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Patent landscape, scope, and claims: |
US Patent 10,558,394 (Buprenorphine/PLGA/N-Methyl-2-Pyrrolidone In Situ Implant): Claim Scope and US Patent Landscape
What exactly does US 10,558,394 claim?
US 10,558,394 claims an injectable, flowable pharmaceutical composition that contains buprenorphine (free base or salt), poly(lactide-co-glycolide) (PLGA), and N-methyl-2-pyrrolidone (NMP), where the composition transforms in situ into an implant when exposed to water/aqueous bodily fluid.
The claims are structured as:
- Composition-level independent scope (Claim 1; and a second independent style centered on Claim 9 and Claim 21 for specific wt% ranges and product forms).
- Dependent claims narrowing wt% ranges, PLGA grade features (copolymer ratios and MW and terminal group), dose amount ranges, and device containers/syringes.
Core mandatory elements across the claim set
| Claim element |
Claim language (summary) |
Coverage effect |
| Drug |
Buprenorphine free base or pharmaceutically acceptable salt (claims 1, 2-6, 7) |
Enables both salt and free base positions, but later claims focus on free base |
| Polymer |
PLGA copolymer present at ~5 wt% to ~70 wt% (claim 1 and several dependent range claims) |
Defines the biodegradable matrix that precipitates/solidifies in situ |
| Solvent/plasticizer |
N-methyl-2-pyrrolidone as the organic liquid (claims 1, 9, 21, 24) |
Solvent identity is a key infringement driver and a likely design-around lever |
| In situ transformation |
Explicitly recited for several claims (claims 13, 22, 25, 28) |
Limits some claims to in vivo/wet-insertion behavior rather than generic injectables |
Independent claim scope: what is the outer boundary?
Claim 1 (broadest composition-without-form factor constraints)
An injectable flowable composition comprising:
- Buprenorphine: 10 wt% to about 50 wt% (free base or salt)
- PLGA: about 5 wt% to about 70 wt%
- NMP: (implied by remainder; not separately range-labeled in claim 1, but NMP must be present as the third component)
Key scope levers inside Claim 1 dependents
- Buprenorphine range narrowing: 10–30 wt% (claim 2); ~15–20 wt% (claim 3)
- PLGA copolymer ratio options: 50/50, 55/45, 60/40, 65/35, 70/30, 75/25, 80/20, 85/15, 90/10, 95/5 (claim 5)
- PLGA fixed ratio option: 50/50 (claim 6)
- Buprenorphine form option: free base (claim 7)
Claim 9 (product anchor with specific wt% “about 18/32/50”)
An injectable flowable pharmaceutical composition comprising:
- ~18 wt% buprenorphine free base
- ~32 wt% PLGA
- ~50 wt% NMP
This claim is a tighter “center-of-mass” formulation than Claim 1. It also introduces further material constraints:
- PLGA terminal group: carboxy terminal group (claim 10)
- PLGA MW: ~5,000 Da to ~20,000 Da (claim 11)
- In situ transformation: by contact with water or bodily fluid (claim 13)
- Dose range: ~3 mg to ~300 mg buprenorphine free base (claim 14)
Claim 21 / Claim 24 (range-based formulations with in situ transformation)
These claims shift from “single-point wt%” to a range architecture.
Claim 21
- Buprenorphine free base: ~15 wt% to ~30 wt%
- PLGA: ~5 wt% to ~50 wt%
- NMP: ~30 wt% to ~70 wt%
(then includes in situ transformation in claim 22)
Claim 24
Claim 24 keeps the same buprenorphine/PLGA wt ranges but expands NMP-based organic liquid to include additional co-solvents:
- NMP plus glycerin, propylene glycol, polyethylene glycol, or mixtures (claim 24)
Then includes in situ transformation (claim 25)
Which dependent claims meaningfully narrow scope (and where could competitors design around)?
