Details for Patent: 7,977,045
Summary for Patent: 7,977,045
| Title: | Aqueous-based pharmaceutical composition | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Abstract: | An aqueous pharmaceutical composition which is capable of being sprayed into the nasal cavity of an individual and which comprises: (A) a pharmaceutically effective amount of solid particles of medicament which is effective in treating a bodily condition by virtue of its being present on the mucosal surfaces of the nasal cavity; and (B) a suspending agent in an amount effective to maintain said particles dispersed uniformly in the composition and to impart to the composition the following thixotropic properties: (i) the viscosity of the position in unsheared form is relatively high, with the composition being in gel-like form; (ii) as the composition is subjected to shear (shaken) in preparation for spraying, the viscosity of the composition becomes relatively low and such that the composition in the form of a mist flows readily into the nasal passages for deposit on the mucosal surfaces of the nasal cavity; and (D) in deposited form on the mucosal surfaces, the viscosity of the composition is relatively high and such that it resists being cleared from the mucosal surfaces by the inherent mucocillary forces which are present in the nasal cavity, a method of use of the composition and a method for preparation of the composition, including in preferred form the use of anti-inflammatory steroid, for example, triamcinolone acetonide, and an odorless form of the composition. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Inventor(s): | Soo-Il Kim | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Assignee: | Aventis Pharmaceuticals Inc | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Application Number: | US12/728,984 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Patent Claim Types: see list of patent claims | Use; Composition; Formulation; Process; | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Patent landscape, scope, and claims: | U.S. Patent 7,977,045: Claim Scope, Expiration, Orange Book Status and Nasal Triamcinolone Patent LandscapeU.S. Patent No. 7,977,045 covers a propellant-free, thixotropic nasal suspension containing micronized triamcinolone acetonide. Its core invention combines three elements: uniform suspension of solid drug particles, shear-thinning behavior during spraying, and higher viscosity after deposition to resist mucociliary clearance. The patent also claims a specific formulation, manufacturing sequence, and precompression-pump package. The patent’s practical commercial value was concentrated in the Nasacort AQ-type formulation. The patent is no longer an effective blocking right if its earliest nonprovisional priority was in 1997, because the ordinary U.S. patent term would have ended in 2017, subject to any patent-term adjustment. Its claims remain relevant for historical freedom-to-operate analysis, validity review, and formulation know-how, but they do not create a current U.S. barrier to generic triamcinolone acetonide nasal products. [1–4] What drug and formulation does U.S. Patent 7,977,045 protect?The patent protects a nasal delivery platform for triamcinolone acetonide rather than the molecule itself. The covered product is an aqueous suspension of micronized solid particles administered by nasal spray. The claimed formulation has the following functional profile:
The claims target the delivery system’s rheology. They do not claim a new chemical form of triamcinolone acetonide, a new therapeutic mechanism, or a new indication independent of the nasal formulation. How many independent claims does Patent 7,977,045 have?The patent has five principal independent claims: claims 1, 7, 12, 16 and 17.
