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Koumine transdermal patch and preparation method thereof

A technology of transdermal patch and kombucha, which can be applied in the directions of anti-inflammatory agents, pharmaceutical formulations, non-central analgesics, etc., and can solve the problems such as the formulation of kokisu which has not yet been seen.

Pending Publication Date: 2021-06-11
FUJIAN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no dosage form for transdermal administration of kinesin

Method used

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  • Koumine transdermal patch and preparation method thereof
  • Koumine transdermal patch and preparation method thereof
  • Koumine transdermal patch and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0112] Embodiment 1: the preparation of the transdermal patch of prescription 1-3

[0113] Weigh 0.92% by weight of kelezin (content in the drug storage layer), dissolve it with ethyl acetate and vortex mix. Add the ethyl acetate solution of kelezin to the pressure-sensitive adhesive DURO-TAK87-4098, DURO-TAK 87-4287 or DURO-TAK 87-2677, and stir at room temperature for 0.5h to make the drug and the pressure-sensitive adhesive Mix well, then ultrasonically degas for 2min. The obtained mixture was uniformly coated on a transparent anti-adhesive film, left to stand for 10 minutes, and then baked at 60° C. for 15 minutes. Lay it with the backing layer after letting it cool, and cut out an area of ​​8cm 2 , to obtain the keloid transdermal patch of prescription 1-3. In vitro transdermal experiments were carried out on the transdermal patches of prescriptions 1-3 to test their transdermal properties.

[0114] Table 1: Composition of drug reservoir layers for formulations 1-3

...

Embodiment 2

[0119] Embodiment 2: the preparation of the patch of prescription 4-13

[0120] In addition to including the step of adding a penetration enhancer to the pressure-sensitive adhesive, according to the method described in Example 1, according to the composition shown in Table 2, transdermal patches (8cm 2 / paste), and in vitro transdermal experiments were carried out on the obtained transdermal patches to test their transdermal properties (Js, Q 24h and t lag ). The results are shown in figure 2 and Table 3 and Table 6.

[0121] Table 2: Composition of drug reservoir layers for formulations 4-13

[0122]

[0123]

[0124] The results showed that 15% by weight of azone as a penetration enhancer achieved the best transdermal performance (prescription 7). However, the inventors have found that the adhesive force of the patch of prescription 7 is too large (peel strength greater than 0.6kN / m), which makes it difficult to remove the release layer and is not suitable for ...

Embodiment 3

[0125] Embodiment 3: the preparation of the transdermal patch of prescription 14 and 15

[0126] By the same method as Example 1, according to the composition shown in Table 4, the transdermal patches (8cm 2 / paste), and in vitro transdermal experiments were carried out on the patches of prescriptions 2, 14 and 15 to test their transdermal properties (Js, Q 24h and t lag ). The results are shown in image 3 and Table 6.

[0127] Table 4: Composition of drug reservoirs for formulations 2, 14 and 15

[0128] prescription number pressure sensitive adhesive Penetration enhancer Gelskin content single patch dosage 2 DURO-TAK 87-4287 none 0.92% by weight 2mg 14 DURO-TAK 87-4287 none 1.83% by weight 4mg 15 DURO-TAK 87-4287 none 3.59% by weight 8mg

[0129] The results showed that the transdermal delivery effect of kelezin was basically positively correlated with its content in the drug storage layer.

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Abstract

The invention relates to a koumine transdermal patch and a preparation method thereof, in particular to a transdermal patch of koumine or pharmaceutically acceptable salts thereof and a preparation method of the transdermal patch. The transdermal patch can be used for the treatment of diseases or conditions treatable by koumine, including but not limited to rheumatoid arthritis.

Description

technical field [0001] The invention relates to a transdermal drug delivery system of kelezin alkaloid monomer kelezin, in particular to a transdermal patch of kelezin or a pharmaceutically acceptable salt thereof and a preparation method thereof. Background technique [0002] Gelsemium elegans is a monomer with the highest content among the alkaloids extracted from Gelsemium elegans Benth., and its toxicity is much lower than that of the total alkaloids of Gelsemium elegans. [0003] Kelsin can be used to treat various diseases or conditions. Chinese patent application CN109953991A discloses the use of kinesin in the treatment of amyloid deposition and / or tauopathy-related diseases or conditions (such as Alzheimer's disease). CN109893528A discloses the use of kelezin in treating lipid metabolism disorders and related diseases or diseases. CN103690539B discloses the use of kelezin for treating diabetic complications. CN103619333A discloses the use of kelezin for treating ...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K31/439A61P25/28A61P3/06A61P3/10A61P19/02A61P37/02A61P25/22A61P29/00A61P25/00
CPCA61K31/439A61K9/7084A61P25/28A61P3/06A61P3/10A61P19/02A61P37/02A61P25/22A61P29/00A61P25/00
Inventor 俞昌喜苏燕评吕文祥杨渐许盈黄慧慧
Owner FUJIAN MEDICAL UNIV