United States Drug Patent 6,027,714: Claims, Scope, Expiration, and Budesonide Dry-Powder Patent Landscape

US Patent 6,027,714 protects a specific budesonide dry-powder formulation and manufacturing process. Its central limitation is the combination of sub-10-micron budesonide and carrier particles with a poured bulk density of 0.28 to 0.38 g/mL. The patent also claims narrower density, particle-size, carrier, uniformity, respiratory-treatment, spheronization, and remicronization limitations.

The patent issued on February 22, 2000, to Astra Aktiebolag. Its twenty-year patent term has expired. As a result, US 6,027,714 does not currently block generic manufacture, formulation, or sale in the United States, although later patents covering specific products, devices, combinations, processes, or regulatory indications may still matter. [1]

What does US Patent 6,027,714 protect?

US 6,027,714 protects a dry-powder pharmaceutical composition containing:

Budesonide as the active ingredient;
A particulate carrier;
Budesonide particles with a mass median diameter below 10 micrometers;
Carrier particles with a mass median diameter below 10 micrometers; and
A poured bulk density from 0.28 to 0.38 g/mL.

The patent is directed to powder engineering rather than to budesonide as a molecule. Budesonide itself was known before the patent. The inventive focus is the physical structure and density of a carrier-based inhalation powder, together with processing steps intended to produce the claimed powder characteristics. [1]

Core claim architecture

Claim	Subject matter	Principal limitation
1	Composition	Budesonide and carrier particles below 10 μm; poured bulk density 0.28-0.38 g/mL
2	Composition	Narrower bulk density of 0.30-0.36 g/mL
3	Composition	Substantially uniform distribution of active and carrier
4	Composition use	Use for treating a respiratory disorder
5	Process	Micronization, optional conditioning, and spheronization
6	Process	Low-energy remicronization after conditioning
7	Treatment method	Administering the composition to a patient with a respiratory disorder
8	Composition	Carrier selected from sugars, polysaccharides, and polyols
9	Composition	Specific carriers, including lactose, glucose, mannitol, starch, and others
10	Composition	Lactose monohydrate
11	Composition	Budesonide and carrier particle size of 1-7 μm
12	Process	1-7 μm particle-size range
13	Process	0.30-0.36 g/mL bulk density
14	Process	Substantially uniform distribution

Claim 1 is the broadest composition claim. Claims 2, 3, and 8 through 11 narrow the composition. Claims 5, 6, and 12 through 14 cover manufacturing conditions and resulting powder properties. Claims 4 and 7 address therapeutic use.

How should claim 1 be interpreted?

Claim 1 requires more than a budesonide-lactose mixture. A potentially infringing composition would need to satisfy all of the following limitations:

It is a dry powder pharmaceutical composition.
It contains budesonide.
It contains a carrier substance.
Budesonide particles have a mass median diameter below 10 μm.
Carrier particles have a mass median diameter below 10 μm.
The composition has a poured bulk density between 0.28 and 0.38 g/mL.

The particle-size limitations apply to both components. A formulation with micronized budesonide but coarse lactose would not literally satisfy claim 1 because the carrier would not have a mass median diameter below 10 μm.

The bulk-density limitation is also essential. A composition falling outside the claimed density range would not literally infringe claim 1, even if it contained budesonide and micronized lactose. Because bulk density depends on measurement protocol, powder handling, conditioning, moisture, and packing behavior, analytical testing must use a reproducible method consistent with the patent specification and applicable industry practice.

What is mass median diameter?

Mass median diameter, or MMD, is the particle diameter at which half of the particle mass is in smaller particles and half is in larger particles. It is not interchangeable with:

Number median diameter;
Volume median diameter;
Aerodynamic diameter;
Geometric mean diameter; or
A single laser-diffraction D50 value without method validation.

A freedom-to-operate analysis would need to compare the accused product’s particle-size measurement method with the method used to characterize the patented composition. Particle-size distributions can produce materially different results depending on dispersion energy, agglomeration control, humidity, and instrument settings.

