Details for Patent: 8,367,102

Summary for Patent: 8,367,102

Title:	Pharmaceutical semi-solid composition of isotretinoin
Abstract:	An oral pharmaceutical composition of isotretinoin containing at least two lipidic excipients, one of them being hydrophilic (i.e. having an HLB value superior or equal to 10), the other being an oily vehicle.
Inventor(s):	Francis Vanderbist, Cécile Servais, Phillippe Baudier
Assignee:	GALEPHAR PHARMACEUTICAL RESEARCH Inc
Application Number:	US11/892,363
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,367,102
Patent Claim Types: see list of patent claims	Use; Composition; Formulation; Dosage form;

United States Patent 8,367,102: Scope, Claims, and US Patent Landscape

United States Patent 8,367,102 is directed to oral isotretinoin formulations and oral dosing methods for treating selected skin disorders using a specific lipid excipient system defined by Hydrophobic Lipidic Balance (HLB) thresholds and composition architecture (hydrophilic lipid excipient plus oily vehicle) in a semi-solid preparation.

What does US 8,367,102 claim in one line?

A method of orally treating a skin disorder by administering an oral pharmaceutical composition of isotretinoin that is a semi-solid lipidic formulation containing:

• at least two lipidic excipients
• at least one hydrophilic lipidic excipient with HLB ≥ 10 (and dependent claims push to ≥12 or ≥13)
• an oily vehicle (explicitly recited lipid classes)
• with isotretinoin present as partly suspended and/or partly dissolved (dependent)
• with optional components (surfactants, disintegrants)
• optionally in a pharmaceutically acceptable capsule
• covering disorders including acne, hypertrophic lupus erythematosus, and basal and squamous cell carcinoma (dependent)

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Claim 1: Core inventive concept and functional scope

Independent claim 1 is the scope anchor. It covers both (i) the composition defined by lipid excipient criteria and (ii) the method of use for oral treatment of specified skin disorders.

1) Treatment method

• “method of treating a skin disorder”
• “orally administering to a mammal”
• mammal is later narrowed to “human” (claim 16)

2) API and administration form

• “oral pharmaceutical composition of isotretinoin”
• composition is “a semi-solid preparation containing at least two lipidic excipients”
• semi-solid is central to structure; dependent claims specify suspension/solution status

3) Lipid excipient architecture (the HLB requirement)

• “at least one of them being hydrophilic having a Hydrophobic Lipidic Balance (HLB) value ≥ 10”
• “the other being an oily vehicle”

4) Specific hydrophilic lipid excipient group

The hydrophilic excipient (HLB ≥10) is selected from:

• glycerol macrogolglycerides

This is a hard recitation: the dependent structure ties the HLB-qualified hydrophilic lipid to a defined excipient family.

5) Dose and clinical outcome framing

• “administered in an amount effective to treat the skin disorder” This is a standard outcome phrasing that does not numerically define dose.

6) Skin disorder coverage

Claim 1 explicitly enumerates:

• acne
• hypertrophic lupus erythematosus
• basal cell carcinoma
• squamous cell carcinoma

So claim 1 is broad within dermatology-oncology.

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How do dependent claims narrow or expand the claim 1 scope?

HLB tightening: claims 2 and 3

• Claim 2: hydrophilic lipid excipient has HLB ≥ 12
• Claim 3: hydrophilic lipid excipient has HLB ≥ 13

Practical reading: claim 1 covers a broader HLB window (≥10), and claims 2-3 carve higher-performance sub-ranges.

Isotretinoin phase state: claims 4 and 13-14

• Claim 4: semi-solid where isotretinoin is:
  • “partially in suspension and/or partially in solution”
• Claim 13: composition is a “semi-solid suspension”
• Claim 14: semi-solid contained in a “pharmaceutically-acceptable capsule”

This creates a formulation-state layer that differentiates from purely dissolved, purely solid, or purely emulsion systems.

