Details for Patent: 8,613,950

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Which drugs does patent 8,613,950 protect, and when does it expire?

Patent 8,613,950 protects STAXYN and is included in one NDA.

This patent has fifty-three patent family members in thirty-eight countries.

Summary for Patent: 8,613,950

Title:	Pharmaceutical forms with improved pharmacokinetic properties
Abstract:	The present application relates to novel drug formulations of vardenafil which dissolve rapidly in the mouth and lead to increased bioavailability and to a plateau-like plasma concentration profile, and to processes for their preparation.
Inventor(s):	Peter Serno, Roland Heinig, Kerstin Pauli, Yutaka Hayauchi
Assignee:	Bayer Intellectual Property GmbH
Application Number:	US11/885,019
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,613,950
Patent Claim Types: see list of patent claims	Formulation; Compound; Device; Dosage form;

United States Patent 8,613,950: Vardenafil Orally Disintegrating Tablet Claims and Patent Landscape

U.S. Patent No. 8,613,950 protects specific orally disintegrating vardenafil hydrochloride trihydrate tablets, particularly uncoated tablets using sorbitol, mannitol, or both. The broadest independent claims require a rapidly disintegrating tablet that releases vardenafil in the mouth without swallowing, combined with defined dissolution or formulation characteristics. The patent does not broadly cover all vardenafil products, conventional swallowed tablets, or every orally disintegrating formulation.

The commercial product most closely associated with this technology is Bayer's Staxyn, an orally disintegrating vardenafil hydrochloride tablet. Staxyn is a small-molecule product regulated through an NDA, so generic competition would proceed through an ANDA and Paragraph IV certification rather than a biosimilar application.

What does U.S. Patent 8,613,950 protect?

The patent protects a dosage form, not vardenafil as a molecule. Its central subject matter is an uncoated, mouth-disintegrating tablet containing vardenafil hydrochloride trihydrate and sugar alcohol excipients.

The principal technical limitations are:

Limitation	Claims containing the limitation
Vardenafil hydrochloride trihydrate	1-18
Uncoated tablet	1, 8, 17
Rapid disintegration in the mouth	1, 8, 17
Release in the mouth without swallowing the tablet	1, 8, 17
At least one sugar alcohol	1-7
At least two sugar alcohols	8-18
Sorbitol and/or mannitol	4-6, 9-11, 17-18
At least 80% dissolution in 10 mL saline at 25°C	1, 13, 15
At least 70% release within five minutes in specified USP test	1, 14-15
Micronized drug with mean particle size below 20 micrometers	2, 17
Sugar alcohol content of 40%-99%	3, 16-17
Vardenafil content of 0.8%-25%, calculated as free base	7, 12, 17

The claims combine structural limitations, compositional ranges, particle-size requirements, and performance testing. A competing product may avoid infringement by omitting one required limitation, but the practical analysis depends on the exact formulation and testing results.

How are the independent claims structured?

Claim 1: broad single-sugar-alcohol formulation

Claim 1 is the broadest independent claim directed to a formulation containing at least one sugar alcohol. It requires:

1. An uncoated tablet.
2. Rapid disintegration in the mouth.
3. Release of vardenafil in the mouth without swallowing the tablet.
4. Vardenafil hydrochloride trihydrate.
5. At least one sugar alcohol.
6. At least 80% dissolution in 10 mL of physiological saline at 25°C.
7. At least 70% release within five minutes under the specified USP paddle test.

Claim 1 does not require mannitol, sorbitol, micronized vardenafil, or a particular sugar-alcohol concentration. Those limitations appear in dependent claims.

The performance requirements are material. A tablet containing the correct ingredients could fall outside claim 1 if it does not meet either the saline dissolution requirement or the five-minute release requirement.

Claim 8: two-sugar-alcohol formulation

Claim 8 is an independent composition claim requiring an uncoated orally disintegrating tablet containing vardenafil hydrochloride trihydrate and at least two sugar alcohols.

Unlike claim 1, claim 8 does not itself require the 80% dissolution or 70% five-minute release thresholds. Those limitations are added by claims 13-15. Claim 8 is therefore potentially broader than claim 1 in relation to performance testing, although it is narrower in requiring at least two sugar alcohols.

Claim 9 specifically identifies a sorbitol-mannitol mixture. Claims 10 and 11 cover formulations containing mannitol or sorbitol as at least one of the sugar alcohols.

