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Patent landscape, scope, and claims: |
United States RE32393 (Drug Patent) = What Its Claims Actually Cover and How to Map the Landscape
RE32393 is a reissue-type US patent claim set built around a single, broad formulation concept: an autoclave-capable, stable oil-in-water emulsion for intravenous (including parenteral/intravenous enhancing language) delivery, where a pharmacologically inert lipoid forms a finely divided hydrophobic phase (mean particle size < 1 micron) and an effective dose of an oil-soluble active agent is predominantly dissolved in the lipoid at a specific “fraction ratio” in the hydrophobic phase. The claims then lock in (1) the emulsion/particle-size/processing robustness and (2) the active-agent universe via species lists and class groupings (central depressants, analgesics, muscle relaxants, vasodepressants).
This claim structure creates a high-leverage infringement surface for any IV oil-in-water emulsion product using: submicron dispersed oil droplets, autoclaving tolerance, inert lipoid hydrophobic phase dissolution of oil-soluble drug, and oil-soluble drug selection within the enumerated compound sets.
What Is the Core Claim Scope (Independent Claim 1 / Claim Backbone)
Claim 1 (composition) and the parallel composition claim 8 (expanded agent list) are the backbone. The claims use a composition template plus a drug-selection limitation.
What does Claim 1 require, in operational terms?
Claim 1 requires all of the following:
- Administration context: “enhancing parenteral administration comprising intravenous administration” language (composition scope) and later method claim pairs (claims 26-44).
- Dosage form: a stable oil-in-water emulsion.
- Processing robustness: capable of withstanding autoclaving.
- Hydrophobic phase: contains a pharmacologically inert lipoid as the hydrophobic phase, dispersed in a hydrophilic phase.
- Active drug location and form:
- an effective dose of a pharmacologically active, oil-soluble agent
- the active is predominantly dissolved in said lipoid (not just suspended).
- the claim ties to a “fraction ratio” of active to lipoid in the hydrophobic phase.
- Particle size: the lipoid particles in the emulsion are finely divided with mean particle size less than 1 micron.
- Therapeutic effect linkage: “to achieve rapid onset of an acceptable therapeutic effect attributable to said effective dose.”
- Active drug class limitation: active is selected from a class consisting of:
- central depressants, analgesics, spasmolytics, muscle relaxants, and vasodepressants.
Claim 1 also functions as a broad composition claim because it does not cap:
- concentration ranges (except later dependent claims),
- specific hydrophilic phase components,
- exact emulsifier systems (except in later dependents),
- exact “fraction ratio” definition (only that it exists),
- exact viscosity/osmolality or droplet distribution metrics (only “mean particle size < 1 micron”).
How Claim 8 broadens drug coverage
Claim 8 reuses the same emulsion/lipoid/particle-size/autoclave template but expands the active universe explicitly to:
- phenyramidol, hexobarbital, mecamylamine, quinidine, chloralose, tribromoethanol, pentazocine, phenylbutazone, cyclandelate, benzocaine, secobarbital, quatacaine, lidocaine, thiopental, pentobarbital, methoxyflurane.
This matters for freedom-to-operate mapping because it converts “class” limitations into an explicit enumerated set for the main formulation and method templates.
Dependent Claims: What Add Specific Patent Hooks (and What Those Hooks Mean for FTO)
Dependent claims add three kinds of limitations:
- Specific active-agent species (compound-level fences).
- Specific emulsion composition components (lipoid sources, stabilizer systems, glycerol, polymer classes).
- Stability/freeze capability and duration assertions (freeze tolerance; longer duration vs water-soluble salts).
Drug species fences (Claims 2-6 and the compound lists later)
Claim 1’s class framing is tightened through dependent claims, including:
- Claim 2 (central depressant species set): hexobarbital, secobarbital, thiopental, pentobarbital, diazepam.
- Claim 3 (anaesthetic species set): hexylether, tribromoethanol, halothane.
- Claim 4 (analgesic species set): pentazocine, phenylbutazone, benzocaine, quatacaine, lidocaine.
- Claim 5 (spasmolytic species set): mecamylamine, cyclandelate.
- Claim 6 (vasodepressant species set): quinidine, cyclandelate.
Practical impact: If an IV oil-in-water emulsion product uses any of these named oil-soluble actives dissolved in the inert lipoid at submicron droplet sizes, the likelihood of hitting the claim family is materially higher.
Stabilizer and lipoid system fences (Claims 9-12, 15, 18-20, 21-23)
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Claim 9 (lipoid oil source): lipoid is from soybean oil, cottonseed oil, coconut oil, olive oil.
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Claim 10 (stabilizer component set): phosphatide, polypropylene glycol, polyethylene glycol, polyglycerol monooleate, polyoxyethylene derivative of fatty acids.
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Claim 11 (phosphatide): stabilizer includes a phosphatide.
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Claim 12 (polyoxyethylene derivative): stabilizer includes polyoxyethylene derivative of fatty acids.
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Claim 15 (egg phosphatide): phosphatide is egg phosphatide.
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Claim 16-17 (glycerol): contains glycerol; about 2.5% by weight per 100 mL.
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Claim 18-20 (diazepam + specific stabilizer package):
- active is diazepam;
- stabilizer also contains acetylated monoglycerides;
- amounts in Claim 19:
- diazepam: 0.5 g / 100 mL
- phosphatide: 1.2 g / 100 mL
- acetylated monoglyceride: 5.0 g / 100 mL
- soybean oil: 15 g / 100 mL
- Claim 20: further contains about 2.5 g glycerol.
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Claim 21 (method/composition hybrid depending on numbering, but still formulation-limited):
- active selected from chloralose, benzocaine, secobarbitol
- stabilizer containing a monoglyceride.
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Claim 22 (active set + block copolymer):
- active selected from chloralose, pentazocine, cycloandelate, quatacaine, lidocaine, phenylbutazone, thiopental, pentobarbitol
- stabilizer containing a block polymer of ethylene oxide and propylene oxide.
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Claim 23 (adds acylated monoglyceride):
- includes an acylated monoglyceride
- active selected from phenylbutazone, lidocaine, thiopental, pentobarbitol.
Practical impact: Even if a product avoids a named active species, it can still land within the claim family if an alternative dependent claim still covers the active and the stabilizer selection. Conversely, if it matches one of these species and uses one of these emulsifier/stabilizer stacks, the scope narrows quickly and design-around options shrink.
Stability and performance assertions
- Claim 13: active provides longer duration than corresponding water-soluble salts.
- Claim 25: composition capable of withstanding freezing.
These are typically used to strengthen formulation differentiation in prosecution or to support commercial value arguments. For infringement, the more relevant elements remain the emulsion structure, particle size, and dissolution in inert lipoid.
Method Claims: What Conduct Gets Captured (Claims 26-44)
The method claims track the composition language but convert it into intravenous administration of the same defined formulation.
Claim 26 (method) maps directly to Claim 1
Claim 26 recites intravenously administering the autoclave-capable, stable oil-in-water emulsion with:
- inert lipoid hydrophobic phase
- active predominantly dissolved in lipoid
- submicron mean particle size < 1 micron
- rapid onset effect language
- active selected from central depressants, analgesics, muscle relaxants, vasodepressants.
Claims 27-40 (method dependents) map to composition dependents
- Claim 27: lipoid contains soybean/cottonseed/coconut/olive oil.
- Claim 28: stabilizer contains at least one member from the same set as Claim 10.
- Claim 29: stabilizer includes phosphatide.
- Claim 30: includes polyoxyethylene derivative of fatty acids.
- Claim 31: active provides longer duration than water-soluble salts.
- Claim 32: lipoid is soybean oil.
- Claim 33: phosphatide is egg phosphatide.
- Claim 34-35: contains glycerol, with the same about 2.5% by weight per 100 mL.
- Claim 36: active is phenyramidol.
- Claim 37-39: diazepam with stabilizer containing acetylated monoglycerides, with the same quantified amounts.
- Claim 40: composition capable of withstanding freezing.
Claims 41-44 (method with narrower active selections + stabilizer systems)
- Claim 41: active selected from chloralose, benzocaine, secobarbitol; stabilizer containing monoglyceride.
- Claim 42: active selected from chloralose, pentazocine, cycloandelate, quatacaine, lidocaine, phenylbutazone, thiopental, pentobarbitol; stabilizer is a block polymer of ethylene oxide and propylene oxide.
- Claim 43: further includes an acylated monoglyceride; active selected from phenylbutazone, lidocaine, thiopental, pentobarbitol.
- Claim 44: hexobarbitol predominantly dissolved in lipoid; mean particle size < 1 micron.
