Montelukast sodium liposome solid preparation

A technology of montelukast sodium lipid and solid preparations, which is applied in the field of medicine, can solve the problems of high bioavailability, liposome stability, poor encapsulation efficiency, and high encapsulation efficiency, and achieve high bioavailability, Improved storage and high encapsulation efficiency

Inactive Publication Date: 2012-01-11
HAINAN MEIDA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] The montelukast sodium liposome provided by the invention has excellent quality, high stability, easy storage, high encapsulation efficiency and high bioavailability, and can solve the technical problems of poor liposome stability and encapsulation efficiency , obtained unexpected formulation effects, thus providing liposome solid formulations with good quality

Method used

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  • Montelukast sodium liposome solid preparation
  • Montelukast sodium liposome solid preparation
  • Montelukast sodium liposome solid preparation

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preparation example Construction

[0053] On the other hand, the present invention provides the preparation method of above-mentioned montelukast sodium liposome, the method comprises the following steps:

[0054] (1) Dissolving hydrogenated soybean lecithin, cholesterol, Tween 80 and soybean sterol in isopropanol to obtain a phospholipid solution;

[0055] (2) Montelukast sodium and mannitol are dissolved in water, and the above-mentioned phospholipid solution is slowly dropped into it, while stirring evenly with a magnetic stirrer to obtain a liposome suspension containing isopropanol;

[0056] (3) Place the above-mentioned suspension in an ultrasonic container and sonicate to a translucent colloidal solution;

[0057] (4) Filter the above-mentioned translucent colloid with a microporous membrane, and place the filtrate at -40 to -45°C to pre-freeze for 4-6 hours, then slowly raise the temperature to -5°C at a rate of 2°C / hour, and keep warm for 2 hour, and then heated up to 30° C. at a rate of 5° C. / hour, a...

Embodiment 1

[0085] The preparation of embodiment 1 montelukast sodium liposome tablet

[0086] The raw and auxiliary materials used are as follows:

[0087]

[0088]

[0089] Preparation Process:

[0090] (1) 22g hydrogenated soybean lecithin, 10g cholesterol, 4g Tween 80 and 2g soybean sterol are dissolved in 600ml isopropanol to obtain lipid solution;

[0091] (2) Dissolve 5g montelukast sodium and 25g mannitol in 300ml water, slowly drop the above-mentioned lipid solution into it, and stir evenly with a magnetic stirrer at the same time, and the stirring time is 60min to obtain isopropanol-containing liposome suspension;

[0092] (3) Place the above-mentioned suspension in an ultrasonic container and sonicate to a translucent colloidal solution;

[0093] (4) Filter the above-mentioned translucent colloid with a 0.45 μm microporous membrane, pre-freeze the filtrate at -45°C for 4 hours, then slowly raise the temperature to -5°C at a rate of 2°C / hour, keep it warm for 2 hours, a...

Embodiment 2

[0098] The preparation of embodiment 2 montelukast sodium liposome capsules

[0099] The raw and auxiliary materials used are as follows:

[0100]

[0101]

[0102] Preparation Process:

[0103] (1) 20g hydrogenated soybean lecithin, 10g cholesterol, 4g Tween 80 and 3g soybean sterol are dissolved in 300ml isopropanol to obtain lipid solution;

[0104] (2) Dissolve 5g montelukast sodium and 20g mannitol in 200ml water, slowly drop the above-mentioned lipid solution into it, and stir evenly with a magnetic stirrer at the same time, and the stirring time is 90min to obtain isopropanol-containing liposome suspension;

[0105] (3) Place the above-mentioned suspension in an ultrasonic container and sonicate to a translucent colloidal solution;

[0106] (4) Filter the above-mentioned translucent colloid with a 0.45 μm microporous membrane, pre-freeze the filtrate at -40°C for 6 hours, then slowly raise the temperature to -5°C at a rate of 2°C / hour, keep it warm for 2 hours,...

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Abstract

The invention provides a montelukast sodium liposome solid preparation which is prepared from raw and auxiliary materials comprising the following components in parts by weight: 5 parts of montelukast sodium, 15-30 parts of hydrogenated soybean phosphatidylcholine (HSPC), 8-20 parts of cholesterol, 4-12 parts of Tween 80, 20-50 parts of mannitol and 1-3 parts of soyasterol. The montelukast sodiumliposome solid preparation has high stability, is stable in light and heat environments, is convenient to store, has the advantages of simple preparation method, high encapsulation rate and uniform particle size and can be preserved in a body for a long time, thereby improving the product quality of the preparation and reducing the toxic side effects.

Description

technical field [0001] The invention relates to a liposome solid preparation, in particular to a liposome solid preparation of montelukast sodium and a preparation method thereof, including tablets, granules and chewable tablets, and belongs to the technical field of medicine. Background technique [0002] Montelukast sodium, the chemical name is [R-(E)]-1-[[[1-[3-[2-[7-chloro-2-quinoline)vinyl]phenyl-3-[2 -(1-Hydroxy-1-methylethyl)phenyl]propyl]thio]methyl]cyclopropane sodium acetate, molecular formula C 35 h 35 C 1 NNaO 3 S, molecular weight 608.18, structural formula: [0003] [0004] Montelukast sodium is a white or off-white crystalline powder, odorless, hygroscopic, and easily soluble in ethanol, acetone, and ethyl acetate. [0005] Montelukast is a highly specific cysteinyl leukotriene receptor antagonist that blocks the interaction between cysteinyl leukotrienes and receptors, thereby blocking the tracheal response to leukotrienes, To achieve the purpose of...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/24A61K47/28A61K47/30A61K47/10A61K9/127A61K31/47A61P11/06
Inventor 廖爱国
Owner HAINAN MEIDA PHARMA
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