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Prepn process of cyclodextrin inclusion for lipophilic medicine

A cyclodextrin inclusion complex and lipophilic technology, applied in the field of biomedicine, can solve problems such as instability and poor water solubility, and achieve the effects of convenient operation, short cycle, and improved solubility and stability

Inactive Publication Date: 2005-12-14
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

To solve the poor water solubility and instability of lipophilic drugs, the difficulties faced in the preparation of clathrates

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Weigh 10 grams of ketoprofen and dissolve it in 500 ml of tert-butanol, weigh the corresponding stoichiometric hydroxypropyl β-cyclodextrin (molar ratio is 1:1) and dissolve it in 500 ml of water, mix the aqueous solution and the tert-butanol solution , 0.22um microporous membrane filtration sterilization, 5ml vials, 2ml per bottle, put into a freeze dryer at -40°C for 4h, turn on the vacuum pump, dry the sample at -30°C for 24h once, and the second drying condition is 20°C Dry at ℃ for 8h, and stopper.

Embodiment 2

[0022] Weigh 10 grams of indomethacin and dissolve it in 500ml of tert-butanol, weigh the corresponding stoichiometric β-cyclodextrin (molar ratio is 1:1) and dissolve it in 600ml of water, mix the aqueous solution and tert-butanol solution, Sterilize by filtration with carbonate 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 at 20°C for 8h for the second time. Cork.

Embodiment 3

[0024] Weigh 2 grams of hydrocortisone and dissolve it in 100 ml of tert-butanol, weigh the corresponding stoichiometric β-cyclodextrin (molar ratio is 1:2) and dissolve it in 300 ml of water, mix the aqueous solution and tert-butanol solution, and separate Pack, 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, dry at 20°C for 8h for the second time, and cover the sample.

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PUM

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Abstract

The present invention is the preparation process of new cyclodextrin inclusion of lipophilic medicine, and solves the problem in preparing inclusion of lipophilic medicine with poor water solubility and lower stability. The preparation process completed inside co-solvent system of tert-butyl alcohol and water includes the following steps: dissolving the lipophilic medicine and cyclodextrin as including material separately in tert-butyl alcohol and water, mixing the obtained two kinds of solution to obtain single phase solution, and drying the mixed solution to obtain powder of cyclodextrin inclusion of lipophilic medicine. The present invention may prepare powder for injection, injection, tablet, capsule or other form. The present invention has simple preparation process, easy operation, short preparation period, low power consumption and no organic solvent residue, and is suitable for industrial production.

Description

Technical field: [0001] The invention belongs to the technical field of biomedicine and relates to a preparation method of a lipophilic drug cyclodextrin inclusion compound. Background technique: [0002] Cyclodextrin is a class of pharmaceutical excipients that can improve the physicochemical properties and biopharmaceutical properties of drugs. Because of its lipophilic cavity and hydrophilic surface, the drug and cyclodextrin are separated by lipophilic force and van der Waals force. , The effect of hydrogen bond forces, making the drug molecule or part of the molecular structure enter the lipophilic cavity of the cyclodextrin to form an inclusion compound. Therefore, the hydrophilicity, stability and absorption of the drug are improved, and the bioavailability is improved. These advantages have been confirmed in many drug cyclodextrin inclusion studies. [0003] Lipophilic drugs have low bioavailability and poor efficacy due to their poor water solubility. Especially s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/40
Inventor 王志宣邓英杰张晓鹏
Owner SHENYANG PHARMA UNIVERSITY
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