# US 2013/0158074 A1 · Small volume oral transmucosal dosage forms containing sufentanil for treatment of pain

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- Number: US 2013/0158074 A1
- Document ID: US20130158074A1
- Status: Published application
- Kind: A1
- Application number: 13/555,948
- Filed: 2012-07-23
- Published: 2013-06-20
- Earliest claimed: 2006-01-06
- Assignees: AcelRx Pharmaceuticals, Inc.
- Inventors: Pamela Palmer; Thomas Schreck; Stelios Tzannis; Larry Hamel; Andrew I. Poutiatine; Charles Rampersaud; Bruce Edwards
- Web page: https://patentgrep.com/patent/US20130158074A1

## CPC

- A61K 9/20: Pills, tablets, {discs, rods (A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095)}
- A61J 7/0038: {Straws}
- A61J 7/0053: {Syringes, pipettes or oral dispensers}
- A61J 7/0481: {working on a schedule basis}
- A61K 9/006: {Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays}
- A61K 9/2009: {Inorganic compounds}
- A61K 9/2018: {Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates}
- A61K 9/2031: {obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers}
- A61K 9/2072: {characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms (A61K9/0004, A61K9/0056, A61K9/0065 take precedence)}
- A61K 31/4535: containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
- A61M 15/00: Inhalators {(drug delivery in endotracheal tubes A61M16/04)}
- A61M 15/008: {Electronic counters}
- A61M 15/0081: {Locking means}
- A61M 15/0083: {Timers}
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/04: Centrally acting analgesics, e.g. opioids
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- G07F 17/0092: {for assembling and dispensing of pharmaceutical articles (medical dispensers for private use, A61J7/00)}
- H01Q 1/2208: {associated with components used in interrogation type services, i.e. in systems for information exchange between an interrogator/reader and a tag/transponder, e.g. in Radio Frequency Identification [RFID] systems (methods or arrangements for sensing record carriers, e.g. for reading patterns G06K7/00; record carrier for use with machines and with at least a part designed to carry digital markings G06K19/00)}
- A61J 7/0418: {with electronic history memory}
- A61J 7/0445: {for preventing drug dispensing during a predetermined time period}
- A61J 2200/30: Compliance analysis for taking medication
- A61M 2205/276: preventing unwanted use
- A61M 2205/3561: local, e.g. within room or hospital
- A61M 2205/3584: using modem, internet or Bluetooth®
- A61M 2205/3592: using telemetric means, e.g. radio or optical transmission
- A61M 2205/52: with memories providing a history of measured variating parameters of apparatus or patient
- A61M 2205/583: by visual feedback
- A61M 2205/6054: Magnetic identification systems
- A61M 2205/609: Biometric patient identification means
- A61M 2209/086: Docking stations
- G07C 9/22: in combination with an identity check of the pass holder
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61J: CONTAINERS SPECIALLY ADAPTED FOR MEDICAL OR PHARMACEUTICAL PURPOSES; DEVICES OR METHODS SPECIALLY ADAPTED FOR BRINGING PHARMACEUTICAL PRODUCTS INTO PARTICULAR PHYSICAL OR ADMINISTERING FORMS; DEVICES FOR ADMINISTERING FOOD OR MEDICINES ORALLY; BABY COMFORTERS; DEVICES FOR RECEIVING SPITTLE
- A61M: DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY (introducing media into or onto the bodies of animals A61D7/00; means for inserting tampons A61F13/26; devices for administering food or medicines orally A61J; containers for collecting, storing or administering blood or medical fluids A61J1/05); DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY (surgery A61B; chemical aspects of surgical articles A61L); DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR {(Electrotherapy, e.g. producing anaesthesia by the use of alternating or intermittent currents A61N1/36021)}
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- G07F: COIN-FREED OR LIKE APPARATUS (coin sorting G07D3/00; coin testing G07D5/00; {handling coins or paper currencies apart from payment activated apparatus G07D; payment architectures, schemes or protocols G06Q20/00})
- H01Q: ANTENNAS, i.e. RADIO AERIALS (radiators or antennas for microwave heating H05B6/72)
- G07C: TIME OR ATTENDANCE REGISTERS; REGISTERING OR INDICATING THE WORKING OF MACHINES; GENERATING RANDOM NUMBERS; VOTING OR LOTTERY APPARATUS; ARRANGEMENTS, SYSTEMS OR APPARATUS FOR CHECKING NOT PROVIDED FOR ELSEWHERE

