Details for Patent: 8,093,219

Summary for Patent: 8,093,219

Title:	Topical application of ivermectin for the treatment of dermatological conditions/afflictions
Abstract:	Dermatological conditions/afflictions such as rosacea, common acne, seborrheic dermatitis, perioral dermatitis, acneform rashes, transient acantholytic dermatosis, and acne necrotica miliaris, most notably rosacea, are treated by topically applying onto the affected skin area of an individual in need of such treatment, a topical pharmaceutical composition which comprises a thus effective amount of ivermectin.
Inventor(s):	Vincent Manetta, Gary R. Watkins
Assignee:	Galderma Holding SA
Application Number:	US12/483,604
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,093,219
Patent Claim Types: see list of patent claims	Use; Composition; Compound;

Patent 8,093,219 scope and claims map for ivermectin topical emulsion regimens for rosacea (US)

US Drug Patent 8,093,219 claims a rosacea treatment regimen that uses a topically applied ivermectin emulsion with tightly specified excipient families and 8-week chemical stability. The claim set is anchored on (i) ivermectin concentration (0.1 to 5% by weight), (ii) emulsion structure defined by a defined oily phase (notably dimethicone and isopropyl palmitate/isopropyl myristate) plus specified fatty substances, (iii) surfactant-emulsifier range (2 to 12%) from a defined list, (iv) solvent/propenetrating agents range (1 to 10%) from a defined list, (v) gelling agents range (0.01 to 5%) from a defined list with a categorical exclusion about aluminum magnesium silicate/titanium dioxide/silica, and (vi) chemically stable for 8 weeks.

A key practical point for freedom-to-operate is that the patent is not a pure “ivermectin for rosacea” claim. It is an ivermectin-in-specific-topical-emulsion claim with explicit component exclusions and an assayable stability condition that can be used as a design-around target.

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What patents protect ivermectin topical emulsion regimens for rosacea under US 8,093,219?

Core protection (independent concept): regimens and formulations that meet the same compositional scaffold across claims 1-4 and the emulsion claims 14-17, plus narrower dependent recitations (claims 5-13, 18-26) and multiple example compositions (claims 27-30).

Claim 1-4: What exact regimen is protected?

All regimen claims require:

• Topical application to affected skin for rosacea.
• A topical pharmaceutical composition comprising effective amount of ivermectin.
• The ivermectin is delivered in an emulsion with defined ranges and component families.
• Chemical stability for 8 weeks.

Claim 1 is the broadest “scaffold” among the regimen claims provided:

• Oily phase (6 to 20%) includes:
  • Dimethicone
  • Cyclomethicone
  • Isopropyl palmitate and/or isopropyl myristate
  • plus fatty substances selected from: cetostearyl alcohol, cetyl alcohol, stearyl alcohol, stearic acid, palmitostearic acid, self-emulsifiable wax
• Surfactant-emulsifier (2 to 12%) from:
  glyceryl/PEG100 stearate, sorbitan monostearate, sorbitan palmitate, Steareth-20, Steareth-2, Steareth-21, Ceteareth-20
• Ivermectin (0.1 to 5%)
• Solvents/propenetrating agents (1 to 10%) from:
  propylene glycol, oleyl alcohol, phenoxyethanol, glyceryl triacetate
• Gelling agent (0.01 to 5%) from:
  carbomers, cellulose derivatives, xanthan gums, aluminum magnesium silicates (with exclusion described below), guar gums, polyacrylamides, modified starches
  • explicit exclusion: excluding aluminum magnesium silicate/titanium dioxide/silica
• Water as remainder.
• Chemically stable over 8 weeks.

Claim 2 and Claim 3 refine the oily phase and gelling agent structure.

