United States Patent 11,097,007: Scope, Claims, and US Drug-Delivery Patent Landscape for Polyvinylpyrrolidone Stabilized High-Viscosity/Shear-Thinning Injectable Suspensions
US Patent 11,097,007 claims injectable (and gel / sustained-release injectable) compositions that combine (i) a poorly soluble active (notably aripiprazole and a second quinolinone structure) with (ii) a polyvinylpyrrolidone (PVP)-containing suspending system engineered to deliver a high low-shear viscosity and a low high-shear viscosity, and (iii) strict particle-size and concentration windows. The claims also extend into dosing-administration constructs and a treatment method for recurrence of psychiatric disorders.
What is the claimed core technology in 11,097,007?
The patent is built around a rheology-defined dispersion that behaves like a gel at rest and becomes a sol under impact/shear, which aligns with injectability requirements (needle flow) while reducing settling or phase separation at rest.
Key functional parameters
- Poorly soluble drug (examples explicitly recited)
- Aripiprazole (or a salt), or
- 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one (or a salt)
- Particle size (primary, and secondary in one dependent claim)
- Claim 1: mean primary particle diameter ≤ 30 μm
- Claim 6: mean primary particle diameter 0.5 to 30 μm
- Sustained-release claims split primary particle size windows (examples):
- Claim 13: 1 to 10 μm
- Claim 15: 4 to 30 μm
- Drug concentration
- Claim 1: 200 to 600 mg/mL
- Claim 13: 200 to 400 mg/mL
- Claim 15: 300 to 600 mg/mL
- PVP grade window
- PVP concentration
- 0.1 to 100 mg/mL (broad enough to capture many PVP formulations, but still constrained)
- Rheometer viscosity targets at specific shear rates
- Low shear: viscosity ≥ 40 Pa·s in 0.01 to 0.02 s−1
- High shear: viscosity ≤ 0.2 Pa·s in 900 to 1,000 s−1
- Measured at 5° C., 25° C., or 40° C. depending on the claim
Dispersion medium / suspending agent composition
- Dispersion medium includes water (Claim 3; gel compositions include water in Claim 6)
- Optional co-thickeners/suspending aids:
- Polyethylene glycol (PEG) (Claims 4, 7, 17, 18)
- Carboxymethyl cellulose (CMC) or salt (Claims 5, 8, 18)
- Quantified ranges when both PEG and CMC are used (Claim 9; Claim 19)
- PEG: 0.05 to 2 mg/mL
- CMC: 0.5 to 50 mg/mL
How broad are the claims as written?
The breadth comes from (i) allowing two different poorly soluble actives, (ii) permitting a wide range of PVP K values and concentrations, and (iii) focusing on measured rheology plus particle-size/concentration windows. The breadth is partially tightened by strict numeric constraints for viscosity, particle size, and drug loading.
Claim family map (what each claim type covers)
| Claim set |
Claim numbers |
Product type / scope axis |
Main limits that drive allowance |
| Foundational injectable suspension |
1-5 |
Injectable preparation with PVP-containing suspending agent; rheology at defined shear rates; specific drugs; numeric particle-size and concentration ranges |
drug identity; primary particle ≤ 30 μm; drug 200-600 mg/mL; PVP K 12-30; PVP 0.1-100 mg/mL; viscosity ≥40 Pa·s (0.01-0.02 s−1) and ≤0.2 Pa·s (900-1000 s−1) at 5/25/40°C |
| Gel compositions (similar composition, gel/sol behavior implicit) |
6-12 |
Gel composition with water and PVP-containing suspending agent; particle-size 0.5-30 μm; adds secondary particle criterion; viscosity constraints |
includes explicit primary range plus “secondary up to 3x primary” (Claim 10); viscosity constraints in 5/25/40°C windows (Claims 11-12) |
| Sustained-release injectable (gel-to-sol under impact, dosing cadence) |
13-22 |
Sustained-release injectable: gel at rest, sol on impact; monthly vs every 2-3 months regimens; tight particle-size and drug loading windows |
primary particle size and drug concentration windows tighten substantially; ties to dosing frequency (once per month or once every 2-3 months); rheology constraints remain present via dependent claims |
Important structural pattern
- Rheology limitation appears as a defining structural/functional feature. In practice, this can be both:
- A strong differentiator versus prior art that does not hit the specified low-shear / high-shear viscosity behavior, and
- A potential non-infringement pathway if a competitor adjusts processing to shift viscosity outside the claimed thresholds while keeping similar particle sizes and drug loadings.
What exactly is claimed in Claim 1 (and why it matters for infringement analysis)?
Claim 1 is the anchor.
