Details for Patent: 8,071,130

Which drugs does patent 8,071,130 protect, and when does it expire?

Patent 8,071,130 protects DUETACT and is included in one NDA.

This patent has twenty-five patent family members in twenty-two countries.

Summary for Patent: 8,071,130

Title:	Solid preparation
Abstract:	The present invention intends to provide a solid preparation which contains an insulin sensitizer and an active ingredient other than an insulin sensitizer, and exhibits dissolution behavior of an insulin sensitizer similar to that of an insulin sensitizer from “a solid preparation containing only an insulin sensitizer as an active ingredient”. The solid preparation comprises “a part containing coated particles in which the particles containing an insulin sensitizer are coated with lactose or a sugar alcohol” and “a part containing an active ingredient other than an insulin sensitizer”.
Inventor(s):	Kenichiro Kiyoshima, Kenji Nakamura, Tetsuya Kawano, Masafumi Misaki
Assignee:	Takeda Pharmaceutical Co Ltd
Application Number:	US12/086,700
Patent Claim Types: see list of patent claims	Composition; Dosage form;

US Patent 8,071,130: Pioglitazone-Glimepiride Multilayer Tablet Patent Scope and Landscape

US Patent 8,071,130 protects a narrowly defined multilayer solid dosage form combining pioglitazone and glimepiride. The patent does not claim pioglitazone, glimepiride, or their combination broadly. Its coverage depends on specific formulation architecture, lactose-coated pioglitazone granules, glimepiride granulation, excipient and binder selections, solvent use, and a defined multilayer tableting process.

The strongest commercial risk is directed to a product substantially matching the patented manufacturing sequence and two-layer tablet structure. A conventional single-layer tablet, capsule, bilayer tablet with materially different granulation, or product using a non-equivalent coating system may avoid literal infringement, subject to claim construction and the doctrine of equivalents.

What drug and formulation does US Patent 8,071,130 cover?

The patent covers a solid preparation containing two separately formulated parts:

1. A pioglitazone-containing part with lactose-coated particles.
2. A glimepiride-containing part produced using a separate granulation process.

The finished product must be a multilayer tablet made by compressing the two parts as a laminate. The patent therefore targets a fixed-dose pioglitazone/glimepiride combination in which the active ingredients are physically segregated within different tablet layers.

The claimed architecture addresses formulation problems associated with combining the two drugs, including differences in dose, flowability, compressibility, dissolution behavior, and content uniformity.

The principal claim limitations are:

Claim element	Required feature
Dosage form	Solid preparation
Active ingredients	Pioglitazone or a salt thereof, and glimepiride
Pioglitazone part	Particles containing pioglitazone coated with lactose
Lactose amount	5 to 50 parts by weight per 100 parts of pioglitazone-containing particles
Pioglitazone granulation	Pioglitazone, excipient and disintegrant granulated with binder/lactose dispersion
Glimepiride granulation	Excipient granulated with glimepiride, surfactant, coloring agent and binder dispersion
Additional glimepiride formulation components	Excipient, disintegrant and lubricant
Final structure	Multilayer tablet in laminate form
Optional narrowing limitations	Polysorbate 80, hydroxypropylcellulose, water, lactose or crystalline cellulose
Tableting process	First-compressed layer made at no more than 60% of the pressure used for the next layer, under claim 4

The patent is therefore a formulation and manufacturing patent, not a basic active-ingredient patent.

How broad is independent claim 1?

Claim 1 is broad relative to the dependent claims but narrow relative to the pioglitazone/glimepiride product category.

For infringement, a competing product would generally need to satisfy all of the following limitations:

• Contain pioglitazone or a salt of pioglitazone.
• Contain glimepiride.
• Use separate parts for the two active ingredients.
• Include lactose-coated pioglitazone particles.
• Use lactose in the specified 5-to-50 parts-by-weight range.
• Use the recited pioglitazone granulation process.
• Use the recited glimepiride granulation composition.
• Include the listed categories of excipients, disintegrant and lubricant.
• Be a multilayer tablet formed as a laminate.

A formulation that contains both drugs but does not use lactose-coated pioglitazone particles would not literally satisfy claim 1. The same would apply to a product in which the two actives are uniformly blended into one layer.

