Galenic form for the oral transmucosal delivery of triptans

A technology for pharmaceutical preparations and triptans, applied in the field of pharmaceutical preparations, can solve problems such as unreachable, and achieve the effects of short action time, considerable dose/effect, and reduced production costs

Active Publication Date: 2011-03-02
菲利普·佩罗维特什 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0028] Furthermore, while it involves the only form of self-administration that is currently the most effective in emergency management, it is still far from 90% relief after 3-4 minutes

Method used

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  • Galenic form for the oral transmucosal delivery of triptans
  • Galenic form for the oral transmucosal delivery of triptans

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0100] Formulation 1:

[0101] - Sumatriptan: 6.0mg

[0102] Introduced in the following form:

[0103] Sumatriptan base 1.20mg

[0104] Sumatriptan Succinate 6.72mg

[0105] -Ethanol 95% V:V: 0.3ml

[0106] -Purified water: sufficient amount up to 0.75ml

[0107] It should be noted that the amount of sumatriptan was 4.8 mg in 6.72 mg of sumatriptan succinate.

[0108] An example of this preparation can be obtained by the following preparation method, a batch of 1000 doses, 0.75L.

[0109] In a stainless steel tank, 0.3 L of 95% V / V ethanol and 1.20 g of sumatriptan base were added.

[0110] Stir with the aid of a paddle stirrer until the sumatriptan base is completely dissolved.

[0111] To this mixture was added 0.450 L of purified water followed by 6.72 g of sumatriptan succinate.

[0112] With the aid of a paddle stirrer, the formulation was stirred until a homogeneous suspension was obtained and completely dissolved.

[0113] Filter the formulation using a 5 μm p...

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Abstract

The invention relates to a galenic form for the oral transmucosal delivery of at least one active ingredient of the family of triptans, comprising at least: said active ingredient in base form and in salt form, and an aqueous-alcoholic solution with a titer of at least 15 degrees alcohol, said active ingredient being present in a stable and complete dissolution state in the aqueous-alcoholic solution, for rapid absorption of said active ingredient through the mucosa of the oral cavity and / or of the oropharynx. The invention also relates to a method for obtaining this galenic formulation and to the use thereof.

Description

technical field [0001] The present invention relates to a pharmaceutical formulation for the immediate systemic administration of at least one active ingredient belonging to the class of triptans, in particular sumatriptan, by the transoral mucosal route. [0002] The invention also relates to methods for obtaining such pharmaceutical preparations and their use. Background technique [0003] Triptans are pharmaceutical active ingredients used to treat migraine attacks, especially cluster headaches (AVF), presenting as acute headaches that require treatment with a real urgency. [0004] Sumatriptan is a major and popular anti-migraine drug on the market, but all triptans share the same physicochemical properties and the same central vascular mode of action. Well known are in particular zolmitriptan, almotriptan, eletriptan, naratriptan and fluvatriptan. [0005] Triptans have the ability to stimulate certain serotonin receptors, more specifically, vascular receptors for 5-h...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K31/404A61P25/06
CPCA61K9/08A61K9/006A61K31/404A61P25/06A61P29/00
Inventor 菲利普·佩罗维特什马克·莫里
Owner 菲利普·佩罗维特什
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