Claim 1 essentials
- Injectable preparation comprising:
- Poorly soluble drug: aripiprazole or 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one, or salt
- Dispersion medium: not fully enumerated in Claim 1, but water appears in dependent Claim 3 and gel claims
- Suspending agent containing PVP
- Rheology (rheometer at 5° C., 25° C., or 40° C.):
- At least one point in 0.01 to 0.02 s−1: viscosity ≥ 40 Pa·s
- At least one point in 900 to 1,000 s−1: viscosity ≤ 0.2 Pa·s
- Drug particle constraint
- mean primary diameter ≤ 30 μm
- Drug loading
- PVP spec
- K value 12 to 30
- concentration 0.1 to 100 mg/mL
Practical implication
A product that matches drug identity, particle size, and drug/PVP concentration but does not reproduce the specified shear-thinning signature at the specified shear-rate ranges and temperature(s) would fail the claim.
How do Claims 2-5 change the scope?
Claim 2
- Narrows measurement condition to 25°C specifically.
- Keeps the same rheology thresholds and shear windows.
Claims 3-5
- Claim 3: at least water as dispersion medium.
- Claim 4: suspending agent additionally contains PEG.
- Claim 5: suspending agent additionally contains PEG and CMC (or salt).
Net effect
These are dependent claims adding ingredients and measurement specificity. Independent coverage remains anchored in Claim 1.
How do Claims 6-12 expand into gel compositions and particle morphology?
Claim 6 (gel composition)
- Gel composition with:
- poorly soluble drug (same two actives)
- water
- PVP-containing suspending agent
- Particle sizes and loading:
- primary diameter 0.5 to 30 μm
- drug concentration 200 to 600 mg/mL
- PVP:
- K 12 to 30
- 0.1 to 100 mg/mL
- Unlike Claim 1, Claim 6 explicitly sets primary lower bound (0.5 μm).
Claims 7-9 (optional PEG and CMC)
- Claim 7: adds PEG.
- Claim 8: adds PEG + CMC.
- Claim 9: quantifies:
- PEG 0.05 to 2 mg/mL
- CMC 0.5 to 50 mg/mL
Claim 10 (primary/secondary particle relationship)
- secondary particle diameter up to but not exceeding three times mean primary particle diameter.
Claims 11-12 (viscosity measurement temperature-specific)
- Claim 11: viscosity thresholds as in Claim 1, measured at 5° C., 25° C., or 40° C.
- Claim 12: same thresholds but measured at 25°C.
How do Claims 13-22 define sustained-release injectable products?
These claims add two additional layers:
- Gel-to-sol under impact behavior and
- Dosing frequency cadence (monthly or every 2-3 months), plus tighter primary particle sizing and drug concentration windows.
Claim 13 (once per month; sustained release injectable)
- Sustained-release injectable preparation with:
- drug: aripiprazole or the quinolinone
- water + PVP suspending agent
- Primary particle and loading:
- primary diameter 1 to 10 μm
- drug concentration 200 to 400 mg/mL
- PVP:
- K 12 to 30
- concentration 0.1 to 100 mg/mL
- Physical behavior:
- composition is gel when allowed to stand
- changes to sol when subjected to impact
- Dosing frequency:
- administered once per month
Claim 15 (once every 2 to 3 months; sustained release injectable)
- Primary diameter 4 to 30 μm
- Drug concentration 300 to 600 mg/mL
- Same PVP constraints and gel-to-sol under impact
- Dosing:
- once every two to three months
Dependent dosing precision
- Claim 14: tighter primary window for Claim 13: 2 to 7 μm
- Claim 16: tighter primary window for Claim 15: 5 to 20 μm
Claims 17-19 (PEG/CMC additions)
- Claim 17: adds PEG
- Claim 18: adds PEG + CMC
- Claim 19 quantifies:
- PEG 0.05 to 2 mg/mL
- CMC 0.5 to 50 mg/mL
Claim 20 (particle aggregation constraint)
- secondary particle up to 3x primary
Claims 21-22 (rheology measurement in sustained-release)
- Claim 21: rheology measured at 5/25/40°C
- Claim 22: rheology measured at 25°C
How do the method claims work (Claims 23-24)?
Claim 23
- Method for treating recurrence of schizophrenia, bipolar disorder, or depression
- comprises administering the injectable preparation according to Claim 1
This is a classic disease-treatment method claim tied directly to the formulation claim.
Claim 24
- Administration route:
- intramuscularly or subcutaneously
Where does 11,097,007 sit in the US patent landscape?
