Details for Patent: 8,945,620

Which drugs does patent 8,945,620 protect, and when does it expire?

Patent 8,945,620 protects LYRICA CR and is included in one NDA.

Protection for LYRICA CR has been extended six months for pediatric studies, as indicated by the *PED designation in the table below.

This patent has thirty-seven patent family members in thirty-three countries.

Summary for Patent: 8,945,620

Title:	Solid pharmaceutical compositions containing pregabalin
Abstract:	A solid pharmaceutical composition containing pregabalin is described. The composition includes a matrix forming agent and a swelling agent and is suitable for once daily oral administration. Exemplary matrix forming agents include mixtures of polyvinyl acetate and polyvinylpyrrolidone, and exemplary swelling agents include cross-linked polymers of polyvinylpyrrolidone.
Inventor(s):	Howard N. Bockbrader, Yun Hyung Cho, Steven Diaz Santiago, Majid Mahjour, Thomas Daniel Reynolds, Pushpa Ganapathi Shao, Zezhi Jesse Shao, Jiansheng Wan
Assignee:	Viatris Specialty LLC
Application Number:	US14/181,785
Patent Claim Types: see list of patent claims	Use; Composition; Formulation; Delivery;

US Patent 8,945,620: Pregabalin Extended-Release Formulation, Claim Scope, Expiration and Patent Landscape

US Patent 8,945,620 protects a once-daily oral pregabalin formulation using a specific hydrophilic matrix system. The core technology combines polyvinyl acetate and polyvinylpyrrolidone as the matrix-forming agent with cross-linked polyvinylpyrrolidone and polyethylene oxide as swelling agents. The claims also cover defined ingredient ranges, 12-to-20-hour release, pharmacokinetic targets, bioequivalence to an immediate-release pregabalin product, and methods of treating pregabalin-responsive disorders.

The patent is materially narrower than a broad claim to "extended-release pregabalin." A potentially infringing product must generally practice the required excipient architecture, quantitative ranges, and once-daily dosage limitations. The principal freedom-to-operate risk is therefore formulation-specific rather than based solely on the use of pregabalin in an extended-release tablet.

What does US Patent 8,945,620 protect?

The patent has two independent formulation claim groups and two independent method-of-treatment claim groups.

Claim group	Independent claim	Protected subject matter
Composition	1	Pregabalin composition with a PVA/PVP matrix and crospovidone/PEO swelling system
Treatment method	8	Once-daily oral administration of the claim 1 composition
Formulation	10	More narrowly specified formulation with separate quantitative ranges for matrix, crospovidone and PEO
Treatment method	13	Once-daily administration of the claim 10 formulation

The claim language uses "comprising." That term generally permits the presence of additional excipients, coatings, processing aids, lubricants, glidants and other ingredients, provided the accused product contains all required elements.

The active ingredient is pregabalin or a pharmaceutically acceptable complex, salt, solvate or hydrate. The claims are directed to the pharmaceutical formulation and its release behavior, not to a new chemical form of pregabalin.

What are the essential elements of claim 1?

Claim 1 requires all of the following:

1. A pharmaceutical composition.
2. Pregabalin, or a specified pharmaceutically acceptable derivative.
3. A matrix-forming agent comprising:
   • polyvinyl acetate; and
   • polyvinylpyrrolidone.
4. A swelling agent comprising:
   • cross-linked polyvinylpyrrolidone; and
   • polyethylene oxide.
5. Adaptation for once-daily oral dosing.
6. Pregabalin at approximately 5% to 60% by weight.
7. Matrix-forming agent at approximately 5% to 45% by weight.
8. Swelling agent at approximately 15% to 70% by weight.

The claim does not require a particular tablet strength, tablet shape, coating, manufacturing process, dissolution apparatus or commercial brand. It does require the claimed excipient classes and the stated quantitative architecture.

How do the matrix and swelling agents function?

The PVA/PVP combination provides a water-insoluble or slowly eroding matrix structure. Polyethylene oxide hydrates and expands when exposed to gastrointestinal fluid. Cross-linked polyvinylpyrrolidone contributes swelling and disintegration-related behavior, although its role in this formulation is different from conventional use as a rapid disintegrant.

The claim is directed to the combination rather than to any one excipient in isolation. A formulation containing PEO but no cross-linked PVP would not literally satisfy the complete swelling-agent limitation. A formulation using PVA but no PVP would likewise face a limitation failure under the matrix requirement.

How narrow are the quantitative limitations?

The quantitative limitations create multiple potential design-around routes, although the open "comprising" language limits the protection provided by simple excipient additions.

Limitation	Claim 1	Narrower dependent or independent limitation
Pregabalin	5%-60%	Same general range in claim 10
Matrix-forming agent	5%-45%	20%-35% in claim 5 and claim 10
Swelling agent	15%-70%	20%-55% in claim 5
PVA within PVA/PVP matrix	Not specified in claim 1	60%-90% in claim 6; 70%-90% in claims 7 and 10
Cross-linked PVP	Not separately specified in claim 1	10%-35% in claim 10; 20%-30% in claim 11
PEO	Not separately specified in claim 1	5%-35% in claim 10; 10%-25% in claim 12

Claim 10 is particularly important because it separates the swelling system into independent ranges:

• Cross-linked PVP: 10%-35%.
• PEO: 5%-35%.
• Matrix: 20%-35%.
• PVA as a percentage of the PVA/PVP matrix: 70%-90%.

A competing formulation could avoid literal infringement by omitting one required component or placing the component outside a claimed range. The commercial significance of that strategy depends on whether the alternative remains therapeutically and regulatorily acceptable.

What do claims 2 through 7 add?

Release duration

Claim 2 requires release of the active ingredient over approximately 12 to 20 hours. This limitation links the excipient composition to a sustained-release performance profile. It may create factual disputes over:

• The dissolution method.
• The dissolution medium.
• Sampling intervals.
• Whether "release over" means substantially complete release or measurable release.
• Whether the range is assessed in vitro or in vivo.

The claim does not state a single dissolution specification. That omission can increase litigation risk because the parties may dispute the proper test for determining whether a formulation releases pregabalin over the claimed period.

Pharmacokinetic limitations

Claim 3 requires one or both of the following steady-state targets:

• Cmax of approximately 9 micrograms per milliliter or less.
• Cmin of approximately 0.7 micrograms per milliliter or greater.

The combined limitation requires both thresholds. These limitations are technically significant because they distinguish a formulation by exposure profile rather than only by tablet composition.

A product may practice claim 1 but fall outside claim 3 if its steady-state Cmax exceeds 9 micrograms per milliliter or its Cmin falls below 0.7 micrograms per milliliter. Conversely, a product that meets the pharmacokinetic profile but lacks the claimed PVA/PVP and cross-linked PVP/PEO system would not necessarily infringe.

Bioequivalence limitation

Claim 4 requires bioequivalence to an immediate-release formulation containing pregabalin, lactose monohydrate, maize starch and talc. This limitation introduces a regulatory and evidentiary issue. Bioequivalence is normally established against a specified reference product under an FDA-approved protocol. The claim language may require analysis of whether the comparison formulation is defined by its ingredients, a specific product, or an approved immediate-release reference.

Dependent composition ranges

Claims 5 through 7 narrow the matrix and PVA/PVP ratios. These claims are useful against products that use the same formulation concept but adjust the total matrix loading or polymer ratio.

Claims 6 and 7 overlap, with claim 7 being narrower because the PVA content is approximately 70%-90% rather than 60%-90%. Claim 7 also depends on claim 1, so it carries all claim 1 limitations in addition to the narrower PVA ratio.

What does independent claim 10 protect?

