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An oral enteric-coated preparation of total flavonoids of Epimedium and its application

A technology of enteric-coated preparations and total flavonoids, which is applied in the field of medicine, can solve the problems of low oral bioavailability of total flavonoids of Epimedium, achieve the effects of improving bioavailability, maintaining stability, and ensuring enzymatic hydrolysis and absorption

Active Publication Date: 2018-05-22
JIANGSU PROVINCE INST OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The purpose of the present invention is to provide an oral enteric-coated preparation of total flavonoids of Epimedium, which can realize real-time enzymolysis and absorption of total flavonoids of Epimedium in the intestinal tract, prolong the residence time of the drug at the intestinal absorption site, and ensure the Sufficient enzymatic hydrolysis and absorption to improve the defects of low oral bioavailability of total flavonoids of Epimedium

Method used

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  • An oral enteric-coated preparation of total flavonoids of Epimedium and its application
  • An oral enteric-coated preparation of total flavonoids of Epimedium and its application
  • An oral enteric-coated preparation of total flavonoids of Epimedium and its application

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Experimental program
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Effect test

Embodiment 1

[0046] Weigh 42.0 g of Epimedium total flavonoids powder, 8.4×10 β-glucosidase 4 U (42.0 g), 10.0 g of hydroxypropyl methylcellulose, and 6.8 g of chitosan, mix well, add an appropriate amount of 95% ethanol as a wetting agent, and make a soft material (to form a ball when held, and to disperse when touched) , sieved and granulated, dried, granulated, added an appropriate amount of magnesium stearate, mixed evenly, compressed into tablets, coated, and made into oral enteric-coated tablets of total flavonoids of Epimedium. The bioavailability of the prepared enteric-coated tablet is 0.52 times higher than that of the total flavonoids powder of Epimedium.

Embodiment 2

[0048] Weigh 42.0 g of Epimedium total flavonoids powder, naringinase 4.2×10 5 U (42.0 g), 15.0 g of low-substituted hydroxypropyl cellulose, 6.0 g of carbomer, and 12.6 g of microcrystalline cellulose, mixed evenly, added an appropriate amount of 95% ethanol as a wetting agent, coated, dried, and prepared Oral enteric-coated pills of total flavonoids of Epimedium. The bioavailability of the prepared enteric-coated pills is 0.88 times higher than that of the total flavonoids powder of Epimedium.

Embodiment 3

[0050] Weigh 42.0 g of Epimedium total flavonoids powder, 3.36×10 cellulase 7 U (84.0 g), hydroxypropyl methylcellulose 16.0 g, carbomer 4.6 g, bletilla striata gum 4.6 g, α-lactose 16.8 g, mix well, add appropriate amount of 95% ethanol as wetting agent, sieve and granulate , dried, whole grains, packed into enteric-coated capsules. The bioavailability of the prepared enteric-coated capsules was 1.13 times higher than that of the total flavonoids powder of Epimedium.

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Abstract

The invention relates to an oral enteric-coated preparation of epimedium total flavonoids and an application thereof, belonging to the technical field of medicine. It is an enteric-coated capsule, enteric-coated pill or enteric-coated tablet etc. prepared from total flavonoids of epimedium, hydrolytic enzyme, bioadhesive preparation and other commonly used auxiliary materials in pharmacy. The biomimetic enzymatic hydrolysis oral drug delivery system of total flavonoids of Epimedium developed according to the technical scheme provided by the present invention can release the total flavonoids of Epimedium before the intestinal emptying time under the intestinal environment (37°C, pH 5.2~7.4). It is completely enzymatically hydrolyzed into secondary glycosides and aglycone forms that are more conducive to absorption, and the residence time of the drug delivery system at the intestinal absorption site is prolonged by adding bioadhesives, so as to achieve "real-time enzymatic hydrolysis and real-time absorption" of the drug , to further ensure that Epimedium flavonoid glycosides can be fully enzymatically hydrolyzed and improve bioavailability, and provide more effective and stable treatments for osteoporosis and other diseases.

Description

technical field [0001] The invention relates to an oral enteric-coated preparation of total flavonoids of Epimedium, which is prepared by preparing total flavonoids of Epimedium, hydrolytic enzymes, bioadhesives and auxiliary materials commonly used in pharmacy into enteric-coated capsules, enteric-coated pills or enteric-coated preparations. The invention also relates to the application of the oral enteric-coated preparation, which belongs to the technical field of medicine. Background technique [0002] Epimedium, as a traditional kidney tonifying Chinese medicine, has been used for thousands of years among the people. It has the functions of tonifying kidney yang, strengthening muscles and bones, and dispelling rheumatism. [0003] Epimedium contains a variety of flavonoids, of which 8-isopentenyl substituted flavone glycosides are the main representative active flavonoids, mainly including icariin, epimedin A, epimedin B, epimedin C and Baohuoside I etc. (see structure ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K9/20A61K9/48A61K36/296A61K47/42A61P19/10
Inventor 陈彦高霞王莹
Owner JIANGSU PROVINCE INST OF TRADITIONAL CHINESE MEDICINE
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