What formulations are protected by US 6,027,714?

The patent covers a broad class of carrier-based budesonide dry powders, subject to the particle-size and density limitations.

Carrier substances

Claim 8 covers carriers selected from:

Monosaccharides;
Disaccharides;
Polysaccharides; and
Polyols.

Claim 9 identifies specific carriers:

Lactose;
Glucose;
Raffinose;
Melezitose;
Lactitol;
Maltitol;
Trehalose;
Sucrose;
Mannitol; and
Starch.

Claim 10 narrows the carrier to lactose monohydrate. This claim is commercially relevant because lactose is a common carrier in dry-powder inhalers, including products based on micronized corticosteroids.

Budesonide-lactose powders

A budesonide-lactose powder may fall within the technical scope if:

Both components meet the claimed particle-size requirement;
The final powder has the required poured bulk density; and
The product otherwise satisfies the composition language.

The claims do not require a particular inhaler device, dose strength, capsule, blister, reservoir, or metering mechanism. They also do not require a specific budesonide polymorph, excipient ratio, or aerodynamic particle-size fraction unless those characteristics are necessary to meet the express claim limitations.

How narrow are the density limitations?

The density limitations are among the most important claim boundaries.

Claim	Bulk-density range
1	0.28-0.38 g/mL
2	0.30-0.36 g/mL
13	0.30-0.36 g/mL

Claim 2 is dependent on claim 1 and therefore retains all limitations of claim 1. Claim 13 applies the same density range to the process of claim 6.

The density range appears designed to control powder flow, dispersibility, dose uniformity, and inhaler performance. A powder with an excessively low density may be difficult to meter consistently. A powder with excessive density may exhibit different deagglomeration behavior and aerosolization characteristics.

From an infringement perspective, density is a measurable product property. A manufacturer may have a design-around argument if its composition consistently falls below 0.28 g/mL or above 0.38 g/mL. That strategy would require validation across manufacturing lots, storage conditions, humidity levels, and commercial packaging because density can change during handling and compaction.

What manufacturing processes are claimed?

Claim 5 covers a process comprising:

Micronizing budesonide and the carrier;
Optionally conditioning the product; and
Spheronizing until the desired bulk density is obtained.

Claim 6 adds a low-energy remicronization step after conditioning.

These claims are process claims, not merely product-by-process claims. The process must include the specified operations. A manufacturer using high-energy blending, spray drying, fluid-bed processing, ordered mixing, or another technique may avoid literal infringement of claims 5 and 6 if it does not perform the claimed sequence.

What is spheronization?

Spheronization in this context refers to processing powder particles or agglomerates to produce a more rounded or controlled powder structure. The claimed endpoint is not simply completion of a processing step. Claim 5 requires spheronization until the desired bulk density is obtained.

That language creates two issues:

The process must include spheronization; and
The process must be controlled by reference to the desired density.

A process that produces a powder within the claimed density range but does not use spheronization may fall outside the literal scope of claim 5, although it could remain relevant to the composition claims if the final product satisfies claim 1.

What is low-energy remicronization?

Claim 6 requires low-energy remicronization after the conditioning step. The patent does not make every remicronization process relevant. The sequence, energy level, and timing matter.

A process using a high-energy mill, remicronization before conditioning, or no remicronization may avoid claim 6. The technical record would need to establish:

The equipment used;
Specific energy input;
Processing duration;
Feed rate;
Particle-size change;
The point at which conditioning occurred; and
Whether the process generated substantially uniform distribution.

How do the treatment claims operate?

Claim 4 covers the composition for treating a respiratory disorder. Claim 7 covers a method of treating a patient by administering a therapeutically effective amount of the composition.

The respiratory indications are not limited to one named disease in the issued claims. The language can encompass disorders such as asthma or chronic obstructive pulmonary disease when the composition is administered for respiratory treatment. The claims do not require a particular dose, dosing frequency, inhaler device, or duration of therapy.