Claim 17: narrow combination claim

Claim 17 requires all of the following:

• An uncoated orally disintegrating tablet.
• Vardenafil hydrochloride trihydrate.
• Sorbitol.
• Mannitol.
• Micronized vardenafil with a mean particle size below 20 micrometers.
• Vardenafil content of 0.8%-25%, calculated as free base.
• Combined sorbitol and mannitol content of 40%-99%.

This is the most formulation-specific independent claim. It does not expressly include the 80% dissolution or 70% release limitations, but it imposes several compositional and particle-size restrictions that may be important in evaluating design-around strategies.

What formulations are protected by the patent?

The patent's strongest protection is directed to sugar-alcohol-based orally disintegrating tablets. Mannitol and sorbitol are central because they can provide bulk, mouthfeel, rapid dissolution, and tablet formation characteristics.

Mannitol-only formulations

A mannitol formulation can fall within claims 4 and 5, provided it satisfies the applicable parent-claim limitations. If it contains only one sugar alcohol, it generally would not fall within claim 8, which requires at least two sugar alcohols, unless another excipient qualifies as a sugar alcohol under the claim construction.

Sorbitol-only formulations

A sorbitol formulation can fall within claims 4 and 6, subject to the requirements inherited from claim 1. It would not ordinarily satisfy claim 17 because claim 17 requires both sorbitol and mannitol.

Sorbitol-mannitol formulations

A formulation containing both excipients is the clearest target of claims 9 and 17. Claim 17 adds the most specific limitations and may correspond closely to the commercial formulation profile associated with vardenafil orally disintegrating tablets.

Other sugar alcohols

Claim 1 is not limited to mannitol or sorbitol. Other sugar alcohols could fall within the claim if the formulation satisfies the remaining limitations. Claims 4-6 narrow the scope to sorbitol, mannitol, or both.

A formulation using a non-sugar-alcohol filler may avoid the literal scope of the sugar-alcohol limitations, but the complete formulation would still require analysis under the doctrine of equivalents.

How important are the dissolution and release limitations?

The patent uses two distinct performance tests.

Test	Requirement
Small-volume dissolution	At least 80% of vardenafil hydrochloride trihydrate dissolves at 25°C in 10 mL physiological saline
USP release test	At least 70% releases within five minutes in 900 mL physiological saline, 50 rpm, 37°C, USP paddle apparatus

The first test addresses dissolution in a small volume approximating the fluid available in the mouth. The second uses a conventional laboratory release apparatus and measures rapid release under standardized conditions.

For claims 1 and 13-15, the results are claim limitations. An accused product should be tested using the stated conditions, including:

• Physiological saline concentration.
• Temperature.
• Sample volume.
• Paddle apparatus.
• Rotation speed.
• Five-minute measurement point.
• Calculation method for released vardenafil.

The wording creates potential claim-construction issues. “Dissolves” and “releases” are not necessarily identical measurements. A formulation may release drug from the tablet without achieving the claimed dissolved fraction in the small-volume saline test.

Does micronized vardenafil matter?

Yes. Claim 2 requires micronized vardenafil hydrochloride trihydrate with a mean particle size below 20 micrometers. Claim 17 incorporates the same particle-size limitation.

Particle-size testing may raise practical issues because the result depends on:

• The measurement technique.
• The particle-size distribution rather than a single maximum size.
• Whether agglomerates are dispersed before testing.
• The definition of “mean particle size.”
• Whether the measurement is based on volume, number, or another distribution basis.

A formulation with larger particles could avoid claims 2 and 17 while remaining exposed to claims that do not require micronization.

How many patents cover the Staxyn-type product?

The relevant protection should be separated into four categories:

1. Active-ingredient patents. These cover vardenafil or its chemical class and are distinct from the orally disintegrating formulation claims.
2. Formulation patents. U.S. Patent 8,613,950 is directed to the orally disintegrating vardenafil tablet technology.
3. Method-of-use patents. These may cover treatment of erectile dysfunction or other therapeutic uses, depending on the patent family and listed indications.
4. Regulatory exclusivity. FDA exclusivity is separate from patent protection and does not arise from the claims of U.S. Patent 8,613,950.

The patent at issue is a formulation patent. It does not claim the therapeutic use of vardenafil in generic terms, nor does it claim all dosage forms containing vardenafil.

