Details for Patent: 9,694,008

Which drugs does patent 9,694,008 protect, and when does it expire?

Patent 9,694,008 protects MEZOFY and is included in one NDA.

This patent has five patent family members in four countries.

Summary for Patent: 9,694,008

Title:	Fast-dissolving oral film preparation comprising aripiprazole
Abstract:	The present invention relates to an orally fast dissolving film formulation including aripiprazole. The orally fast dissolving film formulation includes aripiprazole or a pharmaceutically acceptable salt thereof and an organic acid. The orally fast dissolving film formulation has a pH in the range of 4.7 to 6.0. The orally fast dissolving film formulation may further include a film base polymer. The orally fast dissolving film formulation has a high dissolution rate, causes no risk of damage to oral tissues, masks a bitter taste of aripiprazole, and gives a good feeling upon taking.
Inventor(s):	Yong Soo Kim, Jun Ho SHIN
Assignee:	CMG Pharmaceutical Co Ltd
Application Number:	US14/419,231
Patent Claim Types: see list of patent claims	Formulation; Compound;

United States Patent 9,694,008: Claim Scope, Validity Risks, and Aripiprazole Oral-Film Patent Landscape

U.S. Patent No. 9,694,008 protects a narrowly defined aripiprazole orally fast dissolving film. The independent claim requires a specific combination of citric acid, formulation pH, saliva-dissolved pH, aripiprazole-to-acid ratio, and film dosage form. Dependent claims add citric-acid concentration, a dual-sweetener system, and a hydroxypropyl methylcellulose-based film matrix.

The patent is materially narrower than a general claim to aripiprazole oral films. A competing product that changes the organic acid, pH window, acid concentration, sweetener system, or film polymer may avoid literal infringement, although the doctrine of equivalents and process evidence remain relevant.

What does U.S. Patent 9,694,008 protect?

U.S. Patent 9,694,008 protects an orally fast dissolving film formulation containing aripiprazole or an acceptable salt and citric acid, subject to two separate pH requirements:

1. The film formulation must have a pH of 4.95 to 5.18.
2. After dissolution in the oral cavity, the formulation must have a pH of 6.2 to 6.4.

The claim also requires an aripiprazole-to-citric-acid weight ratio of 2:1 to 66:1. Each limitation is cumulative. A product that satisfies four of the five principal technical limitations but falls outside the claimed ratio or pH range does not literally meet claim 1.

Claim element	Requirement
Dosage form	Orally fast dissolving film
Active ingredient	Aripiprazole or pharmaceutically acceptable salt
Organic acid	Citric acid
Initial formulation pH	4.95 to 5.18
Oral-cavity pH	6.2 to 6.4 after dissolution
Active-to-acid ratio	2:1 to 66:1 by weight
Claim 2 addition	Citric acid at 0.2% to 1.0% by total formulation weight
Claim 3 addition	Sucralose and acesulfame potassium
Claim 4 addition	Film base essentially comprising hydroxypropyl methylcellulose, optionally with polyvinyl alcohol

The claims are formulation claims. They do not claim aripiprazole as a chemical compound, the treatment of schizophrenia generally, or every oral transmucosal delivery system.

How should claim 1 be construed?

Claim 1 is the commercial and litigation center of the patent because claims 2 through 4 depend on it and add narrower limitations.

Orally fast dissolving film

The product must be a film that dissolves rapidly in the mouth. The limitation distinguishes the claimed product from conventional tablets, orally disintegrating tablets, capsules, liquid solutions, suspensions, and long-duration buccal patches.

A thin strip that merely disintegrates but does not meet the relevant dissolution or disintegration characteristics could create a claim-construction dispute. The patent specification and prosecution history would be important in determining whether "fast dissolving" has a defined technical meaning, including any specified test method or time limit.

Aripiprazole or a pharmaceutically acceptable salt

The claim covers aripiprazole and salts accepted for pharmaceutical use. A salt is not outside the claim merely because it has different solubility or stability characteristics. The claim does not require a particular aripiprazole particle size, polymorph, amorphous state, or salt unless those limitations appear elsewhere in the patent specification or prosecution history.