The treatment claims are narrower than a composition claim in one respect: infringement requires the claimed composition and the claimed therapeutic context. They may have limited practical value against a generic manufacturer where the formulation claim is the primary asserted claim. They can have greater relevance to induced-infringement theories if a manufacturer markets instructions directing use of a qualifying composition for a covered respiratory disorder.

When did US 6,027,714 lose exclusivity?

US 6,027,714 expired after the applicable twenty-year patent term. The patent issued on February 22, 2000, and its effective term ran from the relevant US or international filing date rather than from the issue date. The patent was therefore no longer enforceable by the mid-2010s. [1]

Event	Date or period
Patent issued	February 22, 2000
Statutory patent term	Twenty years from the applicable filing date
Expected US expiration	2015
Current status	Expired; no prospective enforcement term

Patent term adjustment or patent term extension can alter a nominal expiration date. US 6,027,714 is not a live US barrier to entry as of 2026. The expiration of this patent does not eliminate other intellectual-property rights covering a commercial budesonide inhaler, suspension, combination product, device, manufacturing method, or formulation.

What is the Orange Book status of US 6,027,714?

An Orange Book listing must be analyzed at the drug-product and NDA level. A patent may be technically relevant to a formulation yet not be listed for a particular approved product. FDA listing requirements focus on patents claiming the drug substance, drug product, or approved method of use. [2]

US 6,027,714 is a formulation and process patent. It does not claim budesonide as a new chemical entity. Its relevance to an approved product depends on whether the listed NDA product met the claimed composition limitations and whether the patent was submitted for listing.

Because the patent has expired, it does not create a current Orange Book exclusivity barrier. Any historic listing would not produce an active patent-based delay for a present ANDA applicant. Current entry analysis must examine the Orange Book for the specific reference product and identify any later unexpired patents. [2]

Did generic manufacturers face Paragraph IV risk?

While the patent was in force, an ANDA applicant seeking approval for a qualifying budesonide dry-powder product could have addressed the patent through:

Paragraph I certification, if no patent was listed;
Paragraph II certification, if the patent had expired;
Paragraph III certification, accepting approval after expiration; or
Paragraph IV certification, asserting that the patent was invalid, unenforceable, or not infringed.

Under the Hatch-Waxman framework, a Paragraph IV notice can trigger patent litigation and a potential 30-month stay of ANDA approval if the statutory conditions are met. [3]

For US 6,027,714, any historic Paragraph IV dispute would now have limited commercial significance because the patent term has ended. A current applicant would not need to overcome this patent through a Paragraph IV challenge unless another legal issue made the expired patent relevant to the regulatory filing record.

Which products and competitors are most relevant?

The patent is most closely associated with the dry-powder inhalation segment for budesonide, including products marketed through AstraZeneca’s Pulmicort franchise. Relevant competitive categories include:

Category	Representative products or technologies	Patent relevance
Budesonide dry powder	Pulmicort Flexhaler and comparable DPI products	Carrier, particle engineering, device and formulation patents
Budesonide inhalation suspension	Pulmicort Respules and generic equivalents	Suspension, container, dosing, and method-of-use patents
Budesonide/formoterol	Symbicort and generic budesonide-formoterol inhalers	Combination, device, formulation, and method-of-use patents
Generic budesonide inhalers	ANDA products and authorized alternatives	Current barriers depend on later patents and product-specific listings
Non-budesonide corticosteroids	Fluticasone, beclomethasone, mometasone products	Compete therapeutically but do not ordinarily implicate this patent

US 6,027,714 does not cover every budesonide inhalation product. A suspension product may avoid the dry-powder limitations. A combination inhaler may avoid the claim if it does not use the claimed carrier-particle structure or density. A device containing a qualifying powder may still implicate other patents directed to the inhaler mechanism.

