Biodegradable nanoparticle-entrapped oral colon-targeted micro-capsule and preparation method thereof

A colon-targeting and nanoparticle technology, which is applied in microcapsules, medical preparations of non-active ingredients, capsule delivery, etc., can solve the problem of complex preparation process of microencapsulated sodium drug-loading system, difficult control of drug-loading efficiency, and lack of pH Responsiveness and other issues, to achieve the effects of enhancing intestinal targeting, increasing bioavailability, and simple and easy preparation methods

Active Publication Date: 2013-12-04
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The preparation process of the microencapsulated sodium drug-loading system of this patent is complicated, the drug-loading efficiency is difficult to control, and it does not have pH responsiveness, so it cannot be used for oral administration
To sum up, at present, most domestic microcapsules are prepared by directly coating drugs, and there is no patent report on enteric-coated embedding of biodegradable nanoparticles to make pH-responsive microcapsules

Method used

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  • Biodegradable nanoparticle-entrapped oral colon-targeted micro-capsule and preparation method thereof
  • Biodegradable nanoparticle-entrapped oral colon-targeted micro-capsule and preparation method thereof
  • Biodegradable nanoparticle-entrapped oral colon-targeted micro-capsule and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0040] Precisely weigh 10mg of the drug and 100mg of PLGA, dissolve the drug and PLGA in 5ml of ethanol-dichloromethane with a volume ratio of 1:4, prepare another 10ml of PVA solution with a concentration of 3%, and add the dichloromethane solution dropwise to the PVA In the solution, an O / W emulsion was formed, and then the emulsion was sonicated for 30s with an amplitude of 40%, and the nanoparticles after the sonication were dispersed into 25ml of a PVA solution with a concentration of 0.3%, stirred at 400rpm for 5h to remove the organic solvent, and then in Nanoparticles were collected by centrifugation at 10000 rpm, and freeze-dried to obtain nanometer freeze-dried powder. Accurately weigh 10 mg of the freeze-dried powder, and evenly disperse it into 5 ml of ethanol solution containing 100 mg of MAE-100P, then add the ethanol solution dropwise to 30 ml of peanut oil containing 1% span80, stir overnight at 800 rpm for 12 hours to evaporate The ethanol was removed, the mic...

Embodiment 2

[0043] Precisely weigh 10mg of drug and 100mg of PLGA, dissolve the drug and PLGA in 5ml of ethanol-dichloromethane with a volume ratio of 1:4, prepare another 10ml of PVA solution with a concentration of 3%, and add the mixed organic phase to the PVA solution dropwise , form an O / W emulsion, and then ultrasonicate the emulsion at 40% amplitude for 30s, disperse the ultrasonicated nanoparticles into 25ml of PVA solution with a concentration of 0.3%, stir at 400rpm for 5h to remove the organic solvent, and then The nanoparticles are collected by centrifugation, and freeze-dried to obtain nano freeze-dried powder. Accurately weigh 10 mg of the lyophilized powder, and evenly disperse it into 5 ml of ethanol solution containing 100 mg of Eudragit L-100, and then add the ethanol solution dropwise to 30 ml of peanut oil containing 1% span80, overnight at 800 rpm Stir for 12 hours to remove ethanol, centrifuge at 3000 rpm for 5 minutes to collect the microcapsules, and finally wash t...

Embodiment 3

[0046] Accurately weigh 10 mg of drug and 100 mg of PLGA-PEG, dissolve the drug and PLGA-PEG in 5 ml of dichloromethane, prepare 10 ml of a 3% PVA solution, add the dichloromethane dropwise to the PVA solution to form O / W emulsion, then the emulsion was sonicated at 40% amplitude for 30s, and the nanoparticles after sonication were dispersed into 30ml of PVA solution with a concentration of 0.3%, stirred at 400rpm for 5h to remove the organic solvent, and then centrifuged at 10000rpm to collect Nanoparticles, freeze-dried to obtain nano freeze-dried powder. Accurately weigh 10 mg of the lyophilized powder, and evenly disperse it into 5 ml of ethanol solution in which 80 mg of MAE-100P is dissolved, then add the ethanol solution dropwise to 30 ml of rapeseed oil containing 1% span80, and stir overnight at 1000 rpm The ethanol was evaporated for 12 hours, the microcapsules were collected by centrifugation at 3000 rpm for 5 minutes, and finally the microcapsules were washed with ...

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Abstract

The invention discloses a biodegradable nanoparticle-entrapped oral colon-targeted micro-capsule and a preparation method thereof. The preparation method comprises the following steps: 1, dissolving drugs and degradable polymers in an organic phase and taking a solution containing polyvinyl alcohol or sodium cholate as a water phase for preparing drug nanoparticles; 2, dissolving an enteric-coated material in absolute ethanol; 3, dispersing the drug nanoparticles in absolute ethanol in which the enteric-coated material is dissolved; 4, preparing edible oil; 5, dropwise adding ethanol liquid into the edible oil, stirring, solidifying, and volatilizing to remove absolute ethanol; 6, centrifuging suspension liquid, collecting the micro-capsule in a lower layer, and washing by normal hexane. The prepared oral colon-targeted micro-capsule has a remarkable pH response, drugs in the micro-capsule are hardly released under the acidic conditions, a capsule material is dissolved under the pH value of enteric canal, the drug nanoparticles are released, the nanoparticles can be transferred to a target point, and the drugs are slowly released, so that the absorption rate of oral administration is greatly increased, the bioavailability is improved, and the treatment effect is enhanced.

Description

[0001] technical field [0002] The invention belongs to the technical field of microcapsule preparation, and in particular relates to an oral colon-targeting microcapsule carrying biodegradable nanoparticles and a preparation method thereof. Background technique [0003] Oral administration is the preferred route of administration for drug therapy. Its administration method is simple, safe, and easy to implement. It has good patient compliance and is especially suitable for long-term administration. However, the bioavailability of oral administration is low, especially for large Most peptide or protein drugs cannot be made into oral preparations because they are easily destroyed by the digestive tract (Hongming Chen and Robert Langer. Oral particulate delivery: status and future trends. Advanced Drug Delivery Reviews, 1998, 34: 339–350). Therefore, oral administration often requires the drug to be packed into capsules or made into enteric-coated preparations to prevent the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K9/52A61K47/34A61K47/32
Inventor 刘杰蒋庆罗新根舒雅俊高迪
Owner SUN YAT SEN UNIV
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