Details for Patent: 8,470,788

Summary for Patent: 8,470,788

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:	US13/529,971
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,470,788
Patent Claim Types: see list of patent claims	Use; Composition;

United States Patent 8,470,788 (Rosacea ivermectin emulsion)

What it covers: Methods of treating rosacea with topically applied ivermectin formulated as a chemically stable topical emulsion using a specified oil phase, surfactant/emulsifier set, solvent/propenetrating agent set, and gelling agent set, with explicit 8-week chemical stability. The scope also claims the emulsion composition itself.

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What are the core claim elements and how narrowly are they defined?

Independent claim strategy

The patent is structured with:

• Method claims directed to topical treatment of rosacea using an ivermectin emulsion with a defined ingredient system and 8-week chemical stability (claims 1, 6, 7).
• Composition claims directed to the stable emulsion for topical use (claims 10, 15, 16).
• Dependent claims that set quantitative ceilings/ranges (claims 2–5, 11–14) and add optional adjuvant lists (claims 8–9, 17–18).

The scope is compound-formulation centered rather than broad “ivermectin for rosacea” coverage.

Hard-edged requirements common to the independent claims

All independent claims share these technical constraints:

1. Indication / use

   • “treatment of rosacea” (method claims), or “topically applicable stable pharmaceutical emulsion” (composition claims).

2. Drug

   • ivermectin in a “thus effective amount” (method claim 1) or in explicit % ranges in the composition/method subgroups (claims 3, 6, 7, 12, 15, 16).

3. Dosage form

   • “formulated as an emulsion” and “said emulsion being chemically stable over … 8 weeks.”

4. Defined emulsion ingredient system Each emulsion must include the following categories within a specified genus:

   (a) Oil phase

   • Contains dimethicone and cyclomethicone
   • Contains isopropyl palmitate and/or isopropyl myristate
   • Additionally includes one or more fatty substances selected from:
     • cetostearyl alcohol, cetyl alcohol, stearyl alcohol, stearic acid, palmitostearic acid, and self-emulsifiable wax.

   (b) Surfactant/emulsifier

   • At least one chosen from:
     • glyceryl/PEG100 stearate
     • sorbitan monostearate
     • sorbitan palmitate
     • Steareth-20
     • Steareth-2
     • Steareth-21
     • Ceteareth-20

   (c) Ivermectin

   • Included as active.

   (d) Solvents/propenetrating agents

   • One or more from:
     • propylene glycol
     • oleyl alcohol
     • phenoxyethanol
     • glyceryl triacetate

   (e) Gelling agents

   • One or more from:
     • carbomers
     • cellulose gelling agents
     • xanthan gums
     • aluminum magnesium silicates excluding aluminum magnesium silicate/titanium dioxide/silica
     • guar gums
     • polyacrylamides
     • modified starches

   (f) Water

   • Present.

Key quantitative guardrails

The patent uses ranges and ceilings that materially narrow infringement scenarios:

• Surfactant/emulsifier cap: up to 15% by weight (claims 2 and 11; also mirrored in claims 6/7/15/16).
• Ivermectin range: 0.1% to 5% by weight (claims 3, 12; also in claims 6/7/15/16).
• Solvent/propenetrating agent range: 0.1% to 20% by weight (claims 4, 13; also mirrored).
• Gelling agent range: 0.01% to 5% by weight (claims 5, 14; mirrored).

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What is the exact scope of the rosacea treatment method claims?

Claim 1 (method, structurally defined emulsion with 8-week stability)

A method for treatment of rosacea by topical application of a pharmaceutical composition comprising:

• ivermectin (effective amount)
• as a topical pharmaceutical emulsion
• containing the ingredient system listed above
• chemically stable for 8 weeks.

Notably absent in claim 1: explicit quantitative ranges for each ingredient (those appear in dependent claims 2–5 and in other independent claims 6 and 7).

Claim 2–5 (dependent limits)

• Claim 2: surfactant/emulsifier is up to 15% by weight.
• Claim 3: ivermectin is 0.1 to 5% by weight.
• Claim 4: solvent/propenetrating agents are 0.1 to 20% by weight.
• Claim 5: gelling agents are 0.01 to 5% by weight.

Claim 6 (method, adds explicit percentage ranges including oil phase 3–50%)

Adds explicit composition percentages:

• Oil phase: 3% to 50% by weight
• Surfactant/emulsifier: up to 15%
• Ivermectin: 0.1% to 5%
• Solvent/propenetrating agent mixture: 0.1% to 20%
• Gelling agents: 0.01% to 5%
• water + stability: 8 weeks chemical stability.

