Lappaconitine Hydrobromide transdermal gel and the preparing method thereof

A technology of homogenin hydrobromide and gel, which is applied in the field of pharmacy, can solve the problems of high quality injections, inconvenient use, and painful injections, so as to avoid the first-pass effect of the gastrointestinal tract and meet the needs of treatment. The effect of reducing side effects

Inactive Publication Date: 2007-10-31
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Injections have high quality requirements, and the preparation process requires specific conditions and equipment. The production cost is high, the price is high, the use is inconvenient, and the injection is painful.

Method used

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  • Lappaconitine Hydrobromide transdermal gel and the preparing method thereof
  • Lappaconitine Hydrobromide transdermal gel and the preparing method thereof
  • Lappaconitine Hydrobromide transdermal gel and the preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Sprinkle 0.1g carbomer evenly on the surface of an appropriate amount of distilled water, let it stand still, make it fully swell, and make carbomer hydrogel, dissolve 0.2g homogenin hydrobromide in 2ml ethanol, add carbomer Stir while adding, then slowly add 0.06g triethanolamine dropwise to make it into a gel, add distilled water to 10g, stir to make a uniform transparent gel. The following operations are the same as in Example 1. The permeation rate is 2.81μg / cm 2 h. Fig. 2 is the drug cumulative penetration-time curve (time is hours) of this embodiment.

Embodiment 2

[0034] Sprinkle 0.05g carbomer evenly on the surface of an appropriate amount of distilled water, let it stand still, make it fully swell, and make carbomer hydrogel, dissolve 0.1g homogenin hydrobromide in 0.5ml ethanol, add to In the carbomer hydrogel, stir while adding, then slowly add 0.03g triethanolamine dropwise to make it into a gel, add distilled water to 5g, stir to make a uniform transparent gel. The following operations are the same as in Example 1. The permeation rate is 1.11μg / cm 2 h. Fig. 3 is the drug cumulative penetration-time curve (time is hours) of this embodiment.

Embodiment 3

[0036] Sprinkle 0.05g of carbomer evenly on the surface of an appropriate amount of distilled water, let it stand still, make it fully swell, and make carbomer hydrogel, dissolve 0.1g of homogenate hydrobromide in 1.5ml of ethanol, and add it to In the carbomer hydrogel, stir while adding, then slowly add 0.03g triethanolamine dropwise to make it into a gel, add distilled water to 5g, stir to make a uniform transparent gel. The following operations are the same as in Example 1. The permeation rate is 0.64μg / cm 2 h. Fig. 4 is the cumulative drug penetration-time curve (time is hours) of this embodiment.

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Abstract

The invention discloses a hydrobromic acid high ebony nail element transdermal gelling agent, which comprises the following steps: allocating 0. 5-2. 5% hydrobromic acid high ebony nail element, 0-3% transdermal absorption promoting agent, 1-3% jel host material, 8-40% alcohol and surplus as water; adding water into jel host material; swelling; dissolving hydrobromic acid high ebony nail element into alcohol; getting solution; adding the solution into the host material; mixing evenly; adding into transdermal absorption promoting agent; choosing water to quantitative; stirring continuously; getting the even and transparent jel. This invention possesses good skin penetrability, which can be used to ease pain percutaneous administer drug treatment.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to a homogenine hydrobromide transdermal gel. Background technique [0002] Homoconitine hydrobromide is the hydrobromide salt of Lappaconitine, an alkaloid extracted from Aconitum sinomoutanum Nakai, a plant of the Ranunculaceae family. The molecular weight is 683.64, the melting point is 217-221°C, soluble in methanol, slightly soluble in water and ethanol, hardly soluble in organic solvents such as chloroform, and its molecular structure formula is: [0003] [0004] Hokine hydrobromide is mainly used clinically for the treatment of moderate pain, postoperative pain and intractable pain, especially cancer pain. It is the first non-addictive analgesic in China. Its analgesic strength is equivalent to that of morphine and 7 times that of aminopyrine. It has a long acting time and is not addictive. Long-term use will not cause physical dependence. Side effects (sedation, dry mouth, swea...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/439A61K9/00A61P25/04
Inventor 高建青钟韵伟吴争梁文权
Owner ZHEJIANG UNIV
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