Details for Patent: 8,877,247

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Which drugs does patent 8,877,247 protect, and when does it expire?

Patent 8,877,247 protects EMBEDA and is included in one NDA.

This patent has fifty-four patent family members in twenty-two countries.

Summary for Patent: 8,877,247

Title:	Abuse-deterrent multi-layer pharmaceutical composition comprising an opioid antagonist and an opioid agonist
Abstract:	Provided herein is a pharmaceutical composition comprising an antagonist, an agonist, a seal coat, and a sequestering polymer, wherein the antagonist, agonist, seal coat and at least one sequestering polymer are all components of a single unit, and wherein the seal coat forms a layer physically separating the antagonist from the agonist from one another. Methods for manufacturing such a pharmaceutical composition are also provided.
Inventor(s):	Frank Matthews, Garth Boehm, Lijuan Tang, Alfred Liang
Assignee:	Alpharma Pharmaceuticals LLC
Application Number:	US12/710,016
Patent Claim Types: see list of patent claims	Composition; Formulation;

US Patent 8,877,247: Scope, Claim Construction, Patent Landscape, and Generic Entry Risk

US Patent 8,877,247 protects multi-layer opioid pellets designed to sequester an opioid antagonist while delivering an opioid agonist in an abuse-deterrent dosage form. The core technical limitation is a sequestering layer containing an ammonium-functional acrylic or methacrylic copolymer, a narrowly defined surfactant concentration, and talc at a specified ratio. Claims 1-13 cover antagonist-containing pellet systems, while claim 14 adds an oxycodone layer and controlled-release coating. Claims 15 and 16 extend the formulations to additional opioid agonists, particularly morphine.

The patent is composition-of-matter and formulation-focused. It does not broadly cover every abuse-deterrent opioid product. A potentially infringing product must practice every limitation of an asserted claim, including the multi-layer pellet architecture and, for claims 3-7, the specified 73-hour sequestration result.

What does US Patent 8,877,247 protect?

The patent protects a multiparticulate dosage form containing a water-soluble core and separate functional layers. The principal architecture is:

1. Water-soluble core.
2. Opioid antagonist layer.
3. Sequestering polymer layer.
4. Osmotic pressure-regulating layer.
5. Optional opioid agonist layer.
6. Optional controlled-release layer.

The antagonist may be naltrexone, naloxone, nalmefene, cyclazacine, levallorphan, a salt, or a combination. The agonist may include morphine, oxycodone, hydrocodone, hydromorphone, dihydrocodeine, codeine, dihydromorphine, buprenorphine, or a salt.

The patent's commercial purpose is to inhibit extraction of the antagonist while permitting normal oral delivery of the opioid agonist. If the dosage form is crushed, dissolved, or otherwise manipulated, the antagonist remains physically associated with the coated pellet structure and is intended to reduce opioid effects or deter abuse.

How are the independent claims structured?

Claim 1: Broad antagonist-pellet formulation

Claim 1 is the primary broad composition claim. It requires:

Limitation	Required scope
Dosage form	A composition comprising a plurality of multi-layer pellets
Core	Water-soluble core
Antagonist	Layer comprising specified opioid antagonist
Sequestering layer	Layer coating the antagonist layer
Osmotic layer	Layer coating the sequestering polymer layer
Polymer	Acrylic/methacrylic ester copolymers with quaternary ammonium groups
Surfactant	1.6% to 6.3% by weight relative to the polymer
Talc	75% to 125% by weight relative to the polymer
Surfactant options	Sodium lauryl sulfate and specified alternatives

The polymer limitation points to ammonium methacrylate copolymers commonly used in pharmaceutical coatings, including products in the Eudragit RL or RS family. The claim, however, is defined by chemical functionality and formulation ratios rather than by a trade name.

A product containing naltrexone in a simple matrix tablet would not fall within claim 1 because the claim requires a plurality of multi-layer pellets. A pellet product lacking the osmotic pressure-regulating layer would also fall outside claim 1 unless an equivalent theory applied.

Claim 14: Oxycodone-specific architecture

Claim 14 independently requires all of the claim 1 architecture and adds:

• An opioid agonist layer coating the osmotic pressure-regulating layer;
• Oxycodone, an oxycodone salt, or a combination; and
• A controlled-release layer coating the opioid agonist layer.