How strong is the patent estate for a current entrant?

The direct estate of US 6,027,714 has no current blocking strength because the patent is expired. Its historical technical scope was meaningful, but its present value is primarily defensive and analytical.

Historical strengths

The composition claims targeted a defined powder architecture.
The claims combined particle-size and bulk-density limitations.
Lactose monohydrate was expressly claimed.
Process claims covered micronization, conditioning, spheronization, and remicronization.
Treatment claims connected the powder to respiratory use.

Historical weaknesses

Budesonide and carrier-based inhalation powders were known technical areas.
The claims depended heavily on measurable physical properties.
Density can be engineered outside the claimed range.
Alternative manufacturing routes could avoid the process claims.
The patent did not claim the budesonide molecule itself.
The claims did not expressly cover every inhaler device or dosage form.

Current commercial assessment

Risk area	Current risk from US 6,027,714
Generic budesonide dry powder	None from this expired patent
Budesonide-lactose formulation	None from this expired patent, subject to later patents
Budesonide inhalation suspension	No direct risk from the dry-powder claims
Budesonide-formoterol combination	No direct risk from this patent alone
Inhaler device	No direct risk from this patent alone
Manufacturing process	No enforceable risk from this expired patent
Paragraph IV litigation	No current litigation trigger based solely on this patent
Biosimilar pathway	Not applicable; budesonide is a small molecule

Is biosimilar risk relevant to budesonide?

No. Budesonide is a chemically synthesized small-molecule drug, not a biologic subject to the biosimilar pathway under the Public Health Service Act. Competitive entry occurs primarily through the ANDA pathway, subject to pharmaceutical equivalence, bioequivalence, device considerations, and any applicable listed patents or regulatory exclusivities. [2,4]

For inhaled products, the principal technical barriers are often:

Dose uniformity;
Delivered-dose performance;
Aerodynamic particle-size distribution;
Device compatibility;
Inhaler resistance;
Stability and moisture control;
Bioequivalence methodology; and
Comparative clinical or pharmacodynamic evidence where required.

These regulatory barriers can remain significant after patent expiry, but they are not patent exclusivity rights.

What geographic coverage does the patent provide?

US 6,027,714 provides rights only in the United States. It does not directly control commercial activity in Canada, Europe, Japan, China, or other jurisdictions.

The invention may have counterpart applications in other countries through a related priority or PCT filing. Each national patent must be reviewed independently for:

Grant status;
Claim scope;
Patent-term calculation;
Supplementary protection certificate status;
Opposition or revocation history;
Maintenance-fee status; and
National expiration date.

A US expiration does not establish that every foreign counterpart has expired, although patents from the same family often reach the end of their terms at roughly comparable times.

What litigation and settlement issues matter?

No current enforcement value attaches to US 6,027,714 after expiration. Any historic litigation or settlement involving budesonide inhalers should be separated into four categories:

Litigation specifically involving US 6,027,714;
Litigation involving later Pulmicort or Symbicort patents;
Device patent litigation;
Regulatory or commercial settlements unrelated to this patent.

A settlement concerning another AstraZeneca patent does not establish that US 6,027,714 remained valid, enforceable, or commercially blocking. Similarly, an ANDA approval date does not prove that a generic product fell outside the claims. The relevant evidence is the asserted patent, court docket, settlement terms, product formulation, and launch restrictions.

What generic launch scenarios existed and what remains relevant?

Scenario 1: Direct launch after expiration

A manufacturer could launch after expiration without overcoming US 6,027,714, assuming no later unexpired patents blocked the product.

Scenario 2: Earlier Paragraph IV launch

Before expiration, an ANDA applicant could have challenged the patent through Paragraph IV certification. The commercial outcome would have depended on litigation, claim construction, validity, infringement, and settlement terms.

