Details for Patent: 7,115,587

United States Patent 7,115,587: Scope, Claim-by-Claim Coverage, and Landscape

What does US 7,115,587 protect?

US Patent 7,115,587 protects (i) aripiprazole inclusion complexes with substituted beta-cyclodextrins and (ii) specific aqueous injectable aripiprazole formulations that use these complexes to address site irritation through pH control and buffering, with explicit examples of SBECD plus tartaric acid and pH targets around 4 to 4.6.

The patent’s independent claim set is structured around two core inventions:

1. Complex-level protection: aripiprazole complexed in a substituted beta-cyclodextrin (claims 1-3).
2. Product-level protection: aqueous injectable formulations combining aripiprazole with the substituted beta-cyclodextrin and an acid buffer system, including explicit compositional and pH ranges (claims 4-21), plus method-of-use claims built on the formulation (claims 22-24).

Claim scope map: what each claim covers

1–3: Inclusion complex compositions

Claim 1

• Scope: “An inclusion complex of aripiprazole in a substituted beta-cyclodextrin.”
• Breadth: Broadest at the complex level because it only requires:
  • aripiprazole
  • inclusion complex formation
  • a “substituted beta-cyclodextrin” (not limited yet)

Claim 2

• Scope: complex as claim 1 where the substituted beta-cyclodextrin is SBECD or HPBCD.
• Effect: narrows the cyclodextrin substituents to two specific commercial types.

Claim 3

• Scope: complex as claim 2 where the cyclodextrin is SBECD.
• Effect: further narrows to one cyclodextrin species.

Practical inference for design-around:
Any competitor complex that uses a non-listed substituted beta-cyclodextrin, or a non-inclusion-complex structure, or avoids the “substituted beta-cyclodextrin” limitation can fall outside this claim family. The patent does not say “beta-cyclodextrin derivatives generally,” it names substituted beta-cyclodextrins and later names SBECD/HPBCD.

4–6: Formulation protection (composition + injectable form)

Claim 4

• Scope: “A pharmaceutical formulation comprising aripiprazole and a substituted β-cyclodextrin.”
• Breadth: broad product claim because it does not require injection, pH, or buffer yet.

Claim 5

• Scope: claim 4 in the form of an injectable formulation.
• Effect: restricts to injectable dosage forms (route not specified here).

Claim 6

• Scope: claim 4 where the substituted β-cyclodextrin is SBECD or HPBCD.
• Effect: narrows to those two.

7–12: Aqueous injectable formulation with pH 3.5–5 and acid buffer

Claim 7

• Scope: aqueous injectable formulation having pH about 3.5 to about 5.
• Significance: this is one of the main “control” limitations. It frames the buffering strategy and limits outside that pH window.

Claim 8

• Scope: claim 7 including an acid buffer.
• Effect: adds buffer presence as a required element.

Claim 9

• Scope: acid buffer is selected from a long but finite list including:
  • tartaric acid (or salt)
  • citric acid (or salt)
  • HCl (or salt)
  • acetic acid (or salt)
  • maleic acid (or salt)
  • malic acid (or salt)
  • sulfuric acid (or salt)
  • toluene sulfonic acid (or salt)
  • benzenesulfonic acid (or salt)
  • naphthalenesulfonic acid (or salt)
  • ethanesulfonic acid (or salt)

Claim 10

• Scope: further includes a base to adjust the aqueous formulation pH to about 3.5 to about 5.
• Design implication: a competitor that uses only acid (no base adjustment) or achieves pH via different components may attempt to contest whether the limitation is met.

Claim 11

• Scope: cyclodextrin-to-aripiprazole weight ratio 10:1 to 100:1.
• Effect: quantitative composition constraint.

Claim 12

• Scope: acid buffer-to-aripiprazole weight ratio 2:1 to 10:1.
• Effect: ties buffer amount to the drug load.

Where these claims sit in the hierarchy:
Claims 7-12 form a layered system: pH range + buffer present + buffer identity + base adjustment + two ratio constraints.

13–16: Dose range and irritation-related performance

Claim 13

• Scope: injectable dosage provides 1 to 10 mg aripiprazole/mL.

Claim 14

• Scope: when cyclodextrin is SBECD, SBECD-to-aripiprazole weight ratio 20:1 to 40:1.