• Claim 2: replaces some oily-phase fatty substances and specifies a gelling agent as aluminum magnesium silicate (with the same exclusion).
• Claim 3: uses oily phase components dimethicone + isopropyl palmitate and defines a narrower surfactant list (notably glyceryl/PEG stearate, sorbitan monostearate, Steareth-20).
• Claim 4: locks in oily phase as dimethicone, isopropyl palmitate, palmitostearic acid, self-emulsifiable wax and surfactants as glyceryl/PEG stearate, sorbitan monostearate, Steareth-20; gelling agent is again aluminum magnesium silicate excluding the TiO2/silica combination.

Claim 5-13: What add-ons expand the “regime” claim set?

Claims 5-13 are dependent layers that do not change the base scaffold; they add “one or more additives” from two families:

1. Cosmetic/pharmaceutical adjuncts (claim 5,7,9,11 and equivalents 18-26):
   flavor enhancers, preserving agents, stabilizers, humidity regulators, pH regulators, osmotic pressure modifiers, UV-A screening agents, UV-B screening agents, antioxidants.

2. Specific excipients group (claim 6,8,10,12 and equivalents 19,21,23,25,26, plus explicit recitations in 13 and examples):
   glycerol, methyl para-hydroxybenzoate, disodium EDTA, citric acid monohydrate, propyl para-hydroxybenzoate, sodium hydroxide.

Claim 13 is stronger than “one or more”; it recites all those listed excipients in combination as part of the further-defined regime.

Claim 14-17: What formulation claims protect?

These are composition-level “topically applicable stable pharmaceutical emulsion” claims mirroring the regimen scaffold.

• Claim 14 matches the Claim 1-like oily phase list but is framed as a stable emulsion (same ranges, components, exclusion, and 8-week chemical stability).
• Claim 15 is similar but with the gelling agent restricted as aluminum magnesium silicate gelling agent with the exclusion.
• Claim 16 uses oily-phase dimethicone + isopropyl palmitate (and permits palmitostearic acid, self-emulsifiable wax, cetyl alcohol, stearyl alcohol).
• Claim 17 further constrains oily-phase and surfactant list.

Claim 18-26: What stable-emulsion dependent claims add?

• Claims 18-25 add either:
  • the “adjunct” additive group (UV screens, preservatives, pH regulators, antioxidants, etc.), or
  • the “specific excipients” group (glycerol, paraben pair, disodium EDTA, citric acid monohydrate, sodium hydroxide).
• Claim 26 recites the specific excipients group (not “one or more”) while still within the Claim 16/17-defined emulsion scaffold.

Claims 27-30: What exact example compositions are claimed?

Claims 27-30 provide specific quantitative formulations (percent by weight) including:

• Ivermectin 1.00
• Glycerol 4.0
• Aluminum magnesium silicate 1.0
• Methyl para-hydroxybenzoate 0.2
• Disodium EDTA 0.05
• Citric acid monohydrate 0.05
• Isopropyl palmitate 4.0
• Glyceryl/PEG 100 stearate 3.0
• Self-emulsifiable wax 2.0
• Palmitostearic acid 2.5 or 3.0
• Steareth-20 3.0
• Sorbitan stearate 2.0
• Dimethicone 20 0.5
• Propyl para-hydroxybenzoate 0.1
• Propylene glycol 4.0
• Glyceryl triacetate 1.0
• Phenoxyethanol 0.5
• 10% sodium hydroxide qs pH
• Water qs to 100

These example claims matter because many generic and competitor formulations attempt to “stay close” to known ivermectin cream/gels. The closer the formulation is to these exact ratios (or functionally equivalent substitutions), the higher the literal infringement risk.

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How broad are the scope limits on 8,093,219 (ranges, component lists, and stability)?

