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Transdermal administration composite containing cucurbitacin-type active ingredient

A technology of active ingredients and cucurbitacins, applied in the field of medicine, can solve problems such as drug absorption disorder, affecting effective blood drug concentration, etc., and achieve the effect of good compliance

Active Publication Date: 2010-01-13
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, not all active substances are suitable for transdermal drug preparations, because the skin of a normal person, as the outermost tissue of the human body, has the function of protecting the body from the invasion of various harmful substances in the external environment. This skin absorption barrier and the distribution of the drug to the subcutaneous layer will affect the effective blood concentration of the drug entering the systemic circulation.
In addition, the dose and concentration of the drug, molecular size and lipid solubility, pH and pK a etc. also pose a challenge to whether the active substance can be made into a transdermal drug delivery preparation

Method used

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  • Transdermal administration composite containing cucurbitacin-type active ingredient
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  • Transdermal administration composite containing cucurbitacin-type active ingredient

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1 : In vitro transdermal permeability research method of cucurbitacin active ingredients.

[0027] The experimental method of the effect of pretreatment of animal skin in vitro on the drug permeability with different transdermal permeation enhancers is as follows: the device used in the experiment is a horizontal diffusion cell, such as figure 1 shown. Take healthy male Wistar rats, cut off the mouse hair on the abdominal skin after anesthesia, trim carefully with a razor, peel off the skin, spread it on a smooth plate with the cuticle down, remove the subcutaneous fat and adhesions, and use Rinse with normal saline repeatedly, cut into appropriate size, and freeze for later use. Before the experiment, visually check the integrity of the mouse skin, and there must be no damage. Take the spare mouse skin to thaw naturally, sandwich it between the two half-cells of the diffusion cell, with the cuticle facing the administration cell, add 5% ethanol solution of p...

Embodiment 2

[0031] Example 2 : Cucurbitacin B gel with oleic acid as transdermal penetration enhancer

[0032] Cucurbitacin B gel was prepared by using different amounts of oleic acid as a percutaneous penetration enhancer. The prescription is shown in Table 1. The preparation method is as follows: Carbomer is fully swollen with some water, and the pH value is adjusted to 6-6 by adding an appropriate amount of triethanolamine. 7. Add 1,2-propanediol and stir well to form a viscous gel matrix; mix EDTA-Na 2 Dissolve with a small amount of water, add to the above gel matrix, and stir well; add ethanol to the gel, stir evenly, then add the prescribed amount of oleic acid as a percutaneous penetration enhancer and an appropriate amount of stabilizer, add water to the prescribed amount , stir well; under continuous stirring, add cucurbitacin B powder into the above-mentioned gel matrix, and stir until the drug is dissolved.

[0033] Table 1. The prescription of cucurbitacin B gel when the p...

Embodiment 3

[0036] Example 3 : Cucurbitacin B gel with azone as a transdermal penetration enhancer

[0037] Cucurbitacin B gel was prepared by using different amounts of azone as a percutaneous penetration enhancer. The prescription is shown in Table 2. The preparation method was the same as in Example 2 except that azone was used instead of oleic acid.

[0038] Table 2. The prescription of cucurbitacin B gel whose percutaneous penetration enhancer is azone and its 24-hour cumulative permeation through the isolated skin of rats

[0039]

[0040]

[0041] The gel prepared according to the above prescription and process is a colorless transparent or translucent, slightly milky white viscous gel with a mellow taste. The 24-hour cumulative drug penetration through the isolated skin of rats is shown in Table 2. The test results show that azone has the best percutaneous penetration when the dosage is 1%.

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Abstract

The invention relates to a transdermal administration composite containing cucurbitacin-type active ingredient. The transdermal transparent accelerator in the transdermal administration preparation of the cucurbitacin-type active ingredient is one or more composites of oleic acid, azone, eucalyptus oil, or isopropyl myristate and the like, and the dosage of the transdermal transparent accelerator is 0.1 to 50%, and 0.3 to 30% is preferred. The transdermal administration of cucurbitacin-type active ingredient can adopt liquid or semisolid preparation of gels, emulsion, ointment, solution agent, micro-emulsion, ethosomes or nebula and the like, or emplastrum such as patch, cataplasma and the like. After the transdermal administration of the preparations, the active ingredient can be absorbed by skin continuously and enter into human body to play a therapeutic role for a long while, the patient adaptability is significantly better than oral administration medication, therefore, the transdermal administration composite can be used for preventing and curing of hepatitis, cancer and other diseases and improving quality life of patients.

Description

technical field [0001] The invention relates to the technical field of medicine, relates to a transdermal composition containing cucurbitacin active ingredients, in particular to a transdermal composition for preventing or treating hepatitis or cancer. Background technique [0002] It has been reported in the literature that cucurbitacin components have multiple therapeutic activities, among which multiple components have cytotoxicity, hepatoprotective effect, anti-inflammatory effect, cardiovascular effect and antidiabetic effect (seeing Jayaprakasam B, et al., Anticancer and anti -Inflammatory activities of cucurbitacins from Cucurbita andreana. Cancer Lett, 2003, 189: 11-16. and Yesilada E, et al., Isolation of ananti-inflammatory principle from the fruit juice of Ecballium elaterium. J NatProd, 1988, 51: 504- 508.). In recent years, research reports have confirmed that: cucurbitacin B, D, E and I can inhibit the growth of some cancer cell lines, and inhibit cyclooxygena...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/575A61P1/16A61P35/00
Inventor 徐晖邓意辉盛秋双
Owner SHENYANG PHARMA UNIVERSITY
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