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Matrine type alkaloid microemulsion and preparation method thereof

A technology of matrine and alkaloids, applied in the field of medicine, can solve the problems of unsatisfactory water solubility of drugs, single dosage form, yellowing, etc.

Inactive Publication Date: 2009-10-07
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, our country started relatively late in the study of this project. One of the outstanding problems to be solved is the single dosage form. This research focuses on increasing the drug content of matrine microemulsion soluble water, enhancing drug efficacy, saving costs, and making drugs more effective. absorbed by crops
[0004] At present, the marketed dosage forms of matrine include matrine for injection, matrine sodium chloride injection, matrine glucose injection, matrine suppository, non-intravenous administration preparations such as matrine suppository, non-intravenous matrine Low bioavailability of ginseng injection, obvious local pain during intramuscular injection, vascular irritation and toxicity of ordinary intravenous water injection, etc., as well as unsatisfactory water solubility and poor stability of the drug, especially after water injection sterilization Degradation and yellowing, long-term storage, its quality and safety are difficult to control, which will affect its curative effect and clinical use

Method used

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  • Matrine type alkaloid microemulsion and preparation method thereof
  • Matrine type alkaloid microemulsion and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Embodiment 1: preparation matrine microemulsion

[0046] Formula and ratio:

[0047] Matrine 0.5g

[0048] Ethyl oleate 2.0g

[0049] Tween-80 5.3g

[0050] Glycerin 2.7g

[0051] Dimethyl sulfoxide 0.1g

[0052] Prepared 30.0g microemulsion containing medicine

[0053] Deionized water 19.4g

[0054] The preparation method is:

[0055] Weigh the oil phase, emulsifier and co-emulsifier according to the above formula, use an ultrasonic machine at room temperature to make the three fully mixed, then add matrine, ultrasonically mix, then add deionized water and dimethyl sulfoxide, and then sonicated at room temperature to form a jelly-like slightly turbid matrine microemulsion.

Embodiment 2

[0056] Embodiment 2: preparation matrine microemulsion

[0057] Formula and ratio:

[0058] Matrine 0.5g

[0059] Ethyl oleate 1.0g

[0060] Tween-80 6.0g

[0061] Absolute ethanol 1.0g

[0062] Dimethyl sulfoxide 0.1g

[0063] Prepare medicated microemulsion 20.5g

[0064] Deionized water 10.0g

[0065] The preparation method is:

[0066] Weigh the oil phase, emulsifier and co-emulsifier according to the above formula, use an ultrasonic machine at room temperature to make the three fully mixed, then add matrine, ultrasonically mix, then add deionized water and dimethyl sulfoxide, and then sonicated at room temperature to form a clear matrine microemulsion.

Embodiment 3

[0067] Embodiment 3: preparation matrine microemulsion

[0068] Formula and ratio:

[0069] Matrine 0.6g

[0070] Oleic acid 1.0g

[0071] Tween-80 6.0g

[0072] Absolute ethanol 3.0g

[0073] Dimethyl sulfoxide 0.1g

[0074] Prepared medicated microemulsion 26.7g

[0075] Deionized water 16.0g

[0076] The preparation method is:

[0077] Weigh the oil phase, emulsifier and co-emulsifier according to the above formula, use an ultrasonic machine at room temperature to make the three fully mixed, then add matrine, ultrasonically mix, then add deionized water and dimethyl sulfoxide, and then sonicated at room temperature to form a turbid matrine microemulsion.

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Abstract

The invention relates to matrine microemulsion and a preparation method thereof, which overcomes the defects of low solubility and low bioavailability of matrine and improves the stability of matrine microemulsion. The invention adopts microemulsion as a pharmaceutical carrier to prepare matrine O / W type microemulsion with liquid drop of 1 to 100nm particle size so as to improve the dispersity of enveloped medicaments, promote the percutaneous absorption of plant surface cuticle and strengthen the effect of eliminiting insect injury, thereby providing scientific basis for theory and application study. The invention also relates to a method of forming stable O / W emulsion by doping matrine into oil. The compound comprises matrine, oil phase, water and surfactant. In a preferred embodiment, the oil is tween 80, an emulgator is ethyl oleate, and an emulgator assistant is absolute ethyl alcohol. The medicament content of soluble water aqua of matrine type alkaloid microemulsion is improved,the medicament effect is strengthened, the cost is saved and the medicament is more effectively to be absorbed by crops by forming matrine type alkaloid O / W microemulsion.

Description

Technical field: [0001] The invention belongs to the technical field of medicine, and relates to a matrine microemulsion and a preparation method thereof, in particular to an agricultural matrine-type alkaloid (including proliposome) microemulsion and a preparation method thereof. Background technique: [0002] Matrine is one of the main alkaloids extracted and isolated from Sophora flavescens, broad bean root, Sophora sophora and other plants of the leguminous genus. It has been proved by pharmacological studies that it has various biological activities, such as anti-tumor, anti-inflammation, Anti-arrhythmia, prevent liver fibrosis, improve liver function and so on. Since Sophora flavescens itself can be directly used as a Chinese herbal medicine for clinical application, its preparation is safe for humans, animals and the environment, does not harm natural enemies of pests, is beneficial to ecological balance, has certain insecticidal and disease-preventing effects, and ca...

Claims

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Application Information

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IPC IPC(8): A01N43/90A01N25/04A01P7/00
Inventor 李铁福李泽
Owner SHENYANG PHARMA UNIVERSITY
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