Complex containing mequitazine, a cyclodextrin and an interaction agent

A technology of mequitazine and complexes, applied in medical preparations containing active ingredients, medical preparations with non-active ingredients, drug combinations, etc., can solve the problems of low solubility and low bioavailability

Inactive Publication Date: 2007-09-26
PIERRE FABRE MEDICAMENT SAS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Therefore, it should be noted that there is a need for pharmaceutical formulations containing mequitazine as an active ingredient, which can overcome the problem of low bioavailability of existing formulations due to the low solubility of mequitazine when administered orally.

Method used

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  • Complex containing mequitazine, a cyclodextrin and an interaction agent

Examples

Experimental program
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Effect test

Embodiment 2

[0093] Example 2: Preparation of mequitazine / β-cyclodextrin / arginine complex

[0094] The procedure was the same as that in Example 1 except for the change of reagent dosage. 2.5 grams of mequitazine in racemic and / or D- or L-form, 20.11 grams of β-cyclodextrin, 1.35 grams of arginine, and 5.63 grams of water were used.

[0095] Solubility and dissolution ratios of complexed mequitazine (D, L or racemate) were determined as indicated in "Mequitazine Dissolution Test". The results are listed in Table 1 and shown in Figure 1 below.

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Abstract

The invention concerns a complex comprising mequitazine, a cyclodextrin and an interactive agent characterized in that the solubilizing rate in water of the complexed mequitazine, measured for a mixture at 2g/l of mequitazine in water at 35 DEG C after being stirred for 15 minutes, in higher than 50 % at a pH of 9. The invention also concerns a method for preparing said complex and a pharmaceutical composition comprising same.

Description

technical field [0001] The present invention relates to complexes of mequitazine, cyclodextrin and an interacting agent which have a higher solubility than mequitazine alone. Background technique [0002] Many pharmaceutically active substances suffer from low solubility in aqueous media and thus in biological media. This solubility can lead to lower bioavailability, necessitating increased dose administration. Such dose increases are not always without both side effects and also unfavorable from an economic point of view when considering the higher costs of the pharmaceutically active ingredients. [0003] Mequitazine is an antihistamine used to treat allergies. The molecule of mequitazine is described in detail in patent FR 2 034 605 . [0004] Mequitazine is usually administered by the oral route in various dosage forms such as syrups, tablets or gel caps. [0005] As with many pharmaceutically active ingredients, the absorption of mequitazine administered by the oral...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/5415
CPCA61K47/48969B82Y5/00A61K47/6951A61P11/06A61P27/14A61P37/00A61P37/08A61P43/00A61K47/50A61K31/5415
Inventor 伯纳德·弗雷斯胡贝特·洛沙尔
Owner PIERRE FABRE MEDICAMENT SAS
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