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20(s)-protopanoxadiol nano-particle and preparation method thereof

A technology of protopanaxadiol and nanoparticles, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., which can solve the problems of low drug loading, poor tumor targeting, and oral bioavailability. Low degree and other issues

Inactive Publication Date: 2014-04-23
INST OF MEDICINAL PLANT DEV CHINESE ACADEMY OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Poor water solubility and low oral bioavailability limit its clinical application and curative effect to a large extent. There are currently many preparations related to 20(s)-protopanaxadiol, and the drug loading is relatively low, such as drug substance ( Han Meihua. Chinese Journal of Traditional Chinese Medicine. 2010, 35(7): 842; Han Meihua. Chinese Journal of New Drugs, 2010, 19(10): 888-890); liposome (public patent No. CN1850098A), etc., non-nano preparations such as solid dispersion body (public patent No. CN1879647A); dry suspension (public patent No. CN102631322A); oil solution or emulsion (HanMH, et al.Analytieal Sei.2010, 26:749-751); Patent No. CN102178956A; Han MH, et al.Journal of Analytical chemistry, 2013, 68(8): 1-6); injections (public patent Nos. CN1526407A, CN1850099A, CN1615901A), etc., have poor tumor targeting

Method used

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  • 20(s)-protopanoxadiol nano-particle and preparation method thereof
  • 20(s)-protopanoxadiol nano-particle and preparation method thereof
  • 20(s)-protopanoxadiol nano-particle and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0029] Accurately weigh 200mg of human serum albumin, put it in a beaker and add 20mL of water to dissolve it, and then accurately weigh 200mg of PPD, put it in a vial and add 4mL of acetone to dissolve it. Under the conditions of 25°C, 250W ultrasound, and paddle stirring (300rpm), the acetone solution of PPD was slowly dropped into water, and the acetone was evaporated at 50°C after the dropwise addition to obtain the PPD nanosuspension, with an average particle size of 220nm ( figure 1 ).

[0030] Take PPD nanoparticle freeze-dried powder, dilute it to a certain multiple, drop it on a special copper grid, and after natural drying, add 1% phosphotungstic acid solution (w / v) to stain for 15-20 minutes, and use filter paper to dry the solution. Put it into the transmission electron microscope to observe the shape of the nanoparticles, such as figure 1 shown.

[0031] PPD nanoparticle freeze-dried sample DSC scanning collection of spectra of the present invention is as follow...

Embodiment 2

[0034] Accurately weigh 200mg of human serum albumin, put it in a beaker and add 20mL of water to dissolve it, and then accurately weigh 200mg of PPD, put it in a vial and add 4mL of acetone to dissolve it. The acetone solution of PPD was quickly injected into water, and then the acetone was evaporated at 50°C, and the obtained solution was placed in a high-pressure homogenizer, and the normal temperature was 2000bar and circulated for 3 times to obtain a PPD nanosuspension with an average particle size of 400nm.

Embodiment 3

[0036] Accurately weigh 200mg of PPD and disperse it in 20mL of aqueous solution containing 200mg of human serum albumin. After mixing evenly, put it into a grinder for mediator grinding, add 50g of zirconia grinding beads, and grind for 60min at 0°C at 300rpm to obtain PPD nanosuspension, the average particle size is about 1 μm.

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Abstract

The invention belongs to the technical field of medicines, and relates to a 20(s)-protopanoxadiol nano-particle and a preparation method thereof. The nano-particle comprises a combination of 20(s)-protopanoxadiol and a stabilizing agent in a ratio of 1:(0.05-50). By virtue of prescription optimization, a human serum albumin (HAS) is screened as an optimal sterilizing agent, and an ultrasonic-precipitation combined method is an optimal method. The prepared 20(s)-protopanoxadiol nano-particle is high in drug loading capacity, stable in property, simple in prescription, and simple and practical in preparation process; the range of particle diameter is 30-600nm; and the dissolution of 20(s)-protopanoxadiol can be remarkably promoted by preparing the nano-particle, so that the oral bioavailability of the nano-particle can be improved, and the anti-tumor activity can be improved. Furthermore, the 20(s)-protopanoxadiol nano-particle can be lyophilized, and a proper amount of excipient can be added into the prepared lyophilized powder to further prepare oral solutions, tablets, particles, capsules and other different dosage forms, or prepare injection for hypodermic, intramuscular or intravenous administration, and facilitates clinical application.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a 20(s)-protopanaxadiol nanoparticle, a preparation method and application. Background technique [0002] 20(s)-protopanaxadiol (PPD) is a saponin extracted from traditional Chinese medicine ginseng, which has poor water solubility. In terms of anti-tumor, domestic and foreign studies have reported that 20(S)-protopanaxadiol has good anti-tumor activity. It has obvious growth inhibitory effect and can enhance the body's immunity. It can be used as an adjuvant drug for tumor treatment. In terms of the nervous system, PPD can resist epilepsy, resist depression, and enhance learning ability. [0003] Poor water solubility and low oral bioavailability limit its clinical application and curative effect to a large extent. There are currently many preparations related to 20(s)-protopanaxadiol, and the drug loading is relatively low, such as drug substance ( Han Meihua. Chine...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/575A61K47/42A61K47/38A61K47/32A61K47/34A61P35/00
Inventor 韩美华王向涛
Owner INST OF MEDICINAL PLANT DEV CHINESE ACADEMY OF MEDICAL SCI