United States Patent 8,187,630: Scope of Claims, Enabling Parameters, and Competitive Landscape (Desloratadine-Protection + Pseudoephedrine Sustained Release, Layered Solid)

US Patent 8,187,630 is directed to a layered solid oral composition that combines immediate-release desloratadine with pseudoephedrine in a sustained-release layer, while constraining desloratadine degradation and prescribing acid dissolution performance. The independent claim (claim 1) is defined by a tight product-definition structure (two-layer solid), three technical performance gates (degradation ceiling, acid dissolution window, and antioxidant “protective amount”), and a specific pairing of actives (desloratadine + pseudoephedrine).

This patent’s enforceable value is concentrated in (i) how desloratadine is protected in an immediate-release layer (antioxidants, degradation limit), and (ii) how the immediate-release layer performs under gastric-like conditions (0.1N HCl at 37°C) while (iii) sustaining pseudoephedrine release via a defined sustained-release agent matrix.

What does claim 1 actually cover (core infringement boundary)?

Structural requirements

Claim 1 requires a solid composition with:

Immediate release layer
- Contains desloratadine at an anti-allergic effective amount
- Contains two desloratadine-protective antioxidants
- Antioxidants are “pharmaceutically acceptable” and used at a “desloratadine-protective amount”
Sustained release layer
- Contains pseudoephedrine or a pharmaceutically acceptable salt
- Contains a pharmaceutically acceptable sustained release agent

Quantitative performance gates (key limitation set)

Claim 1 additionally requires BOTH of these conditions:

Desloratadine degradation constraint:
Total amount of desloratadine degradation products ≤ about 2% by weight of the solid composition.
Acid dissolution performance constraint (immediate release behavior):
At least about 80% of desloratadine dissolves in 0.1N HCl at 37°C in about 45 minutes.

Why this matters for scope

The claim is not just “a desloratadine + pseudoephedrine layered tablet.” It is a product claim tethered to measurable chemical stability and measurable dissolution under acid. A design-around must avoid at least one of these binding limitations:

eliminate one of the required layer roles (e.g., remove true immediate-release or true sustained-release),
change the antioxidant system such that you no longer meet the “two antioxidants protective amount” concept as construed,
or fail the stability/dissolution thresholds as measured by the patent test.

How do dependent claims narrow or lock in specific formulation embodiments?

Two-antioxidant specific pairing

Claim 2: The two antioxidants are edetate disodium and citric acid.

This narrows claim coverage to a specific antioxidant pair, which can be a practical differentiation point for generics or line extensions using different protectants (if they also avoid meeting the performance gates).

Layer naming and the two-phase architecture

Claim 3: Recasts the two-layer scheme as immediate-release first layer (desloratadine + at least one antioxidant) and sustained-release second layer (pseudoephedrine + sustained-release agent).
It preserves the same degradation ≤2% and dissolves ≥80% in 0.1N HCl in ~45 min.

Example-anchored drug loadings and explicit excipient architecture

Claim 4: Supplies explicit quantities:
- Immediate release first layer: ~2.5 mg desloratadine
- Immediate release first layer: at least one antioxidant (protective amount)
- Sustained release second layer: ~120 mg pseudoephedrine (or salt)
- plus “pharmaceutically acceptable excipient”
- and preserves the acid dissolution and degradation limits.
Claim 5: Restates the degradation products ≤2% limit as an explicit dependent lock.
Claim 6: Requires that a desloratadine-protective amount of a binder is present in the sustained release layer.

Claim 7: Specific detailed composition (tightest embodiment)

Claim 7 provides a full two-layer tablet composition with mg amounts.

Immediate release first layer (Total 200.00 mg):

Desloratadine, micronized: 5.0 mg
Corn starch: 36.0 mg
Microcrystalline cellulose: 140.7 mg
Edetate disodium: 10.0 mg
Citric acid: 2.0 mg
Talc: 6.0 mg
Dye: 0.30 mg

Sustained release second layer (Total 350.0 mg):

Pseudoephedrine sulfate: 120.0 mg
Hydroxypropyl methylcellulose (HPMC 2208, 100,000 cps): 105.0 mg
Microcrystalline cellulose: 103.5 mg
Hydroxypropyl methylcellulose (HPMC 2910): 10.5 mg
Edetate disodium: 3.5 mg
Silicon dioxide: 5.0 mg
Magnesium stearate (non-bovine): 2.5 mg

Total tablet weight: 550.0 mg.

This claim hard-codes the antioxidant identities, the binder-like presence of edetate disodium in the sustained-release layer, and the sustained-release agent system (HPMC grades) into a single formulation footprint.

