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Sustained release preparation for treating hypertention and angina, and preparation method thereof

A technology for sustained-release preparations and angina pectoris, applied in the field of preparation of sustained-release preparations of metoprolol succinate, can solve the problems of cumbersome procedures, difficult storage, increased production costs, etc., achieve simple process production, overcome excessive frequency of administration, Ease of mass production

Active Publication Date: 2013-03-20
KAMP PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] CN102085195A discloses a metoprolol succinate sustained-release tablet and a preparation method thereof. The method adopts a hydrophilic gel-type skeleton as a sustained-release means, and uses a mixture of hydroxypropylmethylcellulose and carbomer as a retarding material , the process is simple, and the materials are easy to obtain. However, due to the poor lubricating effect of the carbomer matrix in this method, it is easy to lose water and mildew, and it is often necessary to add humectants and preservatives, and the amount is larger than other substrates, which makes this method produce Metoprolol succinate sustained-release tablets are not easy to preserve to a certain extent, and the content of the drug itself is also affected
[0005] CN102579368A provides a metoprolol sustained-release microsphere, a metoprolol sustained-release pharmaceutical composition and a preparation method thereof. The pharmaceutical composition of the invention has a simple prescription, is controllable, and has a high encapsulation rate. However, this method has extremely strict requirements on equipment, which virtually increases the production cost of the enterprise, and the low toxicity of its preparation greatly reduces the patient's drug compliance. How to overcome it needs further exploration and research.
[0006] CN102274205A discloses a sustained-release capsule of metoprolol sodium succinate and a preparation method thereof. The method prepares metoprolol sodium succinate pellets, and then coats the sustained-release coating layer on the pellets containing medicine Made into capsules, this method is very operable compared with the traditional process, but the process is relatively cumbersome and has certain limitations compared with practical production

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Prescription (10,000 capsules in batch):

[0030] Metoprolol Succinate 475g

[0031] Hypromellose E3-LV 30g

[0032] Hypromellose E5-LV 150g

[0033] Span-85 45g

[0034] Ethyl cellulose aqueous dispersion 1000g

[0035] Blank ball core 600g

[0036] 1. Pellet preparation process:

[0037] Weigh the main drug and auxiliary materials of the prescribed amount respectively, and pass through a 100-mesh sieve. Then weigh the blank pellet core and place it in the fluidized bed, open the induced draft fan and use the vacuum suction pipe to suck the blank pellet core into the coating machine, top the cylinder, open the air door, and open it after the pellets flow in the fluidized bed to a normal state. With an electric heating device, the temperature was raised to 40°C and kept for 30 minutes. Dissolve metoprolol succinate in HPMC E3 aqueous solution, stir well, and grind it with a colloid mill, then make up with p...

Embodiment 2

[0044] Prescription (10,000 capsules in batch):

[0045] Metoprolol Succinate 475g

[0046] Hypromellose E3-LV 30g

[0047] Hypromellose E5-LV 170g

[0048] Span-85 45g

[0049] Ethylcellulose aqueous dispersion 1250g

[0050] Blank ball core 600g

[0051] Preparation:

[0052]Weigh the main drug and auxiliary materials of the prescribed amount respectively, and pass through a 100-mesh sieve. Weigh the blank pellet core and place it in the fluidized bed, turn on the induced fan and use the vacuum suction pipe to suck the blank pellet core into the coating machine, top the cylinder, open the air door, and turn on the electric motor after the pellets flow in the fluidized bed to a normal state. Heating device, the temperature was raised to 40°C and kept for 30 minutes. Dissolve metoprolol succinate in HPMC E3 aqueous solution, stir well, and grind it with a colloid mill, then make up with purified water, stir well...

Embodiment 3

[0058] Prescription (10,000 capsules in batch):

[0059] Metoprolol Succinate 475g

[0060] Hypromellose E3-LV 30g

[0061] Hypromellose E5-LV 150g

[0062] Span-85 45g

[0063] Ethyl cellulose aqueous dispersion 1000g

[0064] Blank ball core 600g

[0065] Weigh the main drug and auxiliary materials of the prescribed amount respectively, and pass through a 100-mesh sieve. Weigh the blank pellet core and place it in the fluidized bed, turn on the induced fan and use the vacuum suction pipe to suck the blank pellet core into the coating machine, top the cylinder, open the air door, and turn on the electric motor after the pellets flow in the fluidized bed to a normal state. Heating device, the temperature was raised to 40°C and kept for 30 minutes. Dissolve metoprolol succinate in HPMC E3 aqueous solution, stir well, and grind it with a colloid mill, then make up with purified water, stir well and set aside. Adju...

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PUM

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Abstract

The invention relates to the field of drug preparations, and discloses a preparation method for a metoprolol succinate sustained release preparation, and a preparation method thereof. The method comprises the following steps: firstly, coating solution with well prepared raw materials and auxiliary materials onto blank pellets to form a medicating layer, coating a well prepared swelling layer and a sustained release layer on the medicating layer, and finally filling the coated pellets into hard capsules. The method is simple to operate, short in production period, high in efficiency, low in cost, controllable in process, the pellets are evenly coated, the appearance is round and normal and uniform, the stability is good, and the sustained release preparation is convenient to use and used for fully reducing the drug use frequencies of patients with hypertention and angina.

Description

technical background [0001] The invention relates to the field of pharmaceutical preparations, and relates to a sustained-release preparation for treating hypertension and angina pectoris and a preparation method thereof, in particular to a preparation method of a sustained-release preparation of metoprolol succinate. Background technique [0002] In recent years, with the improvement of people's living standards, the prevalence of cardiovascular diseases has also shown a growing trend. [0003] Metoprolol is a selective β1 receptor blocker and one of the commonly used drugs for the treatment of hypertension, coronary heart disease and angina pectoris. For patients with tachyarrhythmia, this product can block the effect of increased sympathetic nerve activity and slow down the heart rate. This is mainly by reducing the automaticity of pacemaker cells and prolonging the time of supraventricular conduction. In patients after myocardial infarction, metoprolol can reduce the r...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/52A61K31/138A61K47/38A61P9/10A61P9/12
Inventor 曾培安朱敏吴健民张静刘娟贺莲
Owner KAMP PHARMA
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