United States Patent 11,951,214: Scope, Claim Map, and US Landscape
What the patent claims, in one line: US 11,951,214 claims a solid-solution hard capsule formulation of Compound 1 (free base or pharmaceutically acceptable salt, neutral form permitted) at about 1 to 3 wt% combined with a specific two-component vehicle: a defined non-ionic surfactant (macrogol-40-glycerol hydroxystearate and/or macrogolglycerol ricinoleate and/or macrogol-15-hydroxystearate) plus a defined water-soluble solubilizer (PEGs of specific MW), with the vehicle present at about 97 to 99 wt% and the vehicle ratio surfactant:solubilizer = 45:55 to 55:45.
This is a formulation patent with tight component selection, weight fractions, and ratio controls, plus capsule-size and fill-weight narrowing dependent claim coverage.
What is the claim scope by element? (Independent Claim 1)
1) Dosage form / containment
- “solid solution capsule formulation”
- hard capsule is claimed in dependent form (claim 13), and capsule size #0 is claimed in dependent form (claim 12).
- Claim 1 itself does not restrict to a capsule brand or size, but the overall patent set does include those narrowing parameters in dependent claims (claims 12 and 13).
2) API identity: “Compound 1”
- Compound 1 can be:
- free base in neutral form, or
- pharmaceutically acceptable salt.
- Compound 1 loading:
- about 1 to 3% by weight of the total fill weight.
Scope implication: infringement hinges on using the same “Compound 1” (as defined in the patent specification, not provided in the prompt) in free base/salt forms that fall within the claim’s acceptable category, and loading within the claimed wt% window.
3) Vehicle composition: required dual category
The vehicle must have at least one non-ionic surfactant from a closed list and at least one water-soluble solubilizer from a closed list.
3a) Non-ionic surfactant (closed Markush list)
From the claim:
- macrogol-40-glycerol hydroxystearate
- macrogolglycerol ricinoleate
- macrogol-15-hydroxystearate
3b) Water-soluble solubilizer (closed Markush list)
From the claim:
- PEG-1500
- PEG-1540
- PEG-2000
- PEG-3000
- PEG-3350
- PEG-4000
- PEG-6000
- PEG-8000
4) Weight fractions
- Vehicle comprises about 97 to 99% by weight of the total fill weight.
- Compound 1 comprises about 1 to 3% by weight of total fill weight.
These fractions lock the formulation into an almost entirely excipient-based capsule fill, with API at a low single-digit wt%.
5) Surfactant:solubilizer ratio within the vehicle
The claim states the total weight of the vehicle comprises:
- 45:55 to 55:45 ratio of:
- at least one non-ionic surfactant to at least one water-soluble solubilizer.
Scope implication: even if the correct excipients are used, the formulation must be inside the ratio band.
How do dependent claims narrow coverage? (Claims 2-18)
A. Vehicle fraction narrowing
- Claim 2: vehicle comprises about 98 wt% (fixes the vehicle fraction to a specific point within claim 1’s band).
- Dependent claim 2 increases enforceability for formulations centered around 98% excipient content.
B. API loading narrowing
- Claim 3: about 2 wt% Compound 1 (a single value within 1 to 3 wt%).
- Claim 14: mirrors claim 3 with vehicle at about 98 wt%.
C. Ratio narrowing to 50:50
- Claim 4: vehicle ratio about 50:50
- Claim 15: vehicle comprises about 98 wt% and ratio about 50:50
- Claim 4 and 15 carve out a central ratio position that many developers target for robustness and predictability.
D. Surfactant species narrowing
- Claim 5: surfactant is macrogol-40-glycerol hydroxystearate or macrogolglycerol ricinoleate
- Claim 6: surfactant is macrogol-40-glycerol hydroxystearate
- Claim 16: surfactant is macrogol-40-glycerol hydroxystearate
E. Solubilizer species narrowing
- Claim 7: solubilizer is any PEG among:
- PEG-1540, PEG-2000, PEG-3000, PEG-3350, PEG-4000, PEG-6000
- Claim 8: solubilizer is PEG-4000
- Claim 17: solubilizer is PEG-4000
F. Explicit two-component pairing
- Claim 9: surfactant macrogol-40-glycerol hydroxystearate + solubilizer PEG-4000
- Claim 19 is not present; the pairing shows up again through claims 16-18.