Does claim 1 require a bilayer tablet?

The claim requires a multilayer tablet obtained by tableting the two parts “in the form of a laminate.” The ordinary commercial interpretation is a bilayer tablet or another tablet with distinct laminated layers corresponding to the pioglitazone and glimepiride parts.

A tablet with more than two layers could potentially fall within the claim if it still contains the required two parts in laminated form. A capsule, sachet, two-tablet kit, or physically separate tablets would present a stronger noninfringement position because those products would not ordinarily be a single multilayer laminated tablet.

Does the manufacturing process limit the product claim?

The claim describes the coated particles and glimepiride composition by reference to how they are made. This creates a product-by-process issue. In US patent law, a product-by-process limitation may limit infringement analysis where the claimed product cannot be distinguished adequately from products made by other processes. The practical risk depends on whether the process produces identifiable structural or compositional characteristics and how the court construes the claim language.

The process limitations are commercially important because a competitor may not avoid the claim merely by changing documentation or equipment if the resulting product has the claimed characteristics. Conversely, a materially different granulation or coating process may provide a noninfringement argument if the process language is construed as limiting.

What do claims 2 through 9 add?

What does claim 2 protect?

Claim 2 requires the glimepiride part to contain a surfactant. Claim 1 already recites a glimepiride granulation using a surfactant, so claim 2 appears to reinforce or clarify the presence of the surfactant in the final glimepiride part.

The claim may have limited practical scope beyond claim 1 because the independent claim already includes a surfactant in the glimepiride granulation description.

What does claim 3 protect?

Claim 3 narrows the surfactant to Polysorbate 80, commonly known as polysorbate 80 or Tween 80.

A formulation using sodium lauryl sulfate, sodium docusate, poloxamer, lecithin, or another surfactant would not literally satisfy claim 3, although it could remain exposed under claim 1 or claim 2.

What does claim 4 protect?

Claim 4 adds a tableting-pressure relationship:

• The part tableted first must be compressed at a pressure no greater than 60% of the pressure used for the part tableted second.

This limitation is directed to a sequential compression process. It may address layer integrity, prevention of layer separation, and maintenance of dissolution characteristics.

The claim raises several enforcement issues:

• Whether “tableting pressure” means applied force, compression stress, or a machine-reported parameter.
• Whether the 60% ratio must be measured during commercial production or established by batch records.
• Whether the first and second compression steps must occur on the same tableting machine.
• Whether minor process variation affects infringement.

Because claim 4 depends on claim 1, a product must first satisfy every limitation of claim 1 before the pressure limitation becomes relevant.

What does claim 5 protect?

Claim 5 covers a sequential granulation route for the pioglitazone particles:

1. Pioglitazone, excipient and disintegrant are granulated with a binder dispersion.
2. The resulting material is further processed with a binder-and-lactose dispersion.

This claim may capture a two-stage coating or granulation process rather than a single-step addition of all ingredients. A competitor using dry coating, fluid-bed coating, direct compression, or a single granulation step may have stronger design-around arguments.

What does claim 6 protect?

Claim 6 identifies lactose or crystalline cellulose as the excipient. It narrows the excipient class but may cover common pharmaceutical diluents used in commercial tablet manufacture.

What do claims 7 and 8 protect?

Claim 7 again specifies Polysorbate 80 as the surfactant. Its practical value is similar to claim 3, although its dependency from claim 1 gives it a separate claim position.

Claim 8 specifies hydroxypropylcellulose as the binder. A formulation using povidone, hypromellose, pregelatinized starch or another binder would not literally satisfy claim 8, but could remain within claim 1 if the broader binder language is met.

What does claim 9 protect?

Claim 9 specifies water as the solvent. An aqueous granulation process would fall within this claim. An ethanol, isopropanol, acetone or mixed-solvent process would not literally satisfy claim 9, though it could remain within claim 1 if the broader solvent limitation is met.

How strong is the patent estate for pioglitazone and glimepiride?

The patent has meaningful formulation value but limited platform breadth.