What is the Orange Book status of U.S. Patent 8,613,950?

U.S. Patent 8,613,950 has been associated with the Staxyn NDA, an orally disintegrating vardenafil product. Orange Book listing status must be evaluated against the current FDA Orange Book entry because a patent can be delisted, expire, or remain listed after commercial discontinuation subject to FDA rules.[2]

For an ANDA applicant, the relevant certifications are:

Certification	Meaning
Paragraph I	No patent information is listed
Paragraph II	Listed patent has expired
Paragraph III	Applicant will wait until patent expiration
Paragraph IV	Patent is invalid, unenforceable, or will not be infringed

A Paragraph IV certification could trigger notice and patent litigation under the Hatch-Waxman Act. A successful patent challenge could permit earlier generic launch than a Paragraph III certification.

FDA approval of an ANDA does not itself resolve whether the generic infringes. Patent litigation and regulatory approval operate through separate processes.

When does U.S. Patent 8,613,950 lose exclusivity?

A U.S. utility patent generally expires 20 years from the earliest effective nonprovisional filing date, subject to patent-term adjustment, patent-term extension, terminal disclaimers, and other statutory adjustments.[3] The issue date, December 24, 2013, is not the expiration date.

Public drug-patent listings have associated the patent with a 2027 expiration period. The legally operative date should be taken from the current USPTO patent record and the FDA Orange Book entry, including any patent-term adjustment or extension. Patent protection can also end earlier through invalidation, unenforceability, disclaimer, or a court judgment.

Any pediatric exclusivity or regulatory exclusivity would be separate from the patent term. Small-molecule vardenafil is not subject to biosimilar exclusivity under the Public Health Service Act.

What generic entry risks exist?

Formulation risk

A generic applicant seeking an orally disintegrating vardenafil product would need to assess whether its formulation includes:

• Vardenafil hydrochloride trihydrate.
• Mannitol, sorbitol, or another sugar alcohol.
• An uncoated tablet.
• Release in the mouth without swallowing.
• The claimed dissolution and release profile.
• Micronized vardenafil below 20 micrometers.
• The claimed concentration ranges.

A conventional film-coated or swallowed vardenafil tablet would present a different infringement profile because the claims require oral disintegration and mouth release.

Design-around options

Potential design-around variables include:

• Using a different salt or solid form of vardenafil.
• Using a non-sugar-alcohol excipient system.
• Using a coated or non-disintegrating dosage form.
• Altering the particle-size distribution.
• Using different drug loading.
• Developing a formulation that does not meet the claimed performance thresholds.

Each design-around must be assessed against all claims and the doctrine of equivalents. Changing one excipient may not avoid infringement if the resulting product still satisfies another independent claim.

Launch scenarios

Scenario	Commercial consequence
Paragraph III certification	Launch generally delayed until the relevant patent expires
Paragraph IV certification with no suit	Possible approval after statutory notice and regulatory review
Paragraph IV certification followed by timely suit	FDA approval may be stayed for up to 30 months, subject to statutory exceptions
Patent invalidated or found not infringed	Earlier launch becomes possible
Settlement agreement	Launch date depends on the negotiated terms
Non-infringing formulation	Possible launch without successfully challenging the patent

Which companies are challenging the patent?

The claim set alone does not identify an ANDA filer, Paragraph IV challenger, litigation defendant, or settlement participant. Patent ownership and commercial rights also should not be inferred solely from the marketed product name.

The relevant parties are likely to include:

• The patent owner or successor owner.
• The NDA holder for Staxyn.
• Any ANDA applicant developing vardenafil orally disintegrating tablets.
• Generic manufacturers with approved or pending vardenafil products.
• Contract manufacturers controlling particle-size reduction, blending, compression, or tablet manufacture.

No biosimilar challenger is relevant because vardenafil is a synthetic small molecule rather than a biologic.

What manufacturing and intellectual-property barriers remain?

The patent's manufacturing significance lies in the interaction between particle size, excipient selection, tablet strength, disintegration, taste, and release. A manufacturer must control:

• Micronization of vardenafil hydrochloride trihydrate.
• Uniform distribution of low-dose active ingredient.
• Sorbitol and mannitol ratios.
• Compression force.
• Tablet friability.
• Moisture exposure.
• Mouthfeel and palatability.
• Dissolution and release performance.

