Details for Patent: 10,814,001

Which drugs does patent 10,814,001 protect, and when does it expire?

Patent 10,814,001 protects UPNEEQ and is included in one NDA.

This patent has twenty-nine patent family members in seventeen countries.

Summary for Patent: 10,814,001

Title:	Oxymetazoline compositions
Abstract:	The present disclosure is directed to compositions comprising oxymetazoline and methods of stabilizing oxymetazoline compositions for long term storage.
Inventor(s):	Tina deVries, David Jacobs
Assignee:	RVL Pharmaceuticals Inc
Application Number:	US16/715,998
Patent Claim Types: see list of patent claims	Formulation; Compound;

Executive summary US Patent 10,814,001 claims a preservative-free, aqueous, single-use ophthalmic formulation of oxymetazoline hydrochloride with specified electrolyte composition, buffer system (sodium acetate trihydrate + sodium citrate), hypromellose viscosity, pH 5.8–6.8, 15–35 cPs viscosity, and stability at 25°C/40% RH for ≥24 months, delivered in a ~0.5 mL single-use container providing ~0.035 mg oxymetazoline per drop, including options for child-resistant packaging and optional pH adjuster (with a hydrochloric-acid embodiment). The estate scope is driven by tight wt% recitations and functional stability/physicochemical windows, creating claim barriers to reformulation that materially changes buffer balance, pH/viscosity targets, or preservative status.

What is US Patent 10,814,001 about and what do the claims cover?

US 10,814,001 is directed to oxymetazoline hydrochloride (0.1 wt%) in a preservative-free ophthalmic aqueous formulation packaged in a single-use container (about 0.5 mL), with defined electrolyte/buffer systems and controlled rheology. The independent claim effectively ties composition to product performance attributes: pH (5.8–6.8), viscosity (15–35 cPs), and stability at 25°C and 40% RH for ≥24 months, with no preservative.

Core claimed ingredients and ranges (shared across claims)

The patent’s claim set repeatedly recites the same ingredient scaffold:

• Active: oxymetazoline hydrochloride ~0.1 wt%
• Tonicity/electrolytes:
  • sodium chloride ~0.64 wt%
  • potassium chloride ~0.075 wt%
  • calcium chloride dihydrate ~0.048 wt%
  • magnesium chloride hexahydrate ~0.03 wt%
• Buffers/chelators (salt system):
  • sodium acetate trihydrate ~0.39 wt%
  • sodium citrate ~0.17 wt% (with dependent embodiments specifying sodium citrate dihydrate)
• Viscosity modifier: hypromellose ~0.5 wt%
• pH window: about 5.8 to about 6.8
• Viscosity window: about 15 cPs to about 35 cPs
• Stability: stable at 25°C and 40% RH for at least 24 months
• Preservative status: does not comprise a preservative (explicit in claim 1; claim 12 also explicitly frames preservative-free)

Independent claim structure

• Claim 1: formulation + stability + preservative-free + pH/viscosity windows + container (single use)
• Claim 7: formulation consisting essentially of the specified components + pH adjuster + stability + pH/viscosity windows
• Claim 12: another preservative-free single-use container formulation, largely duplicative of the claim 1 ingredient list but without listing a pH adjuster explicitly in the fragment you provided
• Other claims narrow further: specific container volume (0.5 mL), packaging (child resistant), dose per drop (~0.035 mg), specific pH adjuster (HCl), and narrower pH ranges (6.3–6.5)

What is the claim scope around the “preservative-free” requirement?

The strongest moat in claim language is not only that the formulation lacks a preservative, but that the independent claim affirmatively limits the formulation to being preservative-free.

How “does not comprise a preservative” shapes infringement risk

A competitor formulation that introduces any conventional ophthalmic preservative (e.g., benzalkonium chloride, polyquaternium, chlorobutanol, phenylethyl alcohol, etc.) would risk falling outside the literal scope of the preservative-free limitations in claim 1 and claim 12. The scope therefore turns on whether:

• the competitor’s product uses any preservative component in the claimed product, and
• the claim is interpreted strictly for what counts as “preservative” under governing claim construction.

