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Beta-cyclodextrin inclusion compound of huperzine A, and preparation method and preparation thereof

A technology of cyclodextrin inclusion compound and huperzine A, which is applied in the field of β-cyclodextrin inclusion compound of huperzine A and its preparation, can solve the problem of high cost, unguaranteed product yield and quality, The preparation steps are cumbersome and other problems

Inactive Publication Date: 2011-03-30
上海复旦复华药业有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Therefore, the technical problem to be solved in the present invention is aimed at the defects that existing huperzine A solid preparations have uneven huperzine A content, cumbersome preparation steps, high cost, and unguaranteed product yield and quality. A huperzine A preparation and a preparation method thereof. The active ingredient huperzine A of the huperzine A preparation has a uniform content of huperzine A, and the huperzine A is stable and difficult to degrade; the preparation method has simple steps, reduced raw material loss, reduced cost and stable process Reliable, suitable for high-volume industrial production

Method used

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  • Beta-cyclodextrin inclusion compound of huperzine A, and preparation method and preparation thereof
  • Beta-cyclodextrin inclusion compound of huperzine A, and preparation method and preparation thereof
  • Beta-cyclodextrin inclusion compound of huperzine A, and preparation method and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Take 0.5g of Huperzine A and dissolve it in 20.0ml of 95% medicinal ethanol. Take another 10.0g of β-cyclodextrin, add 50ml of purified water, stir and heat to 80°C to dissolve all, cool to 40°C, slowly add the above-mentioned Huperzine A / ethanol solution within 15 minutes under stirring, Continue stirring for 30 minutes, cool to 0°C, refrigerate for 12 hours, filter with a filter cloth, and dry to obtain 9.85 g of β-cyclodextrin inclusion compound of Huperzine A. The average yield is based on the weight of β-cyclodextrin. Is 98.5%. The average recovery rate of Huperzine A was 98%.

[0046] Calculation formula:

[0047] Average yield = weight of inclusion compound ÷ weight of β-cyclodextrin feed × 100%.

[0048] Average recovery rate = weight of the inclusion compound × weight percentage of Huperzine A in the inclusion compound ÷ feed weight of Huperzine A × 100%.

[0049] The "inclusion compound" mentioned in these two formulas refers to the "β-cyclodextrin inclusion compou...

Embodiment 2

[0051] Take 0.5g of Huperzine A and dissolve it in 20.0ml of 95% medicinal ethanol. Take another 10.0g of β-cyclodextrin, add 50ml of purified water, stir and heat to 80°C to dissolve it completely, cool to 40°C, and slowly add the above-mentioned Huperzine A / ethanol solution within 20 minutes under stirring. Continue stirring for 30 minutes. Take another 20g starch, add 230g water to disperse, heat to 80°C and stir to form a slurry, cool to 40°C, mix with Huperzine A's β-cyclodextrin solution under stirring, and spray dry to obtain Huperzine A The β-cyclodextrin inclusion compound / starch mixture 29.55g. The average yield (based on the weight of the sum of β-cyclodextrin and starch) was 98.5%. The average recovery rate of Huperzine A was 98.5%.

[0052] Calculation formula:

[0053] Average yield=mixture weight÷(β-cyclodextrin weight+starch weight)×100%.

[0054] Average recovery rate = weight of mixture x weight percentage of Huperzine A in the mixture ÷ feeding amount of Huper...

Embodiment 3

[0057] Prescription: Huperzine A for medicinal use 0.5g

[0058] 95% ethanol medicinal 20.0ml

[0059] β-cyclodextrin medicinal 10.0g

[0060] 8% starch slurry medicinal 250g (starch 20g)

[0061] Starch medicinal 379.5g

[0062] Lactose medicinal 580.0g

[0063] Magnesium stearate medicinal 10.0g

[0064] Process: According to the prescription, take Huperzine A and dissolve it with 95% medicinal ethanol. Take another β-cyclodextrin, add 50ml purified water, stir and heat to 80℃ to dissolve it completely, cool to 40℃, add Huperzine A / ethanol solution under stirring, continue stirring for 30 minutes to obtain Huperzine A The β-cyclodextrin inclusion compound solution. Take another 20g starch, add 230g purified water to disperse, heat to 80°C and stir to form a slurry, cool to 40°C, and mix with Huperzine A's β-cyclodextrin inclusion compound solution under stirring to obtain slurry. Boiling granulation, controlling the inlet air temperature to 60°C, ...

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Abstract

The invention discloses a beta-cyclodextrin inclusion compound of huperzine A, and a preparation method and preparations thereof. The beta-cyclodextrin inclusion compound of the huperzine A consists of 2.5 to 9.5 weight percent of huperzine A and 97.5 to 90.5 weight percent of beta-cyclodextrin. The preparation method comprises the following steps of: a) dissolving the huperzine A in an pharmaceutically acceptable organic solvent to prepare solution A, and heating and dissolving the beta-cyclodextrin in water to prepare solution B; and b) slowly adding the solution A into the solution B with stirring, and continuing to perform stirring until the mixed solution is uniform to prepare the beta-cyclodextrin inclusion compound of the huperzine A. The beta-cyclodextrin inclusion compound of the huperzine A further can be mixed with water-soluble carriers with viscosity, such as starch and the like, and then is pelletized, tabletted or filled into capsules with substrates. In the method, an extremely small amount of water-insoluble huperzine A is fully, effectively and uniformly dispersed, so the dissolution rate of the huperzine A is increased and the stability of the huperzine A is improved. The provided beta-cyclodextrin inclusion compound of the huperzine A can be used for preparing solid preparations and liquid preparations, operating steps are reduced and the production cost is remarkably reduced.

Description

Technical field [0001] The invention belongs to the field of pharmaceutical preparations, and particularly relates to a β-cyclodextrin inclusion compound of Huperzine A, and a preparation method and preparation thereof. Background technique [0002] Huperzine A (Huperzine A), alias Haberin, chemical name: (5R, 9R, 11E)-5-amino-11-ethylidene-5,6,9,10-tetrahydro-7-methyl -5,9-Methylcyclooctano(b)pyridine-2(1H)one; molecular formula: C 15 H 18 N 2 O; Molecular weight: 242.32; Structural formula: [0003] [0004] Huperzine A is a white or off-white crystalline powder; odorless, slightly bitter taste; hygroscopic. Melting point: 230°C, optical rotation: -150.4°, easily soluble in methanol, soluble in ethanol, but insoluble in water; slightly soluble in 0.01mol / L hydrochloric acid solution. [0005] Huperzine A is the earliest alkaloid extracted from natural plant Melaleuca (Huperzinaserrata (Thumb.) Trev] in China. It has obvious anti-cholinesterase activity and is selective for true c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K47/38A61K47/36A61K47/32A61K9/20A61K9/48A61K31/4748A61P25/28A61P21/04A61P9/10A61P21/00A61P25/00A61K47/61A61K47/69
Inventor 朱泽龙任昉
Owner 上海复旦复华药业有限公司
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