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Method for preparing carrier of hollow microsphere for medication in use for treating gastrointestinal tract

A gastrointestinal tract, hollow technology, applied in the field of preparation of hollow microsphere carrier, can solve the problems of cumbersome operation, low drug encapsulation rate, and few applications

Inactive Publication Date: 2008-10-22
魏郁梦
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The latter two are rarely used in practice due to their cumbersome operations.
The water / oil type requires the carrier material used to have good solubility in water, which limits the choice of materials
When the water-soluble drug microspheres are prepared by the oil / water method, the drug rapidly partitions from the oil phase to the water, resulting in a very low drug encapsulation efficiency
The oil / oil type can be used for the preparation of both hydrophobic drugs and hydrophilic drugs. In the existing literature reports, most of them use methanol, dichloromethane, chloroform and other toxic drugs. Organic solvents are used as solvents to prepare hollow microsphere carriers, which will cause great harm to the human body

Method used

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  • Method for preparing carrier of hollow microsphere for medication in use for treating gastrointestinal tract
  • Method for preparing carrier of hollow microsphere for medication in use for treating gastrointestinal tract

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach 1

[0035] Dissolve 0.6g ethyl cellulose 10 centipoise (EC10cp) in the mixed solvent that 6.0ml ethanol and 1.0ml ether are prepared, make the mixed solution that concentration is 8.6% (g / ml) as dispersed phase, keep this dispersion The temperature of the phase is 25°C; another 50ml of liquid paraffin is added and added to 0.75g Span-80, stirred evenly and then kept at 25°C as the continuous phase, with a concentration of 1.5% (g / ml); the dispersed phase is slowly added to the continuous phase, and Stir at 300rpm / min until ethanol and ether are completely volatilized, while maintaining the temperature of the entire reaction process at 25°C; filter the solid under reduced pressure, wash the solid with 10ml of n-hexane, and dry the solid at room temperature under vacuum. A hollow microsphere carrier is obtained. The in vitro floating test proves that the hollow microspheres can sustainably float for 48 hours in the artificial gastric juice.

Embodiment approach 2

[0037]Ethanol and ether are formulated into a mixed solvent at a volume ratio of 20:1, and ethyl cellulose 100 centipoise (EC100cp) is added to make a mixed solution with a concentration of 29% (g / ml) as a dispersed phase, and the temperature of the dispersed phase is kept 40°C; add Span-85 into corn oil and stir evenly, then keep warm at 38°C as the continuous phase, the concentration of Span-85 in corn oil is 2% (g / ml); slowly add 1 volume of dispersed phase to 10 volumes in the continuous phase, and stirred at a speed of 1200rpm / min until the ethanol and ether were completely volatilized, while maintaining the temperature of the entire reaction process at 40°C; the solid was obtained by suction filtration under reduced pressure, washed with n-hexane, and the solid was placed in a vacuum Dry at room temperature to obtain the hollow microsphere carrier. The in vitro floating test proves that the hollow microspheres can sustainably float for 48 hours in the artificial gastric ...

Embodiment approach 3

[0039] Prepare ethanol and ether at a volume ratio of 2:1 to make a mixed solvent, add ethyl cellulose 20 centipoise (EC20cp) and ethyl cellulose 45 centipoise (EC45cp) to make a mixed solvent with a concentration of 5% (g / ml) The solution is used as the dispersed phase, and the temperature of the dispersed phase is kept at 20°C; the Span-60 is added into the soybean oil and stirred evenly, and then kept at 22°C as the continuous phase, and the concentration of the Span-60 in the soybean oil is 0.1% (g / ml ); slowly add 1 volume of dispersed phase into 5 volumes of continuous phase, and stir at a speed of 500rpm / min until ethanol and ether are completely volatilized, while maintaining the temperature of the entire reaction process at 20°C; vacuum filtration to obtain a solid, and use n-hexane Wash the obtained solid, and dry the solid at room temperature under vacuum to obtain a hollow microsphere carrier. The in vitro floating test proves that the hollow microspheres can susta...

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Abstract

A process for preparing the hollow microball as the carrier of gastrointestinal medicine includes such steps as mixing ethanol with ether, adding ethyl cellulose to obtain a mixed solution as dispersing phase, adding span-series surfactant to mineral oil or vegetative oil to obtain continuous phase, proportionally and slowly adding said dispersing phase in said continuous phase, stirring at 20-40 deg.C until full volatilization of ethanol and ether, vacuum filtering, washing to obtain solid, and vacuum drying.

Description

technical field [0001] The invention relates to a method for preparing a drug carrier, in particular to a method for preparing a hollow microsphere carrier of drugs used in the gastrointestinal tract. technical background [0002] The drug delivery systems currently used to prolong the residence time of drugs in the stomach mainly include gastric expansion systems, high-density systems, bioadhesion systems, oral magnetic field positioning systems, and gastric floating systems. Among them, the theoretical basis of the floating drug delivery system is the principle of hydrodynamic equilibrium, and the density of this type of system is generally lower than that of gastric juice (1.004g / cm 3 ), which can float in the stomach for a long time and release the drug continuously. After the drug is released, the residual system will be discharged from the stomach. The floating drug delivery system includes single-unit dosage forms and multiple-unit dosage forms. During the gastric em...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/38
Inventor 魏郁梦赵领索国清于明安
Owner 魏郁梦