Details for Patent: 9,084,729

Summary for Patent: 9,084,729

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 an immediate release product as a single dose. The controlled release nature of the tablet 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:	US14/067,821
Patent Claim Types: see list of patent claims	Use; Composition; Dosage form;

United States Patent 9,084,729 (Oxycodone/Naloxone Oral Controlled-Release): Claim Scope, Design-Around Space, and US Patent Estate

US Patent 9,084,729 claims an oral controlled-release oxycodone/naloxone dosage form with defined oxycodone:naloxone ratios and a release pattern in which substantially all naloxone is released over 8-12 hours. The claims also cover specific dose ranges, salt forms, tablet form, and functional release behavior tied to abuse-deterrence upon crushing versus maintained opioid efficacy when intact. Independent claim scope is broad on “controlled release” and moderately constrained by (i) ratio (generally 5:1 to 1:1 or 4:1 to 1:1), (ii) naloxone release window (substantially all over 8-12 hours), and (iii) release-rate relationships tied to oxycodone. Dependent claims carve out dosage strengths (including 10-80 mg and up to 160 mg variants) and release kinetics (4-hour profile fractions; >90% over 10 hours).

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What is claimed in US Patent 9,084,729 for oral controlled release oxycodone/naloxone?

Short answer: The patent is directed to an oral controlled-release oxycodone/naloxone composition where naloxone is released substantially completely over 8-12 hours, with oxycodone:naloxone ratios spanning 5:1 to 1:1 (and in a second claim set, 4:1 to 1:1), plus functional limitations that address crushing behavior and intact oral dosing efficacy.

Independent claim structure

Claim 1 (core composition):

• Oral controlled-release pharmaceutical composition comprising:
  • oxycodone and naloxone
  • oxycodone:naloxone ratio 5:1 to 1:1
  • controlled release such that substantially all naloxone is released over 8-12 hours

This is the central entry barrier for infringement. Any US “oxycodone/naloxone ER” product must map to:

1. both actives in one composition,
2. controlled-release functionality,
3. the ratio range, and
4. the naloxone release timing window.

Claim 22 (method of treating pain):

• Oral administration of the claim 1 composition for pain.

Claim 37 (parallel composition variant with oxycodone hydrochloride and naloxone salt):

• Oral controlled-release composition comprising:
  • oxycodone hydrochloride
  • 2-40 mg of a pharmaceutically acceptable salt of naloxone
  • ratio 4:1 to 1:1
  • substantially all naloxone salt released over 8-12 hours

Key implications of the two independent anchors:

• Claim 1 requires “oxycodone” generically (not explicitly as HCl in the independent claim).
• Claim 37 expressly narrows composition chemistry to oxycodone hydrochloride and naloxone salt, while also constraining the naloxone amount to 2-40 mg.

Release timing and kinetics: how the claims operationalize “controlled release”

The independent claims use “substantially all” over 8-12 hours. Dependent claims then add measurable kinetics, including:

• Claim 30: naloxone release rate ~100% to 25% of oxycodone release rate
• Claim 32: 60-70% of oxycodone released over 4 hours
• Claim 33: 60-70% of naloxone released over 4 hours
• Claim 34: >90% of oxycodone released over 10 hours
• Claim 36: oxycodone and naloxone released over 8-12 hours (explicit repetition of the independent timing concept)
• Claim 42: 60-70% of both actives released over 4 hours, and >90% oxycodone released over 10 hours

These dependent claims increase the ability to target specific dissolution profiles in litigation and enable focused design-arounds that alter the fraction released at 4 hours or push naloxone release outside the 8-12 hour window.

Ratio scope: 5:1 to 1:1 and 4:1 to 1:1

• Claim 1: ratio 5:1 to 1:1
• Claim 21: narrows to 4:1 to 1:1
• Claim 37: ratio 4:1 to 1:1

So the ratio limitations are not “either/or.” They form a layered fence: products that fall between 4:1 and 1:1 are within multiple claim families; products that fall between 5:1 and just above 4:1 may still fall within Claim 1 but not Claim 21/37.

Dose ranges: broad but discretely claimed

The claims include multiple dose and strength ranges that cover common ER strength bands and higher-dose variants.

• Claim 2: oxycodone 10-80 mg
• Claim 3: oxycodone 10-40 mg
• Claims 4-7: specific exemplary pairings for oxycodone (10/20/40/80 mg) with naloxone sub-ranges
• Claim 8: naloxone 5-40 mg
• Claims 11-12: naloxone at least 10 mg and at least 20 mg
• Claim 23: oxycodone up to 10-160 mg
• Claim 24: naloxone up to 5-160 mg
• Claim 26-29: naloxone ranges 2-160 mg and 2-40 mg for subset claims
• Claim 37: naloxone salt in the range 2-40 mg

These create a multi-strength claim landscape. A generic or licensed entrant can’t assume a single strength escapes by range; they must map both actives across the full contemplated dose portfolio.

