Slow release levodropropizine pharmaceutical composition

A technology of levothyroxine and sustained-release drugs, applied in the field of sustained-release drugs, can solve the problems of adverse reactions, high peak blood drug concentration, clinical application limitations and the like

Inactive Publication Date: 2004-08-18
王志刚
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The deficiency that the various oral preparations that use this medicine is made in clinical application is that the half-life (T1 / 2) is about 2.3 hours, and the mean residence time (MRT) is about 3 hours, needs administration 3 times every day and just can maintain relatively good curative effect
In addition, after a single dose of 60 mg of the drug in a healthy person, its peak blood concentration (Cmax) is relatively high, about 1.0 μg / ml, which is likely to cause adverse reactions in the body, so it is limited in clinical application

Method used

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  • Slow release levodropropizine pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] The raw material formula is as follows:

[0020] Levodropropizine 12.4 parts

[0021] Sustained-release excipients:

[0022] Hypromellose K4M 1.5 parts

[0023] Ordinary functional accessories:

[0024] Starch 4.0 parts

[0025] Lactose 12.4 parts

[0026] Microcrystalline cellulose 16.4 parts

[0027] Magnesium stearate 0.5 part

[0028] The solvent is 2 parts of 50% ethanol in water

[0029] The hydroxypropyl methylcellulose K4M in the prescription is a hydrophilic gel skeleton, which swells to form a gel barrier when it encounters water or digestive juices, and controls the diffusion of levodropropizine to achieve the purpose of release.

[0030] The preparation method is as follows: preparing granules according to the preparation method of conventional tablets, and pressing into double-layer tablets by using a double-layer tablet press machine.

Embodiment 2

[0032] The raw material formula is as follows:

[0033] Levodropropizine 24.7 parts

[0034] Sustained-release excipients:

[0035] Hypromellose K4M 8.2 parts

[0036] Ordinary functional accessories:

[0037] Lactose 16.4 parts

[0038] Magnesium stearate 0.5 part

[0039] The solvent is 3 parts of 60% ethanol aqueous solution

[0040] The hydroxypropyl methylcellulose K4M in the prescription is a hydrophilic gel skeleton, which swells to form a gel barrier when it encounters water or digestive juices, and controls the diffusion of levodropropizine to achieve the purpose of release.

[0041] Preparation method: Prepare granules according to the conventional tablet preparation method, and press into double-layer tablets with a double-layer tablet press.

Embodiment 3

[0043] The raw material formula is as follows:

[0044] Levodropropizine 31.4 parts

[0045] Sustained-release excipients:

[0046] Hypromellose (K4M) 14.0 parts

[0047] Ordinary functional accessories:

[0048] Starch 17.4 parts

[0049] Lactose 29.6 parts

[0050] Stearic acid 2.6 parts

[0051] Magnesium stearate 0.5 parts

[0052] Talcum powder 1.5 parts

[0053] The solvent is 3 parts of 60% ethanol aqueous solution

[0054] In the prescription, hydroxypropyl methylcellulose K4M is a hydrophilic gel skeleton, and stearic acid is a bioerodible skeleton, which swells with water or digestive juice to form a gel barrier and emulsion, which controls the diffusion of levodropropizine and achieves release Purpose.

[0055] Preparation method: Prepare granules according to the conventional tablet preparation method, and press into double-layer tablets with a double-layer tablet press.

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Abstract

The present invention provides one kind of delayed releasing levohydroxypropyl piperazine medicine composition and the medicine composition consists of levohydroxypropyl piperazine 10-80 weight portions, supplementary material for delayed releasing 0.5-60 weight portions and other supplementary material 0.5-90 weight portions. The delayed releasing levohydroxypropyl piperazine medicine composition is cough relieving medicine and the supplementary material for delayed releasing results in the effective blood medicine concentration maintained for relatively long period, relatively low blood medicine concentration, raised curative effect, reduced toxic side effect and less medicine taking times.

Description

1. Technical field [0001] The invention relates to a sustained-release drug in the category of peripheral antitussive preparations, in particular to a sustained-release drug composition of levodropropizine. 2. Technical background [0002] European patent "0147847" discloses the peripheral cough medicine levodropropizine and its functional preparations. Levodropropizine has the following structural formula: [0003] [0004] The chemical name of levodropropizine is: (S)-3-(4-phenyl-1-piperazinyl)-1,2-propanediol. [0005] Levodropropizine is mainly used for the treatment of cough symptoms caused by respiratory diseases (such as upper respiratory tract infection, bronchitis and asthma). The antitussive effect of this drug is equivalent to that of racemic dropropizine, but its central sedative effect is small, and it will not form drug dependence, so it is an ideal antitussive drug. [0006] The deficiency that the various oral preparations that use this medicine is made ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K9/52A61K31/495A61P11/14
Inventor 王志刚邓邵民
Owner 王志刚
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