Details for Patent: 12,605,363

Which drugs does patent 12,605,363 protect, and when does it expire?

Patent 12,605,363 protects UPNEEQ and is included in one NDA.

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

Summary for Patent: 12,605,363

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:	Revitalid Inc , RVL Pharmaceuticals Inc
Application Number:	US18/146,127
Patent Claim Types: see list of patent claims	Use; Formulation; Compound;

Scope and Claims Analysis for US Patent 12,605,363 (Oxymetazoline Hydrochloride Preservative-Free Ophthalmic Formulation for Ptosis)

US Patent 12,605,363 claims a highly specified aqueous, sterile, preservative-free ophthalmic formulation for ptosis that combines: (1) a narrow oxymetazoline hydrochloride (about 0.1 wt%) dose per drop (about 0.035 mg/drop); (2) defined tonicity and ionic makeup (NaCl, KCl, CaCl2, MgCl2); (3) buffered systems (0.05 to 1.0 wt% buffer; dependent claims specify sodium acetate and sodium citrate at specific hydration states and wt%); (4) viscosity target windows (15-35 cPs); (5) a maintained pH band (about 5.8 to 6.8, with specific 6.3-6.5 subset claims); and (6) an unusually emphasized shelf/holding stability requirement: maintaining key physical parameters for 24 months (and for certain embodiments, maintaining them for 6 months with narrowed osmolality). The patent’s enforceable core is the specific combination of oxymetazoline concentration, multi-ion composition, preservative-free ocular dosing, and multi-parameter stability over long periods.

What is covered (high level)

• Drug/target: oxymetazoline hydrochloride ophthalmic formulation for treating ptosis.
• Dosage form: aqueous, sterile, preservative-free.
• Key in-claim constraints: pH 5.8-6.8 maintained for 24 months; viscosity 15-35 cPs; osmolality 290-365 mOsm/kg (some claims narrow to 290-330 mOsm/kg for 6 months); delivering ~0.035 mg oxymetazoline per drop.

What is not broadly covered (based on claim language)

• No broad genus claims to “oxymetazoline ophthalmic formulations” generally; the claims are narrow to defined wt% ranges, specific electrolyte/buffer systems, and strict stability performance.
• No claimed packaging regimen, drop size, or device mechanics beyond the “per drop” dose parameter.

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What does US Patent 12,605,363 claim protect for ptosis with oxymetazoline hydrochloride?

Core independent claim 1: what the claim requires

Claim 1 is an apparatus-free formulation claim with multiple simultaneous limitations:

1. Formulation type
   • aqueous ophthalmic, sterile
   • preservative-free
2. Actives and electrolytes
   • about 0.1 wt% oxymetazoline hydrochloride
   • about 0.64 wt% sodium chloride
   • about 0.075 wt% potassium chloride
   • about 0.048 wt% calcium chloride
   • about 0.03 wt% magnesium chloride
3. Buffer content and identity
   • 0.05 wt% to 1.0 wt% one or more buffers
4. Viscosity modifier
   • about 0.5 wt% hypromellose
5. pH and stability requirement
   • pH about 5.8 to about 6.8
   • maintains that pH band for 24 months
6. Dose per drop
   • delivers about 0.035 mg oxymetazoline hydrochloride per drop
7. pH adjustment
   • hydrochloric acid (as an ingredient within the formulation system)
8. Solvent
   • water

Enforcement implication: A competitor that changes the buffer identity, removes hypromellose, changes the electrolyte makeup, or fails to meet the 24-month maintained pH band would fall outside claim 1. Because the claim is a multi-parameter conjunction, “almost the same” compositions are not automatically infringing unless they meet all limitations.

Independent claim 11: what changes versus claim 1

Claim 11 is also an ophthalmic sterile preservative-free formulation for ptosis, but it shifts how viscosity is characterized:

• It recites oxymetazoline (about 0.1 wt%), electrolytes (NaCl, KCl, CaCl2, MgCl2), and buffer identities at specific wt% in the independent claim (sodium acetate and sodium citrate).
• It includes hydrochloric acid and water.
• It uses a general “about 0.5 wt% of a viscosity modifier” and then dependent claims specify hypromellose.

Key difference: Claim 11’s independent structure ties the buffer system directly into the main claim body (0.39 wt% sodium acetate and 0.17 wt% sodium citrate) and emphasizes viscosity maintenance over 24 months in addition to pH and drop-dose.

Claim architecture: how dependent claims narrow

Dependent claims 2-5 and 12-15 and 6-10 and 16-20 split into:

• Buffer identity (claims 2-4, 14)
• Hydration states (claim 4, 14)
• Salt hydrates for CaCl2 and MgCl2 (claim 5, 15)
• Specific pH sub-range (claim 6, claim 17)
• Viscosity window (claim 7)
• Osmolality windows (claims 8, 10, 18, 20)
• Multi-parameter stability over time (claims 9 and 19, plus 10 and 20)

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How narrow are the buffer, tonicity, and viscosity limitations in US 12,605,363?

