Details for Patent: 10,864,175

Which drugs does patent 10,864,175 protect, and when does it expire?

Patent 10,864,175 protects TONMYA and is included in one NDA.

This patent has fifty-three patent family members in twenty-seven countries.

Summary for Patent: 10,864,175

Title:	Eutectic formulations of cyclobenzaprine hydrochloride and amitriptyline hydrochloride
Abstract:	The present invention relates to pharmaceutical compositions and methods of manufacturing the same, comprising a eutectic of Cyclobenzaprine HCl and mannitol or Amitriptyline HCl and mannitol.
Inventor(s):	Marino Nebuloni, Patrizia Colombo
Assignee:	Tonix Pharma Holdings Ltd , Redox SRL
Application Number:	US16/140,090
Patent Claim Types: see list of patent claims

US Patent 10,864,175 Scope, Claims, and Landscape for Cyclobenzaprine HCl–β-Mannitol Eutectic

Executive summary: US Patent 10,864,175 protects a narrowly defined eutectic composition of cyclobenzaprine hydrochloride (Cyclobenzaprine HCl) and β-mannitol, with fixed weight ranges, a specific molar ratio, and optional physical-form and thermal endpoints (micronization; melting point). The claim set is composition-centric, not process-centric, so infringement risk is driven by whether a product’s bulk composition falls inside the stated weight %, molar ratio, and melting point bands. The patent landscape for this type of eutectic typically includes (i) prior art describing eutectics of cyclobenzaprine salts with sugar alcohols/polyols, (ii) formulation patents that rely on crystallinity or particle size (including micronized APIs), and (iii) later patents that attempt design-around by shifting eutectic ratios, using different polymorphs/excipients, or changing thermal targets.

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What is US Patent 10,864,175 and what does it claim for cyclobenzaprine HCl–β-mannitol eutectics?

Direct answer: US 10,864,175 claims a eutectic consisting of:

• 75% ± 2% cyclobenzaprine HCl by weight
• 25% ± 2% β-mannitol by weight
• optionally a specific molar ratio (claim 2)
• optionally micronized cyclobenzaprine HCl (claim 3)
• optionally a specific melting temperature band (claim 4)

Core claim coverage (independent claim 1)

Claim 1 (composition):
“A eutectic of Cyclobenzaprine HCl and β-mannitol comprising 75% ± 2% cyclobenzaprine HCl and 25% ± 2% β-mannitol by weight.”

Practical scope

• The composition must be a eutectic (not merely a physical mixture). That requirement generally forces an argument about phase behavior and eutectic formation.
• The eutectic must fall within the tight weight tolerances:
  • Cyclobenzaprine HCl: 73% to 77% w/w
  • β-mannitol: 23% to 27% w/w
• Composition-level claims usually capture any dosage form containing that eutectic, unless the patent is limited to a dry intermediate (the claims you provided do not mention dosage form, so the safest reading is composition coverage across formulation contexts, subject to enforcement posture and claim construction).

Secondary claim narrowing (claims 2–4)

Claim 2 (molar ratio constraint):
“The eutectic … wherein the Cyclobenzaprine HCl:β-mannitol molar ratio is 1.76 ± 0.1.”

This narrows the composition beyond weight percent by locking the ratio in molar terms, which can catch design-arounds that keep similar weight % but shift molecular-scale stoichiometry (or vice versa).

Claim 3 (particle size of API):
“… wherein Cyclobenzaprine HCl is micronized Cyclobenzaprine HCl.”

This narrows the claim to products using micronized API to form the eutectic or that preserve that physical state as part of the claimed material.

Claim 4 (thermal endpoint):
“… wherein the eutectic melts at 143.6 ± 3° C.”

This adds an objective characterization. In practice, melting-point-based limitations can be used both ways:

• as a validity/novelty anchor (distinguishing over prior eutectics)
• as a design-around target (shifting phase behavior to land outside the temperature band)

Claim interdependence

• Claim 1 stands alone for weight-defined eutectic.
• Claims 2–4 narrow claim 1’s subject matter by adding further limitations.
• If a product avoids claim 2–4 (molar ratio, micronization, melting range) but still sits within claim 1’s weight and eutectic requirement, claim 1 still creates exposure.

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How do the weight-percent tolerances translate into practical infringement triggers?

Direct answer: Claim 1’s infringement window is defined by 73–77% cyclobenzaprine HCl and 23–27% β-mannitol, by weight, in an actual eutectic.

Weight-range math

If a manufacturer’s product material is within the band:

• Cyclobenzaprine HCl (w/w): 73% to 77%
• β-mannitol (w/w): 23% to 27%
• The windows overlap exactly by design (because only two components are present in claim 1 as written).

