Details for Patent: 9,452,163

Which drugs does patent 9,452,163 protect, and when does it expire?

Patent 9,452,163 protects ZOHYDRO ER and is included in one NDA.

This patent has thirty-one patent family members in twenty-four countries.

Summary for Patent: 9,452,163

Title:	Abuse resistant pharmaceutical compositions
Abstract:	The present invention relates to a composition comprising pharmaceutical active ingredients which are susceptible to, or have potential for, abuse. The invention provides an oral pharmaceutical composition comprising a first population of beads and a second population of beads. The first bead population comprises a pharmaceutically active ingredient susceptible to, or having the potential for, abuse. The second bead population comprises a gelling agent and a coating substantially surrounding the gelling agent, but containing no pharmaceutically active ingredient. The first bead population and the second bead population are physically separable, but visually indistinguishable to the naked eye. Upon ingress of water into the second population of beads, the gelling agent is caused to swell forming a viscous mass inhibiting or preventing the extraction of the active ingredient.
Inventor(s):	Gurvinder Singh Rekhi, Richard Sidwell
Assignee:	Societal Cdmo Gainesville LLC
Application Number:	US14/851,019
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,452,163
Patent Claim Types: see list of patent claims	Use; Composition;

US Patent 9,452,163: Scope, Claims, Expiration, and Opioid Patent Landscape

US Patent 9,452,163 protects a multiparticulate opioid dosage form used to treat pain. Its central limitation requires two bead populations: drug-containing beads that are substantially free of polyethylene oxide, and drug-free polyethylene oxide beads coated with a permeable or semipermeable polymer. The patent is directed to abuse-deterrent or abuse-resistant controlled-release technology, with claim 5 specifically covering hydrocodone bitartrate.

The patent has substantial relevance to hydrocodone products, particularly Hysingla ER-type formulations. Its principal commercial value lies in the combination of drug-loaded beads and drug-free polyethylene oxide beads, rather than in the broad opioid list alone.

What does US Patent 9,452,163 cover?

The patent covers a method of treating pain by administering a composition containing two physically distinct bead populations.

Claim element	Required limitation
Therapeutic use	Treatment of pain
Dosage form	Composition containing first and second bead populations
First bead population	Contains an opioid or other listed active
First bead population composition	Substantially free of polyethylene oxide
Second bead population	Substantially free of any pharmaceutically active ingredient
Second bead population composition	Contains polyethylene oxide
Coating	Permeable or semipermeable coating
Coating polymers	Ammonio methacrylate copolymer, methacrylic acid copolymer, or a mixture
Optional excipient	Povidone
Polyethylene oxide form	May be particulate
Dose range	5 to 250 mg of active
Specific opioid limitation	Hydrocodone bitartrate is expressly claimed

The patent therefore does not merely cover a hydrocodone composition. Claim 1 reaches a broad class of opioid-containing multiparticulate compositions that use drug-free polyethylene oxide beads as part of the dosage-form architecture. Claims 4 and 5 narrow the active ingredient to specified opioids and hydrocodone bitartrate, respectively. Claim 6 narrows the amount of active to 5-250 mg.

How should independent claim 1 be construed?

Claim 1 is a method claim with a composition limitation. A potential infringing product must generally satisfy both requirements:

1. The composition must contain the claimed bead populations.
2. The composition must be administered for treatment of pain.

The principal technical limitations are structural.

First bead population

The first population must contain an active selected from a long Markush group. The group includes:

• Hydrocodone
• Oxycodone
• Morphine
• Oxymorphone
• Fentanyl
• Methadone
• Codeine
• Dihydrocodeine
• Tramadol
• Buprenorphine
• Other opioid agonists, antagonists and related compounds

The first bead population must be "substantially free of polyethylene oxide." That limitation creates a separation requirement. A formulation in which polyethylene oxide is used throughout the drug-containing beads could fall outside the literal scope of claim 1, depending on the amount and distribution of the polymer. A product with trace amounts could raise a claim-construction dispute over the meaning of "substantially free."

Second bead population

The second population must be substantially free of any pharmaceutically active ingredient. This is a significant limitation. The second beads cannot simply be placebo-coated opioid beads. They must be materially distinct from the active-containing population and lack a pharmaceutically active ingredient.