Scenario 3: Non-infringing powder design

A manufacturer could design around the claims by using:

A carrier with a mass median diameter of 10 μm or greater;
A final poured bulk density outside 0.28-0.38 g/mL;
A non-powder dosage form;
A suspension formulation;
A different manufacturing sequence; or
A carrier or powder structure that does not meet the claimed limitations.

These approaches would have required technical validation because avoiding one claim limitation does not establish freedom from later patents.

Scenario 4: Combination-product entry

A budesonide-formoterol product requires a separate analysis of combination, device, formulation, and method-of-use patents. US 6,027,714 alone does not resolve entry risk for a combination inhaler.

What is the revenue exposure from this patent?

The patent itself has no current revenue-protection value because it is expired. Its historical revenue exposure likely related to dry-powder budesonide products using a micronized carrier system, particularly products in the Pulmicort inhaler franchise.

Current revenue exposure depends on later rights covering:

The approved inhaler device;
Specific formulation ratios;
Dose strengths;
Combination products;
Manufacturing controls;
Labelled indications;
Pediatric or maintenance-treatment methods; and
Product-specific Orange Book listings.

A financial model should therefore assign zero remaining patent-term value to US 6,027,714 and model any continuing exclusivity under later patent families and regulatory protections.

Key Takeaways

US 6,027,714 covers a budesonide dry powder with micronized budesonide, micronized carrier, and a poured bulk density of 0.28-0.38 g/mL.
The narrower claims cover 0.30-0.36 g/mL density, 1-7 μm particle size, uniform distribution, lactose monohydrate, and specified sugar or polyol carriers.
Process claims cover micronization, conditioning, spheronization, and low-energy remicronization.
Claims 4 and 7 address respiratory treatment using the claimed composition.
The patent issued on February 22, 2000, and expired under the applicable twenty-year term in approximately 2015.
It is not a current US patent barrier to generic budesonide entry.
Budesonide is a small molecule, so biosimilar analysis does not apply.
Current commercial risk must be assessed against later formulation, device, combination, manufacturing, method-of-use, and Orange Book-listed patents.
The patent has no current direct revenue-protection value, but its claim structure remains relevant to historical product and freedom-to-operate analysis.

FAQs

Does US 6,027,714 cover all budesonide inhalers?

No. It covers only products meeting the claimed dry-powder, particle-size, carrier, and density limitations. Suspension products, combination products, and inhalers using different powder structures require separate analysis.

Does lactose monohydrate automatically infringe US 6,027,714?

No. Lactose monohydrate is one limitation in claim 10, but infringement also requires the other applicable limitations, including micronized budesonide, micronized carrier, and the claimed bulk-density range.

Can a generic manufacturer use the same budesonide formulation after patent expiry?

Yes, US 6,027,714 itself no longer blocks use of the claimed formulation in the United States. Later patents and FDA requirements may still affect launch timing.

Is the poured bulk density measured on the finished inhaler dose?

The claim is directed to the composition’s poured bulk density. Testing should focus on the powder composition before device administration and use a reproducible method aligned with the patent disclosure and accepted analytical practice.

Does the patent cover spray-dried budesonide powders?

Not necessarily. Spray drying may produce a powder with the claimed physical properties, but the composition claims depend on the final product limitations. The process claims separately require micronization, conditioning, spheronization, and, for claim 6, low-energy remicronization.

References

Astra Aktiebolag. (2000). Dry powder composition, U.S. Patent No. 6,027,714. United States Patent and Trademark Office.
U.S. Food and Drug Administration. (2024). Approved drug products with therapeutic equivalence evaluations (Orange Book). FDA.
21 U.S.C. § 355(j). Abbreviated new drug applications and patent certifications.
U.S. Food and Drug Administration. (2024). Generic drug user fee amendments and abbreviated new drug application guidance. FDA.

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Sweden	9700133	Jan 20, 1997

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	389390	⤷ Start Trial
Australia	5785798	⤷ Start Trial
Australia	726916	⤷ Start Trial
Belgium	1011400	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Summary for Patent: 6,027,714