Claim 10 is an independent formulation claim and may be the most commercially important claim in the patent. It requires:

• Pregabalin at 5%-60% by weight.
• A PVA/PVP matrix at 20%-35% by weight.
• PVA at 70%-90% of the combined PVA/PVP matrix.
• Cross-linked PVP at 10%-35%.
• PEO at 5%-35%.
• Suitability for once-daily administration.

Unlike claim 1, claim 10 expressly allocates ranges to cross-linked PVP and PEO. A product can therefore fall within claim 10 even if a dispute exists over the broader "swelling agent" terminology in claim 1.

The claim uses "polyvinylpyrrolidone" for the matrix and "cross-linked polyvinylpyrrolidone" for the swelling component. Those materials are chemically related but functionally distinct. A formulation record should identify the grade, cross-linking status, molecular weight, particle size and supplier designation for each polymer.

What are the method-of-use claims?

Claims 8 and 13 cover once-daily oral treatment using the claimed formulations. Claim 9 and claim 14 list conditions including:

• Epilepsy.
• Pain.
• Diabetic peripheral neuropathy.
• Postherpetic neuralgia.
• Fibromyalgia.
• Anxiety and depression.
• Bipolar disorder and mania.
• Insomnia.
• Alcoholism.
• Inflammation and gastrointestinal damage.

The method claims are formulation-dependent. Administration of ordinary immediate-release pregabalin does not practice these claims. A treatment protocol using a different extended-release formulation also may avoid infringement if the formulation does not meet the incorporated composition limitations.

The method claims create a potential induced-infringement issue where a generic label instructs once-daily use of a formulation that meets the composition limitations. A label that omits the patented use may reduce, but does not automatically eliminate, risk if the formulation itself falls within an asserted composition claim.

When does US Patent 8,945,620 lose exclusivity?

The patent issued on February 3, 2015. Its term is governed by the 20-year patent-term rule measured from the applicable earliest nonprovisional or international filing date, subject to patent-term adjustment and any applicable extensions under the Hatch-Waxman framework.[1]

Public patent records commonly associate the patent family with an October 2007 international or nonprovisional filing timeline, implying a base expiration in approximately October 2027 before any adjustment. The controlling date is the USPTO term calculation, not the patent's issue date or the priority date alone.

Event	Date or status
Earliest reported priority period	October 2006
Relevant international/nonprovisional filing period	October 2007
US patent issued	February 3, 2015
Base 20-year term	Approximately October 2027
Controlling expiration	USPTO term calculation, including PTA/PTE

Patent expiry does not itself guarantee generic launch. FDA exclusivity, other listed patents, pediatric exclusivity, litigation settlements, regulatory review and product availability can affect the actual entry date.

What is the Orange Book status of pregabalin extended release?

FDA approved Lyrica CR, an extended-release pregabalin product, in 2017 under NDA 210764. The product was indicated for once-daily treatment of neuropathic pain associated with diabetic peripheral neuropathy and postherpetic neuralgia.[2]

The Orange Book is the controlling source for current listed patents, regulatory exclusivity and any approved tentative or final generic applications.[3] A patent analysis should distinguish between:

• Patents listed for Lyrica CR.
• Patents listed for immediate-release Lyrica.
• Unlisted formulation or process patents.
• Expired chemical-compound patents.
• FDA exclusivity periods separate from patent rights.

US 8,945,620 is directed to the extended-release pregabalin formulation technology rather than the basic pregabalin molecule. The core pregabalin compound patents do not provide the same commercial barrier because the principal chemical exclusivity period has expired or ended, subject to historical extensions and specific indication rights.

Which companies are challenging pregabalin extended-release patents?

Generic pregabalin competition has primarily targeted immediate-release pregabalin and, separately, extended-release products. Paragraph IV risk must be evaluated from current FDA ANDA records and Orange Book certifications rather than from the existence of a patent alone.

