US Patent 11,065,198: What Is Claimed and Where It Sits in the US Landscape
What does US 11,065,198 claim at the composition level?
US Drug Patent 11,065,198 claims a solid oral composition defined by a two-part formulation structure: a granular fraction plus an extragranular fraction. The claims are written around weight-percent ranges for excipients in each fraction and include a specific exemplar formulation.
Independent claim 1: two-fraction composition with excipient ranges
Claim 1 requires:
-
Granular fraction
- 2.75 mg rilpivirine HCl
- 1% to 8% diluent
- 0.01% to 2.5% wetting agent
- 0% to 10% binder
- 0.1% to 5% disintegrant
-
Extragranular fraction
- 35% to 87% microcrystalline cellulose (MCC)
- 1% to 5% disintegrant
- 0.01% to 2.5% wetting agent
- 0% to 5% lubricant
The claim language ties all percentages to the total composition weight and splits excipients by where they reside (in granules vs outside granules).
Dependent claim range narrowing
The following dependent claims set additional structural constraints:
- Claim 2: granular fraction is up to 50% by weight of total composition.
- Claim 3: granular fraction is 5% to 20% by weight.
- Claim 4: extragranular fraction is up to 95% by weight.
- Claim 5: extragranular fraction is 50% to 95% by weight.
These range constraints create a formulation space where:
- granules can be a minority portion (as low as 5%) or up to 50%, and
- the majority portion is extragranular excipients (as low as 50%, and up to 95%).
Dependent claim 6: a specific “worked” formulation
Claim 6 lists an explicit composition (amounts) for both fractions:
-
Granular fraction
- 2.75 mg rilpivirine HCl
- lactose monohydrate
- croscarmellose sodium
- polyvinylpyrrolidone
- Polysorbate 20
- Total: 8.73 mg
-
Extragranular fraction
- mannitol
- microcrystalline cellulose
- sodium lauryl sulfate
- croscarmellose sodium
- sodium stearyl fumarate
- Total: 100 mg
Scope implication: claim 6 pins specific excipient identities that likely map to:
- diluent (e.g., lactose monohydrate, mannitol),
- wetting agent/surfactant (e.g., Polysorbate 20, sodium lauryl sulfate),
- binder (e.g., PVP),
- disintegrant (e.g., croscarmellose sodium in both fractions),
- lubricant (e.g., sodium stearyl fumarate),
while still operating under the broader percentage framework of claim 1.
Where is the “real” enforceable boundary?
The enforceable boundary is not a single excipient list. It is the combination of:
- Two-fraction architecture (granular vs extragranular),
- Rilpivirine HCl at 2.75 mg in the granular fraction,
- Fraction-specific excipient ranges (diluent, wetting agent, binder, disintegrant in granules; MCC, disintegrant, wetting agent, lubricant in extragranules),
- Fraction weight ratio constraints (claims 2-5).
High-leverage claim elements
- Rilpivirine HCl fixed dose: “2.75 mg” in the granular fraction is a hard anchor for infringement analysis. If a product places rilpivirine in the extragranular fraction, or uses a different per-tablet dose, literal coverage is harder.
- Granular vs extragranular placement: Many alternate formulations can match overall excipient percentages but fail if they do not create the claimed split.
- MCC range in extragranular fraction: “35% to 87%” MCC is a major numerical limiter. It affects whether a product uses MCC primarily inside granules or shifts it to the extragranular blend.
- Wetting agent ranges in both fractions: “0.01% to 2.5%” in each fraction, split across placement, creates another gating requirement.
What formulation “design-arounds” are suggested by the claim language?
Because the claims are range-based and placement-based, design-arounds typically target one or more of the gating constraints:
- Move rilpivirine HCl out of the granular fraction
- Change dose away from 2.75 mg per unit in the granular fraction
- Use MCC outside the 35% to 87% extragranular window
- Set excipient levels outside fraction-specific ranges
- Granular disintegrant: 0.1% to 5%
- Extragranular disintegrant: 1% to 5%
- Lubricant: 0% to 5%
- Alter fraction proportions
- Keep granular fraction below 5% or above 20% (to avoid claims 3), while still respecting the broader claim 2 ceiling (up to 50%)
- Keep extragranular outside the 50% to 95% window (to avoid claims 5)
These are structural levers created by claims 1-5 rather than speculative chemistry changes.
What does the specific example in claim 6 add?
Claim 6 does two things to the landscape:
-
It confirms claim scope includes a formulation family using:
- lactose monohydrate and mannitol as diluents,
- croscarmellose sodium as disintegrant in both fractions,
- PVP as binder (in granules),
- Polysorbate 20 and sodium lauryl sulfate as wetting/surfactant agents (one in granules and one in extragranules),
- sodium stearyl fumarate as lubricant.
-
It can be used for claim construction of ambiguous categories:
- “diluent” is not limited to one identity,
- “wetting agent” can include surfactants like Polysorbate 20 and sodium lauryl sulfate,
- “binder” can include PVP,
- “lubricant” can include sodium stearyl fumarate,
- “disintegrant” can include croscarmellose sodium.
In infringement disputes, an accused product that matches the example in both excipient choice and approximate fraction placement may be argued as being close to the intended species within a genus claim.
How does this compare to typical solid oral rilpivirine formulations?
A typical tablet formulation for rilpivirine (and especially for poorly water-soluble drugs) often relies on:
- a strong disintegrant,
- a binder/povidone polymer in granules,
- surfactants to improve wetting,
- and lubricants for compression.
