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Ursolic acid liquid-solid compression tablet

A technology of ursolic acid and compressed tablets, which is applied in the directions of inactive medical preparations, pill delivery, digestive system, etc., can solve problems such as difficulty in utilization, increase difficulty, etc., and achieves low production cost, convenient operation, and disintegration. short time effect

Inactive Publication Date: 2013-03-06
SHANDONG ACAD OF CHINESE MEDICINE +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Ursolic acid has pharmacological effects such as anti-tumor, liver protection, cardiovascular, diabetes, anti-inflammation, disease resistance, immune regulation, sedation and hypnosis, etc., but its poor solubility increases the difficulty of its oral preparations

Method used

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  • Ursolic acid liquid-solid compression tablet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] 1 prescription:

[0036] The liquid auxiliary material is 1,2-propanediol; the ratio of medicine to liquid is 1:4; the R value is 10; L f The value is 0.300. Each tablet contains ursolic acid 10 mg; 1,2-propanediol 40 mg; microcrystalline cellulose 166.67 mg; micropowder silica gel 16.67 mg; sodium carboxymethyl starch 11.67 mg. Tablet weight is 245.01 mg.

[0037] 2 Preparation method:

[0038] Dissolve and disperse ursolic acid in 1,2-propanediol, gradually add MCC, mix evenly, then add micropowder silica gel, thoroughly pulverize and mix evenly, then add sodium carboxymethyl starch, and directly compress the evenly mixed powder.

Embodiment 2

[0040] 1 prescription:

[0041] The liquid auxiliary material is 1,2-propanediol; the ratio of medicine to liquid is 1:4; the R value is 20; L f The value is 0.225. Each tablet contains ursolic acid 10 mg; 1,2-propanediol 40 mg; microcrystalline cellulose 222.22 mg; micropowder silica gel 11.11 mg; sodium carboxymethyl starch 14.17 mg. Tablet weight is 297.50 mg.

[0042] 2 Preparation method:

[0043] Dissolve and disperse ursolic acid in 1,2-propanediol, gradually add MCC, mix evenly, then add micropowder silica gel, thoroughly pulverize and mix evenly, then add sodium carboxymethyl starch, and directly compress the evenly mixed powder.

Embodiment 3

[0045] 1 prescription:

[0046] The liquid auxiliary material is polyethylene glycol 400; the ratio of medicine to liquid is 1:4; the R value is 10; L f The value is 0.314. Each tablet contains ursolic acid 10 mg; polyethylene glycol 400 40 mg; microcrystalline cellulose 159.24 mg; micropowder silica gel 15.92 mg; sodium carboxymethyl starch 11.26 mg. Tablet weight is 236.42 mg.

[0047] 2 Preparation method:

[0048] Dissolve and disperse ursolic acid in polyethylene glycol 400, gradually add MCC, mix evenly, then add micropowder silica gel, thoroughly pulverize and mix evenly, then add sodium carboxymethyl starch, and directly compress the evenly mixed powder.

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Abstract

The invention utilizes a liquid-solid compression tablet technology to provide an ursolic acid liquid-solid compression tablet which is capable of effectively increasing dissolution rate of ursolic acid, and improving bioavailability of medicine, and has a simple preparation method. The method comprises the following steps of: using the ursolic acid as a medicinal material, 1,2-propylene glycol or polyethylene glycol 400 as a liquid auxiliary material, microcrystalline cellulose as a carrier material, superfine silica powder as a coating material, and sodium carboxymethyl starch as disintegrating agent; and compressing to form the liquid-acid compression tablet. The ursolic acid liquid-solid compression tablet has the beneficial effects that: the disintegration time limits is short, the dissolution and the absorbent of the ursolic acid are favored, the dissolution rate of the ursolic acid is improved, the bioavailability of oral ursolic acid is improved, the production cost is low, the requirements of process and equipment are simple, the operation is convenient, and industrial scale production is realized.

Description

technical field [0001] The invention relates to a liquid-solid compressed tablet of ursolic acid. Background technique [0002] Ursolic acid (Ursolic acid, UA), also known as ursolic acid and ursolic acid, is an α-amyresin-type pentacyclic triterpene acid. Ursolic acid has pharmacological effects such as anti-tumor, liver protection, cardiovascular, diabetes, anti-inflammation, disease resistance, immune regulation, sedation and hypnosis, etc., but its poor solubility increases the difficulty of its oral preparations. [0003] Liquid-solid compression technology (Liquisolid compacts technique), also known as solution powdering technology, is to dissolve or disperse poorly water-soluble drugs in non-volatile liquid solvents, and then mix them with the selected carrier and coating materials in a certain proportion to make them Transforms into a non-sticky, free-flowing and easily compressible powder. Drugs exist in an amorphous state in liquid excipients. [0004] The dosag...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/56A61K47/38A61P35/00A61P1/16A61P3/10A61P9/00A61P29/00A61P37/02A61P25/20
Inventor 闫雪生赵许杰生力嵩徐新刚于蓓蓓李义召韩媛媛催兵兵孙丹丹
Owner SHANDONG ACAD OF CHINESE MEDICINE
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