Metroprolol succinate hydrochlorothiazide sustained-release pellet capsule and preparation method thereof

A technology of toprolol hydrochlorothiazide and metoprolol succinate, which is applied in the field of metoprolol hydrochlorothiazide succinate sustained-release pellet capsules and its preparation, can solve the problem of the absence of metoprolol succinate hydrochlorothiazide sustained-release pellet preparations Production and marketing and registration declaration, difficult promotion of production technology, and sudden release of preparations, etc., to achieve the effects of small differences in individual bioavailability, continuous and stable antihypertensive effect, and uniform absorption speed

Inactive Publication Date: 2013-06-12
广州科的信医药技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Sustained-release tablets need to be produced by double-layer tableting equipment, and local damage and defects during production will lead to burst release of the entire preparation, so its production technology is difficult to promote and has poor safety
At present, only metoprolol succinate sustained-release tablets imported by ASTRAZENECA LP and domestic hydrochlorothiazide ordinary preparations have been listed in the domestic market. There is no metoprolol succinate hydrochlorothiazide sustained-release pellets for the time being. , 24-hour release of metoprolol succinate hydrochlorothiazide sustained-release pellets and capsules have good clinical application advantages

Method used

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  • Metroprolol succinate hydrochlorothiazide sustained-release pellet capsule and preparation method thereof
  • Metroprolol succinate hydrochlorothiazide sustained-release pellet capsule and preparation method thereof
  • Metroprolol succinate hydrochlorothiazide sustained-release pellet capsule and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0041] 1. Preparation of metoprolol succinate sustained-release pellets:

[0042] prescription:

[0043]

[0044] Preparation process: Mix metoprolol succinate and microcrystalline cellulose evenly, and make powder for later use. Dissolve PVP K30 in purified water, add the above mixed powder to make a soft material, use the extrusion spheronization method to make the core of the pill, dry, sieve and take the core of the pill of 20-30 mesh, and use it for coating. Prepare Eudrag it NE30D, talcum powder and titanium dioxide with purified water to prepare a slow-release coating solution with a solid content of 20%, dissolve and stir to make it fully dispersed. Put the core of the pellet containing the drug in a fluidized bed, adjust the process parameters to ensure the fluidized state, spray the slow-release coating solution on the surface of the core of the pellet containing the drug, take out the pellet and put it in an oven at 40°C for 24 hours to prepare the succinate To...

Embodiment 2

[0051] 1. Preparation of metoprolol succinate sustained-release pellets:

[0052] prescription:

[0053]

[0054] Preparation process: Dissolve metoprolol succinate and PVP K30 in ethanol, place the blank pellet core in a fluidized bed, adjust the process parameters to ensure the fluidized state, spray the above drug-containing solution on the surface of the pellet core, and dry , and sifted to select 20-30 mesh pill cores containing medicine. Ethyl cellulose, talcum powder and titanium dioxide are prepared with ethanol into a slow-release coating solution with a solid content of 10%, dissolved and stirred to make them fully dispersed. Put the core of the pellet containing the drug in a fluidized bed, adjust the process parameters to ensure the fluidized state, spray the slow-release coating solution on the surface of the core of the pellet containing the drug, take out the pellet and put it in an oven at 50 ° C for 10 hours to prepare the succinate Torol extended-release...

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Abstract

The invention discloses a metroprolol succinate hydrochlorothiazide sustained-release pellet capsule and a preparation method thereof. The metroprolol succinate hydrochlorothiazide sustained-release pellet capsule is prepared by mixing a metroprolol succinate sustained-release pellet and a hydrochlorothiazide quick-release pellet according to provided dose ratio, and filling into a hard capsule. The metroprolol succinate sustained-release pellet constantly releases the medicine for 24 hours, and the medicine is taken once a day, thereby retaining the lasting antihypertensive effect; the hydrochlorothiazide quick-release pellet is rapidly absorbed so as to achieve the diuresis and antihypertensive effect, and by combining the pellets, the antihypertensive effect is doubled, the toxic and side effects of the medicine are reduced, the number of the medicine administrations is reduced, and lasting and stable antihypertensive effects are achieved in vivo, so that the compliance of patients is improved; and meanwhile as the sustained-release pellet preparation is composed of hundreds of pellets of uniform granule sizes, the sudden release of the whole preparation is not caused by the breakage of individual pellets, so that the medicine is safer than a sustained-release tablet, smaller in irritation to gastrointestinal tracts and more stable in blood concentration, and the clinical effectiveness and security are effectively improved.

Description

technical field [0001] The invention relates to the technical field of sustained-release preparations, in particular to metoprolol succinate hydrochlorothiazide sustained-release pellet capsules and a preparation method thereof. It belongs to the class of Sustained-release preparations of antihypertensive drugs. Background technique [0002] Hypertension is one of the most common cardiovascular diseases, and it is also a major risk factor leading to increased morbidity and mortality of congestive heart failure, stroke, coronary heart disease, renal failure, and aortic aneurysm. In recent years, with the continuous improvement of the living standards of the Chinese people and the growth of the elderly population, hypertension is becoming a common disease with a very high prevalence rate and has entered our lives. At present, there is no effective way to cure hypertension in the world. Once the disease is diagnosed, it will be accompanied by lifelong and cause many other rela...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/549A61K31/138A61K9/62A61K9/58A61P9/12A61P7/10
Inventor 黎炜烘
Owner 广州科的信医药技术有限公司
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