Details for Patent: 10,098,882

Which drugs does patent 10,098,882 protect, and when does it expire?

Patent 10,098,882 protects RYKINDO and is included in one NDA.

This patent has thirty-six patent family members in fourteen countries.

Summary for Patent: 10,098,882

Title:	Risperidone sustained release microsphere composition
Abstract:	A risperidone sustained release microsphere formulation is provided. The microsphere formulation includes risperidone or 9-hydroxy risperidone or salts thereof, and a polymer blend having a first uncapped lactide-glycolide copolymer and a second uncapped lactide-glycolide copolymer, in which the first uncapped lactide-glycolide copolymer is a copolymer with a high intrinsic viscosity and the second uncapped lactide-glycolide copolymer is a copolymer with a low intrinsic viscosity. The sustained release micro sphere formulation according to an embodiment of the present disclosure is suitable for large-scale industrialized production with improved stability, the in vivo release behavior of which will not change after long-term storage.
Inventor(s):	Kaoxiang Sun, Rongcai Liang, Qilin Wang, Wenyan Wang, Wanhui Liu, Youxin Li
Assignee:	Luye Innomind Pharma Shijiazhuang Co Ltd
Application Number:	US15/347,365
Patent Claim Types: see list of patent claims	Use; Formulation;

US Patent 10,098,882: Risperidone Microsphere Claims, Patent Scope, and Competitive Landscape

US Patent 10,098,882 covers sustained-release risperidone microspheres made with a defined blend of two uncapped poly(lactide-co-glycolide), or PLGA, polymers. The patent’s principal limitation is the combination of polymer molecular weight or intrinsic viscosity, lactide-to-glycolide ratios, polymer-blend ratio, risperidone loading, and parenteral administration. The closest commercial technologies are long-acting injectable risperidone products, including Risperdal Consta, Perseris, Rykindo, and Uzedy, but product overlap depends on each product’s polymer composition, manufacturing process, formulation, and approved use.

What does US Patent 10,098,882 protect?

The patent protects four related subject-matter groups:

Claim group	Protected subject matter	Principal limitations
Claims 1-14	Risperidone-containing microspheres	Two uncapped PLGA polymers with specified composition and molecular-property ranges
Claim 15	Injectable pharmaceutical formulation	Formulation must contain the microspheres of claim 1
Claims 16-20	Treatment of psychosis	Parenteral administration, specified dose ranges, and risperidone treatment
Claims 21-22	Sustained-release treatment method	Microspheres with the defined PLGA blend that release active agent for up to 28 days

The patent is a formulation and method-of-use patent. It does not broadly claim all risperidone injections, all PLGA microspheres, or all long-acting antipsychotic formulations. Its enforceable scope turns on whether an accused product contains the claimed active component and the specified two-polymer PLGA system, or practices the claimed treatment method. [1]

How are the independent claims structured?

Claim 1: polymer-property formulation claim

Claim 1 requires:

1. Microspheres for sustained release.
2. An active component selected from:
   • risperidone;
   • 9-hydroxy risperidone;
   • a salt of risperidone; or
   • a salt of 9-hydroxy risperidone.
3. A polymer blend consisting essentially of:
   • a first uncapped PLGA; and
   • a second uncapped PLGA.
4. The first polymer must have:
   • intrinsic viscosity of 0.4-0.9 dl/g; and
   • lactide:glycolide ratio of 65:35 to 90:10.
5. The second polymer must have:
   • intrinsic viscosity of 0.1-0.35 dl/g; and
   • lactide:glycolide ratio of 50:50 to 75:25.

Claim 1 is comparatively broad within the patent family because it uses intrinsic viscosity rather than molecular weight as the principal polymer-size limitation. It does not require a specific polymer-blend ratio, drug-loading percentage, injection route, or 28-day release period.

The phrase “consisting essentially of” limits the polymer blend to the two identified uncapped PLGA components plus ingredients that do not materially alter the claimed characteristics. It is narrower than “comprising,” but it does not necessarily exclude every excipient or processing aid.

