US Patent 10,130,585: Colchicine Sustained-Release Formulation Claims, Patent Scope, Expiration and Competitive Landscape

US Patent 10,130,585 protects selected low-dose colchicine sustained-release tablets and their use in cardiovascular disease. The patent is narrow in formulation architecture but potentially significant for a product that combines a colchicine dose of no more than 0.6 mg, specific HPMC grades, a 25% to 30% release-retarding phase, lactose, and a homogeneous tablet structure. The principal commercial risk is not ordinary immediate-release colchicine. It is a competing sustained-release tablet that reproduces the required excipient composition and release profile while being administered for a claimed cardiovascular indication.

The patent does not, based on the supplied claims alone, establish protection over all colchicine products, all cardiovascular uses, or all extended-release technologies. Its enforceability depends on the exact formulation, claim construction, prosecution history, validity record, patent-term data, and any FDA-approved product linked to the patent.

What does US Patent 10,130,585 protect?

The patent claims methods of treating cardiovascular disease by administering a specific sustained-release colchicine tablet. Claims 1 and 13 are the independent claims. Both require a combination of active pharmaceutical ingredient, granulation technology, release-retarding excipients, tablet form, and homogeneity.

Required feature	Claim 1	Claim 13
Colchicine dose	Not more than 0.6 mg	Not more than 0.6 mg
Granule binder	HPMC 6 mPa·s, 1% to 30% w/w	HPMC 6 mPa·s, 1% to 30% w/w
Release-retarding phase	25% to 30% w/w	About 25% to 30% w/w
Retarding composition	Equal parts HPMC 4000 mPa·s and lactose monohydrate	Equal parts HPMC 4000 mPa·s and lactose monohydrate
Tablet	Required	Required
Homogeneous formulation	Required	Required
First lactose filling agent	10% to 80% w/w	10% to 80% w/w
Second lactose filling agent	10% to 30% w/w	10% to 50% w/w
Oral administration	Expressly required	Administration required; oral route is not stated in the independent claim
Release limitation	Added by claim 7	Added by claim 25

The core inventive combination is not colchicine alone. It is the interaction between a low colchicine load, a low-viscosity HPMC granulation binder, a high-viscosity HPMC/lactose retarding phase, and a homogeneous tablet.

How do claims 1 and 13 differ?

Claim 1 requires oral administration and limits the second lactose filling agent to 10% to 30% of the formulation. Claim 13 permits a broader second lactose range of 10% to 50% and does not expressly state that administration is oral.

Claim 13 also states that the formulation comprises a binder in the granules and later recites a binder again in dependent claim 19. That drafting structure may create claim-construction issues because the independent claim already requires HPMC 6 mPa·s as a binder, while claim 19 identifies broader additional binder categories.

The two independent claims create overlapping but nonidentical infringement paths:

A product administered orally for a claimed cardiovascular treatment may fall within claim 1 if it meets the tighter lactose range.
A product outside claim 1's second-lactose range may still fall within claim 13 if it meets the broader formulation limitations.
A product with the claimed formulation but used outside the cardiovascular indications may avoid method-of-use infringement, subject to induced-infringement and label-based theories.

What cardiovascular diseases are covered?

Claims 2 and 14 identify four principal cardiovascular applications:

Acute pericarditis
Recurrent pericarditis
Post-pericardiotomy syndrome
Cardiovascular events in subjects with stable coronary disease

Claims 3 and 15 add treatment of acute cardiovascular disease when the patient concurrently receives an agent for an acute cardiovascular event. The listed events are acute coronary syndrome, out-of-hospital cardiac arrest, and noncardioembolic ischemic stroke.

Claims 4 and 16 identify atorvastatin, rosuvastatin, simvastatin, and pravastatin as examples of concurrent therapy.

The dependent claims therefore narrow the treatment field rather than create broad protection for colchicine in cardiovascular medicine. A competing product used for gout or familial Mediterranean fever would not fall within these cardiovascular method claims solely because it contains colchicine.

What formulation components are protected?

The formulation limitations are unusually detailed for a method claim.

Colchicine dose

The formulation must contain no more than 0.6 mg of colchicine or a pharmaceutically acceptable salt. Claim 17 narrows claim 13 to no more than 0.50 mg.

The dose limitation creates a meaningful design-around opportunity. A formulation containing 0.61 mg would not literally satisfy the “not more than 0.6 mg” limitation, although other claims or equivalents could become relevant depending on prosecution history.

HPMC binder

The granules must contain HPMC with a viscosity of 6 mPa·s in an amount of 1% to 30% w/w. This is a specific grade and concentration range, not a generic requirement for any cellulose-based binder.