Buprenorphine constraints
- Free base only: claim 7; and essentially required in claims 9, 14-18, 16-18, 21-28
- Wt% narrowings:
- 10–30 wt% (claim 2)
- ~15–20 wt% (claim 3)
- Dose (mg) range:
- ~3 mg to ~300 mg (claim 8, 14)
- A second dose expression appears as ~3 mg to ~300 mg again (claim 14 repeats that range)
- Expanded dose example: ~9 mg to ~900 mg (claim 16)
PLGA grade constraints
- Copolymer composition list (claim 5): 50/50 through 95/5 explicitly
- PLGA fixed ratio (claim 6): 50/50
- Terminal group (claim 10): carboxy terminal group
- Molecular weight (claim 11): ~5,000 to ~20,000 Da
- Combination (claim 12): 50/50 + carboxy terminal + 5,000–20,000 Da
These constraints create “fences”:
- A formulation using different PLGA ratios outside the listed set could avoid claim coverage that specifically requires those ratios.
- A formulation using PLGA with terminal group chemistry other than carboxy could avoid the narrower claim 10/12 positions.
- A formulation outside MW 5,000–20,000 avoids claims 11/12.
NMP role and potential substitution points
- NMP is required as the organic liquid in claims 1/9/21.
- Claim 24 allows additional organic co-solvents but keeps NMP as part of the biocompatible organic liquid:
- NMP plus glycerin/propylene glycol/PEG (claim 24)
A competitor strategy to reduce risk in the claim set would focus on removing NMP or ensuring the organic liquid does not meet the claim definition “comprising: NMP and [specified cosolvents]” in claim 24. However, the full landscape risk depends on whether other US patents cover alternative solvents in similar matrices; the provided input does not include the citation set for the patent family.
In situ transformation requirement
Claims that explicitly require transformation into an implant upon exposure to water/aqueous medium:
- claim 13
- claim 22
- claim 25
- claim 28
This narrows coverage to compositions exhibiting the claimed in situ behavior. A competitor using a different depot-formation mechanism would seek to avoid that limitation.
Where does the patent attach to products and devices?
The claims extend beyond a composition to:
- Syringe containing the formulation (claim 19; based on claim 9)
- Container containing the formulation (claim 20; based on claim 9)
- A “container comprising… transforms in situ…” limitation appears in claim 28 (based on claim 19 and claim 9 path)
These device claims capture packaging and delivery hardware that contains the protected formulation.
Dose-volume-linked narrowing claims
The patent includes explicit examples linking dosage to volume:
- claim 15: composition of claim 14 having volume about 0.5 mL
- claim 17: composition of claim 16 having volume about 1.5 mL
- claim 18: composition of claim 9 having volume from 0.10 mL to 2.0 mL
These add product-specific guardrails, which can matter for infringement analysis where the competitor markets a specific injection volume per dose.
Claim-to-parameter matrix (practical infringement map)
Below is a map of the protected formulation space as expressed by the claims.
Formulation space in wt% terms
| Parameter |
Broad cover (claim 1) |
Narrow cover (claim 2/3/9/21/24) |
| Buprenorphine (wt%) |
10–50% (free base or salt) |
10–30% (claim 2); ~15–20% (claim 3); ~18% free base (claim 9); 15–30% free base (claim 21/26/27) |
| PLGA (wt%) |
~5–70% |
~32% in claim 9; ~5–50% in claim 21/24 |
| NMP (wt%) |
NMP present as third component (range not explicit in claim 1) |
~50% in claim 9; 30–70% in claim 21 |
PLGA identity constraints
| Feature |
Claims |
| Copolymer ratios allowed |
claim 5 lists 50/50 up to 95/5 |
| 50/50 specifically |
claim 6; also present in claim 12 |
| Carboxy terminal group required |
claim 10; combined in claim 12 |
| MW range |
claim 11 (5,000–20,000 Da); combined in claim 12 |
Transformation behavior
| Feature |
Claims |
| Transforms in situ into implant with water/bodily fluid/aqueous medium |
claim 13; 22; 25; 28 |
Dose and format
| Feature |
Claims |
| Buprenorphine amount (mg) |
3–300 (claim 8; 14); 9–900 (claim 16) |
| Injection volume |
0.5 mL (claim 15); 1.5 mL (claim 17); 0.10–2.0 mL (claim 18) |
| Syringe/container |
claim 19; claim 20; plus transformation-based container claim 28 |
US patent landscape: what can be concluded from the provided record?