Claim 7 (method, narrows oil phase to 6–20%)

Same architecture as claim 6 but with:

• Oil phase: 6% to 20% by weight (instead of 3–50%)

Implication for enforcement: claims 6 and 7 create overlapping but distinct infringement bands depending on oil phase percentage.

Claim 8–9 (method, adds optional additives lists)

• Claim 8: further comprises additives selected from:
  • flavor enhancers, preserving agents, stabilizers, humidity regulators, pH regulators, osmotic pressure modifiers, UV-A screening agents, UV-B screening agents, antioxidants.
• Claim 9: further comprises one or more from:
  • glycerol
  • methyl para-hydroxybenzoate
  • disodium EDTA
  • citric acid monohydrate
  • propyl para-hydroxybenzoate
  • sodium hydroxide

These are typical formulation adjuvants that do not alter the core “ingredient genus + stability” requirement.

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What is the exact scope of the composition claims?

Claim 10 (composition: stable topical ivermectin emulsion with 8-week chemical stability)

A “topically applicable stable pharmaceutical emulsion” comprising:

• oil phase with the specific mandatory elements:
  • dimethicone + cyclomethicone
  • isopropyl palmitate and/or isopropyl myristate
  • plus fatty substances selected from the defined fatty/alcohol/acid/self-emulsifiable wax set
• at least one surfactant/emulsifier from the defined list
• ivermectin
• solvent/propenetrating mixture selected from the defined list
• one or more gelling agents from the defined list (with the explicit aluminum magnesium silicate exclusion)
• water
• chemically stable for 8 weeks.

This claim is the cleanest handle for product-level enforcement.

Claim 11–14 (dependent quantitative limits mirrored)

• Claim 11: surfactant/emulsifier up to 15%
• Claim 12: ivermectin 0.1–5%
• Claim 13: solvent/propenetrating mixture 0.1–20%
• Claim 14: gelling agent 0.01–5%

Claim 15–16 (composition: adds explicit oil-phase range bands)

• Claim 15: oil phase is 3–50% by weight
• Claim 16: oil phase is 6–20% by weight Both maintain the same genus/percentage constraints for the other categories and the 8-week stability condition.

Claim 17–18 (composition additives lists)

• Claim 17: optional additives from the broad list (flavor enhancers, preservatives, stabilizers, etc.).
• Claim 18: optional additives from the specific list (glycerol, methyl parahydroxybenzoate, disodium EDTA, citric acid monohydrate, propyl parahydroxybenzoate, sodium hydroxide).

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How strong is the “chemical stability over 8 weeks” limitation for infringement?

The stability requirement is an explicit claim element in the independent claims (1, 6, 7, 10, 15, 16) and functions as a gate for both:

• literal infringement (the product must meet the stability requirement), and
• validity/obviousness arguments (the patentee framed the formulation as stable for an 8-week period).

Because stability is claimed as “chemically stable over a period of time of 8 weeks,” an accused product outside that performance period, or with an emulsion chemistry designed to fail that stability metric, is a direct non-infringement lever. Conversely, products meeting chemical stability would still need to satisfy the ingredient-genus constraints and quantity ranges.

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Where the claim language creates practical “design-around” pressure

The constraints create multiple infringement tripwires:

1. Oil phase specificity

   • Requires dimethicone + cyclomethicone plus isopropyl palmitate and/or isopropyl myristate.
   • Requires fatty substances from the defined fatty set.

2. Emulsifier genus

   • Must use at least one emulsifier from a limited list (glyceryl/PEG100 stearate, specific sorbitans, Steareth series, Ceteareth-20).

3. Propenetrating/solvent set

   • Limited to propylene glycol, oleyl alcohol, phenoxyethanol, and glyceryl triacetate.

4. Gelling agent genus with exclusion

   • Must use gelling agents from the set, and specifically excludes the combined “aluminum magnesium silicate/titanium dioxide/silica” member.

5. Quant ranges

   • Surfactant cap 15%.
   • Ivermectin 0.1 to 5%.
   • Solvent mixture 0.1 to 20%.
   • Gelling agent 0.01 to 5%.
   • Separate independent bands based on oil phase:
     • 3–50% (claims 6 and 15)
     • 6–20% (claims 7 and 16)

6. Stability period

   • 8-week chemical stability condition is part of the claim.

