Intranasal dhe for the treatment of headache

Inactive Publication Date: 2016-08-11
SATSUMA PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0030]The methods and formulations may further comprise a microcrystalline cellulose component with a mean particle size diameter of about 100 μm or less. The microcrystalline cellulose component may have a mean particle size diameter of less than about 100 μm, for example, about 95, 90, 85, 80, 75, 70, 65, 60, 55, 50, 45, 40, 35, 30, 25, 20, 15, 10, 5 μm or less.
[0031]The microcrystalline cellulose component may comprise a first microcrystalline cellulose portion with a mean particle diameter size of about 30 μm or less, and a second microcrystalline cellulose portion with a mean particle size diameter of about 30 to about 100 μm. The first microcrystalline cellulose portion may have a mean particle diameter size of about 30 μm or less, for example, 30-25, 30-20, 30-15, 30-10, 30-5, 25-20, 25-15, 25-10, 25-5, 20-15, 20-10, 20-5, 15-10, 15-5 or 10-5 μm. In a specific embodiment, the first microcrystalline cellulose portion has a mean particle diameter size of about 15-30 μm. In another specific embodiment, the first microcrystalline cellulose portion has a mean particle diameter size of about 18-20 μm. In yet another specific embodiment, the first microcrystalline cellulose portion has a mean particle diameter size of about 20 μm. The second microcrystalline cellulose portion may have a mean particle diameter size of about 30 to about 100 μm, for example, 30-90, 30-80, 30-70, 30-60, 30-50, 30-40, 40-90, 40-80, 40-70, 40-60, 40-50, 50-90, 50-80, 50-70, 50-60, 60-90, 60-80, 60-70, 70-90, 70-80, or 80-90 μm. In a specific embodiment, the second microcrystalline cellulose portion has a me

Problems solved by technology

Migraine is a very common, often

Method used

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  • Intranasal dhe for the treatment of headache
  • Intranasal dhe for the treatment of headache
  • Intranasal dhe for the treatment of headache

Examples

Experimental program
Comparison scheme
Effect test

example 1

6.1 Example 1

Preparation of DHE Powder Formulations

[0132]6.1.1 Preparation of 0.1 Mg DHE Powder Formulation

[0133]Powder formulations comprising 0.1 mg DHE were prepared as described herein.

[0134]Materials.

[0135]Dihydroergotamine mesylate (99.7% purity; primary particle distribution: Dv10: 5.3 μm; Dv50: 17.7 μm; Dv90: 69.3 μm; “DvX” refers to the maximum particle diameter below which X % of the sample exists; for example, “Dv10” refers to the maximum particle diameter below which 10% of the sample exists); microcrystalline cellulose, Ceolus® PH-F20JP (nominal particle size: 20 μm, less than 1% retained when sieved through mesh size 400; Asahi Kasei Chemicals Corporation); Microcrystalline cellulose, Ceolus® PH-301 (nominal particle size: 50 μm, less than 1% retained when sieved through mesh size 60 and less than 30% retained when sieved through mesh size 200; Asahi Kasei Chemicals Corporation); Tribasic calcium phosphate (Ca5(OH)(PO4)3; Mallinckrodt Chemicals); HPMC capsule, size 2, ...

example 2

6.2 Example 2

Pharmacokinetic Study of Intranasal Dihydroergotamine Formulations in Primates

[0154]The study described herein is designed to assess the pharmacokinetics of plasma dihydroergotamine (DHE) and 8′-hydroxy DHE levels after intranasal administration using DHE powder formulations described herein, and to compare the pharmacokinetic profiles achieved via intranasal administration of such formulations with those of comparative DHE formulations administered via various dosing routes.

[0155]The study utilizes Cynomolgus monkeys (macaca fascicularis, purpose bred) because the nasal cavity of such monkeys is morphologically similar to that in humans, and is commonly used as an experimental animal.

[0156]Methods.

[0157]Animals.

[0158]Six male Cynomolgus monkeys (macaca fascicularis, purpose bred), 4 to 6 years old are used, following accredited animal welfare standards.

[0159]Test Powder Formulations.

[0160]Powder formulations containing 0.1 mg DHE, 0.5 mg DHE and 1.0 mg DHE, as describe...

example 3

6.3 Example 3

A Randomized, Open-Label, 5-Way Crossover Study to Evaluate the Pharmacokinetics, Dose Proportionality, Safety, and Tolerability of Single Doses of Dihydroergotamine 1, 1.5, 2 and 3 mg Intranasal Powder and Assess the Relative Bioavailability to Dihydroergotamine 1 mg Administered Subcutaneously as a Solution in Healthy Volunteers

[0178]The study described herein is designed to determine the pharmacokinetic profile, dose-proportionality, safety and tolerability of DHE intranasal powder 1 mg, 1.5 mg, 2 mg and 3 mg in young healthy subjects and compare its bioavailability with DHE 1 mg administered subcutaneously as a solution. The pharmacokinetics of DHE and its metabolite (8′-β-hydroxydihydroergotamine; 8′-β-OH-DHE) are characterized in this study.

[0179]Methodology.

[0180]This is a single-center, single-dose, randomized, open-label, 5-way crossover, pharmacokinetic and safety study. Thirty (30) eligible subjects, not less than 40% or more than 60% of either gender, receiv...

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Abstract

Presented herein are powder formulations comprising dihydroergotamine (DHE), or a pharmaceutically acceptable salt thereof. In addition to such formulations, also presented herein are methods comprising intranasally administering powder formulations comprising dihydroergotamine, or a pharmaceutically acceptable salt thereof. The presented methods can be used for treating headache, for example, for rapid onset treatment of headache, including migraine, e.g. acute treatment of migraine with or without aura.

Description

1. CROSS-REFERENCE[0001]This application claims priority to U.S. Provisional Patent Application Ser. No. 61 / 881,947, filed Sep. 24, 2013, which is entirely incorporated herein by reference.2. BACKGROUND[0002]Migraine is a very common, often debilitating, form of headache. Typically the headache is unilateral (affecting one half of the head) and pulsating in nature. In addition to head pain, associated symptoms may include nausea, vomiting, photophobia, (increased sensitivity to light), and phonophobia (increased sensitivity to sound). Migraines can also be associated with “auras,” which are transient visual, sensory, language, or motor disturbances often manifest as flashes of colored or blinking lights that occur shortly before the onset of head pain.[0003]Symptomatic treatment of migraine generally involves administration of triptans, such as sumatriptan or zolmitriptan, or ergot alkaloids, such as ergotamine or dihydroergotamine. While various routes of administration of these dr...

Claims

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Application Information

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IPC IPC(8): A61K31/4985A61K47/22A61K9/14A61K47/02A61K47/38A61K9/00
CPCA61K9/0043A61K9/146A61K31/48A61K45/06A61K31/4985A61K31/522A61K47/38A61K47/22A61K47/02A61K2300/00A61P25/06A61P43/00
Inventor HARUTA, SHUNJISINGH, NIKHILESH N.KOLLINS, JOHNRICO, SALVADOR
Owner SATSUMA PHARMA INC
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