Details for Patent: 9,511,066

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Summary for Patent: 9,511,066

Title:	Abuse-resistant controlled-release opioid dosage form
Abstract:	Abuse-resistant, controlled release opioid tablets are a combination containing an opioid antagonist such as naloxone at a level above that needed to suppress the euphoric effect of the opioid, if the combination were crushed to break the controlled release properties causing the opioid and opioid antagonist to be released as a immediate release product as a single dose. The controlled release nature of the table prevents the accumulation of orally effective amounts of opioid antagonist when taken normally. The opioid antagonist is contained in a controlled-release matrix and released, over time, with the opioid.
Inventor(s):	Frank S. Caruso, Huai-Hung Kao
Assignee:	Purdue Pharma LP
Application Number:	US15/159,465
Patent Claim Types: see list of patent claims	Use; Composition; Dosage form;

Scope and Claims Breakdown of U.S. Patent 9,511,066 (Oxycodone/Naloxone Abuse-Deterrent Controlled Release) and the U.S. Patent Landscape

U.S. Patent 9,511,066 is directed to preventing oral abuse of an oxycodone-containing, controlled-release oral product by incorporating naloxone in a specific dose/range and enforcing a controlled release relationship where most naloxone is released over 8 to 12 hours. Independent claim 1 is a method claim covering administration (providing) of the specified controlled-release formulation to prevent abuse, with dependent claims narrowing to dose ranges, release kinetics, tablet form, non-separability, and anti-crush/anti-withdrawal behavior.

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What does U.S. Patent 9,511,066 claim for abuse-deterrent oxycodone/naloxone?

Direct answer: Claim 1 covers a method of preventing oral abuse by providing a therapeutically effective amount of an oral controlled release oxycodone/naloxone composition with:

1. an oxycodone:naloxone ratio of 5:1 to 1:1, and
2. naloxone release such that at least 87.5% of naloxone is released over 8 to 12 hours (with additional dependent claims narrowing “approximate” release-rate relationships and functional outcomes when crushed vs intact).

Independent claim 1 element-by-element (claim construction anchors)

1. Method purpose: “preventing abuse of an oral opioid pharmaceutical composition”
   Abuse is further specified in dependent claims as crushing.

2. Act of “providing” a therapeutically effective amount
   This is a formulation-centric method of use claim. In enforcement, it typically requires that the accused product is administered/used as claimed (or that a label/instructions support the method).

3. Oral controlled release pharmaceutical composition containing:

   • oxycodone
   • naloxone
   • ratio constraint: oxycodone and naloxone present at 5:1 to 1:1

4. Controlled release timing/kinetics constraint:

   • at least 87.5% of naloxone released over 8–12 hours

Key dependent-claim scope controls

Below are the main scope “gates” that narrow infringement risk and define likely design-around options.

Dose/range dependent claims (oxycodone and naloxone amounts)

• Oxycodone amounts:
  • Claim 2: 10–160 mg
  • Claim 3: 10–80 mg
  • Claim 4: 10–40 mg
  • Claim 5: oxycodone 10 mg with naloxone 2–10 mg
  • Claim 6: oxycodone 20 mg with naloxone 5–20 mg
  • Claim 7: oxycodone 40 mg with naloxone 8–40 mg
  • Claim 8: oxycodone 80 mg with naloxone 16–80 mg
• Naloxone amounts:
  • Claim 9: 2–160 mg
  • Claim 10: 2–40 mg
  • Claim 11: 5–20 mg

Ratio dependent claims

• Claim 12: ratio 4:1 to 1:1 (narrower than Claim 1)

Salt/identity dependent claims

• Claim 13: oxycodone is oxycodone hydrochloride
• Claim 14: naloxone is a pharmaceutically acceptable salt

These can meaningfully affect design-around by switching salt form, but note that salts and polymorphs are often captured by “pharmaceutically acceptable salt” language.

Naloxone release-rate relationship dependent claims

These claims set relative release behaviors between naloxone and oxycodone, in addition to the “% released over 8–12 hours” metric.

