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Flumazenil complexes, compositions comprising same and uses thereof

一种氟马西尼、络合物的技术，应用在可溶性络合物领域，能够解决未满足等问题

Inactive Publication Date: 2014-01-08
COERULEUS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] There remains an unmet need to formulate flumazenil derivatives that are highly soluble and thus suitable for the preparation of highly concentrated flumazenil formulations

Method used

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  • Flumazenil complexes, compositions comprising same and uses thereof
  • Flumazenil complexes, compositions comprising same and uses thereof
  • Flumazenil complexes, compositions comprising same and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0136] Example 1 . Preparations of Flumazenil Salts and Flumazenil Complexes Containing 1% Flumazenil

[0137] Formulations containing 1% flumazenil in the form of flumazenil salts or flumazenil complexes are presented in the table below. All formulations were evaluated for appearance and only clear solutions, ie clear solutions in which no precipitate ('ppt') or slight precipitate ('sl-ppt') or few particles ('part') formed, were tested for pH.

[0138] First, the composition comprising niacinamide and meglumine as complexing agents resulted in a clear solution. After 12 hours, a precipitate formed in the formulation containing meglumine. Formulation No. 2 containing 4.5% niacinamide showed less precipitate (designated "ppt" in the table) after 12 hours compared to formulation No. 1 containing 1.5% niacinamide (Table 1). This result suggests that high niacinamide concentrations may be preferred, although not necessary to achieve the invention. The appropriate pH of the c...

Embodiment 2

[0147] Example 2 .Preparation of flumazenil (1.2% w / w and 1.5% w / w) nicotinamide complex

[0148] Formulations comprising 1.2% w / w to 1.5% w / w of flumazenil in the form of flumazenil complexes containing niacinamide were prepared and are presented in the table below.

[0149] Table 5. Flumazenil Formulations Containing Flumazenil Niacinamide Complex (% w / w)

[0150]

Embodiment 3

[0151] Example 3 . Preparation of flumazenil nicotinamide complex and menthol

[0152]A formulation containing 1.2% w / w flumazenil based on formulation 16B (Table 6, above) was prepared using menthol and is presented in the table below.

[0153] Table 6. Flumazenil Formulations Containing 1.2 Flumazenil (% w / w) and Menthol

[0154]

[0155] The results were similar to those obtained in the absence of menthol (see Tables 4-5, above), suggesting that menthol is not necessary to achieve the invention, especially the flumazenil salts or flumazenil complexes improved solubility.

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Abstract

Soluble complexes of flumazenil, methods for the preparation thereof, pharmaceutical compositions including same and use of the compositions for alleviating or counteracting the various types of hypersomnia, drowsiness, residual effects associated with the administration of sleep / hypnotic drugs, alcohol intoxication or hepatic encephalopathy.

Description

field of invention [0001] The present invention provides a soluble complex of flumazenil, a method for preparing it, a pharmaceutical composition containing it, and the composition is used to alleviate or eliminate various types of hypersomnia, drowsiness, and sleep / hypnosis drugs administration of , sedation, alcoholism and residual effects associated with hepatic encephalopathy. Background of the invention [0002] Flumazenil (chemical name 8-fluoro-5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a][1, 4] Benzodiazepine-3-carboxylate), which is also known as Ro 15-1788, Anexate TM 、Lanexat TM 、Mazicon TM and Romazicon TM . Flumazenil is against GABA A / benzodiazepine receptor complex, the specific binding site for benzodiazepines, imidazobenzodiazepines with high affinity. Because flumazenil is a competitive inhibitor of benzodiazepines, it is used to reverse benzodiazepine-induced sedation and anesthesia after therapeutic or diagnostic procedures (eg WO 2009 / 114740). Fl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D245/06
CPCC07D245/06A61K31/455A61K31/5517A61K45/06C07D487/04A61K47/10A61K47/18A61K47/40A61K9/0056A61P25/00A61P39/02A61P43/00A61P5/26A61K2300/00
Inventor 希蒙·艾姆萨勒姆
Owner COERULEUS
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