Felodipine solid dispersion (SD) and preparation method thereof

A technology of solid dispersion and dipine solid state, which is applied in the direction of non-active ingredient medical preparations, drug combinations, pharmaceutical formulas, etc., can solve the problems of complex preparation process, cumbersome production process, and no description of dissolution results, etc., and achieve simple preparation process , the effect of easy-to-control preparation methods

Inactive Publication Date: 2013-04-03
SUZHOU INST OF NANO TECH & NANO BIONICS CHINESE ACEDEMY OF SCI
View PDF6 Cites 6 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chinese patent application number 200410018414.3 fully mixes felodipine and filler, binding agent, disintegrating agent, and tabletting makes felodipine dispersible tablet, but the patent only discloses the preparation method of dispersible tablet, does not do to dissolution result further description
Chinese patent application number 200610103992.6 discloses a felodipine single-chamber double-layer osmotic pump controlled-release pharmaceutical composition, which effectively controls the release of the drug, but the patent composition is divided into a drug-containing layer, a booster layer, a coating layer, etc. Different compositions, the production process is relatively cumbersome
Aiming at the problem of the impact of the use of solvents on the stability of felodipine caused by wet granulation, Cao Chengyong et al. disclosed a method based on dry granulation (application number 201010549054.5), which micronizes felodipine together with a dispersant After chemicalization, dry granulation is used to prepare felodipine pharmaceutical preparations, which avoids the use of water and organic solvents, reduces the heat and humidity process and production energy consumption, and is convenient for quality control in the production process, but the dry method also has the disadvantage that it is not easy to mix the medicine with the Phenomenon of mixing of excipients
[0004] Above-mentioned prior art method has played the effect of solubilization and slow-release to the dissolving of felodipine medicine to a certain extent, but preparation process is complicated, exists the solvent residue problem that brings because of the adding of organic solvent
Although the preparation of solid dispersions by dry granulation and melting methods can eliminate the problem of solvent residues, there are still technical defects such as uneven sample mixing

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
  • Felodipine solid dispersion (SD) and preparation method thereof
  • Felodipine solid dispersion (SD) and preparation method thereof
  • Felodipine solid dispersion (SD) and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0023] The embodiment of the present invention also discloses the preparation method of the above-mentioned felodipine solid dispersion, comprising: weighing and uniformly mixing the felodipine active drug and the solid dispersion carrier according to a certain mass ratio, and hot-melt extruding the mixture to obtain an extrudate , cooled to room temperature, and a solid dispersion was obtained after grinding.

[0024] The present invention is further illustrated by the following examples: According to the following examples, the present invention can be better understood. However, those skilled in the art can easily understand that the specific material ratios, process conditions and results described in the examples are only used to illustrate the present invention, and should not and will not limit the present invention described in the claims.

Embodiment 1

[0025] Embodiment 1: solid dispersion 1

[0026] Take by weighing 2 g of felodipine medicine and 18 g of solid dispersion carrier Soluplus, after uniform mixing, the mixture is fed into a hot-melt extruder at a suitable temperature, the screw speed of the extruder is: 20 rpm, and the extrusion temperature is: At 130 ℃, a transparent strip-shaped extrudate was obtained from the exit of the extruder, cooled to room temperature, crushed to a certain particle size according to subsequent preparation or analysis requirements, sieved, and collected a solid dispersion with a particle size of 75-250 μm.

Embodiment 2

[0027] Embodiment 2: solid dispersion 2

[0028] Weigh 4 g of felodipine drug and 16 g of solid dispersion carrier Soluplus, after uniform mixing, the mixture is fed into a hot-melt extruder, the extruder screw speed is: 20 rpm, extrusion temperature: 130 °C, Obtain a transparent strip extrudate from the exit of the extruder, cool to room temperature, crush to a certain particle size according to subsequent formulation or analysis requirements, sieve, and collect a solid dispersion with a particle size of 75-250 μm.

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

No PUM Login to view more

Abstract

The invention discloses a felodipine drug solid dispersion (SD) and a preparation method thereof. The felodipine SD is prepared by taking the indissolvable drug felodipine as the active ingredient, mixing the active drug with a polymer carrier uniformly in a certain proportion and then carrying out hot-melt extrusion. The SD and the preparation method have the beneficial effects that the dissolution rate of felodipine can be effectively increased; and meanwhile, the preparation process is simple and the problems of solvent residues and the like caused by addition of organic solvents are avoided.

Description

technical field [0001] The application belongs to the technical field of chemical pharmacy, in particular to a solid dispersion of felodipine and a preparation method thereof. Background technique [0002] Felodipine, the chemical name is 2,6-dimethyl-4-(2,3-dichlorophenyl)-1,4-dihydro-3,5-pyridine dicarboxylic acid methyl ethyl ester, the molecular formula is C 18 h 19 Cl 2 NO 4 , is a selective calcium antagonist with good antihypertensive effect. The antihypertensive mechanism of felodipine is mainly by inhibiting the inflow of extracellular calcium in arteriolar smooth muscle, selectively dilating arterioles, and has no direct effect on myocardial contractility and cardiac conduction within the therapeutic dose range, and has no direct effect on venous smooth muscle and epinephrine. Vascular tone has no effect, so it is not easy to cause orthostatic hypotension. At the same time, the cheap price and high safety of felodipine also make it one of the most commonly use...

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): A61K9/14A61K31/4422A61K47/34A61K47/32A61P9/12
Inventor 张海禄汪莲艳宋越军邓宗武
Owner SUZHOU INST OF NANO TECH & NANO BIONICS CHINESE ACEDEMY OF SCI
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