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

Metoprolol tartrate sustained release pellet and preparation method thereof

A technology of metoprolol tartrate and sustained-release pellets is applied in the directions of pharmaceutical formulations, medical preparations containing active ingredients, and bulk delivery, which can solve problems such as danger, air pollution, and difficulty in recycling, and achieve true spherical High density, low production cost and uniform particle size distribution

Active Publication Date: 2012-07-11
JINLING PHARMA
View PDF12 Cites 3 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Organic solvents have obvious disadvantages, such as unsafe, explosive hazards; air pollution, potential toxicity; difficult recovery and expensive recovery equipment, etc.

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
  • Metoprolol tartrate sustained release pellet and preparation method thereof
  • Metoprolol tartrate sustained release pellet and preparation method thereof
  • Metoprolol tartrate sustained release pellet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] Ball core formula: parts by weight

[0067] Metoprolol tartrate 100 parts

[0068] 95% ethanol 50 parts

[0069] Sustained-release coat formula (taking metoprolol tartrate core as 100 parts by weight):

[0070] Hypromellose 5 parts

[0071] 10% Surelease 250 parts of water dispersion

[0072] Note: 10% Surelease The aqueous dispersion is ethyl cellulose aqueous dispersion.

[0073] Preparation process: prepare three batches of ball cores according to the "Example Description" and the above formula, the quality evaluation results are shown in Table 3 below, and the properties of the ball cores are shown in Table 3. Picture 1-1 , 1-2 , 1-3.

[0074] Table 3: Ball core quality evaluation

[0075] Evaluation index / batch Batch 1 Batch 2 Batch 3 aspect ratio (E) 1.07 1.1 1.08 Comprehensive form factor (eR) 0.97 0.94 0.98 Friability (Fl) 0.007 0.007 0.008 Yield (Yd) 0.85 0.88...

Embodiment 2

[0077] Ball core formula: parts by weight

[0078] Metoprolol tartrate 100 parts

[0079] 75% ethanol 50 parts

[0080] Isolation gown formula (taking metoprolol tartrate core as 100 parts by weight):

[0081] 5% hydroxypropyl methylcellulose aqueous solution 80 parts

[0082] Sustained-release coat formula (based on 100 parts by weight of the metoprolol tartrate ball core of the pack isolation coat):

[0083] 10% Surelease Water dispersion 200 parts

[0084] Note: 10% Surelease The aqueous dispersion is ethyl cellulose aqueous dispersion.

[0085] Preparation process: Prepare three batches of ball cores according to the "Example Description" and the above formula, the quality evaluation results are shown in Table 4 below, and the properties of the ball cores are shown in Table 4. diagram 2-1 , 2-2 , 2-3.

[0086] Table 4: Ball core quality evaluation

[0087] Evaluation index / batch Batch 1 Batch 2 Batch 3 aspect ratio (E) 1.04 1.07 ...

Embodiment 3

[0089] Ball core formula: parts by weight

[0090] Metoprolol tartrate 100 parts

[0091] 70% ethanol 40 parts

[0092] Sustained-release coat formula (taking metoprolol tartrate core as 100 parts by weight):

[0093] 10% Eudragit NE30D water dispersion 300 parts

[0094] Note: Utage NE30D aqueous dispersion is the aqueous dispersion of ethyl acrylate-methyl methacrylate copolymer (2:1).

[0095] Preparation process: prepare three batches of ball cores according to the "Example Description" and the above formula, the quality evaluation results are shown in Table 5 below, and the properties of the ball cores are shown in Table 5. Figure 3-1 , 3-2 , 3-3.

[0096] Table 5: Ball core quality evaluation

[0097] Evaluation index / batch Batch 1 Batch 2 Batch 3 aspect ratio (E) 1.07 1.1 1.06 Comprehensive form factor (eR) 0.97 0.95 0.98 Friability (Fl) 0.008 0.01 0.007 Yield (Yd) 0.84 ...

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
particle diameteraaaaaaaaaa
particle size (mesh)aaaaaaaaaa
Login to View More

Abstract

The invention belongs to the field of medicinal preparation and discloses a metoprolol tartrate sustained release pellet and a preparation method thereof. The pellet is prepared by the following steps: preparing a parent kernel and a pellet core by using a centrifugal granulation method and spraying a sustained release coat on the pellet by using a fluidized bed coating method; and the method specifically comprises the following steps: (a) preparation of the parent kernel: taking metoprolol tartrate fine powder; adding the metoprolol tartrate fine powder into a pellet processing machine; spraying a wetting agent into the fine powder so as to form a certain number of parent kernels; and screening the parent kernels by using a screening method; (b) preparation of the pellet core: taking the parent kernels; adding the parent kernels into the pellet processing machine; spraying a wetting agent so that the surfaces of the parent kernels are wet; meanwhile, feeding the metoprolol tartrate fine powder into the pellet processing machine so that the parent kernels are laminated to be grown to pellet cores; and screening the pellet cores by using a screening method so as to obtain target pellet cores; and (c) coating of the pellet cores: taking the pellet cores; adding the pellet cores into a fluidized bed; and spraying sustained release coats on the pellet cores by using the fluidized bed coating method. The metoprolol tartrate sustained release pellet disclosed by the invention has the advantages of high true sphericity, small particle size, uniform particle size distribution, low production cost and medicine content of 100% in the pellet core.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a metoprolol tartrate sustained-release pellet and a preparation method thereof. Background technique [0002] The chemical name of metoprolol tartrate is 1-isopropylamino-3-[p-(2-methoxyethyl)phenoxy]-2-propanol, and its molecular formula is (C 15 h 25 NO 3 ) 2 ·C 4 h 6 o 6 , the molecular weight is 652.83, and the chemical structural formula is as follows: [0003] [0004] Metoprolol tartrate is suitable for the relief of symptoms including hypertension, angina pectoris, myocardial infarction, hypertrophic cardiomyopathy, aortic dissection, arrhythmia, hyperthyroidism, and heart failure. [0005] Due to the advantages of beautiful appearance, good fluidity, large drug content, easy to make sustained and controlled release preparations, stable drug release, high bioavailability, and small local irritation, micropills have become one of the key dosage forms in ...

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
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/138A61K31/205A61P9/12A61P9/10A61P9/00A61P9/06A61P5/16A61P9/04
Inventor 黄春玉薛斐王明浩邢芸杨俊孙烨姬晓燕
Owner JINLING PHARMA
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