The claim does not cover a different active pharmaceutical ingredient that has a similar pharmacological mechanism. It also does not necessarily cover a prodrug or covalent derivative of aripiprazole if that material is not legally treated as aripiprazole or a pharmaceutically acceptable salt.

Citric acid

Citric acid is mandatory. The broader wording referring to an organic acid does not preserve coverage for all organic acids because the claim expressly narrows the limitation to citric acid.

A formulation using malic acid, tartaric acid, fumaric acid, lactic acid, succinic acid, or another acid would not literally satisfy claim 1. The patentee could assert equivalence, but the express selection of citric acid and the prosecution history could restrict that argument.

Two pH limitations

The pH limitations create a significant infringement and validity issue. The claim distinguishes the pH of the manufactured film from the pH after dissolution in the oral cavity.

Measurement	Claimed range	Likely evidentiary issue
Film formulation pH	4.95-5.18	Sample preparation, extraction medium, temperature, calibration
Dissolved oral-cavity pH	6.2-6.4	Saliva volume, buffer capacity, dissolution time, measurement location

A generic developer would need to determine how the patent defines each pH measurement. A pH value measured after dissolving the film in purified water may not be equivalent to a value measured in artificial saliva or an oral cavity. The patent’s examples, analytical methods, and prosecution record may determine whether the ranges are measured at a fixed concentration or under a specified protocol.

The narrow 4.95-to-5.18 range is only 0.23 pH units wide. The 6.2-to-6.4 oral-cavity range is only 0.2 pH units wide. Small differences in test conditions could affect infringement conclusions.

Aripiprazole-to-citric-acid ratio

The claimed ratio ranges from 2:1 to 66:1 by weight. This is broad numerically but restricted to a specific active-acid combination.

A ratio below 2:1 or above 66:1 would fall outside literal coverage. The calculation should use the same basis for aripiprazole and citric acid. A salt-based calculation may generate disputes if the product label reports aripiprazole-equivalent content while the formulation uses the mass of an aripiprazole salt.

For example, a product containing 20 mg of aripiprazole equivalent cannot automatically be analyzed as containing 20 mg of the salt. The relevant calculation depends on the claim construction and the actual composition.

What do claims 2, 3, and 4 add?

What formulation is covered by claim 2?

Claim 2 requires citric acid at 0.2% to 1.0% by total formulation weight. It narrows claim 1 by adding a concentration limitation.

Claim 2 therefore covers only products that meet all claim 1 limitations and contain citric acid within the specified concentration range. A product outside that concentration range may still infringe claim 1 but would not infringe claim 2.

The weight percentage should be calculated against the total formulation weight, including active ingredient, polymer, sweeteners, plasticizers, flavors, water or residual solvents as legally relevant, and other excipients. Manufacturing records and batch formulas would be central evidence.

What sweeteners are protected by claim 3?

Claim 3 requires both sucralose and acesulfame potassium. The use of either sweetener alone does not meet the claim. A formulation containing saccharin, aspartame, steviol glycosides, or another sweetener without both named components would not literally satisfy claim 3, although it could still fall within claim 1.

Claim 3 is commercially narrower than claim 1 and may be less important if competing products use different taste-masking systems. It remains relevant because aripiprazole is bitter and sweetener combinations can affect patient acceptability, formulation stability, and product sameness.

What film polymers are protected by claim 4?

Claim 4 requires a film base polymer that essentially comprises hydroxypropyl methylcellulose, or HPMC. Polyvinyl alcohol may also be present.

The phrase "essentially comprising" generally permits additional components that do not materially alter the basic and novel characteristics of the claimed film base. It is broader than "consisting of," but narrower than unrestricted "comprising." The scope will depend on the specification’s identification of the essential characteristics and the prosecution history.

A film based primarily on pullulan, maltodextrin, hydroxypropyl cellulose, polyethylene oxide, or another polymer may avoid literal infringement if HPMC is absent or not part of the film base. A formulation containing a small amount of HPMC as a secondary excipient could present a closer issue.

