US Patent 9,040,085 is a formulation-driven method-of-use patent covering delayed-release oral dosage forms containing prednisone, prednisolone, or methylprednisolone. Its commercial significance is concentrated in prednisone products using a rupturable compression coating, including delayed-release products such as RAYOS. The independent claims require a specific tablet architecture, excipient profile, absence of gum-based or strongly gelling diffusion-barrier materials, and a defined lag-time or dissolution outcome. An immediate-release prednisone tablet does not practice these claims.

US Patent 9,040,085: Claim Scope, Expiration, and Patent Landscape for Delayed-Release Glucocorticosteroids

What does US Patent 9,040,085 protect?

US 9,040,085 protects methods of administering a delayed-release oral dosage form containing prednisone, prednisolone, or methylprednisolone. The dosage form must have:

A defined drug-containing core.
A compression coating that completely surrounds the core.
A disintegrant in the core that generates force in aqueous media.
A coating designed to rupture rather than function primarily as a diffusion membrane.
A coating containing specified hydrophobic or surfactant-type excipients.
Substantially no natural or synthetic gum.
A delayed-release performance profile.

The patent does not broadly cover every delayed-release glucocorticosteroid product. It targets a particular mechanism: the core hydrates and expands, generating internal force that ruptures the surrounding compression coating.

The patent issued on June 2, 2015, as US 9,040,085 B2. The relevant patent record, prosecution history, assignments, and term information are maintained by the USPTO Patent Center and Patent Examination Data System.[1]

What are the independent claims in US 9,040,085?

Claims 1, 6, and 9 are independent method claims. They describe overlapping but legally distinct performance requirements.

Claim	Required release limitation	Principal technical focus
1	No active release after four hours; 100% release by five hours in specified USP dissolution testing	In vitro dissolution profile
6	Compression coating ruptures after approximately two to six hours in aqueous medium	Physical rupture timing
9	No more than 10% release before the lag time and substantially complete release within about one hour after the lag time; lag time of two to six hours	In-use or physiological delayed-release profile

Each independent claim also requires the glucocorticosteroid selection, core, compression coating, disintegrant, excipient limitations, and absence of a substantial gum or strongly gelling diffusion barrier.

A product can therefore avoid claim 1 while potentially raising issues under claim 6 or claim 9 if it uses the same core-and-coating architecture but produces a different measured release profile.

How does claim 1 define the protected dosage form?

Claim 1 has the most specific laboratory performance requirement. The dosage form must release:

No active substance after four hours; and
100% of the active substance by five hours.

The testing conditions are material:

500 mL purified water;
USP dissolution apparatus No. 2;
Paddles;
Stationary baskets;
100 rpm.

The claim therefore does not merely require "delayed release." It requires a sharply defined dissolution transition under a specified test protocol. A competing product could potentially avoid literal infringement if it releases more than the permitted amount before four hours, fails to reach complete release by five hours, or uses materially different testing conditions that are not equivalent to the claimed method.

The word "completely" in the limitation requiring the compression coating to cover the core also narrows the claim. A dosage form with an exposed core, an incomplete coating, or a different multilayer structure may present a noninfringement position, subject to the doctrine of equivalents.

What does claim 6 add to the patent scope?

Claim 6 shifts from a precise dissolution endpoint to a structural and functional requirement. The compression coating must rupture after immersion in an aqueous medium for approximately two to six hours.

The claim is potentially broader than claim 1 in one respect because it does not require the exact four-hour and five-hour dissolution results. It remains narrow in other respects because the dosage form must still use:

A drug-containing core;
A disintegrant that provides rupture force;
A complete compression coating;
The listed coating excipient categories;
No coating composition that swells and gels sufficiently to form a diffusion barrier; and
Substantially no natural or synthetic gum.

The claim creates potential design-around opportunities for products that use erosion, osmotic pressure, pH-triggered dissolution, enteric polymer dissolution, or membrane diffusion rather than rupture caused by core disintegration.

What does claim 9 protect?

Claim 9 focuses on the clinical release sequence:

Not more than 10% release before expiry of the lag time;
Substantially all release within approximately one hour after the lag time; and
A lag time between two and six hours after administration.

This claim is directed to a pulsatile or chronotherapeutic delivery pattern. It is particularly relevant to glucocorticosteroid administration intended to align drug release with early-morning inflammatory activity.

Claim 9 may create enforcement complexity because "after administration to the patient" introduces a physiological performance concept, while the claim also relies on measurable release behavior. Product testing, pharmacokinetic data, in vitro-in vivo correlation, and formulation specifications would be important in an infringement dispute.

