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Oral medicinal composition of glycyrrhizic acid or glycyrrhetate and preparation method thereof

A technology of composition and glycyrrhizic acid, which is applied in the direction of drug combination, medical formula, medical preparations containing active ingredients, etc., can solve the problems of affecting the full contact of drugs and affecting drug absorption, so as to improve bioavailability, improve curative effect, The effect of effective absorption

Active Publication Date: 2011-04-13
CHIA TAI TIANQING PHARMA GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The phospholipid complex of glycyrrhizic acid or its salt is very easy to form a gel-like mass in the intestinal juice environment, which affects the full contact between the drug and the small intestinal wall and ultimately affects the absorption of the drug
At the same time, the absorption of glycyrrhizic acid substances in the small intestine may be related to the carrier, and there is a saturation phenomenon. The absorption rate obtained when the drug is released in a concentrated manner will be much lower than that obtained when the drug is uniformly dispersed.

Method used

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  • Oral medicinal composition of glycyrrhizic acid or glycyrrhetate and preparation method thereof
  • Oral medicinal composition of glycyrrhizic acid or glycyrrhetate and preparation method thereof
  • Oral medicinal composition of glycyrrhizic acid or glycyrrhetate and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation Embodiment 1

[0046] Preparation Example 1: 18-α magnesium glycyrrhizinate (magnesium isoglycyrrhizinate) enteric-coated pellets and capsules

[0047] Pellet Prescription:

[0048] Component name 1000 capsule dosage (g)

[0049] Magnesium 18-α Glycyrrhizinate 50 (as C 42 h 60 MgO 16 count)

[0050] Medicinal blank pellet core (sucrose type) 100

[0051] Soy Lecithin 50

[0052] Polyethylene glycol 6000 0.16

[0053] Talc 5

[0054] Proper amount of ethanol

[0055] Prescription of enteric coating solution:

[0056] Component name Amount per 1000 grams of pellets (g)

[0057] Opadry (ACRYC-EZE MP) 300

[0058] water 2000

[0059] Production Process:

[0060] 1. After dissolving the prescribed amount of 18-α magnesium glycyrrhizinate and soybean lecithin in ethanol (if necessary, a small amount of water can be added dropwise to dissolve), evaporate the ethanol to dryness to obtain a compound of 18-α magnesium glycyrrhizinate and soybean lecithin;

[0061] 2. Disperse the compoun...

preparation Embodiment 2

[0066] Preparation Example 2: Diammonium 18-α Glycyrrhizinate Enteric-Coated Pellet Capsules

[0067] Pellet Prescription:

[0068] Component name 1000 capsule dosage (g)

[0069] 18-α diammonium glycyrrhizinate 50(C 42 h 68 N 2 o 16 count)

[0070] Polyene Phosphatidylcholine 25

[0071] Microcrystalline Cellulose 100

[0072] Low-substituted hydroxypropyl cellulose 100

[0073] Talc 37.5

[0074] Proper amount of ethanol

[0075] 15% alcohol solution in proper amount

[0076] Prescription of enteric coating solution:

[0077] Component name Amount per 1000 grams of pellets (g)

[0078] Opadry (ACRYC-EZE MP) 300

[0079] water 2000

[0080] Production Process:

[0081] 1. Dissolve the prescription amount of 18-α diammonium glycyrrhizinate and polyene phosphatidylcholine in ethanol (if necessary, a small amount of water can be added dropwise to dissolve) and evaporate the ethanol to dryness to obtain 18-α diammonium glycyrrhizinate and polyene phosphatidylcholin...

preparation Embodiment 3

[0088] Preparation Example 3: Dipotassium 18-β Glycyrrhizinate Enteric-Coated Pellet Capsules

[0089] Pellet Prescription:

[0090] Component name 1000 capsule dosage (g)

[0091] Dipotassium 18-β Glycyrrhizinate 100(C 42 h 60 K 2 o 16 count)

[0092] Phosphatidylcholine 30

[0093] Lactose 30

[0094] Microcrystalline Cellulose 100

[0095] Low-substituted hydroxypropyl cellulose 5

[0096] Talc powder 10

[0097] Proper amount of ethanol

[0098] 30% alcohol solution in proper amount

[0099] Prescription of enteric coating solution:

[0100] Component name Amount per 1000 grams of pellets (g)

[0101] EUDRAGIT (L100-55) 300

[0102] water 2000

[0103] Using the production process described in Preparation Example 2, using the various components of the prescription amount described in the above prescription to prepare enteric-coated pellets with a diameter of 0.5mm to 1.5mm, and then measuring the drug content of the enteric-coated pellets Filling capsules. ...

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Abstract

The invention discloses an oral medicinal composition of glycyrrhizic acid or glycyrrhetate and a preparation method thereof. The composition consists of a plurality of units, wherein each unit consists of an outer layer enteric coating and content; and the content contains glycyrrhizic acid or glycyrrhetate and at least one intestinal absorption accelerator. The composition can be used for treating chronic hepatitis and improving liver dysfunction.

Description

technical field [0001] The invention relates to an oral pharmaceutical composition of glycyrrhizic acid or a salt thereof and a preparation method thereof, in particular to an oral enteric-coated pharmaceutical composition containing glycyrrhizic acid or a salt thereof. Background technique [0002] Glycyrrhizae (Glycyrrhiza) is a commonly used medicinal plant, and its main active ingredients are glycyrrhizic acid substances, namely glycyrrhizic acid in 18-β configuration and glycyrrhizic acid in 18-α configuration (also known as isoglycyrrhizic acid). Pharmacological, biochemical and structure-activity relationship analysis studies have proved that glycyrrhizic acid or its salts have strong anti-inflammatory, liver cell protection and liver function improvement effects (see Chinese patent publications CN1381462A and CN1569005A). [0003] At present, all oral preparations of glycyrrhizic acid or its salts have the problem of low oral bioavailability, because glycyrrhizic aci...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/704A61P1/16A61K9/16A61K9/48A61K9/20
CPCA61K31/704A61K9/5021A61K9/4891A61P1/16A61P31/14
Inventor 董平左丞夏春光
Owner CHIA TAI TIANQING PHARMA GRP CO LTD
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