Claims 2 through 6 narrow claim 1. Claims 8 through 11 narrow claim 7. Claims 13 through 15 narrow claim 12. The strongest practical claim is likely claim 16 because it recites a defined formulation. The broadest product-oriented claim is claim 7, although its functional viscosity limitations create infringement and validity questions. Claim 17 is directed to a commercial package rather than the formulation alone. What does claim 1 require?Claim 1 requires all of the following elements:
The claim is geographically demanding inside the nasal cavity. It identifies the anterior nose, frontal sinus, maxillary sinuses and mucosa overlying the turbinates and conchas. A challenger could contest whether a commercial spray deposits pharmaceutically effective amounts on every recited region. The claim also includes a retention requirement. A product that delivers triamcinolone acetonide but clears rapidly from the nasal mucosa may fall outside the claim if the retention limitation is not met. What does “consisting essentially of” mean in the claims?Claims 1, 4, 5 and related dependent claims use “consisting essentially of.” That language generally permits ingredients that do not materially alter the basic and novel characteristics of the claimed formulation. The basic characteristics here are likely uniform particle suspension, shear-thinning sprayability, mucosal deposition and retention. An accused formulation containing additional excipients would not automatically avoid infringement. The analysis would focus on whether the additional ingredient materially changes the claimed rheological and delivery properties. What formulations are protected by claims 7 through 11?Claims 7 through 11 protect the formulation’s thixotropic behavior. Claim 7 requires:
Claims 8 and 11 provide numerical viscosity ranges, but the claim text presents the ranges in different orientations:
This creates a drafting and construction issue. Claims 3 and 11 should be read with the specification’s definitions of “shear viscosity” and “setting viscosity.” If the patent specification uses those terms in the opposite sense from ordinary rheological terminology, the specification may control the interpretation. The inconsistency could affect infringement analysis and provide an indefiniteness or claim-construction argument, depending on the intrinsic record. [1, 5] The formulation claims are narrower than a generic claim to any aqueous triamcinolone nasal spray. A competing product could potentially avoid them by using:
What is the significance of claim 16?Claim 16 recites a near-commercial formulation:
Claim 16 is potentially important for historical product comparison because it identifies exact excipient concentrations. It is also easier to design around than a functional claim. A formulation with a different concentration, different suspending polymer, or different preservative system could avoid literal infringement, subject to equivalents analysis. The claim contains an apparent drafting ambiguity concerning the benzalkonium chloride solution. If the stated 0.03 wt% refers to the commercial 50% solution, the active benzalkonium chloride concentration is approximately 0.015 wt%. If it refers to active benzalkonium chloride, the formulation is materially different. The specification and prosecution history would control that issue. What does claim 17 protect?Claim 17 covers an article of manufacture comprising:
Claim 17 is commercially significant because it links the formulation to the container and delivery system. It does not require the narrower pH of claim 16 or the exact weight percentages in claim 16. It therefore provides broader package-level coverage, although every listed component remains required. A formulation manufacturer that sells the composition in bulk without the claimed vessel and pump may not practice claim 17, but could still implicate claims 7, 12 or 16. What manufacturing process is protected by claim 12?Claim 12 covers a specific order of operations:
Claim 13 narrows the process by requiring the particle suspension to be introduced into the bottom of the thixotropic suspension. Claim 14 adds a hydrophilic nonionic surfactant, a quaternary ammonium antimicrobial, EDTA and an anti-osmotic agent. Claim 15 specifies Polysorbate-type surfactant chemistry, benzalkonium chloride, EDTA and dextrose. These claims create a manufacturing-process barrier only if the accused manufacturer follows the claimed sequence. The final product alone may not prove infringement of the process claims. Manufacturing records, batch instructions, equipment configuration and process validation documents would be central evidence. When did U.S. Patent 7,977,045 lose exclusivity?The ordinary U.S. patent term is 20 years from the earliest effective nonprovisional filing date, subject to patent-term adjustment, patent-term extension and terminal disclaimers. [2, 3] For Patent 7,977,045, the relevant priority framework places the ordinary term in the 2017 period. On that basis, the patent is expired and cannot support a current U.S. injunction against a generic triamcinolone acetonide nasal spray.
A patent-term adjustment could move the endpoint later, but it would not ordinarily move a 1997-based patent into the current decade. Patent expiration removes the exclusionary right, although it does not erase the patent’s relevance to historical litigation, licensing, or prior-art analysis. What is the Orange Book status of Patent 7,977,045?Orange Book relevance depends on whether the patent was submitted for listing against the applicable approved drug application and whether its listing remained active during the relevant period. Patent 7,977,045 is associated with the triamcinolone acetonide nasal-suspension product technology historically commercialized as Nasacort AQ, but the claims alone do not establish the precise FDA listing history. For Hatch-Waxman purposes, an Orange Book-listed drug patent can support a Paragraph IV notice and patent litigation under 21 U.S.C. § 355(j). Once the patent expires, it cannot support a prospective patent bar to ANDA approval. [4, 6] The regulatory landscape differs from the patent landscape:
Were Paragraph IV challenges and generic-entry risks significant?The principal generic-entry risk concerned products seeking approval after the expiration of formulation and product patents associated with triamcinolone acetonide nasal spray. A Paragraph IV challenge would have focused on one or more of the following:
The strongest noninfringement pathway is a product that does not contain the claimed suspension system or does not have the claimed viscosity transition. The strongest validity pathway is prior art showing an aqueous nasal suspension with triamcinolone acetonide, cellulose-based thixotropy, benzalkonium chloride, EDTA and a pump dispenser. Because the patent is expired, a new ANDA filer no longer faces a current statutory stay based solely on this patent. Any historical Paragraph IV case or settlement would need to be evaluated against the patent’s term and the date of the generic filing. How strong is the patent estate for triamcinolone acetonide nasal spray?The estate was technically focused but commercially important during its term.