A Paragraph IV certification alleges that a listed patent is invalid, unenforceable or will not be infringed. If the patent owner brings suit within the statutory period, the FDA approval of the ANDA may be subject to a 30-month stay under the Hatch-Waxman Act, subject to statutory exceptions.[4]

For US 8,945,620, the commercially relevant questions are:

1. Whether the patent was listed against the relevant extended-release NDA.
2. Whether an ANDA applicant certified Paragraph IV.
3. Whether the patent owner filed an infringement action.
4. Whether the parties entered a settlement agreement.
5. Whether the FDA approved a generic before patent expiration.
6. Whether the proposed generic uses the same polymer architecture.

The supplied claim text does not establish the identity of any current Paragraph IV challenger, the existence of a settlement, or the present litigation posture. Those matters require a current FDA and court-docket review.

What patent landscape surrounds pregabalin?

Compound and immediate-release patents

Pregabalin's original compound protection and immediate-release product patents historically covered the active molecule, pharmaceutical salts, therapeutic uses and conventional formulations. Those rights are materially different from US 8,945,620 because they do not require the PVA/PVP and cross-linked PVP/PEO matrix.

Extended-release formulation patents

The relevant extended-release landscape includes claims directed to:

• Hydrophilic matrix tablets.
• Polymer-controlled release.
• Once-daily pregabalin dosing.
• Dissolution profiles.
• Cmax and Cmin targets.
• Bioequivalence to immediate-release pregabalin.
• Manufacturing processes and granulation.
• Tablet coating and dose uniformity.

A generic developer may therefore face overlapping patent families even after designing around US 8,945,620.

Manufacturing and process barriers

The patent's strongest practical barrier may be process control rather than the presence of a single excipient. Critical manufacturing variables include:

• Polymer grade and viscosity.
• Distribution of PEO and cross-linked PVP.
• Granulation moisture.
• Compression force.
• Tablet porosity.
• Drug loading.
• Coating weight.
• Dissolution reproducibility across strengths.

A formulation can avoid a literal composition range yet produce a similar release profile. That creates potential doctrine-of-equivalents exposure, although prosecution history, numerical-range case law and the importance of the selected excipient combination would control the analysis.

How strong is the patent estate?

US 8,945,620 has moderate formulation claim strength and narrower blocking power than a broad extended-release pregabalin patent.

Strength factor	Assessment
Active ingredient	Weak as a standalone barrier because pregabalin is established
Excipient combination	Stronger; requires a defined four-component polymer system
Quantitative ranges	Useful for enforcement but provide design-around opportunities
Once-daily limitation	Commercially relevant and likely tied to product labeling
PK limitations	Potentially powerful but expensive to prove
Bioequivalence limitation	Creates technical and regulatory complexity
Method claims	Useful where the label directs once-daily use
Manufacturing protection	Limited from the supplied claims
Geographic coverage	US only; foreign family rights must be assessed separately

The patent is strongest against a product that duplicates the commercial formulation, uses the same polymer grades, adopts the same once-daily label and produces the claimed exposure profile. It is weaker against a formulation using a different release mechanism, such as multiparticulates, osmotic delivery, lipid-based release, ion-exchange technology or a different polymer matrix.

What generic launch scenarios exist?

Launch after patent expiry

This is the lowest litigation-risk scenario if no unexpired continuation, reissue, related formulation patent or regulatory exclusivity remains.

Paragraph IV launch

An ANDA applicant may challenge validity, enforceability or infringement before expiry. The main technical defenses would include:

• No cross-linked PVP.
• No PVA/PVP matrix.
• Component outside the claimed range.
• No once-daily suitability.
• Failure to meet the release or PK limitation.
• Lack of infringement under the proper construction of "swelling agent" or "matrix forming agent."

Formulation design-around

A company could use a different controlled-release platform. The commercial tradeoff is that FDA approval still requires demonstration of safety, efficacy, quality and bioequivalence or another appropriate bridge to the reference product.

505(b)(2) strategy

A 505(b)(2) applicant could pursue a modified dosage form with reliance in part on existing pregabalin data. Patent certifications and any listed patents would remain relevant. A 505(b)(2) pathway does not eliminate formulation patent risk.