G. Fill weight narrowing
- Claim 10: total fill weight about 130 mg to 900 mg
- Claim 11: total fill weight about 500 mg
- Claim 18: total fill weight about 500 mg
H. Capsule size and type narrowing
- Claim 12: capsule size #0
- Claim 13: capsule is a hard capsule
I. Consolidated narrowing chain (Claims 1 + 16-18)
Claims 16-18 create a tight “best-coverage” path:
- Claim 16: macrogol-40-glycerol hydroxystearate + (ratio 50:50 implied through claim 15; but claim 16 is dependent from claim 15 per numbering)
- Claim 17: PEG-4000
- Claim 18: fill weight about 500 mg
These dependent claims collectively pinpoint a specific formulation “sweet spot” that can be easier to design around only by changing at least one required element (API wt%, vehicle ratio, surfactant type, PEG MW, capsule size/type, or fill weight).
Key claim matrix: what must match to hit independent Claim 1?
| Claim element |
What the claim requires |
Practical infringement trigger |
| API identity |
“Compound 1” free base (neutral) or acceptable salt |
Use of the specific Compound 1 (as defined by the patent) |
| API wt% |
1 to 3 wt% |
Formulation must place API in that band |
| Vehicle wt% |
97 to 99 wt% |
Excipient load must satisfy complementary band |
| Non-ionic surfactant (closed list) |
macrogol-40-glycerol hydroxystearate / macrogolglycerol ricinoleate / macrogol-15-hydroxystearate |
Must use one or more of these specific surfactants |
| PEG solubilizer (closed list) |
PEG-1500, 1540, 2000, 3000, 3350, 4000, 6000, 8000 |
Must use PEG from the permitted MW list |
| Ratio in vehicle |
surfactant:PEG = 45:55 to 55:45 |
Ratio must fall within band |
What does the patent likely cover across product development? (Design space & likely variants)
Given the Markush lists and banded parameters, the claim set supports at least these formulation “families” under Claim 1:
- API at ~1–3 wt% with vehicle ~97–99 wt%
- Surfactant options: three non-ionic surfactants
- PEG options: eight PEG MW options
- Vehicle ratio band: 45:55 to 55:45 (continuous range)
The dependent claims then concentrate on a subset that likely corresponds to a preferred embodiment used in examples: macrogol-40-glycerol hydroxystearate + PEG-4000, at ~2 wt% API, ~98 wt% vehicle, 50:50 ratio, and ~500 mg fill, in hard capsule #0 (via claims 12 and 13 plus claims 11 and 18).
Where are the likely “escape hatches” for competitors? (Literal scope pressure points)
Because the vehicle categories are closed lists and the ratio is banded, the most straightforward literal design-around levers are:
- Use a surfactant not in the claim’s closed list (e.g., a different macrogol-based surfactant outside the specified set).
- Use a PEG not in the allowed PEG MW set (the claim’s list is specific; “PEG” alone is not enough).
- Move the vehicle ratio outside 45:55 to 55:45 (still using allowed components but selecting proportions that breach the ratio band).
- Move API wt% outside 1 to 3 wt%, or vehicle wt% outside 97 to 99 wt%.
- Change capsule operational parameters only if a dependent claim is being targeted (hard capsule type and #0 are dependent claims). Independent claim 1 can still be asserted against a formulation that uses a different capsule size/type unless the “solid solution capsule formulation” construction is interpreted to require the specific capsule constraints.
Practical note for enforcement strategy: claim-set coverage is structured so that even if a competitor avoids the specific preferred pairing (macrogol-40-glycerol hydroxystearate + PEG-4000), Claim 1 still remains broad as long as the competitor stays within the component lists and ratio and wt% bands.
