# US 2021/0275445 A1 · Method of rapidly achieving therapeutic concentrations of triptans for treatment of migraines

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 2021/0275445 A1
- Document ID: US20210275445A1
- Status: Published application
- Kind: A1
- Application number: 17/330,289
- Filed: 2021-05-25
- Published: 2021-09-09
- Earliest claimed: 2016-02-19
- Assignees: Zosano Pharma Corporation
- Applicants: Zosano Pharma Corporation
- Inventors: Mahmoud Ameri; Donald Kellerman; Peter E. Daddona; Yi Ao
- Web page: https://patentgrep.com/patent/US20210275445A1

## CPC

- A61K 9/0021: {Intradermal administration, e.g. through microneedle arrays or needleless injectors}
- A61K 9/0014: {Skin, i.e. galenical aspects of topical compositions (non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00)}
- A61K 31/422: not condensed and containing further heterocyclic rings
- A61K 47/12: Carboxylic acids; Salts or anhydrides thereof
- 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)

## Abstract

Compositions, devices and methods employing therapeutic concentrations of a triptan for treatment of migraine are described. Also described are methods and apparatuses for delivery of zolmitriptan for achieving a Tmax as quick as 2 minutes and not later than 30 minutes in the majority of subjects.

## Claims

### Claim at position 1

1-30. (canceled)

### Claim 31

An intracutaneous delivery system that is bioequivalent to an intracutaneous delivery system comprising a plurality of microprojections that are adapted to penetrate or pierce the stratum corneum of a human patient, the microprojections having a solid formulation coating disposed thereon, wherein the coating comprises zolmitriptan or a pharmaceutically acceptable salt thereof in an amount of about 1 mg to about 5 mg per system, and wherein at least 95% of the zolmitriptan is released from the system within about 5 minutes when measured by USP Paddle Over Disk Method (Apparatus 5), wherein:
bioequivalence is established by (a) a 90% Confidence Interval (CI) for AUC which is between 0.80 and 1.25; and (b) a 90% CI for Cmax which is between 0.80 and 1.25.

### Claim 32

An intracutaneous delivery system that is bioequivalent to an intracutaneous delivery system comprising:
a. A disposable patch assembly having a plurality of microprojections disposed in an array of about 3 cm2 to about 6 cm2, the array having a density of about 200 to about 2000 microprojections/cm2, the microprojections adapted to penetrate or pierce the stratum corneum of a human patient;
b. the microprojections having a solid formulation coating disposed thereon, wherein the coating comprises amorphous zolmitriptan or a pharmaceutically acceptable salt thereof in an amount greater than about 0.6 mg/cm2 to less than about 1 mg/cm2;
c. the microprojections having a width of about 10 μm to about 500 μm and a tip angle of about 30 to about 70 degrees; and
d. wherein at least 95% of the zolmitriptan is released from the system within about 5 minutes when measured by USP Paddle Over Disk Method (Apparatus 5), wherein:
bioequivalence is established by (a) a 90% Confidence Interval (CI) for AUC which is between 0.80 and 1.25; and (b) a 90% CI for Cmax which is between 0.80 and 1.25.

### Claim 33

An intracutaneous delivery system that is bioequivalent to an intracutaneous delivery system for the treatment or alleviation of migraine or cluster headache, comprising a plurality of microprojections that are adapted to penetrate or pierce the stratum corneum of a human patient, the microprojections having a solid formulation coating disposed thereon, wherein the coating comprises amorphous zolmitriptan or a pharmaceutically acceptable salt thereof in an amount of about 1 mg to about 5 mg per system, wherein at least 95% of the zolmitriptan is released from the system within about 5 minutes when measured by USP Paddle Over Disk Method (Apparatus 5), and wherein upon application of the system to a selected area of skin of the patient, the Tmax of a therapeutically effective blood plasma concentration occurs within about 45 minutes of the application, the Cmax is about 5 to about 25 ng/ml, and the AUCO-2 hr is about 5 to about 20 ng/ml*hour, wherein:
bioequivalence is established by (a) a 90% Confidence Interval (CI) for AUC which is between 0.80 and 1.25; and (b) a 90% CI for Cmax which is between 0.80 and 1.25.