Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Preparation method of metoprolol succinate pellet sustained-release tablet

A technology of metoprolol succinate and toprolol pellets, which can be used in medical preparations containing non-active ingredients, medical preparations containing active ingredients, and pill delivery, etc., and can solve the problem of short half-life elimination and fluctuations in plasma drug concentration Larger problems, to achieve the effect of stable process and stable release

Pending Publication Date: 2021-07-23
苏州康恒研新药物技术有限公司
View PDF0 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Metoprolol succinate is a dose-dependent β1 receptor blocker, and the peak blood concentration of sustained-release preparations is lower than that of common preparations with the same dose. Currently, it is widely used in China for hypertension, coronary heart disease, chronic heart failure and Metoprolol tartrate, a selective β1 receptor blocker for the treatment of arrhythmia, is a common tablet of metoprolol. 4 doses

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Preparation method of metoprolol succinate pellet sustained-release tablet
  • Preparation method of metoprolol succinate pellet sustained-release tablet
  • Preparation method of metoprolol succinate pellet sustained-release tablet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Example 1: Preparation of Metoprolol Succinate Pellet Sustained Release Tablets of 190mg Specifications

[0051] 1. The prescription information is as follows:

[0052]

[0053]

[0054] 2. Preparation method:

[0055] (1) Take 60% of the prescription amount of metoprolol succinate and sucrose to manufacture drug-containing pellet cores by high-speed centrifugal atomization. The air inlet temperature is 100°C, and the air outlet temperature is 75°C. 0.079mm;

[0056] (2) The remaining prescription amount of metoprolol succinate is dissolved in purified water, and in a fluidized state, the bottom spray technology is used to spray on the surface of the pill core, and the atomization pressure is maintained at 1.5bar, and the air inlet speed is 10 ~20m 3 / h, the inlet air temperature is controlled at 60-80°C, the material temperature is at 38-45°C, the droplet size is controlled at 20-40μm, and the liquid supply peristaltic pump speed is controlled at 10-25rpm, the...

Embodiment 2

[0061] Embodiment 2: the preparation of the metoprolol succinate pellet sustained-release tablet of 95mg specification

[0062] 1. The prescription information is as follows:

[0063]

[0064]

[0065] 2. Preparation method:

[0066] (1) Take 60% of the prescription amount of metoprolol succinate and sucrose to manufacture drug-containing pellet cores by high-speed centrifugal atomization. The air inlet temperature is 120°C, and the outlet temperature is 75°C. 0.111mm;

[0067] (2) The remaining prescription amount of metoprolol succinate is dissolved in purified water, and in a fluidized state, the bottom spray technology is used to spray on the surface of the pill core, the atomization pressure is maintained at 2.3bar, and the air inlet speed is 15 ~25m 3 / h, the inlet air temperature is controlled at 60-80°C, the material temperature is at 38-45°C, the droplet size is controlled at 20-40μm, and the liquid supply peristaltic pump speed is controlled at 10-25rpm, the...

Embodiment 3

[0072] Example 3: Preparation of Metoprolol Succinate Pellet Sustained Release Tablets of 47.5mg Specification

[0073] 1. The prescription information is as follows:

[0074]

[0075]

[0076] 2. Preparation method:

[0077] (1) Take 60% of the prescription amount of metoprolol succinate and sucrose to manufacture drug-containing pellet cores by high-speed centrifugal atomization, the air inlet temperature is 120°C, the outlet air temperature is 75°C, and the particle size of the drug-containing pellet cores is (D90) Measured to be 0.094mm;

[0078] (2) The metoprolol succinate of remaining prescription quantity is dissolved with 50% methanol water, and under fluidized state, adopts bottom spray technology, sprays on the surface that contains pill core, under the condition that atomization pressure keeps 1.8bar, the air inlet velocity 15-20m 3 / h, the inlet air temperature is controlled at 60-80°C, the material temperature is at 38-45°C, the droplet size is controlle...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
Granularityaaaaaaaaaa
Granularityaaaaaaaaaa
Granularityaaaaaaaaaa
Login to View More

Abstract

The invention discloses a preparation method of a metoprolol succinate pellet sustained-release tablet. The preparation method comprises the following steps of: based on the solubility of metoprolol succinate, spraying part of metoprolol succinate and sucrose in a dissolved state to prepare a metoprolol succinate drug-containing pellet core, and coating the surface of the metoprolol succinate drug-containing pellet core with a drug layer to prepare a drug-loaded pellet; then coating the drug-loaded pellet core with a sustained-release material to prepare a sustained-release coated pellet; and mixing and tabletting the sustained-release coated pellet as a material to prepare a pellet tablet, and wax-sealing the surface of the pellet tablet to isolate water, oxygen and other influencing factors. The metoprolol succinate pellet sustained-release tablet prepared by the preparation method disclosed by the invention is stable in process, can play a good sustained-release role, is stable in release within 24 hours, avoids the phenomena of burst release and difficult dissolution, and can achieve the dissolution behavior consistent with that of an original developing agent in vitro.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a method for preparing metoprolol succinate pellet sustained-release tablets. Background technique [0002] Hypertension is the number one killer of cardiovascular diseases that cause death and disability to the elderly. The World Health Organization pointed out that the number of deaths caused by cardiovascular diseases led by hypertension accounts for 79% of the total death toll in the country. Hypertension and its induced disease seriously threatens human life and health. [0003] Metoprolol Succinate, the chemical name is 1-isopropylamino-3-[p-(2-methoxyethyl)phenoxy]-2-propanol succinate, and the molecular formula is C 34 h 56 N 2 o 10 , the molecular weight is 652.82, and the structural formula is as follows: [0004] [0005] Metoprolol succinate is a dose-dependent β1 receptor blocker, and the peak blood concentration of sustained-release prepa...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K9/22A61K47/38A61K47/32A61K47/10A61K47/26A61K31/138A61P9/12
CPCA61K9/2054A61K9/2018A61K9/5042A61K9/5031A61K9/5026A61K31/138A61P9/12
Inventor 杨永忠刘婷婷高婵
Owner 苏州康恒研新药物技术有限公司
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com