Claim 14 is narrower than claim 1 because it requires the additional oxycodone and controlled-release layers. It is commercially important because it is directed to a formulation resembling an abuse-deterrent oxycodone multiparticulate product.

Claims 15 and 16: Agonist combinations

Claim 15 adds an opioid agonist to the composition of claim 1 or claim 14. Claim 16 narrows claim 15 to morphine or a pharmaceutically acceptable salt.

These claims create a bridge between the broad antagonist-only formulation and a complete opioid agonist/antagonist product. Morphine sulfate formulations are particularly relevant because claim 6 expressly identifies morphine sulfate and hydroxypropyl cellulose in the opioid agonist layer.

What formulation features are most important?

The patent's enforceable value is concentrated in the interaction among the polymer, surfactant, talc, and multilayer arrangement.

Sequestering polymer layer

The polymer must comprise copolymers of acrylic and methacrylic acid esters carrying quaternary ammonium groups. These polymers form a water-permeable but relatively restrictive coating around the antagonist-containing layer.

The claim does not merely require a polymer coating. It requires the specified class of ammonium-functional copolymers. A formulation using ethylcellulose, hypromellose, polyvinyl acetate, or another non-equivalent polymer may avoid literal infringement, although equivalence would depend on the product and claim construction.

Surfactant concentration

The surfactant must be present at 1.6% to 6.3% by weight relative to the ammonium-functional copolymer. This is a narrow numerical limitation.

For example, if the formulation contains 100 mg of the claimed polymer, the surfactant must generally be present in an amount corresponding to 1.6 mg to 6.3 mg under the claim's weight-to-weight relationship. The relevant denominator is the amount of the specified copolymer, not necessarily the total coating weight or total dosage-form weight.

Sodium lauryl sulfate is the most commercially significant option because it appears in claims 5-11 and is combined with naltrexone hydrochloride in claims 7-11.

Talc concentration

Talc must be present at 75% to 125% by weight relative to the polymer. The range is unusually specific and can create design-around opportunities.

A formulation with talc below 75% or above 125% may avoid literal infringement of claim 1, although the effect of other patent claims, prosecution history, and the doctrine of equivalents would remain relevant.

Osmotic pressure-regulating layer

The layer may contain sodium chloride, sodium bromide, sodium iodide, hydroxypropyl methyl cellulose, or combinations. Claims 5-11 narrow the formulation to specific osmotic agents:

Claim	Antagonist	Surfactant	Osmotic agent
5	Opioid antagonist salt	Sodium lauryl sulfate	Sodium chloride
7	Naltrexone HCl	Sodium lauryl sulfate	Sodium chloride
9	Naltrexone HCl	Sodium lauryl sulfate	Sodium bromide
10	Naltrexone HCl	Sodium lauryl sulfate	Sodium iodide
11	Naltrexone HCl	Sodium lauryl sulfate	Hypromellose

The osmotic layer is a meaningful structural limitation. A product using a different release-regulating material may not satisfy the literal language of these claims.

How do claims 3-7 define the sequestration performance?

Claims 3-7 require at least 80% sequestration of the opioid antagonist after 73 hours under a defined dissolution protocol:

1. 500 mL of 0.1 N hydrochloric acid.
2. One hour at 37°C.
3. USP paddle apparatus at 100 rpm.
4. Transfer to 500 mL of pH 7.5, 0.05 M phosphate buffer.
5. Seventy-two additional hours at 37°C and 100 rpm.
6. Measurement of the amount of antagonist sequestered.

The total test period is 73 hours. The result is a functional limitation, not merely an intended use. An accused product would need to be evaluated under the specified method. Claims 6 and 7 apply the 80% threshold to morphine-associated naltrexone salts and naltrexone hydrochloride, respectively.

The protocol creates litigation issues over:

• The meaning of "sequestered";
• Whether the entire composition or only the pellet fraction is tested;
• Analytical recovery of the antagonist;
• Sampling and assay methodology;
• Whether deviations from USP paddle conditions affect claim satisfaction;
• Whether the test result is reproducible across batches.

A product may have the same structural layers but avoid claims 3-7 if it does not meet the 80% performance threshold. Conversely, a product that meets the threshold but lacks the claimed structure would not necessarily infringe because the claims are combination claims.

Which claims are strongest from an enforcement perspective?

The most commercially important claims are claims 1, 7, 14, and 16.

Claim	Practical significance	Relative breadth
1	Covers antagonist-containing multilayer pellets	Broadest independent claim
7	Narrows to naltrexone HCl, sodium lauryl sulfate, sodium chloride, and 80% sequestration	Strong product-specific claim
14	Covers oxycodone multilayer pellets with controlled release	Narrower but commercially targeted
15	Adds broad opioid agonist coverage to claims 1 or 14	Combination claim
16	Narrows agonist to morphine or a salt	Product-specific morphine claim

Claim 1 has the broadest literal coverage but also presents the largest prior-art exposure because multiparticulate abuse-deterrent formulations and ammonium methacrylate coatings were established technologies before the patent's filing date.

Claims 6 and 7 may be more useful against a product that closely follows a naltrexone HCl and morphine formulation. Their narrower structure and quantitative performance limitation may improve differentiation from earlier generalized abuse-deterrence disclosures.

Claim 14 is potentially important against oxycodone products because it requires a defined vertical pellet sequence rather than merely the presence of oxycodone and an antagonist.

What is the patent's likely geographic coverage?

US Patent 8,877,247 provides rights only in the United States. The claims do not establish protection in Canada, Europe, Japan, China, or other jurisdictions.

International coverage must be assessed through the patent family. Relevant questions include:

• Whether a PCT application was filed;
• Which national-stage applications entered Europe, Canada, Australia, Japan, or China;
• Whether corresponding applications issued;
• Whether foreign counterparts were abandoned or lapsed;
• Whether claim scope was materially amended outside the United States.

A US formulation patent can have materially different protection abroad because European and other patent offices may apply stricter added-matter, clarity, support, and inventive-step standards to functional sequestration claims.

What manufacturing and intellectual-property barriers does the patent create?

The principal manufacturing barrier is process integration. A manufacturer must produce:

• Uniform water-soluble cores;
• A consistent antagonist layer;
• A continuous ammonium-functional polymer coating;
• Controlled surfactant and talc ratios;
• A separate osmotic layer;
• An optional agonist layer;
• A controlled-release outer coating.

The risk is not limited to ingredient selection. Coating weight gain, spray uniformity, pellet size distribution, drying conditions, residual solvent, and layer adhesion can affect whether the finished product satisfies the structural and performance limitations.

The narrow surfactant and talc ranges create potential design-around strategies:

Design-around approach	Potential effect
Use a non-ammonium-functional polymer	May avoid the polymer limitation
Use surfactant below 1.6% or above 6.3%	May avoid claims containing the numerical range
Use talc below 75% or above 125%	May avoid the talc limitation
Use a non-listed osmotic agent	May avoid claims 5 and 7-11
Use a matrix tablet instead of pellets	May avoid the pellet limitation
Place surfactant in another layer	Relevant to claims 2 and 4
Use a different antagonist	May avoid naltrexone-specific claims but not necessarily claim 1

These approaches must be evaluated against the full patent family, continuation claims, and other patents covering abuse-deterrent opioid products.

How does US Patent 8,877,247 compare with competing abuse-deterrent technologies?

Technology	Core design	Relationship to US 8,877,247
Multilayer antagonist pellets	Sequestered naltrexone or related antagonist	Closest technical overlap
Physical-hardening tablets	Crush-resistant polymer matrix	Different dosage-form architecture
Gel-forming formulations	Polymer forms viscous gel when manipulated	May avoid the pellet structure
Oxidation or aversion systems	Irritant, bitterant, or aversive excipients	Claim 12 expressly excludes several aversive approaches
Opioid-antagonist combinations	Antagonist is released under abuse conditions	May overlap depending on pellet layers
Controlled-release oxycodone systems	Extended-release oxycodone with abuse-deterrent properties	Potential overlap with claim 14
Morphine/naltrexone multiparticulates	Morphine agonist with naltrexone antagonist	Potential overlap with claims 6, 7, 15, and 16

Claim 12 is commercially relevant because it excludes a bittering agent, gelling agent, irritant, or emetic. The patent therefore targets a sequestration-based approach rather than an aversive-excipient approach.

