Precursor micelle prepn and its production process

A production method and micellar technology, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve problems such as unfavorable sterilization treatment, many intermediate links, and complicated production processes. To achieve the effect of solving the problem of physical stability, improving absorbency, and being easy to use

Active Publication Date: 2010-01-13
新疆维吾尔自治区包虫病临床研究所 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] The currently published methods for preparing micellar systems have their own advantages and disadvantages, but they generally have low drug loading, complex production processes, and many intermediate links, which are not conducive to large-scale control of industrial production, and the excipients contain phospholipids and other properties. Unstable substances, so the stability is poor, which is not conducive to various problems of sterilization
At the same time, the above methods are mostly suitable for drugs that are only insoluble in water, and for drugs that are insoluble in both water and most organic solvents, it is difficult to make micellar solutions or precursor micellar preparations using the above methods

Method used

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  • Precursor micelle prepn and its production process
  • Precursor micelle prepn and its production process

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1: Add 1 g of albendazole (principal drug) to 3 g of lactic acid (solvent), fully stir and dissolve at 50 ° C, then add 1 g of Tween-80 (surfactant) to the previous solution, and mix well to form a transparent liquid Shaped albendazole precursor micelle is a new precursor micelle preparation; the new precursor micelle preparation contains 20% of the main drug, 60% of the solvent content, and 20% of the surfactant content; the new precursor The hydration encapsulation rate of the micellar preparation is 80%, and the particle size is 30-450nm.

Embodiment 2

[0028] Embodiment 2: The preparation method is the same as in Example 1, except that the addition of Tween-80 (surfactant) is 2g, and the addition of Albendazole (main ingredient) and lactic acid (solvent) is all the same as in Example 1; In the obtained transparent liquid albendazole precursor micelle, that is, the novel precursor micelle preparation, the main drug content is about 17%, the solvent content is 50%, and the surfactant content is 33%; the novel precursor The encapsulation efficiency of the micelle preparation was 81% after hydration, and the particle size was 20nm to 400nm.

Embodiment 3

[0029] Embodiment 3: the preparation method is the same as in Example 1, except that the addition of Tween-80 (surfactant) is 6g, the addition of Albendazole (main ingredient) and lactic acid (solvent) is all the same as in Example 1; In the obtained transparent liquid albendazole precursor micelle, that is, the novel precursor micelle preparation, the main drug content is 10%, the solvent content is 30%, and the surfactant content is 60%; the novel precursor The hydration encapsulation efficiency of the micellar preparation is 85%, and the particle size is 20nm to 400nm.

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Abstract

The present invention is one new kind of precursor micelle preparation and its production process and usage. The precursor micelle preparation contains main medicine, solvent, surfactant and supplementary material. The production process includes the steps of dissolving the main medicine in solvent, adding surfactant, and mixing to obtain the precursor micelle preparation. Or, the production process includes the steps of dissolving the main medicine in volatile solvent, adding the surfactant into the solution, and volatizing the solvent to obtain the precursor micelle preparation. The usage of the precursor micelle preparation includes diluting in water for hydration, dissolving carrier material and forming micelle automatically. The precursor micelle preparation of the present invention may be applied widely in agriculture, chemical industry, food and other fields.

Description

technical field [0001] The present invention relates to a novel precursor micelle preparation and its preparation method and use method. It is a novel precursor micelle preparation and its production method and use method. It is especially suitable for drugs that are difficult to dissolve in water and most organic solvents. in vivo absorption and efficacy. Background technique [0002] Some drugs that are insoluble in both water and most organic solvents cause difficulties in the preparation process and clinical application of the drugs, and the single dosage form of these drugs also affects the absorption and efficacy of the drugs in the body. To solve the above problems, we invented a new precursor micellar preparation. [0003] Surfactants are typical amphiphilic molecules, which contain lipophilic hydrocarbon chains and hydrophilic functional groups. If a very small amount of surfactant is added to pure water, it will be adsorbed on the surface of the water phase and a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K45/00A61K31/4164A61K31/4184A61K47/30
Inventor 温浩王建华陈迹林筱琦孙殿甲高晓黎牛若觉陈启龙徐志新陈雪鸿苗玉清潘金凤
Owner 新疆维吾尔自治区包虫病临床研究所
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