Executive summary
US Patent 9,555,027 is a US-focused formulation and process estate that claims lurasidone (as the hydrochloride solid form) in a specific tablet composition defined by (i) pregelatinized starch quantity, (ii) water-soluble excipient (notably mannitol or lactose), (iii) water-soluble polymer binders (HPMC, HPC, PVP, PVA), (iv) granulation conditions by binder application (binder solution vs binder mixed with lurasidone), and (v) multiple performance/particle parameters (dissolution profile equivalence, F2 similarity factor, lurasidone particle size distribution). The claim set also includes tablet/disintegrant/lubricant dependents and a method-of-use for schizophrenia.
Scope in force risk terms: generics attempting “easy” label-to-label reformulation with high lurasidone loading may still fall into composition-in-range capture if they mirror the wt% windows and key excipient/binder selections and (where asserted) process steps and/or dissolution/similarity metrics.
US Patent 9,555,027 scope: what does it claim for lurasidone tablets?
Core claim theme (Claim 1): an oral preparation (tablet) containing lurasidone hydrochloride with a defined composition package:
- Lurasidone: 20 to 45% wt/wt
- Pregelatinized starch: 10 to 50% wt/wt
- Water-soluble excipient: recited generally in Claim 1, then narrowed in dependents (mannitol/lactose)
- Water-soluble polymer binder: recited generally in Claim 1, then narrowed in dependents (HPMC, PVA, PVP, HPC)
Formula capture: the lurasidone active is specifically defined as N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]-(2R,3R)-2,3-tetramethylene-butyl]-(1′R,2′S,3′R,4′S)-2,3-bicyclo[2,2,1]heptanedicarboxyimide hydrochloride, i.e., lurasidone hydrochloride (a fixed identity constraint).
What excipient and binder selections are actually locked down
While Claim 1 is broad on excipient/binder categories, the dependents function as practical infringement tripwires:
- Water-soluble excipient (Claim 7) includes: mannitol, lactose, saccharose, sorbitol variants, erythritol, xylitol
- Further narrowing (Claim 8): mannitol or lactose only
- Water-soluble polymer binder (Claim 10): HPMC, PVA, PVP, HPC
In Claim 30 and Claim 31, those selections are reinforced into narrower product-defining combinations:
- Claim 30: lurasidone 20–40%, pregelatinized starch 10–40%, excipient mannitol or lactose, binder HPC/HPMC/PVP/PVA (subset list)
- Claim 31: a specific “final package” for a tablet with mannitol, binder HPMC, plus disintegrant and lubricant constraints
Composition parameter windows (the real freedom-to-operate hinge)
These windows are repeated across multiple independent and dependent claims, increasing the chance that a competing formulation will meet at least one claim if it is designed to be within the claimed formulation design space:
- Lurasidone wt%: 20–45% (Claim 1); with narrower dependents at 20–40% (Claim 6/16/17/18/23/30/31)
- Pregelatinized starch wt%: 10–50% (Claim 1); narrower dependents at 10–40% and 10–30%
- Lurasidone per tablet (mg): multiple ranges
- 10–160 mg (Claim 12)
- 20–120 mg (Claim 13, 14)
- 40–120 mg (Claim 15)
- plus combinations tied to particular wt% selections (Claims 17–18, 23)
- Binder level per tablet: 0.5–10% wt/wt (Claim 11)
- Excipient per tablet: 30–60% wt/wt (Claim 9)
- Disintegrant content: 0.5–5% wt/wt (Claims 22–24)
- Lubricant content: 1.0–1.43% wt/wt (Claims 26–27)
Performance/quality attributes embedded into the claims
The patent’s reach is not limited to “recipe.” It also incorporates process-linked and performance-linked parameters.
- Particle size distribution (Claim 20): 50% by volume particle size of lurasidone = 0.1 to 8 μm
- Pregelatinized starch water-soluble matter (Claim 21): ≤ 30%
- Similarity factor for dissolution (Claim 25): f2 between 50 and 100 when lurasidone per tablet changes within 20–120 mg
- Dissolution profile equivalence (Claim 29): tablet “exhibits an equivalent dissolution profile across the range” of lurasidone per tablet
These create claim vulnerability for generics that may use different particle engineering, starch grade, or dissolution profile settings. For litigation, they also create an evidence-driven path: particle size testing, starch soluble matter assay, and dissolution testing with f2 calculations.
How broad is the claim coverage: formulation composition vs process vs use?
US 9,555,027 is a mixed estate:
- Composition claims (primarily Claim 1 and its dependents, plus Claim 29 and Claim 30),
- Process claims tied to granulation by specific “binder application” logic (Claims 2–3 and mirrored method claims 32–33),
- Method-of-use (Claim 34) for schizophrenia.
Composition claims (highest likelihood of capture)
- Claim 1 is the broad anchor: lurasidone wt% + pregelatinized starch wt% + excipient + binder.
- Claim 28 specifies oral preparation as a tablet, aligning with typical generic ANDA dosage forms.
