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Huperzine a lyotropic liquid crystal preparation and preparation method thereof

A technology of huperzine A and lyotropic liquid crystal, which is applied in pharmaceutical formulations, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc. , the effect of slowing down the speed and reducing the frequency of administration

Active Publication Date: 2017-07-07
武汉百纳礼康生物制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Nowadays, in order to exert the efficacy of huperzine A, huperzine A is directly prepared into tablets, capsules or injections, but as a strong fat-soluble drug, huperzine A needs to be used every day, and patients with poor memory often suffer from Physical discomfort caused by forgetting to take medicine or multiple injections

Method used

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  • Huperzine a lyotropic liquid crystal preparation and preparation method thereof
  • Huperzine a lyotropic liquid crystal preparation and preparation method thereof
  • Huperzine a lyotropic liquid crystal preparation and preparation method thereof

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preparation example Construction

[0036] The present invention also provides a preparation method of the huperzine A lyotropic liquid crystal preparation described in the technical scheme, comprising: mixing the huperzine A, an organic solvent, phospholipid and oil to obtain a huperzine A lyotropic liquid crystal preparation .

[0037] In the present invention, the mixing is preferably: (1) mixing the huperzine A with an organic solvent to obtain a huperzine A solution; (2) mixing the huperzine A solution with the phospholipid and oil .

[0038] In the present invention, the huperzine A is mixed with an organic solvent to obtain a huperzine A solution, and then mixed with phospholipids and oils, which helps the composition to be uniformly dispersed inside when used as a preparation and improves the uniformity of the preparation.

[0039] The present invention has no special requirements on the mixing method of the huperzine A and the organic solvent, and the mixing method known to those skilled in the art can...

Embodiment 1

[0045] Weigh 3 mg of huperzine A, 0.075 g of absolute ethanol, 0.2975 g of soybean lecithin and 0.1275 g of glyceryl dioleate.

[0046] Above-mentioned huperzine A is placed in the non-transparent glass vial of 5ml black cover, then add 0.075g dehydrated alcohol to dissolve, then add 0.2975g soybean lecithin (SPC) and 0.1275g glyceryl dioleate (GDO) successively, in Wrap the glass vial with aluminum foil at room temperature and rotate it on a rotational rheometer at a speed of 15 rpm for 12 hours to obtain the huperzine A lyotropic liquid crystal preparation.

Embodiment 2

[0048] Prepare huperzine A lyotropic liquid crystal according to the mode of embodiment 1, the difference with embodiment 1 is that the quality of huperzine A is 3mg, the quality of dehydrated alcohol is 0.075g, the quality of soybean lecithin is 0.255g, two The mass of glyceryl oleate is 0.17g.

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Abstract

The invention provides a huperzine a lyotropic liquid crystal preparation and a preparation method thereof. The huperzine a lyotropic liquid crystal preparation is prepared from the following components in parts by weight: 0.12 to 0.7 part of huperzine a, 10 to 18 parts of organic solvent, 12 to 70 parts of phospholipid, and 12 to 59.5 parts of grease. According to the huperzine a lyotropic liquid crystal preparation provided by the invention, the phospholipid, the grease and the organic solvent are used as carriers of the huperzine a, so that the solubleness of the huperzine a is effectively improved, the defect that the huperzine a is insoluble in water is overcome, the pharmacological function of the huperzine a is played favorably; meanwhile, under the condition of the limited component proportion, the huperzine a lyotropic liquid crystal preparation encounters water to form a lyotropic liquid crystal after being injected into a human body, so that the adhesion of a medicine and the preparation is improved, the medicine diffusion speed is retarded, the administration period is increased, the administration times are reduced, and thus the compliance of a patient is greatly improved.

Description

technical field [0001] The invention relates to the technical field of pharmacy, in particular to a huperzine formazine-induced liquid crystal preparation and a preparation method thereof. Background technique [0002] Huperzine A is a highly active natural semiterpene alkaloid extracted from the fern Huperzine serrata, the English name is Huperzine-A, and its chemical name is (5R,9R,11E)-5-amino-11-sub Ethyl-5,8,9,10-tetrahydro-7-methyl-5,9-methylenecyclooctatetra[b]pyridin-2-(1H)-one with the formula C 15 h 18 N 2 O, white or off-white crystalline powder, easily soluble in chloroform, methanol or ethanol, slightly soluble in water, is a highly selective and reversible acetylcholinesterase inhibitor with high therapeutic index and long acting time. It has no toxic and side effects, and has good curative effect on senile dementia and Alzheimer's disease. [0003] Nowadays, in order to exert the efficacy of huperzine A, huperzine A is directly prepared into tablets, capsu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/4748A61K47/24A61K47/10A61K47/14A61P25/28
CPCA61K9/0002A61K9/0087A61K31/4748A61K47/10A61K47/14A61K47/24
Inventor 罗亮郭偲刘宏孟凡玲周萌萌
Owner 武汉百纳礼康生物制药有限公司
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