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Oleanolic acid nanometer suspension and preparation method thereof

A technology of nano-suspension and oleanolic acid, which is applied in the field of medicine, can solve the problems of affecting oral absorption and low solubility in water, etc., and achieve the effect of low preparation cost and mild preparation method conditions

Inactive Publication Date: 2013-10-23
JIANGSU PROVINCE INST OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Oleanolic acid has good activity on liver diseases, etc., but its solubility in water is very small, which affects oral absorption. Therefore, it is necessary to adopt appropriate formulation strategies to improve its dissolution rate in vivo to improve oral bioavailability and curative effect

Method used

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  • Oleanolic acid nanometer suspension and preparation method thereof

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Comparison scheme
Effect test

Embodiment 1

[0017] Dissolve 0.1 g of oleanolic acid and 0.01 g of polyethylene glycol 1000 vitamin E succinate in 50 mL of absolute ethanol, slowly add 0.01 g of polyethylene glycol 4000 into 1000 mL of water, and evaporate at 40 ° C. After wiping off the ethanol, the nano-suspension of oleanolic acid is obtained, and the concentration of oleanolic acid is 0.1 mg / ml. The average particle diameter of the oleanolic acid nanosuspension was measured, and the result was 363nm, and the suspension remained stable within 48h.

Embodiment 2

[0019] Dissolve 0.1 g of oleanolic acid and 0.04 g of polyethylene glycol 1000 vitamin E succinate in 80 mL of 95% ethanol, slowly add 0.04 g of polyethylene glycol 4000 into 400 mL of water, and evaporate at 40 ° C. After wiping off the ethanol, the nano-suspension of oleanolic acid is obtained, and the concentration of oleanolic acid is 0.25 mg / ml. Measure the average particle diameter of oleanolic acid nanosuspension, the result is 185nm (the transmission electron microscope figure of oleanolic acid nanosuspension is shown in figure 1 ), the suspension remained stable within 48h.

Embodiment 3

[0021] Dissolve 0.1 g of oleanolic acid and 0.02 g of polyethylene glycol 1000 vitamin E succinate in 50 mL of absolute ethanol, slowly add 0.02 g of polyethylene glycol 4000 into 200 mL of water, and evaporate at 40 ° C. After wiping off the ethanol, the oleanolic acid nanosuspension was obtained, and the concentration of the oleanolic acid was 0.5 mg / ml. The average particle diameter of the oleanolic acid nanosuspension was measured, and the result was 315nm, and the suspension remained stable within 48h.

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Abstract

The invention belongs to the technical field of medicines, and discloses an oleanolic acid nanometer suspension and a preparation method thereof. The curative effect of oleanolic acid is restricted because oleanolic acid has small solubility in water and low oral bioavailability. The oleanolic acid nanometer suspension of the invention is characterized by comprising oleanolic acid, tocopherol polyethylene glycol succinate 1000 and polyethylene glycol 4000 with a mass ratio of 10-5:1-2:1-2. The preparation method of the nanometer suspension is mild in condition, simple and controllable; and oleanolic acid in the prepared nanometer suspension has higher oral bioavailability.

Description

technical field [0001] The invention relates to an oleanolic acid nano-suspension and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Oleanolic acid has good activity on liver diseases, etc., but its solubility in water is very small, which affects oral absorption. Therefore, it is necessary to adopt appropriate formulation strategies to improve its dissolution rate in vivo to improve oral bioavailability and curative effect. Nanosuspension refers to a dosage form in which drug particles are dispersed in an aqueous solution containing a stabilizer with a nanoscale particle size. And it can be solidified by post-treatment processes such as spray drying and freeze drying, and further prepared into various dosage forms according to different administration routes, such as tablets, pills, capsules, etc. Since the drug in the nanosuspension is in a solid state, it can be made into a high-dose insoluble drug preparation, a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/56A61K47/34A61P1/16
Inventor 宁青沈陶贾晓斌
Owner JIANGSU PROVINCE INST OF TRADITIONAL CHINESE MEDICINE
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