Claim 15

• Scope: aripiprazole and substituted β-cyclodextrin are in the form of an inclusion complex.
• Effect: reinforces that not just a mixture, but complexed state is required.

Claim 16

• Scope: formulation produces minimal irritation at the injection site.
• Effect: adds a functional/performance characteristic. It can be used in enforcement even where composition matches, but it can also become a litigation focal point (what test qualifies as “minimal,” what standard is used, etc.).

17–21: Specific formulation embodiment with explicit pH, components, and concentrations

Claim 17

• Scope: aqueous injectable formulation comprising:
  • aripiprazole
  • SBECD
  • tartaric acid
  • sodium hydroxide
  • water
• pH: about 4 to about 4.6

Claim 18

• Scope: explicit concentrations (per 1 mL formulation):
  • aripiprazole: 1.5 to 8 mg/mL
  • SBECD: 100 to 200 mg/mL
  • tartaric acid: 7 to 9 mg/mL
  • sodium hydroxide: qs to adjust pH to 4 to 4.6
  • water: qs to 1 mL

Claim 19

• Scope: aripiprazole and SBECD form an inclusion complex.

Claim 20

• Scope: designed for intramuscular administration “without causing unacceptable irritation.”

Claim 21

• Scope: inclusion complex provides at least 2 mg aripiprazole/mL when measured at a substituted-β-cyclodextrin concentration of 5% w/v in water.
• Effect: establishes a quantitative complexing-performance condition tied to cyclodextrin concentration.

This is the patent’s tightest claim family because it locks in:

• the exact cyclodextrin identity (SBECD)
• the buffer identity (tartaric acid)
• the base (sodium hydroxide)
• a narrow pH window (4 to 4.6)
• explicit concentration ranges for aripiprazole, SBECD, tartaric acid
• route/performance limitations (IM; no unacceptable irritation)
• inclusion complex performance (measured at 5% w/v cyclodextrin)

22–24: Method-of-use built on the formulation

Claim 22

• Scope: administering injectable aripiprazole to avoid “unacceptable irritation” using the formulation of claim 17.

Claim 23

• Scope: route limited to intramuscular.

Claim 24

• Scope: treating schizophrenia using the formulation of claim 5 without undue irritation at the site of administration.

Landscape implication:
If a product avoids claim 17 (the narrow embodiment) but matches claim 5 (broad formulation with injectable + substituted beta-cyclodextrin), claim 24 still creates a method-use hook, unless the pH/buffer constraints in claim 5 are also avoided. Claim 24 incorporates “the formulation as defined in claim 5,” so the route and irritation limitation are anchored to claim 5’s definition, not claim 17’s explicit pH/tartaric system.

How broad is the protection across embodiments?

Breadth tiers

Where competitors are most exposed

Exposure drivers

The highest-risk overlap zones are:

1. SBECD-based inclusion complexes with aripiprazole (claims 1–3; 15; 19).
2. Aqueous injectable dosing at pH 3.5–5 with an acid buffer and base adjustment (claims 7–10).
3. Tartaric-acid buffered SBECD system at pH 4–4.6, with explicit concentration bands (claims 17–18).
4. Intramuscular administration with performance claims framed as “minimal/unacceptable/undue” irritation (claims 16, 20, 22–24).
5. The quantitative ratio bands:
   • cyclodextrin:aripiprazole 10:1 to 100:1 (claim 11)
   • SBECD:aripiprazole 20:1 to 40:1 (claim 14)
   • acid buffer:aripiprazole 2:1 to 10:1 (claim 12)

High-leverage enforcement positions

• A product that matches claim 17/18 is exposed to both product and method claims (claims 17–23).
• A product that matches cyclodextrin identity and injectable inclusion-complex structure and lands inside pH/buffer/ratio zones is exposed to broader claim families (claims 1–16 and 24, depending on exact definition of claim 5).

Design-around pressure points (claim-limiting features)

A design-around typically targets at least one element that is required in the asserted claim set:

For complex claims (1–3):

• Use a cyclodextrin type outside “substituted beta-cyclodextrin” as construed in the patent, or outside SBECD/HPBCD if trying to avoid 2–3.

For formulation claims (7–12):

• Avoid pH 3.5–5 as a formulated target.
• Avoid a listed “acid buffer” chemistry, or avoid the “acid buffer” and “base adjustment” structure as specified.
• Avoid the mandated weight ratios (cyclodextrin:drug and buffer:drug bands).