Landscape logic
The claimed formulation overlaps with well-established categories of injectable suspensions for poorly soluble drugs and with known “long-acting” approaches (typically depot-like behavior with controlled release). The differentiators, as drafted, are not generic “use of a long-acting injectable.” They are:
- Specific PVP K value window
- Defined drug concentration and particle size windows
- Defined shear-rate viscosity signature
- Gel-to-sol under impact behavior for sustained-release constructs
- Dosing frequency tied to the sustained-release composition
Practical consequence for freedom-to-operate
From an infringement perspective, the claim set is best attacked or defended by:
- rheology replication: viscosity at specified shear rates and temperature(s)
- particle-size distribution: primary (and secondary cap in dependent claims)
- formulation composition: PVP K and concentration range; optional PEG/CMC not required for independent claims but can narrow design-around
From an invalidity/obviousness perspective, the most relevant prior art would be:
- depots or suspensions for aripiprazole or other poorly soluble actives
- long-acting injectables using PVP or related stabilizers
- long-acting injectable systems that combine shear thinning at high shear for injection with high viscosity at rest
The claim’s tight numeric rheology windows and particle-size/load windows are the main pressure points for prior-art matching.
Claim-by-claim claim-scope “design-around” pressure points
1) Shear rheology thresholds
A design-around route is to shift either:
- low shear region viscosity below 40 Pa·s at 0.01-0.02 s−1, or
- high shear region viscosity above 0.2 Pa·s at 900-1,000 s−1,
while keeping everything else similar.
Because the claims use “at least one point” within each shear range, challengers must consider whether the measured flow curve intersects those thresholds anywhere within the ranges, not just averages.
2) Particle size windows
- Claim 1: primary diameter ≤ 30 μm
- Gel: primary diameter 0.5 to 30 μm
- Sustained release:
- monthly: 1 to 10 μm
- every 2-3 months: 4 to 30 μm
A competitor can potentially match rheology but move particle size outside windows, especially for sustained-release dosing claims.
3) Drug concentration
- Claim 1: 200-600 mg/mL
- Monthly: 200-400 mg/mL
- Every 2-3 months: 300-600 mg/mL
4) PVP K value
- Claims require K 12 to 30
This can be a direct differentiation lever if a competitor uses PVP grades outside that window.
5) PVP concentration
- 0.1-100 mg/mL
Most competing PVP-stabilized suspension systems can fall within this broad band; the K value and rheology constraints then become more decisive.
What claim scope is actually covered for drug identity?
The claims cover:
- aripiprazole (or salt)
- 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one (or salt)
This is narrower than “any poorly soluble drug,” which is important for landscape filtering. Many prior art depot suspensions for other actives will fall outside these independent claims unless they disclose these specific actives and the same rheology/particle/load constraints.
How do the sustained-release claims interact with the base injectable claims?
Sustained-release claims (13-22) are additional product-scoped constraints on top of the foundational rheology and formulation architecture:
- gel-to-sol under impact
- dosing frequency
- tighter particle-size and drug-loading windows
Even if a competitor makes a Claim 1-like injectable, they may avoid sustained-release claims by failing the gel/sol behavior and/or dosing frequency-linked structure (and/or particle/load windows).
Key Takeaways
- US 11,097,007 is defined by a specific rheology profile: ≥40 Pa·s at 0.01-0.02 s−1 and ≤0.2 Pa·s at 900-1,000 s−1 (measured at specified temperatures), combined with PVP K 12-30 and PVP 0.1-100 mg/mL.
- The claim’s active scope is limited to two poorly soluble drugs: aripiprazole and a specific quinolinone structure, each at strict drug loading and particle-size parameters.
- Sustained-release coverage is not generic: it is bound to gel-to-sol under impact plus monthly vs every 2-3 months dosing and tighter primary particle-size/drug concentration windows.
- Design-around paths concentrate on rheology and particle/load windows: small formulation changes that shift viscosity at the specified shear-rate ranges or move primary particle size outside the sustained-release windows are the most direct levers.
- Method claims (recurrence treatment) depend on administering a formulation that meets Claim 1 and are limited further by IM/SC route.
FAQs
1) Does Claim 1 require the formulation to be water-based?
No. Claim 1 requires an injectable preparation with a dispersion medium and PVP-containing suspending agent. Water is explicitly required in Claim 3 and in the gel composition claims.
2) Are PEG and carboxymethyl cellulose required for infringement?
No. They are introduced in dependent claims (Claims 4-5, 7-9, 17-19). Claim 1 and Claim 6 do not require PEG or CMC as essential elements beyond the PVP-containing suspending agent and the numeric constraints.
3) What is the single biggest measurable differentiator in the claims?
The rheometer viscosity behavior at two specific shear-rate ranges: high viscosity at low shear and low viscosity at high shear, with explicit numeric thresholds and specified temperature measurement windows.
4) Can a competitor avoid sustained-release claims by changing dosing frequency?
Yes, within the logic of the claim set. The sustained-release claims (13 and 15) tie the sustained-release injectable construct to administration once per month or once every two to three months, respectively, alongside compositional and particle-size constraints.
5) Is the “secondary particle diameter ≤ 3x primary” limitation mandatory for all claims?
No. The secondary particle constraint appears as a dependent limitation in Claim 10 for the gel composition and in Claim 20 for sustained release.
References
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