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Patent landscape, scope, and claims: |
United States Patent 10,925,829: Scope, Claims, and Patent Landscape for Fingolimod Lauryl Sulfate Orally Disintegrating Tablets
What does US 10,925,829 claim, in scope terms?
US 10,925,829 is directed to solid orally disintegrating tablets (ODTs) containing fingolimod lauryl sulfate salt at 0.1 mg to 1 mg per tablet, with oral disintegration/dissolution performance defined by USP disintegration apparatus time thresholds and in-mouth disintegration time thresholds, plus stability limits for fingolimod degradation products under defined humidity and temperature stress. The claims also cover formulation excipient systems (sugar alcohols and polymer/binder sets) and a process for generating the lauryl sulfate salt in situ via solution reaction (molar ratio controls), followed by solvent removal.
Core claim pillars (as claimed)
- Active + dose range
- Fingolimod lauryl sulfate salt: “about 0.1 mg to about 1 mg” (Claims 1, 14, 17).
- Oral disintegration performance
- USP disintegration apparatus: < 2.5 min (Claim 1), with dependent narrowing to < 2.0 min (Claim 2), < 1.5 min (Claims 3, 14, 24).
- Oral cavity dissolution/disintegration (instructed no-bite/no-chew): < 60 sec (Claims 4, 14, 25), with dependent narrowing to < 45 sec (Claims 5) and < 30 sec (Claims 6, 27).
- Formulation excipient scope
- Broad class list in Claim 1 and Claim 17: sugar alcohols, lubricants, fillers, binders, disintegrants, glidants, solubilizing agents, flavoring agents, gas producing agents, pH adjusting agents, antioxidants, chelating agents (open-ended “one or more”).
- Narrow dependent embodiments specify:
- Sugar alcohols selected from a defined list (Claim 8).
- Binders selected from a defined list (Claims 10-11, 16).
- Salt-form vs excipient formulation
- The salt is explicitly “fingolimod lauryl sulfate salt” (Claim 1, 14).
- The process claim requires reacting fingolimod (or salt) with an anionic lauryl sulfate (or salt) (Claim 17), with molar ratio limits (Claims 18-20).
- Stability / degradation-product limits
- Individual fingolimod degradation product: ≤ 2.0%
- Total fingolimod degradation products: ≤ 2.5%
- Under: sealed bottle or aluminum foil pouch, 40°C, 75% RH, 1 month (Claims 13, 14, 23).
This yields a relatively tight “active + salt identity + disintegration performance + degradation acceptance under stress” claim strategy, with flexibility in excipient selection.
How broad are the independent claims (1, 14, 17)?
Claim 1 (independent)
A solid ODT comprising:
- fingolimod lauryl sulfate salt: about 0.1 mg to 1 mg
- excipients selected from the listed excipient classes
- tablet disintegrates in < 2.5 min (USP disintegration)
- does not require the oral cavity time threshold nor the degradation limits
Breadth drivers
- Excipients are open-ended within enumerated categories.
- Performance is anchored to USP disintegration only (<2.5 min).
Claim 14 (independent, performance + stability + excipient selections)
A solid ODT comprising:
- fingolimod lauryl sulfate salt: 0.1 mg to 1 mg
- excipients must include:
- sugar alcohol from a specified list (Claim 14 b)
- binder from a specified list (Claim 14 c)
- optional additional excipients within the same class list
- disintegration:
- USP: < 1.5 min
- in-mouth (no bite/no chew): < 60 sec
- stability:
- individual degradation product ≤ 2.0%
- total degradation products ≤ 2.5%
- after 40°C/75% RH/1 month in sealed bottle or foil pouch
Breadth drivers
- Sugar alcohol and binder are constrained to listed sets.
- Performance is more demanding than Claim 1 (USP <1.5 min + in-mouth <60 sec).
- Stability requirement is additional narrowing.
Claim 17 (independent, process claim)
A solid orally disintegrating tablet prepared by:
1) dissolve fingolimod (or acceptable salt) in solvent
2) dissolve anionic lauryl sulfate (or salt) in solvent
3) allow fingolimod and lauryl sulfate to react
- molar ratio: 1 mole fingolimod : 3 moles or less lauryl sulfate
4) remove solvent
- and the resulting tablet disintegrates <2.5 min (USP)
Breadth drivers
- Excipients are not explicitly required in Claim 17 itself, though Claim 22 adds a dependent excipient list.
- The key differentiator vs generic “mix and dry” approaches is the salt-forming reaction in solution with molar ratio control, plus the performance requirement tied to USP disintegration.
What do the dependent claims add (practical claim fencing)?
