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Tetrandrine composition, preparation method of tetrandrine composition, external tetrandrine preparation, and preparation method and application of external tetrandrine preparation

A technology of tetrandrine and topical preparations, applied in the field of preparation of tetrandrine topical preparations and tetrandrine compositions, which can solve problems such as low bioavailability, poor targeting, and renal toxicity, and achieve good therapeutic effects , Solubility improvement, and the effect of reducing toxic and side effects

Pending Publication Date: 2020-03-06
UNIVERSITY OF MACAU
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, a large number of tetrandrine on the market are tablets, injections, etc. The above-mentioned drugs have problems such as large amount of use in clinical practice, poor solubility, low bioavailability, poor targeting and high renal toxicity.

Method used

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  • Tetrandrine composition, preparation method of tetrandrine composition, external tetrandrine preparation, and preparation method and application of external tetrandrine preparation
  • Tetrandrine composition, preparation method of tetrandrine composition, external tetrandrine preparation, and preparation method and application of external tetrandrine preparation
  • Tetrandrine composition, preparation method of tetrandrine composition, external tetrandrine preparation, and preparation method and application of external tetrandrine preparation

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preparation example Construction

[0060] The embodiment of the present invention also provides a preparation method of a tetrandrine composition, comprising: mixing an oil phase, an emulsifier and an emulsifier, and then mixing with a tetrandrine and a water phase to form the tetrandrine composition.

[0061] Specifically, the oil phase, emulsifier and co-emulsion agent are uniformly mixed at a temperature of 40-60° C., and then tetrandrine is added to the above mixture and stirred until the tetrandrine is dissolved.

[0062] Then heat the water phase to 40-60°C, then add the water phase to the mixture of oil phase, emulsifier, co-emulsion agent and tetrandrine, stop heating, and continue stirring to room temperature (generally 25°C).

[0063] The embodiment of the present invention also provides a preparation method of an external preparation of tetrandrine. When the external preparation of tetrandrine is a gel, the preparation method comprises: mixing the above-mentioned tetrandrine composition with the swoll...

Embodiment 1

[0071] This embodiment provides a tetrandrine composition, which includes 0.015 g of the tetrandrine composition, 1 g of Labrafil M1994CS, 0.5 g of PEG4000, 151 g of SolutolHS, and 7.5 g of ultrapure water.

[0072] The present embodiment also provides a gel containing the above tetrandrine composition, which contains 1 gram of LabrafilM1994CS, 0.5 grams of PEG4000, 151 grams of SolutolHS, 7.5 grams of ultrapure water and carbomer 974N, wherein carbomer is present in the gel The mass content in is 0.8%, and the pH of the gel is 7.

[0073] This embodiment also provides a preparation method of tetrandrine composition, comprising:

[0074] Mix LabrafilM1994CS, SolutolHS15 and PEG400 evenly in a beaker with magnetic stirring, in a constant temperature water bath at 50°C, add tetrandrine powder, and continue stirring until the powder dissolves. The prepared ultrapure water was preheated to 50°C, added dropwise to the above mixture, the heating in the water bath was stopped, and t...

Embodiment 2- Embodiment 3

[0079] The gel is prepared according to the preparation method of Example 1. The consumption of each substance in the tetrandrine composition is the same as in Example 1, the difference is that the mass content of Carbomer 974N in the gel is different, and in Example 2, Carbomer The mass content of 974N is 1.2%, and the mass content of Carbomer 974N in Example 3 is 1.6%.

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Abstract

The invention relates to the field of medicines, in particular to a tetrandrine composition, a preparation method of the tetrandrine composition, an external tetrandrine preparation, and a preparationmethod and application of the external tetrandrine preparation. The tetrandrine composition comprises the following components in parts by weight: 0.005-0.015 part of tetrandrine, 1 part of an oil phase, 0.5 part of an emulsifier, 7-8 parts of a water phase and 1 part of a co-emulsifier. According to the invention, the emulsifier, the co-emulsifier, the oil phase and the like are utilized to enable the tetrandrine composition to become nanoemulsion, so that the solubility of the tetrandrine is improved, the retention amount of the tetrandrine on skin is increased, the toxic and side effects of the tetrandrine are reduced, and the economic cost of the tetrandrine composition is low. Meanwhile, the tetrandrine composition has good effects of inhibiting desquamation, erythema, epidermal thickening and the like of psoriasis vulgaris by inhibiting expression of related inflammatory factors.

Description

technical field [0001] The invention relates to the field of medicines, in particular to a tetrandrine composition, a preparation method thereof, an external preparation of tetrandrine, a preparation method thereof and an application thereof. Background technique [0002] Psoriasis is a chronic skin inflammatory disease, commonly known as psoriasis. It is clinically divided into four types, vulgaris, pustular, arthropathy and erythrodermic psoriasis. Among them, psoriasis vulgaris is more common, mainly manifested as thickened skin scales at the lesions, forming plaques, covered with white scales, often accompanied by rash. So far, there is no clinical method that can completely cure psoriasis. Patients with mild to moderate psoriasis usually take chemical drugs or traditional Chinese medicine compound treatment, which can be cured in a short period of time but are prone to relapse; patients with severe psoriasis are usually treated with antibody drugs. The curative effect...

Claims

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Application Information

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IPC IPC(8): A61K31/4748A61K9/06A61K47/44A61K47/14A61P17/06
CPCA61K9/0014A61K9/06A61K31/4748A61K47/14A61K47/44A61P17/06
Inventor 陈新郑颖陈少魁林子贝
Owner UNIVERSITY OF MACAU
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