The method claims are vulnerable to factual disputes because they require deposition in multiple nasal regions and retention for at least approximately one hour. The composition claims are more practical for enforcement because they focus on ingredients and rheological properties that can be tested, although the viscosity terminology introduces construction risk. How does Patent 7,977,045 compare with competing nasal corticosteroid patents?Patent 7,977,045 differs from many nasal corticosteroid patents because it emphasizes formulation mechanics rather than only the corticosteroid, indication or dose.
A competitor using fluticasone propionate, mometasone furoate, budesonide or beclomethasone would generally not infringe the claims because the claims require triamcinolone acetonide. A competitor using triamcinolone acetonide in a materially different nasal dosage form could avoid the principal formulation claims. What licensing and litigation issues matter?The claims indicate a product-development and lifecycle-management strategy centered on a branded nasal suspension. Commercial licensing analysis would focus on:
A patent assignment or license would not transfer FDA approval, manufacturing authorization or bioequivalence data unless those rights were separately documented. Patent expiration also does not eliminate confidentiality obligations covering manufacturing know-how. No current infringement risk can be inferred from the claim text alone. The relevant question for a present-day product is whether it practices any unexpired continuation, divisional, reissue or related patent with materially overlapping claims. Patent 7,977,045 itself is not a current blocking patent under the ordinary term calculation. What geographic coverage does the patent provide?Patent 7,977,045 provides U.S. rights only. It does not establish protection in Europe, Canada, Japan, China or other markets. International protection would depend on corresponding national patents and their individual expiration dates. A multinational launch therefore requires separate review of:
The U.S. expiration date cannot be used as a proxy for foreign expiration dates. Key Takeaways
FAQsDoes Patent 7,977,045 cover all triamcinolone acetonide nasal sprays?No. It targets specified aqueous suspension, rheology, excipient, deposition, manufacturing and packaging features. A materially different triamcinolone nasal formulation may fall outside the claims. Can a generic use triamcinolone acetonide after the patent expires?Yes. Patent expiration removes the patent-based exclusion, but the generic must still satisfy FDA requirements for the applicable abbreviated or full approval pathway. Is a triamcinolone acetonide solution covered by claim 7?Probably not literally, because claim 7 requires solid particles of triamcinolone acetonide. A solution could still raise other patent issues, but it would not meet that express limitation. Does changing benzalkonium chloride avoid the entire patent?No. It may avoid dependent claims requiring benzalkonium chloride, but broader claims do not necessarily require that preservative. The full claim set must be analyzed. Does the patent protect the precompression pump by itself?No. Claim 17 requires the pump to be associated with the specified triamcinolone-containing composition and vessel. The claim is not a standalone pump patent. References
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Drugs Protected by US Patent 7,977,045
| Applicant | Tradename | Generic Name | Dosage | NDA | Approval Date | TE | Type | RLD | RS | Patent No. | Patent Expiration | Product | Substance | Delist Req. | Patented / Exclusive Use | Submissiondate |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| >Applicant | >Tradename | >Generic Name | >Dosage | >NDA | >Approval Date | >TE | >Type | >RLD | >RS | >Patent No. | >Patent Expiration | >Product | >Substance | >Delist Req. | >Patented / Exclusive Use | >Submissiondate |
International Family Members for US Patent 7,977,045
| Country | Patent Number | Estimated Expiration | Supplementary Protection Certificate | SPC Country | SPC Expiration |
|---|---|---|---|---|---|
| African Regional IP Organization (ARIPO) | 1045 | ⤷ Start Trial | |||
| African Regional IP Organization (ARIPO) | 9901495 | ⤷ Start Trial | |||
| Austria | 250432 | ⤷ Start Trial | |||
| >Country | >Patent Number | >Estimated Expiration | >Supplementary Protection Certificate | >SPC Country | >SPC Expiration |
