US Patent 10,149,843: Claim Scope, Orange Book Position, Exclusivity and Generic-Entry Risk

US Patent 10,149,843 protects a specific method of using a 4% cocaine hydrochloride nasal solution with absorbent pledgets before diagnostic procedures. Its core limitation is not cocaine hydrochloride alone. The claims require a defined formulation, nasal-septum administration, a treatment period of up to about 20 minutes, and a measured cocaine absorptivity factor of approximately 0.640 to 0.687 h⁻¹.

The patent is directed primarily to the clinical administration protocol associated with 4% cocaine hydrochloride nasal solution, including Numbrino. It does not, based on the claims provided, broadly claim every cocaine nasal formulation, every topical anesthetic, or every nasal diagnostic procedure.

What patent protects 4% cocaine hydrochloride nasal anesthesia?

US Patent 10,149,843 is a method patent covering topical nasal administration of an aqueous cocaine hydrochloride composition before diagnostic procedures involving the nasal or adjacent mucous membranes.[1]

Field	Patent 10,149,843
Patent number	US 10,149,843
Patent type	Utility patent
Issue date	December 11, 2018
Core subject	Nasal administration of 4% cocaine hydrochloride solution using absorbent articles
Primary dosage form	Aqueous topical nasal solution
Administration device	Absorbent articles, including pledgets and cottonoid pledgets
Required excipients	Citric acid and sodium benzoate within specified ranges
Key pharmacokinetic limitation	Cocaine absorptivity factor of approximately 0.640 to 0.687 h⁻¹
Primary procedures	Nasal endoscopy, laryngoscopy, transnasal esophagoscopy and nasal stroboscopy
Expected basic patent expiration	June 29, 2037, before any patent-term adjustment or extension
Commercial product most closely associated	Numbrino, cocaine hydrochloride nasal solution, 4%

The patent’s importance comes from the combination of formulation, delivery method and pharmacokinetic result. A competing product would need to avoid at least one required limitation to avoid literal infringement.

How broad are the independent claims?

Claims 1 and 9 are the principal independent claims. They overlap substantially but protect different commercial activities.

Claim 1: diagnostic-procedure method

Claim 1 requires:

A method for inducing local anesthesia.
A diagnostic procedure on, through or adjacent to a nasal mucous membrane.
A plurality of absorbent articles.
Soaking the articles in an aqueous solution containing:
- About 4% cocaine hydrochloride;
- More than 0% and less than about 0.150% citric acid; and
- About 0.07% to about 0.20% sodium benzoate.
Contacting the articles with the nasal mucous membrane against the septum.
Contact for up to about 20 minutes.
A resulting cocaine absorptivity factor from about 0.640 to about 0.687 h⁻¹.

The claim is cumulative. Omitting any required element may avoid literal infringement, although the doctrine of equivalents could remain relevant depending on the facts.

Claim 9: topical administration method

Claim 9 removes the diagnostic-procedure requirement and instead claims a method of administering the topical anesthetic composition. It retains the formulation, pledget-placement and absorptivity limitations.

This creates two infringement pathways:

A provider using the claimed method before a covered diagnostic procedure may implicate claim 1.
Administration of the claimed composition to the nasal mucosa may implicate claim 9 even when the procedure is not one of the expressly listed procedures in dependent claims 2 through 8.

The distinction matters in an ANDA case. A generic applicant may attempt to carve out diagnostic uses while still confronting the broader administration language in claim 9.

What formulation is required by US 10,149,843?

The claimed formulation is narrow in several respects.

Component	Claimed concentration
Cocaine hydrochloride	About 4% by weight
Citric acid	Greater than 0% to less than about 0.150% by weight
Sodium benzoate	About 0.07% to about 0.20% by weight
Vehicle	Aqueous solution

The claims do not claim a composition standing alone. They claim a method using the composition. The patent therefore does not automatically block all manufacture or sale of a 4% cocaine hydrochloride solution. The relevant conduct must be tied to the claimed administration method, or another unexamined claim in the patent family must provide separate composition or product protection.

The use of “about” gives the claim a potential numerical margin, but it does not make the boundaries unlimited. Courts generally assess “about” in light of the specification, prosecution history and technical context. The citric-acid limitation is asymmetric: it excludes zero and excludes concentrations at or above approximately 0.150%.