Below is a claim-by-claim mapping of what each dependent claim tightens.
Performance tightening
- USP disintegration:
- Claim 2: < 2.0 min
- Claim 3: < 1.5 min
- Claim 24: < 1.5 min (process-based)
- In-mouth disintegration/dissolution:
- Claim 4: < 60 sec (no bite/no chew; tongue or cheek/gum placement)
- Claim 5: < 45 sec
- Claim 6: < 30 sec
- Claim 25: < 60 sec (process-based)
- Claim 26: < 45 sec
- Claim 27: < 30 sec
Excipients tightening
- Sugar alcohol requirement and list:
- Claim 7: excipients comprise a sugar alcohol
- Claim 8: sugar alcohol is selected from the listed members (arabitol, mannitol, sorbitol, dextrose, dextrin, sucrose, maltose, xylitol, maltitol, lactitol, erythritol, isomalt, mixtures)
- Binder requirement and list:
- Claim 9: excipients comprise a binder
- Claim 10: binder selected from povidone, hypromellose, hydroxypropylcellulose, hydroxyethylcellulose, polymethacrylates, methyl cellulose, gelatin, ethyl cellulose, mixtures
- Claim 11: binder comprises gelatin
- Claim 16: binder comprises gelatin
- Lyophilization:
- Claim 12: tablet prepared by lyophilization
- Claim 15: lyophilized tablet (dependence on Claim 14)
- Claim 28: lyophilized tablet (dependence on Claim 17)
Stability tightening
- Claims 13, 14, 23:
- individual degradation product ≤ 2.0%
- total degradation products ≤ 2.5%
- after 1 month at 40°C and 75% RH
- tested in sealed bottle or aluminum foil pouch
Salt-forming reaction tightening
- Molar ratio limits (Claims 18-20) refine Claim 17:
- Claim 18: 1 : 0.5 to 3 moles lauryl sulfate
- Claim 19: 1 : 0.5 to 2 moles lauryl sulfate
- Claim 20: 1 : 0.5 to 1.5 moles lauryl sulfate
- Fingolimod starting material:
- Claim 21: fingolimod used is fingolimod hydrochloride
Excipient class in process claim
- Claim 22: process-based tablet includes excipients selected from the enumerated class list.
What is the claim “center of gravity” for infringement risk?
The patent most strongly targets:
- products where the active is explicitly the lauryl sulfate salt (not just fingolimod with lauryl sulfate present),
- fast oral disintegration meeting defined thresholds, and
- stability limits for degradation under stress.
If a competitor product uses a different salt (e.g., different counterion) or does not meet the disintegration or stability limits, it can fall outside the tightest dependent claim layers. If the competitor uses the same salt and meets performance, then they face exposure under Claim 1 and related performance dependent claims even without the in-mouth and degradation limitations.
Claim map: “coverage lattice” by attribute
A compact way to view coverage:
| Attribute |
Claim(s) that require it |
Practical effect |
| Fingolimod lauryl sulfate salt |
1, 14, 17 |
Identity lock: salt is required |
| Dose per tablet 0.1 mg to 1 mg |
1, 14 |
Limits formulation changes tied to mg strength |
| USP disintegration <2.5 min |
1, 17 |
Baseline speed threshold |
| USP disintegration <2.0 min |
2 |
Narrower performance window |
| USP disintegration <1.5 min |
3, 14, 24 |
Higher speed threshold |
| In-mouth time <60 sec (no bite/no chew; tongue or cheek/gum) |
4, 14, 25 |
Orally directed dissolution/disintegration |
| In-mouth <45 sec |
5, 26 |
Faster threshold |
| In-mouth <30 sec |
6, 27 |
Fastest threshold |
| Sugar alcohol excipient required + list |
7, 8; also in 14(b) |
Excludes formulations lacking sugar alcohol or outside list |
| Binder excipient required + list |
9-11, 16 |
Excludes formulations using binders not listed |
| Binder = gelatin |
11, 16 |
Tight dependent option |
| Lyophilized/lyophilization |
12, 15, 28 |
Locks manufacturing method in dependent layers |
| Stability limits (degradation %) |
13, 14, 23 |
Adds chemical/analytical acceptance window |
| Salt-forming process in solution with defined molar ratio |
17-20 |
Locks method and stoichiometry into process claim layers |
| Fingolimod hydrochloride as starting material |
21 |
Narrows starting material in process claims |
What does the process claim cover beyond the formulation claims?
Claim 17 is designed to capture manufacturing-route variants, even when final excipient composition is not fully specified in the independent formulation claims.