How strong is the patent estate for aripiprazole oral films?

The strength of U.S. Patent 9,694,008 is concentrated in formulation specificity rather than broad molecule or therapeutic claims.

Strength factor	Assessment
Chemical compound coverage	Weak or absent; the patent does not claim aripiprazole as a molecule
Dosage-form coverage	Strong for the claimed fast-dissolving film combination
Acid limitation	Narrow because citric acid is required
pH limitations	Narrow but potentially useful if supported by reproducible testing
Ratio limitation	Provides a measurable infringement boundary
Polymer limitation	Relevant only to dependent claim 4
Orange Book leverage	Likely limited unless the patent is listed for an approved film NDA
Generic tablet impact	Limited because conventional tablets do not meet the film limitation
Generic oral-film impact	More significant
Validity exposure	Potential obviousness and measurement-method challenges

The patent may be commercially valuable against a competing aripiprazole film, but it would not ordinarily block generic aripiprazole tablets or orally disintegrating tablets that lack the claimed film architecture.

What prior-art issues could affect validity?

The principal validity question is whether the claimed combination would have been obvious over prior art disclosing aripiprazole oral films, acidic taste-masking systems, HPMC film bases, and pH-controlled formulations.

Obviousness under 35 U.S.C. § 103

A challenger could combine references directed to:

• aripiprazole oral or buccal films;
• HPMC or HPMC/PVA film-forming matrices;
• citric acid as a taste modifier, salivary-pH modifier, or stabilizer;
• sucralose and acesulfame potassium as pharmaceutical sweeteners;
• controlled pH ranges in oral thin films.

The patentee’s strongest response would likely rely on the specific combination of:

• the narrow initial pH range;
• the distinct post-dissolution oral-cavity pH range;
• the aripiprazole-to-citric-acid ratio;
• acceptable taste, dissolution, stability, or bioavailability results.

Unexpected-results evidence would be important if the claimed pH and ratio produce a demonstrated benefit that would not have been predictable from the prior art.

Anticipation under 35 U.S.C. § 102

Anticipation would require one prior-art reference to disclose every claim 1 limitation, arranged as claimed. A reference that discloses aripiprazole film and citric acid but lacks the specified pH values would not anticipate claim 1.

Because the claim contains multiple numerical limitations, prior-art testing and examples become important. A broad prior-art disclosure may not anticipate a narrow numerical range unless the range is expressly disclosed or inherently present.

Indefiniteness and enablement

Potential disputes include:

• whether "orally fast dissolving" has a sufficiently definite meaning;
• how "when dissolved in an oral cavity" is measured;
• whether the pH range can be reproduced across patients and saliva conditions;
• whether the specification enables the full 2:1 to 66:1 ratio range;
• whether "essentially comprising" gives adequate notice regarding permitted polymer components.

The oral-cavity pH limitation is particularly sensitive because saliva composition, volume, flow rate, and measurement timing vary. A well-defined test method in the patent specification would improve enforceability.

When does U.S. Patent 9,694,008 expire?

U.S. Patent 9,694,008 was granted on May 9, 2017.[1] Its expiration date cannot be determined from the claim text alone. U.S. utility patents generally expire 20 years from the earliest effective nonprovisional filing date, subject to patent-term adjustment, patent-term extension, terminal disclaimers, and priority claims.[2]

The grant date is not the expiration date. A patent granted in 2017 can expire before or after 2033 depending on its earliest effective filing date and any term adjustments. The official patent record and USPTO Patent Examination Data System control the expiration analysis.[1,2]

The practical exclusivity assessment should separate:

1. patent term;
2. any terminal disclaimer;
3. patent-term adjustment;
4. FDA regulatory exclusivity for the product;
5. Orange Book listing status;
6. enforceability after maintenance-fee events.

What is the Orange Book status of U.S. Patent 9,694,008?

