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Usnic acid nanometer suspension, and preparation method and use thereof

A nano-suspension and usnic acid technology, which is applied in liquid transportation, pharmaceutical formula, emulsion transportation, etc., can solve the problems of low solubility of usnic acid and poor druggability, and achieve good application value, less excipients, and stability good sex effect

Active Publication Date: 2015-03-11
BEIJING UNIV OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Thereby overcome the shortcoming of usnic acid low solubility, poor druggability, provide a kind of technologically feasible, stable and reliable, easy industrialized technical means and the preparation technology of preparation intermediate for the development of its preparation, and thus make a kind of having good Oral absorption and application prospect of usnic acid composition

Method used

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  • Usnic acid nanometer suspension, and preparation method and use thereof
  • Usnic acid nanometer suspension, and preparation method and use thereof
  • Usnic acid nanometer suspension, and preparation method and use thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0045] Embodiment 1: the preparation one of usnic acid nanocrystal suspension

[0046] Usnic acid nanocrystal suspension was prepared by medium dispersion method (grinding method).

[0047] prescription:

[0048]

[0049] Preparation process:

[0050] In a 100ml flask, accurately weigh about 1.6g of HPC-SL and place it in 45ml of distilled water to swell completely to obtain solution A; accurately weigh about 0.03g of SDS and dissolve it in 20ml of distilled water to obtain solution B; Mix well to obtain solution C.

[0051] Accurately weigh about 8 g of usnic acid that has passed through an 80-mesh sieve and slowly add it to solution C and keep stirring to make it evenly dispersed, and make a coarse suspension of usnic acid for later use.

[0052] start up Mill LAB level wet grinding machine (Mill Research Lab, Switzerland WAB Machinery Co., Ltd.), pour the above-mentioned coarse suspension of usnic acid prepared above into the hopper, and add it to the hopper for gri...

Embodiment 2

[0056] Embodiment 2: the preparation two of usnic acid nanocrystal suspension

[0057] Nano-precipitation method (solvent diffusion method) was used to prepare usnic acid nanocrystal suspension.

[0058] prescription:

[0059] Water phase - 1.5% polyvinyl alcohol (W / V) and 0.5% sodium lauryl sulfate (W / V) aqueous solution, 20ml;

[0060] Oil phase - 0.8% usnic acid and 3% polylactic acid ethyl acetate solution, 5ml.

[0061] Preparation Process:

[0062] Take the prescribed amount of water phase, keep stirring (1000rmp / min), slowly drop the oil phase solution into the water phase, treat it with an ultrasonic probe for 90 seconds (ice bath), and then homogenize it three times with a high-pressure homogenizer APV2000. The obtained emulsion was stirred at room temperature (600rmp / min) for 8 hours, and the ethyl acetate was evaporated to obtain the obtained emulsion.

[0063] According to the particle size and potential measurement method in Example 1, the average particle siz...

Embodiment 3

[0064] Embodiment 3: Freeze-drying test of usnic acid nanocrystal suspension

[0065] Long-term storage of the suspension is not only detrimental to the stability of the drug, but also may cause the problem of particle focus and sedimentation, so we freeze-dried the prepared usnic acid nanosuspension. Glucose or mannitol was selected as the lyoprotectant, and the freeze-drying test was carried out at the ratio of 1%, 2% and 4% (g / 100mL) respectively.

[0066] Adopt CHRIST laboratory small-sized lyophilizer to test, get the usnic acid nano-suspension 10ml that prepares in embodiment 1, respectively follow the ratio listed in table 1, add suitable lyoprotectant, and After adding 10ml of distilled water, shake it to fully dissolve, and divide it into 5ml vials (thickness of 10-15mm), pre-freeze at -80°C overnight, take it out and put it in a freeze dryer, and slowly raise the temperature under vacuum , carry out sublimation drying and re-drying, and the entire freeze-drying time...

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Abstract

The invention relates to an usnic acid nanometer suspension, and a preparation method and a use thereof, and concretely relates to the usnic acid nanometer suspension, the preparation method thereof, the use of the suspension in the preparation of other medicinal preparations as a preparation intermediate, and a medicinal composition prepared by using the usnic acid nanometer suspension.

Description

technical field [0001] The present invention relates to a nano-suspension of insoluble drug usnic acid and a preparation method thereof, and further relates to the use of the usnnic acid nano-suspension as a preparation intermediate to prepare other solid or liquid pharmaceutical preparations, and the obtained Usnic acid composition in solid or liquid state. Background technique [0002] Usnic acid (Usnic Acid, UA), also known as lichenic acid, is derived from the dried lichens of Usnea diffracta Vain. and Usnea longissima Ach. Since 1948, there have been related research reports on usnic acid in foreign countries, and the research content has mostly focused on the extraction and separation, biosynthesis, and pharmacological activity of usnic acid. Because of its antibacterial, anti-radiation, antiseptic and other effects, usnic acid has been used in dietary additives, perfumes, cosmetics and other industries, and added as a pure substance to toothpaste, mouthwash, deodoran...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/343A61P31/04
Inventor 曲昌海屠鹏飞赵云芳
Owner BEIJING UNIV OF CHINESE MEDICINE
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