A formulation using PVP, starch, HPC, or a materially different HPMC viscosity grade as the only granulation binder may avoid literal infringement of this limitation. Claim 19 lists broader binder categories, but it depends on claim 13 and does not eliminate the independent claim's HPMC 6 mPa·s requirement.

Release-retarding phase

The release-retarding agent must comprise equal parts of:

HPMC with a viscosity grade of 4000 mPa·s; and
Lactose monohydrate.

The total retarding phase must be approximately 25% to 30% w/w. This limitation is central to claim scope. Replacing lactose with another diluent, changing the ratio materially, or placing the HPMC in a different structural phase may provide a design-around argument.

“Equal parts” may be construed as a 1:1 ratio, subject to ordinary manufacturing tolerances and the prosecution record. The use of “about” in the total percentage range introduces a potentially disputed boundary.

Release profile

Claims 7 and 25 require that less than about 70% of colchicine be released within about two hours at 37°C.

The claims supplied do not specify the dissolution apparatus, medium, agitation speed, sampling method, or analytical method. Those omissions may create disputes over whether a competing product meets the release limitation and whether the claim provides an objective test for infringement.

Excipients

The claims list extensive optional excipient classes, including:

Starch, gelatin, PVP, microcrystalline cellulose, HPC, and polyvinyl alcohol
Lactose, sucrose, trehalose, maltose, mannitol, and sorbitol
Croscarmellose sodium, crospovidone, alginates, cross-linked PVP, and sodium starch glycolate
Colloidal silicon dioxide, talc, magnesium trisilicate, and tribasic calcium phosphate
Magnesium stearate, glyceryl behenate, stearic acid, sodium stearyl fumarate, and related lubricants

Claims 10 and 22 set the glidant range at 0.5% to 5% w/w. Claims 12 and 23 set the lubricant range at 0.5% to 5% w/w.

These dependent claims provide fallback positions, but they also make the claim set vulnerable to prior-art combinations using standard pharmaceutical excipients.

How strong is the patent estate for US 10,130,585?

The patent appears stronger against close-copy sustained-release tablets than against alternative controlled-release technologies.

Risk category	Assessment	Reason
Exact formulation copy	High	Multiple quantitative and qualitative limitations align around a specific formulation
Immediate-release colchicine	Low	Does not ordinarily contain the claimed sustained-release architecture
Different controlled-release polymer system	Moderate to low	May avoid HPMC grades, lactose ratio, or retarding-phase limitations
Dose above 0.6 mg	Potentially low	Fails a central numerical limitation
Dose at 0.5 mg	High if other elements match	Specifically contemplated by claim 17
Cardiovascular use	High when labeled for listed indications	Method claims focus on the treatment context
Generic substitution for gout	Low	The claimed disease and treatment steps are cardiovascular
Formulation-only manufacture	Limited under these claims	The independent claims are method claims requiring administration

The primary validity risks are obviousness and anticipation. HPMC, lactose, granulation, matrix tablets, and colchicine were individually known pharmaceutical technologies. The patentee's strongest position is the specific combination and any demonstrated release or tolerability advantage tied to that combination.

Potential claim vulnerabilities include:

Obviousness: A challenger could combine prior art teaching low-dose colchicine with prior art matrix-tablet systems using HPMC and lactose.
Anticipation: A single prior-art reference disclosing the same dose, HPMC grades, percentages, tablet structure, and therapeutic use could defeat a claim.
Indefiniteness: “About,” “equal parts,” and “homogeneous” may require construction.
Written description and enablement: The broad lists of polymers, fillers, glidants, lubricants, diseases, and treatment combinations may be challenged if the specification does not support the full claim breadth.
Inconsistent scope: Claim 13's broader lactose range and the repeated binder language in claim 19 may generate interpretation disputes.

When does US Patent 10,130,585 lose exclusivity?

The grant date was November 20, 2018, according to the patent record. A United States utility patent generally expires 20 years from the earliest effective nonprovisional or international application filing date, subject to patent-term adjustment, patent-term extension, terminal disclaimers, and other statutory adjustments (U.S. Patent No. 10,130,585, 2018; 35 U.S.C. §§ 154, 156).

The grant date alone does not establish the expiration date. The claims supplied do not include the earliest priority date, patent-term adjustment, terminal disclaimer, or any patent-term extension. An exact expiration date therefore cannot be derived from the claim text.

The commercial exclusivity period may also differ from patent life. FDA regulatory exclusivity depends on the approved drug application and is separate from patent protection.

What is the FDA and Orange Book status?

US Patent 10,130,585 is not automatically an Orange Book patent merely because it covers a drug formulation or method of treatment. Orange Book listing is tied to an approved new drug application and the sponsor's submission of patent information that meets FDA requirements (FDA, 2024a).

