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Method for obtaining modafinil-based pharmaceutical composition, obtained pharmaceutical composition and use thereof

A composition and medicine technology are applied to obtain a modafinil-based pharmaceutical composition, the obtained pharmaceutical composition and its application field, and can solve the problems of disturbing the normal sleep cycle of patients, insomnia and the like

Inactive Publication Date: 2016-10-26
DEBREGEAS & ASSOCIES PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The problem with the currently available commercial forms is that the effect of modafinil lasts far longer than the patient expects, and even this residue of alertness eventually naturally disrupts the patient's normal sleep cycle and may even induce insomnia

Method used

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  • Method for obtaining modafinil-based pharmaceutical composition, obtained pharmaceutical composition and use thereof
  • Method for obtaining modafinil-based pharmaceutical composition, obtained pharmaceutical composition and use thereof
  • Method for obtaining modafinil-based pharmaceutical composition, obtained pharmaceutical composition and use thereof

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Embodiment Construction

[0026] The present invention will be better understood by the following facts.

[0027] Modafinil appears as a crystalline white powder that is practically insoluble in water but partially soluble in methanol and acetone. A consequence of this is that the bioavailability of modafinil is low; estimated at about 40%; indeed, the solubility of modafinil is too low for absolute bioavailability to be determined.

[0028] Thus, seeking to improve the solubility of modafinil; in particular, which is one of the objects of the present invention, the solubility of modafinil was studied in supercritical fluids.

[0029] Among these supercritical fluids, mention may be made of CO 2 : Supercritical CO 2 technology based on CO 2 The dissolving ability of CO can be adjusted freely according to the pressure and temperature conditions applied to it. 2 of dissolving power.

[0030] In the supercritical state (greater than 74 bar and 31 °C), CO 2 have very special properties. The obtained...

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Abstract

The present invention relates to a new method for obtaining modafinil-based pharmaceutical compositions. This method consists in: dissolving S modafinil in a fluid in a supercritical state; then, after reducing the pressure of said fluid, recovering said S modafinil by adsorbing said S modafinil on the surface of a matrix in particulate form. described S modafinil. The fluid may be CO2 or another solvent, and the base may be anhydrous lactose or mannitol. Use of the pharmaceutical composition in situations where a person taking said pharmaceutical composition needs to increase alertness in a short and short period of time.

Description

technical field [0001] Modafinil is 2-[(diphenylmethyl)sulfinyl]acetamide, its molecular formula is C15H15NO2S, and its structural formula is: [0002] Background technique [0003] In 1970, French Lafon pharmaceutical laboratory developed benzhydrylsulfinyl derivatives. In 1986, Adrafinil was tested for the treatment of narcolepsy, but was abandoned because of gastrointestinal properties, rash phenomena and significant skin sensitization problems. Modafinil is a wakefulness drug that has been used in Europe since 1992; it increases wakefulness and daytime alertness and is therefore currently prescribed for the treatment of narcolepsy. Mode of action not fully explained, but involves inhibition of recapture of norepinephrine at the sleep-inducing nucleus of the ventrolateral nucleus of the preoptic area; it also has alpha1-adrenergic agonistic effects, with positive effects on glutamate transmission , and it binds to the dopamine transporter and reduces its recapture. ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K9/20A61K31/165
CPCA61K9/1676A61K9/2077A61K31/165A61P25/00A61P25/20A61P25/26A61K9/1623A61K9/1682A61K9/2018
Inventor 克里斯托弗·勒邦帕斯卡·祖普利法布里斯·勒伯夫詹尼弗·荣格弗朗茨·德尚
Owner DEBREGEAS & ASSOCIES PHARMA