Method for preparing gallic acid quinolone drug salt and preparation method thereof

A technology of gallic acid quinolone and gallic acid, which is applied in the field of medicine to achieve the effect of expanding antibacterial spectrum, enhancing antibacterial activity, and reducing the production of drug-dependent strains

Inactive Publication Date: 2012-03-28
HUNAN UNIV OF CHINESE MEDICINE
View PDF0 Cites 6 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The application of the above two types of drugs is a single drug. With the change of the global environment, human diseases have become more and more complicated. Therefore, it is very necessary to develop drugs that have antibacterial, anti-inflammatory, antiviral and tumor effects at the same time.

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
  • Method for preparing gallic acid quinolone drug salt and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Embodiment 1 The preparation of ofloxacin gallate

[0016] Add 170.1 g (1 mol) of gallic acid (1 mol) and 361.4 g (1 mol) of ofloxacin into a 1000 mL three-neck reaction flask, add them to an appropriate amount of 80% ethanol solution, stir, heat to dissolve, and reflux for 2~3 h, add an appropriate amount of activated carbon, reflux for 0.5 h, filter while it is hot, the filtrate is cooled and crystallized, filtered, washed with a small amount of 80% ethanol, and dried in vacuum at 60-80 °C for 8-10 h.

[0017]

Embodiment 2

[0018] Embodiment 2, norfloxacin gallate tablet:

[0019] Prescription: Norfloxacin Gallate 153 g

[0020] Starch 40 g

[0021] Lactose 30 g

[0022] Microcrystalline cellulose 12 g

[0023] Sodium carboxymethyl starch 3 g

[0024] 3%HPMC appropriate amount

[0025] Magnesium stearate 1 g

[0026] A total of 1000 pieces

[0027] Preparation method: take norfloxacin gallate, microcrystalline cellulose, carboxymethyl starch sodium starch and lactose, mix uniformly, add 3% HPMC aqueous solution appropriate amount, make suitable soft material, granulate with 16 mesh nylon mesh, The wet granules are evenly spread on the drying tray, and are quickly ventilated and dried at 60 ℃, and the moisture content is controlled at 1~2%. Add magnesium stearate to the dry granules, mix well, sizing the granules with a 14-mesh nylon net, and control the pressure at 4~5 kg / cm after mixing 2 Compress the tablet to get norfloxacin gallate tablet.

[0028] Other embodiments: adopt 2...

Embodiment 3

[0029] Embodiment 3, levofloxacin gallate dispersible tablet:

[0030] Prescription: Levofloxacin Gallate 147 g

[0031] Microcrystalline cellulose 100 g

[0032] Croscarmellose Sodium 80 g

[0033] 5% povidone K30 ethanol solution appropriate amount

[0034] Micronized silica gel 6g

[0035] Magnesium stearate 1.5 g

[0036] Makes 1000 pieces

[0037]Preparation method: Weigh 80-100 mesh gallo-levofloxacin, croscarmellose sodium, and microcrystalline cellulose, mix well and add 5% povidone K30 ethanol solution to make a suitable soft material. Use 16-mesh nylon mesh to granulate, spread the wet granules evenly in the drying tray, and dry quickly at 60°C, controlling the moisture content to 1-2%. Add micropowder silica gel and magnesium stearate to the dry granules, mix well, and sizing the granules with a 14-mesh nylon net. After mixing, control the pressure to 4~5 kg / cm 2 Diffusion tablet promptly gets levofloxacin gallate dispersible tablet.

[003...

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 relates to a method for preparing a gallic acid quinolone drug salt and a preparation method thereof. By adopting the method provided by the invention, a series of gallic acid quinolone drug salts are prepared, such as gallic acid norfloxacin, gallic acid ciprofloxacin, gallic acid ofloxacin, gallic acid levofloxacin, gallic acid prulifloxacin, gallic acid pefloxacin, gallic acid mosifloxacin and the like. The gallic acid quinolone drug salt prepared by the invention has pharmacological action of quinolone and also has the pharmacological action of gallic acid, two different pharmacological action mechanisms can realize synergic antibacterial action, and the gallic acid quinolone drug salt can be prepared into tablets, dispersible tablets and capsules used for oral administration and injection used for injection and also can be prepared into suppository and lotion which are used for local application (rectum application and vagina application). The quinolone drug is a broad spectrum antibiotic, and the gallic acid has antibacterial, antiviral and antitumour functions. The preparation method of the quinolone drug salt can mutually enhance antibacterial action after being applied.

Description

technical field [0001] The invention relates to medicinal quinolone gallic acid salts, preparations and preparation methods thereof, and belongs to the technical field of medicines. Background technique [0002] The chemical name of gallic acid is 3,4,5-trihydroxybenzoic acid, also known as gallic acid, research on the medicinal use of gallic acid and the activity of its extract. Gallic acid has a long history of medicinal use and has been included in the national pharmacopoeia. The drug has antibacterial and antiviral effects, and has antibacterial and antiviral effects in vitro on Staphylococcus aureus, Sarcina, α-type key coccus, Neisseria, Pseudomonas aeruginosa, Shigella flexneri, Salmonella typhi Hd, Salmonella paratyphi A, etc. Inhibitory effect, its antibacterial concentration is 5mg / ml, in vitro, it has antibacterial effect on 17 kinds of fungi at a concentration of 3%. Combined application with amphotericin B, terbinacol, etc., has obvious antifungal synergistic e...

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): C07C65/03C07C51/41C07D215/56C07D498/06C07D401/04C07D471/04C07D513/04C07D513/06A61K31/542A61K31/5383A61K31/519A61K31/496A61K31/4709A61K31/4375A61K31/192A61P31/02A61P31/04A61P31/10A61P29/00A61P31/12A61P35/00
Inventor 彭东明刘艳飞王福东卢茂芳
Owner HUNAN UNIV OF CHINESE MEDICINE
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