# US 10,245,228 B2 · Small volume oral transmucosal dosage forms containing sufentanil for treatment of pain

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- Number: US 10,245,228 B2
- Document ID: US10245228B2
- Status: Granted
- Kind: B2
- Application number: 15/655,316
- Filed: 2017-07-20
- Published: 2018-06-14
- Granted: 2019-04-02
- Earliest claimed: 2006-01-06
- Assignees: AcelRx Pharmaceuticals, Inc.
- Applicants: AcelRx Pharmaceuticals, Inc.
- Inventors: Pamela Palmer; Thomas Schreck; Stelios Tzannis; Larry Hamel; Andrew I. Poutiatine
- Web page: https://patentgrep.com/patent/US10245228B2

## CPC

- 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 9/7007: {Drug-containing films, membranes or sheets (A61K9/0041, A61K9/0043, A61K9/006, A61K9/0063 take precedence)}
- A61K 31/4535: containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
- 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]
- G16H 20/10: relating to drugs or medications, e.g. for ensuring correct administration to patients
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- G16H: HEALTHCARE INFORMATICS, i.e. INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR THE HANDLING OR PROCESSING OF MEDICAL OR HEALTHCARE DATA

## Abstract

Compositions, systems and methods for administration of small volume sufentanil drug dosage forms to the sublingual mucosa of a subject for treatment of pain using a device are disclosed.

## Claims

### Claim 1

A dosage form for oral transmucosal administration to a subject, comprising: from 5.0 micrograms to 100 micrograms sufentanil, wherein said dosage form is bioadhesive and has a volume of less than 30 microliters or a mass of less than 30 mg, wherein the administration of the dosage form to the subject provides a Tmax with a coefficient of variation less than 40%.

### Claim 2 (depends on 1)

The dosage form of claim 1, wherein the dosage form has a volume of less than 10 microliters or a mass of less than 10 mg.

### Claim 3 (depends on 1)

The dosage form of claim 1, wherein after administration of the dosage form to the subject, at least 50% of the drug delivery of sufentanil occurs via the oral transmucosal route.

### Claim 4 (depends on 3)

The dosage form of claim 3, wherein after administration of the dosage form to the subject, at least 55% of the drug delivery of sufentanil occurs via the oral transmucosal route.

### Claim 5 (depends on 3)

The dosage form of claim 3, wherein after administration of the dosage form to the subject, at least 60% of the drug delivery of sufentanil occurs via the oral transmucosal route.

### Claim 6 (depends on 1)

The dosage form of claim 1, wherein after administration of the dosage form to the subject, the dosage form provides a Tmax of from about 19.8 minutes to about 60 minutes.

### Claim 7 (depends on 1)

The dosage form of claim 1, wherein after administration of the dosage form to the subject results in a dose-normalized Cmax of about 2.72+/−0.84 pg/mL per mcg dosed.

### Claim 8 (depends on 1)

The dosage form of claim 1, wherein after administration of the dosage form to the subject, the dosage form provides a Tmax of from about 19.8 minutes to about 60 minutes and a dose-normalized Cmax of about 2.72+/−0.84 pg/mL per mcg dosed.

### Claim 9 (depends on 8)

The dosage form of claim 8, wherein the transmucosal administration is to the sublingual membrane.

### Claim 10 (depends on 8)

The dosage form of claim 8, wherein the administration is to the buccal membrane.

### Claim 11 (depends on 1)

The dosage form of claim 1, wherein a single oral transmucosal administration of the dosage form to the subject results in a bioavailability of greater than 65%.

### Claim 12 (depends on 1)

The dosage form of claim 1, wherein a single oral transmucosal administration of the dosage form to the subject results in a bioavailability of greater than 75%.

### Claim 13 (depends on 1)

The dosage form of claim 1, wherein a single oral transmucosal administration of the dosage form to the subject results in a bioavailability of greater than 80%.

### Claim 14 (depends on 1)

The dosage form of claim 1, wherein sufentanil is sufentanil citrate.

### Claim 15 (depends on 1)

A drug delivery device comprising the dosage form of claim 1.

### Claim 16

A method of treating pain in a subject, comprising administering a dosage form to the oral mucosa of a subject, wherein said dosage form is bioadhesive and comprises 5.0 micrograms to 100 micrograms, sufentanil, wherein said dosage form is bioadhesive and has a volume of less than 30 microliters or a mass of less than 30 mg.

### Claim 17 (depends on 16)

The method of claim 16, wherein the dosage form has a volume of less than 10 microliters or a mass of less than 10 mg.

### Claim 18 (depends on 16)

The method of claim 16, wherein the administration of the dosage form to the subject provides a Tmax with a coefficient of variation less than 40%.

### Claim 19 (depends on 16)

The method of claim 16, wherein after administration of the dosage form to the subject, the dosage form provides a Tmax of from about 19.8 minutes to about 60 minutes.

### Claim 20 (depends on 16)

The method of claim 16, wherein after administration of the dosage form to the subject, at least 50% of the drug delivery of sufentanil occurs via the oral transmucosal route.

### Claim 21 (depends on 16)

The method of claim 16, wherein after administration of the dosage form to the subject, at least 55% of the drug delivery of sufentanil occurs via the oral transmucosal route.

### Claim 22 (depends on 16)

The method of claim 16, wherein after administration of the dosage form to the subject, at least 60% of the drug delivery of sufentanil occurs via the oral transmucosal route.