What this means for formulation developers

Because the claim is directed to the eutectic, not a finished dosage form, a key legal question becomes whether the “eutectic” is present as the predominant crystalline/solid-state system and meets characterization. Typical evidentiary routes in US patent disputes include:

• DSC (differential scanning calorimetry) and melting onset/peak evaluation
• XRD (powder X-ray diffraction) for presence/absence of distinct phases
• phase diagram or eutectic formation evidence

Your provided claim set does not include exclusivity over salts, polymorphs, or additional excipients. The claims you supplied appear to cover the eutectic composition itself. If a competitor uses additional excipients or diluents, they may still infringe if the marketed API/excipient system includes the claimed eutectic material as such.

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What is the cyclobenzaprine HCl:β-mannitol molar ratio band in claim 2 and how can it be used to design around?

Direct answer: Claim 2 fixes the molar ratio at 1.76 ± 0.1 (nominal 1.66 to 1.86).

Why molar ratio matters vs weight %

Weight % tolerances can be met while shifting molar ratio if one component has different effective molecular weight due to:

• different salt form (not applicable if cyclobenzaprine is always HCl)
• inclusion of hydrates or solvate formation (if β-mannitol or cyclobenzaprine exists in an associated solid-state form, though β-mannitol is typically not “variable” like salts)
• impurities or deviations from assumed molecular weights (minor)

Practically, a design-around for claim 2 often targets:

• changing the eutectic stoichiometry used to prepare the solid
• using different polyols or excipient systems that yield a eutectic at a different ratio
• changing the eutectic endpoints so the resulting eutectic does not match claim 2’s molar ratio

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When does the micronized-cyclobenzaprine limitation (claim 3) create narrower exposure?

Direct answer: Claim 3 requires the cyclobenzaprine HCl in the eutectic to be micronized.

Claim 3 as a design-around lever

A competitor can attempt to avoid claim 3 by using non-micronized API. However, two legal/technical points drive enforceability:

1. If claim 1 is satisfied, claim 3 avoidance does not remove claim 1 exposure.
2. “Micronized” is often a contested technical term. If the patent specification defines micron size, that definition would control. The claim text you provided does not include a numeric particle-size cutoff.

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How strong is the melting-point limitation in claim 4 for cyclobenzaprine HCl–β-mannitol eutectics?

Direct answer: Claim 4 narrows to a eutectic that melts at 143.6 ± 3° C. (nominal band 140.6 to 146.6° C.).

Role in litigation

Melting point is an objective measurement but can vary based on:

• heating rate in DSC
• sample preparation
• calibration and instrument settings
• eutectic purity and thermal history

Even with those variables, claim 4 can still be strong if the specification ties the melting measurement method to a standard test.

Design-around strategy

To avoid claim 4, a competitor typically targets:

• composition shift so the eutectic temperature moves outside the band
• solid-state modification that alters thermal behavior
• use of a different excipient system that yields a different eutectic melting profile

Again, avoidance of claim 4 does not remove claim 1 or claim 2 if those are still met.

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What patent estate surrounds this kind of eutectic: where do prior art and adjacent IP usually sit?

Direct answer: For cyclobenzaprine solid-state/formulation inventions, the surrounding IP estate usually clusters into four buckets:

1. Eutectic/co-crystal/salt–polyol systems (composition inventions)
2. Particle-size control and micronization for dissolution/bioavailability (often process- or starting-material claims)
3. Thermal and solid-state characterization (DSC/XRD-defined solid forms)
4. Formulation dosage forms (compressed tablets, granules, controlled release blends) that incorporate the solid intermediate

US 10,864,175 as presented is primarily in bucket (1) and partly (2) and (4).

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How does US 10,864,175 compare with typical formulation patents for cyclobenzaprine products?

Direct answer: Compared with standard cyclobenzaprine formulation patents that claim:

• a tablet with a blend ratio,
• a controlled-release matrix,
• or a method of preparing a formulation,

US 10,864,175 is narrower: it claims a specific eutectic composition with fixed quantitative bands and optional characterization limits.

Infringement surface area

• Higher risk for competitors using the same eutectic material as an intermediate.
• Lower risk for competitors whose products use different solid-state systems (different excipient, different eutectic ratio, or different eutectic identity).

Litigation posture

In disputes, the patentee’s strongest route usually combines:

• compositional analysis demonstrating the weight % bands
• DSC showing eutectic melting behavior
• XRD demonstrating eutectic formation (or absence of separate phases)

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What generic entry risks exist if a rival challenges formulation IP tied to eutectics?

Direct answer: Generic entry risk is driven by whether the generic can:

1. use an alternative solid-state system (not the claimed eutectic), or
2. use a eutectic that shifts outside the claim’s weight %, molar ratio, micronization, and melting parameters.

Paragraph IV landscape relevance

If cyclobenzaprine (or a product using this eutectic) is under Hatch-Waxman, Paragraph IV challenges typically focus on:

• listed Orange Book patents,
• exclusivity expiration,
• and whether the generic’s formulation avoids infringement.

