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Asiatic acid lipid nanoparticle capable of stimulating oral absorption and preparation method thereof

A technology of lipid nanoparticles and asiatic acid, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc., to improve oral bioavailability, simple preparation process, and simple prescription composition Effect

Inactive Publication Date: 2013-04-17
ZHEJIANG ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] After searching, there is currently no patent application or literature report on the improvement of intestinal absorption by asiatic acid lipid nanoparticles

Method used

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  • Asiatic acid lipid nanoparticle capable of stimulating oral absorption and preparation method thereof
  • Asiatic acid lipid nanoparticle capable of stimulating oral absorption and preparation method thereof
  • Asiatic acid lipid nanoparticle capable of stimulating oral absorption and preparation method thereof

Examples

Experimental program
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preparation example Construction

[0019] The above-mentioned preparation method of asiatic acid lipid nanoparticles comprises the following process:

[0020] 1. Using absolute ethanol as a solvent, add lipid materials and asiatic acid (chromatographic purity greater than 90%), heat and dissolve in a water bath at (70±2) ° C, as an organic phase, in which the mass of asiatic acid and lipid materials The ratio is 1:7-11, and the solution concentration of the lipid material is 7-11 mg / mL.

[0021] 2. With water as the dispersed phase, heat to (70±2)°C.

[0022] 3. Under 400r / min mechanical stirring, inject the organic phase into the dispersed phase, the volume ratio of absolute ethanol to water is 1:10; continue stirring for 5 minutes to obtain a cloudy liquid with opalescence. After the turbid solution was cooled to room temperature, the pH was adjusted to 1.2 with hydrochloric acid, centrifuged, the precipitate was washed with a small amount of deionized water, centrifuged again, and the upper liquid was disca...

Embodiment 1

[0024] Example 1: Preparation of asiatic acid glyceryl monostearate lipid nanoparticles (mass ratio of main drug to lipid material is 1:7)

[0025] Accurately weigh 5 mg of asiatic acid and 35 mg of glyceryl monostearate (commercially available, purity > 90%), dissolve in 5 mL of absolute ethanol under heating in a water bath at (70±2) °C, and use it as the organic phase, lipid material The concentration of the solution is 7mg / mL. With water as the dispersed phase, heat to (70±2)°C. Under mechanical stirring at 400 rpm, inject the organic phase into 50 mL of the dispersed phase, and continue stirring for 5 min to obtain a cloudy liquid with opalescence. After the turbid solution was allowed to cool to room temperature, the pH was adjusted to 1.2 with hydrochloric acid, centrifuged, the precipitate was washed with a small amount of deionized water, and the supernatant liquid was discarded by centrifugation to obtain asiatic acid lipid nanoparticles. The nanoparticles can be d...

Embodiment 2

[0029] Example 2: Preparation of asiatic acid glyceryl monostearate lipid nanoparticles (mass ratio of main drug to lipid material is 1:9)

[0030] Accurately weigh 5 mg of asiatic acid and 45 mg of glyceryl monostearate (commercially available, purity> 90%), (70

[0031] ±2) Dissolve in 5mL of absolute ethanol under heating in a water bath at ℃, and use as the organic phase, the solution concentration of the lipid material is 9mg / mL. Use water as the dispersed phase, heat to (70±2)°C, and under mechanical stirring at 400rpm, inject the organic phase into 50mL of the dispersed phase, and continue stirring for 5min to obtain a cloudy liquid with opalescence. After the turbid solution was cooled to room temperature, the pH was adjusted to 1.2 with hydrochloric acid, centrifuged, the precipitate was washed with a small amount of deionized water, centrifuged again, and the upper liquid was discarded to obtain asiatic acid lipid nanoparticles. The nanoparticles can be dispersed in...

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Abstract

The invention discloses an asiatic acid lipid nanoparticle capable of stimulating oral absorption and a preparation method thereof. The asiatic acid lipid nanoparticle is prepared by taking a lipid material as a carrier and asiatic acid as a main drug through a solvent diffusion method. The particle size of the obtained lipid nanoparticle is smaller than 700nm, the entrapment rate is 40-90% and the drug-loading rate is 7-11%. By utilizing the nanoparticle, the intestinal drug absorption can be increased, and the oral bioavailability is improved.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to asiatic acid lipid nanoparticles capable of increasing intestinal drug absorption and oral bioavailability and a preparation method thereof. Background technique [0002] Centella asiatica (L.) Urban. is the dried or rooted whole plant of Centella asiatica (L.) Urban. It has the effects of clearing heat and dampness, detoxifying and reducing swelling (Zhang Leilei, et al. Chemical composition of Centella asiatica Research [J]. Chinese Herbal Medicine, 2005,36(12):1761-1763.). Asiatic Acid (Asiatic Acid) is one of the active ingredients of Centella asiatica, which belongs to pentacyclic triterpene acid. It has the effects of treating skin wounds and resisting liver and kidney fibrosis. It is often used in the treatment of scars related to beautifying the skin (Chen Jun, Etc. Research on the biological activity of Asiatic acid and its derivatives [J]. Chinese H...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K31/56A61K47/14A61K9/10A61P17/02A61P1/16A61P13/12
Inventor 王胜浩张雅雯尹丽娜梁泽华冯霞
Owner ZHEJIANG ACAD OF MEDICAL SCI
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