Oily vehicle identity: claims 5-7

• Claim 5: oily vehicle selected from glycerol macrogolglycerides (note: claim 5 says oily vehicle is one selection; claim 1 already mandates a hydrophilic lipid excipient from glycerol macrogolglycerides. The combination implies glycerol macrogolglycerides may span both “hydrophilic” and “oily vehicle” roles depending on product grade/HBL behavior.)
• Claim 6: oily vehicle selected from:
  • vegetable oils
  • medium chain triglycerides
  • fatty acid esters
  • amphiphilic oil
  • glycerol oleate
  • mixtures
• Claim 7: oily vehicle amount is 5 to 70% by weight

This is a meaningful quantitative handle that can drive design-around attempts around lipid loading.

Surfactant optionality: claims 8-10

• Claim 8: at least one surfactant
• Claim 9: surfactants from a long listed set, including:
  • sorbitan fatty acid esters
  • polysorbate compounds
  • polyoxyethylene sorbitan fatty acid esters
  • sodium laurylsulfate
  • lecithin compounds
  • propylene glycol esters
  • fatty acid esters of propylene glycol
  • fatty acid esters of glycerol
  • polyethylene glycol
• Claim 10: at least one additional surfactant 1 to 10% by weight

These claims create an additional dependent overlay: even if claim 1 is satisfied, adding surfactants can pull the formulation into further coverage.

Disintegrant optionality: claims 11-12

• Claim 11: further comprises at least one disintegrant
• Claim 12: disintegrant from:
  • povidone
  • crossprovidone
  • sodium croscaramellose
  • mixtures

Capsule types: claims 14-15

• Claim 14: semi-solid contained in a capsule
• Claim 15: capsule is:
  • hard gelatin
  • soft gelatin
  • hypromellose
  • starch capsules

Human limitation and disorder-specific dependencies: claims 16-20

• Claim 16: mammal is human
• Claims 17-20: disorder identity narrowed to:
  • acne
  • hypertrophic lupus erythematosus
  • basal cell carcinoma
  • squamous cell carcinoma

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What is the enforceable “shape” of coverage? (Claim-to-design-space map)

Below is a practical claim decomposition, translating language into enforceable technical features.

A. Minimum required features (to hit claim 1)

1. Drug: isotretinoin
2. Dosage form: oral
3. Preparation state: semi-solid
4. Excipient system:
   • at least two lipidic excipients
   • ≥1 hydrophilic lipidic excipient with HLB ≥ 10
   • other excipient is an oily vehicle
   • hydrophilic excipient is specifically glycerol macrogolglycerides
5. Indication: one of the enumerated skin disorders
6. Route: orally administered to a mammal (human in dependent claim 16)

B. Additional features that expand or narrow coverage via dependents

• HLB tighter: HLB ≥12 (claim 2), ≥13 (claim 3)
• Phase state: partial suspension/solution (claim 4), semi-solid suspension (claim 13)
• Oily vehicle amount: 5-70% w/w (claim 7)
• Surfactant inclusion: at least one surfactant (claim 8) from specific families (claim 9), plus an additional surfactant at 1-10% w/w (claim 10)
• Disintegrant inclusion: povidone / crossprovidone / sodium croscaramellose (claim 12)
• Container: capsule types (claim 15)

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What does “HLB” do as a legal lever?

The HLB requirement is the most constraint-heavy language. It converts a broad lipid-excipient concept into a measurable threshold:

• Independent claim: HLB ≥ 10
• Dependent claims: HLB ≥ 12 and HLB ≥ 13

Because claim 1 also hard-codes the hydrophilic lipid excipient group to glycerol macrogolglycerides, infringement depends less on generic surfactants and more on whether the candidate formulation uses a glycerol macrogolglyceride grade meeting the claimed HLB threshold while fitting the semi-solid architecture and isotretinoin inclusion.

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How broad is the indication coverage?

Within claim 1’s enumerated list, coverage spans:

• Acne (common indication)
• Hypertrophic lupus erythematosus (rare dermatologic indication)
• Basal cell carcinoma and squamous cell carcinoma (oncology use)

Claims 17-20 are dependencies that narrow to one disorder at a time, which can matter for validity challenges and for commercial case targeting.

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Patent landscape in the US: what is likely covered vs. what is likely outside

Without issuing-level bibliographic data (patent title, applicants, filing dates, CPC/IPC, prosecution history, and related family members), the landscape can only be mapped to the claim logic exposed here. That said, the claim set signals how US entrants would be assessed.

