Cyclovirobuxine D solid dispersion preparation method and novel medical application thereof

A technology of Cyclovitamin and solid dispersion, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., which can solve the problems of low intestinal mucosal permeability and improve solubility and intestinal mucosal permeability, significant technological progress and innovation, and the effect of improving bioavailability

A technology of Cyclovitamin and solid dispersion, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., which can solve the problems of low intestinal mucosal permeability and improve solubility and intestinal mucosal permeability, significant technological progress and innovation, and the effect of improving bioavailability

CN109078002AInactive Publication Date: 2018-12-25JILIN ACAD OF TRADITIONAL CHINESE MEDICINE
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  • Cyclovirobuxine D solid dispersion preparation method and novel medical application thereof
  • Cyclovirobuxine D solid dispersion preparation method and novel medical application thereof
  • Cyclovirobuxine D solid dispersion preparation method and novel medical application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0089] Example 1 , the preparation of ring-dimensional buxicine D

[0090] 5 kg of Euonymus microphylla was crushed into coarse powder, refluxed and extracted 3 times with 80% ethanol containing 2% glacial acetic acid, each time for 2 hours, combined the extracts, added 0.2% active carbon of the liquid volume, stirred, filtered, and the filtrate decompressed and recovered ethanol to obtain Extract, add water to dissolve, so that each 1ml contains 1g of medicinal materials, centrifuge, take the supernatant, pass through D001-CC macroporous strong acid cation exchange resin, first elute with 15% ethanol for 5 times the volume of the resin, and then adjust the pH with ammonia water Elute 5 times the volume of the resin with 70% ethanol of 11, collect the eluate of ammonia ethanol, recover the solvent, dry under reduced pressure, and obtain the composition with Cyclovirubuxin D as the main component. The content of cyclovirboxicin D in the composition is 83.5%. Take 1.0 g of the...

Embodiment 2

[0091] Example 2 , Preparation of Cycloviral Buxusine D Solid Dispersion

[0092] Take 10g of Cycloviral Buxillus D, 60g of PEG6000, and 5g of sodium caprate; dissolve Cycloviral Buxusin D in 500ml of ethanol, then add PEG6000 to dissolve completely, add the absorption-promoting agent sodium caprate, and then under reduced pressure The solvent was removed by rotary evaporation, dried by heating, pulverized and sieved.

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Abstract

The invention relates to fields of chemical pharmacy, pharmaceutical preparations, pharmacokinetics and pharmacodynamics and discloses a solid dispersion prepared from cyclovirobuxine D extracted fromBuxus micr ophylla Sieb.et Zucc.var.sinica Rehd.et Wils. and congeners and application of the solid dispersion to prevention and treatment of senile dementia. According to enzymological and animal experiments, the cyclovirobuxine D solid dispersion has a great senile dementia prevention and treatment function. According to further researches, activity of the cyclovirobuxine D solid dispersion isremarkably improved as compared with that of cyclovirobuxine D. The cyclovirobuxine D solid dispersion has the advantage that the a preparation method is simple, convenient and easy in operation, thecyclovirobuxine D solubility and intestinal mucosa permeation rate are greatly increased, and accordingly bioavailability is improved.

Description

technical field [0001] The invention relates to the fields of chemical pharmacy, pharmaceutical preparations, pharmacokinetics and pharmacodynamics, in particular to a solid dispersion of cyclovirbuxine D and its application in the treatment of senile dementia. Background technique [0002] Alzheimer's is a degenerative disease of the central nervous system. It is mainly manifested in the middle-aged and old age with progressive memory impairment and intellectual loss, memory impairment, abstract thinking disorder, language disorder, behavior and direction disorder and other symptoms. Its pathogenesis is not very clear, it is a very complicated process of nerve and cell aging. Therefore, the prevention and treatment of Alzheimer's disease is still a worldwide problem. At present, the prevention of Alzheimer's disease is basically based on the pathological characteristics, which can be divided into anti-β-amyloid protein deposition drugs, cholinomimetic drugs, acetylcholine...

Claims

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Application Information

Patent Timeline
25 Dec 2018
Publication
CN109078002A
IPC
A61K9/14; A61K31/57; A61K47/10; A61K47/38; A61K47/32; A61K47/26; A61P25/28
CPC
A61K9/146; A61K31/57; A61P25/28
Inventors
南敏伦; 赫玉芳