Details for Patent: 8,318,800

Summary for Patent: 8,318,800

Title:	Solid pharmaceutical compositions containing benzofuran derivatives
Abstract:	The present invention relates to a solid pharmaceutical composition for oral administration characterized in that it comprises a benzofuran derivative with antiarrhythmic activity, or one of the pharmaceutically acceptable salts thereof, as an active principle, and a pharmaceutically acceptable nonionic hydrophilic surfactant optionally in combination with one or more pharmaceutical excipients.
Inventor(s):	Bernard Abramovici, Jean-Claude Gautier, Jean-Claude Gromenil, Jean-Marie MARRIER
Assignee:	Sanofi SA
Application Number:	US11/955,565
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,318,800
Patent Claim Types: see list of patent claims	Composition; Compound; Dosage form;

Executive summary United States Patent 8,318,800 is directed to solid, oral dronedarone formulations defined by (i) the active (dronedarone or a pharmaceutically acceptable salt, specifically including dronedarone hydrochloride) and (ii) a nonionic hydrophilic surfactant present at 1%–50% by weight of dronedarone (base), with dependent claim coverage narrowed to poloxamers / specific poloxamer species (including poloxamer 407), and to practical tablet/capsule compositions and dosed strengths (50–500 mg, including 200–400 mg; with examples of ~10% surfactant in base-relative terms). The claim set indicates a patent landscape concentrated on formulation carve-outs around surfactant identity and loading, and on dosage-form execution (tablet or gelatin capsule).

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United States Patent 8,318,800 claims scope: dronedarone solid oral composition with nonionic hydrophilic surfactant (poloxamer)

What is patented?
A US solid oral formulation of dronedarone in which a nonionic hydrophilic surfactant is present in a defined weight proportion relative to dronedarone base, with coverage spanning:

• Salt form (explicitly includes dronedarone hydrochloride)
• Surfactant type (nonionic hydrophilic surfactants, with examples of poloxamers, polyethoxylated castor oils, and polyethylene hydroxystearates)
• Surfactant species (dependent claims list multiple poloxamer grades, and single out poloxamer 407)
• Dosage form (tablet or gelatin capsule in dependent claims)
• Surfactant loading windows (broad 1%–50%; narrower 1%–20% and then 5%–15% for tablets/capsules)
• Active dose range (50–500 mg; with narrower 200–400 mg)

Independent claim 1 is the core “catch-all” covering any acceptable nonionic hydrophilic surfactant meeting the loading requirement, with downstream claims tightening to specific chemical classes and specific poloxamer grades.

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What is the claim scope of US Patent 8,318,800 (independent claim 1 vs dependent claims)?

Featured snippet answer: Claim 1 covers solid oral dronedarone compositions with nonionic hydrophilic surfactant at 1%–50% w/w relative to dronedarone base, optionally with excipients, where dronedarone can be free base or a pharmaceutically acceptable salt.

Claim 1 scope (breadth and boundaries)

Claim 1 requires all of the following:

1. Dosage form: “solid pharmaceutical composition for oral administration”
2. Active: dronedarone or a pharmaceutically acceptable salt
3. Essential formulation feature: at least one pharmaceutically acceptable nonionic hydrophilic surfactant
4. Quantitative limitation: surfactant is present in a proportion of 1% to 50% by weight of the active principle in base form
5. Optional excipients allowed

Key interpretive points for claim construction

• Relative basis is fixed: the proportional language is explicitly tied to “active principle in base form.” That locks the calculation basis even if the administered API is a salt (e.g., HCl salt).
• “Nonionic hydrophilic surfactant” is the gating term: the claim does not limit to a specific hydrophilic-lipophilic balance or specific polymer block ratios in the independent claim. Dependent claims do that.
• “1% to 50%” is a wide window: this is a broad formulation patent in quantitative terms.

Claim 2 (salt-specific coverage)

• Limits active to dronedarone hydrochloride.
• This is narrower than claim 1 but provides a straightforward salt-specific infringement target.

Claim 3 and 4 (surfactant family and poloxamer-grade list)

• Claim 3 limits surfactant selection to a set:
  • poloxamers
  • polyethoxylated castor oils
  • polyethylene hydroxystearates
• Claim 4 narrows to listed poloxamer grades:
  • poloxamer 124, 188, 237, 338, 407
  • and polyethylene hydroxystearate 660 is also included in the dependent list

Claim 5 (poloxamer 407 singled out)

• Narrows surfactant to poloxamer 407.

Claims 6–7 (tablet/capsule execution and narrower loading window)

• Claim 6 limits form to tablet or gelatin capsule and narrows surfactant loading to 1%–20% (relative to dronedarone base).
• Claim 7 further narrows to 5%–15%.

Practical effect: these dependents define a realistic “development space” for generic or follow-on formulation strategies by focusing on typical excipient loading.

Claims 8–10 (strength range and a specific surfactant-relative example)

• Claim 8: composition contains 50 to 500 mg active principle.
• Claim 9: in tablet/capsule, contains 200 to 400 mg.
• Claim 10: in tablet/capsule contains 200 to 400 mg, and surfactant is 10% by weight relative to dronedarone base.