US patent landscape for this formulation class (what the claim structure implies)
1) The patent is formulation-focused
The claim language is limited to:
- composition
- vehicle excipient selection
- quantitative proportions
- capsule fill and capsule size/type (dependent)
This is characteristic of formulation patents that often coexist with:
- earlier patents on the API molecule (compound claims, salts, polymorphs, etc.)
- later patents on delivery form and excipient systems
- process patents (manufacturing or solid solution formation)
2) Scope is narrow at the formulation-component level but broad within the chosen design space
- Closed Markush lists for both surfactant and PEG narrow enforceability.
- Continuous bands for ratio and wt% allow the patentee to capture multiple quantitative variants within the same excipient system.
3) Dependent claims cluster around one “preferred recipe”
Claims 8, 9, 11, 12, 13, 16, 17, 18 collectively narrow to a likely example set:
- PEG-4000
- macrogol-40-glycerol hydroxystearate
- ~500 mg fill
- hard capsule #0
- ~2 wt% API
- ~98 wt% vehicle
- ~50:50 ratio
This clustering supports a landscape expectation: competitors face the highest risk when they adopt the same practical formulation controls rather than merely the same API.
What “scope and claims” means for infringement analysis (claim mapping framework)
For any accused US product, a literal infringement analysis against Claim 1 proceeds as follows:
- Confirm the API is “Compound 1” (free base neutral or a claimed acceptable salt).
- Determine fill composition on a wt% basis:
- API wt% between ~1 and 3
- vehicle wt% between ~97 and 99
- Identify the vehicle excipients:
- at least one non-ionic surfactant must match one of the three specified macrogol surfactants
- at least one PEG solubilizer must match one of the specified PEG MW values
- Calculate ratio in the vehicle:
- surfactant mass fraction vs PEG mass fraction must fall in 45:55 to 55:45
- If targeting dependent claims, also check:
- exact API wt% at ~2
- exact vehicle wt% at ~98
- exact 50:50 ratio
- specific surfactant and PEG pairing
- fill weight at ~500 mg
- capsule size #0 and hard capsule type
This claim architecture makes “partial overlap” insufficient: missing one required component type, PEG MW, or ratio band breaks Claim 1.
Key Takeaways
- US 11,951,214 is a solid-solution hard capsule formulation patent built on Compound 1 with 1 to 3 wt% API and a 97 to 99 wt% vehicle.
- The vehicle is constrained to a closed list of three non-ionic surfactants and a closed list of PEG solubilizers (specific MWs).
- The formulation also requires a tight vehicle internal ratio of 45:55 to 55:45 (surfactant:PEG).
- Dependent claims concentrate on a likely preferred embodiment: macrogol-40-glycerol hydroxystearate + PEG-4000, ~2 wt% API, ~98 wt% vehicle, ~50:50 ratio, ~500 mg fill, hard capsule #0.
- For competitive design-arounds, the highest-probability literal escape points are: changing surfactant to one outside the list, using a PEG MW outside the list, or selecting a formulation that breaches the 45:55 to 55:45 ratio band.
FAQs
1) Does Claim 1 require PEG-4000?
No. Claim 1 requires a PEG solubilizer from the listed set; PEG-4000 is only required in dependent claim 8/17/9 pathways.
2) Can a formulation using macrogol-15-hydroxystearate still infringe Claim 1?
Yes, if it uses that surfactant (or another listed surfactant), uses PEG from the listed MW set, and meets the wt% and ratio requirements.
3) Is the #0 capsule size required for Claim 1?
No. #0 is in dependent claim 12; Claim 1 does not specify capsule size.
4) What is the key quantitative constraint besides API loading?
The vehicle internal ratio of surfactant to PEG must be 45:55 to 55:45.
5) If a competitor changes the API to a different salt form, is Claim 1 avoided?
Not if the new salt is still within “pharmaceutically acceptable salt” for Compound 1 as claimed; Claim 1 explicitly permits pharmaceutically acceptable salts and neutral free base.
References
[1] US Patent 11,951,214 (claims provided in prompt).