Buffers: genus to specific salts

• Claim 1 allows 0.05 to 1.0 wt% one or more buffers (genus).
• Claim 2 narrows to buffers comprising sodium acetate and sodium citrate.
• Claim 3 further narrows to ~0.39 wt% sodium acetate and ~0.17 wt% sodium citrate.
• Claim 4 narrows the hydration states to:
  • sodium acetate trihydrate
  • sodium citrate dihydrate
• Claim 11 hard-codes sodium acetate and sodium citrate at those specific wt% levels in the independent claim.

Practical consequence: The broadest infringement hook is claim 1’s buffer genus. The strongest and most defensible subset is the sodium acetate/sodium citrate system with specific hydration forms.

Viscosity: numeric window and stability emphasis

• Claim 7: viscosity 15-35 cPs.
• Claim 9: maintains pH 5.8-6.8, viscosity 15-35 cPs, and osmolality 290-365 mOsm/kg for 24 months.
• Claim 11: viscosity 15-35 cPs maintained for 24 months.
• Claim 13 and claim 12-13: viscosity modifier is hypromellose at about 0.5 wt%.

Practical consequence: A formulation that holds pH and osmolality but drifts in viscosity outside 15-35 cPs over 24 months weakens infringement risk. Conversely, designs that match viscosity without the specified electrolyte/buffer composition still may avoid claim 1.

Osmolality: broad for 24 months, narrower for 6 months

• Claim 8: osmolality 290-365 mOsm/kg.
• Claim 10: maintains pH 5.8-6.8 and osmolality 290-330 mOsm/kg for 6 months.
• Claim 9 and claim 19: maintain osmolality 290-365 mOsm/kg for 24 months.

Practical consequence: The 24-month osmolality band is wider than the 6-month band, suggesting different design targets for shelf versus accelerated/short-term conditions. The time-period language makes testing protocol and stability study interpretation highly relevant to infringement analysis.

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How do the stability requirements (pH and physicochemical parameters) expand or constrain infringement?

24-month “maintains” language creates a performance claim posture

Claims 1, 9, 11, 19 are anchored on the formulation “maintains” specified parameter ranges for 24 months. That structure shifts the infringement focus from composition alone to composition-plus-performance over time.

• Claim 1: maintains pH 5.8-6.8 for 24 months.
• Claim 9: maintains pH + viscosity + osmolality for 24 months.
• Claim 11: maintains viscosity for 24 months.
• Claim 19: maintains pH + viscosity + osmolality for 24 months.

Time-based narrowing: 6-month embodiment exists

• Claim 10 and claim 20: maintain pH 5.8-6.8 and a narrower osmolality band (290-330 mOsm/kg) for 6 months.
• This provides an alternate “lower-time” infringement path if a challenger targets stability only for shorter durations or uses a different formulation that fails the 24-month osmolality band but passes the 6-month narrower band.

Practical consequence: Stability data become central evidence. For litigation, the presence of time-bound “maintains” limitations makes product testing, sample timepoints, and study design more important than for purely compositional patents.

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What are the key claim subsets competitors would design around?

Design-around levers directly mapped to claim terms

1. Remove or reduce hypromellose
   • Claim 1 includes about 0.5 wt% hypromellose.
   • Dependent claim 12-13 locks viscosity modifier to hypromellose.
2. Change buffer identity away from sodium acetate/citrate
   • Claim 2-4 are specific; claim 11 hard-codes sodium acetate and sodium citrate at specific wt%.
   • Claim 1 has buffer genus (0.05-1.0 wt%), so changing buffer may still land in claim 1’s broad range unless pH maintenance or concentration requirements fail.
3. Shift electrolyte levels
   • NaCl, KCl, CaCl2, MgCl2 have defined wt%.
   • Dependent claims lock hydrate forms for CaCl2 and MgCl2.
4. Alter pH window
   • Broad claim: 5.8-6.8.
   • Sub-range dependent: 6.3-6.5.
5. Alter viscosity window
   • 15-35 cPs.
6. Alter osmolality band
   • 290-365 mOsm/kg for 24 months; 290-330 mOsm/kg for 6 months.
7. Preservative-free status
   • All listed independent claims require preservative-free.

Core insight: For a generic or reformulation entrant, changing one parameter may not be sufficient. Because claims are conjunctive, avoiding a single limiter is a clean design-around if it moves the product outside the relevant numeric window or eliminates a required component.

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How does the claim language “per drop delivers about 0.035 mg” affect generic and reformulation risk?