Claims 11 and 12–13 (poloxamer 407 + excipient ecosystems)

• Claim 11: repeats that surfactant is poloxamer 407.
• Claim 12: excipients can include binder, flow agent, vinylpyrrolidone polymer/copolymer, diluent, starch, lubricant.
• Claim 13: excipient exemplars are enumerated (methylcellulose, hydroxyethylcellulose, methylhydroxypropylcellulose, macrogol, colloidal silica, PVP/PVP copolymer, lactose, mannitol, wheat/corn starch, magnesium stearate, sodium stearyl fumarate).

Claims 14–15 (“consisting essentially of” tablet form and essential components)

• Claim 14 recites “solid pharmaceutical composition in tablet form … consisting essentially of”
  • dronedarone (or salt) as active
  • a nonionic hydrophilic surfactant that is a poloxamer
  • one or more pharmaceutical excipients
  • surfactant loading 5%–15% relative to active base

Claim 15 enumerates excipient selection categories similar to claims 12–13 (binder/flow agent/vinylpyrrolidone/diluent/starch/lubricant).

Scope consequence of “consisting essentially of”: This standard phrase generally allows additional components that do not materially change basic and novel characteristics. Here, the “basic and novel” characteristics are the poloxamer-based nonionic hydrophilic surfactant at 5%–15% and the tablet format with dronedarone.

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How do the poloxamer and surfactant loading limits affect infringement risk for generics?

Featured snippet answer: Infringement risk is highest where a generic matches (i) a solid oral dronedarone tablet/capsule and (ii) includes a nonionic hydrophilic surfactant at within 1%–50% of dronedarone base, with tighter risk if it uses poloxamer at 5%–15% (or 10%) relative to dronedarone base.

Quantitative “design-around” realities

Because claim 1 is keyed to weight percent of dronedarone base, design-around strategies typically target:

• Lowering surfactant below 1% of dronedarone base (to avoid claim 1/6)
• Eliminating the “nonionic hydrophilic surfactant” function (e.g., swapping to non-overlapping surfactants)
• Using a surfactant outside the claimed families (to avoid claim 3/4)
• Avoiding poloxamer grades listed in dependent claims (to avoid claims 4–5)
• Avoiding the tablet/capsule loading windows (5%–15% and 10% are explicitly called out)

But the breadth of claim 1 (1%–50%) is the main barrier: many common wetting/dispersing excipients in solid oral dosage forms can fall into “nonionic hydrophilic surfactant,” and poloxamers are frequently used at around the dependent-claim levels (5%–15%).

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Which formulations are explicitly covered (tablets, gelatin capsules, strength ranges, and excipient sets)?

Featured snippet answer: Explicit coverage exists for tablets and gelatin capsules with 1%–20% surfactant and especially 5%–15%, and for strength configurations of 50–500 mg (and 200–400 mg in tablets/capsules), including an explicit example at 10% surfactant.

Dosage form

• Claim 1: any “solid pharmaceutical composition for oral administration”
• Claim 6–7: tablet or gelatin capsule
• Claim 14–15: tablet only

Strength

• Claim 8: 50–500 mg active
• Claim 9–10: 200–400 mg active in tablet/capsule

Surfactant loading windows

• Claim 1: 1%–50%
• Claim 6: 1%–20% (tablet/capsule)
• Claim 7: 5%–15% (tablet/capsule)
• Claim 10: 10% (tablet/capsule, 200–400 mg)

Excipient categories (not limited to any single excipient)

• Binders: methylcellulose/hydroxyethylcellulose/methylhydroxypropylcellulose
• Flow agents: colloidal silica
• Vinylpyrrolidone polymers: PVP
• Diluents: macrogol, lactose, mannitol
• Starches: wheat/corn starch
• Lubricants: magnesium stearate, sodium stearyl fumarate

Implication: excipient “menus” are compatible with infringement if the essential surfactant feature is met.

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What patents likely sit around US 8,318,800 in the dronedarone formulation landscape?

Featured snippet answer: US 8,318,800 is a formulation patent. In practice, the closest neighboring patent clusters for dronedarone are typically:

• earlier dronedarone drug substance or salt form patents
• intermediate solid oral formulation patents (including excipient/surfactant selection and manufacturing)
• later “improvement” formulation patents that narrow to specific surfactants, loading ranges, or dosage strengths
• process/manufacturing patents for producing dronedarone tablets/capsules with specific surfactant handling

Scope linkage to the claim text

• Because claim 1 is excipient-identity and loading based, adjacent patents often cover:
  • alternative surfactant classes or grades
  • alternative wetting/dispersing agents
  • particle size modulation, granulation methods, or dissolution-control systems
  • alternative salt forms (beyond HCl)
  • alternative dosage forms (capsules vs tablets)

Practical positioning: US 8,318,800 functions like a “surfactant loading guardrail” that blocks generic replication of a dronedarone solid oral product if it uses poloxamer-class excipients in the claimed amounts.

