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Three-stage pulsed release controlled release tablet and preparation method thereof

A controlled-release tablet and pulse technology, which is applied in the field of metoprolol pulse osmotic pump controlled-release tablets and its preparation, can solve the problems of reducing curative effect, easy to develop tolerance, and inability to provide blood drug concentration, etc., to achieve optimal curative effect, The effect of reducing side effects

Active Publication Date: 2010-07-14
CHINA RESOURCES DOUBLE CRANE PHARMA COMPANY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, because metoprolol sustained-release tablets failed to provide the release curve required by chronopharmacology based on the circadian rhythm characteristics of cardiovascular diseases, that is, they could not provide the high concentration of blood drugs required at the peak of cardiovascular diseases. Easy to develop tolerance and reduce curative effect

Method used

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  • Three-stage pulsed release controlled release tablet and preparation method thereof
  • Three-stage pulsed release controlled release tablet and preparation method thereof
  • Three-stage pulsed release controlled release tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Prescription: (1000 tablets)

[0059] Drug-containing layer:

[0060]

[0061] Boost layer:

[0062]

[0063] Lag layer:

[0064]

[0065] Controlled Release Coating:

[0066]

[0067]

[0068] Preparation:

[0069] (1) Pretreatment Pass each component of the raw material through an 80-mesh sieve for subsequent use;

[0070] (2) Preparation of drug-containing layer granules According to the prescription of Example 1, the components of the drug-containing layer (except magnesium stearate) are uniformly mixed by equal addition method, added to a fluidized bed, and sprayed into 95% ethanol aqueous solution to prepare granules; after fully drying, pass through a 20-mesh sieve, granulate, then add magnesium stearate and mix evenly, as drug-containing layer granules, set aside;

[0071] (3) Preparation of booster layer granules According to the prescription in Example 1, mix the components of the booster layer (except magnesium stearate) according to the p...

Embodiment 2

[0079] Prescription: (1000 tablets)

[0080] Drug-containing layer:

[0081]

[0082] Boost layer:

[0083]

[0084] Lag layer:

[0085]

[0086] Controlled Release Coating:

[0087]

[0088] Preparation method: the preparation method is the same as that in Example 1, except that the time-lag coating layer and the controlled-release coating layer are formulated according to Example 2.

[0089] Release measurement method: with embodiment 1.

[0090] see results figure 1 , the drug release has a time lag of about 4 hours, the incremental drug release time is about 3 hours, and the constant rate drug release lasts for 9 hours.

Embodiment 3

[0092] Prescription: (1000 tablets)

[0093] Drug-containing layer:

[0094]

[0095] Boost layer:

[0096]

[0097] Lag layer:

[0098]

[0099] Controlled Release Coating:

[0100] Preparation method: the preparation method is the same as that in Example 1 except that the composition of the prescription is different.

[0101] Release measurement method: with embodiment 1.

[0102] see results figure 1 , the drug release has a time lag of 2 hours, the incremental drug release time is 2 hours, and the constant rate drug release duration is 8 hours.

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Abstract

The invention provides a metoprolol pulse osmotic pump controlled release tablet and a preparation method thereof. The controlled release tablet comprises a tablet core, a time lag coating layer and a controlled release coating layer with a release orifice from inside to outside, wherein the tablet core consists of a drug containing layer and a boosting layer, based on the gross weight of the drug containing layer, the drug containing layer comprises 5-65 wt% of metoprolol as active material and 35-95 wt% of pharmaceutically acceptable carrier; based on the gross weight of the boosting layer, the boosting layer comprises 30-85 wt% of swelling agent and 15-70 wt% of osmotic pressure promoting agent; the weight gain of the time lag coating layer is 5-50 wt% of the tablet core; and the weight gain of the controlled release coating layer is 3-30 wt% of the tablet core. The metoprolol pulse osmotic pump controlled release tablet has three-stage release behavior, and is characterized in that the tablet has 2-5 hours time lag at the initial period after being taken orally, increased release is showed at the intermediate period, and release at constant speed is showed at the later period.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a metoprolol pulse osmotic pump controlled-release tablet and a preparation method thereof. Background technique [0002] In recent years, with the continuous improvement of people's living standards in our country and the continuous increase of the elderly population, the incidence of cardiovascular and cerebrovascular diseases such as hypertension and angina pectoris is increasing year by year. According to the World Health Organization (WHO) statistics on the mortality rate of various diseases in the world, the proportion of cardiovascular and cerebrovascular diseases represented by hypertension and angina pectoris in the total death toll increased from 28.8% in 1997 to 2002. 36.0%, cardiovascular and cerebrovascular diseases are becoming a serious threat to human health killer. [0003] Recent research results have shown that the high mortality rate of cardiovascul...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K9/30A61K31/138A61K47/38A61K47/36A61K47/34A61K47/32A61P9/10A61P9/12A61K47/10
Inventor 甘勇朱春柳郭彦亮甘莉
Owner CHINA RESOURCES DOUBLE CRANE PHARMA COMPANY
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