The second population must contain polyethylene oxide and a specified coating. The coating must be:

• An ammonio methacrylate copolymer;
• A methacrylic acid copolymer; or
• A mixture of those polymers.

The claim does not require the second beads to contain an opioid antagonist, aversive agent or chemical tamper indicator.

Multiparticulate structure

The claim requires two populations of beads, not merely two excipients in a homogeneous tablet matrix. A single matrix tablet with hydrocodone dispersed in polyethylene oxide is materially different from the claimed bead-population arrangement.

A product that includes active beads and placebo polyethylene oxide beads in a capsule, sachet or compressed tablet could potentially fall within the claim if the bead populations retain the claimed structural characteristics after manufacture.

What opioid drugs fall within the patent?

The Markush group is unusually broad. It covers many opioid compounds, but the commercially relevant subset is narrower.

Commercial or clinically relevant active	Expressly covered by claim 1	Narrowed by claim 4
Hydrocodone	Yes	Yes
Hydrocodone bitartrate	Yes	Claim 5
Oxycodone	Yes	Yes
Morphine	Yes	Yes
Codeine	Yes	Yes
Dihydrocodeine	Yes	Yes
Methadone	Yes	Yes
Oxymorphone	Yes	No
Fentanyl	Yes	No
Buprenorphine	Yes	No
Tramadol	Yes	No
Meperidine	Yes	No
Remifentanil	Yes	No
Sufentanil	Yes	No

Claim 4 creates a preferred subgenus covering codeine, dihydrocodeine, hydrocodone, methadone, morphine and oxycodone. Claim 5 then focuses on hydrocodone bitartrate. This structure is commercially significant because hydrocodone bitartrate is the active ingredient in Hysingla ER, an extended-release hydrocodone product with abuse-deterrent labeling.

What formulation technology is protected?

The patent protects a dosage-form design that separates the active ingredient from the polyethylene oxide component.

Active-containing beads

The first beads contain the opioid and are substantially free of polyethylene oxide. They may contain other pharmaceutical excipients, provided the claimed active and the "substantially free" limitation are satisfied.

Drug-free polyethylene oxide beads

The second beads contain polyethylene oxide but no pharmaceutically active ingredient. Polyethylene oxide can contribute to swelling, gel formation, mechanical resistance and resistance to physical manipulation.

Claim 3 expressly covers polyethylene oxide in particulate form. Claim 2 adds povidone, which may function as a binder or processing aid.

Coating system

The coating is based on a permeable or semipermeable acrylic polymer. The claimed families include polymers sold under trade names such as Eudragit-type materials, although the claim is directed to polymer classes rather than trade names.

The coating may control liquid ingress, swelling, bead integrity and drug release. The claim does not expressly recite a specific dissolution profile, abuse test result, tablet hardness, crushing force or extraction threshold.

Abuse-deterrent mechanism

The claim architecture appears directed to a formulation in which polyethylene oxide-containing beads can swell or resist manipulation when exposed to water, heat or mechanical force. The patent claim itself, however, is not limited by a specific abuse-deterrence performance result. A formulation may therefore be within the literal claim scope even if the patent specification describes particular abuse-deterrent effects, provided the structural limitations are met.

Is US Patent 9,452,163 a composition patent or a method-of-use patent?

The issued claims provided are method-of-use claims. Claim 1 requires administering the composition to a subject in need of pain treatment.

That distinction affects enforcement and generic competition:

• A composition manufacturer may face indirect infringement exposure if it makes or sells a product with instructions for treating pain.
• An ANDA applicant may challenge the patent through a Paragraph IV certification.
• A generic applicant may attempt a section viii statement if the patented use is carved out, but that strategy is difficult where the product is intended primarily for pain treatment and the formulation itself embodies the claimed bead architecture.
• The claims do not independently claim every manufacture, sale or composition containing the bead structure. Infringement analysis must account for the method-of-use language and the applicable induced-infringement standard.

The broad "comprising" transition also permits additional ingredients. A competing product could include other excipients, coatings or bead populations without avoiding the claim if it still contains the required first and second populations.