• Claim 15: naloxone release rate is ~100% to ~25% of oxycodone release rate
• Claim 16: naloxone release rate is ~100% of oxycodone release rate
• Claim 17: >90% naloxone released over 10 hours
• Claim 18: oxycodone and naloxone released over >4 hours

Formulation architecture and physical/abuse behavior dependent claims

• Claim 19: controlled release matrix containing oxycodone and naloxone
• Claim 20: tablet
• Claim 21: naloxone not readily separable from oxycodone
• Claim 22: enough naloxone released to block opioid euphoric effect when crushed
• Claim 23: naloxone released as immediate release capable of inducing withdrawal when crushed
• Claim 24: naloxone released at a rate ineffective for inducing withdrawal when taken intact
• Claim 25: naloxone release does not block oxycodone when controlled release intact
• Claim 26–27: method prevents oral abuse; abuse comprises crushing
• Claim 28–30: an alternative dependent pathway specifying a particular combination with salt and matrix details

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How do claims 28–30 broaden or narrow the scope versus claim 1?

Direct answer: Claim 28 restates the core controlled-release/ratio/% release concept but tightens the identity and narrows naloxone to a specific mg range with a controlled release matrix limitation. Claim 30 adds a matrix material limitation (methacrylate copolymer).

Claim 28 (sub-claim architecture)

Claim 28 requires:

• oxycodone as oxycodone hydrochloride
• naloxone as a pharmaceutically acceptable salt
• naloxone amount: 2–40 mg
• ratio: 4:1 to 1:1
• controlled release matrix
• release: at least 87.5% naloxone released over 8–12 hours

This is narrower than Claim 1 due to:

• the naloxone mg cap (2–40 mg)
• the ratio narrower band (4:1 to 1:1)
• explicit oxycodone hydrochloride identity

Claim 29 (oxycodone discrete strengths)

Oxycodone present as 10, 20, 40, or 80 mg, matching common staged dose strengths for combination products.

Claim 30 (material limitation)

Matrix comprises a methacrylate copolymer.
This is a strong narrowing limitation that can be used for design-around (switching from methacrylate copolymer to a different controlled-release polymer system), but only for infringement of Claim 30 specifically. The independent and other dependent claims may still be asserted depending on whether the formulation falls under broader matrix language (Claim 19 says “controlled release matrix” without specifying methacrylate chemistry).

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What formulation “theory of protection” is embedded in these claims?

Direct answer: The patent’s protective concept is a controlled-release oxycodone/naloxone combination where naloxone remains sub-therapeutic with respect to withdrawal risk when intact, but becomes effectively immediate-release upon crushing, driven by (i) matrix entrapment/non-separability and (ii) release kinetics calibrated so that a high fraction of naloxone is released over the full 8–12 hour dosing window.

The claims also recite:

• “naloxone not readily separable”
• functional anti-crush thresholds (block euphoric effect; induce withdrawal in dependent individuals if crushed)
• maintained oxycodone action when intact

This indicates that enforcement is likely not only about mass balance and dissolution curves, but about the product’s performance in abuse scenarios (crushed vs intact), which can be tested in regulatory or litigation-grade studies.

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What is the independent claim coverage for “abuse” and “crushing”?

Direct answer: Claim 1 is not limited to crushing by the independent clause, but dependent claims 22, 23, 24, 26, and 27 explicitly tie the abuse prevention mechanism to crushing and withdrawal/euphoric effect outcomes.

Practical infringement map for “crush vs intact”

A formulation that releases most naloxone over 8–12 hours could satisfy the kinetic gate, but for the narrower functional dependent claims the accused product must also show:

• crushed: naloxone released at a rate effective to induce withdrawal or block euphoric effect
• intact: naloxone release ineffective for inducing withdrawal while oxycodone remains active

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What patents likely surround U.S. Patent 9,511,066 in the oxycodone/naloxone abuse-deterrent landscape?

This is a formulation-and-use patent family typically adjacent to:

• abuse-deterrent controlled-release oxycodone/naloxone product patents (matrix and release kinetics)
• tablet/solid dosage form abuse-deterrent approaches (non-separability, physical integrity)
• process and component patents (manufacturing methods enabling specific release behavior)

However, without the patent’s bibliographic data (assignee, priority, filing dates, and patent family members) and the Orange Book and litigation record for the corresponding FDA product, a definitive landscape mapping with exact patent numbers, expiration dates, and assignee attribution cannot be produced from the claim text alone.

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What parts of the claim set are most vulnerable to design-around?

Direct answer: The most design-around-sensitive limitations are the ones that are either numeric/quantified or material-specific.

Highest design-around leverage

1. Naloxone release kinetics gate:

   • “at least 87.5% released over 8–12 hours”
     Changing polymer type, diffusion pathways, or manufacturing parameters to reduce naloxone release fraction or shift the time profile could avoid literal infringement, depending on test methods.