Form and physical characteristics: salt and tablet limitations

• Claim 13: oxycodone is oxycodone hydrochloride
• Claim 15: naloxone is a pharmaceutically acceptable salt
• Claim 16: composition is a tablet
• Claim 20: naloxone is not readily separable from oxycodone
• Claim 17-19: functional abuse-deterrence via crushing vs intact ingestion

Functional abuse-deterrence limitations: “crushed” vs intact release behavior

These claims are designed to read on formulations intended to deter extraction/abuse.

• Claim 17: sufficient naloxone is released to block opioid euphoric effect when crushed
• Claim 18: naloxone released as immediate release capable of inducing withdrawal in dependent individuals if crushed
• Claim 19: naloxone released at a rate ineffective for inducing withdrawal when taken orally in intact form
• Claim 25: release does not block action of oxycodone when controlled-release properties are intact

This is a two-part functional test:

• in the “broken” condition (crushed), naloxone release is fast enough to trigger deterrent effects;
• in the “intact” condition, naloxone release is slow enough that the opioid effect remains.

For infringement and validity challenges, these limitations can drive expert evaluation of:

• mechanical stress-induced release,
• dispersion/solubilization kinetics after crushing,
• and whether naloxone acts as an “instant” blocker vs a slow-release antagonist.

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Which elements of claim 1 are most likely to drive infringement or validity?

Short answer: The highest-impact claim elements are (1) the oxy:naloxone ratio limits, (2) “substantially all naloxone released over 8-12 hours,” and (3) the functional crushing vs intact release limitations.

Claim 1 elements mapped to product attributes

1. Oral controlled-release dosage form

   • Typically ER matrix/coating, not IR bolus.

2. Oxycodone + naloxone in one composition

   • Combination drug, not co-packaging.

3. Oxycodone:naloxone ratio 5:1 to 1:1

   • Dose-strength matrix must align.

4. Naloxone release: substantially all over 8-12 hours

   • Dissolution profile and in vitro release are central. “Substantially all” invites a quantitative interpretation; dependent claims partially operationalize this via >90% oxycodone and 60-70% at 4 hours.

5. Crushing behavior limitations (dependent claims)

   • Claim 17-19 narrow infringement if the product doesn’t exhibit the same deterrent behavior upon crushing.

Dependent claims as “litigation dials”

Dependent claims provide measurable targets:

• 60-70% release at 4 hours for oxycodone and/or naloxone,

• 90% oxycodone by 10 hours,

• naloxone release rate ~25% to 100% of oxycodone release rate.

These enable an infringement theory that does not need the full functional crushing record if the dissolution kinetics are mapped and the ratio/timing are met.

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How strong is the patent estate around US 9,084,729 for generic or licensing entry?

Short answer: Based on claim breadth, the patent is strong in capturing a wide formulation space that matches ER oxycodone/naloxone abuse-deterrence designs with similar timing and ratio. Entry risk rises when a competitor’s formulation uses comparable ER release of naloxone and includes functional behavior intended to deter crushing.

Infringement risk factors for a generic or new entrant

A product faces lower risk only if it can avoid one of the key constraints:

• ratio outside 5:1 to 1:1 (or outside the stricter 4:1 to 1:1),
• naloxone release not “substantially all over 8-12 hours,”
• or controlled-release behavior that fails the functional crushing deterrence or fails the intact efficacy requirement (for claims that incorporate those features).

Design-around leverage points visible from the claim text

1. Shift naloxone release outside 8-12 hours

   • If naloxone is substantially not fully released in that window, Claim 1 and Claim 37 are vulnerable.

2. Alter naloxone:oxycodone ratio

   • Moving below the upper end or above the lower end can remove coverage.

3. Decouple naloxone and oxycodone release rates

   • Claim 30 and Claims 32-33-42 tie to relative or parallel release fractions.

4. Change mechanical robustness and “not readily separable” profile

   • Claim 20 can be a factor if the formulation allows separation.

5. Adjust abuse-deterrence mechanism

   • If crushing does not trigger immediate release sufficient to block euphoric effect or induce withdrawal, dependent claims 17-19 may not be met.

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What patent claims cover oxycodone/naloxone release kinetics (4-hour and 10-hour profiles) and why does it matter?

Short answer: The claims include quantitative release benchmarks at 4 hours and 10 hours, which are the most litigation-ready features for dissolution testing.

Kinetic-dependent claim set (extract)

• Claim 32: 60-70% of oxycodone released over 4 hours
• Claim 33: 60-70% of naloxone released over 4 hours
• Claim 34: >90% of oxycodone released over 10 hours
• Claim 36: release period >4 hours; also 8-12 hours
• Claim 42: 60-70% of both actives over 4 hours; >90% oxycodone over 10 hours
• Claim 30: naloxone release rate ~100% to 25% of oxycodone release rate
• Claim 31: naloxone release rate ~100% of oxycodone release rate

Practical consequence

Even if a competitor matches ratio and naloxone release “over 8-12 hours,” missing the 4-hour fraction or the 10-hour >90% oxycodone benchmark can reduce the number of dependent claims implicated.

