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Salmeterol lipid complex and preparation method thereof

A technology of lipid complexes and complexes, applied in the field of preparation of salmeterol aggregates, can solve problems such as poor stability

Active Publication Date: 2018-12-25
ENKANG PHARMA GUANGZHOU LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, there are relatively few studies on the improvement of salmeterol dosage forms, such as salmeterol liposome dosage forms. In addition, the current domestic liposome research also has technical barriers to poor stability.
Therefore, salmeterol liposome preparations with high efficiency, stability and sustained release characteristics have not been applied in domestic clinical treatment.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Dissolve 12mg of salmeterol, 60mg of DPPC and 24mg of cholesterol in 300ul of absolute ethanol, preheat to 60°C, and keep the temperature constant for 30min to prepare salmeterol lipid solution. The lipid solution was injected into 3 ml of physiological saline solution preheated to 60 °C. Stir slowly at constant temperature for 2 h, and then slowly cool down to room temperature 25° C. to obtain salmeterol lipoplex. The free salmeterol is removed by dialysis to obtain a salmeterol lipoplex solution. The encapsulation efficiency was 85% before removing free drug.

Embodiment 2

[0022] Dissolve 12mg of salmeterol, 60mg of DPPC and 24mg of cholesterol in 300ul of absolute ethanol, preheat to 60°C, and keep the temperature constant for 30min to prepare salmeterol lipid solution. The lipid solution was injected into 3 ml of physiological saline solution preheated to 60 °C. Slowly stir at constant temperature for 2 hours, then slowly lower the temperature to 10°C, then heat up to 55°C, repeat the temperature rise and fall 6 times, and then cool down to room temperature. Obtain salmeterol lipid suspension. The free salmeterol is removed by dialysis to obtain a salmeterol lipoplex solution. The encapsulation efficiency was 95% before removing free drug.

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Abstract

The invention discloses a salmeterol lipid complex and a preparation method thereof. The complex comprises salmeterol, a lipid material, a buffer solution and the like. The lipid complex can compriseone or more lipids. In addition, the invention further discloses the ratio of the high-activity compound salmeterol to the lipids in the complex. The encapsulation efficiency of the salmeterol lipid complex can be increased, and in combination with a pharmaceutically acceptable vector or an optional medicament formula, the complex can prevent or treat related diseases, and has the characteristicsof good stability, high targeting property, low toxic and side effects and the like. The preparation method involved in the invention is simple, and is high in operability, and industrialized production is easy to implement.

Description

Background of the invention [0001] Salmeterol is a β2-receptor agonist with bronchodilator effect, evolved from albuterol. There is an aliphatic side chain in the molecular formula of salmeterol that can be tightly combined with the β2 receptor, which also determines that salmeterol has strong lipophilicity and is easy to enter the lipid layer of the cell membrane, while the dissociation speed is relatively slow, which can make the drug Stay at the medication site for a long time to play its role. [0002] At present, salmeterol is widely used in the prevention and treatment of asthma (including nocturnal asthma and exercise-induced asthma), asthmatic bronchitis and emphysema with reversible airway obstruction. drug. [0003] According to the structural characteristics of salmeterol and salmeterol, the drug is generally used for the prevention and treatment of related diseases by inhalation of the respiratory tract. The common drug dosage forms of salmeterol include aerosol ...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/137A61K47/24A61K47/28A61K47/12A61K47/26A61P11/06A61P11/00
CPCA61K47/12A61K47/24A61K47/26A61K47/28A61K9/127A61K31/137
Inventor 刘海滨梁纯
Owner ENKANG PHARMA GUANGZHOU LTD
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