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Daphnetin slow-release composition and preparation method thereof

A slow-release composition and technology of daphnetin, applied in drug combination, active ingredient of heterocyclic compounds, drug delivery, etc., can solve the problems of affecting the therapeutic effect of daphnetin, poor patient compliance, low bioavailability, etc., to reduce medication The effect of frequency, delayed drug release, and simple production process

Inactive Publication Date: 2013-07-03
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, the dosage form of daphnetin is only capsules, and the dosage form is single. Since the elimination biological half-life of daphnetin is 10-20min, ordinary capsule preparations are administered frequently, three times a day, three capsules each time, and patient compliance is poor.
In vivo experiments in dogs showed that the blood concentration of daphnetin decreased rapidly after reaching the peak value within 1-2 hours, poor absorption and low bioavailability, which affected the therapeutic effect of daphnetin

Method used

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  • Daphnetin slow-release composition and preparation method thereof
  • Daphnetin slow-release composition and preparation method thereof
  • Daphnetin slow-release composition and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0066] The preparation of embodiment 1 Daphnetin Sustained-release Tablets

[0067] Daphnetin Sustained Release Tablets Prescription Composition:

[0068]

[0069]

[0070] Preparation method: Weigh the prescribed amount of daphnetin, starch, hydroxypropylmethylcellulose, and polyvinylpyrrolidone, mix them and pass through an 80-mesh sieve, use 90% ethanol as a wetting agent to make a soft material, make wet granules, dry, add Magnesium stearate, mixed evenly, granulated, compressed into tablets, ready to be obtained.

[0071] Its in vitro release curve is shown in figure 1 .

Embodiment 2

[0072] The preparation of embodiment 2 daphnetin sustained-release tablets

[0073] Daphnetin Sustained Release Tablets Prescription Composition:

[0074]

[0075] Preparation method: Weigh the prescribed amount of daphnetin, starch, hydroxypropylmethylcellulose, and polyvinylpyrrolidone, mix them evenly and pass through an 80-mesh sieve, use 5% ethanol solution of polyvinylpyrrolidone as a binder to make a soft material, and make wet Granules, dried, added with magnesium stearate, mixed evenly, granulated, compressed into tablets, to obtain.

[0076] Its in vitro release curve is shown in figure 2 .

Embodiment 3

[0077] The preparation of embodiment 3 daphnetin sustained-release tablets

[0078] Daphnetin Sustained Release Tablets Prescription Composition:

[0079]

[0080]

[0081] Preparation method: Weigh the prescribed amount of daphnetin, starch, hydroxypropylmethylcellulose, and polyvinylpyrrolidone, mix them and pass through an 80-mesh sieve, use 15% ethanol solution of polyvinylpyrrolidone as a binder to make a soft material, and make wet Granules, dried, added with magnesium stearate, mixed evenly, granulated, compressed into tablets, to obtain.

[0082] Its in vitro release curve is shown in image 3 .

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Abstract

The invention relates to a daphnetin slow-release composition and a preparation method thereof. The slow-release composition is a matrix tablet. The matrix tablet comprises daphnetin, filler, a matrix material, a bonding agent and a lubricating agent. The matrix material is a high-viscosity hydrophilic matrix material or a soluble matrix material. The daphnetin slow-release tablet prepared with the method has a good slow-release effect and is long in action time, low in dosage, low in frequency of taking and high in bioavailability in comparison with a capsule on the market. The process is simple in operation, low in cost and easy to control, and is suitable for industrial mass production.

Description

technical field [0001] The invention relates to a sustained-release dosage form of medicine, in particular to a daphnetin sustained-release composition and a preparation method of the sustained-release composition. Background technique [0002] Daphnetin (also known as Daphnetin, Daphnetin, Daphnetin) chemically named 7,8-dihydroxycoumarin, is an effective pharmaceutical ingredient widely distributed in a variety of plants. Various pharmacological studies have shown that it can dilate coronary blood vessels, increase coronary blood flow, reduce myocardial oxygen consumption, improve myocardial metabolism, promote cardiac function recovery, expand peripheral blood vessels, resist Egyptian thrombosis and inhibit platelet aggregation; and stimulate the pituitary gland ---Anti-inflammatory effect of the adrenal cortex system; in addition, it also has analgesic, sedative and hypnotic, antibacterial, immune-enhancing, blood-lipid-lowering, cardiotonic, blood-pressure-lowering, ant...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K31/37A61K47/44A61K47/38A61K47/36A61K47/34A61K47/32A61P7/02A61P9/14A61P9/10A61K47/10A61K47/14
Inventor 梅兴国李雪如刘燕李志平
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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