For the tight exemplar (17–21):

• Change one or more of the explicit component identity locks (SBECD; tartaric acid; sodium hydroxide), or move pH outside 4–4.6, or move concentrations outside the explicit ranges, or avoid “designed for IM without unacceptable irritation” and the inclusion-complex performance measurement condition.

Patent landscape: what this claim set implies

Landscape structure around cyclodextrin solubilization

US 7,115,587 sits in the formulation IP cluster where key variables are:

• drug-cyclodextrin inclusion complexation
• pH control
• buffer selection and amount
• irritation reduction for parenteral use
• dose concentration constraints

The claim architecture mirrors common litigated formulation patterns: broad compositional hooks (claims 1–6) backed by narrower, numerically defined embodiments (claims 7–21) and then method-of-use (claims 22–24).

Where it likely overlaps with adjacent formulation patents

Even without enumerating other specific US family numbers here, the claim set indicates likely contention with:

• patents claiming aripiprazole inclusion complexes with cyclodextrins
• patents claiming injectable aripiprazole solutions with SBECD or HPBCD
• patents claiming tartaric-acid buffered parenteral systems at ~pH 4
• patents claiming IM injectability with reduced local irritation
• patents with quantified concentration and ratio windows for reproducible complex formation

Enforceability posture by claim type

Composition claims (1–6)

• Generally easier to map if the accused product uses the same ingredients and achieves inclusion complex status.
• “Substituted β-cyclodextrin” language can enlarge scope if the substituted derivative meets the claim’s definition and interpretation; claims 2 and 3 reduce this by limiting to SBECD/HPBCD.

Formulation claims with numeric ranges (7–15; 17–21)

• Strong for enforcement because they provide numeric limitations:
  • pH ranges (3.5–5; 4–4.6)
  • concentration bands (1.5–8 mg/mL aripiprazole; 100–200 mg/mL SBECD; 7–9 mg/mL tartaric acid)
  • weight ratios (10:1–100:1; 20:1–40:1; 2:1–10:1)

Performance/irritation claims (16; 20; 22–24)

• Adds functional language likely tied to experimental evaluation.
• Still enforceable when the accused product meets the objective formulation constraints and the irritation testing is aligned to the patent’s implied criteria.

Key Takeaways

• US 7,115,587 protects aripiprazole inclusion complexes with substituted beta-cyclodextrins, especially SBECD and HPBCD (claims 1–3; 2–3; 6).
• Product protection tightens from broad injectable formulation (claims 4–6) to pH-buffered aqueous systems at pH 3.5–5 with an acid buffer and base adjustment (claims 7–10), then to explicit weight ratios (claims 11–12).
• The patent’s enforcement core is the tight SBECD + tartaric acid + NaOH aqueous injectable formulation at pH 4–4.6 with explicit concentration bands (claims 17–18), reinforced by inclusion-complex requirements (claim 19) and IM administration without unacceptable irritation (claims 20–23).
• Method claims (claims 22–24) track the formulation definitions and add therapeutic and route framing around avoiding local irritation.

FAQs

1) What is the most commercially meaningful claim family in US 7,115,587?

Claims 17–21 because they define a concrete aqueous injectable composition (SBECD + tartaric acid + NaOH, pH 4–4.6) plus concentration ranges and IM performance limitations.

2) Does the patent require the inclusion complex to be formed, or can it be a simple mixture?

It requires the relationship as an inclusion complex in multiple places, especially claims 15 and 19 (and broadly in claims 1–3).

3) What pH window is most important for freedom-to-operate?

• Broad formulation window: pH 3.5 to 5 (claim 7).
• Tight exemplar window: pH 4 to 4.6 (claim 17).

4) Are SBECD and HPBCD the only cyclodextrins covered?

The broad concept is “substituted β-cyclodextrin” (claim 1), but several key claims limit explicitly to SBECD or HPBCD (claims 2, 6), and the narrow exemplar is SBECD (claims 3, 17–21).

5) Does the patent protect schizophrenia treatment specifically?

Yes. Claim 24 is a method of treating schizophrenia using the formulation defined in claim 5, framed to avoid undue irritation.

References

[1] United States Patent 7,115,587. Claims provided in prompt (claims 1-24).