The process requires:
- solvent dissolution of fingolimod (or acceptable salt) and lauryl sulfate (or salt),
- reacting them with molar ratio constraints (Claim 17 overall; Claims 18-20 refine),
- solvent removal,
- and resulting disintegration performance (<2.5 min USP).
This creates a route-based barrier for competitors that attempt to form the lauryl sulfate salt via different chemistry (e.g., different order of addition, different salt-forming method, non-solution formation, different stoichiometric regime), or that use a different counterion.
How does this patent fit into a broader fingolimod ODT salt/formulation landscape?
Without inserting unverified bibliographic details for overlapping patents you have not provided, the landscape can be framed by the structural features that are typical of defensible formulation IP around oral disintegrating products:
- Salt identity is used as the main differentiator
- Here, the specific counterion is lauryl sulfate and the claims require the active is the fingolimod lauryl sulfate salt.
- Performance thresholds are used to lock product phenotype
- USP disintegration times and in-mouth time windows act as measurable endpoints.
- Stress stability and degradation specs are used to block “works-on-day-one” workarounds
- The claims tie degradation acceptance to a specific stress regimen (40°C/75% RH/1 month) and container types (sealed bottle or foil pouch).
- Manufacturing route can be separately protected
- Claim 17 adds a stoichiometry-controlled reaction in solution followed by solvent removal, plus a performance requirement.
From an enforcement and freedom-to-operate standpoint, this design means competitors face layered challenges:
- reformulation (different salt, different excipients, different binders),
- reprocessing (different manufacturing method),
- reformulation plus test-driven repackaging (disintegration and degradation specs).
What are the main “workaround levers” implied by the claim set?
Because the claims repeatedly constrain measurable endpoints and identity, workaround paths typically run through at least one of these levers:
| Lever |
Claimed element being moved |
Claim(s) affected |
| Counterion change |
Replacing lauryl sulfate salt with another salt form |
1, 14, 17 |
| Slower disintegration |
Failing the USP or in-mouth time thresholds |
1-6, 14, 24-27 |
| Remove required excipient classes |
Eliminating sugar alcohol or using non-listed sugar alcohols |
7-8; 14(b) |
| Binder substitutions |
Using binder types not listed |
10; 14(c) |
| Avoid lyophilization |
Different dosage form processing |
12, 15, 28 |
| Avoid specified salt-forming stoichiometry |
Changing fingolimod:lauryl sulfate molar ratio or reaction route |
17-20 |
| Stability acceptance failure |
Allow degradation product levels beyond limits under stress |
13, 14, 23 |
Key Takeaways
- US 10,925,829 is built around a specific active salt phenotype: fingolimod lauryl sulfate salt at 0.1 mg to 1 mg per ODT.
- The strongest claim layers require fast disintegration defined by USP time (<2.5 min baseline; <1.5 min for narrower claims) and in-mouth disintegration (<60 sec down to <30 sec) under a no-chew/no-bite instruction.
- The narrowest coverage layers add stability constraints: ≤2.0% individual and ≤2.5% total fingolimod degradation products after 40°C/75% RH/1 month in sealed bottle or foil pouch.
- Excipients and manufacturing route are separately fenced via dependent claims for sugar alcohols, binders (including gelatin), and lyophilization.
- Process protection exists: Claim 17 covers formation of the lauryl sulfate salt through solution reaction with controlled fingolimod:lauryl sulfate molar ratios, tied to disintegration performance.
FAQs
1) Which single feature most directly distinguishes the product covered by US 10,925,829?
The active is fingolimod lauryl sulfate salt, required in Claims 1, 14, and 17.
2) If a tablet meets USP disintegration <2.5 minutes but fails in-mouth <60 seconds, which claims may still apply?
Claims anchored only to USP <2.5 minutes include Claim 1 and Claim 17 (process-based), while the <60 sec limitation is required for Claims 4, 14, and 25 and their faster dependents.
3) How do the stability limits constrain formulation changes?
They require fingolimod degradation product levels capped at ≤2.0% individual and ≤2.5% total after 40°C/75% RH/1 month in sealed bottle or aluminum foil pouch (Claims 13, 14, 23).
4) Does US 10,925,829 include lyophilized tablets as a protected embodiment?
Yes. Lyophilization is explicitly recited in Claims 12, 15, and 28.
5) What manufacturing-related element is protected beyond mixing?
Claim 17 protects a solution reaction between fingolimod (or salt) and anionic lauryl sulfate (or salt) with controlled molar ratio ranges (Claims 17-20), followed by solvent removal, tied to USP disintegration performance.
References
- US Patent 10,925,829. Claims 1-28 (provided claim text).
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