Scope architecture is built from three concentric rings:

1. Ring 1: product type and use
   Topical emulsion regimen for rosacea using ivermectin.

2. Ring 2: emulsion component families and ranges
   Strict weight-percentage bands with fixed component lists:

• Oily phase: 6-20%
• Surfactant-emulsifier: 2-12%
• Ivermectin: 0.1-5%
• Solvents/propenetrating agents mixture: 1-10%
• Gelling agent: 0.01-5% (or aluminum magnesium silicate for certain claims)
• Water: remainder

3. Ring 3: exclusions and performance condition

• Exclusion tied to the gelling agent: excluding aluminum magnesium silicate/titanium dioxide/silica.
• Chemical stability for 8 weeks.

Design-around levers embedded in the claim language

For infringement avoidance, the most direct “knock-out” features in the claim set are:

• Oily phase marker components: dimethicone and isopropyl palmitate (or isopropyl myristate) appear in multiple independent claims.
• Surfactant-emulsifier marker list: the claims limit surfactant choices to enumerated members (glyceryl/PEG100 stearate, sorbitan esters, Steareth family, Ceteareth-20, etc.). Substituting with an unlisted emulsifier can reduce literal coverage.
• Gelling agent restriction + categorical exclusion: aluminum magnesium silicate is allowed in certain claims but is expressly excluded when combined in a specific multi-component TiO2/silica composite.
• Stability condition: “chemically stable over 8 weeks” is performance-limiting.

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Which specific formulation elements in 8,093,219 are most vulnerable in a litigation claim construction?

Claim construction pressure points (based on enumerated lists and exclusion language):

1) “Oily phase comprising dimethicone, cyclomethicone, isopropyl palmitate and/or isopropyl myristate”

A literal match depends on whether the formulation includes the listed components within the claimed oily phase definition and whether those components fall within the oily phase weight band (6-20%).

2) “Surfactant-emulsifier selected from the group…”

Because the claim lists discrete surfactant candidates, infringement depends on using one or more of those candidates at 2-12% by weight.

3) “Mixture of solvents and/or propenetrating agents”

The claim allows mixtures made from the listed solvents/propenetrants, but constrains the total weight at 1-10%. A product using different solubilizers/emollients can reduce literal infringement even if it performs similarly.

4) “Gelling agents… excluding aluminum magnesium silicate/titanium dioxide/silica”

This categorical exclusion is a carve-out that can be strategically relevant for formulation vendors using that composite gelling system.

5) “Chemically stable over… 8 weeks”

This injects a measurable performance element. In litigation, the stability protocol and the product’s chemical assay over time can become a focal point.

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What patent landscape risks exist around US 8,093,219 for generics and branded rosacea topicals?

Within the excerpt provided, US 8,093,219 is clearly a formulation-anchored patent for an ivermectin emulsion with specific excipient architecture. The generic entry risk is therefore tied to:

• Whether an entrant copies the excipient scaffold, not just ivermectin presence.
• Whether entrants target the same dosage form class: an emulsion (not a gel, cream without emulsion structure, lotion with different phase definitions, etc.).
• Whether stability and exclusions can be met while still staying within the claimed component lists/ranges.

Practical infringement scenarios implied by the claims

• High risk: products using ivermectin emulsion with dimethicone and isopropyl palmitate/myristate (or cyclomethicone), a surfactant from the listed Steareth/sorbitan/glyceryl/PEG group at 2-12%, and aluminum magnesium silicate gelling (not the excluded TiO2/silica composite), with 8-week chemical stability.
• Moderate risk: products that move one band (for example, surfactant outside 2-12% or gelling outside 0.01-5%) or substitute one unlisted emulsifier, but still meet remaining scaffold elements.
• Lower literal risk: products using ivermectin in a non-emulsion delivery system (or using a different excipient architecture outside enumerated lists) while also demonstrating the absence of “chemically stable over 8 weeks” under the claimed conditions.

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Where do claim 8,093,219 examples create “near-copy” infringement exposure?

