Huperzine and its derivant or its salt implantation agent, its preparation method and application

A technology of huperzine A and an implant is applied in the directions of medical preparations containing active ingredients, drug delivery, and drug combinations, which can solve the problems of inability to take medicines on time, low bioavailability, etc. The preparation process is simple and the effect of reducing toxic and side effects

Inactive Publication Date: 2008-08-20
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Based on the consideration of the above-mentioned problems, the present invention provides an implant of huperzine A and its derivatives or its salts. After one administration, the drug can be slowly decomposed and corroded by the continuous decomposition and erosion of biodegradable polymer materials. The ground is released into the b

Method used

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  • Huperzine and its derivant or its salt implantation agent, its preparation method and application
  • Huperzine and its derivant or its salt implantation agent, its preparation method and application
  • Huperzine and its derivant or its salt implantation agent, its preparation method and application

Examples

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Example Embodiment

[0047] Example 1

[0048] A long rod-shaped mold was prepared with dimethylsiloxane (PDMS), and the PDMS mold was soaked in acetone for 0.5h to fully infiltrate the surface. Dissolve 18 g of PLGA in 100 ml of acetone at 30°C, pour the solution on a PDMS mold, dry at 60°C for 2 hours, and after sufficient cooling, peel off the PDMS mold, take out the PLGA cavity, and add 150 mg of Huperzine A. At both ends of the cavity, take 1g of PLGA film and heat-press and encapsulate it to form a solid implant of Huperzine A. Use the conductivity method to test its tightness. That is, the drug-containing implant is put into quantitative deionized water, and the change in the current value is detected after stirring. If the current value increases to a fixed value after inserting the implant, it means that the device is leaking and it is a substandard product.

Example Embodiment

[0049] Example 2

[0050] The PDMS was soaked in acetone for 0.5h to fully wet the surface to serve as a rod-shaped mold. Dissolve PLA10g and PLGA 15g in a mixed solvent of 100ml acetone and 20ml dichloromethane at 30°C, pour the solution on the PDMS mold, dry at 60°C for 2h, after sufficient cooling, peel off the PDMS mold and take out the PLGA cavity , Add 200mg of Huperzine A. At both ends of the cavity, 4g PLGA film was hot-pressed and encapsulated to make a solid implant of Huperzine A. And use the conductivity method to test its tightness.

Example Embodiment

[0051] Example 3

[0052] The PDMS was soaked in acetone for 1 hour to fully infiltrate it as a rod-shaped mold. Dissolve PLA20g and PLGA10g in a mixed solvent of 100ml chloroform and 80ml tetrahydrofuran at 30°C, pour the solution on the PDMS mold, dry at 45°C for 6h, and after sufficient cooling, peel off the PDMS mold, take out the PLGA cavity, and add 600mg Huperzine A. At both ends of the cavity, 9g PLGA film was hot-pressed and encapsulated to make a solid implant of Huperzine A. And use the conductivity method to test its tightness.

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Abstract

The invention provides an implantable dosage for huperzine-a and the derivatives or the salt, which comprises essentially huperzine-a, the derivatives or the salt, and macromolecule accessories. The invention is characterized in that the solid implantable dosage of the huperzine-a and the derivatives or the salt can be conveyed into the body by way of implant surgery; or the solution or gel of the implantable dosage of the huperzine-a and the derivatives or the salt are injected into the body to form semi-solid or gel implanted object. When used to cure senile diseases such as alzheimer disease and vascular dementia, The implantable dosage has the advantages of lengthened drug treating time, reduced times for drug taking, enhanced bioavailability of the huperzine-a and the derivatives or the salt, decreased poison and side effects of the drug, and greatly enhanced drug compliance of the patients.

Description

technical field [0001] The invention relates to implants of huperzine A and its derivatives or salts thereof, their preparation method and application. Background technique [0002] Huperzine A (Huperzine A), chemical name: (5R,9R,11E)-5-amino-11-ethylene-5,6,9,10-tetrahydro-7-methyl-5,9 -Methylene cycloaryl octane-2(1H)-pyridone, which is an alkaloid obtained from the phenolic part extracted from the Chinese herbal medicine Melaleuca [Huperzia serrata(Thunb)Thev], is a high-efficiency, low-toxicity and reversible acetylcholinesterase inhibitors (AChEI). In 1993, the US FDA approved it as a cholinergic agent. Pharmacological tests have proved that huperzine A and some of its derivatives are effective for treating Alzheimer's disease, vascular dementia and other senile dementias. Huperzine A and its derivatives involved in the present invention are respectively the following structures: [0003] [0004] With the improvement of today's living standards and the increasi...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/439A61P25/28
Inventor 李亚平顾王文陈伶俐
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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