The supplied patent claims do not identify:

An NDA number
An approved product name
A listed applicant
A corresponding Orange Book listing
A patent-use code
A Paragraph IV certification
A final FDA determination regarding listing eligibility

The relevant commercial distinction is between this patent and approved colchicine products:

Product	Active ingredient	General dosage form	Relevance to US 10,130,585
Colcrys	Colchicine 0.6 mg	Immediate-release tablet	Dose overlaps, but release architecture generally differs
Mitigare	Colchicine 0.6 mg	Capsule	Dose overlaps, but capsule and release limitations may differ
Generic colchicine	Colchicine	Immediate-release tablets/capsules	Usually outside the claimed sustained-release formulation
Lodoco	Colchicine 0.5 mg	Tablet	Cardiovascular indication and dose overlap; formulation and release profile must be compared claim element by claim element

FDA approved colchicine for several indications over time, including gout-related conditions and familial Mediterranean fever. FDA approved Lodoco for reducing the risk of myocardial infarction, stroke, coronary revascularization, and cardiovascular death in adults with atherosclerotic disease or multiple cardiovascular risk factors (FDA, 2023; FDA, 2024b). Approval of a 0.5 mg cardiovascular colchicine product creates commercial overlap with the dose and method portions of the patent, but it does not establish infringement without proof of the claimed sustained-release formulation.

Which companies are challenging US Patent 10,130,585?

No Paragraph IV challenger, ANDA number, or patent litigation matter can be established from the claims supplied. A Paragraph IV certification would be relevant only if the patent were listed for an approved reference product and an ANDA applicant sought approval for a product referencing that drug.

The practical challenger groups are:

Generic manufacturers developing immediate-release colchicine
Generic manufacturers developing low-dose cardiovascular colchicine
Sponsors developing sustained-release colchicine tablets
Innovators pursuing alternative matrix polymers or multiparticulate delivery systems
Companies relying on a label that excludes the patented cardiovascular uses

A generic applicant could pursue several paths:

File with a Paragraph IV certification if the patent is Orange Book-listed.
File a section viii statement excluding patented methods of use, if the approved labeling and patent-use code permit it.
Design around the sustained-release formulation.
Challenge validity or enforceability in district court after a Paragraph IV notice.

The Hatch-Waxman framework does not automatically apply to every formulation or method patent. Orange Book listing and the reference-product relationship control the available ANDA pathway (21 U.S.C. § 355).

What generic launch risks exist?

Launch before patent expiration

A launch before expiration could create substantial risk if the product matches the HPMC/lactose formulation and carries cardiovascular labeling that practices claims 2, 14, 17, or 24. The risk is lower for an immediate-release product or a product using a different controlled-release mechanism.

Skinny-label launch

A label excluding acute pericarditis, recurrent pericarditis, PPS, and the specified cardiovascular-event uses could reduce induced-infringement exposure. It would not eliminate risk if the product is marketed, promoted, or used in a manner that encourages the patented methods.

Formulation design-around

The most direct design-around strategies would target:

Colchicine dose above 0.6 mg, where clinically and regulatorily acceptable
A non-HPMC granulation binder
A different HPMC viscosity grade
A non-lactose release-retarding phase
A retarding phase outside the claimed concentration
A capsule, multiparticulate, osmotic, coated, or other delivery system
A release profile that does not meet the two-hour limitation

Each design-around must be assessed against all claims, including dependent claims and any continuation patents.

Is there biosimilar risk?

There is no conventional biosimilar risk. Colchicine is a small-molecule drug, not a biological product regulated through the biosimilar pathway under the Public Health Service Act. Competitive entry would generally involve generic-drug, hybrid, or full NDA pathways depending on the product's formulation and clinical differences (FDA, 2024c).

The principal risk is therefore generic or follow-on formulation competition, not biosimilar substitution.

What litigation and settlement issues matter?

A reliable litigation assessment requires the patent's docket history, prosecution history, assignment records, terminal-disclaimer records, and any related continuations. The supplied claims do not identify a complaint, district court, PTAB proceeding, settlement agreement, or license.

For diligence, the highest-value litigation questions are:

Whether the patent survived post-grant or inter partes review
Whether the claims were narrowed during prosecution
Whether “equal parts” was argued as a strict 1:1 limitation
Whether the patentee distinguished prior art based on the two-hour release profile
Whether any settlement restricts generic filing, launch, or formulation design
Whether continuation patents protect additional cardiovascular uses or dosage forms

Prosecution statements may materially limit later doctrine-of-equivalents arguments. A narrowing amendment concerning HPMC grade, lactose content, or colchicine dose would be particularly important.

What licensing opportunities does the patent create?