The sodium-benzoate range is broader than the citric-acid range. A formulation containing no sodium benzoate, or a concentration materially outside 0.07% to 0.20%, presents a stronger non-infringement position under the literal claim language. That position would still depend on whether other claims in the patent family cover the alternative formulation.

How does the absorptivity-factor limitation affect patent strength?

The absorptivity-factor limitation is the most technically distinctive element in the independent claims.

The claimed range is:

Lower boundary: about 0.640 h⁻¹
Upper boundary: about 0.687 h⁻¹

This limitation can strengthen patentability by tying the method to a defined pharmacokinetic outcome rather than merely reciting a known composition and route of administration. It also creates an evidentiary issue in litigation.

A patentee would need to establish that the accused method results in the claimed absorptivity factor. A generic manufacturer may challenge the claim by arguing that:

The factor is not inherent in the accused product or method.
The factor depends on patient-specific variables.
The clinical protocol does not reliably produce the claimed range.
The claim lacks sufficient measurement detail.
The accused product produces a result outside the claimed range.

The claim language uses “provided that the method results in,” making the pharmacokinetic result a condition of the claimed method. It is not merely a statement of intended use.

From a freedom-to-operate perspective, the factor is both a barrier and a potential attack point. It may be difficult for the patentee to prove in every patient, but a generic applicant cannot assume that lack of routine labeling data eliminates risk. Bioequivalence, clinical pharmacology and product-composition data may be used to establish inherency.

What procedures are protected by the dependent claims?

Claims 2 through 8 define specific procedural applications.

Claim	Procedure
2	Nasal endoscopy
3	Nasal endoscopy with debridement
4	Laryngoscopy
5	Nasal laryngoscopy
6	Nasopharyngeal laryngoscopy
7	Transnasal esophagoscopy
8	Nasal stroboscopy

These claims narrow claim 1 by identifying the diagnostic procedure. They may be useful against a provider or product label that expressly promotes one of these uses.

Claim 3 is particularly specific because it adds debridement to nasal endoscopy. A competitor avoiding debridement-related language would not necessarily avoid claim 1 or claim 2.

The dependent claims do not expand the patent beyond the limitations of claim 1. Each still requires the formulation, absorbent articles, nasal-septum contact, time limitation and absorptivity-factor result inherited from the parent claim.

What pledget and cottonoid limitations are protected?

Claims 10 through 14 address the absorbent articles used to administer the solution.

Claim	Additional limitation
10	Absorbent articles are pledgets
11	Four pledgets
12	Four pledgets soaked for at least 10 minutes before contact
13	Pledgets are cottonoid pledgets
14	Each cottonoid pledget retains up to 90% of the composition after removal from the nasal mucosa

Claim 11 is highly operational. It focuses on a four-pledget protocol. Claim 12 adds a pre-soaking period of at least 10 minutes, which may correspond to the commercial administration procedure.

Claim 14 raises a construction issue. “Retains up to 90%” ordinarily describes a maximum retention amount, not a minimum. The claim therefore appears to cover pledgets retaining no more than approximately 90% of the composition after removal. The specification and prosecution history would be important in determining whether the phrase was intended to mean “retains approximately 90%” or “retains up to 90%.”

The pledget claims are narrower than claim 9. A competing product administered by spray, atomizer, gel, swab or another non-pledget device could avoid claims 10 through 14, but would still need to assess claim 9.

When does US 10,149,843 lose exclusivity?

The ordinary 20-year patent term appears to run from the relevant nonprovisional filing date of June 29, 2017, producing an expected expiration date of June 29, 2037.[1] The effective date could change if the patent has patent-term adjustment or if the product receives patent-term extension under 35 U.S.C. § 156.

Event	Date
Earliest cited priority date	June 29, 2016
Relevant nonprovisional filing date	June 29, 2017
Patent issued	December 11, 2018
Expected basic expiration	June 29, 2037
Earliest ordinary entry point after basic patent expiration	June 30, 2037

A patent expiration date does not by itself establish the date when an ANDA product may launch. Regulatory exclusivity, other patents, pediatric exclusivity, litigation stays and settlement terms can change the commercial launch date.

The patent term also does not establish whether the patent is listed in the FDA Orange Book. Orange Book listing must be confirmed against the relevant reference-listed drug and current FDA listing data.[2]

What is the FDA regulatory status of the related product?