No patent citations, family members, prosecution history, examiner references, or related US application publication numbers were provided for US 10,558,394. Without those bibliographic and citation facts, a complete and accurate landscape (including:
- closest prior art patents for “buprenorphine in situ implant”,
- competitors’ overlapping formulations,
- freedom-to-operate map by assignee and expiry bands,
- continuation/divisional webs,
- terminal disclaimers, and
- patent term adjustments affecting US exclusivity)
cannot be produced from the input.
Risk concentration: which design-around attempts are most likely to matter under these claims
Based on the claim language alone, the most salient infringement-risk axes are:
-
NMP inclusion
- Required in claim 1 and essentially fixed in claims 9 and 21 as the principal organic liquid.
- Claim 24 allows co-solvents but still requires NMP.
- Removing NMP or using a different principal organic liquid is the fastest theoretical route to avoiding these claims. The practical viability depends on whether alternative solvents are already covered by other patents in the family or by later publications, which is not provided here.
-
PLGA grade constraints
- Claims 10/11/12 add specificity (carboxy terminal group; MW 5,000–20,000; and 50/50 ratio).
- A competitor could remain within the broad buprenorphine/NMP/PLGA structure while selecting different PLGA grade boundaries to avoid the narrow-dependent claims.
- However, claim 1 does not require PLGA MW or terminal group, so grade changes do not remove risk against claim 1 if NMP and broad wt% ranges are still met.
-
Buprenorphine wt% and free-base requirement
- Claim 1 allows salts or free base, but later claims focus on free base (claim 7 and claims 9/14/16/21+).
- A competitor could target salt-only formulations to reduce exposure to free-base dependent claims, but claim 1 still covers salts.
-
In situ transformation limitation
- For claims that explicitly require conversion to implant in situ, a competitor could aim for a formulation that remains a solution/flowable depot substitute rather than the claimed implant formation behavior.
- Claim 1 does not include that transformation limitation in the text provided, so transformation-based arguments likely reduce only the narrower dependent claims (13, 22, 25, 28), not the outermost coverage.
Key Takeaways
- US 10,558,394 is anchored on an injectable buprenorphine/PLGA/NMP formulation that forms an in situ implant upon contact with aqueous media in multiple dependent claims.
- Outer claim coverage (Claim 1) is defined by broad wt% ranges for buprenorphine (10–50%) and PLGA (5–70%) with NMP present as the third component; it does not require PLGA MW or terminal group.
- Narrow claim fences include:
- fixed wt% center (~18% buprenorphine free base / ~32% PLGA / ~50% NMP) in claim 9,
- PLGA grade constraints (carboxy terminal group and MW 5,000–20,000; plus 50/50 ratio) in claims 10–12,
- in situ transformation in claims 13, 22, 25, 28,
- and device/delivery forms (syringe/container).
- A complete US patent landscape cannot be determined from the provided input because no citations, family data, or related-patent references were supplied.
FAQs
1) Does US 10,558,394 protect buprenorphine salts or only free base?
Claim 1 covers buprenorphine as free base or pharmaceutically acceptable salt. Multiple narrower claims focus specifically on buprenorphine free base (e.g., claim 7 and the claim 9/14/16/21 series).
2) Is N-methyl-2-pyrrolidone required in all claims?
NMP is a required component in the claim set as presented:
- claim 1 requires NMP as the third component,
- claim 9 sets NMP at ~50 wt%,
- claim 21 defines NMP at ~30–70 wt%,
- claim 24 requires an organic liquid that includes NMP plus optional specified cosolvents.
3) What PLGA compositions are explicitly allowed?
Claim 5 lists PLGA copolymer ratios: 50/50, 55/45, 60/40, 65/35, 70/30, 75/25, 80/20, 85/15, 90/10, 95/5. Claim 6 specifically fixes PLGA at 50/50.
4) Which dependent claims impose molecular-weight and end-group requirements?
Claim 10 requires carboxy terminal group. Claim 11 requires PLGA MW 5,000–20,000 Da. Claim 12 requires 50/50 + carboxy terminal + 5,000–20,000 Da.
5) Does the patent cover syringes and containers?
Yes. Claim 19 covers a syringe comprising the formulation of claim 9, and claim 20 covers a container comprising the formulation of claim 9. Claim 28 adds an in situ transformation limitation tied to a container.
References
[1] US Patent 10,558,394. Claims provided in prompt (buprenorphine/PLGA/N-methyl-2-pyrrolidone injectable flowable composition; in situ implant conversion).
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