US Patent 8,722,679 scope and claims: controlled-release sterile aripiprazole freeze-dried injectable (particle size 1–10 μm)
US Patent 8,722,679 claims a controlled-release, sterile aripiprazole injectable that is freeze-dried and then reconstituted with water for injection to form a homogeneous suspension with a defined aripiprazole particle size (mean 1–10 μm) and a release profile of at least ~1–4 weeks, depending on dependent claim limits. The core claim scope is driven by three technical pillars: (1) particle size specification, (2) vehicle/suspending-agent and excipient package, and (3) freeze-dry/reconstitution manufacturing steps.
What is the patent scope of US 8,722,679 and how broadly does it cover aripiprazole injections?
Independent claim 1 covers a controlled-release sterile aripiprazole formulation made by mixing a freeze-dried composition with water for injection, where:
- aripiprazole has mean particle size ~1 to 10 microns
- aripiprazole is combined with a vehicle suitable for suspension
- the resulting product is a homogeneous suspension that releases aripiprazole for at least one week after injection
Key claim-interpretation levers
- “Freeze-dried composition + water for injection”
- Reads on a two-part product where the sterile drug product bulk is freeze-dried, then reconstituted.
- “Homogeneous suspension”
- Requires final product appearance/behavior consistent with suspension uniformity.
- “Mean particle size of about 1 to 10 microns”
- Enforces a particle-size window as a gating limitation; this is the sharpest, easiest-to-map infringement barrier for competitors.
- “Releases over a period of at least one week”
- Sets a minimum performance threshold; longer release is covered by dependent claims.
What do the main claim limitations require (particle size, excipients, loading, and release duration)?
US 8,722,679 is structured so dependent claims narrow the formulation along excipient identity, loading ranges, and release duration.
Particle size ranges across the claim set
- Core: mean 1–10 μm (claims 1, 2, 7, 11–16, 17–23, 26–30, 31–34)
- Further narrowings:
- ~2.5 μm (claims 4, 20, 33–34)
- ~2–4 μm (claim 26)
- Distribution detail for 2.5 μm product:
- 95% < 20 μm
- 90% < 15 μm
- 50% < 10 μm
- 10% < 2 μm (claims 33–34)
Practical impact: Any design-around strategy that moves mean particle size outside the claimed band or changes the distribution could avoid literal scope, assuming particle-size is measured in a way that supports claim metrics.
Aripiprazole loading ranges (mg/mL)
Multiple numeric constraints create additional fences:
- 0.1 to 400 mg per 1 mL (claims 2, 21, 17)
- 0.1 to 600 mg per 1 mL (claim 22)
- 100 to 400 mg per 2 mL (claim 35)
- 100 to 200 mg per 1 mL (claim 36)
Release duration timeline coverage
- At least one week (claim 1)
- At least two weeks (claims 2, 22)
- At least three weeks (claim 3; also claim 7 explicitly recites ≥3 weeks)
- At least about three weeks to specific windows:
- claim 8: ~3–4 weeks
- claim 9: 3 or 4 weeks
- claim 10: ~4 weeks
The claims are written so performance (release duration) scales with dependent narrowing: the longer the claimed duration, the more precisely other formulation constraints attach.
Which excipients and suspending agents are explicitly covered in US 8,722,679?
The formulation claims include explicit excipient lists plus functional categories.
Suspensions and suspending agents
For claims that specify suspending agents (claim 18):
- carboxymethylcellulose or sodium salt
- hydroxypropyl cellulose
- hydroxypropylethyl cellulose
- hydroxypropylmethyl cellulose
- polyvinylpyrrolidone (PVP)
Bulking agents
From claim 18:
- mannitol
- sucrose
- maltose
- lactose
- xylitol
- sorbitol
Buffering agents / pH adjustment package
From claims 7 and 18:
- sodium phosphate (also potassium phosphate)
- TRIS buffer
- pH is repeatedly tied to about 7 (claim 7)
- and generally tied to 6 to 7.5 in numeric composition claims (claims 17, 31, 32)
“CMC + mannitol + phosphate ~7” is a recurring tight subgroup
Claims 7 and 25 lock a specific excipient combination:
- aripiprazole (mean 1–10 μm)
- carboxymethyl cellulose (or sodium salt)
- mannitol
- sodium phosphate to adjust pH to about 7
- optionally sodium hydroxide for pH adjustment
- release: at least about three weeks (claim 7), with similar duration language in related dependents
What formulation compositions with percent-by-weight/volume are claimed?
Numeric composition claim language provides a high-resolution target for product mapping.
Claim 17: general percent ranges (by w/v on total volume)
Requires:
- aripiprazole mean 1–10 μm, 1–40% (w/v)
- suspending agent 0.2–10%
- bulking agent 1–10%
- buffering agent 0.02–2%, pH 6–7.5
Claim 31: tighter particle size and subranges
- aripiprazole mean 1–5 μm, 1–40%
- suspending agent 0.2–10%
- bulking agent 1–10%
- buffering agent 0.02–2%, pH 6–7.5
Claim 32: even tighter subset with specific numeric targets
- aripiprazole mean 2.5 μm, 5–20%
- suspending agent 0.5–5%
- bulking agent 4–5%
- buffering agent 0.03–1%, pH 6–7.5
These percent-by-weight/volume claims are “needle-threading” constraints and typically control infringement risk more than broad categorical language.
What are the exact formulation “Formulation A, B, C” examples claimed in US 8,722,679?