The formulation claims do not necessarily block every manufacturing process. They can, however, create risk where the manufacturing process predictably produces the claimed composition and performance profile.

How strong is the patent estate?

U.S. Patent 8,613,950 has meaningful but bounded scope.

Its strengths are:

• Multiple independent claims.
• Coverage of both single- and multiple-sugar-alcohol formulations.
• Specific protection for sorbitol-mannitol combinations.
• Particle-size protection in claims 2 and 17.
• Quantitative dissolution and release limitations.
• Coverage of an orally disintegrating dosage form associated with Staxyn.

Its limitations are:

• No broad claim to vardenafil itself.
• No coverage of conventional swallowed tablets.
• No universal coverage of all vardenafil salts or solid forms.
• Dependence in several claims on technically specific testing.
• Potential design-around opportunities involving excipients, coating, particle size, salt form, and dosage-form architecture.

The estate is strongest against a close copy of a Staxyn-type uncoated orally disintegrating tablet and weaker against conventional tablets, alternative solid forms, and formulations that avoid the sugar-alcohol or performance requirements.

Key Takeaways

• U.S. Patent 8,613,950 is a formulation patent for orally disintegrating vardenafil hydrochloride trihydrate tablets.
• Claims 1, 8, and 17 are the principal independent claims.
• Claim 1 focuses on a single-sugar-alcohol formulation with specified dissolution and release results.
• Claim 8 requires at least two sugar alcohols but does not independently require the performance thresholds.
• Claim 17 specifically targets micronized vardenafil with sorbitol and mannitol.
• The patent does not broadly cover all vardenafil products.
• Generic applicants would use the ANDA pathway and could file Paragraph II, III, or IV certifications.
• A 2027 expiration period has been associated with the patent, but the operative date depends on the current USPTO and Orange Book records.
• Biosimilar competition is irrelevant because vardenafil is a small-molecule drug.
• The principal design-around variables are salt form, excipient system, tablet coating, particle size, drug loading, and release performance.

FAQs

Is U.S. Patent 8,613,950 a patent on Staxyn?

It is a formulation patent associated with the orally disintegrating vardenafil product Staxyn. It is not a patent on every vardenafil product or on vardenafil as a chemical entity.

Does a vardenafil orally disintegrating tablet infringe automatically?

No. The product must satisfy every limitation of at least one asserted claim. The analysis may require testing for sugar-alcohol content, particle size, tablet coating, dissolution, release rate, and drug concentration.

Can a generic use mannitol without infringing?

Possibly, but not automatically. Mannitol appears in claims 4, 5, 10, 17, and 18. A mannitol formulation must be evaluated against the full combination of limitations in each claim.

Are vardenafil tablets eligible for a biosimilar application?

No. Vardenafil is a synthetic small molecule. A generic vardenafil product would ordinarily use the ANDA pathway under the Federal Food, Drug, and Cosmetic Act.

Does patent expiration eliminate all Staxyn market barriers?

No. Patent expiration removes that patent-based barrier, but other listed patents, regulatory exclusivity, manufacturing constraints, supply agreements, trademarks, and separate intellectual-property rights may affect market entry.

References

1. Bayer Intellectual Property GmbH. (2013). U.S. Patent No. 8,613,950, Drug formulation. United States Patent and Trademark Office.

2. 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/

3. United States Patent and Trademark Office. (n.d.). Patent term calculator. https://www.uspto.gov/patents/laws/patent-term-calculator

4. U.S. Food and Drug Administration. (2017). Approved drug products with therapeutic equivalence evaluations. U.S. Department of Health and Human Services.

5. Federal Food, Drug, and Cosmetic Act, 21 U.S.C. § 355(j).

Drugs Protected by US Patent 8,613,950

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Bayer Hlthcare	STAXYN	vardenafil hydrochloride	TABLET, ORALLY DISINTEGRATING;ORAL	200179-001	Jun 17, 2010		DISCN	Yes	No			Y

Foreign Priority and PCT Information for Patent: 8,613,950

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Germany	10 2005 009 240	Mar 1, 2005

PCT Information
PCT Filed	February 16, 2006	PCT Application Number:	PCT/EP2006/001393
PCT Publication Date:	September 08, 2006	PCT Publication Number:	WO2006/092207

International Family Members for US Patent 8,613,950

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	053552
Argentina	111572
Austria	E552828
Australia	2006220100