Numbrino is a 4% cocaine hydrochloride nasal solution approved by the FDA for the induction of local anesthesia of the mucous membranes of the nasal cavities before diagnostic procedures.[3]

FDA item	Information
Product	Numbrino
Active ingredient	Cocaine hydrochloride
Strength	4% nasal solution
Dosage form	Nasal solution administered with absorbent pledgets
NDA	211821
Approval date	January 14, 2020
Regulatory category	Prescription drug
Controlled-substance status	Cocaine is a Schedule II controlled substance
Principal clinical use	Local anesthesia before nasal diagnostic procedures

The approved product closely tracks the claim architecture of US 10,149,843: 4% cocaine hydrochloride, nasal mucosal administration, pledgets and diagnostic procedures. The FDA label is relevant to claim construction because it describes the approved administration method and procedural use, although labeling alone does not determine infringement.[3]

FDA approval does not confer patent rights. Conversely, a patent does not establish FDA approval. A generic applicant must satisfy both the Hatch-Waxman approval pathway and the relevant patent-certification requirements.

What is the Orange Book status of US 10,149,843?

The Orange Book identifies patents and exclusivity associated with approved drug products. For a listed patent to delay an ANDA launch, it generally must be listed against the relevant reference-listed drug and must fall within the FDA’s statutory listing framework.[2]

The principal Orange Book questions for this patent are:

Whether US 10,149,843 is listed against Numbrino.
Whether the listing covers the approved product, an approved method of use, or both.
Whether a use code corresponds to nasal anesthesia before diagnostic procedures.
Whether related patents are listed separately.
Whether any pediatric or patent-term extension modifies the practical exclusivity date.

The claims supplied are method claims rather than composition claims. That distinction makes the use-code description important. An ANDA applicant may attempt a section viii statement and omit a patented method of use from its labeling. Whether that strategy works depends on the exact Orange Book use code and the scope of the approved label.

What Paragraph IV challenges could target the patent?

A Paragraph IV certification could challenge US 10,149,843 on invalidity, non-infringement or both.[4]

Likely non-infringement theories

A generic applicant could attempt to avoid the claims by:

Using a cocaine hydrochloride concentration materially outside approximately 4%.
Omitting citric acid.
Using citric acid at or above the claimed upper range.
Using sodium benzoate outside the claimed range or omitting it.
Using a delivery system other than multiple absorbent articles.
Avoiding contact against the septum.
Using a treatment duration outside the claimed “up to about 20 minutes.”
Demonstrating an absorptivity factor outside the claimed range.
Omitting the patented diagnostic use from the label where permitted.
Using a formulation that does not retain the claimed amount on cottonoid pledgets.

These strategies are not equally strong. A label carve-out may avoid a method-of-use claim, but it may not avoid an independent administration claim that is broad enough to cover the remaining labeled use.

Likely invalidity theories

Potential invalidity arguments could address:

Anticipation by an earlier cocaine nasal-anesthesia protocol.
Obviousness based on known cocaine hydrochloride nasal solutions, preservatives and pledget administration.
Written-description support for the exact absorptivity-factor range.
Enablement of patient-specific absorption results.
Definiteness of “about,” “up to,” “against a septum” and “retains up to 90%.”
Patent-term or priority issues, if the effective filing history does not support the claimed subject matter.

The absorptivity-factor limitation may be central to both sides. The patentee may argue that it reflects a clinically relevant, reproducible pharmacokinetic profile. The challenger may argue that the range is an inherent result of routine formulation and administration or that the specification does not enable the full range without undue experimentation.

Which companies are challenging the patent?

The supplied claim text does not identify an ANDA filer, Paragraph IV notice, district-court action, settlement or license. No company-specific challenge can be attributed reliably from the claims alone.

The likely competitive set is limited because cocaine hydrochloride is a Schedule II controlled substance and the product has a specialized procedural market. A generic competitor would need to address:

Controlled-substance registration and quotas.
DEA security and recordkeeping requirements.
FDA approval of the nasal product.
Bioequivalence and local tolerability.
Pledget administration and delivery reproducibility.
Orange Book patent certifications.
Potential method-of-use litigation.

The absence of a publicly identified challenger in the supplied record should not be treated as evidence that no Paragraph IV filing exists. ANDA litigation can arise after FDA acceptance of a certification and may involve confidential commercial timing before a launch becomes visible.

How strong is the patent estate for Numbrino?

US 10,149,843 is commercially meaningful but technically narrow.

