Executive summary
US Patent 10,213,442 claims a broad sustained/controlled release oral vitamin D composition based on 25-hydroxyvitamin D2 and/or 25-hydroxyvitamin D3, with claim 1 acting as the core “composition + sustained release + multi-drug combination” hook. Downstream claims narrow into specific oral delivery architectures: matrix dispersion, encapsulation with coating materials, defined melting-point relationships, lipid matrices, and permeable overcoatings with defined release mechanisms (diffusion, disintegration, or both). Independent-style coverage also exists for D3-only controlled release using pharmaceutical-grade matrix excipients and rate-controlling constituents including poly(meth)acrylate. The landscape risk for generic entry is primarily claim-scope circumvention (removing certain co-ingredients from the combination claim 1 ecosystem, and/or changing release architecture away from the claimed matrix/coating/melting-point/release-mechanism formulations).
US Patent 10,213,442 scope and claims summary: sustained release 25-hydroxyvitamin D2/D3 oral dosage formulations
What the patent broadly covers (functional + ingredient scope)
The patent’s claim set targets an oral sustained/controlled release formulation containing:
- Active(s): 25-hydroxyvitamin D2, 25-hydroxyvitamin D3, or a combination.
- Sustained/controlled release structure: matrix dispersion and/or coating-encased delivery system.
- Optional combination partners: in claim 1, a wide set of co-therapies spanning calcium, bisphosphonates, calcimimetics, nicotinic acid, iron, phosphate binders, glycemic and hypertension control agents, and antineoplastic agents.
Key practical implication:
- Claim 1 is a “combination product” style claim whose literal scope can be satisfied by formulation plus the presence of one or more specified adjunct drug categories, which can increase infringement leverage for combination labeling or co-formulation strategies.
- At the same time, many “real-world” commercial products may avoid literal infringement by not including those adjunct categories in the same dosage form, or by using a different release mechanism and/or delivery structure.
What patents protect sustained release oral 25-hydroxyvitamin D2/D3 combinations in the US? (Claim 1 coverage and interpretation)
Claim 1 is the widest anchor claim
Claim 1 recites:
A sustained release oral dosage formulation comprising 25-hydroxyvitamin D2, 25-hydroxyvitamin D3, or both, in combination with one or more calcium salts, bisphosphonates, calcimimetics, nicotinic acid, iron, phosphate binders, cholecalciferol, ergocalciferol, active vitamin D sterols, glycemic control agents, hypertension control agents, and antineoplastic agents.
Scope vectors embedded in Claim 1
-
Active vitamin D ingredient scope
- D2 and/or D3 via 25-hydroxy forms. The use of “25-hydroxy” is limiting versus “cholecalciferol/ergocalciferol” being merely co-ingredients allowed in some embodiments.
-
Sustained release requirement
- “Sustained release oral dosage formulation” imposes a release-profile limitation, typically tested via dissolution behavior. This can be a battleground for infringement in generic products.
-
Multi-class co-ingredient menu
- The phrase “one or more” makes the claim easier to meet if the accused product includes any single member of the listed categories.
- Inclusion of “phosphate binders” and “calcimimetics” is notable for patients with mineral bone disorders and CKD-related hyperparathyroidism contexts; inclusion of “antineoplastic agents” broadens potential oncology-combination relevance.
How Claim 1 is likely used in enforcement
- Asserting infringement against products explicitly marketed as combination vitamin D therapies in one capsule/tablet.
- Using claim dependencies (claims 2-9) to narrow to single co-ingredient categories for alternative non-invalidation pathways.
Which drug product elements satisfy infringement for US 10,213,442 claim 1 (active, sustained release, and co-ingredients)?
Literal elements (as written)
- The product is an oral sustained release dosage form.
- It contains 25-hydroxyvitamin D2 and/or D3.
- It includes at least one of the listed co-ingredient classes as part of the same formulation.
Circumvention levers
- Remove all listed co-ingredient classes from the dosage form.
- Keep 25-hydroxyvitamin D2/D3 but change dosage architecture so it is not a “sustained release” formulation under the patent’s functional/dissolution characterization.
- Use 25-hydroxyvitamin D but change the combination: e.g., use adjuncts not covered by the claim 1 category list.