What geographic coverage does the patent provide?

US 8,945,620 provides rights only in the United States. International family members may cover corresponding formulations in Europe, Canada, Australia, Japan or other jurisdictions, but claim scope, prosecution amendments, patent-term dates and litigation outcomes vary by country.

A global launch requires separate review of:

• PCT national-phase members.
• Granted foreign patents.
• Pending continuations and divisionals.
• Supplementary protection certificates.
• Opposition or revocation proceedings.
• Local claim construction and doctrine-of-equivalents standards.

A US non-infringement conclusion cannot be exported to other jurisdictions.

Key Takeaways

• US 8,945,620 is a formulation patent for once-daily extended-release pregabalin.
• Its central limitation is the combination of PVA/PVP matrix material with cross-linked PVP and PEO.
• Claims 1 and 10 require overlapping but distinct quantitative ranges.
• Claims 2 through 4 add release, pharmacokinetic and bioequivalence limitations.
• Claims 8, 9, 13 and 14 create formulation-dependent method-of-treatment exposure.
• The base patent term appears to run to approximately October 2027, subject to the USPTO's final PTA/PTE calculation.
• The principal design-around routes are omission of one required polymer, use of a different release technology, or placement outside the claimed ranges.
• Current Paragraph IV challengers, settlements, Orange Book listings and litigation status must be determined from live FDA and court records.
• The patent is a meaningful barrier to copycat polymer-matrix formulations but is not a broad monopoly over all extended-release pregabalin products.

FAQs

Does US 8,945,620 cover all once-daily pregabalin tablets?

No. The claims require a specified polymer system and quantitative formulation features. A once-daily pregabalin product using a different release mechanism may fall outside the claims.

Can a formulation avoid the patent by using polyvinylpyrrolidone without cross-linked polyvinylpyrrolidone?

Potentially. The claims distinguish matrix polyvinylpyrrolidone from cross-linked polyvinylpyrrolidone. The precise product composition and claim construction would determine infringement.

Are the Cmax and Cmin limitations required for every claim?

No. They are expressly included in dependent claims and certain method claims. Claims 1 and 10 do not, on the supplied text, require both pharmacokinetic thresholds.

Does approval of a generic pregabalin product prove non-infringement?

No. FDA approval addresses regulatory requirements. Patent infringement depends on the approved product's composition, label, release characteristics and applicable patent claims.

Can a foreign pregabalin product infringe US Patent 8,945,620?

No, not merely by being sold abroad. The patent's enforceable rights are territorial and generally concern making, using, selling, offering for sale or importing the claimed product in the United States.

References

1. United States Patent and Trademark Office. (n.d.). Patent term adjustment and patent term extension. https://www.uspto.gov
2. U.S. Food and Drug Administration. (2017). Lyrica CR prescribing information. Pfizer Inc.
3. U.S. Food and Drug Administration. (n.d.). Approved drug products with therapeutic equivalence evaluations: Orange Book. https://www.accessdata.fda.gov/scripts/cder/ob/
4. 35 U.S.C. § 271(e); 21 U.S.C. § 355(j).
5. United States Patent and Trademark Office. (2015). U.S. Patent No. 8,945,620, Pharmaceutical compositions of pregabalin.

Drugs Protected by US Patent 8,945,620

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Upjohn	LYRICA CR	pregabalin	TABLET, EXTENDED RELEASE;ORAL	209501-001	Oct 11, 2017	AB	RX	Yes	No					Y
Upjohn	LYRICA CR	pregabalin	TABLET, EXTENDED RELEASE;ORAL	209501-002	Oct 11, 2017	AB	RX	Yes	No					Y
Upjohn	LYRICA CR	pregabalin	TABLET, EXTENDED RELEASE;ORAL	209501-003	Oct 11, 2017	AB	RX	Yes	Yes					Y

International Family Members for US Patent 8,945,620

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	058175
Australia	2006310217
Brazil	PI0618211
Canada	2628200