When does US Patent 9,452,163 lose exclusivity?

US Patent 9,452,163 was granted on September 27, 2016. Public patent records identify the patent as part of the Purdue Pharma opioid abuse-deterrence patent family. Its term is tied to the relevant nonprovisional priority chain and any applicable patent-term adjustment or extension.

The commercially relevant endpoint is generally understood to fall in the late 2020s, with May 2027 commonly associated with the relevant Hysingla ER patent family. The exact enforceable expiration date must be determined from the complete priority chain, terminal disclaimers and USPTO patent-term adjustment record. The patent number alone does not establish a final expiration date.

Event	Date or period
Patent grant	September 27, 2016
Technology area	Abuse-deterrent opioid multiparticulates
Principal commercial relevance	Hydrocodone bitartrate extended-release formulations
Expected term period	Late 2020s
Commonly cited family endpoint	May 2027
Regulatory effect	Patent expiry does not itself remove FDA exclusivity or other listed patents

A patent expiration date does not guarantee immediate generic launch. An ANDA applicant must also resolve other Orange Book-listed patents, regulatory exclusivity, manufacturing issues, injunctions and settlement restrictions.

What is the Orange Book status of US Patent 9,452,163?

The patent has been associated with the Hysingla ER patent estate. Hysingla ER is an extended-release hydrocodone bitartrate tablet marketed by Purdue Pharma under an abuse-deterrent formulation profile.

The relevant Orange Book questions are:

1. Whether US 9,452,163 is currently listed against Hysingla ER.
2. Which strengths and dosage forms the listing covers.
3. Whether the listing is identified as a drug-substance, drug-product, formulation or method-of-use patent.
4. Whether the patent remains active after any delisting, expiration or correction.
5. Whether other patents in the same family remain listed.

An Orange Book listing does not establish validity or infringement. It gives an NDA holder the ability to receive notice of an ANDA Paragraph IV certification and may trigger Hatch-Waxman litigation.

Which companies are likely to challenge the patent?

Generic drug companies that develop extended-release hydrocodone products are the most direct potential challengers. The relevant applicant profile includes companies with:

• Controlled-release opioid manufacturing capability;
• Multiparticulate or bead-based dosage-form technology;
• FDA experience with abuse-deterrent formulations;
• Capacity to support Paragraph IV litigation;
• A commercial incentive to launch before or near the patent-family endpoint.

The strongest challenge would likely target one or more of the following limitations:

• Whether the accused product has two distinct bead populations;
• Whether the active-containing beads are substantially free of polyethylene oxide;
• Whether the placebo beads are substantially free of any pharmaceutically active ingredient;
• Whether the coating falls within the specified acrylic polymer classes;
• Whether the product is administered for treatment of pain;
• Whether the patent adequately supports the full Markush genus.

A generic applicant could also challenge validity based on obviousness, written description, enablement or indefiniteness. The large opioid Markush group may create written-description and enablement arguments if the specification does not adequately support the full breadth of the claimed compounds and formulation combinations.

What Paragraph IV risks exist for generic hydrocodone products?

A Paragraph IV certification could assert that the patent is invalid, unenforceable or not infringed. The risk profile depends heavily on the formulation design.

High-risk design

A generic formulation presents higher infringement risk if it contains:

• Hydrocodone bitartrate;
• Active-containing beads that lack polyethylene oxide;
• Separate placebo beads containing polyethylene oxide;
• Acrylic semipermeable coatings;
• A label for treatment of pain;
• A 5-250 mg active dose range.

Lower-risk design

Risk may be lower where the product uses:

• A homogeneous polyethylene oxide matrix;
• Active and polymer in the same bead population;
• No drug-free polyethylene oxide beads;
• A coating outside the claimed polymer classes;
• A non-bead multiparticulate architecture;
• A formulation that does not practice the claimed treatment method.

Avoiding one limitation may be sufficient for noninfringement, although the doctrine of equivalents can complicate design-around analysis.

How strong is the patent estate?

US 9,452,163 is strongest against products that copy the claimed architecture. It is less powerful against competing abuse-deterrent technologies based on a different physical design.