How does US 10,213,442 narrow scope in dependent claims 2–9 (single-category combination coverage)?
Claims 2–9 provide dependent variations that map claim 1 into narrower “any-one-of-these categories” sub-portfolios:
| Claim |
Co-ingredient category explicitly required (in combination with 25-hydroxyvitamin D2/D3) |
| 2 |
One or more calcium salts |
| 3 |
One or more bisphosphonates |
| 4 |
nicotinic acid |
| 5 |
iron |
| 6 |
phosphate binders |
| 7 |
glycemic control agents |
| 8 |
hypertension control agents |
| 9 |
antineoplastic agents |
Enforcement value
- Each dependent claim can function as a fallback if an accused product disputes the presence of some other class members listed in claim 1 or if validity is attacked against the broader “menu” language.
What formulations are protected by US 10,213,442 independent “matrix + coating” claims (claims 10–22)?
Claims 10–22 define delivery architectures
- These claims focus on physical form: dispersion within a matrix, encasement with coating material, and release behavior.
Claim 10: matrix dispersion plus encasing coating
“A sustained release oral dosage formulation … dispersed within a matrix and encased with a coating material.”
Claim 11: melting point relationship
- Melting point higher than body temperature but lower than melting temperature of coating material.
- This introduces a materials-property constraint that can be difficult to reproduce exactly.
Claims 12–17: lipid matrix chemistry
- Claim 12: matrix comprises a lipid.
- Claims 13–17: lipid is defined by subtypes:
- glycerides (14)
- fatty acids (15)
- fatty alcohols (16)
- fatty acid esters (17)
Claims 18–21: permeable overcoating and release mechanism
- Claim 18: permeable overcoating.
- Claim 19: release by diffusion.
- Claim 20: release by disintegration.
- Claim 21: release by combination of diffusion and disintegration.
Claim 22: matrix solid at body temperature
- “dispersed within a matrix which is solid at body temperature.”
- This is a thermal-state limitation that impacts formulation design for dissolution and release kinetics.
Enforcement value
- The physical-form claims allow targeting not just “ingredient combinations” but the internal formulation system, including excipient/material selection and thermal properties.
What controlled-release D3 formulations are protected (claims 23–31): matrix excipients, rate controlling constituents, and poly(meth)acrylate?
Claims 23–31 shift to D3-centered controlled release
- Claim 23: controlled release oral formulation comprising 25-hydroxyvitamin D3 and pharmaceutical-grade matrix excipient.
- Claim 24: controlled release formulation with matrix containing mixture of rate controlling constituents and excipients.
- Claim 25: encased with coating material.
- Claim 26–27: rate controlling constituents are lipophilic and encased with coating material.
Claim 28 is a standout material-specific limitation
- Rate controlling constituent comprises a poly(meth)acrylate polymer.
This is a distinct formulation-enabling element with a clearer design-around map:
- If an accused product uses different polymer families for rate control, claim 28 is harder to meet literally.
Capsule and composition claims
- Claim 30: capsule comprising 25-hydroxyvitamin D3 and controlled release excipient.
- Claim 31: pharmaceutical composition comprising 25-hydroxyvitamin D3 and controlled release delivery system.
Scope implication
- The D3 cluster likely covers a commercial “controlled release D3” format even when not using D2 or combination partners in claim 1.
What is the effective breadth and which claims are most likely to be asserted in practice?
Breadth ranking (most to least)
- Claim 1: sustained release oral + D2/D3 + combination with any one of many co-ingredient categories.
- Claims 2–9: same core with narrower co-ingredient categories.
- Claims 10–12 / 18 / 22: delivery architecture constraints that could cover a wide range of excipient specifics as long as matrix/coating and thermal/solid-state conditions fit.
- Claims 13–17: lipid subtype limitations narrow further.
- Claims 19–21: defined release mechanism can be contested with dissolution and modeling evidence.
- Claim 11: strict melting-point relationship adds a materials-property carve-in.
- Claim 28: poly(meth)acrylate is specific and is more vulnerable to design-around.
Litigation posture you’d expect
- Plaintiffs often assert:
- claim 1 first (broad “menu” + sustained release);
- in the alternative, assert architecture-based claims (10, 18, 22) that can be met even if combination categories are disputed;
- use claim 28 as a targeted fallback if the accused product’s rate-controlling polymer matches.
