Multi-unit release pharmaceutical composition of amlodipine maleate and preparation method of pharmaceutical composition

A technology of amlodipine maleate and its composition is applied in the multi-unit release pharmaceutical composition of amlodipine maleate and its preparation field, which can solve the problems of low bioavailability and achieve high bioavailability, no The effect of residual organic solvent and low extrusion temperature

Active Publication Date: 2017-04-26
NORTHEAST PHARMA GRP
View PDF3 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, amlodipine is a water-insoluble drug with a solubility of only 75.3 mg / L in water and low bioavailability

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
  • Multi-unit release pharmaceutical composition of amlodipine maleate and preparation method of pharmaceutical composition
  • Multi-unit release pharmaceutical composition of amlodipine maleate and preparation method of pharmaceutical composition
  • Multi-unit release pharmaceutical composition of amlodipine maleate and preparation method of pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Pass the amlodipine maleate through an 80-mesh sieve, and pass the dry granulation-related auxiliary materials through an 80-mesh sieve.

[0034] Amlodipine maleate (40%), dry granulation related excipients microcrystalline cellulose (22%), lactose (32%) croscarmellose sodium (4%), colloidal silicon dioxide ( 1%), magnesium stearate (1%) mix homogeneously, it is 5kN to set dry granulator pressure, and the feeding rod rotating speed is 10rpm, and 24 orders of pulverized granules obtain quick-release granules, measure its angle of repose and be 40.64 °, fluidity It is acceptable, but there is a phenomenon that the fill level is unstable during the capsule filling process, and the difference in tablet weight is 3.4%. Capsules are filled according to drug content. The in vitro dissolution results show that 50% of the dissolution takes 5 minutes, and more than 85% of the dissolution is reached in 10 minutes (note, the dissolution conditions in each embodiment of the applica...

Embodiment 2

[0036] Pass amlodipine maleate through an 80-mesh sieve, and pass hot-melt extrusion-related auxiliary materials through an 80-mesh sieve.

[0037] Amlodipine maleate (30%), hot-melt extrusion-related auxiliary materials polyvinyl acetate / polyvinylpyrrolidone (Kollidon SR, BASF) (59%), Span 20 (10%) anhydrous calcium hydrogen phosphate (0.5 %), sodium stearyl fumarate (0.5%) mix homogeneously, set the temperature of twin-screw extruder to be 125 ℃, when temperature rises to set temperature, add in the extruder of raw material system by feeding scale, The obtained molten extrudate is extruded in flake form by cold roll cooling, and then pulverized with a hammer mill. The number of meshes is 24 orders to obtain slow-release granules. The angle of repose is 32.13°, and the fluidity is good. During the process, the filling amount is relatively stable. It is 0.3% to measure its sheet weight difference. Capsules are filled according to drug content. The in vitro dissolution curve...

Embodiment 3

[0039]Pass amlodipine maleate through a 80-mesh sieve, and pass through an 80-mesh sieve for dry granulation-related auxiliary materials and hot-melt extrusion-related auxiliary materials.

[0040] Amlodipine maleate (40%), dry granulation related excipients microcrystalline cellulose (22%), lactose (32%) croscarmellose sodium (4%), colloidal silicon dioxide ( 1%), magnesium stearate (1%) mix homogeneously, set dry granulator pressure to be 5kN, feed rod rotating speed is 10rpm, pulverizes 24 orders of granules to obtain quick-release granules. Amlodipine maleate (30%), hot-melt extrusion related accessories polyvinyl acetate / polyvinylpyrrolidone (Kollidon SR) (59%), Span 20 (10%), anhydrous calcium hydrogen phosphate (0.5%) ), sodium stearyl fumarate (0.5%) are mixed evenly, the temperature of setting twin-screw extruder is 125 ℃, when temperature rises to set temperature, add in the extruder of raw and auxiliary material system by feeding scale, obtain The melted extrudate ...

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 sizeaaaaaaaaaa
Login to view more

Abstract

The invention belongs to the technical field of pharmaceutical preparations, and relates to a multi-unit release pharmaceutical composition of amlodipine maleate and a preparation method of the pharmaceutical composition. The pharmaceutical composition consists of the following components in percentage by weight: 10-95% of sustained-release particles containing the amlodipine maleate, 5-90% of quick-release particles containing the amlodipine maleate and 0-5% of other adjuvants. The sustained-release particles are prepared by virtue of hot-melt extrusion and the quick-release particles are prepared by virtue of dry granulation, the sustained-release particles and the quick-release particles are mixed according to a certain proportion and a lubricant is added in accordance with a formulated amount, so that the pharmaceutical composition is prepared. The pharmaceutical composition and a preparation method thereof have the advantages that the rapid dissolution of drugs can be promoted to achieve a treatment concentration and the drugs can take lasting effects, the bioavailability of the amlodipine maleate is high, the stability of the finished product (the composition) is good, and the preparation process is simple and easy to operate, low in energy consumption, free from residue of organic solvents and easy for implementation of large-scale continuous production.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to a multi-unit release pharmaceutical composition of amlodipine maleate and a preparation method thereof. Background technique [0002] Amlodipine maleate is a calcium antagonist, which can be widely used in the treatment of various types of hypertension and angina, especially spontaneous angina. The mechanism of action of amlodipine is to lower blood pressure by reducing total peripheral resistance by relaxing the smooth muscle of the arterial wall; in angina pectoris, amlodipine increases blood flow to the myocardium. However, amlodipine is a poorly water-soluble drug with a solubility of only 75.3 mg / L in water and low bioavailability. [0003] At present, hot-melt extrusion technology is used to mix insoluble drugs and polymer materials to prepare solid dispersions, and then cut them into fine particles, so as to improve the solubility, bioavailability and ...

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): A61K9/52A61K31/4422A61K47/38A61K47/32A61P9/12A61P9/10A61P9/08
CPCA61K9/0002A61K9/1635A61K9/1652A61K9/1694A61K31/4422
Inventor 孙聚魁宋林黄文姝邢丹周联波
Owner NORTHEAST PHARMA GRP
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap