Details for Patent: 10,182,995

Which drugs does patent 10,182,995 protect, and when does it expire?

Patent 10,182,995 protects JORNAY PM and is included in one NDA.

This patent has forty-two patent family members in fourteen countries.

Summary for Patent: 10,182,995

Title:	Compositions for treatment of attention deficit hyperactivity disorder
Abstract:	Therapeutic compositions deliver a therapeutic amount of methylphenidate in a delayed and extended release formulation. The dosage form exhibits a lag time prior to release of from 6 to 8 hours or longer, followed by a sustained release period.
Inventor(s):	David Lickrish, Feng Zhang
Assignee:	Ironshore Pharmaceuticals and Development Inc Cayman Island , Formulation Technologies LLC
Application Number:	US15/359,202
Patent Claim Types: see list of patent claims	Composition; Formulation; Compound; Dosage form;

United States Patent 10,182,995: Methylphenidate Delayed-Release and Extended-Release Patent Analysis

US Patent 10,182,995 protects a multiparticulate oral methylphenidate formulation designed to combine an extended gastrointestinal lag period with subsequent sustained release. The broadest claim requires four technical elements: a methylphenidate core, a specific sustained-release coating, a pH-dependent outer polymer, and a defined dissolution profile. Claims 3, 4, and 9 materially narrow the estate to ethyl cellulose, hydroxypropyl cellulose, dibutyl sebacate, and metal stearates, particularly magnesium stearate.

The patent is commercially relevant to delayed-release and extended-release methylphenidate products, including the formulation technology used in Jornay PM. The principal enforcement value is the functional dissolution limitation in claim 1 combined with the coating-composition limitations. A competing product could avoid literal infringement by omitting a required coating component, using a different pH-dependent polymer system, or failing the claimed lag and release profile. The doctrine of equivalents remains a potential risk where the substitute materials perform substantially the same function in substantially the same way.

What does US Patent 10,182,995 protect?

The patent protects a solid oral dosage form containing coated methylphenidate particles. The claim architecture is directed to the composition as a whole, not merely to methylphenidate, a capsule shell, or a method of treating attention-deficit/hyperactivity disorder.

Claim element	Scope of protection
Solid oral composition	Covers capsules, tablets, multiparticulate systems, or other solid oral forms, subject to the particle and coating limitations
Core	Must contain methylphenidate or a pharmaceutical salt
Sustained-release layer	Must enclose the core and contain a water-insoluble, water-permeable polymer, a water-soluble polymer, a hydrophobic plasticizer, and a hydrophobic binder
pH-dependent polymer	Must be insoluble in aqueous medium below pH 5.5
Release profile	Must provide at least an eight-hour lag with no more than 10% release, followed by sustained release
Dosage strength	Claims 7 and 8 cover 1-150 mg and 1-80 mg, respectively
Test method	USP Apparatus I, 37°C ±0.5°C, with sequential acidic and buffered media

The claim is composition-based but includes a performance limitation. A product may contain the same ingredients yet avoid claim 1 if it does not satisfy the specified dissolution profile. Conversely, a product with a different commercial name may infringe if its composition and release characteristics fall within the claim.

How should claim 1 be construed?

Claim 1 contains a layered particulate architecture:

1. A methylphenidate-containing core.
2. A sustained-release layer around that core.
3. A pH-dependent layer or component.
4. A defined delayed and sustained dissolution profile.

The phrase "comprising" generally permits additional excipients, coating layers, binders, stabilizers, lubricants, and capsule materials. A formulation containing extra materials would not avoid the claim if all recited elements remain present.

The term "coated particles" is important. The claim is directed to discrete particles having a core and surrounding coating structure. A monolithic matrix tablet with methylphenidate dispersed throughout a polymer matrix may not satisfy the particle limitation unless it contains the claimed coated-particle architecture.

The claim also requires that the sustained-release layer comprise:

• A water-insoluble and water-permeable polymer.
• A water-soluble polymer.
• A hydrophobic plasticizer.
• A hydrophobic binder.

A coating that uses only an insoluble polymer and a plasticizer, without the required water-soluble polymer or hydrophobic binder, presents a potential noninfringement position. That position depends on the formulation record and whether one material performs more than one claimed function.

What dissolution profile does Patent 10,182,995 require?

The release profile is the principal functional limitation. The formulation must provide:

• At least an eight-hour lag period.
• No more than 10% total methylphenidate release during that lag period.
• A subsequent sustained-release period of 10-12 hours.
• Testing in 700 mL of 0.1N hydrochloric acid at pH 1.1 for up to two hours.
• Subsequent testing in sodium phosphate buffer at pH 6.0 for four hours.
• Further testing in sodium phosphate buffer at pH 7.2 for 14 hours.
• Testing at 37°C ±0.5°C using USP Apparatus I.

The claim presents a potential construction issue because the stated media sequence and the eight-hour lag requirement must be read together. The two-hour acid phase and four-hour pH 6.0 phase account for six hours of testing. The claim therefore appears to require continued control of release during the early portion of the pH 7.2 phase to reach an eight-hour lag.

For infringement analysis, dissolution testing should be performed using the exact claimed apparatus, media volumes, pH values, temperature, sampling intervals, and assay method. Small changes in agitation speed, sink conditions, buffer preparation, or sampling correction can affect whether a product releases more than 10% during the claimed lag period.

What do claims 2 through 9 add?

What does claim 2 protect?

Claim 2 narrows the active ingredient to methylphenidate hydrochloride. It excludes formulations using another methylphenidate salt unless the salt is treated as equivalent under the applicable claim-construction analysis.

What does claim 3 protect?

Claim 3 requires a sustained-release layer containing:

• Ethyl cellulose.
• Hydroxypropyl cellulose.
• Dibutyl sebacate.
• A metal stearate.

This claim is narrower than claim 1 because it identifies specific excipient classes and polymers.

What does claim 4 protect?

Claim 4 further limits the metal stearate to magnesium stearate. A formulation using calcium stearate, zinc stearate, or another lubricant may avoid literal infringement of claim 4 while remaining potentially exposed under claim 3 or claim 1.

What does claim 5 protect?

Claim 5 identifies methacrylic acid copolymer Type B as the pH-dependent copolymer. This limitation is directed to an enteric or pH-responsive polymer system that remains substantially insoluble under acidic conditions and becomes more permeable or soluble at a higher pH.

The commercial identity of a polymer is not enough to establish infringement. The relevant issue is the polymer's compendial or chemical identity, grade, substitution pattern, molecular characteristics, and behavior under the claim's pH conditions.

What does claim 6 protect?

Claim 6 adds mono- and diglycerides, dibutyl sebacate, and polysorbate 80. Because dibutyl sebacate is also recited in the sustained-release layer of claim 1, claim 6 may cover formulations in which these materials occur in different layers or in the overall dosage form.

What do claims 7 and 8 protect?

Claim 7 covers a single dosage form containing 1-150 mg of methylphenidate or its salt. Claim 8 narrows that range to 1-80 mg.

Claim 8 is not a separate, nonoverlapping commercial category. It is a subset of claim 7. A 20 mg product, for example, would fall within both dosage ranges if the remaining limitations are met.

What does claim 9 protect?

Claim 9 is the most compositionally specific claim. It requires:

• Ethyl cellulose and hydroxypropyl cellulose in an approximate 1:3 to 1:5 ratio.
• Dibutyl sebacate.
• Magnesium stearate at 25%-50% by weight.

The meaning of "by weight" must be determined from the specification and prosecution history, particularly whether the percentage is calculated against the sustained-release layer, the coating solids, or the entire composition. This limitation creates a potentially strong design-around route if a competitor materially changes the polymer ratio or magnesium stearate concentration.

How strong is the patent estate for delayed-release methylphenidate?

The patent has meaningful technical scope because it combines structural and functional limitations. A challenger cannot focus only on the ingredient list. It must address the entire combination, including the coating architecture and the dissolution profile.

Strength factor	Assessment
Core technology	Strongly focused on delayed and extended release of methylphenidate
Structural limitations	Moderate to strong; multiple required coating components narrow the claim
Functional limitation	Potentially strong if the test method is reproducible and commercially relevant
Design-around potential	Material; alternative polymers, coating systems, or release profiles may avoid literal infringement
Enablement exposure	Depends on the breadth of formulations that can achieve the claimed profile
Written-description exposure	Depends on whether the specification supports the full range of polymers, ratios, salts, doses, and release profiles
Obviousness exposure	Depends on prior art combining methylphenidate cores, ethyl cellulose systems, pH-dependent polymers, and delayed-release profiles
Invalidity risk from functional claiming	Moderate; the claim is measurable, but the boundaries of the release profile must be clear

The strongest validity challenge would likely combine prior art on methylphenidate multiparticulates with prior art on enteric or pH-dependent coatings and sustained-release ethyl cellulose systems. The patent holder's principal response would be that the claimed combination produces a specific delayed-onset and extended-release profile not taught or reasonably predictable from the individual references.

What formulations are most likely to infringe?

A formulation presents the highest risk when it has all of the following characteristics:

• Methylphenidate hydrochloride in discrete coated particles.
• Ethyl cellulose in the sustained-release layer.
• Hydroxypropyl cellulose as the water-soluble polymer.
• Dibutyl sebacate as the hydrophobic plasticizer.
• Magnesium stearate as the hydrophobic binder or metal stearate.
• Methacrylic acid copolymer Type B as the pH-dependent coating.
• A delayed release profile with minimal release for approximately eight hours.
• A later extended-release phase lasting approximately 10-12 hours.
• A single dose containing 1-80 mg or 1-150 mg of methylphenidate.

A formulation using the same active ingredient but an immediate-release core, a monolithic matrix, a non-pH-dependent outer coating, or an earlier release profile would present lower literal infringement risk.

What is the relationship to Jornay PM?

Jornay PM is an extended-release methylphenidate hydrochloride product approved by the FDA for attention-deficit/hyperactivity disorder. The FDA label describes a delayed-release and extended-release dosage form intended for evening administration, with therapeutic release occurring after a delay and continuing through the following day (U.S. Food and Drug Administration, 2018).

The claim limitations in Patent 10,182,995 closely track the technical characteristics expected from a delayed-release and extended-release methylphenidate multiparticulate product. The commercial product, however, must be compared against the issued claims using its approved formulation, manufacturing records, coating composition, and dissolution specifications. Similar clinical behavior alone does not establish infringement.

Product characteristic	Patent 10,182,995	Jornay PM profile
Active ingredient	Methylphenidate or salt	Methylphenidate hydrochloride
Dosage form	Solid oral coated particles	Delayed-release and extended-release capsule
Delayed onset	Required by claim 1	Described in FDA labeling
Sustained release	Required by claim 1	Described in FDA labeling
Exact excipient identity	Required for narrower claims	Must be confirmed against approved product records
Exact dissolution sequence	Required for claim 1	Must be compared with regulatory and patent testing data

What is the Orange Book status of Patent 10,182,995?

Orange Book status is determined by FDA listing records, not by the issued patent alone. A patent may be relevant to a branded product without every claim or patent family member being listed for that product.

For an ANDA applicant, the controlling issues are:

• Whether Patent 10,182,995 is listed for the relevant NDA.
• Whether the listing carries a composition, formulation, or method-of-use code.
• Whether the proposed generic falls within the listed claims.
• Whether the applicant files a Paragraph IV certification.
• Whether the patent holder sues within 45 days of receiving notice.

The patent claims supplied are composition claims. They are not limited to a method of treating ADHD, so any Orange Book listing would most naturally relate to the product's composition or formulation rather than a method-of-use code. FDA Orange Book records and the NDA's current patent listing control the regulatory analysis (U.S. Food and Drug Administration, n.d.).

When does exclusivity expire?

Patent exclusivity and FDA regulatory exclusivity are separate.

Exclusivity type	Relevance
Patent term	Depends on the effective filing date, patent-term adjustment, terminal disclaimers, and any patent-term extension
New chemical entity exclusivity	Applies to the active moiety and is separate from formulation patents
Three-year clinical investigation exclusivity	May restrict approval of certain ANDAs relying on the NDA during the applicable period
Orphan exclusivity	Applies only if the product has an orphan designation and approval for the protected indication
Pediatric exclusivity	Can add six months to qualifying regulatory exclusivity or patent periods

The grant date of US Patent 10,182,995 is not, by itself, the expiration date. The legally operative term must be taken from the USPTO patent record after accounting for patent-term adjustment and any terminal disclaimer. The supplied claims do not provide the priority chain or prosecution data needed to state a reliable terminal expiration date.

Which companies are challenging Patent 10,182,995?

No Paragraph IV challenger, ANDA applicant, federal litigation docket, or settlement agreement can be established from the claim text alone. A complete challenge assessment requires matching the patent to the relevant Orange Book listing, reviewing FDA Paragraph IV notices, and searching federal court and appellate dockets.

Potential challengers would include manufacturers developing generic delayed-release and extended-release methylphenidate capsules. The most credible challenge strategies would be:

1. Noninfringement based on a different multiparticulate coating system.
2. Failure to meet the eight-hour lag limitation.
3. Failure to meet the claimed sequential dissolution profile.
4. Use of a pH-dependent polymer other than methacrylic acid copolymer Type B.
5. Invalidity based on obviousness over multiparticulate methylphenidate and enteric-coating prior art.
6. Lack of written description or enablement for the full claimed formulation and dose ranges.

What generic launch risks exist?

A generic launch risk analysis should distinguish three scenarios.

At-risk launch before patent expiry

If the applicant files Paragraph IV and the patent holder files suit within 45 days, FDA approval may be subject to a 30-month stay under the Hatch-Waxman framework, subject to statutory exceptions and court developments (21 U.S.C. § 355).

Launch after patent expiry

A generic that satisfies bioequivalence and regulatory requirements could launch after the listed patents and applicable regulatory exclusivities expire, assuming no other blocking patents remain.

Design-around launch

A competitor could seek approval using a formulation that does not meet the claimed coating composition or release profile. This route carries formulation-development risk because the product must still reproduce the required pharmacokinetic performance and demonstrate bioequivalence to the reference drug.

What manufacturing and geographic barriers exist?

The patent is a United States right. It does not directly block manufacturing or sale outside the United States. Foreign risk depends on corresponding national patents, including patents in Europe, Canada, Japan, Australia, and other commercial markets.

Manufacturing risk is significant because the claimed performance depends on process-sensitive variables:

• Particle size and core density.
• Coating weight gain.
• Polymer ratios.
• Plasticizer distribution.
• Magnesium stearate concentration.
• Spray rate and drying conditions.
• Coating uniformity.
• Final dissolution testing.

A manufacturer may avoid a claim on paper but still face development failure if its alternative coating cannot reproduce the delayed and sustained exposure profile.

Key Takeaways

• US Patent 10,182,995 targets coated methylphenidate particles with delayed onset and subsequent sustained release.
• Claim 1 requires both a specific coating architecture and a defined dissolution profile.
• Claims 3, 4, and 9 narrow the estate to ethyl cellulose, hydroxypropyl cellulose, dibutyl sebacate, and metal stearates, particularly magnesium stearate.
• Claim 5 specifically identifies methacrylic acid copolymer Type B.
• Claims 7 and 8 cover single dosage forms containing 1-150 mg and 1-80 mg of methylphenidate, respectively.
• The most important infringement issue is whether a competing product satisfies the eight-hour lag and sequential dissolution requirements.
• A precise patent expiration date cannot be calculated from the claims alone because the priority chain, patent-term adjustment, and terminal-disclaimer data are not provided.
• Orange Book listing, Paragraph IV activity, litigation, and settlement status require current FDA and federal court records.
• The principal commercial relevance is to delayed-release and extended-release methylphenidate products such as Jornay PM.

FAQs

Does Patent 10,182,995 cover immediate-release methylphenidate?

No. The claims require coated particles, a sustained-release layer, a pH-dependent polymer, and a delayed-release profile. An ordinary immediate-release methylphenidate tablet would not satisfy those limitations.

Can a generic avoid the patent by changing only the capsule shell?

Usually not. The claims focus on the internal coated particles and their dissolution profile. A different capsule shell would not avoid infringement if the underlying particles still meet every claim limitation.

Does use of methylphenidate free base avoid the patent?

Not necessarily. Claim 1 covers methylphenidate and pharmaceutical salts. Whether a particular free-base formulation falls within the claim depends on claim construction and the remaining coating and dissolution limitations.

Is magnesium stearate required in every claim?

No. Magnesium stearate is required by claim 4 and claim 9. Claim 3 requires a metal stearate, while claim 1 does not specify magnesium stearate.

Is a different dissolution apparatus automatically noninfringing?

No. The claim specifies USP Apparatus I as the measurement method. Regulatory testing using another apparatus does not alone determine infringement. The relevant question is whether the accused product satisfies the claim when tested under the specified method.

References

1. U.S. Food and Drug Administration. (2018). Jornay PM prescribing information. NDA 209311.

2. U.S. Food and Drug Administration. (n.d.). Approved drug products with therapeutic equivalence evaluations: Orange Book. https://www.accessdata.fda.gov/scripts/cder/ob/

3. United States Patent and Trademark Office. (n.d.). Patent Center. https://patentcenter.uspto.gov/

4. United States Patent No. 10,182,995. (2019). Methylphenidate pharmaceutical composition claims.

5. 21 U.S.C. § 355. New drugs and antibiotics.

Drugs Protected by US Patent 10,182,995

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Ironshore Pharms	JORNAY PM	methylphenidate hydrochloride	CAPSULE, EXTENDED RELEASE;ORAL	209311-001	Aug 8, 2018		RX	Yes	No	10,182,995		Y
Ironshore Pharms	JORNAY PM	methylphenidate hydrochloride	CAPSULE, EXTENDED RELEASE;ORAL	209311-002	Aug 8, 2018		RX	Yes	No	10,182,995		Y
Ironshore Pharms	JORNAY PM	methylphenidate hydrochloride	CAPSULE, EXTENDED RELEASE;ORAL	209311-003	Aug 8, 2018		RX	Yes	No	10,182,995		Y
Ironshore Pharms	JORNAY PM	methylphenidate hydrochloride	CAPSULE, EXTENDED RELEASE;ORAL	209311-004	Aug 8, 2018		RX	Yes	No	10,182,995		Y
Ironshore Pharms	JORNAY PM	methylphenidate hydrochloride	CAPSULE, EXTENDED RELEASE;ORAL	209311-005	Aug 8, 2018		RX	Yes	Yes	10,182,995		Y

International Family Members for US Patent 10,182,995

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2012230733
Australia	2016228307
Australia	2018202002
Brazil	112013024401
Canada	2830788
China	103608004
China	110151731