How does this claim set map to likely generic entry risks for 25-hydroxyvitamin D oral sustained/controlled release?
Key entry pathways vs infringement exposure
-
Generic with same active(s) but different release system
- Risk persists under claims 10/18/22 if the generic uses a matrix + coating and meets thermal-state constraints.
- Lower risk under claim 28 if generic avoids poly(meth)acrylate.
-
Generic that removes combination co-ingredients
- Claim 1 can be avoided if the dosage form excludes all the specified co-ingredient categories.
- Architecture-based claims (10–22) remain possible if the generic still uses the matrix/coating system.
-
Generic that changes to diffusion-only or disintegration-only profiles
- If the product is engineered toward diffusion-only or disintegration-only, it may still fall into claim 19 or claim 20 depending on the mechanism characterization.
- Mixed diffusion/disintegration (claim 21) can capture hybrid profiles.
Design-around checklist implied by the claims
- Matrix: avoid “lipid matrix” if targeting claims 12–17; but lipid is not required for claims 10 or 18.
- Coating: avoid “encased” or “permeable overcoating” structures if possible.
- Thermal: avoid matching melting-point relationships for claim 11 and avoid matrix solid at body temperature for claim 22 (often hard because many matrices are solid in normal conditions).
- Polymer: if targeting claim 28, avoid poly(meth)acrylate rate-controlling constituents.
What is the patent landscape strategy implied by US 10,213,442: freedom-to-operate and licensing targets
Landscape patterns typically paired with this claim type
Even without enumerating other specific patent numbers here, this claim set suggests an estate that is likely complemented by adjacent patents covering:
- 25-hydroxyvitamin D stabilization and manufacturing.
- Specific excipient systems for controlled release (lipid matrices, polymer rate-controlling layers).
- Co-formulation kits for CKD-mineral bone disorder combinations (calcium/phosphate binders/calcimimetics) and potentially oncology-adjunct regimens.
Where licensing pressure would be highest
- Products that include calcium/bisphosphonate/calcimimetic/iron/phosphate binder combinations in the same sustained release dosage.
- Products that replicate a lipid matrix with coating and defined release kinetics.
Key takeaways
- US 10,213,442 has two main protected themes: (1) sustained release oral vitamin D2/D3 compositions with broad combination adjunct categories under claim 1, and (2) controlled-release oral delivery systems defined by matrix + coating architectures under claims 10–22 and D3-specific controlled release matrices under claims 23–31.
- The “menu” language in claim 1 is the strongest infringement hook for combination products. The physical-form claims (10, 18, 22) can still capture generics that omit co-ingredients if they copy the release architecture and thermal/overcoating characteristics.
- The most design-around-sensitive elements are claim 11 (melting-point relationship) and claim 28 (poly(meth)acrylate rate-controlling constituent).
FAQs
1) Can a product containing only 25-hydroxyvitamin D3 avoid claim 1 of US 10,213,442?
Yes, claim 1 also requires combination with one or more listed co-ingredient categories. A product that contains 25-hydroxyvitamin D3 alone could avoid claim 1 but may still face architecture claims (10–22) or D3 controlled-release claims (23–31).
2) What claim elements most affect whether a generic is captured for infringement?
For generics, the decisive factors are whether the dosage is “sustained/controlled release,” whether it uses a matrix with coating/overcoating, and whether thermal properties and release mechanism align with claims 11, 18–22.
3) Is poly(meth)acrylate required for infringement of the whole patent?
No. Poly(meth)acrylate is explicitly required only for claim 28. Other claims can be met using different matrix excipients or rate-controlling constituents.
4) Does using a lipid matrix automatically trigger infringement of the patent?
Not automatically. Lipid matrices are explicitly required only for claims 12–17. Claims 10, 18, and 22 can still be implicated depending on matrix/coating and thermal-state requirements.
5) How does diffusion vs disintegration matter legally in these claims?
Claims 19–21 define release mechanisms. A formulation engineered to a single mechanism may map to a specific mechanism claim, while mixed profiles can fall under the combined mechanism claim.
References (APA)
No sources were provided for US Patent 10,213,442, its prosecution history, expiration data, Orange Book listings, or related US/EP/CN patent family members.
