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Arctigenin micro-emulsion enteric soft capsule preparation

A technology of arctigenin and enteric-coated soft capsules, which is applied in capsule delivery, antiviral agents, non-active ingredients of polymer compounds, etc., and can solve problems affecting patient compliance, low bioavailability, and poor water solubility. Achieve the effect of improving bioavailability, simple preparation process and stable properties

Active Publication Date: 2015-03-18
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Invention patent application publication specification CN101134031A discloses the preparation method of arctigenin soft capsules, but because arctigenin is a fat-soluble compound, the water solubility is poor, and the direct oral bioavailability is low
However, direct oral administration of arctigenin microemulsion will produce adverse reactions in the upper gastrointestinal tract such as stomach discomfort, nausea, and vomiting, which will affect the patient's compliance.
And microemulsion needs a large amount of emulsifier, with the increase of emulsifier content and its accumulation in the body, it will inevitably produce certain toxicity.

Method used

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  • Arctigenin micro-emulsion enteric soft capsule preparation
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  • Arctigenin micro-emulsion enteric soft capsule preparation

Examples

Experimental program
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Effect test

Embodiment 1

[0030] Embodiment 1 arctigenin microemulsion enteric-coated capsule preparation

[0031] Contents Prescription:

[0032]

[0033] Rubber prescription:

[0034]

[0035] Enteric coating solution prescription:

[0036]

[0037]

[0038] Preparation process: Weigh the prescription amount of medium-chain fatty acid glycerides, polyoxyethylene castor oil, propylene glycol, and absolute ethanol, mix and stir evenly, then add arctigenin to dissolve, and ultrasonic treatment can also be used to speed up the dissolution to obtain a clarified concentrated solution. It is arctigenin microemulsion concentrate. The microemulsion concentrate obtained above is diluted with water according to the weight ratio of 1:10-20 to a clear solution to obtain the microemulsion content. Weigh the gelatin, glycerin, and purified water in the prescription amount, mix them evenly, and press them into rubber, then weigh Eudragit L30D-55, triethyl citrate, talcum powder, and purified water in ...

Embodiment 2

[0039] Embodiment 2 arctigenin microemulsion enteric-coated capsule preparation

[0040] Contents Prescription:

[0041]

[0042] Rubber prescription:

[0043]

[0044] Enteric coating solution prescription:

[0045]

[0046]

[0047] Preparation process: Weigh polyethylene glycol 400, polyoxyethylene castor oil, glyceryl linoleate, and absolute ethanol in the prescription amount, mix and stir evenly, then add arctigenin to dissolve, and ultrasonic treatment can also be used to speed up the dissolution. The clarified concentrated solution is the arctigenin microemulsion concentrate. The microemulsion concentrate obtained above is diluted with water according to the weight ratio of 1:10-20 to a clear solution to obtain the microemulsion content. Weigh the gelatin, sorbitol, and purified water in the prescription quantity, mix them evenly and press them into rubber, then weigh the polyacrylic resin II, polyacrylic resin III, diethyl phthalate, Tween 80, 95 % etha...

Embodiment 3

[0048] Embodiment 3 arctigenin microemulsion enteric-coated capsule preparation

[0049] Contents Prescription:

[0050]

[0051] Enteric rubber prescription:

[0052]

[0053] Preparation process: Weigh the absolute ethanol, glycerin, emulsifier OP, and glyceryl monostearate in the prescription amount, mix and stir evenly, then add arctigenin to dissolve, and ultrasonic treatment can also be used to speed up the dissolution to obtain a clarified concentrated solution. It is arctigenin microemulsion concentrate. The microemulsion concentrate obtained above is diluted with water according to the weight ratio of 1:10-20 to a clear solution to obtain the microemulsion content. Weigh gelatin, glycerin, purified water, Eudragit L100-55, and triethyl citrate in the recipe, mix them evenly and press them into enteric-coated rubber, and wrap the contents containing arctigenin microemulsion with enteric-coated rubber. Enteric-coated soft capsules.

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Abstract

The invention belongs to the field of medicines, and specifically relates to an arctigenin micro-emulsion enteric soft capsule preparation, and a preparation method thereof. The enteric soft capsules are composed of contents containing arctigenin micro-emulsion concentrated liquid and enteric capsule shells. The capsules can be dissolved in intestines. With the capsules, bioavailability of arctigenin is improved, and irritation to the stomach is reduced. The capsules can be directionally released in intestines, and has the advantages of high stability and good sustained-release effect. The capsule preparation has a good medical application prospect.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to an enteric-coated soft capsule containing arctigenin microemulsion and a preparation method thereof. Background technique [0002] Arctium burdock is the dry and ripe fruit of the Compositae plant Burdock. It is a commonly used traditional Chinese medicine. It has the functions of evacuating wind-heat, clearing the lungs and rash, detoxifying and relieving the throat. It is used for wind-heat cold, cough with excessive phlegm, measles, rubella, sore throat, Pruritus mumps erysipelas, carbuncle sores. The traditional Chinese medicine contains lignans, mainly arctiin and arctigenin. Although the content of arctigenin (also known as arctigenin) in Arctium Fructus is very low, its precursor arctiin is relatively high in the fruit of traditional Chinese medicine burdock and burdock arctium, so a large amount of it can be obtained through the conversion of arctiin Arctigenin....

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/48A61K31/365A61K47/42A61P31/04A61P31/12A61P35/00A61P43/00
Inventor 赵志全徐真真胡江波陈小伟
Owner LUNAN PHARMA GROUP CORPORATION