A patent is not automatically listed in the FDA Orange Book because it covers a pharmaceutical formulation. Listing depends on an approved NDA holder submitting the patent as one that claims the drug substance, drug product, or an approved method of use under FDA listing rules.[3]

The patent’s claim language is directed to an orally fast dissolving aripiprazole film. That scope is different from conventional Abilify aripiprazole tablets and orally disintegrating tablets. Unless an approved NDA specifically covers the claimed film formulation and the NDA holder submitted the patent for listing, the patent would not necessarily create an Orange Book Paragraph IV pathway against ordinary generic aripiprazole tablets.

A Paragraph IV certification becomes relevant if:

• the patent is listed against an approved product;
• an ANDA applicant seeks approval of a product covered by the listed claims;
• the applicant certifies that the patent is invalid, unenforceable, or will not be infringed;
• the NDA holder or patent owner files suit within the statutory period.

The patent could still be asserted in district court without Orange Book listing, but the ANDA-specific 30-month-stay framework would not automatically apply.

Which companies are challenging the patent?

No challenge, Paragraph IV filing, ANDA litigation, or settlement agreement can be established from the claim text supplied. U.S. Patent 9,694,008 should be checked in the USPTO Patent Center, PACER, the FDA Orange Book, and PTAB records for:

• inter partes review petitions;
• post-grant review activity;
• district-court infringement complaints;
• ANDA litigation;
• covenant-not-to-sue agreements;
• patent settlements;
• terminal disclaimers;
• ownership assignments.

The absence of an Orange Book listing would reduce the likelihood of an ANDA case tied specifically to this patent, but it would not eliminate a conventional patent dispute involving an oral-film product.

What generic launch risks exist for aripiprazole films?

A competing manufacturer can pursue several design-around strategies.

Design-around approach	Claim 1 impact	Main residual risk
Replace citric acid with another acid	Likely avoids literal infringement	Doctrine of equivalents
Set formulation pH outside 4.95-5.18	Avoids one express limitation	Testing variability and equivalents
Set dissolved oral pH outside 6.2-6.4	Avoids one express limitation	Oral-cavity measurement dispute
Use active-to-acid ratio below 2:1 or above 66:1	Avoids ratio limitation	Salt-equivalence calculation
Use a tablet rather than a film	Avoids dosage-form limitation	Product classification dispute
Use a non-HPMC film matrix	May avoid claim 4	Claim 1 remains potentially relevant
Omit one of the two named sweeteners	Avoids claim 3	Claims 1 and 2 may remain
Use a different aripiprazole salt	Not necessarily sufficient	Claim expressly covers salts

The cleanest design-around is usually a change to the acid system combined with a documented pH profile outside both claimed ranges. Changing only the sweetener system avoids claim 3 but leaves claim 1 and potentially claim 2 in play.

How does this patent compare with the core aripiprazole patent estate?

The aripiprazole landscape divides into four categories:

Patent category	Typical subject matter	Relevance to U.S. Patent 9,694,008
Compound patents	Aripiprazole molecule and related chemistry	Separate estate; not claimed here
Conventional drug-product patents	Tablets, orally disintegrating tablets, dosage strengths	May not reach fast-dissolving films
Method-of-use patents	Schizophrenia, bipolar disorder, adjunctive depression treatment	Not claimed here
Oral-film formulation patents	Film matrix, taste masking, pH, dissolution, excipients	Directly relevant

The patent is therefore a formulation-layer right. Its value depends on whether an approved or commercially viable aripiprazole product uses the claimed film design. It does not restore broad exclusivity for aripiprazole after expiration of the original compound patent.

What manufacturing and IP barriers matter?

The main manufacturing barrier is reproducible control of the claimed pH profile. A film manufacturer must control:

• citric-acid concentration;
• active-to-acid ratio;
• polymer hydration and mixing;
• drying temperature and residual moisture;
• film thickness;
• content uniformity;
• dissolution conditions;
• taste and mouthfeel;
• pH before and after dissolution.

These variables can affect both regulatory comparability and patent infringement analysis. A manufacturer may technically design around the claims but still face development problems if changing the acid or polymer alters dissolution, stability, palatability, or dose uniformity.

The patent’s manufacturing significance is greater for an oral-film applicant than for a conventional tablet applicant. Film products require specialized casting, drying, slitting, packaging, and moisture-control systems. Those process capabilities are not necessarily claimed by the patent, but they can create practical barriers to entry.