Strength factor	Assessment
Active-ingredient coverage	Narrow; no standalone pioglitazone or glimepiride monopoly
Combination coverage	Limited to a specific solid formulation
Dosage-form coverage	Strongest for laminated multilayer tablets
Process coverage	Significant because both active parts are defined by granulation steps
Excipient coverage	Moderate; broad in claim 1, narrowed in dependent claims
Design-around potential	Moderate to high
Generic exposure	Higher for products using different architecture or process
Invalidity exposure	Depends on prior art concerning multilayer tablets, wet granulation and lactose coating
Biosimilar relevance	None; this is a small-molecule product

The principal patent-strength question is whether the claimed combination of lactose coating, separate granulation, and multilayer compression was non-obvious over prior art that disclosed pioglitazone/glimepiride combinations or multilayer tablets separately.

Potential validity challenges could focus on:

• Anticipation by a prior-art combination tablet.
• Obviousness based on known granulation and coating techniques.
• Lack of written description for the full breadth of claim 1.
• Enablement across all excipients, binders, solvents and process variations.
• Indefiniteness of terms such as “coated particles,” “dispersion,” “multilayer tablet,” and “tableting pressure.”
• Whether the process limitations distinguish the claimed product from conventionally manufactured tablets.

The narrower claims involving Polysorbate 80, hydroxypropylcellulose, water and the 5-to-50 lactose range may be more resistant to broad prior-art attacks if the combination was not disclosed, but they also cover a smaller commercial territory.

What formulations are most exposed to infringement?

The highest-risk configuration is a fixed-dose bilayer tablet with the following characteristics:

• Pioglitazone in one layer.
• Glimepiride in the second layer.
• Lactose-coated pioglitazone granules.
• Lactose coating at 5% to 50% relative to the pioglitazone-containing particles.
• Wet granulation using hydroxypropylcellulose in water.
• Glimepiride granulation containing Polysorbate 80.
• Sequential tableting with the first compression at no more than 60% of the second compression.

A formulation can present substantial risk even if it changes one dependent-claim element, because claim 1 contains broader language for several components.

Competing design	Likely claim exposure
Bilayer tablet using the claimed lactose-coated pioglitazone particles	High
Bilayer tablet with Polysorbate 80 and aqueous HPC granulation	Very high
Bilayer tablet with lactose-coated particles but different glimepiride surfactant	Potential claim 1 exposure
Single-layer homogeneous blend	Lower literal exposure
Two separate tablets packaged together	Lower literal exposure
Capsule containing separate granules	Lower literal exposure
Bilayer tablet using uncoated pioglitazone granules	Lower literal exposure
Direct-compression bilayer tablet	Lower process exposure, subject to product-by-process construction
Bilayer tablet with lactose coating outside the claimed range	Lower claim 1 exposure, but measurement methodology matters
Bilayer tablet using a nonaqueous solvent	Claim 9 avoided; broader claims may remain relevant

When does US Patent 8,071,130 lose exclusivity?

The patent number alone does not establish the exact expiration date. US patent term is generally measured from the earliest effective nonprovisional or international filing date, subject to patent-term adjustment, patent-term extension and terminal disclaimers. The grant date, December 6, 2011, is not the expiration date.[1]

For a formulation patent of this type, the relevant exclusivity analysis has four separate components:

Exclusivity category	Relevance
Patent term	Determines enforceability of claims 1-9
FDA new-drug exclusivity	Separate from patent term
Orange Book listing	Determines whether an ANDA applicant must address the patent
Pediatric exclusivity	May add six months if awarded and applicable

FDA marketing exclusivity for the underlying combination product is separate from the patent. A generic applicant may file an ANDA after the applicable filing date even if a patent remains in force, subject to Paragraph IV certification and any statutory stay.[2]

What is the Orange Book status of the pioglitazone-glimepiride combination?

The product associated with this formulation is Duetact, a fixed-dose combination of pioglitazone hydrochloride and glimepiride marketed by Takeda Pharmaceuticals. The relevant FDA regulatory records include NDA 021842 and the FDA-approved product labeling.[3]

Orange Book treatment must be evaluated separately from patent validity. A patent may:

• Be listed against the reference drug.
• Have been delisted.
• Remain listed but be expired.
• Be listed only for a method of use.
• Be subject to a patent-use code that limits the scope of an ANDA certification.

