Unlock instant, AI-driven research and patent intelligence for your innovation.

Preparation of salified medicinal particles of levosalbutamol and traditional Chinese medicine monomer and preparation of particle inhalable aerosol

A technology for levosalbuterol and medicine is applied in the field of preparation of inhaled aerosols, which can solve the problems of increasing drug permeability, increasing drug solubility and the like, and achieves multiple clinical indications, good dispersion performance and stability, and improved delivery efficiency. Effect

Active Publication Date: 2013-09-25
MEDONCARE PHARMA CO LTD
View PDF3 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the preparation of combined drugs is also a difficult problem faced by those skilled in the art. How to make the drug particles containing active ingredients ultra-fine or nano-sized, with better dispersibility, high deposition efficiency on lesions, and increase the effect of drugs on biological The permeability of the membrane is conducive to the transdermal absorption of drugs, the exertion of intracellular drug effects, and the increase of drug solubility. These issues need to be further studied by those skilled in the art.

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] (L)-4-[2-(tert-butylamino)-1-hydroxyethyl]-2-(hydroxymethyl)phenol 4.79g (0.02mol) and 4-hydroxy-3-methoxycinnamic acid 4.10 g (0.021mol) was dissolved in 100mL ethanol, heated to reflux for 2-7 hours, cooled to room temperature, filtered, eluted with 3X10mL ethanol, suction filtered, and vacuum-dried to constant weight to obtain 8.2g solid substance. The purity determined by liquid chromatography is greater than or equal to 99.5%. The state of the solid may be amorphous, polycrystalline, eutectic, hydrate, solvate.

Embodiment 2

[0031] Mix (L)-4-[2-(tert-butylamino)-1-hydroxyethyl]-2-(hydroxymethyl)phenol 4.79g (0.02mol) with 1,8-dihydroxy-3-carboxyanthraquinone Dissolve 5.69g (0.02mol) in a mixed solution of 100mL methanol and 10mL acetone, heat and reflux for 2-7 hours, distill off methanol and add 60mL of ethanol at the same time, stop heating when methanol is distilled off, cool to room temperature, filter, and use 3X10mL ethanol Elution, suction filtration, vacuum drying to constant weight. 9.84 g of solid material were obtained. Purity >99.8% as determined by liquid chromatography. The state of the solid may be amorphous, polycrystalline, eutectic, hydrate, solvate.

Embodiment 3

[0033]Mix (L)-4-[2-(tert-butylamino)-1-hydroxyethyl]-2-(hydroxymethyl)phenol 4.79g (0.02mol) with 3,4-dihydroxybenzoic acid 3.23g (0.021 mol) was dissolved in 100mL ethanol, heated to reflux for 2-7 hours, cooled to room temperature, filtered, filtered with 3X10mL ethanol, vacuum-dried to constant weight to obtain 7.62g solid substance. The purity determined by liquid chromatography is greater than or equal to 99.5%. The state of the solid may be amorphous, polycrystalline, eutectic, hydrate, solvate.

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
Login to View More

Abstract

The invention relates to preparation of salified medicinal particles of levosalbutamol and a traditional Chinese medicine monomer and a preparation of a particle inhalable aerosol. The invention provides a method for preparing three salbutamol acid salts obtained by levosalbutamol and the traditional Chinese medicine monomer compounds including ferulic acid, rheinic acid and protocatechuic acid. The invention also provides a method for preparing the medicinal particles obtained by a single active component or more than two active components of the salt and the medicinal adjuvants under the supercritical fluid state, and a combination of a preservative preparation and a compound medicinal preparation containing at least one salt. The obtained medicinal particles can be prepared into the quantitatively inhalable aerosol, power aerosols and other physiologically acceptable preparation types.

Description

technical field [0001] The present invention relates to levosalbutamol and three kinds of traditional Chinese medicine monomer compounds used for the treatment of bronchial asthma, asthmatic bronchitis, bronchospasm, emphysema and other symptoms into salts and made into drug granules; Process for the preparation of an inhalation aerosol as active ingredient. Background technique [0002] β2 receptor agonists are currently the most widely used bronchodilators in clinical practice, among which salbutamol and terbutaline are short-acting β2 receptor agonists widely used in the treatment of acute attacks of asthma in aerosol inhalation. Inhalation administration, including aerosol, dry powder and nebulized solution, can directly act on bronchial smooth muscle. Its anti-asthma effect is fast, usually takes effect within a few minutes, and the curative effect can last for 4-6 hours. However, there may be overdose or adverse reactions including palpitations, skeletal muscle tremo...

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 Patents(China)
IPC IPC(8): A61K9/16A61K9/12A61K31/205A61P11/06A61P11/00A61P31/04A61K31/137A61K31/192
Inventor 刘晓忠
Owner MEDONCARE PHARMA CO LTD