- Claims 16–18 tighten the likely infringing design space by locking simultaneous lurasidone wt% + starch wt% + mg per tablet while also specifying excipient (mannitol or lactose).
- Claim 23 is a “mega dependent” that aggregates multiple constraints, effectively building a very specific formulation target.
Process claims (secondary but still relevant)
- Claim 2 / Claim 32: granulate powder mixture containing lurasidone + pregelatinized starch + water-soluble excipient by applying solution of water-soluble polymer binder.
- Claim 3 / Claim 33: granulate powder mixture containing pregelatinized starch + excipient by applying a solution or dispersion of lurasidone + binder.
These are not classic manufacturing process claims that protect “any granulation method.” They protect particular granulation assembly sequences and binder delivery forms (solution vs dispersion; whether lurasidone is present pre-mix vs introduced in binder granulation fluid).
Practical implication: if a challenger uses a different manufacturing order (e.g., pre-blending lurasidone into starch-excipient blend then spraying binder solution) it may still meet Claim 2 depending on exact sequence. If it dissolves/disperses lurasidone in the binder feed stream, it may meet Claim 3.
Method-of-use claim (Claim 34)
- Claim 34: treating schizophrenia by administering the oral preparation of Claim 1.
This creates a labeling linkage issue: if an ANDA is approved with indications for schizophrenia and the ANDA product practices Claim 1, the method-of-use claim becomes a direct infringement theory in US Hatch-Waxman litigation for “use” language and induced infringement dynamics.
What do the dependent claims add: excipient, disintegrant, lubricant, and tablet form?
Tablet form and disintegration mechanics:
- Claim 22: optional disintegrant with 0.5–5% wt/wt
- Claim 24: disintegrant selection list includes:
corn starch; crystalline cellulose; low substituted HPC; carmellose and salts (carmellose Ca/Na); croscarmellose Na; carboxymethyl starch Na; crospovidone
Lubricant mechanics:
- Claim 26–27: lubricant is 1.0–1.43% wt/wt, selected from magnesium stearate, talc, PEG, silica, hydrogenated vegetable oil
Unit-dose quantitative lock:
Claims 12–15 and 17–18 and 23 explicitly bind lurasidone dose mg ranges, increasing the chance that an ANDA strength will align with a claim range:
- Claim 14: 20–160 mg
- Claim 15: 40–120 mg
- Claim 17 ties 20–120 mg
- Claim 18 ties 40–120 mg
Where are the strongest “infringement pressure points” for generics?
1) wt/wt windows for lurasidone and pregelatinized starch
If a generic aims for a formulation with lurasidone at 20–45% by weight and pregelatinized starch at 10–50% by weight, Claim 1 is positioned for broad capture. Many “high drug-load” tablet approaches can land in this design space.
2) use of mannitol or lactose with the specified binder class
If the generic uses a typical water-soluble filler system (mannitol/lactose) and uses a water-soluble polymer binder from HPMC/HPC/PVA/PVP, it converges on Claim 8 and Claim 10 plus Claim 30.
3) granulation method sequencing
If the generic uses a granulation process that matches Claim 2 or Claim 3 (binder delivered as solution or dispersion; lurasidone present in the powder mixture vs introduced with binder), the process claims can be invoked as additional independent paths.
4) particle size and starch soluble matter constraints
Claim 20 and Claim 21 are narrower and testing-driven. If a generic cannot match the lurasidone d50 (50% vol. particle size) 0.1–8 μm or the pregelatinized starch water-soluble matter ≤30%, it can reduce risk under those dependents.
5) dissolution similarity (f2) / dissolution equivalence
Claim 25 and Claim 29 create a challenge for challengers that rely on bioequivalence but not on matching a specific in vitro dissolution similarity metric across the claimed dose range.
How does claim wording change risk across different generic strengths?
Claim 25 and the mg-per-tablet dependents indicate that risk is not uniform across all strengths. Claim 25 uses a scenario “when lurasidone per tablet changes over 20 to 120 mg,” locking f2 range 50 to 100. That is designed to protect across dose sizes rather than a single strength.
Claims 17 and 18 and 23 incorporate specific mg ranges into combination with wt% windows:
- Claim 17: lurasidone 20–40% wt%; pregelatinized starch 10–40% wt%; excipient mannitol/lactose; lurasidone 20–120 mg
- Claim 18: same but lurasidone 40–120 mg
- Claim 23: aggregates a set of constraints including excipient, binder, disintegrant, and specific mg range 40–120 mg
So, if a competitor’s dosage strengths map into these ranges, infringement exposure becomes strength-specific and formulation-specific.
Patent landscape structure for US 9,555,027: how this estate typically positions in litigation
Without external bibliographic data (filing date, assignees, family members, prosecution history, maintenance status, and whether claims are still in force), the analysis can only characterize the estate as claim-structured, not as a litigation timeline.