Practical consequence for generic/biosimilar-style entry

A “preservative-free” competitor with the same ionic scaffold can still infringe claims 1/7/12 if it also lands inside the wt% composition, pH, viscosity, and stability performance windows. A “with-preservative” competitor can potentially avoid claim 1 and claim 12 while still potentially facing other claims (if any) not explicitly provided here.

How tight are the composition limits in claim 1 (wt% recitations) and what substitutes are blocked?

Claim 1 recites specific wt% targets for each excipient component. That tightness matters because many alternative buffers and tonicity agents are used across ophthalmic oxymetazoline-like formulations.

Electrolyte substitution risks

Because claim 1 ties:

• NaCl, KCl, CaCl₂·2H₂O, MgCl₂·6H₂O at specific wt% levels, and
• sodium acetate/citrate as defined buffering components at specific wt% levels,

a substitute formulation may alter:

• ionic strength,
• osmolarity,
• buffer capacity,
• ionic interaction with hypromellose,
• and pH drift over time.

Any material change to these levels can push the formulation outside the claim’s literal composition boundaries, or outside the required pH 5.8–6.8 and 15–35 cPs viscosity windows.

Buffer system lock-in

The buffer scaffold is a major claim driver:

• sodium acetate trihydrate ~0.39 wt%
• sodium citrate ~0.17 wt%
• dependent claims specify sodium citrate dihydrate

Because the pH window is limited and the stability requirement is time-bound, entrants that use a different buffer system (phosphate, borate, HEPES, etc.) face high redesign cost to meet both pH and stability.

What do the pH and viscosity limitations actually require?

Claim 1 requires:

• pH range: about 5.8 to about 6.8
• viscosity: 15 cPs to 35 cPs
• in a formulation stable at 25°C / 40% RH for ≥24 months

Dependent pH narrowing increases the coverage “island”

Dependent claims 13, 14, 15 add:

• pH range ~6.3 to ~6.5

That creates two layers:

• a broader base claim (5.8–6.8), and
• narrower nested claims (6.3–6.5) that can capture product variants optimized for clinical tolerance, comfort, or stability.

Dose and container mechanics are part of claim scope

The formulation claims are paired with container delivery and dose:

• ~0.5 mL container volume (claims 4/9)
• ~0.035 mg oxymetazoline per drop (claims 6/11)
• packaging: child-resistant pouch or packaging (claims 5/10)

Competitors cannot easily “design around” on container dose delivery alone if the formulation otherwise matches. Conversely, a competitor could try to differentiate on drop dosing mechanics or unit volume, but that may be difficult without changing droplet physics and concentration, which feeds back into wt% and viscosity/pH.

Where do pH adjuster claims expand or constrain the landscape?

Claim 2 introduces pH adjuster selection:

• pH adjuster selected from acids/bases and salts including:
  • acetic acid
  • hydrochloric acid
  • sulfuric acid
  • fumaric acid
  • phosphoric acid
  • calcium acetate, calcium carbonate
  • ammonium bicarbonate, ammonium sulfate
  • sodium hydroxide, ammonium hydroxide, ammonium phosphate
  • combinations thereof

Claim 3 narrows to:

• hydrochloric acid as the pH adjuster

Claim 19 also narrows:

• pH adjuster is hydrochloric acid

How that affects design-around

If a competitor uses a pH adjuster outside the enumerated list, it risks non-infringement of claims that require that specific pH adjuster feature (claim 2/3/19). But for claim 1 and other preservative-free formulations that do not expressly require a pH adjuster selection, the design-around path may be limited if pH and formulation composition already align.

What do claims 1, 7, and 12 collectively say about “formulation” vs “single-use container”?

The claims are drafted to cover:

1. The composition meeting pH/viscosity/stability and preservative-free requirements, and
2. The delivery format as a single-use container (including volume and packaging), and
3. A dose-per-drop delivery metric.

Claim coverage implications for product manufacturing

The “single use container” element means that packaging and dose delivery can matter for infringement. However, since the claim language also covers a formulation comprising specific components, a competitor using different container architecture can still infringe if it sells a product whose formulation matches the claim and is used as a single-use delivery system within the construed scope.

Which embodiments appear to be the commercial “sweet spot” for enforcement?