What dependent claims cover 1 mg and 5 mg prednisone tablets?

Claims 4, 5, 7, 8, 10, and 11 narrow the independent claims to dosage forms containing either 1 mg or 5 mg of prednisone.

Claims	Active ingredient and strength
4, 7, 10	1 mg prednisone
5, 8, 11	5 mg prednisone

These claims are commercially important because 1 mg and 5 mg strengths are commonly used for dose titration and maintenance therapy. A product containing another strength would not literally satisfy these dependent claims, although it could still fall within the corresponding independent claim.

The dependent claims do not require prednisone in every case. They narrow only the amount where prednisone is used. The independent claims continue to cover prednisolone and methylprednisolone without the 1 mg or 5 mg limitation.

What excipients are required by US 9,040,085?

The compression coating must include at least one excipient from a defined group:

Fatty acids, esters, or salts;
Long-chain fatty alcohols;
Polyoxyethylene alkyl ethers;
Polyoxyethylene stearates;
Sugar esters;
Lauroyl macrogol-32 glyceryl; or
Stearoyl macrogol-32 glyceryl.

The claims also permit additional excipients under dependent claims 2 and 3, including:

Cellulosic derivatives;
Other polymers;
Polymethacrylic polymers; and
Alkylcellulose.

The claims exclude a coating that contains ingredients swelling and gelling to such an extent that the coating operates as a diffusion barrier. They also require that the coating contain substantially no natural or synthetic gum.

This negative limitation is central. A formulation using hydroxypropyl methylcellulose, carbomer, xanthan gum, guar gum, alginate, or another polymer in a manner that creates a swelling diffusion membrane may have a stronger noninfringement position. The result depends on the amount, function, and physical behavior of the material in the finished dosage form, not merely its presence in the ingredient list.

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

The patent has meaningful claim density around the specific compression-coating technology but is not a broad monopoly over delayed-release prednisone.

Strengths

The claims combine several limitations that can make a design-around difficult:

Drug identity;
Core-and-coating architecture;
Complete coating coverage;
Disintegrant-driven rupture;
Specified excipient classes;
Exclusion of gum-based and strongly gelling diffusion barriers;
Lag-time requirements; and
Exact dissolution performance in claim 1.

This combination can protect a commercial formulation even where individual elements, such as delayed release or prednisone, are old.

Weaknesses

The same combination creates multiple potential noninfringement routes:

Use of a polymeric diffusion membrane;
Use of an enteric coating;
Use of a pH-dependent coating;
Use of an osmotic delivery system;
Use of multiparticulates or coated granules;
Use of a capsule rather than a compression-coated tablet;
Use of an incomplete or noncompression coating;
Use of a different glucocorticosteroid;
Use of a release lag outside the claimed interval; or
Failure to meet the claim 1 dissolution endpoints.

The patent is strongest against a product that copies the same compression-coated tablet mechanism and release profile. It is weaker against a technically different delayed-release platform.

What products are commercially relevant to this patent?

RAYOS is the principal US commercial reference for delayed-release prednisone. The product contains prednisone in delayed-release tablets and is indicated for selected inflammatory and autoimmune conditions. Its release is delayed so that prednisone becomes available several hours after evening administration.[2]

Lodotra is a related delayed-release modified-release prednisone product marketed outside the United States. It uses a timed-release tablet concept designed for night-time dosing and morning release. Its commercial and patent relevance depends on country-specific approvals, licenses, and formulation rights.

Product or category	Active substance	Release type	Relevance to US 9,040,085
RAYOS	Prednisone	Delayed release	Primary US commercial comparator
Lodotra	Prednisone	Modified or delayed release	International comparator
Conventional prednisone tablets	Prednisone	Immediate release	Generally outside the claims
Prednisolone delayed-release products	Prednisolone	Potentially delayed release	Covered only if all claim limitations are met
Methylprednisolone delayed-release products	Methylprednisolone	Potentially delayed release	Covered only if all claim limitations are met
Enteric-coated steroid products	Various	pH-triggered release	Possible design-around category
Osmotic or membrane systems	Various	Diffusion or osmotic release	Possible design-around category

An immediate-release generic prednisone tablet does not satisfy the compression-coating, lag-time, and dissolution limitations. Conventional prednisone generics therefore do not represent a direct product-level infringement threat under these claims.

What is the FDA and Orange Book status of this patent?