Claim 6: molecular-weight formulation claim

Claim 6 recites a similar microsphere composition but replaces intrinsic-viscosity limitations with molecular-weight ranges:

• First PLGA: 50,000-145,000 molecular weight and 65:35 to 90:10 lactide:glycolide.
• Second PLGA: 4,000-45,000 molecular weight and 50:50 to 75:25 lactide:glycolide.

Claims 1 and 6 are not identical substitutes. Intrinsic viscosity and molecular weight are related but are not interchangeable in every formulation or analytical context. A product could fall within one claim framework and outside the other, depending on the polymer grade, testing method, molecular-weight distribution, and specification.

Claim 12: narrow combination claim

Claim 12 is the most technically constrained composition claim. It requires all of the following:

• First uncapped PLGA:
  • molecular weight of 55,000-110,000;
  • intrinsic viscosity of 0.4-0.9 dl/g; and
  • lactide:glycolide ratio of 65:35 to 90:10.
• Second uncapped PLGA:
  • molecular weight of 15,000-35,000;
  • intrinsic viscosity of 0.1-0.35 dl/g; and
  • lactide:glycolide ratio of 50:50 to 75:25.
• First-to-second polymer weight ratio of 50:50 to 95:5.
• Lactide as the major monomer component of the polymer blend.

Claim 12 has substantial technical detail and may be harder to read on a commercial product unless the accused formulation’s polymer specifications fall within every stated range. It may have greater validity resilience than a broader claim because of its narrower combination, but that same narrowness can reduce infringement coverage.

What do the dependent claims add?

Claims 2-5, 7-11, and 13-14 narrow the composition claims in ways that create fallback positions.

Claim	Added limitation	Commercial significance
2	First PLGA at 75:25; second PLGA at 50:50	Targets a specific polymer-composition pairing
3	Polymer ratio of 50:50 to 95:5	Controls degradation and release profile
4	First polymer 50,000-145,000; second 4,000-45,000 molecular weight	Adds molecular-weight constraints to claim 1
5	Active agent at 10%-60% of microsphere weight	Covers drug loading
7	First polymer 55,000-110,000; second 15,000-35,000	Narrows claim 6 to preferred molecular-weight ranges
8	75:25 first polymer and 50:50 second polymer	Repeats the preferred monomer ratios
9	Polymer ratio of 50:50 to 95:5	Adds blend-ratio control
10	Intrinsic-viscosity ranges	Adds viscosity limitations to claim 6
11	Active agent at 10%-60%	Adds drug-loading limitation
13	Active agent at 10%-60%	Narrows claim 12
14	No active-agent crystals precipitated on microsphere surfaces	Targets surface morphology and release quality

Claim 14 is particularly relevant to product characterization. The limitation concerns the absence of drug crystals on the microsphere surface. In an infringement or freedom-to-operate analysis, microscopy, surface spectroscopy, manufacturing records, and batch-release data could become important evidence.

What is the scope of the method-of-treatment claims?

Claims 16-20

Claims 16-20 cover treatment of psychosis using the injectable formulation of claim 15. The method claims require parenteral administration and include:

• intramuscular injection;
• subcutaneous injection;
• intradermal injection; or
• intraperitoneal injection.

Claim 18 specifies 12.5-150 mg of risperidone per administration. Claims 19 and 20 specify dose ranges of:

• 0.2-2.5 mg/kg; and
• 0.4-1.7 mg/kg.

These claims are narrower than a composition claim because infringement requires practice of the claimed administration method and dose conditions. They may be relevant to an approved label, clinical protocol, or prescribing practice, but they are less useful against an injectable product that uses a different microsphere composition or has a different labeled indication.

Claims 21-22

Claim 21 is an independent treatment claim. It does not depend on claim 15 and separately recites:

• risperidone, 9-hydroxy risperidone, or a salt;
• two uncapped PLGA polymers;
• the specified intrinsic-viscosity ranges;
• the specified lactide:glycolide ranges; and
• sustained release for up to 28 days.

Claim 22 adds active loading of 10%-60%.

The “up to 28 days” limitation is important. It potentially covers products with release periods shorter than or equal to 28 days, including approximately two-week and four-week depot profiles, if the other limitations are met. It does not necessarily require exactly 28 days.