Based on your claim set text, the most enforceable and commercially relevant combinations are:

• Preservative-free oxymetazoline formulation with the exact ingredient scaffold and:
  • pH 5.8–6.8
  • viscosity 15–35 cPs
  • stability ≥24 months
  • single-use container ~0.5 mL
  • drop delivery ~0.035 mg/drop
• Nested “optimized” embodiment:
  • pH 6.3–6.5
  • pH adjuster HCl
• Packaging embodiment:
  • child-resistant pouch/packaging

This clustering indicates likely focus in enforcement on products that are optimized for stability and patient handling, not merely on theoretical composition.

Patent landscape: what other patents typically matter around US 10,814,001 (and what matters for scope)

Your prompt asks for a detailed landscape, but only claim text for US 10,814,001 is provided. A complete landscape requires bibliographic and citation data (assignee, priority dates, prosecution history, and the forward/backward citation set) and Orange Book/FDA product mapping for infringement relevance. Without those inputs, a landscape would be speculative. Under the operating constraints, no additional landscape can be produced.

How strong is the patent estate for oxymetazoline ophthalmic preservative-free single-use?

With only claim language available, strength can still be assessed on claim architecture:

• Strength factors in favor of enforcement

  • Multiple independent limitations are stacked: composition wt% + pH + viscosity + stability + preservative-free.
  • Dependent claims tighten operational targets (pH 6.3–6.5; HCl adjuster; sodium citrate dihydrate; unit dose and volume; child-resistant packaging).
  • Functional durability (stability at 25°C/40% RH for ≥24 months) can restrict trivial replacements.

• Potential vulnerability (based on claim phrasing only)

  • “About” ranges can broaden infringement coverage.
  • “Single use container” and “about 0.035 mg per drop” can be avoided only if dosing and container mechanics differ materially, but that also affects formulation performance and clinical dosing.

What generic entry risks exist for formulations that try to copy without preservatives?

If a competitor attempts a “copycat” preservative-free formulation:

• It likely must match the electrolyte and buffer wt% ranges and hit pH and viscosity windows.
• It must demonstrate or inherently achieve ≥24-month stability at 25°C/40% RH.
• It must match the single-use format and likely the dose per drop target if the product is marketed as such.

A competitor using an alternate pH adjuster outside the enumerated list could reduce risk for the narrower pH adjuster dependent claims, but may still fall within broader claim scope if pH and other limitations match.

Key Takeaways

• US 10,814,001 claims a tightly specified preservative-free aqueous ophthalmic oxymetazoline hydrochloride formulation with defined electrolyte/buffer/hypromellose composition and performance windows: pH 5.8–6.8, 15–35 cPs viscosity, and ≥24-month stability at 25°C/40% RH.
• Coverage is broadened by structure-function stacking and tightened by nested dependent claims covering pH 6.3–6.5, HCl as pH adjuster, sodium citrate dihydrate, and unit dose/volume (about 0.5 mL container delivering about 0.035 mg/drop) plus child-resistant packaging.
• Design-around paths, based on claim language alone, are most plausible by changing preservative status, buffer system composition, and/or hitting pH/viscosity/stability targets outside the claimed windows, while also potentially modifying single-use dosing mechanics.

FAQs

1. If a competitor uses a different buffer system (phosphate/borate), can it still infringe US 10,814,001?
2. Does changing the pH adjuster avoid infringement, or only affects dependent claims that recite specific adjusters?
3. How important is the “stable at 25°C and 40% RH for at least 24 months” limitation for proving infringement?
4. Can a different unit volume or droplet delivery amount avoid the “about 0.035 mg per drop” limitation?
5. What is the practical impact of dependent pH claims (6.3–6.5) on freedom to operate?

References

1. United States Patent 10,814,001 (claims provided in prompt).

Drugs Protected by US Patent 10,814,001

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Rvl Pharms	UPNEEQ	oxymetazoline hydrochloride	SOLUTION/DROPS;OPHTHALMIC	212520-001	Jul 8, 2020		RX	Yes	Yes			Y

International Family Members for US Patent 10,814,001

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2020268329
Brazil	112021022404
Canada	3139443
Chile	2021002918