Method for improving levodropropizine taste by cyclodextrin clathration

A technology of levothyroxine and cyclodextrin, applied in the field of antitussive drugs, can solve problems such as poor taste, and achieve the effects of improving compliance, improving application and improving taste

Inactive Publication Date: 2013-11-06
GUIZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The technical problem to be solved by the present invention is to overcome the defect of poor mouthfeel of existing levodropropizine preparations, and provide a method for improving the mouthfeel of levodropropizine through cyclodextrin inclusion, which does not affect the taste of levodropropizine. It can effectively remove the special smell and bitterness of levodropropizine, reduce irritation, improve taste, and improve patient compliance

Method used

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  • Method for improving levodropropizine taste by cyclodextrin clathration
  • Method for improving levodropropizine taste by cyclodextrin clathration
  • Method for improving levodropropizine taste by cyclodextrin clathration

Examples

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Embodiment 1

[0056] Example 1: Dissolve 0.1-5 mole parts of levodropropizine in absolute ethanol, then slowly add it into a saturated solution containing 1 mole part of β-cyclodextrin, stir at 70°C for 1.5h, and mix the obtained The solution was refrigerated for 12 hours, filtered with suction, washed with absolute ethanol, and dried to obtain the clathrate of levodropropizine.

Embodiment 2

[0057] Example 2: Grind 1 molar part of hydroxypropyl-β-cyclodextrin with 3 times the mass of distilled water, then add 0.5-2 molar parts of levodropropizine to dissolve in absolute ethanol, and grind it into a paste , After drying at low temperature, wash with absolute ethanol and dry to obtain levodropropizine clathrate.

Embodiment 3

[0058] Example 3: Take 1 mole of levodropropizine, add ethanol solution, and set aside, dissolve 1 mole of hydroxypropyl-β-cyclodextrin with an appropriate amount of 60°C hot distilled water, add levodropropizine ethanol solution, and mix Stir for 0.5h, lyophilize after freezing in the refrigerator, wash with absolute ethanol, and dry to obtain levodropropizine clathrate.

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Abstract

The invention discloses a method for improving a levodropropizine taste by cyclodextrin clathration. The method comprises that cyclodextrin or cyclodextrin derivatives as carriers are added into levodropropizine so that levodropropizine is included in the cavity of the cyclodextrin or cyclodextrin derivatives and thus a levodropropizine clathrate is obtained. In oral administration, levodropropizine does not contact with the oral cavity of a patient so that the patient does not feel a peculiar smell and a bitter taste of levodropropizine. Therefore, the method effectively improves a levodropropizine taste and patient compliance, can prepare the levodropropizine solid dispersoid of which levodropropizine effects are not influenced, and can effectively improve clinical application of levodropropizine.

Description

technical field [0001] The invention relates to the technical field of antitussive drugs, in particular to a method for improving the mouthfeel of levodropropizine through cyclodextrin inclusion. Background technique [0002] The English name of Levodroproprazine is Levodroproplzine, white crystal, mp98-100℃, molecular formula: [0003] [0004] Soluble in alcohols, dichloromethane and other organic solvents, can be recrystallized with acetone, hardly soluble in water. Levodropropizine is a new type of chiral antitussive drug, which produces antitussive effect through selective inhibition of C-fibers in the trachea and bronchi and relaxation of bronchial smooth muscle. Compared with the existing antitussive drugs, this product has the characteristics of high selectivity, good curative effect, and small side effects. The State Medical Administration listed it as a recommended product for development in the "Ninth Five-Year Plan" and the 2010 Medical Science and Technology...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/495A61P11/14A61K47/69
Inventor 王慧娟郭东贵周英左文娟
Owner GUIZHOU UNIV
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