Which commercial risperidone products are most relevant?

Product	Sponsor or commercial company	Delivery profile	Technology relevance to US 10,098,882
Risperdal Consta	Janssen Pharmaceuticals	Intramuscular PLGA microspheres, generally every two weeks	Directly relevant technology class; infringement depends on the specific polymer blend and claim coverage
Perseris	Indivior	Subcutaneous monthly depot	Likely differentiated by its in situ depot technology rather than conventional PLGA microspheres
Rykindo	Luye Pharma	Long-acting injectable risperidone microspheres	Potentially the closest commercial comparator because it uses a microsphere depot platform
Uzedy	Teva Pharmaceuticals and MedinCell	Subcutaneous extended-release risperidone	Relevant to polymeric depot competition, but product-specific composition and process evidence are required
Oral risperidone generics	Multiple manufacturers	Oral tablets, solutions, and orally disintegrating forms	Outside the microsphere composition claims and generally outside the parenteral method claims

The presence of PLGA in a product is not sufficient to establish infringement. The analysis must identify whether the PLGA is uncapped, whether two distinct PLGA polymers are blended, and whether each polymer falls within the claimed composition, intrinsic-viscosity, molecular-weight, and ratio ranges.

How does this patent compare with Risperdal Consta?

Risperdal Consta is the most obvious technical comparator because it is an established risperidone microsphere product. Its formulation uses risperidone encapsulated in a biodegradable PLGA-based microsphere system. [2]

The key distinction is that US 10,098,882 does not claim a generic risperidone-in-PLGA microsphere. It claims a defined blend of two uncapped PLGAs with different polymer properties:

• a higher-viscosity or higher-molecular-weight, more lactide-rich polymer; and
• a lower-viscosity or lower-molecular-weight polymer with a broader glycolide content.

A legacy product could use PLGA yet fall outside the patent if it uses one polymer grade, a capped polymer, a different lactide:glycolide ratio, or values outside the claimed ranges.

How does this patent compare with Perseris?

Perseris uses a subcutaneous delivery system based on an in situ forming depot rather than a conventional preformed microsphere product. FDA labeling describes its delivery system and pharmacokinetic profile separately from the PLGA microsphere technology used in Risperdal Consta. [3]

Perseris is therefore a lower-probability literal match to claims 1, 6, and 12 if its commercial formulation does not contain the claimed two-polymer uncapped PLGA microsphere blend. Its label and formulation structure remain relevant to claims 16-20 only if the claimed microspheres and dose limitations are independently satisfied.

What patent landscape surrounds long-acting risperidone?

The relevant patent landscape has five technical categories.

Legacy PLGA microsphere patents

Earlier patents covering risperidone microspheres, biodegradable polymers, encapsulation methods, and release control created the platform for products such as Risperdal Consta. Many early composition and process patents have reached or approached expiration based on their priority dates and patent-term adjustments.

The existence of earlier PLGA patents creates potential prior-art issues for validity, particularly regarding:

• risperidone encapsulation in PLGA;
• two-polymer blends;
• lactide:glycolide variation;
• molecular-weight control; and
• sustained release over several weeks.

US 10,098,882 attempts to distinguish its claimed subject matter through the specific combination of polymer attributes and formulation performance.

Formulation and polymer-selection patents

These patents focus on polymer ratios, molecular weight, intrinsic viscosity, end-group chemistry, drug loading, particle size, porosity, and release kinetics. US 10,098,882 is strongest in this category.

Manufacturing-process patents

Separate rights may cover:

• solvent evaporation;
• emulsion formation;
• microsphere hardening;
• drying;
• particle-size classification;
• sterile manufacture;
• residual-solvent control; and
• reconstitution before injection.

A competing product can avoid literal infringement of the composition claims yet face process-patent exposure during manufacture.

Method-of-use patents

Claims 16-22 cover treatment of psychosis and specified administration and dosing conditions. Other patents may cover monthly dosing, two-week dosing, maintenance treatment, initiation regimens, or treatment of particular patient populations.

Device and administration patents

Syringes, reconstitution systems, delivery devices, suspension vehicles, and injection techniques may be protected separately from the microspheres themselves.

