Nasal administration gel preparation for treating brain diseases

A technology of gel preparation and nasal administration, which is applied in the direction of blood diseases, antiviral agents, and extracellular fluid diseases, etc., to achieve the effects of improving compliance, obvious slow-release effect, and improving bioavailability

Active Publication Date: 2011-12-21
JIANGXI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, there is no report on the nasal administration gel preparation of geniposide or gardenia to

Method used

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  • Nasal administration gel preparation for treating brain diseases
  • Nasal administration gel preparation for treating brain diseases
  • Nasal administration gel preparation for treating brain diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0244] Embodiment 1 geniposide nasal administration gel preparation

[0245] 1) Weigh 5 g of geniposide, 16 g of poloxamer 407, 0.9 g of sodium chloride, and 0.2 g of ethylparaben;

[0246] 2) Dissolve geniposide, sodium chloride, and ethylparaben in water, add poloxamer 407 while stirring to make the dispersion uniform, and place it at 4°C for 24 hours to make the gel fully swell and disperse evenly to obtain The clear solution is filled into a nasal cavity inhalation device and made into a spray, that is, ready.

Embodiment 2

[0247] Embodiment 2 geniposide nasal administration gel preparation

[0248] 1) Weigh 2.5g of geniposide, 18g of poloxamer 407, 5g of poloxamer 188, 0.9g of sodium chloride, and 0.2g of ethylparaben;

[0249] 2) Dissolve geniposide, sodium chloride, and ethylparaben in water, add Poloxamer 407 and Poloxamer 188 while stirring to make the dispersion uniform, and place it at 4°C for 24 hours to make the gel Fully swell and disperse to obtain a clear solution, put it into a nasal cavity inhalation device, and make it into a spray.

Embodiment 3

[0250] The preparation of embodiment 3 gardenia total iridoid glycosides

[0251] Take 1 kg of gardenia coarse powder, add 6 times of water to decoct 3 times, each time for 30 minutes, filter, combine the decoction, concentrate to 1000 ml of thick paste (each 1 ml is equivalent to 1 g of medicinal materials), add 730 ml of 95% ethanol to contain Alcohol content 40%, stand for 24 hours, take the supernatant, recycle ethanol, concentrate to 500ml of thick cream with no alcohol smell (each 1ml is equivalent to 2g of medicinal materials), add 2700ml of 95% ethanol to alcohol content of 80%, stand for 24 hours, Filter, the filtrate is concentrated to a relative density of 1.05 to 1.10 (60° C.), and dried to obtain 130 g of dry cream. The content of total iridoid glycosides of geniposide is determined to be 55% by ultraviolet spectrophotometry, and the content of total iridoid glycosides of geniposide is determined by high-performance liquid phase. The glycoside content is 26.8%.

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Abstract

The invention discloses a nasal drug delivery gel preparation for curing cerebral diseases. Water is used as solvent in the preparation. The preparation includes geniposide or total iridoid glycoside of cape jasmine fruit, poloxamer 407 and poloxamer 188. The phase transformation temperature of the preparation is 25-35 DEG C. Based on the weight of the preparation, the geniposide or total iridoid glycoside of cape jasmine fruit is 1-5%; the poloxamer 407 is 16-18%; the poloxamer 188 is 0-5%; preferably, based on the weight of the preparation, the preparation is composed of 2% of the geniposide, 16% of the poloxamer 407, 2.5% of the poloxamer 188, 0.2% of ethylparaben, 0.9% of sodium chloride and the balance of water; and the phase transformation temperature of the preparation is 25-33 DEG C. According to the preparation disclosed by the invention, the gel preparation has proper phase transformation temperature by adjusting kinds and proportions of gelling matrixes in the preparation; after the gel preparation is sprayed in a nasal cavity in the form of solution so that gel is rapidly formed under a body temperature condition, therefore, the contact time of the geniposide or total iridoid glycoside of cape jasmine fruit and nasal mucosa is increased; and the distribution of drugs in brain tissue is increased.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a gel preparation for nasal cavity administration which uses geniposide or total iridoid glycosides of Gardenia jasminoides as active ingredients and has a suitable phase transition temperature for treating brain diseases. It exists in the form of solution at room temperature, enters the nasal cavity, and forms a gel rapidly after contacting the nasal mucosa. Background technique [0002] Gardenia has the effects of clearing heat, purging fire, cooling blood, and detoxifying. It is often used in the treatment of heat syndrome in traditional Chinese medicine. Modern research has found that the total iridoid glycosides of Gardenia jasminoides represented by Geniposide is one of the main active ingredients of Gardenia jasminoides. Geniposide pure product is white powder, molecular formula: C 17 h 24 o 10 , Molecular weight: 388.366. Geniposide is easily so...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K31/7048A61K36/744A61K47/34A61K9/12A61P25/00A61P7/04A61P7/02A61P9/10A61P9/00A61P31/12
Inventor 杨明张海燕汪建民陈晓燕宋伟胡鹏翼
Owner JIANGXI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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