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Lipophilic medicine hydroxypropyl beta cyclodextrin clathrate preparing method

A technology of β-cyclodextrin and hydroxypropyl, which is applied in the field of preparation of lipophilic drug hydroxypropyl β-cyclodextrin inclusion complex, which can solve the problems of unfavorable human health and unsuitability for industrial production, so as to save energy and increase drug production. Solubility, the effect of simple operation

Inactive Publication Date: 2005-12-21
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Residual organic solvents, some additives, and excess cyclodextrin are harmful to human health
and not suitable for industrial production

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] Take by weighing 20 grams of ketoprofen and dissolve in 2000 ml of tert-butanol, take by weighing corresponding stoichiometric hydroxypropyl β-cyclodextrin (molar ratio is 1:1) and dissolve in drug tert-butanol solution to obtain a single-phase solution, Sterilize by filtration with 0.22um microporous membrane, pack in 5ml vials, 2ml per bottle, freeze in a freeze dryer at -40°C for 4h, turn on the vacuum pump, dry the sample at -30°C for 24h once, and dry the sample at 20°C for the second time Dry for 8 hours and stopper.

[0015] Ketoprofen made hydroxypropyl β-cyclodextrin inclusion compound, the solubility in artificial gastric juice increased by 25.6 times. Promote drug absorption and reduce drug gastrointestinal irritation.

Embodiment 2

[0017] Weigh 10 grams of indomethacin, dissolve hydroxypropyl β-cyclodextrin (molar ratio 1:1) in 500ml tert-butanol, filter and sterilize with a 0.22um microporous membrane, pack in 5ml vials, 2ml per bottle , put it into a freeze dryer at -40°C for 4 hours, turn on the vacuum pump, and dry the sample at -30°C for 24 hours for the first time, and the second drying condition is 20°C for 8 hours, and stoppering.

Embodiment 3

[0019] Weigh 2 grams of hydrocortisone, and dissolve the corresponding stoichiometric hydroxypropyl β-cyclodextrin (molar ratio 1:2) in 200 ml of tert-butanol, pack in 2 ml per bottle, and put it into a freeze dryer at -40°C Freeze for 4h, turn on the vacuum pump, dry the sample at -30°C for 24h once, and dry at 20°C for 8h for the second time, and cover the sample with a stopper.

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PUM

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Abstract

The present invention relates to a preparation method of lipophilic medicine hydroxypropyl beta cyclodextrin inclusion compound. It is implemented in tert-butanol, and it preparation process includes the following steps: dissolving hydroxypropyl beta cyclodextrin in tert-butanol, then making the correspondent stoichiometric medicine by dissolved in hydroxypropyl beta cyclodextrin tert-butanol solution, freeze-drying said solution so as to obtain dried medicine cyclodextrin inclusion compound powder, according to the requirements making said dried medicine cyclodextrin inclusion compound powder into various dosage forms of powder injection, tablet and capsule, etc.

Description

Technical field: [0001] The invention belongs to the technical field of biomedicine, and relates to a method for preparing lipophilic drug hydroxypropyl beta cyclodextrin inclusion compound. Background technique: [0002] Cyclodextrins are natural products of oligosaccharides linked by α-1,4 glycosidic bonds. β-cyclodextrin is composed of 7 glucose molecules connected with a hollow cavity, the cavity is hydrophobic, and the cavity is hydrophilic. The entire molecule or lipophilic structure of lipophilic drugs can enter the cavity of cyclodextrin, so that the water-soluble Increased, facilitated absorption, improved bioavailability. However, β-cyclodextrin is limited in its application due to its low water solubility (1.85g / 100ml) and nephrotoxicity. Hydroxypropyl β-cyclodextrin is an amorphous hydrophilic derivative formed by condensation of β-cyclodextrin and 1,2-propylene oxide, with a solubility of >50% (w / v). Hydroxypropyl β-cyclodextrin has low nephrotoxicity, low...

Claims

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Application Information

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IPC IPC(8): A61K47/40
Inventor 王志宣邓英杰张晓鹏
Owner SHENYANG PHARMA UNIVERSITY