Because US 10,864,175 appears to be an API/excipient eutectic composition claim, a Paragraph IV filer must do solid-state characterization and provide a non-infringement theory aligned to the claim numbers above.

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What regulatory status would this patent typically interact with in the US?

Direct answer: This kind of solid-state composition patent most commonly appears on the Orange Book as a listed patent for an NDA or ANDA product covering either:

• a drug substance intermediate,
• or a formulation that contains the intermediate.

Once listed, it can block approval timing if not addressed by the generic with:

• carve-out to non-infringing formulations,
• licensing,
• or non-infringement/invalidity positions via Paragraph IV.

(Your prompt did not supply the Orange Book listing details for the specific NDA/ANDA tied to US 10,864,175, so no product-level regulatory timeline can be stated from the claim text alone.)

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What would constitute literal infringement versus non-infringement for US 10,864,175?

Direct answer: Literal infringement requires the accused material to meet the claimed eutectic composition elements.

Literal infringement elements (claim 1)

To fall within claim 1 as provided, the product must contain or consist of:

• a eutectic of cyclobenzaprine HCl and β-mannitol
• with cyclobenzaprine HCl at 73–77% w/w
• β-mannitol at 23–27% w/w

Optional limitations in dependent claims add further requirements:

• claim 2: molar ratio 1.66–1.86
• claim 3: micronized cyclobenzaprine HCl
• claim 4: melting point 140.6–146.6° C.

Common non-infringement routes

• Use a different excipient than β-mannitol
• Use a different cyclobenzaprine salt form
• Maintain approximate weight % but shift eutectic identity so it does not meet “eutectic” characterization under claim interpretation
• Shift composition so the weight or molar ratio lands outside the bands
• Engineer thermal behavior so melting lands outside the claim 4 window (relevant for claim 4 only)

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How can competitors design around US 10,864,175 while staying within cyclobenzaprine solid-state formulation goals?

Direct answer: The claim’s numeric bands make “inside/outside” engineering possible, and competitors usually pursue one of three approaches:

1. Change composition bands: shift weight %, molar ratio, or both.
2. Change physical state: avoid micronized API or change thermal behavior outside the melting range.
3. Change solid-state system: substitute β-mannitol or avoid eutectic formation via different crystallization strategies to create a different solid form.

Because claim 1 is already narrow, the easiest path is usually to avoid forming the specific eutectic with the stated weight ratio.

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Key Takeaways

• US 10,864,175 is composition-anchored: it protects a cyclobenzaprine HCl–β-mannitol eutectic with 73–77% w/w cyclobenzaprine HCl and 23–27% w/w β-mannitol.
• Dependent claims add measurable constraints: molar ratio 1.66–1.86 (claim 2), micronized API (claim 3), and melting point 140.6–146.6°C (claim 4).
• Design-around is feasible by moving outside the weight bands, molar ratio band, and thermal window, or by avoiding β-mannitol eutectics altogether.
• The infringement inquiry is primarily solid-state characterization plus quantitative composition: DSC for eutectic/melting, compositional assays for weight %, and particle-size evidence when claim 3 is asserted.

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FAQs

1) Does US 10,864,175 cover tablet formulations containing the eutectic?

The claim set you provided is directed to the eutectic composition. Coverage for tablets depends on how the eutectic is incorporated, but the claim language supports composition-based protection regardless of final dosage form, subject to claim construction and infringement proof.

2) If a product matches the weight %, but the melting point is outside 143.6 ± 3°C, does it still infringe?

It can still infringe claim 1 if the eutectic and weight bands are met, since claim 4’s melting-point restriction applies only to the dependent claim 4.

3) Can a generic avoid infringement by changing only cyclobenzaprine particle size?

Avoiding micronization may avoid claim 3 but does not avoid claim 1 if the composition eutectic and weight ranges are still met.

4) What is the most direct experimental evidence to enforce or defeat claim 1?

Quantitative composition (to show the 73–77%/23–27% w/w bands) and solid-state characterization to show the material is an actual eutectic, typically supported by DSC (and often XRD).

5) What parameters are easiest to move for a design-around?

The patent includes narrow numeric bands, so composition and thermal behavior are the most direct levers. Moving outside the weight % and molar ratio bands is often the most robust non-infringement route.

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References

1. US Patent 10,864,175 (claims as provided in prompt).

Drugs Protected by US Patent 10,864,175

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Tonix	TONMYA	cyclobenzaprine hydrochloride	TABLET;SUBLINGUAL	219428-001	Aug 15, 2025		RX	Yes	Yes			Y

International Family Members for US Patent 10,864,175

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2014233277
Brazil	112015022095
Canada	2904812
Canada	3119755
China	105142730
China	110152005
Cyprus	1122740