What is the FDA and Orange Book significance?

The patent itself does not establish FDA approval, Orange Book listing, or regulatory exclusivity. Those are separate regulatory questions.

For an approved drug, Orange Book listing depends on whether the patent claims:

• The active ingredient;
• The approved drug product formulation or composition; or
• An approved method of use.

A formulation patent may be listed if it claims the approved product and satisfies FDA listing requirements. A patent directed only to manufacturing methods, packaging, or unapproved uses may not qualify for listing in the same manner.

The claims provided are composition claims directed to multilayer pellets. They could be relevant to an approved abuse-deterrent opioid product if the approved product contains the claimed architecture. The patent number and claim text alone do not establish that the patent was listed in the Orange Book for a particular reference-listed drug.

FDA regulatory status is separate from patent validity. FDA approval does not validate the patent, and an issued patent does not establish that the FDA will approve a product using the claimed formulation.

What Paragraph IV and generic-entry risks exist?

A generic applicant could challenge the patent through an ANDA Paragraph IV certification if the patent is listed for the relevant reference product. Likely challenge theories would include:

1. Lack of anticipation based on prior multiparticulate opioid-antagonist formulations.
2. Obviousness based on combining known ammonium methacrylate coatings, surfactants, talc, osmotic agents, and opioid antagonists.
3. Lack of written description for the full genus of antagonists, surfactants, and osmotic agents.
4. Lack of enablement across the broad claim scope.
5. Indefiniteness involving "sequestering," "comprising layer," and relative weight percentages.
6. Non-infringement based on polymer identity, layer placement, pellet structure, or concentration ranges.
7. Failure to meet the 80% performance limitation.

The highest infringement risk would arise where a generic reproduces naltrexone HCl, sodium lauryl sulfate, sodium chloride, an ammonium methacrylate polymer, and talc within the specified ranges. A generic using a different antagonist, non-pellet dosage form, or alternative sequestering polymer may have a stronger non-infringement position.

A Paragraph IV notice could trigger a Hatch-Waxman action and a 30-month stay if the statutory conditions for the stay were satisfied. Settlement terms could include delayed entry, a license, or a reformulated product, but the claim text does not establish whether any settlement agreement exists.

What is the patent expiration date and current litigation status?

US Patent 8,877,247 issued on October 21, 2014. The patent's precise expiration date cannot be determined from the claims supplied. It depends on the earliest effective nonprovisional filing date, any patent-term adjustment, terminal disclaimer, and whether the patent belongs to a continuation chain.

The issued patent number also does not establish:

• Current ownership;
• Assignments or security interests;
• Maintenance-fee status;
• Patent-term adjustment;
• Orange Book listing;
• Paragraph IV certifications;
• ANDA litigation;
• Settlement agreements;
• Pending continuation applications.

Those matters are recorded in USPTO assignment and patent-status systems, FDA Orange Book records, and federal court dockets rather than in the claim language. No litigation or settlement conclusion follows from the claims alone.

How strong is the patent estate?

The patent has a technically coherent but relatively narrow claim center. Its strongest features are:

• A defined multilayer pellet sequence;
• A chemically specific sequestering polymer;
• Narrow surfactant and talc ratios;
• Specific naltrexone HCl embodiments;
• A measurable 80% sequestration threshold;
• An oxycodone embodiment with a controlled-release outer layer.

Its vulnerabilities are:

• Dependence on known coating technologies;
• Numerous numerical limitations that facilitate design-around;
• Potential written-description and enablement challenges for broad genus claims;
• Ambiguity in claim dependencies and layer terminology;
• The need to prove the composition's structure and, for some claims, its performance under a specialized test.

The practical value of the patent therefore depends less on claim 1 in isolation than on whether a marketed product matches the narrower naltrexone, surfactant, osmotic-agent, and pellet limitations.

