Triptolide nano lipsome gelling agent of external use and its preparation method

A technology of triptolide and nanoliposomes, which is applied in the field of triptolide topical gels and new dosage forms of triptolide, and can solve the problems of many adverse reactions, low bioavailability, restrictions and the like

Inactive Publication Date: 2005-07-06
GUANGZHOU RUIXUN BIO TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Solid lipid nanotechnology is a kind of nanoparticle made of endogenous physiological substance - long-chain saturated fatty acid (stearic acid). Its products are liniment and freeze-dried powder after removing water. External application on the skin must be prepared before use, and liniment is a colloidal solution, which is inconvenient to carry and transport, and has poor stability
[0004] Most of the conventional external preparations are oil-soluble bases, which have disadvantages such as greasy, difficult to spread, wash off, low bioavailability, poor stability, and many adverse reactions, so the application is limited

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Embodiment 1, the preparation of triptolide common gel:

[0046] Weigh 3 g of acrylic polymer material carbomer (product of Wanlong Co., Ltd.), swell with about 90 ml of distilled water, add 4.5 g of triethanolamine dropwise until the gel is transparent, and obtain about 100 g of 3% carbomer blank gel. Take another 2g of triptolide (the product provided by Fujian Academy of Medical Sciences), dissolve it in a small amount of absolute ethanol, add it to the above-mentioned gel matrix, stir and mix in the same direction, and obtain 2% triptolide ordinary gel .

Embodiment 2

[0048] 1. Preparation of triptolide nanoliposome suspension (film-ultrasonic process):

[0049] Weigh 200mg of triptolide, 4g of soybean lecithin, 1g of cholesterol, 0.2g of vitamin E, 0.2g of sodium deoxycholate, dissolve in 20ml of absolute ethanol, transfer to a 1000ml eggplant-shaped bottle, and keep at a constant temperature of 37°C Ethanol was removed by rotary evaporation under reduced pressure in a water bath, and a uniform lipid film was formed on the wall of the bottle. About 15ml of water was added, and the film was washed by rotation to form an initial suspension, which was placed in a water-bath ultrasonic instrument and ultrasonicated intermittently to a translucent colloidal solution to obtain Tripterygium wilfordii. Ester alcohol nano liposome suspension 20g;

[0050] 2. Preparation of blank gel;

[0051] Weigh 5.4 g of acrylic polymer material carbomer (product of Wanlong Co., Ltd.), swell with about 167 ml of distilled water, add 7.5 g of triethanolamine dro...

Embodiment 3

[0055] 1. Preparation of triptolide nanoliposome suspension (ethanol dripping-ultrasonic process):

[0056] Weigh 200 mg of triptolide, 3 g of egg yolk lecithin, 0.75 g of cholesterol, 0.15 g of ethylparaben, and 0.15 g of sodium cholate, dissolve them in 20 ml of absolute ethanol to obtain a lipid solution, and slowly dissolve the lipid solution Drop into about 30ml of pH7.4 phosphate buffer solution, and shake gently while dripping to obtain the initial liposome suspension, place it in a water-bath ultrasonic instrument and ultrasonicate intermittently to a translucent colloidal solution, and obtain triptolide nanolipid Plastid suspension 50g;

[0057] 2. Preparation of blank gel;

[0058] Weigh 0.6 g of carbomer, swell with about 27 ml of distilled water, add 2.4 g of triethanolamine dropwise until the gel is transparent, and obtain 30 g of 2% carbomer blank gel.

[0059] Three, the preparation of gel:

[0060] Add 50 g of nano liposome suspension into 30 g of blank gel ...

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PUM

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Abstract

The invention relates to a triptolide nano lipsome gelling agent of external use and its preparation method, which comprises externally used gelling agent composed of 10-70% of triptolide alcohol nano liposome turbid liquor and 90-30% of blank gel, wherein the weight ratio content of the triptolide alcohol in the total gelling agent is 0.1-2.0%, and the triptolide alcohol alcohol nano liposome turbid liquor comprises 0.7-4.2% of triptolide alcohol, 14-64% of phosphatides, 3.5-16% of cholesterin, 0.7-3.2% of anti-oxidant, 0.7-3.2% of surface active agent, and hydration medium. Its preparing process is also disclosed in the invention.

Description

Technical field: [0001] The invention relates to a pharmaceutical preparation and a preparation method thereof, in particular to a new dosage form of triptolide, namely a triptolide external-use gel prepared by nano-liposome technology. Background technique: [0002] Tripterygium wilfordii is the drug of choice for the treatment of rheumatoid arthritis. Triptolide, also known as triptolide and triptolide, is one of the main active ingredients in triptolide, and products are now on the market. Pharmacological studies have shown that triptolide can not only inhibit the proliferation and activation of T and B lymphocytes, but also induce apoptosis of activated T cells and prevent their further proliferation; increase the level of cAMP in immune cells, reduce the levels of IL-2 and immune globulin protein production. Triptolide can also inhibit the inflammatory joint edema caused by carrageenan, croton oil and Freund's complete adjuvant, reduce the infiltration of acute pleuri...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/127A61K31/365A61P19/00A61P19/02
Inventor 晏亦林陈志彪符砺
Owner GUANGZHOU RUIXUN BIO TECH
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