Transdermal therapeutic system of huperzine A and derivatives thereof

A technology of huperzine A and a treatment system, applied in the field of treatment systems, can solve the problems of limiting the clinical application of HA and the inability of patients to take continuous medication, and achieves the effect of avoiding first-pass effect and improving compliance

Inactive Publication Date: 2021-08-31
YANTAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Oral administration of HA does not have hepatotoxicity and is relatively safe for clinical application, but long-term use is prone to adverse reactions such as nausea and vomiting in the gastrointestinal tract, which makes some patients unable to take continuous medication; in addition, AD patients often forget to eat due to memory loss and mental decline. Drugs, or take more medicines, take the wrong medicine, which further limits the clinical application of HA to a certain extent

Method used

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  • Transdermal therapeutic system of huperzine A and derivatives thereof
  • Transdermal therapeutic system of huperzine A and derivatives thereof
  • Transdermal therapeutic system of huperzine A and derivatives thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] The huperzine A transdermal patch for treating senile dementia of the present invention is prepared by the following prescription:

[0027]

[0028] Preparation process: Mix acrylate-vinyl acetate copolymer, ethyl acetate and huperzine A evenly, and use it for the coating of the active layer. A homogeneous coating of the active layer was applied on the siliconized membrane ("intermediate liner"), dried at 70° C. / 20 minutes, and covered with polyvinyl chloride. Weigh the silicone pressure sensitive adhesive adhesive and add the ethyl acetate, titanium dioxide, polyvinylpyrrolidone, and glycerin with stirring and stir until homogeneous for coating of the adhesive layer. A homogeneous coat of the adhesive layer was applied to the release layer and dried at 85°C / 5 minutes. The dried adhesive matrix is ​​laminated to the medicated adhesive matrix of the active layer while removing the intermediate liner to prepare the final laminate. Transdermal patches of appropriate s...

Embodiment 2

[0030] The composition of the prescription is as follows:

[0031]

[0032] Preparation process: uniformly mix polypropylene ester, ethanol and huperzine A salt, and use it for the coating of the active layer. A homogeneous coating of the active layer was applied to the siliconized membrane ("intermediate liner"), dried at 70°C / 20 minutes, and covered with polyethylene. Weigh the silicone pressure sensitive adhesive adhesive and add the ethanol, silicon dioxide, polyvinylpyrrolidone and neutral oil with stirring and stir until homogeneous for coating of the adhesive layer. A homogeneous coat of the adhesive layer was applied to the release layer and dried at 85°C / 5 minutes. The dried adhesive matrix is ​​laminated to the medicated adhesive matrix of the active layer while removing the intermediate liner to prepare the final laminate. Transdermal patches of appropriate size are punched out from the final laminate obtained.

Embodiment 3

[0034] The composition of the prescription is as follows:

[0035]

[0036]

[0037] Preparation process: uniformly mix polyisobutene, ethanol and huperzine A hydrate, and use it for the coating of the active layer. A homogenous coating of the active layer was coated on the siliconized membrane ("intermediate liner"), dried at 70°C / 20 minutes, and covered with polypropylene. Weigh the silicone pressure sensitive adhesive adhesive and add the ethanol, silicon dioxide, polyvinylpyrrolidone and neutral oil with stirring and stir until homogeneous for coating of the adhesive layer. A homogeneous coat of the adhesive layer was applied to the release layer and dried at 85°C / 5 minutes. The dried adhesive matrix is ​​laminated to the medicated adhesive matrix of the active layer while removing the intermediate liner to prepare the final laminate. Transdermal patches of appropriate size are punched out from the final laminate obtained.

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PUM

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Abstract

The invention discloses a transdermal therapeutic system of huperzine A and derivatives thereof. A patch disclosed by the invention is safe, non-irritating and non-allergic to skin, and long in drug action time, so that the administration frequency is reduced. The medicine can be continuously released for a long time, the peak valley phenomenon of blood concentration caused by oral administration is avoided, the first-pass effect of the liver and degradation of the medicine in the gastrointestinal tract are avoided, the transdermal therapeutic system is suitable for patients who fall asleep, do not react or cannot swallow the oral medicine (the compliance of the patients is improved), and administration can be interrupted at any time when side effects are found.

Description

technical field [0001] The invention belongs to the field of therapeutic systems, and mainly relates to a transdermal therapeutic system (Transdermal Therapeutic System, TTS) of huperzine A and its derivatives. Background technique [0002] Alzheimer's disease (AD) is a chronic neurodegenerative disease first discovered by German psychiatrist and neurologist Alzheimer Alois in 1906 and named after him. The main clinical manifestations of AD are gradual loss of memory, cognitive dysfunction, abnormal behavior and social barriers, etc., which will lead to the complete loss of the patient's ability to perform activities of daily living, bring a heavy burden to society and families, and become a serious social and medical health problem. . Alzheimer's disease is an important cause of disease that threatens the health of the elderly after cardiovascular disease, cerebrovascular disease and tumors. [0003] "World Alzheimer's Disease Report 2018" reported that China's elderly po...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K47/34A61K47/32A61K47/10A61K31/4748A61P25/28
CPCA61K9/7069A61K9/7053A61K9/7023A61K31/4748A61P25/28
Inventor 由春娜李铭安王天
Owner YANTAI UNIV
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