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Patent landscape: what this means for competitive freedom-to-operate

1) Claim scope positioning

This patent is a formulation/technology patent aimed at an ivermectin topical emulsion system with explicit excipient selection and stability. It is not a broad method-of-use patent that covers any ivermectin rosacea topical.

So the main competitive risk concentrates on products that:

• use ivermectin at 0.1–5%,
• are emulsions with dimethicone/cyclomethicone oil phase and the listed emulsifier/solvent/gelling genuses,
• and meet 8-week chemical stability.

2) Where carve-outs are likely if competitors change the vehicle

Competitors can reduce risk by changing at least one of the following structural blocks:

• Replace the dimethicone/cyclomethicone oil phase,
• Replace the emulsifier with something outside the claimed list,
• Replace the solvent/propenetrating mixture with a different solubilizer/propenetrant set,
• Use a gelling agent outside the defined genuses or use the excluded aluminum magnesium silicate combination,
• Formulate to fail or not demonstrate chemical stability for 8 weeks (where defensible and acceptable clinically/operationally).

3) Overlap with typical rosacea topical design

Rosacea topical products commonly use:

• moisturizers/emollients,
• penetration enhancers,
• polymeric gels or creams,
• and optional preservatives/pH adjusters.

This patent’s lists and ranges are consistent with those archetypes, but the specific excipient genuses and the 8-week chemical stability clause narrow overlap to vehicles that match the claim recipe.

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Enforcement-relevant claim map (product-level)

If a competitor sells a topical ivermectin emulsion for rosacea, the likely infringement analysis will proceed by checking, in order:

1. Is it an emulsion (not a gel-only formulation)?
2. Is it an ivermectin product at 0.1–5%?
3. Does the oil phase include:
   • dimethicone + cyclomethicone
   • and isopropyl palmitate and/or isopropyl myristate
   • and one or more fatty substances from the defined list?
4. Does it use at least one surfactant/emulsifier from the enumerated set, and is that component ≤15%?
5. Does it include a solvent/propenetrating agent mixture within 0.1–20% from the enumerated set?
6. Does it contain a gelling agent within 0.01–5% from the enumerated set and avoid the aluminum magnesium silicate/titanium dioxide/silica exclusion?
7. Is the formulation chemically stable for 8 weeks?

Failure on any one of these stops literal infringement.

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Key Takeaways

• 8,470,788 is a formulation-centric patent: it requires a topical ivermectin emulsion for rosacea with specific excipient genuses and explicit percentage ranges in key independent claims.
• The claims are enforced around a constrained vehicle: dimethicone + cyclomethicone oil phase, enumerated emulsifiers, enumerated solvent/propenetrants, enumerated gelling agents (with a specific exclusion), and water.
• The strongest differentiator is the explicit “chemically stable over … 8 weeks” limitation, which can be a performance-based non-infringement lever.
• Risk concentration for competitors is highest when their rosacea product matches the claimed excipient system and stays within the stated ranges, especially oil phase 3–50% or 6–20% bands and ivermectin 0.1–5%.

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FAQs

1. Does the patent cover any topical ivermectin for rosacea?
   No. It requires an ivermectin emulsion with specific excipient lists and 8-week chemical stability.

2. Which ingredient category most constrains vehicle design?
   The oil phase and emulsifier selections: the claims require dimethicone/cyclomethicone plus specified fatty substances and at least one emulsifier from a limited enumerated set.

3. How do the oil-phase ranges affect infringement risk?
   They create separate independent compositions: 3–50% (claims 6/15) versus 6–20% (claims 7/16). Products outside the relevant oil-phase band may avoid those specific independent claims.

4. Are preservatives and UV filters covered?
   Yes as optional additives in dependent claims, via broad lists and a specific subset (claims 8–9 and 17–18). These do not replace the core emulsion ingredient system.

5. Is “8-week chemical stability” part of all claim types?
   It appears in the independent method and composition claims (claims 1, 6, 7, 10, 15, 16) and is not merely a background descriptor.

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References

[1] United States Patent No. 8,470,788 (claims as provided in the prompt).

Drugs Protected by US Patent 8,470,788

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: 8,470,788

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

International Family Members for US Patent 8,470,788

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
European Patent Office	1620113		122015000079	Germany
European Patent Office	1620113		92915	Luxembourg
European Patent Office	1620113		56/2015	Austria