Sustaining agent of Duosuo theosine and its preparation

A technology of doxofylline and sustained-release preparations, which can be used in pharmaceutical formulations, medical preparations with non-active ingredients, respiratory diseases, etc., and can solve problems such as inability to quickly relieve asthma symptoms and low blood drug concentrations

Active Publication Date: 2007-09-05
HEFEI HEYUAN PHARM TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These controlled-release or sustained-release preparations release the drug at a constant rate to maintain the blood concentration of the drug, but the disadvantage is that due to the constant release rate, the blood drug concentration of the patient is too l

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Doxofylline double-layer tablet, calculated by 1000 tablets

[0016] quick release part

[0017] Component Weight (g)

[0018] Doxofylline 80

[0019] Dextrin 25

[0020] Microcrystalline Cellulose 25

[0021] Low-substituted hydroxypropyl cellulose 5

[0022] Sodium carboxymethyl starch 5

[0023] Polyvinylpyrrolidone ethanol solution K-30 QS

[0024] Magnesium Stearate 2

[0025] Preparation method: Pass the raw material drug through a 100-mesh sieve, weigh the raw and auxiliary materials in the prescribed amount, pass through an 80-mesh sieve and mix evenly, add an appropriate amount of binder to make a soft material, granulate with a 24-mesh, and granulate with a 18-mesh. Add the prescribed amount of lubricant and mix well.

[0026] Sustained release part

[0027] Component Weight (g)

[0028] Doxofylline 320

[0029] Microcrystalline Cellulose 120

[0030] HPMC K4M 180

[0031] Polyvinylpyrrolidone ethanol solution K-30 QS

[...

Embodiment 2

[0036] Doxofylline double-layer tablet, calculated by 1000 tablets

[0037] quick release part

[0038] Component Weight (g)

[0039] Doxofylline 100

[0040] Lactose 25

[0041] Microcrystalline Cellulose 25

[0042] Low-substituted hydroxypropyl cellulose 5

[0043] Sodium carboxymethyl starch 5

[0044] Polyvinylpyrrolidone ethanol solution K-30 QS

[0045] Magnesium Stearate 2

[0046] Sustained release part

[0047] Component Weight (g)

[0048] Doxofylline 300

[0049] Lactose 120

[0050] HPMC K4M 160

[0051] Polyvinylpyrrolidone ethanol solution K-30 QS

[0052] Magnesium stearate 3

[0053] The preparation method is the same as in Example 1.

Embodiment 3

[0055] Doxofylline double-layer tablet, calculated by 1000 tablets

[0056] quick release part

[0057]Component Weight (g)

[0058] Doxofylline 120

[0059] Microcrystalline Cellulose 50

[0060] Low-substituted hydroxypropyl cellulose 8

[0061] Sodium carboxymethyl starch 2

[0062] Polyvinylpyrrolidone ethanol solution K-30 QS

[0063] Magnesium Stearate 2

[0064] Sustained release part

[0065] Component Weight (g)

[0066] Doxofylline 280

[0067] Lactose 140

[0068] HPMC K10 80

[0069] HPMC 100cp 50

[0070] Polyvinylpyrrolidone ethanol solution K-30 QS

[0071] Magnesium Stearate 3

[0072] The preparation method is the same as in Example 1.

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PUM

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Abstract

A slow-release doxofylline is composed of a fast-release component prepared from doxofylline (10-60%) and fast-release assistant and a slow-release component prepared from doxofylline (40-90%) and slow-release assistant. Its preparing process is also disclosed.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a sustained-release preparation of doxofylline, and also discloses a preparation method of the sustained-release preparation. Background technique [0002] Doxofylline, whose chemical name is 1,3-dimethyl-7-(1,3-dioxol-2-yl)methyl-3,7-dihydro-1H-purine-2, 6-diketone, a bronchodilator, is a derivative of methylxanthine, which can directly act on the bronchi and relax bronchial smooth muscle. By inhibiting the action of phosphodiesterase in smooth muscle cells, it relaxes smooth muscle, thereby achieving the effect of inhibiting asthma. [0003] Doxofylline currently used clinically has tablets, capsules, and injections. Because the tablet or capsule disintegrates quickly after oral administration, a large amount of doxofylline is absorbed by the gastrointestinal tract in a short period of time. Although it can quickly relieve the symptoms of bronchial asthma, the blood...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K9/52A61K31/522A61K47/12A61K47/14A61K47/32A61K47/34A61K47/36A61K47/38A61K47/44A61P11/06A61K47/10
Inventor 高署
Owner HEFEI HEYUAN PHARM TECH CO LTD
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