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Theophylline chitin micro-balls slow-release preparation, and its preparation method

A technology of sustained-release preparations and chitosan, which is applied in the direction of bulk delivery, respiratory diseases, and active ingredients of heterocyclic compounds, can solve the problems of theophylline’s microsphere preparations, such as less reports, and reduce the incidence and side effects

Inactive Publication Date: 2009-06-10
INST OF PROCESS ENG CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the sustained-release preparations of theophylline are usually tablets and coating agents, and the microsphere preparations of theophylline are rarely reported.

Method used

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  • Theophylline chitin micro-balls slow-release preparation, and its preparation method
  • Theophylline chitin micro-balls slow-release preparation, and its preparation method
  • Theophylline chitin micro-balls slow-release preparation, and its preparation method

Examples

Experimental program
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Effect test

Embodiment 1

[0026] 5 g of chitosan (molecular weight: 150,000, degree of deacetylation: 95.7%) was dissolved in 100 mL of 0.2 mol / L acetic acid solution to prepare a chitosan solution. Take 10 mL of this solution and disperse into 25.2 mg of theophylline to form an aqueous phase. Take 50mL of liquid paraffin (oil phase) and add it to the reactor, add 0.5mL of Span 80 and 0.5mL of Tween 85, stir at a speed of 500 rpm, and disperse for 10 minutes. Chitosan solution (water phase), continued to stir and disperse for 30 minutes with the same rotating speed, formed stable emulsion; In this emulsion, add the ammonium sulfate solution 40mL that concentration is 10% (w / v), stop after continuing to stir for 3 hours . Centrifuge, pour out the upper liquid, and separate the ammonium sulfate-precipitated microspheres in the lower layer, wash the precipitates with pure water, petroleum ether, and absolute ethanol in turn, and dry them in vacuum at room temperature to obtain the theophylline-embedded s...

Embodiment 2

[0033] 3g of chitosan (molecular weight: 550,000, degree of deacetylation: 86.3%) was dissolved in 100mL of 0.25mol / L lactic acid solution to prepare a chitosan solution. Take 10mL of this solution and disperse into 60.5mg of theophylline to form an aqueous phase. Get 80mL peanut oil (oil phase) and join in the reactor, add 0.5mL Span 80, the rotating speed is 1000 revs / min, after dispersing for 10 minutes, add the chitosan solution (water phase) that above-mentioned preparation is dispersed with theophylline, After continuing to stir and disperse at the same rotation speed for 30 minutes, add 100 mL of ammonium sulfate solution with a concentration of 30% (w / v), and continue stirring for 2 hours before stopping. After centrifugal separation, the precipitate is fully washed with pure water, petroleum ether and absolute ethanol in turn, and vacuum-dried at room temperature to obtain the chitosan microspheres embedded with theophylline of the present invention. The diameter of ...

Embodiment 3

[0036] 4g chitosan (molecular weight 810,000, deacetylation degree 72.7%) was dissolved in 100mL0.25mol / L propionic acid solution to prepare chitosan solution. Take 10mL of this solution and dissolve it into 100.5mg of theophylline to form an aqueous phase. Take 100mL soybean oil (oil phase) and add it to the reactor, add 0.5mL Span 20 and 0.5mL Tween 81, stir at a speed of 1200 rpm, and disperse for 10 minutes, then add the theophylline dispersion prepared above Chitosan solution (water phase), after continuing to stir and disperse for 30 minutes with the same rotating speed, add the ammonium sulfate solution 200mL that concentration is 50% (w / v), stop after continuing to stir for 1 hour. After centrifugal separation, the precipitate is fully washed with pure water, petroleum ether and absolute ethanol in turn, and vacuum-dried at room temperature to obtain the chitosan microspheres embedded with theophylline of the present invention. The diameter of the chitosan microsphere...

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Abstract

A slow-releasing theine-chitosan microball for treating chronic bronchitis and chronic asthma is prepared through dispersing theine in chitosan solution, adding the oil-phase substance containing surfactant, stirring, adding the aqueous solution of ammonium sulfate, stirring, depositing, separating, washing and vacuum drying.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations of medical engineering, and in particular relates to a slow-release preparation of chitosan microspheres of theophylline and a preparation method thereof. Background technique [0002] Among the common respiratory diseases, chronic bronchitis and bronchial asthma are intractable chronic diseases that are recurrent and difficult to cure. Modern medicine believes that the disease is related to infection, allergy, and decreased immune function. Theophylline is the drug of choice for the treatment of this disease. However, the therapeutic index of theophylline is narrow, and its effective blood concentration is 10-20 μg / mL, which cannot play a therapeutic role below this concentration range, while the blood concentration of more than 20 μg / mL is likely to cause cardiovascular system and central nervous system damage. System side effects. In addition, the biological half-life of theophyllin...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/522A61K9/16A61P11/00
Inventor 李巧霞宋宝珍
Owner INST OF PROCESS ENG CHINESE ACAD OF SCI
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