Scope Summary: The “Claim Coverage Box” You Can Use for FTO Triage
What a product must do to be inside the claim box
A potentially infringing product must satisfy, at minimum:
- Form: stable oil-in-water emulsion suitable for IV administration
- Processing: withstands autoclaving
- Dispersed phase: pharmacologically inert lipoid dispersed as hydrophobic droplets
- Drug placement: the active is oil-soluble and is predominantly dissolved in the lipoid
- Droplet size: mean particle size < 1 micron
- Active selection: active is within the enumerated species lists and/or class definitions:
- central depressants (hexobarbital, secobarbital, thiopental, pentobarbital, diazepam)
- analgesics (pentazocine, phenylbutazone, benzocaine, quatacaine, lidocaine)
- spasmolytics (mecamylamine, cyclandelate)
- vasodepressants (quinidine, cyclandelate)
- plus the expanded set in Claim 8 (includes phenyramidol, chloralose, tribromoethanol, methoxyflurane, etc.)
What pushes a design into specific dependent-claim risk
- soybean/cottonseed/coconut/olive oil as lipoid (Claim 9 and Claim 14)
- phosphatide-based stabilization and/or egg phosphatide (Claims 10-11, 15; method claims parallel)
- glycerol at ~2.5% w/w per 100 mL or 2.5 g (Claims 17 and 20, method claims 35 and 39)
- acetylated/acylated monoglycerides (Claims 18-20, 21-23)
- block polymer of ethylene oxide/propylene oxide (Claim 22)
- freezing capability (Claim 25, method claim 40)
Patent Landscape Notes for RE32393 (How It Likely Sits in a Landscape)
No priority, issue, assignee, expiration, or family identifiers are provided in the prompt. Without those, a complete landscape (inventor/assignee mapping, continuation chain, prosecution history, citations to related patents, and term-expiry schedule) cannot be produced accurately.
What can be concluded from the claim architecture itself is the competitive map shape:
Landscape hot spots
- IV injectable emulsions using oil-soluble drugs dissolved in inert oils with submicron droplet sizes.
- Autoclave-stable emulsion technologies for barbiturates, diazepam, local anesthetic/analgesic agents, and related oil-soluble central nervous system actives.
- Emulsifier/stabilizer stacks: phosphatides, glycerol, mono-/acylated monoglycerides, and EO/PO block polymers.
Design-around pressure points
- Avoiding submicron mean droplet size is a high-friction route because it is a core claim limitation.
- Avoiding “predominantly dissolved” can be difficult if the formulation uses true solubilization into the lipoid phase rather than suspension.
- Avoiding named actives is more straightforward when the selected active is not in the enumerated list, but Claim 1’s broad class language can still capture class-defined actives unless the active is outside those class definitions.
Key Takeaways
- RE32393’s claim center is an IV autoclave-stable oil-in-water emulsion with an inert lipoid hydrophobic phase, submicron mean particle size (< 1 micron), and an oil-soluble active predominantly dissolved in the lipoid.
- Active selection is the gating element: Claim 1 uses class language (central depressants, analgesics, spasmolytics, muscle relaxants, vasodepressants) and Claim 8 provides a broad explicit species list including diazepam, barbiturates, lidocaine, benzocaine, tribromoethanol, chloralose, phenylbutazone, pentazocine, quinidine, cyclandelate, quatacaine, thiopental, pentobarbital, methoxyflurane, phenyramidol.
- Dependent claims add formulation-specific fences: soybean oil, phosphatides (including egg phosphatide), glycerol at specified levels, acetylated/acylated monoglycerides, and EO/PO block polymer stabilizers.
- Method claims mirror the composition limitations, so manufacture + distribution + IV administration of a covered product is within the claim risk set.
FAQs
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Does RE32393 cover suspensions or only emulsions?
It covers stable oil-in-water emulsions with a hydrophobic lipoid phase dispersed in a hydrophilic phase.
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What droplet size threshold matters most?
The claims require mean particle size less than 1 micron for the lipoid dispersed in the emulsion.
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Is the active required to be dissolved in the oil phase?
Yes. The active is an oil-soluble agent predominantly dissolved in the lipoid in the hydrophobic phase.
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Do dependent claims create narrower “product profiles” that increase infringement risk?
Yes. They add specific combinations like diazepam + phosphatide + acetylated monoglycerides + soybean oil + glycerol and specific stabilizers like EO/PO block polymer.
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Can changing the active avoid the patent?
The safest path is selecting an active that is outside the enumerated species and class definitions in the claims. If the active remains within the listed universe, design-around must focus on the emulsion structure, dissolution requirement, and particle size.
References
[1] United States reissue patent RE32393 (claims as provided in the prompt).
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