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Rutaecarpin transdermal patch and preparation method thereof

A technology of evodiamine and transdermal patch, which is applied in the field of formula and preparation of transdermal patch, and can solve the problem of not contacting clothing, avoiding contact with water, sweat, poor adhesion, poor stability, etc. problems, to achieve the effect of reducing the number of medications, stable quality, and good flexibility

Active Publication Date: 2016-03-16
ZUNYI MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The traditional application of Evodia rutaecarpa acupoint application is powder application, which has the disadvantages of poor stability, poor adhesion, easy to scatter, temporary preparation, and large randomness, which limits its clinical efficacy.
Chinese patent CN100431547 discloses evodiamine ointment and gel, which are used for local treatment of psoriasis on the skin, and this preparation belongs to the topical preparation, mainly used for local skin treatment, and its application is limited by many factors For example, it is best not to contact with clothes after use, avoid contact with water, sweat, etc., when using it, there are still many inconveniences

Method used

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  • Rutaecarpin transdermal patch and preparation method thereof
  • Rutaecarpin transdermal patch and preparation method thereof
  • Rutaecarpin transdermal patch and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-3

[0026] Prepare evodiamine transdermal patch, which is composed of a backing layer, a drug-containing adhesive layer and a protective layer, and its preparation method is as follows:

[0027] Accurately weigh the prescribed amount of pressure-sensitive adhesive, add appropriate amount of evodiamine dispersed in ethyl acetate, stir evenly, add penetration enhancer, mix evenly, and degas. Control the thickness of the coating, so that the drug-containing pressure-sensitive adhesive is evenly coated on the protective film, stand at room temperature to evaporate the solvent, heat and cure, cover with a backing film, and cut to obtain the Evodiaecarpine transdermal patch.

[0028] Table 1 embodiment 1-3 prescription (weight percentage %)

[0029]

[0030] *: Duro-Tak87-2677 solid content is 38.0% (WT), Duro-Tak87-4098 solid content is 33.0% (WT), Duro-Tak87-2852 solid content is 33.5% (WT), the same below.

[0031] **: The part removed during final drying, the same below.

Embodiment 3-9

[0033] Evodiacarpine transdermal patch was prepared, which consisted of a backing layer, a drug-containing adhesive layer and a protective layer, and its preparation method was the same as in Examples 1-3.

[0034] Table 2 embodiment 3-9 prescription (weight percentage %)

[0035]

Embodiment 10-13

[0037] Evodiacarpine transdermal patch was prepared, which consisted of a backing layer, a drug-containing adhesive layer and a protective layer, and its preparation method was the same as in Examples 1-3.

[0038] Table 3 embodiment 10-13 prescription (weight percentage %)

[0039]

[0040] *: The data in brackets are the data of drug loading converted without solvent.

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Abstract

The invention provides a rutaecarpin transdermal patch which is composed of a backing layer, a medicine-containing adhesion layer and an anti-adhesion layer. The medicine-containing adhesion layer is composed of rutaecarpin, transdermal penetration enhancer and pressure-sensitive adhesive; the transdermal penetration enhancer is formed by mixing and using one or more of alcohol, fatty acid and esters of fatty acid, surface active agents, terpene, terpene, amino acid and ester or phospholipid compounds of amino acid, or combined penetration enhancer of oleic acid and azone; the pressure-sensitive adhesive is one of polyisobutylene class pressure-sensitive adhesive, silicone class pressure-sensitive adhesive, polyacrylic resin class pressure-sensitive adhesive or cellulose. The preparation method of the rutaecarpin transdermal patch includes the steps that medicine-containing adhesive is prepared; solvent is picked to disperse rutaecarpin, the pressure-sensitive adhesive is added and stirred to be uniform, then the penetration enhancer is added and stirred uniformly, and degassing is conducted for standby use; obtained medicine-containing adhesive liquid is arranged on the anti-adhesion layer in a coated mode, the coating thickness is controlled accurately, the anti-adhesion layer stands still at the room temperature to remove solvent and is heated, cured, coated with a backing film and cut, and the rutaecarpin transdermal patch is obtained.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to a formula of a transdermal patch containing evodiamine and a preparation method thereof. Background technique [0002] Evodiarutaecarpa (Juss.) Benth., Evodiarutaecarpa (Juss.) Benth.var.officinalis (Dode) Huang or Evodiarutaecarpa (Juss.) Benth.var.officinalis (Dode) Huang Dried near-ripe fruit of Evodiarutaecarpa (Juss.) Benth.var.bodinieri (Dode) Huang. Evodiamine and evodiamine, the main active ingredients in Evodia rutaecarpa, have pharmacological effects such as dilating blood vessels, lowering blood pressure, anti-tumor, anti-inflammation, and analgesia. Relevant studies have shown that evodiamine is an insoluble drug with low oral absorption and extremely low bioavailability (oral bioavailability of evodiamine in Beagle dogs is 0.089%), which greatly limits its clinical application. Evodia rutaecarpa powder vinegar is externally applied to Zuxin Yongquan acupoint, which nourishes ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K31/519A61K47/12A61K47/22A61P1/02A61P11/04A61P9/12A61P17/06
CPCA61K9/7023A61K31/519A61K47/12A61K47/22
Inventor 王森欧水平雷小娟
Owner ZUNYI MEDICAL UNIVERSITY
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