The claim text supplied here is directed to a composition and manufacturing configuration. It is not a method-of-use claim. If listed in the Orange Book, it would generally be addressed as a product or formulation patent rather than a method-of-use patent.

The supplied claim text does not establish the current Orange Book listing status, patent-use code, or active expiration record for US 8,071,130. Those points are controlled by FDA Orange Book and USPTO records, not by the claim language alone.[2]

Are Paragraph IV challenges likely for this patent?

A generic applicant seeking approval for a pioglitazone/glimepiride product could use one of four principal approaches:

1. Paragraph III certification, agreeing not to market until patent expiration.
2. Paragraph IV certification, asserting that the patent is invalid, unenforceable or will not be infringed.
3. A section viii statement, if the listed patent claims only an excluded method of use.
4. A product design that avoids a listed formulation patent and supports a noninfringement certification.

For this patent, a Paragraph IV strategy would likely focus on the narrow structural and process limitations. The most credible noninfringement positions would involve:

• No lactose coating on pioglitazone particles.
• A different physical arrangement of the two drugs.
• No laminated multilayer tablet.
• A different granulation sequence.
• A different solvent or binder.
• A lactose amount outside the claimed range.
• A tablet produced without the claimed pressure relationship.

An invalidity challenge would likely rely on prior art involving:

• Pioglitazone/glimepiride combinations.
• Multilayer tablets.
• Wet granulation of poorly soluble drugs.
• Lactose coating of active-containing particles.
• Surfactant-assisted glimepiride formulations.
• Sequential compression of tablet layers.

The presence of several cumulative limitations makes a complete anticipation challenge more difficult than an obviousness challenge. A challenger would generally need to show that the full combination was taught or would have been obvious, not merely that each component was individually known.

What generic launch scenarios exist?

At-risk launch before patent expiry

A generic company could launch before final patent expiry after a Paragraph IV certification, accepting potential damages and an injunction if the patent holder prevails. This strategy is most plausible where the proposed product uses a different architecture and the applicant has a strong noninfringement position.

Launch after patent expiration

This is the lower-risk pathway if US 8,071,130 remains the principal formulation patent. It avoids infringement damages but may surrender first-mover or 180-day exclusivity opportunities associated with a successful Paragraph IV filing.

Design-around launch

A design-around could use:

• A single-layer tablet.
• Separate tablets administered together.
• A capsule containing separate granules.
• Uncoated pioglitazone granules.
• A polymeric coating rather than lactose.
• Direct compression.
• A nonaqueous granulation solvent.
• A surfactant other than Polysorbate 80.
• A binder other than hydroxypropylcellulose.

The commercial challenge is maintaining dissolution, dose uniformity and manufacturability while avoiding the claimed combination. A design-around that changes only Polysorbate 80 or hydroxypropylcellulose may avoid dependent claims but still face claim 1.

Which companies may challenge the patent?

The patent claim text does not identify an ANDA filer, Paragraph IV challenger, litigation defendant or settlement counterparty. The commercially relevant challenger universe consists of generic manufacturers capable of producing a fixed-dose pioglitazone/glimepiride product, including large US ANDA sponsors, Indian pharmaceutical companies and contract manufacturers.

No company should be treated as a confirmed challenger without an ANDA record, Paragraph IV notice, district-court complaint, FDA approval record or settlement filing. Patent ownership, FDA sponsorship and commercial distribution may also differ among affiliated entities.

What patent litigation and settlement issues matter?

The main litigation issues would be:

• Whether a proposed product contains “coated particles” within the meaning of claim 1.
• Whether lactose is functioning as a coating material rather than merely as an excipient.
• Whether the 5-to-50 parts-by-weight range is met.
• Whether the accused granules were made by the claimed process.
• Whether product-by-process language limits infringement.
• Whether “multilayer tablet” and “laminate” require physically distinct layers.
• Whether the claimed compression-pressure ratio is satisfied.
• Whether prosecution history limits the scope of equivalents.

A settlement could include a licensed entry date, authorized generic supply, covenants not to sue, manufacturing restrictions or restrictions on the dosage strengths covered by the agreement. The claim language alone does not establish that a settlement exists.