However, from the claim set alone, the estate is consistent with a formulation strategy that targets:
- ANDA-ready tablet reformulations (composition and excipient/binder windows)
- Manufacturing robustness (granulation process steps and binder delivery modes)
- Bio-relevant performance (f2 similarity and dissolution equivalence)
This increases its use in Paragraph IV-style disputes because challengers typically prepare for “generic product equals covered composition” arguments. The presence of performance and particle parameters also pushes evidence beyond standard recipe similarity into dissolution and particle analytics.
Which alternative product designs might avoid coverage inside the same technical space?
Based on the claim constraints, design-around efforts often focus on changing at least one of the following axes so that the formulation falls outside every asserted independent claim and key dependents:
- Excipient swap away from mannitol/lactose (if litigated on the narrower dependents)
- Binder substitution outside the recited water-soluble binder list (if litigated on dependents)
- Starch parameter changes (pregelatinized starch amount 10–50 wt% and/or water-soluble matter ≤30% for dependent)
- Lurasidone wt% outside 20–45 wt%
- Particle size outside 0.1–8 μm d50 range
- Dissolution similarity outside f2 50–100 across the claimed dose window
- Manufacturing sequence changes relative to Claim 2 or Claim 3 (binder delivery mode and whether lurasidone is pre-mixed vs fed in the binder solution/dispersion)
Key claim chart: US 9,555,027 coverage elements
| Claim element |
What is required |
Practical generic design implication |
| Active |
Lurasidone hydrochloride (fixed formula) |
No avoidance by switching salts without changing API identity |
| Lurasidone % wt |
20–45% (Claim 1); 20–40% in key dependents (Claims 6, 16–18, 23, 30, 31) |
High drug-load tablets likely converge |
| Pregelatinized starch % wt |
10–50% (Claim 1); narrowed to 10–40% and 10–30% in dependents |
Starch load is a main risk lever |
| Excipient |
Water-soluble excipient; narrowed to mannitol/lactose (Claims 8, 16–18, 30, 31) |
Avoiding mannitol/lactose can reduce dependent exposure |
| Binder |
Water-soluble polymer binder; narrowed to HPMC, PVA, PVP, HPC (Claim 10; reinforced in Claims 30–31) |
Binder selection must avoid the recited class list if dependents asserted |
| Binder amount per tablet |
0.5–10% wt/wt (Claim 11) |
Even if recipe matches, binder level can be a line |
| Granulation process |
Claim 2/32 vs Claim 3/33 |
Manufacturing sequence and binder feed matter |
| Tablet strength mg |
10–160 mg; 20–120 mg; 40–120 mg dependents |
Dose strength alignment drives claim mapping |
| Disintegrant |
Optional 0.5–5% wt/wt (Claims 22–24) |
Presence and amount can be used in infringement mapping |
| Lubricant |
Optional 1.0–1.43% wt/wt (Claims 26–27) |
Presence and amount can be used in infringement mapping |
| Particle size |
d50 (50% vol) 0.1–8 μm (Claim 20) |
Particle engineering and milling become relevant |
| Starch soluble matter |
≤30% (Claim 21) |
Starch grade selection and QC tests matter |
| Dissolution profile |
f2 50–100 across 20–120 mg (Claim 25) and “equivalent dissolution profile” (Claim 29) |
Dissolution testing protocol becomes critical |
Key takeaways
- US 9,555,027 is a lurasidone hydrochloride tablet formulation patent that locks wt/wt ranges for lurasidone (20–45%) and pregelatinized starch (10–50%), with major dependent claims tightening to mannitol/lactose and water-soluble binders (HPMC/HPC/PVP/PVA).
- The estate includes granulation process sequencing via binder application form (solution vs dispersion) and whether lurasidone is introduced pre-mix vs with binder feed.
- Risk is increased when a generic targets multiple dose strengths because the claims include mg-per-tablet ranges and dissolution similarity metrics (f2 50–100; dissolution equivalence).
- The narrower technical dependents (lurasidone particle size d50, pregelatinized starch water-soluble matter) create potential design-around levers, but they also create evidence-based infringement tests.
FAQs
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Does US 9,555,027 cover lurasidone oral solutions or only tablets?
The claims expressly include an oral preparation that is a tablet (Claim 28) and repeatedly define per-tablet composition and per-tablet mg ranges.
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What excipients are most likely implicated by the claims?
The strongest dependent coverage centers on mannitol or lactose (Claims 8, 16–18, 30, 31), with broader excipient coverage in Claim 7.
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Which manufacturing steps are tied to the process claims?
Claims 2/32 and 3/33 are linked to granulation by applying a binder solution to one powder mixture (with lurasidone present) or applying a solution/dispersion of lurasidone and binder to a starch/excipient mixture.
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How do dissolution similarity metrics affect infringement risk?
Claim 25 requires an f2 similarity factor of 50–100 when lurasidone per tablet changes over 20–120 mg; Claim 29 requires equivalent dissolution profile across dose range.
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Is particle size engineering relevant under this patent?
Yes. Claim 20 requires lurasidone 50% by volume particle size (d50) in the 0.1–8 μm range.
References
- US Patent 9,555,027 (claims as provided by user text).
