Preparation method of tripterygium glycosides solid lipid nanoparticle

A technology of lipid nanoparticles and tripterygium glycosides, which can be applied to medical preparations with no active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc. It can solve problems such as lack of pertinence, application limitations, and simple methods. question

Inactive Publication Date: 2010-03-03
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The former two are mainly aimed at the tripterygium alcohol extract and the tripterygium twig extract, rather than the effective parts, and the pertinence is not strong and the method is simple. The administration method of the latter is only limited to external use, and the application is limited. The preparation process of Tripterygium wilfordii polyglycoside solid lipid nanoparticles, after literature search, it is the first time that it is made into solid lipid nanoparticles. Solid lipid nanoparticles (SLN) was developed in the 1990s A new type of nano drug delivery system introduced in the early 1990s

Method used

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  • Preparation method of tripterygium glycosides solid lipid nanoparticle
  • Preparation method of tripterygium glycosides solid lipid nanoparticle
  • Preparation method of tripterygium glycosides solid lipid nanoparticle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Example 1 Preparation of tripterygium glycosides solid lipid nanoparticles (1 prescription amount)

[0031] Tripterygium glycosides 60mg

[0032] Glyceryl monostearate 360mg

[0033] Soy Lecithin 360mg

[0034] Poloxamer 60mg

[0035] Preparation Process:

[0036] Add tripterygium glycosides and glyceryl monostearate to 8ml of acetone, heat and dissolve at 80°C; add soybean lecithin to 1ml of ethanol, and ultrasonically dissolve for 10min; mix the above two solutions as the organic phase; take another poloxamer solution Use 20ml of water as the water phase, inject the organic phase into the water phase at 80°C with a needle under stirring conditions, keep stirring for 4 hours, evaporate the organic solvent, quickly disperse the suspension into 30ml of water at 0-2°C, and solidify at low temperature for 2 hours. 0.45um microporous membrane filtration, that is. The average particle size of the obtained nanoparticles is: 204.5nm, the potential: -6.8mv

Embodiment 2

[0037] Example 2 Preparation of tripterygium glycosides solid lipid nanoparticles (1 prescription amount)

[0038] Tripterygium glycosides 60mg

[0039] Stearic acid 300mg

[0040]Soy Lecithin 300mg

[0041] Poloxamer 60mg

[0042] Preparation Process:

[0043] Dissolve tripterygium glycosides, stearic acid, and soybean lecithin in absolute ethanol; remove the organic solvent by rotary evaporation under reduced pressure to form a layer of lipid film, dry under reduced pressure overnight, then add the poloxamer aqueous solution, slowly Inject into the above-mentioned lipid film, sonicate for 1 hour, and filter through a 0.45um microporous membrane to obtain the product. The average particle size of the obtained nanoparticles is: 73.8nm Potential: -14.7mv

Embodiment 3

[0044] Example 3 Preparation of tripterygium glycosides solid lipid nanoparticles (1 prescription amount)

[0045] Tripterygium glycosides 60mg

[0046] Glyceryl monostearate 300mg

[0047] Glyceryl Caprylate 200ul

[0048] Soy Lecithin 60mg

[0049] Poloxamer 60mg

[0050] Preparation Process:

[0051] Add tripterygium glycosides to 80°C glyceryl monostearate, soybean lecithin, and glyceryl caprylate mixed lipid liquid; then disperse the hot lipid phase into poloxamer aqueous solution to obtain the initial dispersion, and homogenize under high pressure for 5 ~ 6 cycles, cooling and crystallization at 0 ~ 4 ° C to obtain. The average particle size of the obtained nanoparticles is: 182.7nm Potential: -27.6mv

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Abstract

The invention relates to a preparation method of tripterygium glycosides solid lipid nanoparticle. The preparation method comprises the following steps: dissolving 1 portion of tripterygium glycosidesinto 5 to 15 portions of mixed lipid solution (wherein the ratio of lipin to lipid carrier is 1 to 5) to be used as oil phase; slowing adding the oil phase into a water phase containing 0.5 to 1.5 portions of surface active agent in equal temperature; keeping temperature and stirring; carrying out probe ultrasonography; naturally cooling to obtain primary dispersoid; and freezing and drying to obtain the tripterygium glycosides solid lipid nanoparticle. The nanoparticle is faint yellow, has stable quality with the partical size of 10-200 nm, and can be applied to various routes of administration, such as oral administration and intravenous injection. The preparation method is reliable, has simple and convenient operation and low energy consumption and is suitable for industrial production. Compared with tripterygium glycosides material, the prepared tripterygium glycosides solid lipid nanoparticle has higher dissolvability so as to improve the absorption, improve the bioavailability,enhance the drug action and reduce the toxicity.

Description

technical field [0001] The invention relates to the field of traditional Chinese medicine preparations, in particular to a method for making the effective part of tripterygium wilfordii polyglycoside into solid lipid nanoparticles. Background technique [0002] Tripterygium wilfordii is a plant of the genus Tripterygium wilfordii, which has anti-inflammatory, anti-tumor, immunosuppressive and other activities. It is widely used in clinical treatment of rheumatoid arthritis, chronic nephritis, lupus erythematosus and various skin diseases, but its oral Poor absorption, large gastrointestinal irritation, and many adverse reactions limit its application, and dosage form modification is an effective way to increase its efficiency and reduce its toxicity. Among them, tripterygium glycosides are the most widely used, and it is also believed that tripterygium glycosides are the main pharmacological active ingredients, mainly including a group of active ingredients such as diterpene...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/37A61K9/14A61K47/14A61K47/24A61K47/34A61K47/28A61P29/00A61P35/00A61P37/06A61P31/18
Inventor 张陆勇薛梅江振洲
Owner CHINA PHARM UNIV
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