Strength factor	Assessment
Product alignment	Strong; the claims closely track a 4% cocaine nasal solution and pledget protocol
Formulation breadth	Moderate to weak; concentration and excipient ranges are specific
Delivery-method coverage	Strong for multiple pledget administration
Alternative delivery coverage	Limited on the claims supplied
Diagnostic-use coverage	Broad in claim 1, with specific procedural fallbacks in claims 2-8
Pharmacokinetic limitation	Potentially strong for differentiation, but difficult to prove
Design-around potential	Material
Generic litigation risk	Moderate to high if the generic copies the labeled formulation and pledget method
Composition-only protection	Not established by the claims supplied
Manufacturing protection	Not established by the claims supplied

The estate is strongest against a product that copies the approved formulation and administration instructions. It is weaker against a redesigned formulation, an alternative delivery system or a product with a non-infringing label, assuming no related patent covers those alternatives.

What manufacturing and intellectual-property barriers affect generic entry?

The principal barriers are regulatory and operational as well as patent-based.

Controlled-substance manufacturing

Cocaine hydrochloride is a Schedule II controlled substance. A manufacturer must comply with DEA registration, procurement quotas, inventory controls, physical security, recordkeeping and distribution restrictions.[5]

Formulation reproducibility

A generic product must reproduce the relevant pharmaceutical characteristics of the reference product while managing:

Cocaine hydrochloride concentration.
Solution pH.
Citric-acid level.
Sodium-benzoate level.
Container and closure compatibility.
Pledget loading.
Pledget retention and release.
Nasal tolerability.
Stability and preservative performance.

Local-delivery equivalence

Systemic bioequivalence alone may not resolve all product risks. The claimed absorptivity factor suggests that the delivery protocol affects cocaine uptake. A generic applicant may therefore face technical questions about dose retention, contact time, nasal placement and variability between pledgets.

Manufacturing-method exposure

The claims supplied do not recite a manufacturing process. They do, however, create potential exposure based on how the finished product is administered. A manufacturer that produces a product with a different manufacturing process may still face infringement if its customers use the product in the claimed manner.

How does US 10,149,843 compare with a conventional generic nasal anesthetic?

Issue	Claimed cocaine nasal method	Conventional nasal anesthetic
Active ingredient	Cocaine hydrochloride	May use lidocaine, tetracaine or another anesthetic
Controlled substance	Yes	Usually no
Delivery	Multiple absorbent articles	Spray, gel, pledget or other device
Formulation	4% cocaine HCl with defined excipients	Varies
Pharmacokinetic limitation	Required absorptivity-factor range	Usually absent
Procedural use	Nasal diagnostic procedures	Broad topical anesthesia
DEA controls	Applicable	Usually not applicable
Patent risk under US 10,149,843	High if copied closely	Low if cocaine-free

A product using lidocaine or another non-cocaine anesthetic would not literally satisfy the cocaine hydrochloride limitation in the supplied claims. Such a product could still compete clinically but would not be a direct generic substitute for Numbrino under the same active ingredient.

What is the commercial exposure if generic entry occurs?

The commercial exposure is concentrated in office-based and hospital diagnostic procedures that use topical nasal anesthesia. The relevant market is narrower than the market for general local anesthetics because the product contains cocaine and requires controlled-substance handling.

A generic launch could affect:

Product price.
Hospital purchasing contracts.
Ambulatory surgery and ENT procedure economics.
Physician preference for premeasured administration.
Distribution margins.
Controlled-substance inventory management.

The patent risk is highest for an ANDA product that copies the Numbrino label, formulation and four-pledget administration process. A label carve-out or alternate delivery design could reduce risk, but the independent administration claim remains a key obstacle.

What licensing deals or settlements affect this patent?

No licensing agreement, covenant not to sue or settlement can be established from the claim language supplied. The commercial relationship between the patent owner, NDA sponsor and manufacturer should not be assumed to be a third-party license without assignment, licensing or corporate transaction records.

For diligence, the decisive documents are:

USPTO assignment records.
FDA Orange Book listing history.
Paragraph IV notice letters.
District-court complaints and docket orders.
Settlement agreements filed under the Medicare Modernization Act.
SEC disclosures by publicly traded parties.
DEA and FDA manufacturing records where publicly available.