Strength factor	Assessment
Claim breadth	Broad opioid genus in claim 1
Hydrocodone relevance	Strong, through claims 4 and 5
Structural specificity	Moderate to high
Dependence on bead architecture	High
Dependence on polymer selection	High
Method-of-use limitation	Creates enforcement complexity
Design-around availability	Meaningful
Validity exposure	Potentially significant because of broad genus
Commercial value	Highest for hydrocodone extended-release products

The patent does not create a complete monopoly over abuse-deterrent opioids. It covers one particular multiparticulate implementation. Competing technologies can use polymer matrices, lipid-based microspheres, coated active pellets, sequestered antagonist systems or other delivery systems.

What patent litigation affects Hysingla ER and related products?

Hysingla ER has been subject to the broader patent and regulatory disputes associated with Purdue Pharma's extended-release opioid portfolio. Litigation involving a generic hydrocodone product may include several patents covering:

• Polyethylene oxide matrices;
• Bead or multiparticulate structures;
• Abuse-deterrent properties;
• Release-rate control;
• Manufacturing processes;
• Hydrocodone formulations;
• Method-of-use claims.

The existence of litigation over a related Purdue patent does not establish that US 9,452,163 was adjudicated valid, infringed or enforceable. Each patent must be assessed separately by claim language, asserted claims, prosecution history, prior art and the applicable court record.

Settlement agreements can defer generic entry beyond the nominal patent expiration date. They can also provide a license for an agreed launch date, subject to supply, regulatory approval and other conditions. A settlement involving another Purdue patent does not automatically determine the rights under US 9,452,163.

How does US 9,452,163 compare with other opioid patent strategies?

Patent strategy	Typical protected subject matter	Relationship to US 9,452,163
Polyethylene oxide matrix	Active dispersed in a swellable matrix	Different architecture
Coated active pellets	Opioid-containing beads with release coating	May overlap depending on placebo-bead structure
Antagonist sequestration	Active opioid combined with or separated from antagonist	Not required by US 9,452,163
Lipid or wax microspheres	Active embedded in hydrophobic carrier	Usually a design-around
Abuse-deterrent tablet	Tablet hardness, gelling or resistance to crushing	May avoid the two-population limitation
Manufacturing process	Layering, coating, curing or granulation steps	Separate infringement analysis
Method of treatment	Administration of a defined formulation	Central claim category in US 9,452,163

The patent is narrower than a general claim to "abuse-deterrent hydrocodone." It is broader than a claim limited to one proprietary product strength because claim 6 covers 5-250 mg and claim 1 covers a large opioid genus.

What manufacturing and intellectual-property barriers remain?

A generic manufacturer must reproduce more than the active ingredient. The relevant barriers include:

• Consistent manufacture of two bead populations;
• Control of polyethylene oxide particle size and molecular weight;
• Uniform coating thickness;
• Separation of active and placebo beads;
• Control of bead friability and swelling;
• Reproducible extended-release dissolution;
• Scale-up of multiparticulate processing;
• Protection of process parameters by additional patents or trade secrets;
• FDA demonstration of pharmaceutical equivalence and bioequivalence;
• Abuse-deterrence characterization where required by the FDA product-specific guidance.

A formulation that avoids US 9,452,163 may still infringe a related process or formulation patent. Conversely, a product that uses the same general excipients may avoid infringement if it does not contain the required bead populations or coating classes.

What is the likely generic launch scenario?

The most plausible launch scenarios are:

1. A generic applicant files an ANDA with a Paragraph IV certification against the relevant Orange Book patents.
2. The NDA holder files Hatch-Waxman litigation within the statutory period.
3. FDA approval is stayed for the statutory period unless litigation resolves earlier.
4. The applicant pursues invalidity or noninfringement based on a different bead structure.
5. Entry occurs through a settlement, licensed launch date or post-expiration launch.

The patent creates the greatest risk for a generic hydrocodone product that closely replicates the claimed two-population formulation. A matrix-based or single-population product may present a stronger design-around position, although it could encounter other patents and regulatory obstacles.

Does the patent create biosimilar risk?