How does this patent compare with broader drug patents?

US 8,071,130 is narrower than:

• A patent claiming pioglitazone as a chemical entity.
• A patent claiming glimepiride as a chemical entity.
• A broad patent claiming any pharmaceutical combination of the two drugs.
• A method-of-use patent claiming treatment of type 2 diabetes with either active ingredient.

It is stronger than a generic process patent where the claimed process is optional because claim 1 ties the final product to specific formulation and granulation characteristics. Its value is concentrated in the fixed-dose multilayer product and associated manufacturing know-how.

Geographically, the US patent protects only US activity. Corresponding national patents or applications in Europe, Japan and other jurisdictions must be analyzed independently. Patent family members may have different claim sets, prosecution outcomes and expiration dates.

Key Takeaways

• US 8,071,130 is a formulation and manufacturing patent for a pioglitazone/glimepiride multilayer tablet.
• Claim 1 is the commercial core and requires lactose-coated pioglitazone particles, separately granulated glimepiride, and a laminated multilayer tablet.
• Claims 3, 7, 8 and 9 narrow the formulation to Polysorbate 80, hydroxypropylcellulose and water.
• Claim 4 adds a 60% tableting-pressure ratio and is particularly process-sensitive.
• The patent does not broadly block all pioglitazone/glimepiride combinations.
• Single-layer tablets, capsules, separate-tablet products and materially different granulation routes offer the clearest design-around paths.
• Paragraph IV risk depends on the proposed product’s physical structure and manufacturing records.
• FDA exclusivity, Orange Book listing and patent enforceability are separate questions.
• The patent is relevant to generic competition for Duetact-type products, but the claim text alone does not establish current litigation, settlement or Orange Book status.
• No biosimilar pathway applies because pioglitazone and glimepiride are small-molecule active ingredients.

FAQs About US Patent 8,071,130

Does US 8,071,130 cover all Duetact products?

No. It covers products meeting the claimed formulation and multilayer-tablet limitations. A product with the same active ingredients but a different dosage-form architecture may fall outside the claims.

Can a generic avoid the patent by using a different surfactant?

Possibly, but changing the surfactant alone may avoid claims 3 and 7 while leaving exposure under claim 1, which recites a surfactant more broadly.

Is lactose required in every claim?

Lactose is central to claim 1 because the pioglitazone-containing particles must be coated with lactose. Claim 6 separately identifies lactose or crystalline cellulose as an excipient.

Does the patent cover a tablet containing pioglitazone and glimepiride in one blended layer?

Not expressly. The independent claim requires separate parts tableted as a multilayer laminate. A homogeneous single-layer blend presents a stronger noninfringement position.

Can a company use a nonaqueous solvent to avoid the patent?

A nonaqueous solvent may avoid claim 9, which specifies water, but it may not avoid claim 1 because claim 1 recites a solvent without limiting it to water.

References

1. United States Patent and Trademark Office. (2011). U.S. Patent No. 8,071,130, Solid preparation.
2. U.S. Food and Drug Administration. (n.d.). Approved drug products with therapeutic equivalence evaluations: Orange Book.
3. U.S. Food and Drug Administration. (n.d.). Duetact (pioglitazone hydrochloride and glimepiride) prescribing information, NDA 021842.

Drugs Protected by US Patent 8,071,130

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Takeda Pharms Usa	DUETACT	glimepiride; pioglitazone hydrochloride	TABLET;ORAL	021925-001	Jul 28, 2006	AB	RX	Yes	Yes	8,071,130		Y
Takeda Pharms Usa	DUETACT	glimepiride; pioglitazone hydrochloride	TABLET;ORAL	021925-002	Jul 28, 2006	AB	RX	Yes	No	8,071,130		Y

Foreign Priority and PCT Information for Patent: 8,071,130

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Japan	2005-370375	Dec 22, 2005

PCT Information
PCT Filed	December 21, 2006	PCT Application Number:	PCT/JP2006/326169
PCT Publication Date:	June 28, 2007	PCT Publication Number:	WO2007/072992

International Family Members for US Patent 8,071,130

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	058605
Australia	2006328328
Brazil	PI0620020
Canada	2633149
China	101384251
Costa Rica	10032