What is the likely litigation posture?

The strongest enforcement case would involve a competitor whose product:

• is an aripiprazole fast-dissolving film;
• uses citric acid;
• falls within the 4.95-to-5.18 formulation-pH range;
• produces a 6.2-to-6.4 dissolved oral pH;
• uses an active-to-acid ratio within 2:1 to 66:1.

Claims 2 through 4 would provide additional infringement positions only if the accused product also meets their narrower limitations. The patentee would likely seek formulation records, batch specifications, analytical methods, stability data, and samples to establish infringement.

A conventional aripiprazole tablet manufacturer presents a lower risk because the dosage-form limitation is central to claim 1. An oral-film manufacturer presents the highest risk, especially if it relies on the same HPMC, citric-acid, and sweetener architecture.

Key Takeaways

• U.S. Patent 9,694,008 is a narrow formulation patent for an aripiprazole orally fast dissolving film.
• Claim 1 requires citric acid, two pH ranges, a defined active-to-acid ratio, and a film dosage form.
• Claims 2 through 4 narrow the scope through citric-acid concentration, sucralose plus acesulfame potassium, and an HPMC-based film matrix.
• The patent does not claim aripiprazole generally, conventional tablets, or broad psychiatric treatment methods.
• The principal validity risks are obviousness, reproducibility of pH testing, oral-cavity measurement ambiguity, and enablement across the claimed ratio range.
• The principal design-around options are changing the acid, shifting one or both pH measurements, altering the ratio, or abandoning the film dosage form.
• Orange Book and Paragraph IV relevance depends on whether the patent is listed against an approved aripiprazole film NDA.
• The grant date was May 9, 2017, but the expiration date requires the patent’s priority and term-adjustment records.
• Commercial risk is concentrated in competing aripiprazole oral films, not ordinary generic aripiprazole tablets.

FAQs About U.S. Patent 9,694,008

Does U.S. Patent 9,694,008 cover Abilify tablets?

No. The asserted claims require an orally fast dissolving film. Conventional Abilify tablets generally do not satisfy that dosage-form limitation.

Can a product avoid the patent by using malic acid instead of citric acid?

A product using malic acid would not literally meet the express citric-acid limitation. Equivalence risk would depend on the patent’s prosecution history, the technical function of the acid, and the specific formulation.

Does using only sucralose avoid the patent?

It would likely avoid claim 3, which requires both sucralose and acesulfame potassium. It would not necessarily avoid claim 1 or claim 2.

Is a different aripiprazole salt outside the patent?

Not automatically. Claim 1 expressly covers aripiprazole and pharmaceutically acceptable salts. A different salt may remain within the claim if the other limitations are met.

Can the patent block a biosimilar or generic injection of aripiprazole?

The claims are directed to an oral film and would not ordinarily cover an injectable aripiprazole product. The relevant analysis would depend on the product’s dosage form and formulation.

References

1. United States Patent and Trademark Office. (2017). U.S. Patent No. 9,694,008, orally fast dissolving film formulation comprising aripiprazole.
2. United States Code, 35 U.S.C. §§ 154, 156.
3. U.S. Food and Drug Administration. (2023). Approved drug products with therapeutic equivalence evaluations, Orange Book. FDA.

Drugs Protected by US Patent 9,694,008

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Cmg Pharm Co Ltd	MEZOFY	aripiprazole	FILM;ORAL	211448-001	Apr 15, 2025		DISCN	Yes	No			Y
Cmg Pharm Co Ltd	MEZOFY	aripiprazole	FILM;ORAL	211448-002	Apr 15, 2025		DISCN	Yes	No			Y
Cmg Pharm Co Ltd	MEZOFY	aripiprazole	FILM;ORAL	211448-003	Apr 15, 2025		DISCN	Yes	No			Y

International Family Members for US Patent 9,694,008

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2883540
Spain	2636792
South Korea	101571670
South Korea	20140021141
World Intellectual Property Organization (WIPO)	2014025206