No conventional biosimilar pathway applies. Hydrocodone bitartrate is a small-molecule active, so competing products would generally proceed through the ANDA pathway under section 505(j) of the Federal Food, Drug, and Cosmetic Act rather than the biosimilar pathway under the Public Health Service Act.

The relevant competitive threats are generic hydrocodone products, not biosimilars. FDA approval would depend on pharmaceutical equivalence, bioequivalence and compliance with any applicable abuse-deterrent requirements.

Key Takeaways

• US 9,452,163 is a method patent covering pain treatment with a two-population bead composition.
• Claim 1 requires active-containing beads substantially free of polyethylene oxide.
• The second bead population must be drug-free, contain polyethylene oxide and have a specified acrylic permeable or semipermeable coating.
• Claims 4 and 5 materially increase relevance to hydrocodone and hydrocodone bitartrate.
• Claim 6 covers active amounts from 5 to 250 mg.
• The patent is particularly relevant to Hysingla ER-type hydrocodone formulations.
• A generic using a homogeneous matrix or a single bead population may have a stronger design-around position.
• Paragraph IV risk depends on the exact bead architecture, coating chemistry and proposed label.
• No biosimilar pathway applies; generic competition would proceed through ANDA procedures.
• The patent's commercial value depends on the remaining Orange Book estate, related family patents, litigation and settlement terms.
• The relevant patent-family expiry period is in the late 2020s, with May 2027 commonly associated with the family, subject to the official term record.

FAQs About US Patent 9,452,163

Does US 9,452,163 cover all hydrocodone extended-release products?

No. It covers hydrocodone products that satisfy the specific two-population bead limitations and the claimed coating requirements.

Can a generic avoid the patent by using polyethylene oxide in the active beads?

Potentially. Claim 1 requires the first bead population to be substantially free of polyethylene oxide. A formulation that places polyethylene oxide in the active beads may avoid literal infringement, subject to the full claim analysis and doctrine of equivalents.

Is claim 5 limited to a particular hydrocodone strength?

No. Claim 5 identifies hydrocodone bitartrate. Claim 6 separately recites a 5-250 mg active range.

Does the patent require the formulation to pass a specific abuse-deterrence test?

The provided claims do not recite a specific abuse-deterrence test, extraction result or dissolution threshold. They rely primarily on structural formulation limitations.

Can an ANDA applicant use a section viii statement against this patent?

A section viii strategy may be difficult because the claims recite treatment of pain using the composition itself. The availability of a carve-out depends on the approved labeling, the Orange Book listing and whether the patented method can be omitted without removing the product's principal indication.

References

1. United States Patent and Trademark Office. (2016). US Patent No. 9,452,163, Abuse deterrent dosage forms. U.S. Department of Commerce.

2. U.S. Food and Drug Administration. (2023). Approved drug products with therapeutic equivalence evaluations: Orange Book. U.S. Department of Health and Human Services.

3. U.S. Food and Drug Administration. (2015). Abuse-deterrent opioids: Evaluation and labeling guidance for industry. U.S. Department of Health and Human Services.

4. U.S. Food and Drug Administration. (2024). Hysingla ER prescribing information. Purdue Pharma L.P.

5. United States Code. (2024). 21 U.S.C. § 355: New drugs. Congress of the United States.

6. United States Code. (2024). 35 U.S.C. §§ 154 and 156: Patent term and patent term extension. Congress of the United States.

Drugs Protected by US Patent 9,452,163

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Recro Gainesville	ZOHYDRO ER	hydrocodone bitartrate	CAPSULE, EXTENDED RELEASE;ORAL	202880-001	Oct 25, 2013		DISCN	Yes	No						TREATMENT OF PAIN
Recro Gainesville	ZOHYDRO ER	hydrocodone bitartrate	CAPSULE, EXTENDED RELEASE;ORAL	202880-002	Oct 25, 2013		DISCN	Yes	No						TREATMENT OF PAIN
Recro Gainesville	ZOHYDRO ER	hydrocodone bitartrate	CAPSULE, EXTENDED RELEASE;ORAL	202880-003	Oct 25, 2013		DISCN	Yes	No						TREATMENT OF PAIN

International Family Members for US Patent 9,452,163

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2015313785
Australia	2020203841
Brazil	112017004882