Claims 27-30 provide a quantitative “roadmap” close to a typical commercial semisolid emulsion:

• Ivermectin at 1.0% (within 0.1-5%)
• Oily phase with dimethicone 20 (0.5), isopropyl palmitate (4.0), palmitostearic acid (2.5 or 3.0), self-emulsifiable wax (2.0)
• Surfactant system dominated by glyceryl/PEG 100 stearate (3.0), steareth-20 (3.0), sorbitan stearate (2.0)
• Solvent/propenetrating components: propylene glycol (4.0), glyceryl triacetate (1.0), phenoxyethanol (0.5)
• Gelling: aluminum magnesium silicate (1.0)
• Preservatives and pH: methyl and propyl paraben + disodium EDTA + citric acid + sodium hydroxide to pH

A formulation that hits these values will align strongly with both:

• the broad independent scaffold ranges, and
• the specific dependent example ratios.

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What regulatory and exclusivity questions matter alongside this formulation patent?

The patent is not an FDA exclusivity right; it is a patent on a specific composition and stability/performance within a rosacea treatment context. Risk and timing thus come from:

• whether a rosacea ivermectin product is already marketed under an approved application, and
• whether a competitor files an abbreviated pathway and submits a patent certification tied to this patent.

Because the question is framed as “patent landscape analysis” and not as a request for Orange Book status, the actionable linkage is the following:

• If a later sponsor seeks approval for a topical ivermectin emulsion that falls within these compositional constraints, the product’s chemistry package will likely be analyzed against the patent’s enumerated ranges and exclusions.
• If the later sponsor designs around by switching emulsifier families, gelling agent systems, or phase components, the patent’s claim language provides a roadmap for what changes reduce overlap.

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Key Takeaways

• US 8,093,219 protects rosacea regimens that deliver ivermectin via a chemically stable (8 weeks) topical emulsion with tightly enumerated excipient families and weight ranges.
• The claims’ strongest “scope anchors” are: ivermectin 0.1-5%, emulsion oily phase 6-20% featuring dimethicone + isopropyl palmitate/myristate (and sometimes cyclomethicone), surfactant-emulsifier 2-12% from a fixed list, solvent/propenetrant 1-10% from a fixed list, and gelling agents 0.01-5% with a specific carve-out for aluminum magnesium silicate/titanium dioxide/silica.
• Claims 27-30 provide exact quantitative formulations that create “near-copy” infringement exposure for entrants using similar semisolid emulsion excipient systems.
• Design-around is most directly pursued by changing one or more of: the listed emulsifier family, the gelling agent system (especially the TiO2/silica composite), the oil-phase marker components, or the stability/performance profile relevant to “8-week chemical stability.”

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FAQs

1. Does US 8,093,219 cover ivermectin creams that are not emulsions?
   Coverage is limited to topically applicable pharmaceutical compositions formulated as emulsions with the claimed excipient structure and stability language.

2. Is the aluminum magnesium silicate exclusion limited to a specific composition form?
   Yes. The claims exclude aluminum magnesium silicate/titanium dioxide/silica as a gelling agent composition system.

3. What is the highest-risk excipient substitution area in the claim set?
   The surfactant-emulsifier and oily phase component selections are enumerated and range-bound, creating the most straightforward literal-infringement “pass/fail” points.

4. Do the example claims (27-30) broaden the patent beyond the range claims?
   They narrow to specific compositions while maintaining alignment with the broader scaffold; near-matching formulations face the tightest risk.

5. Can a product avoid infringement by slightly changing ingredient percentages?
   Potentially. Literal infringement depends on meeting the claimed weight percentage ranges and using ingredients within the enumerated lists for each functional excipient category.

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References

1. United States Patent US 8,093,219.

Drugs Protected by US Patent 8,093,219

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate

Foreign Priority and PCT Information for Patent: 8,093,219

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
France	03 05048	Apr 24, 2003

International Family Members for US Patent 8,093,219

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1620113		C300756	Netherlands
European Patent Office	1620113		CA 2015 00045	Denmark
European Patent Office	1620113		PA2015033	Lithuania