The “per drop” delivery requirement ties dosing performance to product characteristics that can be influenced by:

• concentration,
• drop size governed by packaging (dropper tip, bottle design),
• viscosity and surface tension.

However, the claims do not include explicit packaging-device structure. That said, “about 0.035 mg per drop” functions like a functional limitation. A product can nominally match oxymetazoline wt% but still deviate in per-drop deliverable amount if the effective drop volume differs.

Litigation posture implication: Accused products will need evidence on droplet size distribution and actual measured mg/drop. Plaintiffs can argue viscosity and buffer system control physical properties that affect drop formation.

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What patent landscape conclusions can be drawn for US 12,605,363 (without relying on external citation)?

Based strictly on claim scope provided, the patent’s landscape position is that it is not a general oxymetazoline composition patent. It is a niche stability-performance formulation patent with narrow numeric constraints. That tends to:

• increase overlap with formulation patents from competitors seeking to commercialize preservative-free ocular oxymetazoline for ptosis or related indications;
• increase the evidentiary burden around stability studies for infringement and invalidity.

Most likely competitive collision zones (mapped to claim features)

• preservative-free ophthalmic oxymetazoline formulations;
• buffered systems targeting pH 5.8-6.8 with maintained stability for multi-year periods;
• hypromellose-based viscosity systems within 15-35 cPs;
• fixed ionic strength systems with NaCl/KCl/CaCl2/MgCl2 set to the stated wt%;
• drop-delivery claims where per-drop mg matters for clinical dosing equivalence.

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Does US 12,605,363 read on common reformulation strategies?

Strategy: switch viscosity system (replace hypromellose)

• Likely avoids claim 1 because hypromellose content is required.
• Dependent claims 12-13 also narrow to hypromellose at about 0.5 wt%.

Strategy: use different buffers

• Can avoid dependent claims 2-4.
• But claim 1’s buffer genus (0.05-1.0 wt% “one or more suitable buffers”) still leaves risk if pH maintenance and the other parameter windows are met.

Strategy: change pH target

• Moving pH outside 5.8-6.8 avoids claim 1.
• Even if pH is within 5.8-6.8 at time zero, failure to maintain over 24 months can avoid claim 1 and 9, depending on which limitations are targeted.

Strategy: accept preservative

• Any preservative inclusion likely avoids “preservative-free” limitation.

Strategy: target lower stability time (6 months) only

• Claim 10/20 provide a 6-month infringement pathway with narrower osmolality.
• A product designed for 6-month shelf life but outside osmolality 290-330 mOsm/kg avoids those dependent claims.

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Key Takeaways

• US 12,605,363 is a preservative-free aqueous ophthalmic formulation patent for ptosis using oxymetazoline hydrochloride at about 0.1 wt% with a defined electrolyte matrix and hypromellose-based viscosity.
• The enforceable scope is driven by multi-parameter numeric ranges plus 24-month “maintains” stability requirements, making performance data central to infringement analysis.
• Dependent claim sets lock in buffer identity (sodium acetate/citrate with specific hydration states), viscosity modifier identity (hypromellose), and salt hydrates (CaCl2 dihydrate, MgCl2 hexahydrate).
• The most direct design-arounds are removing hypromellose, shifting pH outside 5.8-6.8 (or failing 24-month maintenance), shifting osmolality outside 290-365 mOsm/kg for 24 months (or outside 290-330 mOsm/kg for 6 months), changing the buffer system away from sodium acetate/citrate hydrates, or using a preservative.

FAQs

1. What is the broadest infringement path under US 12,605,363?
   Claim 1, which requires the specific electrolyte set, hypromellose at about 0.5 wt%, preservative-free status, pH 5.8-6.8 maintained for 24 months, and delivery of about 0.035 mg per drop.

2. Do the sodium acetate and sodium citrate requirements apply to the broadest claim?
   No. They appear in dependent claim 2 and are hard-coded in dependent claim 3/4 and in independent claim 11.

3. Which claim elements are most likely to be outcome-determinative in stability testing?
   The “maintains” limitations tied to pH, viscosity, and osmolality over defined timepoints (24 months and, in certain embodiments, 6 months).

4. Can a product meet oxymetazoline wt% but avoid infringement by changing droplet volume?
   Potentially, because “about 0.035 mg per drop” is a functional delivery limitation, but it still depends on demonstrating the actual delivered mg/drop for the accused product.

5. Is the patent limited to a single pH band or does it include sub-ranges?
   The claims include the broader pH range of 5.8-6.8 and dependent sub-range embodiments of 6.3-6.5.

References

1. US Patent 12,605,363 (claims as provided by user).

Drugs Protected by US Patent 12,605,363

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 12,605,363

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2020268329
Brazil	112021022404
Canada	3139443
Chile	2021002918
China	111888326
China	117045596
Colombia	2021015265