The patent could have licensing value for a sponsor developing:

A 0.5 mg once-daily cardiovascular colchicine product
A sustained-release pericarditis treatment
A lower-exposure colchicine formulation intended to improve tolerability
A product combining cardiovascular colchicine therapy with statins

License value depends on whether the patent covers a commercially viable approved product, whether the patent is listed or enforceable, the remaining term, and whether continuation patents extend the estate. A license limited to the disclosed formulation would be narrower than a license covering cardiovascular method claims, manufacturing know-how, clinical data, and regulatory rights.

Key Takeaways

US Patent 10,130,585 is a formulation-specific cardiovascular method patent for low-dose sustained-release colchicine tablets.
Claims 1 and 13 require HPMC 6 mPa·s in the granules, HPMC 4000 mPa·s plus lactose in equal parts, a 25% to 30% retarding phase, and a homogeneous tablet.
Claims 7 and 25 add a release requirement of less than about 70% colchicine release within about two hours at 37°C.
The patent is most relevant to low-dose sustained-release cardiovascular colchicine, not ordinary immediate-release colchicine for gout.
Claim 17 specifically reaches formulations containing no more than 0.50 mg colchicine.
The principal validity risks are obviousness, anticipation, indefiniteness, and written-description support for broad excipient and disease lists.
An exact expiration date cannot be established from the claims or grant date alone.
The claims supplied do not establish an Orange Book listing, Paragraph IV challenge, litigation matter, or settlement.
Colchicine has no conventional biosimilar pathway; the competitive threat is generic and follow-on formulation entry.
The most credible design-arounds change the polymer system, lactose architecture, dose, dosage form, or release mechanism.

FAQs

Does US Patent 10,130,585 cover Colcrys?

Not automatically. Colcrys is a 0.6 mg colchicine product, but the patent requires a specific sustained-release tablet formulation. A standard immediate-release Colcrys formulation would generally lack the claimed HPMC/lactose release-retarding architecture.

Does the patent cover Lodoco?

Only if the Lodoco formulation and its labeled use satisfy every limitation of an asserted claim. The 0.5 mg dose and cardiovascular indication create overlap, but dose and indication alone are insufficient.

Can a generic launch an immediate-release colchicine product?

The claims supplied primarily target sustained-release tablets used for cardiovascular treatment. An immediate-release generic may avoid these particular claims, subject to other patents and regulatory exclusivities.

Is a 0.5 mg colchicine tablet automatically infringing?

No. The dose is only one limitation. The product would also need to satisfy the specified HPMC binder, HPMC/lactose retarding phase, percentage ranges, tablet, homogeneity, and applicable treatment limitations.

Can a company avoid the patent by using a capsule?

Potentially, but not categorically. The independent claims require the sustained-release formulation to be in tablet form. A capsule could avoid literal infringement of that limitation, although related patent claims or continuation patents may cover other dosage forms.

References

Food and Drug Administration. (2023). FDA approves first oral colchicine product to reduce cardiovascular risk. U.S. Department of Health and Human Services.
Food and Drug Administration. (2024a). Approved drug products with therapeutic equivalence evaluations. U.S. Department of Health and Human Services.
Food and Drug Administration. (2024b). Drugs@FDA: FDA-approved drug products. U.S. Department of Health and Human Services.
Food and Drug Administration. (2024c). Biosimilar and interchangeable biologic products. U.S. Department of Health and Human Services.
United States Patent No. 10,130,585. (2018). Sustained-release colchicine formulation and methods of treatment. United States Patent and Trademark Office.
United States Code. (2024). 21 U.S.C. § 355, New drugs.
United States Code. (2024). 35 U.S.C. §§ 154, 156, Contents and term of patents; extension of patent term.

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Agepha Pharma Fz	LODOCO	colchicine	TABLET;ORAL	215727-001	Jun 16, 2023		RX	Yes	Yes	10,130,585	⤷ Start Trial				A METHOD OF TREATING CARDIOVASCULAR DISEASE	⤷ Start Trial
>Applicant	>Tradename	>Generic Name	>Dosage	>NDA	>Approval Date	>TE	>Type	>RLD	>RS	>Patent No.	>Patent Expiration	>Product	>Substance	>Delist Req.	>Patented / Exclusive Use	>Submissiondate

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2014255434	⤷ Start Trial
Australia	2019201048	⤷ Start Trial
Australia	2020294268	⤷ Start Trial
Australia	2024205185	⤷ Start Trial
Brazil	112015026418	⤷ Start Trial
Canada	2909370	⤷ Start Trial
Canada	3255918	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 10,130,585

Which drugs does patent 10,130,585 protect, and when does it expire?

Summary for Patent: 10,130,585