RAYOS was approved by the FDA in 2012 under NDA 202992.[2] The Orange Book is the controlling FDA source for patents listed against an approved small-molecule drug product, including patent numbers, use codes, and listed expiration information.[3]

For commercial diligence, the relevant questions are:

Whether US 9,040,085 is listed against the applicable RAYOS NDA.
Whether it is listed for the product generally or only for a particular method of use.
Whether the listed use code covers the proposed ANDA labeling.
Whether the patent has an unexpired term after any patent-term adjustment.
Whether later-issued patents or continuations remain listed.

The patent is a drug-product patent in the Hatch-Waxman context because its claims are method claims tied to a particular oral dosage form and therapeutic administration. It is not a biologic patent and does not create biosimilar litigation exposure.

The statutory term ordinarily runs for 20 years from the earliest effective US nonprovisional filing date, subject to patent-term adjustment and any applicable patent-term extension. Prednisone is an old active ingredient, so FDA regulatory exclusivity is distinct from the patent term and is not equivalent to new chemical entity exclusivity.[4]

When does US 9,040,085 lose exclusivity?

The patent's enforceability ends at the expiration of its adjusted patent term unless it is earlier cancelled, disclaimed, invalidated, or otherwise limited. The controlling date should be taken from the USPTO patent record and the current Orange Book entry, rather than calculated solely from the issue date.[1,3]

The patent does not receive a new chemical entity exclusivity period because prednisone, prednisolone, and methylprednisolone are established active ingredients. Any historical FDA exclusivity for the delayed-release product would have been limited and separate from the patent term.

For launch planning, a generic applicant must assess both:

The listed patent expiration date; and
Whether an ANDA applicant can obtain approval before that date through a Paragraph IV certification and associated litigation or settlement strategy.

Are there Paragraph IV challenges to US 9,040,085?

A Paragraph IV challenge would assert that the patent is invalid, unenforceable, or not infringed. A generic applicant would typically challenge the patent through an ANDA certification if it seeks approval before the listed patent expiration.

The most credible Paragraph IV theories would likely focus on:

Anticipation and obviousness

A challenger could combine prior-art references concerning:

Compression-coated tablets;
Delayed-release glucocorticosteroids;
Disintegrant-driven rupture;
Hydrophobic excipient coatings;
Timed drug delivery; and
Prednisone chronotherapy.

The claim's defined dissolution profile may create an evidentiary issue. A challenger would need to show that the prior art disclosed or rendered obvious the claimed combination, not merely that each component was separately known.

Indefiniteness

Terms such as "substantially no," "substantially all," "about," "defined core," and "provides a force" could be scrutinized. The specification and prosecution history would determine whether these terms have sufficiently objective boundaries.

Written description and enablement

The breadth of the steroid selection, excipient categories, release intervals, and coating structures could support a challenge if the disclosure does not enable the full claim scope without undue experimentation.

Noninfringement

A generic product could pursue a formulation that avoids one or more required elements, particularly the compression-coating mechanism, listed excipient categories, gum exclusion, or rupture-based release.

No biosimilar pathway applies. Prednisone products are chemically synthesized small molecules and are regulated through ANDAs or, for certain products, other drug-approval pathways rather than the abbreviated biologics pathway.

What patent litigation affects this technology?

The principal litigation risk is formulation-specific rather than active-ingredient-specific. A dispute would likely turn on:

Whether the generic tablet has a compression coating;
Whether the coating completely covers the core;
Whether the core disintegrant creates rupture force;
Whether the coating acts as a diffusion barrier;
Whether gums or gelling polymers are present at a legally significant level;
Whether the release profile falls within the claimed time window; and
Whether the proposed labeling induces the claimed method of administration.

The patent's method format also creates a divided-infringement issue. The claims require administering the dosage form to a patient. A brand owner would normally focus on the generic label, product design, instructions for use, promotional materials, and the predictable use of the product. Under Hatch-Waxman litigation, the proposed labeling and formulation may be evaluated before commercial launch.

A settlement agreement could delay generic entry, authorize an earlier launch, or impose restrictions on strengths or indications. The existence and terms of any settlement should be checked in the FTC's pharmaceutical patent-settlement resources and applicable federal court docket.[5]

What manufacturing and IP barriers matter most?

The principal manufacturing barrier is reproducible control of the rupture event. The product must maintain:

Uniform core composition;
Consistent compression force;
Complete coating coverage;
Stable coating thickness;
Controlled water penetration;
Reliable disintegrant expansion;
Minimal premature leakage; and
Rapid release after rupture.

These parameters can create a practical barrier even if a competitor avoids literal infringement. A generic applicant would also need comparative dissolution data, stability data, bioequivalence evidence, and manufacturing controls acceptable to FDA.

The patent does not prevent all delayed-release steroid development. It creates the greatest risk for a direct copy of the patented compression-coated platform.

