Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Protopanaxadiol liposome and its preparing method

A technology of panaxadiol lipid and panaxadiol lipid, applied in the field of medicine, can solve the problems of low bioavailability, lack of targeting, thermodynamic instability, etc., to enhance the activity of macrophages, improve the efficacy and safety , The effect of improving storage stability

Inactive Publication Date: 2006-10-25
浙江金石亚药医药科技有限公司
View PDF4 Cites 19 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, protopanaxadiol is a tetracyclic triterpenoid drug, which is insoluble in water and has strong fat solubility. Oral administration with common preparations has the disadvantages of low bioavailability and lack of sufficient targeting in vivo.
The preparation of former ginseng diol injection (patent publication number CN1526407A) needs to use organic solvent or use relatively large amount of solubilizing agent such as polyoxyethylene castor oil (Cremophor~EL) etc., patient can appear allergic reaction after this kind of surfactant is used, Symptoms such as dyspnea and elevated blood pressure need to be pre-treated with steroid hormones and antihistamines to avoid allergic reactions. In addition, protopanaxadiol is unstable in normal saline or 5% glucose diluent and is easy to precipitate precipitation
There is a patent (publication number: CN1626101A) to make protopanaxadiol into nanoemulsion for injection, but the preparation process needs to be sterilized by hot pressing, which will have a certain destructive effect on surfactants such as drugs, oil and phospholipids, and the emulsion belongs to thermodynamics. Unstable heterogeneous system, may appear stratification, flocculation, phase inversion, rupture and rancidity during storage
And the research of protopanaxadiol liposome and its lyophilized product has not been reported at home and abroad

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Weigh 200mg 20(S)-protopanaxadiol, 4000mg soybean lecithin and 1000mg cholesterol, add 10ml ethanol, heat and dissolve at 50°C, add 10mmol / L phosphate buffer (pH6. 5. Containing sucrose (280mmol / L) 100ml, stirred and hydrated for 0.5 hours, and then passed through a high-pressure homogenizer (NS1001L, Italy) at 8.0×10 7 After cycling under Pa pressure for 6 times, filter and sterilize with a 0.22 μm microporous membrane, divide into vials, fill with nitrogen and seal to obtain protopanaxadiol liposomes.

[0029] The obtained liposome has an average particle size of 125nm. The free drug in the liposome is separated by ultracentrifugation, and the drug encapsulation efficiency is measured to be 99.2%. There is no precipitation within 12 hours after diluting 10 times with 5% glucose.

Embodiment 2

[0031] The liposomes prepared in Example 1 were pre-frozen at -45°C for 4 hours, and the vacuum pump was turned on to make the vacuum degree below 20 Pa, and the water was removed by freeze-drying to obtain the protopanaxadiol liposome freeze-dried product.

[0032] The average particle size of the liposome obtained after hydration and reconstitution of the freeze-dried product is 134nm, and the free drug in the liposome is separated by ultracentrifugation. Precipitate out.

Embodiment 3

[0034] Weigh 600mg of 20(R)-protopanaxadiol, 2000mg of hydrogenated soybean lecithin and 1000mg of cholesterol into a 500ml round bottom flask, add 50ml of chloroform to dissolve, and evaporate under reduced pressure at 50°C on a rotary evaporator until a dry film is formed , put it in a vacuum desiccator, dry it in vacuum at room temperature for 12 hours, add 50ml of 10mmol / L phosphate buffer (pH6.5) under nitrogen flow, rotate and shake to hydrate the lipid film to form a uniform suspension, and Quality machine (NS1001L, Italy) in 1.2×10 8 After circulating 8 times under Pa pressure, filter and sterilize with a 0.22 μm microporous membrane, divide into vials, fill with nitrogen and seal to obtain protopanaxadiol liposomes.

[0035] The average particle size of the obtained liposome is 195nm. The free drug in the liposome is separated by ultracentrifugation, and the drug encapsulation efficiency is measured to be 88.6%. There is no precipitation within 12 hours after diluting...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
The average particle sizeaaaaaaaaaa
The average particle sizeaaaaaaaaaa
The average particle sizeaaaaaaaaaa
Login to View More

Abstract

The present invention discloses a protopanoxadiol liposome and its preparation method. Its composition includes protopanoxadiol, phospholipids and cholesterol, their weight ratio is 1:2-100:0-50. Said protopanoxadiol liposome can be made into injection for intravenous injection and can be used for curing various cancer. Besides, said invention also provides the concrete steps of its preparation method.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular it is protopanaxadiol liposome and a preparation method thereof. Background technique [0002] The anti-tumor drug "Shenyi Capsule" is composed of 20(R)-ginsenoside Rg3 single component, and its anti-tumor mechanism is: induction of tumor cell apoptosis, inhibition of tumor cell proliferation and infiltration, anti-tumor cell metastasis, inhibition of vascular endothelial cell Proliferation and improving the immune function of tumor-bearing mice (Zhao Yi. Journal of Clinical Oncology 2001; 6 (1): 81-85). However, the oral bioavailability of ginsenoside Rg3 is extremely low, only 0-2.63%, indicating that it may be rapidly metabolized in vivo (Xie HT, et al.J Chromatogr.B 2005; 818:167-173; Qian T, et al. al. J Chromatogr. B 2005;816:223-232.). Bae et al. found that ginsenoside Rg3 can be metabolized by human fecal microorganisms into ginsenoside Rh2 and aglycone protopanaxadiol, a...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K31/7048A61K9/127A61K9/19A61K47/24A61P35/00
Inventor 金圣煊孙静芸林燕飞晏桂敏雷荣剑
Owner 浙江金石亚药医药科技有限公司
Features
  • Generate Ideas
  • Intellectual Property
  • Life Sciences
  • Materials
  • Tech Scout
Why Patsnap Eureka
  • Unparalleled Data Quality
  • Higher Quality Content
  • 60% Fewer Hallucinations
Social media
Patsnap Eureka Blog
Learn More

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2025 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com