Claim 19 lists three explicitly described formulations.
| Parameter |
Formulation A |
Formulation B |
Formulation C |
| Aripiprazole dose |
100 mg |
200 mg |
400 mg |
| Mean particle size |
1–10 μm |
1–10 μm |
1–10 μm |
| Carboxymethyl cellulose |
9 mg |
9 mg |
9 mg |
| Mannitol |
45 mg |
45 mg |
45 mg |
| Sodium phosphate |
0.8 mg |
0.8 mg |
0.8 mg |
| Water for injection |
qs to 1 mL |
qs to 1 mL |
qs to 1 mL |
Scope note: These examples anchor the claim landscape but do not necessarily limit independent scope. They matter for validity attacks (best mode, written description) and for direct infringement mapping to product labels or manufacturing records.
What process claims are included, and do they create additional manufacturing/IP barriers?
US 8,722,679 contains process/product-by-process style claim 27 and dependents 28–30.
Claim 27: freeze-dried product made via defined particle-size reduction
A controlled release sterile aripiprazole formulation obtained by a process:
- preparing sterile bulk aripiprazole with desired particle-size distribution
- preparing sterile vehicle with one or more suspending agents
- combining into sterile primary suspension
- reducing mean particle size to ~1–10 μm
- freeze-drying the sterile final suspension
- adding water to the freeze-dried product
The claim binds the end product through the stated manufacturing sequence and, critically, the particle-size reduction step.
Claim 28–29: wet milling route
- claim 28: mean particle-size reduction is carried out using wet milling
- claim 29: wet milling is wet ball milling
Claim 30: freeze-drying conditions
Freeze-drying performed by:
- cooling homogeneous suspension to about -40°C
- drying below about 0°C under vacuum
Scope impact: Even if an accused product differs in excipients, process claims can create parallel infringement theories if the manufacturing method and particle-size outcome fall within the claim constraints.
How does US 8,722,679 compare with typical aripiprazole long-acting injection patent themes?
This patent’s claim strategy is aligned with common LAI (long-acting injectable) patent fencing, but with specific aripiprazole-formulation hooks:
- Particle-size engineering (mean 1–10 μm; tight distribution for ~2.5 μm)
- Freeze-drying and reconstitution (freeze-dried composition + water for injection)
- Suspension formulation with CMC/sodium phosphate/mannitol style package
- Duration claims tied to pharmacotechnical release (≥1 week through ~4 weeks)
What is the litigation and validity risk profile for US 8,722,679?
No litigation dataset, Orange Book listing, or Patent Trial and Appeal Board (PTAB) file history is provided in the input. Without a verified case docket or public filings tied to US 8,722,679, a reliable risk assessment cannot be produced.
Orange Book status: what FDA listings does US 8,722,679 likely cover?
No FDA Orange Book listing details, NDA/BLA identifiers, or listed patents are provided in the input. Without those, a definitive mapping of the patent to the specific US-listed drug product and dosage form cannot be produced.
Generic entry risks: what would a Paragraph IV challenger have to prove to avoid US 8,722,679?
A challenger seeking to avoid infringement would typically target at least one of the independent claim’s gating features:
- Particle size outside “about 1–10 μm” or avoid literal satisfaction of mean particle-size.
- Composition structure: avoid a freeze-dried composition reconstituted with water for injection into a homogeneous suspension meeting the release threshold.
- Excipients/pH package: if narrowed dependents are asserted, avoid the claimed excipient set (CMC/sodium phosphate/mannitol style) or avoid claimed numeric ranges.
- Release duration: show that release is not “at least one week” for claim 1 or does not meet the dependent time windows (≥2 weeks, ≥3 weeks, etc.).
Because the input contains only claim text and not the specification’s measurement methods (e.g., D50 vs. mean definition; particle-size measurement technique) or product assay details, infringement mapping can’t be finalized beyond the claim language itself.
Key Takeaways
- US 8,722,679 is a formulation-centric IP estate for freeze-dried, reconstituted sterile aripiprazole that forms a homogeneous suspension and achieves controlled release of ≥1 week, with dependent coverage extending to ~4 weeks.
- The claim set is engineered around aripiprazole mean particle size (about 1–10 μm) and tighter subranges including ~2.5 μm with explicit distribution criteria.
- Several dependents lock a specific excipient and pH package, especially CMC (or sodium salt) + mannitol + sodium phosphate (pH ~7), with optional NaOH.
- Numeric subclaims constrain w/v excipient percentages and pH (6–7.5), increasing the specificity of infringement and design-around analysis.
- Process claims add barriers via wet milling (including wet ball milling) and specific freeze-drying temperature/vacuum conditions, tied to achieving the claimed particle-size range.
FAQs
1) Does US 8,722,679 require a specific particle-size distribution or only a mean value?
The independent claims require mean particle size ~1–10 μm. Distribution metrics appear in dependent claims for the ~2.5 μm subgroup (with stated percent cutoffs).
2) Can a formulation avoid infringement by using aripiprazole as a different hydrate form?
The claims include dependents that specify Aripiprazole Anhydrous Crystals B and Aripiprazole Hydrate A. Avoidance could be possible for those dependent claims, but claim 1/2/7 scope still centers on particle size and formulation performance unless those dependents are asserted.
3) What freeze-drying step is claimed in US 8,722,679?
Claim 27 generically requires freeze-drying the sterile final suspension. Claim 30 narrows to cooling to about -40°C and drying below about 0°C under vacuum.
4) Are the suspension excipients limited to carboxymethylcellulose and mannitol?
No. Many dependents provide examples and lists. However, several narrower claims explicitly require CMC (or sodium salt) + mannitol + sodium phosphate style buffers.
5) What release profile does the patent cover?
Claim 1 covers at least one week; dependent claims cover at least two weeks, at least about three weeks, and specific ranges including ~3–4 weeks and ~4 weeks.
References (APA)
- United States Patent 8,722,679 (claims provided in prompt).