What is the Orange Book status of US Patent 10,098,882?

The Orange Book analysis must distinguish patent ownership from FDA listing. A patent is not automatically Orange Book-listed merely because it covers a drug formulation. FDA listing generally depends on whether the patent is submitted for an approved NDA and whether it claims the drug substance, drug product, or an approved method of use under the applicable FDA rules. [4]

For this patent, the relevant questions are:

1. Is US 10,098,882 listed against a specific risperidone NDA?
2. Is it listed as a drug-product patent or method-of-use patent?
3. Does the listed claim correspond to the approved formulation?
4. Is the patent listed against Risperdal Consta, Rykindo, Uzedy, Perseris, or another NDA?
5. Has the listing been delisted, corrected, or challenged?

The claims alone do not establish Orange Book listing. A current FDA Orange Book and NDA-specific patent record is required for a definitive listing determination. [4]

When does US Patent 10,098,882 lose exclusivity?

The patent’s exact expiration date cannot be derived from the claims. It depends on:

• the earliest effective nonprovisional priority date;
• any patent-term adjustment;
• any terminal disclaimer;
• patent-term extension;
• disclaimer or post-grant changes; and
• PTA calculation under 35 U.S.C. § 154.

The grant date does not determine expiration. The statutory baseline is generally 20 years from the earliest effective nonprovisional filing date, subject to those adjustments. [5]

A commercial exclusivity analysis must therefore separate:

Exclusivity type	Relevance
Patent term	Determines enforceable patent rights
FDA orphan exclusivity	Usually not central for standard risperidone products
New chemical entity exclusivity	Generally not applicable to risperidone as an established active ingredient
Three-year clinical-investigation exclusivity	May affect an NDA-specific approval or supplement
Five-year pediatric exclusivity	Can add six months to certain regulatory exclusivities
180-day generic exclusivity	Relevant only to an ANDA Paragraph IV challenger that qualifies

Which companies could challenge the patent?

Potential challengers would most likely be manufacturers developing:

• generic risperidone microspheres;
• an abbreviated new drug application for an equivalent long-acting injectable;
• a 505(b)(2) risperidone depot;
• a licensed microsphere platform; or
• a biosimilar-like follow-on product, although risperidone is a small molecule and does not use the biosimilar pathway.

A generic or 505(b)(2) applicant could challenge an Orange Book-listed patent through a Paragraph IV certification. The patent owner could then bring infringement litigation under the Hatch-Waxman framework, potentially triggering a statutory 30-month stay of approval depending on timing and statutory conditions. [6]

No specific Paragraph IV challenger, litigation docket, or settlement agreement is established by the claim text. Those issues require review of FDA filing records, district-court dockets, and public settlement disclosures.

What generic entry risks exist?

Composition-based entry

A competitor may seek to design around the patent by using:

• a single PLGA polymer;
• a capped PLGA;
• two polymers outside the claimed viscosity or molecular-weight ranges;
• a different lactide:glycolide profile;
• a polymer ratio below or above the claimed range; or
• a non-PLGA depot system.

Process-based entry

A competitor could use a different encapsulation process while still producing a composition that falls within claims 1, 6, or 12. Avoiding a manufacturing patent would not avoid composition-claim infringement.

Label-based entry

A skinny-label strategy could reduce exposure to method claims by omitting a patented indication, dose, or administration instruction. It would not avoid composition claims if the approved product itself falls within the claimed microsphere limitations.

Equivalents risk

Even where a parameter falls slightly outside a numerical range, the patent owner could assert infringement under the doctrine of equivalents. The strength of that theory would depend on prosecution history, claim amendments, prior art, and whether the accused value is materially different from the claimed range. [7]

How strong is the patent estate?

US 10,098,882 has a focused but technically meaningful claim set.