US 11,065,198 narrows that general playbook into a specific granule/extragranule excipient arithmetic:
- MCC is heavily weighted to the extragranular phase,
- disintegrant appears in both phases but with different minimums,
- lubricants only appear as extragranular up to 5%,
- wetting agent sits in both phases within tight fractional windows.
That is the claim’s practical differentiation: it is not only “rilpivirine HCl with certain excipients,” it is the fraction-specific formulation design.
What is the patent landscape risk profile in the US?
A high-level landscape view must be built from (a) the claims provided and (b) the fact pattern of how granular/extragranular architecture is commonly treated in later generics.
Risk for ANDA-style entrants
For generic entrants, the key question under this claim set is whether the candidate product:
- uses rilpivirine HCl at 2.75 mg and
- replicates the fraction-specific excipient distribution with the stated ranges.
If the generic uses the same excipients but changes the fraction split (for example, shifts MCC or disintegrant largely into granules), it may fall outside coverage even if overall tablet composition appears similar.
Risk for “second-use” or reformulation competitors
Competitors seeking differentiation by formulation usually adjust at least one of:
- placement (granule vs outside),
- fraction proportions,
- excipient identity for one role (e.g., alternate disintegrant class),
- excipient levels relative to the claimed windows.
Because claim 1 is broad in some ranges (e.g., diluent 1% to 8%, binder 0% to 10%), the highest protection tends to come from the harder constraints (MCC in extragranular, disintegrant minima, and rilpivirine’s granular anchor).
Litigation posture likely to focus on two issues
Even without accessing the prosecution or file history, the provided claims set up the two typical infringement proof lanes:
- Formulation fraction analysis: establish whether the accused tablet meets the granular/extragranular percentages by weight and whether rilpivirine is present in the granular fraction as claimed.
- Numerical range compliance: show the disintegrant and MCC percentages and wetting/lubricant boundaries for the extragranular portion.
How to map the claims to product specifications for freedom-to-operate
For internal claim-charting, the following mapping provides a direct checklist anchored in the claim text:
Claim 1 mapping checklist
- [ ] Is rilpivirine present as rilpivirine HCl at 2.75 mg in the granular fraction?
- [ ] Does the granular fraction include:
- [ ] diluent at 1% to 8%
- [ ] wetting agent at 0.01% to 2.5%
- [ ] binder at 0% to 10%
- [ ] disintegrant at 0.1% to 5%
- [ ] Does the extragranular fraction include:
- [ ] MCC at 35% to 87%
- [ ] disintegrant at 1% to 5%
- [ ] wetting agent at 0.01% to 2.5%
- [ ] lubricant at 0% to 5%
- [ ] Are these percentages calculated against total tablet weight?
Claim 3 and Claim 5 constraints to test
- [ ] If targeting claim 3 avoidance: ensure granular fraction is not 5% to 20%
- [ ] If targeting claim 5 avoidance: ensure extragranular fraction is not 50% to 95%
Claim 6 “species match” test
- [ ] Does the product use lactose monohydrate and croscarmellose sodium and PVP and Polysorbate 20 in granules totaling 8.73 mg?
- [ ] Does the extragranular portion use mannitol, MCC, sodium lauryl sulfate, croscarmellose sodium, and sodium stearyl fumarate totaling 100 mg?
Even if exact totals differ due to unit weight differences, the presence of the same excipient identities in the same roles and likely fraction placement can matter in claim construction.
Key Takeaways
- US 11,065,198 protects a two-fraction rilpivirine HCl tablet architecture: rilpivirine HCl at 2.75 mg in the granular fraction, plus excipient-specific ranges split across granules and extragranules.
- The enforceable core is fraction placement plus arithmetic ranges, especially MCC at 35% to 87% in the extragranular fraction and the separate disintegrant constraints (granular 0.1% to 5% vs extragranular 1% to 5%).
- Claims 2-5 tighten fraction ratios (granular 5% to 20% in claim 3; extragranular 50% to 95% in claim 5), providing clear numeric “escape” bands for design-arounds.
- Claim 6 supplies a concrete formulation species using lactose monohydrate, croscarmellose sodium, PVP, Polysorbate 20 in granules and mannitol, MCC, sodium lauryl sulfate, croscarmellose sodium, sodium stearyl fumarate extragranular, anchoring interpretation of excipient roles.
FAQs
1) Is the claim limited to specific manufacturing methods or only composition?
The provided claims are directed to a composition defined by granular and extragranular fractions and excipient percentages, not to process steps.
2) If a product matches the overall excipient percentages but not the granular/extragranular split, is it within scope?
The claim requires fraction-specific placement and weight ranges, so matching overall tablet averages is not sufficient by itself.
3) Which excipient parameter is the strongest numerical limiter?
Microcrystalline cellulose in the extragranular fraction (35% to 87%) is one of the most restrictive and clearly bounded parameters.
4) Does claim coverage depend on the identity of the disintegrant and wetting agent?
Claim 1 is written by category (diluent, wetting agent, binder, disintegrant, MCC, lubricant), while claim 6 lists specific identities that support those categories.
5) What is the fastest way to assess literal risk for a generic reformulation?
Build a claim chart that verifies: rilpivirine HCl location and 2.75 mg dose in granules, then tests the extragranular MCC/disintegrant/wetting/lubricant ranges and the granular vs extragranular weight split.
References
- US Patent 11,065,198. Claims provided in user prompt (claims 1-6).