High likelihood of overlap (format-level)

Formulations that aim to improve oral isotretinoin exposure by using:

• lipid excipients
• hydrophilic lipids with specified HLB ranges
• semi-solid suspensions
• capsule presentation

would be the closest technical neighborhood.

Likely weaker overlap (non-HLB or non-semi-solid)

Design-around attempts that:

• keep lipid systems but remove the HLB-defined hydrophilic glycerol macrogolglyceride element
• shift away from semi-solid into different dosage architectures (for example, purely solution, different emulsion types not meeting claim-defined semi-solid suspension language)
• omit the lipid architecture or change the hydrophilic excipient identity

reduce the chance of matching claim 1’s gating elements.

Likely weaker overlap (dose-range and excipient-load carveouts)

Even if a competitor’s system is lipid-based and oral, it may avoid dependent claims by:

• operating outside the 5 to 70% w/w oily vehicle window (claim 7)
• omitting surfactants/disintegrants or using those not on the recited lists (claims 8-12)
• using a dosage container type not matching claim 15 (though this is typically easy to vary)

These do not necessarily remove claim 1 risk if the independent elements remain satisfied.

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Claim coverage vs. US competitive strategy: infringement risk checkpoints

For a US product development team, the claim language yields a checklist.

Checkpoint 1: Does the formulation use a hydrophilic glycerol macrogolglyceride with HLB ≥ 10?

This is the first gate for claim 1.

Checkpoint 2: Is it semi-solid (and does isotretinoin exist partly in suspension and/or solution)?

Dependent claims enforce this more tightly. But claim 1 already calls for “semi-solid preparation.”

Checkpoint 3: Is there a separate oily vehicle and does the lipid system have at least two lipidic excipients?

Claim 1 requires at least two lipidic excipients with the roles split between hydrophilic and oily.

Checkpoint 4: Is the intended use within the enumerated skin disorders?

Acne and two skin cancers create direct coverage risk.

Checkpoint 5: Are optional ingredients used in ways that pull into dependent claims?

Surfactants/disintegrants/capsule type and oily vehicle content can increase coverage surface area through dependents.

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Key Takeaways

• US 8,367,102 is centered on oral isotretinoin semi-solid formulations using a two-role lipid excipient system: at least one hydrophilic glycerol macrogolglyceride with HLB ≥ 10 plus an oily vehicle.
• HLB is the hardest constraint: independent claim covers HLB ≥ 10; dependents require ≥12 and ≥13.
• Enforceable formulation-state language exists: isotretinoin is “partially in suspension and/or partially in solution,” and the composition is a “semi-solid suspension.”
• Indication coverage includes acne, hypertrophic lupus erythematosus, basal cell carcinoma, and squamous cell carcinoma, with dependent claims narrowing each disorder.
• Dependent claim parameters create additional design paths (oily vehicle 5-70% w/w, surfactant/disintegrant inclusion, and capsule type), but avoiding dependents does not avoid claim 1 if the core HLB-based lipid architecture remains.

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FAQs

1. What is the main novelty anchor in US 8,367,102?
   The use of an oral isotretinoin semi-solid formulation containing hydrophilic glycerol macrogolglycerides with HLB ≥ 10 alongside an oily vehicle.

2. Does claim 1 require specific excipient identities beyond glycerol macrogolglycerides?
   It requires glycerol macrogolglycerides as the hydrophilic lipidic excipient (HLB-qualified) and an “oily vehicle” as the other lipidic component. Surfactants and disintegrants are optional via dependents.

3. Which dependent claims most affect formulation design?
   Claims 2-3 (HLB thresholds), claim 7 (oily vehicle 5-70% w/w), and claims 8-12 (surfactants/disintegrants).

4. Is the patient population limited?
   Claim 1 covers a “mammal”; dependent claim 16 specifies human.

5. Can a product avoid risk by changing capsule type?
   Changing capsule type can avoid claim 15, but it does not avoid claim 1 if the core lipid excipient and HLB requirements remain satisfied.

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References

[1] US Patent 8,367,102 (claims as provided in prompt).

Drugs Protected by US Patent 8,367,102

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: 8,367,102

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Belgium	2000/0111	Sep 22, 2000

International Family Members for US Patent 8,367,102

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	270544
Australia	8943801
Brazil	102013032172