Claim 8: Another detailed composition with alternate layer loads

Claim 8 provides a second full embodiment.

Immediate release first layer (Total 100.00 mg):

Desloratadine, micronized: 2.5 mg
Corn starch: 18.0 mg
Microcrystalline cellulose: 71.22 mg
Edetate disodium: 5.0 mg
Citric acid: 1.0 mg
Talc: 3.0 mg
Dye: 0.28 mg

Sustained release second layer (Total 350.0 mg):

Pseudoephedrine sulfate: 120.0 mg
Hydroxypropyl methylcellulose (HPMC 2208): 105.0 mg
Microcrystalline cellulose: 103.5 mg
Edetate disodium: 3.5 mg
Hydroxypropyl methylcellulose (HPMC 2910): 10.5 mg
Silicon dioxide: 5.0 mg
Magnesium stearate: 2.5 mg

Claim 8 preserves the degradation ≤2% constraint.

Claim 9: Dissolution performance explicit dependence

Claim 9: restates at least about 80% desloratadine dissolves in 0.1N HCl at 37°C in about 45 minutes.

What about method claims (medical use scope and “label” coverage)?

The patent includes broad “treating” methods that track the composition claims and cover both:

upper and lower airway passages and skin inflammatory/allergic conditions,
nasal congestion linked to allergic/inflammatory etiologies,
urticaria,
and perennial or seasonal allergic rhinitis nasal and non-nasal symptoms.

Composition-to-method mapping

Composition claim 1 maps to methods 10 and 15 and 20.
Composition claim 3 maps to methods 11, 16, and 21.
Composition claim 4 maps to methods 12, 17, 22.
Composition claim 7 maps to methods 13, 18, 23.
Composition claim 8 maps to methods 14, 19, 24.
Method 25-29 cover allergic/inflammatory airway and skin conditions using claims 3, 4, 7, 8 (and repeats to form a set).

Treatment categories covered

From the claim set provided:

Upper/lower airway passages and skin (allergic/inflammatory conditions):
- claims 10, 11? (nasal congestion) + 25-28 are explicit for this broader set.
Nasal congestion (allergic/inflammatory upper or lower airway):
- claims 11, 12, 13, 14.
Urticaria (signs and symptoms):
- claims 15-19.
Perennial or seasonal allergic rhinitis (nasal and non-nasal symptoms):
- claims 20-24.

Enforcement implications

For a competitor, method coverage matters most when product labeling or prescribing practices align with these indications and the product meets the underlying composition limitations. A product that avoids claim 1’s formulation performance gates should reduce composition-based infringement risk even if the clinical indication overlaps.

What are the non-negotiable technical “hooks” competitors must clear to design around?

1) Desloratadine degradation ceiling

≤ about 2% by weight of total desloratadine degradation products.

This likely acts as a chemistry and manufacturing control limitation. A design-around needs to ensure that the product does not accumulate degradation products above the defined threshold under the patent’s measurement conditions (the claim ties to “in the solid composition,” not a stability study per se, but enforceability will still hinge on the measured content).

2) Acid dissolution window

≥ about 80% desloratadine dissolves in 0.1N HCl at 37°C within ~45 minutes.

This is a performance-based immediate-release requirement. If a competitor changes film coat strategy, excipient porosity, or layer composition in ways that shift dissolution curves below this threshold, the product is less likely to meet claim 1.

3) Two-layer architecture

Immediate release desloratadine layer + sustained release pseudoephedrine layer.

If a product blends both actives into a single matrix or creates a different release profile architecture, it may avoid structural claim language.

4) Antioxidant role

Claim 1 requires two desloratadine-protective antioxidants.
Claim 2 fixes edetate disodium + citric acid.
Claim 6 adds binder in the sustained-release layer as “desloratadine-protective” in that layer.

Practically, the antioxidant system and its placement (including edetate disodium presence in the sustained-release layer in claim 7 and 8) act as a guardrail against “generic antioxidant swaps” unless the new system still avoids meeting the claim definition and still maintains the degradation/dissolution limits.

How broad is the claim set in practice (coverage tiers)?

Tiering view

Tier	Claim(s)	What defines the boundary	Breadth
Broad independent	Claim 1	Two-layer composition, two antioxidants in immediate-release layer, sustained-release pseudoephedrine layer, degradation ≤2 wt%, dissolution ≥80% in 0.1N HCl/37°C/~45 min	Highest
Mid dependent	Claims 2, 3	Specific antioxidants (claim 2) or at-least-one antioxidant plus same performance gates (claim 3)	Medium
Tight quantitative	Claims 4-6	Specific loadings and binder/protective additions	Narrower
Tight embodiment	Claims 7-9	Full mg-by-mg exemplar with specific excipients and HPMC grades	Narrowest

This structure means a competitor can attempt to:

avoid claim 1 by missing any of the three core functional limitations (antioxidant count/identity, degradation threshold, acid dissolution threshold), or
aim for a “close” formulation that still avoids the specific antioxidant pairing and/or performance constraints to escape dependent claims.

