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Tripterine nano structure lipid carrier and preparation method and application thereof

A technology of nanostructured lipids and tripterine, applied in liposome delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc.

Inactive Publication Date: 2011-10-26
JIANGSU PROVINCE INST OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no research report on tripterygine nanostructured lipid carrier that can treat psoriasis, rheumatoid arthritis, skin cancer and breast cancer by transdermal administration

Method used

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  • Tripterine nano structure lipid carrier and preparation method and application thereof
  • Tripterine nano structure lipid carrier and preparation method and application thereof
  • Tripterine nano structure lipid carrier and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Preparation of tripterine nanostructured lipid carrier

[0032] Prescription: take tripterine 60mg, monoglyceride 450mg, caprylic / capric glyceride 150mg, phospholipid 60mg, vitamin E polyethylene glycol succinate 60mg, poloxamer (1%, w / v) 150mL.

[0033] Preparation process: heat and melt monoglyceride at 80°C, then add caprylic / capric glycerides, phospholipids, vitamin E polyethylene glycol succinate and tripterine, fully dissolve and stir vigorously (4000r / min) Disperse the molten liquid into 150mL aqueous phase containing poloxamer (1%, w / v) at the same temperature to obtain colostrum, and emulsify the colostrum through a high-pressure homogenizer (500bar), and circulate for 3- 6 times; then cooling and solidifying in a low-temperature water phase (0-2° C.) to obtain tripterine nanostructured lipid carrier. The average particle size of the obtained nanoparticles is: 102.3nm, the electric potential is -38.7mv, the encapsulation efficiency is 97.4%, and the drug load...

Embodiment 2

[0035] Preparation of tripterine nanostructured lipid carrier lyophilized powder

[0036]Add 5% mannitol to the obtained tripterine nanostructured lipid carrier suspension prepared in Example 1 and freeze-dry. The resulting freeze-dried powder has good redispersibility. After redispersing, the particle diameter of nanoparticles, Potential is almost constant.

Embodiment 3

[0038] Preparation of tripterine nanostructured lipid carrier ointment

[0039] The tripterygine nanostructured lipid carrier lyophilized powder prepared in Example 2 was pulverized and passed through a 60-mesh sieve for later use. Take 335040g of polyethylene glycol and 40060g of polyethylene glycol, mix and heat to 65°C on a water bath, add 5g of vitamin E and 5g of sorbic acid, stir until condensed, and obtain a water-soluble ointment base. Add the sieved tripterine nanostructured lipid carrier into the above-mentioned matrix, and stir evenly to obtain.

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Abstract

The invention relates to the field of Chinese medicine preparation, in particular to a method for preparing tripterine nano structure lipid carrier containing traditional Chinese medicine monomer and application of the tripterine nano structure lipid carrier in preparation of transdermal drugs used for treating psoriasis, rheumatoid arthritis, skin cancer and breast cancer. The tripterine nano structure lipid carrier is characterized by comprising the following components in parts by weight: 1 part of tripterine, 5-100 parts of mixed lipid, 0.5-10 parts of phospholipid, 0.1-15 parts of poloxamer-188 and 0.5-10 parts of vitamin E and tocopherol polyethylene glycol succinate, wherein the mixed lipid is composed of solid lipid monoglycerine and liquid lipid octylic acid / caprin according to the weight ratio of 1: 0.1-10: 1. Tripterine is prepared into the nano structure lipid carrier, the tripterine nano structure lipid carrier in a semi-solid or liquid preparation form is applied in a transdermal way, bioavailability of the tripterine can be improved, toxic response of tripterine can be reduced, and the nano structure lipid carrier provided by the invention has great clinical application value in the improvement of the treatment effect of tripterine.

Description

technical field [0001] The present invention relates to the field of traditional Chinese medicine preparations, specifically tripteryglide, a triterpenoid monomer component of the traditional Chinese medicine Tripterygium wilfordii, is made into a nanostructured lipid carrier, a preparation method of the nanostructured lipid carrier and a transdermal method used in the preparation. Application of route of administration in the treatment of psoriasis, rheumatoid arthritis, skin cancer and breast cancer. Background technique [0002] Tripterine is a pentacyclic triterpene quinone compound isolated and purified from Triperygium Wilfordii Hook f. Molecular formula: C 29 h 38 o 4 , molecular weight: 450.61, CAS number: 34157-83-0, structural formula: [0003] Tripteryglide is insoluble in water, but easily soluble in dimethyl sulfoxide, chloroform, acetone and ether. It has strong immune response suppression, anti-inflammatory and anti-cancer effects, and can be used for a...

Claims

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Application Information

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IPC IPC(8): A61K47/34A61K47/24A61K47/14A61K9/127A61K31/56A61P17/06A61P19/02A61P29/00A61P35/00
Inventor 陈彦张振海周蕾吴青青
Owner JIANGSU PROVINCE INST OF TRADITIONAL CHINESE MEDICINE
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