claims add a performance gate
Claims 10, 19, and 28 require:
- >95% dissolved after about 50 minutes using USP Apparatus II.
This is a strong constraint for oral capsule products: even if particle size and ratio are matched, formulations with different microstructure or wetting behavior can be designed to miss the dissolution target.
What formulation parameters are explicitly claimed in US 12,318,367? (TPGS dispersion, ambient solid/semi-solid, capsule)
Matrix and dispersion
The claims require “the hydrogen sulphate salt … is dispersed within” TPGS. That implies:
- the salt is not merely dissolved,
- not simply blended as free crystals, unless dispersion is interpreted broadly.
Because the claims also define particle size, they likely presume micronized salt distributed through a TPGS-based semi-solid/solid matrix.
Ambient temperature state
“Semi-solid or solid at ambient temperature” is a stability/physical-state product feature. It can be used to argue non-infringement for:
- wax-like low-melting mixtures treated as liquid at room temperature,
- hot-fill liquid systems,
- formulations that are semi-solid only transiently.
Oral capsule embodiment
Claims 9 and 18 and 27 cover “an oral capsule filled with” the composition. Claim 10/19/28 add dissolution performance in those capsule embodiments.
Enforceable scope: if a capsule fill matches the “consisting of” composition and the dissolution/particle constraints, both composition and capsule claims are implicated.
How many claims are there and what is the claim dependency tree? (quick map of scope coverage)
Claim set overview
- Composition independent claims: 1, 11, 20
- Capsule independent claims: 9, 18, 27 (each dependent on 1/11/20 respectively)
- Dependent claims focusing on: mg loading (2–6, 12–15, 21–24), particle size (7–8, 16–17, 25–26), dissolution (10, 19, 28)
Table: key scope elements by claim group
| Claim group |
Salt:TPGS ratio (by weight) |
“Consisting of” |
Particle size |
Dissolution (USP App II) |
Dosage mg dependent? |
Dosage form |
| Claim 1 / 9 / 10 |
5–10 : 95–90 |
Yes |
Yes (claims 7–8) |
Yes (>95% in ~50 min, claim 10) |
Yes (claims 2–6) |
Capsule (claim 9) |
| Claim 11 / 18 / 19 |
~10 : ~90 |
Yes |
Yes (claims 16–17) |
Yes (>95% in ~50 min, claim 19) |
Yes (claims 12–15) |
Capsule (claim 18) |
| Claim 20 / 27 / 28 |
~20 : ~80 |
Yes |
Yes (claims 25–26) |
Yes (>95% in ~50 min, claim 28) |
Yes (claims 21–24) |
Capsule (claim 27) |
What patent estate risks exist for competitors? (design-around vs literal infringement)
High-risk design targets
A competitor is at higher infringement risk if it makes any of the following categories of products:
- the same H2SO4 salt identity (same chemical structure and salt form),
- formulated as a TPGS-based dispersed semi-solid/solid,
- with salt wt% in the 5–10% band (or near the approximate 10% and 20% embodiments),
- with micron-scale particle size and “90% < 15 μm” style distribution,
- achieving >95% dissolution in ~50 minutes using USP Apparatus II,
- packaged as an oral capsule filled with the formulation.
Likely non-infringing routes (based on claim language)
Because the claims require “consisting of” and specific salt and matrix:
- switching from TPGS to another solubilizer/lipid system likely avoids literal composition coverage,
- using a different salt form (e.g., HCl, fumarate) likely avoids the specific “hydrogen sulphate salt” definition,
- adding additional excipients could fall outside “consisting of” (unless treated as part of one constituent),
- using a formulation that is liquid at ambient temperature avoids the physical-state limitation,
- avoiding the particle size band could avoid the dependent-claim particle limitations but may still fall under independent claims 1/11/20 depending on how “dispersed” is construed.
When does US 12,318,367 lose exclusivity? (expiration and term)
No filing date, priority date, maintenance status, terminal disclaimer information, or PTA adjustment is provided in the prompt. Without those inputs, an accurate U.S. exclusivity/expiration timetable cannot be produced.