## Abstract

Compositions, methods and systems for administration of small volume sufentanil-containing drug dosage forms to the oral mucosa of a subject are disclosed.

## Claims

### Claim at position 1

1-63. (canceled)

### Claim 64

A method of treating pain in a subject, comprising administering a dosage form to the oral mucosa of a subject, wherein said dosage form comprises:
from about 5 to about 100 micrograms (mcg) of sufentanil, and a bioadhesive material, wherein:
(i) said bioadhesive material adheres the dosage form to the oral mucosa of said subject during the period of drug delivery;
(ii) said dosage form has a volume of less than 30 microliters or a mass of less than 30 mg; and
(iii) after administration of said dosage form to said subject, said dosage form provides a minimal saliva response and minimal swallowing of sufentanil;
at least 55% of drug delivery of sufentanil occurs via the oral transmucosal route;
said dosage form provides a dose-normalized mean Cmax of 1.59-2.75 pg/mL per mcg dosed;
said dosage form provides a Tmax of from about 19.8 minutes to about 60 minutes; and
said dosage form provides a Tmax with a coefficient of variation of less than 40%.

### Claim 65 (depends on 64)

The method according to claim 64, wherein said dosage form comprises a dose of sufentanil selected from the group consisting of 5 mcg, 10 mcg, 15 mcg, 20 mcg, 30 mcg, 40 mcg, 50 mcg, 60 mcg, 70 mcg, 80 mcg and 100 mcg.

### Claim 66 (depends on 64)

The method according to claim 64, wherein said dosage form has a mass of less than 10 mg or a volume of less than 10 μl.

### Claim 67 (depends on 64)

The method according to claim 64, wherein said oral transmucosal administration is sublingual or buccal administration.

### Claim 68 (depends on 64)

The method according to claim 64, wherein said dosage form has an erosion time of from 30 seconds up to a time selected from the group consisting of 5 minutes, 10 minutes, 15 minutes and 30 minutes.

### Claim 69 (depends on 67)

The method according to claim 67, wherein said dosage form delivers at least 60% of the total amount of sufentanil in said dosage form via the sublingual route.

### Claim 70 (depends on 67)

The method according to claim 67, wherein a single sublingual administration of said dosage form to a subject results in a bioavailability of sufentanil of greater than 50%.

### Claim 71 (depends on 67)

The method according to claim 67, wherein a single sublingual administration of said dosage form to a subject results in a bioavailability of sufentanil of greater than 60%.

### Claim 72 (depends on 67)

The method according to claim 67, wherein a single sublingual administration of said dosage form to a subject results in a bioavailability of sufentanil of greater than 70%.

### Claim 73 (depends on 67)

The method according to claim 67, wherein the bioavailability of sufentanil following repeated sublingual administrations of said dosage form to a subject, is greater than the bioavailability of sufentanil following a single sublingual administration to said subject.

### Claim 74 (depends on 64)

The method according to claim 64, wherein said dosage form is selected from the group consisting of a lozenge, a pill, a tablet, a membrane and a strip.

### Claim 75 (depends on 74)

The method according to claim 74, wherein said dosage form is a tablet.

### Claim 76 (depends on 64)

The method according to claim 64, wherein said pain is acute pain, breakthrough pain or post-operative pain.

### Claim 77 (depends on 76)

The method according to claim 76, wherein said pain is acute inpatient pain.

### Claim 78 (depends on 76)

The method according to claim 76, wherein said pain is post-operative pain.