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Octanedioyl benzohydroxamic acid cyclodextrin clathrate liposome

A technology for inclusion complex of suberoylanilide hydroxime and cyclodextrin, which is applied in the application field of pharmaceutical preparations, can solve the problems of slow onset, poor water solubility of suberoylanilide hydroxamic acid and the like, and achieves delayed release , Improve the drug-to-lipid ratio, increase the effect of stability

Inactive Publication Date: 2012-04-04
EVERYTHING BEIJING MEDICAL TECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Suberoylanilide hydroxamic acid has poor water solubility and is a weakly acidic drug. It can only be absorbed at the lower end of the gastrointestinal tract after oral administration, and its onset is slow. Therefore, increasing the water solubility of suberoylanilide hydroxamic acid is beneficial to improve The bioavailability and efficacy of drugs are very necessary for the development of new dosage forms and better clinical applications

Method used

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  • Octanedioyl benzohydroxamic acid cyclodextrin clathrate liposome
  • Octanedioyl benzohydroxamic acid cyclodextrin clathrate liposome
  • Octanedioyl benzohydroxamic acid cyclodextrin clathrate liposome

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Embodiment 1

[0039] The formula that present embodiment adopts is as follows:

[0040] Suberoylanilide hydroxamic acid 10mg

[0041] Hydroxypropyl-β-cyclodextrin 150mg

[0042] Lecithin 200mg

[0043] Cholesterol 60mg

[0044] Weigh the prescribed amount of suberoylanilide hydroxamic acid and hydroxypropyl-β-cyclodextrin, first dissolve the hydroxypropyl-β-cyclodextrin in an appropriate amount of water to form a saturated solution, control the temperature at about 60°C, Stir constantly. Suberoylanilide hydroxamic acid is ground with a small amount of alcohol, slowly added dropwise to the above-mentioned cyclodextrin saturated solution with constant stirring, filtered, and the filtrate is vacuum-dried. Dissolve the prepared suberoylanilide hydroxamic acid clathrate together with the prescribed amount of lecithin and cholesterol in an appropriate amount of chloroform, remove the solvent by rotary evaporation under reduced pressure at 50°C, and continue rotary evaporation under reduced pr...

Embodiment 2

[0046] The formula that present embodiment adopts is as follows:

[0047] Suberoylanilide hydroxamic acid 20mg

[0048] Dimethyl-beta-cyclodextrin 350mg

[0049] Lecithin 280mg

[0050] Weigh the prescribed amount of suberoylanilide hydroxamic acid and dimethyl-β-cyclodextrin, dissolve suberoylanilide hydroxamic acid in an appropriate amount of methanol, blow dry with nitrogen stream to remove the solvent, and dissolve the cyclodextrin Saturated aqueous solution was added to the above dried drug film, and the dispersion of the clathrate was centrifuged at 70,000 g for 60 min, the unclad precipitate in the lower layer was filtered off, and the filtrate was dried. Wet the prepared suberoylanilide hydroxamic acid inclusion compound with a small amount of water, vortex mix with phospholipids at 60°C for 2 minutes, add appropriate amount of water to dilute, freeze-dry, add a small amount of water to the freeze-dried solid, hydrate at high speed Centrifuge (12000rpm × 10min), tak...

Embodiment 3

[0052] The formula that present embodiment adopts is as follows:

[0053] Suberoylanilide hydroxamic acid 12mg

[0054] Hydroxypropyl-β-cyclodextrin 180mg

[0055]Soy Lecithin 240mg

[0056] Cholesterol 70mg

[0057] Vitamin C 5mg

[0058] Mannitol 22mg

[0059] pH adjusted to 6.5-8.0

[0060] Water for injection to the full amount of 1000ml

[0061] Weigh the prescribed amount of suberoylanilide hydroxamic acid and hydroxypropyl-β-cyclodextrin, first dissolve the hydroxypropyl-β-cyclodextrin in an appropriate amount of water for injection to form a saturated solution, and control the temperature at about 60 °C, stirring continuously. Suberoylanilide hydroxamic acid is ground with a small amount of alcohol, slowly added dropwise to the above-mentioned cyclodextrin saturated solution with constant stirring, filtered, and the filtrate is vacuum-dried. Dissolve the prepared suberoylanilide hydroxamic acid clathrate together with the prescribed amount of lecithin and chole...

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Abstract

The invention relates to a novel octanedioyl benzohydroxamic acid cyclodextrin clathrate liposome, a preparation method thereof, and an application thereof in medicine preparations. The octanedioyl benzohydroxamic acid cyclodextrin clathrate liposome provided by the invention is composed of an active component octanedioyl benzohydroxamic acid, a cyclodextrin clathration agent, and a phospholipid material. Preferably, the octanedioyl benzohydroxamic acid cyclodextrin clathrate liposome comprises cholesterol. The invention also provides a method for preparing the octanedioyl benzohydroxamic acid cyclodextrin clathrate liposome, and an octanedioyl benzohydroxamic acid intravenous infusion composition. The octanedioyl benzohydroxamic acid cyclodextrin clathrate liposome provided by the invention is advantaged in good stability, and provides functions of medicine releasing delaying, toxicity reducing, treatment effect improving, and the like.

Description

technical field [0001] The invention relates to a new suberoylanilide hydroxamic acid cyclodextrin inclusion complex liposome, a preparation method of the inclusion complex liposome and its application in pharmaceutical preparations. Background technique [0002] Suberoylanilide hydroxamic acid is a histone deacetylase inhibitor antineoplastic drug with the molecular formula C 14 h 20 N 2 o 3 , the molecular weight is 264.33, and the structure is as follows: [0003] [0004] The chemical name is N-hydroxy-N'-phenylsuberamide, it is white to light yellow powder, non-hygroscopic, insoluble in dichloromethane, very slightly soluble in water, slightly soluble in ethanol, isopropanol and acetone, soluble in In methanol, easily soluble in dimethyl sulfoxide. [0005] Acetylation of histones is a master regulator of gene expression by altering the proximity of transcription factors to DNA to activate gene expression. The inhibition of histone deacetylase gene expression p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/24A61K47/28A61K47/48A61K31/167A61P35/00
Inventor 韩南银郑玉刚曹红辉徐超群陈鑫朱靖华
Owner EVERYTHING BEIJING MEDICAL TECH DEV
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