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What formulation variants are included (salt form, tablet form, non-separability) and how do they narrow coverage?

Short answer: Claim 1 is broad on active identity; dependent claims add salt/form-factor constraints and non-separability. Claim 37 directly locks oxycododone HCl and naloxone salt.

Chemistry and dosage form limitations

• oxycodone hydrochloride: Claim 13
• naloxone pharmaceutically acceptable salt: Claims 14-15
• tablet: Claim 16
• not readily separable naloxone from oxycodone: Claim 20
• naloxone salt amount range in Claim 37: 2-40 mg

Why these matter for design-around

A product that is:

• not a tablet (or does not meet the claim construction for “tablet”), or
• uses different salt forms or different active forms that avoid “oxycodone hydrochloride” and/or “pharmaceutically acceptable salt” mapping, could attempt to avoid specific dependent claims while still risking coverage under Claim 1 if the core ratio and release-window constraints are met.

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What are the method-of-use implications of claim 22 for pain treatment?

Short answer: Claim 22 is a straightforward method-of-use claim: oral administration of the claim 1 composition to treat pain. Method-of-use coverage becomes relevant when a product is sold for pain treatment and the composition matches the formulation claims.

Infringement trigger

• If a marketed product practices the underlying composition (Claim 1), the act of prescribing/dispensing for pain can implicate Claim 22.

Litigation relevance

Method-of-use claims often become leverage in enforcement and licensing because they can be asserted even where product-specific evidence is indirect, but they generally depend on proving composition infringement.

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What is the comparative claim scope versus claim 37’s oxycodone HCl + naloxone salt frame?

Short answer: Claim 37 is narrower in chemistry and in naloxone amount (2-40 mg) but overlaps on the core ER release window (substantially all over 8-12 hours) and the ratio (4:1 to 1:1).

Overlap matrix

• Both sets cover oral controlled-release oxycodone/naloxone and 8-12 hour naloxone completion.
• Both set ratio constraints that share the 4:1 to 1:1 subrange.
• Claim 37 adds:
  • oxycodone hydrochloride,
  • naloxone as a pharmaceutically acceptable salt,
  • and naloxone dose cap at 2-40 mg.

Consequence for entrants

A formulation that uses other oxycodone forms or naloxone presentations may reduce claim 37 exposure but still fall under claim 1 if it meets claim 1’s broader active-identity and ratio/release constraints.

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What generic entry risks exist for US oral controlled-release oxycodone/naloxone products relative to US 9,084,729?

Short answer: Risk concentrates on products with (i) ER naloxone release completing over 8-12 hours, (ii) oxycodone:naloxone ratios within 5:1 to 1:1 (or 4:1 to 1:1), and (iii) release kinetics consistent with the dependent benchmarks. Crushing-deterrence designs that release naloxone as immediate release upon crushing increase dependent claim exposure.

Risk ladder by claim tier

• Lowest risk: if naloxone is not substantially released over 8-12 hours.
• Medium risk: if naloxone release timing aligns, but ratio is outside the claimed range.
• High risk: if timing and ratio align, and the dissolution profile matches 4-hour and 10-hour dependent benchmarks.
• Highest risk: if crushing creates immediate-release naloxone sufficient to block euphoric effect/induce withdrawal, and intact dosing preserves oxycodone effect.

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Key Takeaways

• US 9,084,729 claims an oral controlled-release oxycodone/naloxone composition with defined oxy:naloxone ratios and a core requirement that substantially all naloxone is released over 8-12 hours.
• The independent claim is broad on product class but constrained on ratio and naloxone ER completion timing; dependent claims add measurable kinetic fences (notably 60-70% at 4 hours and >90% oxycodone by 10 hours).
• Dependent claims add abuse-deterrence behavior tied to crushing vs intact ingestion and can materially raise enforcement leverage where competitors use similar mechanical-break triggered naloxone release.
• Claim 37 overlaps the same ER release concept but narrows chemistry to oxycodone hydrochloride and naloxone salt, with naloxone dose capped at 2-40 mg and a tighter ratio band (4:1 to 1:1).

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FAQs

1. What does “substantially all naloxone released over 8-12 hours” mean for a competitor’s dissolution profile?
2. How can a formulation avoid claim 1 while still matching approved oxycodone/naloxone dosing strengths?
3. Do the 4-hour and 10-hour dependent release claims matter more than the independent “8-12 hour” window?
4. When do the crushing-triggered withdrawal and euphoric-effect blocking functional limitations become central in infringement analysis?
5. How does Claim 37’s naloxone salt and oxycodone hydrochloride limitation change freedom-to-operate compared with Claim 1?

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References

1. United States Patent 9,084,729. (Claims and claim text as provided in the prompt).

Drugs Protected by US Patent 9,084,729

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 9,084,729

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