Key Takeaways

US 10,149,843 is a method patent, not a broad claim to cocaine hydrochloride itself.
The independent claims require a 4% aqueous cocaine hydrochloride solution with defined citric-acid and sodium-benzoate ranges.
The method requires multiple absorbent articles contacting the nasal mucosa against the septum.
The claims also require an absorptivity factor of approximately 0.640 to 0.687 h⁻¹.
Dependent claims cover nasal endoscopy, debridement, laryngoscopy, transnasal esophagoscopy, nasal stroboscopy and pledget-specific protocols.
Claims 10 through 14 narrow the delivery method to pledgets, four pledgets, pre-soaking and cottonoid retention.
The expected basic expiration date is June 29, 2037, subject to patent-term adjustment, extension and any separate patent rights.
Generic risk is highest for a product that copies Numbrino’s formulation, pledget protocol and labeled diagnostic uses.
A reformulated or non-pledget product may have meaningful design-around arguments, but the independent administration claim must still be analyzed.
The supplied record does not establish a specific Paragraph IV challenger, litigation outcome, settlement or licensing arrangement.

FAQs

Does US 10,149,843 claim cocaine hydrochloride nasal solution by itself?

No. The claims supplied are method claims. They require use of the solution in a specified nasal administration process.

Can a generic avoid the patent by using a nasal spray?

Potentially, but not automatically. A spray may avoid the absorbent-article and pledget limitations, while claim 9 and any related patent claims would require separate analysis.

Does omitting citric acid avoid infringement?

It may avoid literal infringement of the supplied claims because the claims require more than 0% citric acid. Other patents or the doctrine of equivalents could alter the analysis.

Is a 4% cocaine hydrochloride product automatically blocked until 2037?

No. The patent does not automatically block every 4% cocaine hydrochloride product. Infringement depends on the product’s formulation, administration method, labeling and resulting pharmacokinetic profile.

Can a generic launch before June 2037 with a Paragraph IV certification?

Potentially. A Paragraph IV certification can support an early challenge based on invalidity or non-infringement. Litigation, regulatory exclusivity, settlements and other patents may determine the actual launch date.

References

United States Patent and Trademark Office. (2018). US Patent No. 10,149,843, methods of administering cocaine hydrochloride.
U.S. Food and Drug Administration. (2024). Approved drug products with therapeutic equivalence evaluations: Orange Book.
U.S. Food and Drug Administration. (2020). Numbrino (cocaine hydrochloride) nasal solution prescribing information.
U.S. Food and Drug Administration. (2024). Abbreviated new drug application approvals and patent certifications under the Hatch-Waxman Act.
U.S. Drug Enforcement Administration. (2024). Controlled substances schedules and requirements for Schedule II manufacturers.

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Lxo Ireland	GOPRELTO	cocaine hydrochloride	SOLUTION;NASAL	209963-001	Dec 14, 2017		RX	Yes	Yes	⤷ Start Trial	⤷ Start Trial				METHOD OF ADMINISTERING A LOCAL ANESTHETIC TO THE MUCOUS MEMBRANES	⤷ Start Trial
Lxo Ireland	GOPRELTO	cocaine hydrochloride	SOLUTION;NASAL	209963-001	Dec 14, 2017		RX	Yes	Yes	⤷ Start Trial	⤷ Start Trial				METHOD FOR THE INDUCTION OF LOCAL ANESTHESIA PRIOR TO PERFORMING A PROCEDURE ON, THROUGH, OR ADJACENT TO THE MUCOUS MEMBRANES	⤷ Start Trial
Omnivium Pharms	NUMBRINO	cocaine hydrochloride	SOLUTION;NASAL	209575-001	Jan 10, 2020		RX	Yes	Yes	⤷ Start Trial	⤷ Start Trial				METHOD FOR THE INDUCTION OF LOCAL ANESTHESIA PRIOR TO PERFORMING A PROCEDURE ON, THROUGH, OR ADJACENT TO THE MUCOUS MEMBRANES	⤷ Start Trial
Omnivium Pharms	NUMBRINO	cocaine hydrochloride	SOLUTION;NASAL	209575-001	Jan 10, 2020		RX	Yes	Yes	⤷ Start Trial	⤷ Start Trial				METHOD OF ADMINISTERING A LOCAL ANESTHETIC TO THE MUCOUS MEMBRANES	⤷ Start Trial
>Applicant	>Tradename	>Generic Name	>Dosage	>NDA	>Approval Date	>TE	>Type	>RLD	>RS	>Patent No.	>Patent Expiration	>Product	>Substance	>Delist Req.	>Patented / Exclusive Use	>Submissiondate

Details for Patent: 10,149,843

Which drugs does patent 10,149,843 protect, and when does it expire?

Summary for Patent: 10,149,843