What Orange Book status does US 12,318,367 have? (FDA-listed patents)
No Orange Book listing data (application number, NDA/RLD, listed patent numbers tied to this patent, or exclusivity codes) is provided. Without the FDA listing linkage, status cannot be stated accurately.
What generic entry risks exist for a TPGS-dispersed hydrogen sulphate salt product? (ANDA/505(j) / 505(b)(2) scenarios)
No NDA/RLD identity, FDA reference product, or ANDA paragraph IV history is provided. Without the product context, generic entry risk (including whether this patent is listed and whether carveouts exist) cannot be quantified.
Is this patent more relevant to ANDA generics or biosimilars?
This is a small-molecule salt-and-excipient formulation claim, not a biologic. Biosimilar pathways are not implicated by the claim content.
What is the most likely claim-construction focus in litigation? (composition meaning, dispersion, and dispersion proof)
“Dispersed within”
Key disputes typically center on whether:
- the salt must be present as discrete micron particles dispersed throughout a TPGS continuous phase,
- or whether any mixture meeting particle size targets qualifies.
Particle size measurement methodology
Claims tie to “about” and “diameter” thresholds. In practice, disputes often hinge on:
- whether measurement is laser diffraction vs microscopy vs sieve,
- how “about” is treated around boundary values.
USP Apparatus II dissolution test setup
The dissolution requirement is fixed to “USP Apparatus II” with “after about 50 minutes.” Disputes often turn on:
- whether media and conditions match the patent’s test protocol (not provided),
- how results are normalized for unit-dose loading.
What other U.S. patents likely cluster around this formulation? (typical landscape pattern)
A formulation patent of this structure usually sits within clusters that include:
- the underlying active pharmaceutical ingredient (API) polymorph/salt patents,
- process patents for producing the micronized salt or the salt form,
- additional formulation patents with other carriers or ratio windows,
- method-of-use patents tied to therapeutic indications,
- capsule shell/coating patents.
However, no bibliographic data, assignee, related family members, or prosecution history is provided. A specific “which patents cover the same salt, same ratios, same TPGS carrier, or the same dissolution window” list cannot be produced accurately from the prompt.
Key Takeaways
- US 12,318,367 is a narrow composition-of-matter formulation patent centered on a specific hydrogen sulphate salt dispersed in Vitamin E TPGS, where the composition is solid/semi-solid at ambient temperature and the salt:TPGS ratio sits in 5–10 wt% (claim 1) with additional approximate 10 wt% (claim 11) and approximate 20 wt% (claim 20) embodiments.
- The independent claim scope is tightly limited by “consisting of,” excluding additional excipients unless they fall within the construed boundaries of the two specified constituents.
- Dependent claims add enforceable product constraints: micron-scale particle size/distribution and >95% dissolution in ~50 minutes using USP Apparatus II, plus capsule embodiments.
- Infringement risk is highest for competitors that match (i) the exact salt form, (ii) the TPGS dispersion matrix, (iii) the ratio windows, and (iv) particle size/dissolution performance, and that package the product as an oral capsule filled with the claimed composition.
- Expiration, Orange Book status, ANDA/paragraph IV exposure, and detailed U.S. patent landscape mapping cannot be stated from the provided prompt alone because no bibliographic identifiers or FDA listing links are included.
FAQs
- Does changing the hydrogen sulphate salt to a different salt form avoid US 12,318,367?
- If a competitor uses Vitamin E TPGS but changes the salt:TPGS ratio slightly outside 5–10 wt%, is it outside claim 1?
- How do the particle size “about 1 to about 20 microns” and “about 90% < 15 microns” limits affect formulation design?
- What USP Apparatus II dissolution results could be used to show non-infringement for the capsule claims?
- Can a capsule still infringe if it contains additional excipients beyond salt and TPGS?
References (APA)
No external sources were provided or cited.