Key Takeaways

• US Patent 8,877,247 covers multilayer opioid pellets with a sequestered opioid antagonist.
• Claim 1 requires a water-soluble core, antagonist layer, ammonium-functional polymer layer, osmotic layer, specified surfactant range, and specified talc range.
• Claims 6 and 7 are directed to morphine-associated naltrexone and naltrexone HCl formulations.
• Claim 14 targets oxycodone pellets with an agonist layer and controlled-release coating.
• Claims 3-7 impose an 80% antagonist-sequestration requirement after a 73-hour dissolution protocol.
• The most credible design-arounds involve changing the polymer, pellet architecture, osmotic agent, surfactant concentration, or talc ratio.
• FDA approval, Orange Book listing, Paragraph IV activity, ownership, maintenance status, and expiration require records outside the claim text.
• The patent issued October 21, 2014; its exact expiration date is not derivable from the supplied claims.

FAQs About US Patent 8,877,247

Does US Patent 8,877,247 cover all naltrexone opioid formulations?

No. The claims require a multilayer pellet structure with specific coating layers, polymer chemistry, surfactant concentration, and talc ratio. A tablet, capsule, matrix formulation, or formulation using a different coating system may fall outside the literal claims.

Does the patent cover Embeda?

The claims are technically relevant to morphine-and-naltrexone abuse-deterrent formulations, but the patent number alone does not establish whether Embeda practices the claims or whether the patent was listed for Embeda in the Orange Book.

Can a generic avoid the patent by replacing sodium lauryl sulfate?

Potentially. Claims 1 and 14 list several alternative surfactants, so replacement with another listed surfactant may not avoid the claims. A non-listed surfactant could avoid literal infringement, subject to the remaining claim limitations and any equivalents analysis.

Is the 80% sequestration test required for every claim?

No. Claims 3-7 expressly include the 80% sequestration limitation. Claims 1, 2, 8-16 do not all contain that performance limitation, although they require other structural or compositional limitations.

Does claim 14 cover morphine products?

No, not by itself. Claim 14 specifically requires an opioid agonist selected from oxycodone, an oxycodone salt, or combinations. Morphine coverage arises through claim 15 and is narrowed further by claim 16.

References

1. United States Patent No. 8,877,247, Abuse deterrent dosage forms and methods of use thereof (issued October 21, 2014).

2. U.S. Food and Drug Administration. (2023). Approved drug products with therapeutic equivalence evaluations (Orange Book). https://www.fda.gov/drugsatfda

3. U.S. Food and Drug Administration. (2015). Guidance for industry: Abuse-deterrent opioids: Evaluation and labeling. https://www.fda.gov

4. United States Patent and Trademark Office. (2024). Manual of patent examining procedure: Patent term adjustment and patent term extension. https://www.uspto.gov

5. U.S. Food and Drug Administration. (2016). General principles for evaluating abuse deterrence of generic solid oral opioid drug products. https://www.fda.gov

Drugs Protected by US Patent 8,877,247

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Alpharma Pharms	EMBEDA	morphine sulfate; naltrexone hydrochloride	CAPSULE, EXTENDED RELEASE;ORAL	022321-001	Aug 13, 2009		DISCN	Yes	No	8,877,247		Y
Alpharma Pharms	EMBEDA	morphine sulfate; naltrexone hydrochloride	CAPSULE, EXTENDED RELEASE;ORAL	022321-002	Aug 13, 2009		DISCN	Yes	No	8,877,247		Y
Alpharma Pharms	EMBEDA	morphine sulfate; naltrexone hydrochloride	CAPSULE, EXTENDED RELEASE;ORAL	022321-003	Aug 13, 2009		DISCN	Yes	No	8,877,247		Y
Alpharma Pharms	EMBEDA	morphine sulfate; naltrexone hydrochloride	CAPSULE, EXTENDED RELEASE;ORAL	022321-004	Aug 13, 2009		DISCN	Yes	No	8,877,247		Y
Alpharma Pharms	EMBEDA	morphine sulfate; naltrexone hydrochloride	CAPSULE, EXTENDED RELEASE;ORAL	022321-005	Aug 13, 2009		DISCN	Yes	No	8,877,247		Y
Alpharma Pharms	EMBEDA	morphine sulfate; naltrexone hydrochloride	CAPSULE, EXTENDED RELEASE;ORAL	022321-006	Aug 13, 2009		DISCN	Yes	No	8,877,247		Y

International Family Members for US Patent 8,877,247

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	E552829
Australia	2007261451
Australia	2013257508
Australia	2016238844
Australia	2018201915
Brazil	PI0714039
Canada	2655835