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Alpha-asarone mixed micelle injectio and preparation method thereof

A technology of mixing micelles and Asarum, applied in the field of injections, can solve the problems of limited wide application, limited solubilization and drug loading, and insufficient stability of the system, so as to improve blood drug concentration, reduce liver distribution, and improve hydrophilicity. sex-enhancing effect

Active Publication Date: 2009-12-09
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Xu Ximing and others believe that the advantage of binary micelles is to solve the problem of solubilization of insoluble drugs and at the same time promote the absorption of drugs by the body. Smaller, limited solubilization capacity and drug loading capacity, and the system is not stable enough, thus limiting its wide application in the solubilization of poorly soluble drugs

Method used

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  • Alpha-asarone mixed micelle injectio and preparation method thereof
  • Alpha-asarone mixed micelle injectio and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0043] Weigh 50 mg of soybean lecithin, place it in a 50 ml round bottom flask, add 7.5 ml of ethanol solution (10 mg / ml) of sodium deoxycholate, and dissolve to obtain stock solution 1. Dissolve 10 mg of α-asarone in 100 μl ethyl acetate solution to obtain stock solution 2, mix stock solution 1 and stock solution 2, and disperse evenly by ultrasonication. Then spin evaporate to remove the organic solvent, the temperature of the water bath is 35°C, spin until there is no alcohol smell, and form a transparent film, then disperse with 2.5ml of water for injection to obtain a dispersion solution containing drug-mixed micelles, centrifuge at 13000rpm / min for 5min , take the supernatant to obtain α-asarone mixed micelles injection, and then filter it with a 0.22 μm microporous membrane. The filtrate was taken to obtain α-asarone mixed micelles injection. The solubilization amount was measured to be 3.80 mg / ml, and the drug loading amount was 7.6%.

Embodiment 2

[0045] Weigh 35.7 mg of polyene phosphatidylcholine, place it in a 50 ml round bottom flask, add 9 ml of ethanol solution (10 mg / ml) of sodium glycinate cholate, and dissolve to obtain stock solution 1. Dissolve 10 mg of α-asarone in 100 μl ethanol solution to obtain stock solution 2, mix stock solution 1 and stock solution 2, and disperse evenly by ultrasonication. Rotary evaporation to remove the solvent and organic solvent, the water bath temperature is 35 ℃, spin until there is no alcohol smell, form a transparent film, and then disperse with 2.5ml of water for injection to obtain a dispersion solution containing drug mixed micelles, centrifuge at 13000rpm / min After 5 minutes, the supernatant was taken to obtain α-asarone mixed micelles injection, which was then filtered through a 0.22 μm microporous membrane. The filtrate was taken to obtain α-asarone mixed micelles injection. The measured solubilization amount is 3.65 mg / ml, and the drug loading amount is 7.3%.

Embodiment 3

[0047] Weigh 50 mg of egg yolk lecithin, place in a 50 ml round bottom flask, add 8 ml of sodium hyocholate in chloroform-methanol as a 1:1 (volume ratio) solution (10 mg / ml), dissolve, and obtain stock solution 1. Dissolve 10 mg of α-asarone in 1 ml of chloroform solution to obtain stock solution 2, mix stock solution 1 and stock solution 2, and disperse evenly by ultrasonication. The organic solvent is then removed by rotary evaporation, the water bath temperature is 45°C, and the taste of the organic solvent is spun to form a transparent film, and then 2.5ml of pH 7.4 NaH 2 PO 4 -Na 2 HPO 4 Disperse to obtain a dispersion solution of drug-containing mixed micelles, centrifuge at 13,000 rpm / min for 5 minutes, take the supernatant to obtain α-asarone mixed micelles injection, and then filter with a 0.22 μm microporous membrane. The filtrate was taken to obtain α-asarone mixed micelles injection. It was measured to be 3.67 mg / ml, with a drug loading of 7.0%.

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Abstract

The invention provides an alpha-asarone mixed micelle injectio, adopting alpha-asarone of which the chemical name is 2,4,5-trimethoxy-1- propenylbenzene as an active ingredient, and adopting a cholate / phospholipid mixed micelle system for preparing the injectio. The invention not only effectively solves the problem of hard water dissolution of the alpha-asarone, but also greatly increases the drug-loading rate of the micelle injectio. The mixed micelle injectio prepared by the invention has the advantages of favorable stability and simple preparation process.

Description

technical field [0001] The present invention relates to an injection containing α-asarone, in particular, the present invention relates to a mixed micelle injection containing α-asarone. technical background [0002] The chemical name of α-asarone is 2,4,5-trimethoxy-1-propenylbenzene, which is one of the main active ingredients of the traditional Chinese medicine Shichangpu, which has the functions of sedation, anticonvulsion, asthma, expectorant, cough, It has various pharmacological effects such as antispasmodic, anticancer, blood lipid lowering, choleretic, etc. It also has different degrees of inhibitory effects on the growth of pneumococcus, Staphylococcus aureus and Escherichia coli, and is widely used clinically to treat upper respiratory tract infection, bronchial Inflammation, bronchial asthma, acute and chronic cholecystitis, cholelithiasis, grand mal epilepsy and other diseases, especially for the treatment of pneumonia, bronchial asthma and acute exacerbation of...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K9/19A61K31/09A61K47/28A61P11/00A61P11/06A61P1/16A61P25/12
Inventor 张志荣龚涛任春娟
Owner SICHUAN UNIV
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