2. Oxycodone:naloxone ratio gates:

   • 5:1 to 1:1 (Claim 1)
   • 4:1 to 1:1 (Claim 12 and Claim 28)
     Reformulating outside these ratios is a straightforward route to non-infringement of those claims.

3. Matrix polymer chemistry limitation in Claim 30:

   • “methacrylate copolymer”
     Switching to a different controlled-release matrix can avoid Claim 30 specifically, though it may still fall within the broader “controlled release matrix” language of Claim 19.

4. Identity of salt forms:

   • oxycodone hydrochloride (Claim 13)
   • naloxone salt (Claim 14)
     If an asserted claim requires oxycodone hydrochloride explicitly, switching to a different oxycodone salt form could matter.

Lower leverage (still relevant but less “binary”)

• “not readily separable” and the crush/withdrawal functional language can be contested on test methods, but they often track measurable physical attributes and performance outcomes.

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How would an accused generic/biosimilar-style challenge likely be framed?

Direct answer: The likely dispute is not “what oxycodone is,” but whether the accused product meets the numeric release fraction and time window plus ratio constraints, and whether functional crush/inact behavior maps to dependent-claim requirements.

Common litigation focal points:

• dissolution testing method equivalence for the “% released over 8–12 hours” limitation
• evidence that naloxone is “not readily separable”
• whether naloxone release rate relationships (claims 15–17) match the accused product’s profile
• whether crushing causes naloxone to act as “immediate release capable of inducing withdrawal”

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What does this claim set imply for freedom-to-operate (FTO) strategy?

Direct answer: A product must simultaneously avoid:

• the ratio bands
• the naloxone release fraction and timing metrics
• and, for certain dependent claims, the abuse-behavior performance profile (crushed vs intact)

FTO gating checklist aligned to claim language

• Composition: does it contain oxycodone + naloxone in the required ratio?
• Salt forms: does it use oxycodone hydrochloride and a naloxone salt (for salt-dependent claims)?
• Release profile: does it achieve ≥87.5% naloxone release over 8–12 hours?
• Matrix: is it a controlled release matrix, and is it methacrylate copolymer (Claim 30)?
• Physical attribute: is naloxone “not readily separable”?
• Abuse scenario performance: does crushing trigger the specified naloxone immediate-release/withdrawal effect while intact dosing prevents it?

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Key Takeaways

• U.S. Patent 9,511,066 is a method-of-prevention claim tied to an oral controlled-release oxycodone/naloxone formulation with specific ratios and naloxone release kinetics.
• The central numeric gate is: ≥87.5% naloxone released over 8–12 hours, coupled with oxycodone:naloxone ratio of 5:1 to 1:1 (and narrower 4:1 to 1:1 in some dependents).
• Dependent claims add high-value narrowing on oxycodone/naloxone dose ranges, salt identities, tablet form, controlled-release matrix structure, and functional outcomes tied to crushing vs intact ingestion.
• Claim 30 is the clearest material-specific bottleneck: a methacrylate copolymer matrix.
• Design-around risk concentrates on dissolution release fraction/timing and ratio compliance, with additional exposure on non-separability and crush-triggered naloxone behavior.

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FAQs

1) Does U.S. Patent 9,511,066 cover only crushed-abuse scenarios?
No. Claim 1 covers preventing oral abuse, and dependent claims specify crushing and corresponding functional outcomes.

2) What is the most important numeric limitation for infringement risk?
The requirement that at least 87.5% of naloxone is released over 8–12 hours (Claims 1 and 28).

3) If a formulation changes the naloxone amount but keeps the same ratio, is it still in-scope?
It may still be in-scope for Claim 1 if the ratio remains within 5:1 to 1:1 and the release kinetics are met. Other dependent claims impose specific mg ranges.

4) Can switching from methacrylate copolymer avoid all coverage?
It can avoid Claim 30 specifically, but it may not avoid broader “controlled release matrix” coverage in other claims.

5) Are salt-form changes a meaningful design-around route?
They can be for salt-dependent claims requiring oxycodone hydrochloride (Claim 13) or specifying naloxone as a pharmaceutically acceptable salt (Claim 14), but Claim 1 is not explicitly limited to those identities in your provided claim set.

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References

1. U.S. Patent 9,511,066. (Claim text provided in prompt).

Drugs Protected by US Patent 9,511,066

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate

International Family Members for US Patent 9,511,066

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	493130
Australia	2002305559
Australia	2008202967
Canada	2446550
China	1525851