How does this patent compare with conventional prednisone patents?

Issue	US 9,040,085	Conventional prednisone patent
Protected subject matter	Method using a specific delayed-release dosage form	May cover composition, indication, salt, or formulation
Active ingredient	Prednisone, prednisolone, or methylprednisolone	Often one active ingredient
Core requirement	Required	Usually not required
Compression coating	Required	Usually not required
Release profile	Central limitation	May be absent or less specific
Immediate-release generic risk	Low under these claims	Depends on claim scope
Biosimilar risk	None	None for small-molecule prednisone
Design-around potential	Moderate to high using different release technology	Depends on the patent

What is the generic launch risk?

Generic launch risk is highest where an ANDA product:

Uses 1 mg or 5 mg prednisone;
Uses a complete compression coating;
Contains one of the listed hydrophobic or surfactant excipients;
Uses a disintegrant-containing core;
Avoids gums but relies on core expansion to rupture the coating;
Produces a two-to-six-hour lag time; and
Matches the RAYOS dissolution profile.

Risk is lower for:

Immediate-release prednisone;
A pH-triggered enteric formulation;
A capsule containing delayed-release beads;
An osmotic system;
A diffusion-membrane product that does not use the claimed rupture mechanism; or
A product with a release lag outside the claimed range.

The strongest launch strategy would usually combine a product-specific noninfringement position with a Paragraph IV invalidity challenge where the commercial value justifies litigation.

Key Takeaways

US 9,040,085 protects a delayed-release glucocorticosteroid method using a rupture-based compression-coated dosage form.
Claims 1, 6, and 9 are independent and use different release-performance tests.
The patent covers prednisone, prednisolone, and methylprednisolone, with dependent claims directed to 1 mg and 5 mg prednisone.
The exclusion of gum-based and strongly gelling diffusion-barrier coatings is a major claim boundary.
Immediate-release prednisone generics generally do not practice the claimed invention.
RAYOS is the primary US commercial product relevant to the patent.
The main generic threat is a delayed-release product that copies the core-expansion and compression-coating architecture.
Biosimilar risk is not relevant because the products are small-molecule drugs.
Exact launch timing depends on the current USPTO term record, Orange Book listing, any Paragraph IV litigation, and any settlement agreement.

FAQs

Does US 9,040,085 cover all delayed-release prednisone tablets?

No. The tablet must use the claimed core, complete compression coating, disintegrant-driven rupture mechanism, specified coating excipients, gum limitation, and release profile.

Can an enteric-coated prednisone product avoid US 9,040,085?

Potentially. An enteric-coated product using pH-dependent dissolution rather than rupture of a compression coating may avoid literal infringement, depending on its complete formulation and release behavior.

Are 1 mg and 5 mg prednisone strengths separately protected?

Yes. Claims 4, 5, 7, 8, 10, and 11 specifically recite 1 mg or 5 mg prednisone. The independent claims are broader and are not limited to those strengths.

Does this patent block generic immediate-release prednisone?

Generally no. Immediate-release prednisone lacks the delayed-release compression-coating and lag-time limitations required by the independent claims.

Is a biosimilar application relevant to this patent?

No. Prednisone, prednisolone, and methylprednisolone are small-molecule active ingredients. The relevant abbreviated pathway is generally an ANDA or another small-molecule FDA pathway, not a biosimilar application.

References

United States Patent and Trademark Office. (2015). US Patent No. 9,040,085 B2. USPTO Patent Center. https://patentcenter.uspto.gov/
U.S. Food and Drug Administration. (2012). RAYOS (prednisone) delayed-release tablets: Prescribing information. https://www.accessdata.fda.gov/
U.S. Food and Drug Administration. (n.d.). Approved drug products with therapeutic equivalence evaluations, Orange Book. https://www.fda.gov/drugs/drug-approvals-and-databases/approved-drug-products-therapeutic-equivalence-evaluations-orange-book
U.S. Food and Drug Administration. (2017). Guidance for industry: Listed drugs, 30-month stays, and approval of ANDAs and 505(b)(2) applications under Hatch-Waxman. https://www.fda.gov/
Federal Trade Commission. (n.d.). Agreements filed with the Federal Trade Commission under the Medicare Prescription Drug, Improvement, and Modernization Act. https://www.ftc.gov/legal-library/browse/agreements-filed-federal-trade-commission-under-medicare-prescription-drug-improvement-modernization-act

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
United Kingdom	0309342.4	Apr 24, 2003

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	512659	⤷ Start Trial
Australia	2004231362	⤷ Start Trial
Brazil	PI0409652	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 9,040,085

Summary for Patent: 9,040,085