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How strong is US 8,318,800 as a patent estate barrier (claim structure, breadth, and coverage depth)?

Featured snippet answer: Strength is driven by (i) a broad independent claim with a wide 1%–50% surfactant loading window, (ii) extensive dependent narrowing that captures common commercial excipient selections (poloxamers including poloxamer 407), and (iii) explicit narrowing to the frequently used tablet/capsule format with realistic dose ranges and a specific 10% example.

Coverage depth

• Multiple nested dependents create overlapping infringement theories:
  • even if a product avoids exact poloxamer grades, claim 1 can still read if the surfactant is a “nonionic hydrophilic surfactant” in 1%–50%.
  • if the product uses poloxamer but outside 1%–50%, it can still fall into dependent claims only if it matches the narrower windows and dosage-form limits.

Claim construction pressure points

• “nonionic hydrophilic surfactant” is a functional-structural category. A challenger can argue that a selected excipient lacks sufficient hydrophilicity or nonionic character as used.
• “proportion … by weight of the active principle in base form” can be attacked via calculation methodology or the definition of “base form” in the test framework (especially for salts).

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What does this mean for Paragraph IV or generic entry risk on dronedarone solid oral products?

Featured snippet answer: The risk is highest for generic applicants whose ANDA formulation uses poloxamer-class nonionic hydrophilic surfactants at 1%–50% (and especially 5%–15% or 10%) relative to dronedarone base, in tablets or gelatin capsules with strengths that match 50–500 mg (and 200–400 mg).

Generic design-around scenarios implied by claim language

1. Swap away from poloxamers/poloxamer 407
2. Use a nonionic hydrophilic surfactant outside the 1%–50% window
3. Use a surfactant that is not “nonionic hydrophilic”
4. Use a dosage form outside tablet/capsule ranges referenced in dependent claims (though independent claim 1 still covers any solid oral composition)

Because claim 1 covers “solid pharmaceutical composition for oral administration” without confining to tablets/capsules, moving only to another solid oral form may not eliminate risk if that form still uses a nonionic hydrophilic surfactant at 1%–50%.

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Orange Book and FDA status: what is the likely regulatory hook for US 8,318,800?

Featured snippet answer: The legal and commercial mechanism for this kind of formulation patent in the US market is typically Orange Book listing for an FDA-approved dronedarone drug product and a triggered exclusivity/eligibility posture for ANDA certifications.

However: no Orange Book listing data, FDA product code, patent listing number, or expiration/term details were provided in the input. Without that, a precise status read cannot be produced here.

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Company and litigation landscape: which parties are likely implicated?

Featured snippet answer: In dronedarone formulation patents, likely actors include:

• originator/product holder(s) for dronedarone tablets/capsules
• generic manufacturers pursuing ANDAs for dronedarone
• challengers filing Paragraph IV certifications

But: the input does not include docket numbers, parties, settlement names, or court decisions tied to US 8,318,800. Without those identifiers, listing the exact litigation parties for this patent would risk factual error.

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Key Takeaways

• US 8,318,800 is a formulation patent for solid oral dronedarone compositions built around a nonionic hydrophilic surfactant with 1%–50% w/w loading relative to dronedarone base.
• Dependent claims narrow to dronedarone hydrochloride and specific surfactant families/grades, with poloxamers and explicit coverage of poloxamer 407.
• Tablet/capsule dependents narrow to 1%–20% and 5%–15% surfactant, and a specific example of 10% at 200–400 mg strengths.
• The claim breadth makes it a high-friction barrier against generics that use common poloxamer-type wetting agents at conventional loading levels.

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FAQs

1. Does US 8,318,800 cover dronedarone salts or only free base?
It covers dronedarone or pharmaceutically acceptable salts, including a dependent claim specific to dronedarone hydrochloride.

2. What surfactants are explicitly within the dependent claim scope?
Dependent claims list poloxamers, polyethoxylated castor oils, and polyethylene hydroxystearates, with poloxamer grade and poloxamer 407 specified.

3. What happens if a formulation uses poloxamer outside 1%–50% of dronedarone base?
If the surfactant is outside the 1%–50% range, claim 1 does not read; infringement depends on whether any narrower dependent claim windows are met (e.g., 5%–15% for tablet/capsule).

4. Is “tablet vs capsule” important for infringement?
Yes for dependent claims 6–7 and 9–10 and for “consisting essentially of” claim 14, but independent claim 1 covers any “solid pharmaceutical composition for oral administration.”

5. Can excipient selection avoid infringement under this patent?
Excipient selection alone is unlikely to avoid infringement because claim 1 allows “one or more pharmaceutical excipients” and is driven by the surfactant identity/class and surfactant loading.

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References (APA)

1. U.S. Patent 8,318,800.

Drugs Protected by US Patent 8,318,800

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: 8,318,800

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
France	97 07795	Jun 23, 1997

International Family Members for US Patent 8,318,800

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1007030		PA2010003	Lithuania
European Patent Office	1007030		C300446	Netherlands
European Patent Office	1007030		91673	Luxembourg