Metoprolol succinate sustained-release tablet and preparation method thereof

A technology of metoprolol succinate and sustained-release tablets, which can be applied to pharmaceutical formulations, medical preparations containing no active ingredients, medical preparations containing active ingredients, etc., and can solve the differences in drug release and release consistency defects, etc. problems, to achieve the effect of simplifying the production process, reducing the difficulty of process amplification, and reducing environmental pollution

Active Publication Date: 2022-01-14
北京联嘉医药科技开发有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Our research found that the in vitro drug release of such sustained-release tablets will have significant differences before and after splitting, and there are potential defects in the release consistency after patients follow the doctor's instructions to split and take

Method used

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  • Metoprolol succinate sustained-release tablet and preparation method thereof
  • Metoprolol succinate sustained-release tablet and preparation method thereof
  • Metoprolol succinate sustained-release tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Metoprolol succinate hot-melt granules with different compositions and their preparation

[0055] Weigh each component of F3-1 to F3-6 prescription amount, mix each component evenly, and prepare the premixture into slow-release granules by hot-melt extrusion process under the condition of 100-110°C. See Table 5 for the compositions of F3-1 to F3-6 hot-melt particles.

[0056]

[0057] Weigh a certain amount of metoprolol succinate hot-melt granules from F3-1 to F3-6 (equivalent to 47.5 mg of metoprolol succinate), and measure the release rate of each prescription hot-melt granule within 24 hours . The results showed that the metoprolol succinate hot-melt granules prepared by using the selected molten materials could achieve the sustained-release effect in the 24-hour in vitro dissolution test. It can be used in the preparation of sustained-release solid preparations such as capsules or tablets.

[0058]

Embodiment 2

[0066] Preparation of Metoprolol Succinate Sustained-release Tablets by Direct Compression Tablets Using Hot-melt Granules

[0067] Use the metoprolol succinate hot-melt granule prepared in embodiment 1, take by weighing each component of F5-1 to F5-6 prescription amount respectively according to table 9, each prescription is mixed with each component except lubricant, and then Mix it again with an additional lubricant, and after mixing thoroughly, use a punch with a score to directly compress the tablet to prepare metoprolol succinate sustained-release tablets F5-1 to F5-6.

[0068]

[0069] Take metoprolol succinate sustained-release tablets F5-1 to F5-6, and measure the release rate of the sustained-release tablets before and after splitting along the notch direction. The measurement results are shown in Table 10. The results showed that metoprolol succinate sustained-release tablets F5-1 to F5-6 showed sustained-release effects in the 24-hour in vitro dissolution test, ...

Embodiment 3

[0072] Preparation of metoprolol succinate extended-release tablets by wet granulation process using hot-melt granules

[0073] Weigh the hot-melt granules F3-4 prepared in Example 1, lactose, and pregelatinized starch according to the prescription in Table 11, and after mixing thoroughly, use PVP K29 / 32 aqueous solution to carry out wet granulation, and dry the obtained wet granulated granules. Sieve, then crush the granules on the sieve, and finally mix the granules under the sieve and the crushed granules on the sieve with the added lubricant stearic acid, and then use a punch with a score to perform tableting to prepare metoprolol succinate Sustained-release tablet F6-1.

[0074]

[0075] Take metoprolol succinate sustained-release tablet F6-1, and measure the release rate of the sustained-release tablet before and after splitting along the notch direction, and see Table 12 for the measurement results. The results showed that metoprolol succinate sustained-release tabl...

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Abstract

The present invention provides a metoprolol succinate sustained-release tablet and a preparation method thereof. Metoprolol succinate sustained-release particles are firstly prepared by adopting a hot melting process, and then the metoprolol succinate sustained-release tablet is prepared by granulating and tabletting the sustained-release particles, a disintegrating agent and other additional auxiliary materials. The metoprolol succinate sustained-release tablet provided by the invention has dissolution consistency before and after breaking under the condition that the metoprolol succinate sustained-release tablet is broken off by a patient according to the doctor's advice, can avoid the problem that a sustained-release particle coating layer in the existing sustained-release tablet is easy to break during tablet pressing, can significantly simplify the production process, and reduces the manufacturing cost of a unit preparation, and the clinical medication requirements under the condition of medical insurance cost control in China are met.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to metoprolol sustained-release tablets with dissolution consistency before and after splitting and a preparation method thereof. Background technique [0002] Metoprolol is a commonly used drug for the treatment of hypertension, coronary heart disease, chronic heart failure and arrhythmia. The blocking effect on the β2 receptor is relatively strong, and the blocking effect on the β2 receptor is very weak, and the receptor selectivity is more significant, and this selectivity is closely related to the dosage at the same time. [0003] AstraZeneca (AstraZeneca) Pharmaceutical Co., Ltd. has released Metoprolol Succinate Sustained-release Tablets (trade name: Betaloc), with specifications of 23.75mg, 47.5mg, 95mg and 190mg. Since the solubility of metoprolol succinate in water at 37°C (270mg / ml) is significantly lower than that of metoprolol tartrate (above 700mg / ml), it can...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K31/138A61K47/38A61K47/32A61K47/36A61P9/12A61P9/10A61P9/04A61P9/06
CPCA61K9/2054A61K9/2059A61K9/2027A61K9/2095A61K31/138A61P9/12A61P9/10A61P9/04A61P9/06
Inventor 龚健徐彦李敏钱云飞顾鑫
Owner 北京联嘉医药科技开发有限公司
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