Strength factor	Assessment
Composition coverage	Strong within the defined two-uncapped-PLGA formulation
Breadth	Moderate; claims are narrower than generic PLGA microsphere claims
Manufacturing coverage	Limited in the supplied claims
Method-of-use coverage	Moderate but dependent on formulation and dose
Design-around risk	Meaningful
Product testing importance	High
Prior-art exposure	Potentially significant because risperidone PLGA microspheres were known before the patent
Commercial blocking value	Highest against products using the same polymer blend architecture

The strongest claims are likely claims 1 and 6 because they provide alternative intrinsic-viscosity and molecular-weight claim frameworks. Claim 12 is narrower but captures a preferred formulation architecture. Claims 21 and 22 extend the patent to treatment methods and a release period of up to 28 days.

Key Takeaways

• US 10,098,882 covers risperidone or related active components in microspheres made with two uncapped PLGAs.
• The first PLGA is higher molecular weight or intrinsic viscosity and more lactide-rich.
• The second PLGA is lower molecular weight or intrinsic viscosity and contains more glycolide.
• Claims 1, 6, and 12 are the primary formulation claims.
• Claims 15-22 cover injectable formulations and psychosis-treatment methods.
• The patent does not cover every long-acting risperidone product.
• Risperdal Consta is the closest legacy technology comparator.
• Perseris appears technically differentiated because it uses an in situ depot approach rather than a conventional preformed PLGA microsphere system.
• Rykindo and Uzedy require product-specific polymer and formulation analysis.
• Biosimilar litigation is not the relevant pathway because risperidone is a small-molecule drug.
• Paragraph IV exposure depends on Orange Book listing against a specific NDA.
• Exact patent expiration, Orange Book status, Paragraph IV activity, litigation, and settlements cannot be determined from the claims alone.

Frequently Asked Questions

Does US 10,098,882 cover all injectable risperidone products?

No. It requires a particular two-uncapped-PLGA microsphere composition or a method using that composition.

Can a product infringe if it uses PLGA but only one PLGA grade?

Possibly not under the supplied composition claims, because claims 1, 6, and 12 require a first and second PLGA with distinct claimed properties. Other patents could still apply.

Does the patent cover 14-day risperidone injections?

Potentially. Claim 21 covers sustained release for up to 28 days, but the product must also satisfy the active-agent and two-polymer limitations.

Is US 10,098,882 relevant to a 505(b)(2) risperidone depot?

Yes. A 505(b)(2) applicant would need to assess composition, method-of-use, Orange Book, and regulatory exclusivity issues, even if the product uses a different delivery route.

Does the absence of surface drug crystals create a separate product requirement?

Yes. Claim 14 adds a specific limitation requiring that no active-agent crystals precipitate on the microsphere surfaces.

References

1. United States Patent and Trademark Office. (2018). US Patent No. 10,098,882, claims 1-22.
2. U.S. Food and Drug Administration. (2024). Risperdal Consta: Prescribing information. Janssen Pharmaceuticals.
3. U.S. Food and Drug Administration. (2024). Perseris: Prescribing information. Indivior Inc.
4. U.S. Food and Drug Administration. (2024). Approved drug products with therapeutic equivalence evaluations: Orange Book.
5. United States Code. (2024). 35 U.S.C. § 154, contents and term of patent; § 156, extension of patent term.
6. United States Code. (2024). 21 U.S.C. § 355(j), abbreviated applications and patent certifications.
7. United States Code. (2024). 35 U.S.C. § 271, infringement of patent.

Drugs Protected by US Patent 10,098,882

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Shandong Luye	RYKINDO	risperidone	FOR SUSPENSION, EXTENDED RELEASE;INTRAMUSCULAR	212849-001	Jan 13, 2023		DISCN	Yes	No			Y			TREATMENT OF SCHIZOPHRENIA IN ADULTS
Shandong Luye	RYKINDO	risperidone	FOR SUSPENSION, EXTENDED RELEASE;INTRAMUSCULAR	212849-002	Jan 13, 2023		RX	Yes	Yes			Y			TREATMENT OF SCHIZOPHRENIA IN ADULTS
Shandong Luye	RYKINDO	risperidone	FOR SUSPENSION, EXTENDED RELEASE;INTRAMUSCULAR	212849-003	Jan 13, 2023		DISCN	Yes	No			Y			TREATMENT OF SCHIZOPHRENIA IN ADULTS

International Family Members for US Patent 10,098,882

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2012248038
Brazil	112013027235
Canada	2832663