Patent landscape: where this patent sits relative to “combination cold/allergy” and stability-and-dissolution formulation patents

Positioning in the landscape

US 8,187,630 is squarely in the “fixed-dose combination with performance constraints” slice of pharmaceutical patenting:

It combines an antihistamine (desloratadine) with a decongestant (pseudoephedrine) in a layered immediate/sustained release format.
It also uses product-defined chemical stability and dissolution performance to differentiate from prior combinations that may not have the same stability/dissolution characterization.

Competitive pressure points

In the US market, competitors typically come from four directions:

Generic versions of the same combination with layered architectures.
Reformulations that adjust excipients and release agents to match dissolution and stability requirements without copying exact antioxidant systems.
New-release architectures (different release mechanisms, different layer thicknesses, different solubilizers) that move the product away from the “test outcomes” in claim language.
Label and indication strategies that focus on narrowed indication coverage, reducing method claim exposure.

For 8,187,630, (1) and (2) are the main infringement risk routes because claim language is anchored to measurable dissolution/stability parameters rather than proprietary equipment or process steps.

Freedom-to-operate levers (what can change without “breaking” the claim)?

This patent is a formulation claim, so small changes can matter if they shift measurable outcomes.

Key levers a product development team can pull to reduce risk (without changing the clinical intent) include:

altering the immediate-release excipient matrix to shift dissolution kinetics under 0.1N HCl/37°C/~45 min,
altering antioxidant selection or distribution such that total degradation does not reach the “≤2% by weight” boundary as interpreted (or, more realistically, ensuring compliance while still not matching claim scope by changing required antioxidant count/identity),
shifting release architecture away from a “first immediate-release layer” plus “second sustained-release layer” structure,
changing sustained-release agent system away from the specific HPMC-based choices in tight embodiments (claims 7-9), while ensuring overall release remains acceptable.

Key takeaways

Claim 1 is a tightly defined two-layer formulation: immediate-release desloratadine + sustained-release pseudoephedrine, with two antioxidants in the immediate-release layer.
The enforceability hinges on two measurable gates: desloratadine degradation products ≤2% by weight and ≥80% desloratadine dissolution in 0.1N HCl at 37°C in ~45 minutes.
Dependent claims add specific antioxidant identity (edetate disodium + citric acid) and mg-level exemplar formulations that strongly narrow the “literal” infringement surface (claims 7-9).
Method claims broaden medical use coverage for nasal congestion, urticaria, and perennial or seasonal allergic rhinitis (nasal and non-nasal symptoms), but they still ride on meeting the underlying composition claim limitations.

FAQs

1) What is the main claim limitation to watch for in formulation infringement analysis?
The combination of (a) desloratadine degradation products ≤ about 2% by weight and (b) ≥ about 80% desloratadine dissolves in 0.1N HCl at 37°C in about 45 minutes, within a two-layer immediate/sustained release structure.

2) Does the patent require a specific pseudoephedrine salt?
Claim 1 allows pseudoephedrine or a pharmaceutically acceptable salt; specific salts are exemplified in dependent claims (e.g., pseudoephedrine sulfate in claim 7 and 8).

3) Are the antioxidants flexible in all claims?
Not fully. Claim 1 requires two antioxidants at desloratadine-protective amounts. Claim 2 fixes edetate disodium + citric acid. Tight embodiments (claims 7-9) also hard-code antioxidant excipient placement and amounts.

4) Which claims provide the tightest formulation “copy points”?
Claims 7 and 8 (full mg compositions by layer) and claim 4 (explicit desloratadine and pseudoephedrine loads). These are the most literal-match targets.

5) Do method claims cover allergic rhinitis and urticaria?
Yes. The claim set includes methods for urticaria (claims 15-19) and perennial or seasonal allergic rhinitis nasal and non-nasal symptoms (claims 20-24), plus broader allergic/inflammatory airway-and-skin conditions and nasal congestion-linked indications.

References (cited)

[1] US Patent No. 8,187,630. Claims provided in the prompt text.

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1110543	⤷ Start Trial	91403	Luxembourg	⤷ Start Trial
European Patent Office	1110543	⤷ Start Trial	CA 2008 00010	Denmark	⤷ Start Trial
European Patent Office	1110543	⤷ Start Trial	300328	Netherlands	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 8,187,630

Summary for Patent: 8,187,630