Oral berberine microcapsule nanoparticle chimeric preparation and dosage regimen

A technology of nanoparticles and berberine, applied in the field of -nanoparticles, can solve the problem of low intestinal absorption rate of oral berberine

Active Publication Date: 2022-04-15
INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In order to solve the disadvantages of the extremely low intestinal absorption rate of berberine orally, increase the water solubility or fat solubility of berberine, and develop a new drug delivery system to improve bioavailability has become the focus of drug development

Method used

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  • Oral berberine microcapsule nanoparticle chimeric preparation and dosage regimen
  • Oral berberine microcapsule nanoparticle chimeric preparation and dosage regimen
  • Oral berberine microcapsule nanoparticle chimeric preparation and dosage regimen

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Structural diagram of microcapsule nanoparticle chimeric preparation prepared by three components of PLGA, Eudragit FS30D and berberine hydrochloride in specific proportions ( figure 1 ). In the invention, a UV spectrophotometer is firstly used to establish an analysis method as a preferred detection means for quality control, and the method is feasible and meets the requirements of pharmacy. Taking the drug dosage, organic solvent dosage, PLGA dosage, and polyvinyl alcohol concentration as the inspection factors of the prescription, and taking the emulsification strength, emulsification time, stirring speed, and stirring time as the inspection factors of the process, L9 was designed according to four factors and three levels of orthogonal optimization ( 3 4 ) test to optimize the optimal ratio and process of the prescription to obtain the appropriate prescription and process.

[0043] Weigh 3 mg of berberine hydrochloride and dissolve the drug in water as a solvent t...

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Abstract

The invention discloses a preparation method and an oral application method of a microcapsule nanoparticle chimeric preparation of oral berberine intestinal targeted delivery release and long-short double-effect differential integration and its oral application method. The three components of degradable sustained-release material and enteric coating material are prepared according to a specific ratio to form microcapsules, and the chimeric dosage form of berberine and biodegradable sustained-release material loaded with berberine hydrochloride nanoparticles is simultaneously encapsulated, which not only effectively protects the content, and target specific intestinal segments to play a differential integration of the first-dose effect provided by the microcapsules and the sustained-release and long-acting effect provided by the nanoparticles, while improving the bioavailability and efficacy of the drug, reducing the number of medications , improve medication compliance.

Description

technical field [0001] The invention relates to a chimeric preparation carrying berberine microcapsules-nanoparticles orally, and realizes the field of development of a differentiated integration system for intestinal targeted delivery and release, specifically involving the use of biodegradable slow-release materials, enteric coating materials and berberine Alkaline three components, according to a specific ratio to form a chimera in which berberine hydrochloride and biodegradable sustained-release material-loaded berberine hydrochloride nanoparticles are simultaneously present in enteric-coated microcapsules, exerting intestinal targeted release, Long-short double-effect differential integration. Background technique [0002] Berberine is a natural quaternary ammonium isoquinoline alkaloid, mainly found in Coptis chinensis of Ranunculaceae, Amur corkberry of Rutaceae and Berberis of Berberidaceae. Berberine in nature usually exists in the form of quaternary ammonium salt....

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/50A61K9/52A61K47/32A61K9/51A61K47/34A61K31/4375A61P31/04
Inventor 竺青张灵芝
Owner INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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