Check patentability & draft patents in minutes with Patsnap Eureka AI!

Freeze-dried powder injection for injecting brazilein and preparation method thereof

A technology of hematoxylin and needle injection, applied in the field of medicine, can solve problems such as poor water solubility, and achieve the effects of being convenient for transportation and storage, overcoming poor water solubility and high safety

Inactive Publication Date: 2011-03-16
TSINGHUA UNIV
View PDF3 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The object of the present invention is to provide a kind of brazilian hematoxylin injection freeze-dried powder injection and its preparation method, to overcome the defect of brazilian hematoxylin poor water solubility, so as to meet the concentration requirements of clinical injections; at the same time, it is convenient for transportation and storage

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
  • Freeze-dried powder injection for injecting brazilein and preparation method thereof
  • Freeze-dried powder injection for injecting brazilein and preparation method thereof
  • Freeze-dried powder injection for injecting brazilein and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0014] Experimental Example 1 Pre-prescription study of Brazilian hematoxylin powder injection

[0015] Brazil hematoxylin (brasilein or brazilein) extracted from hematoxylin (C 16 h 12 o 5 ) structural formula as attached figure 1 .

[0016] The physical and chemical characteristics are as follows:

[0017] Brown-black powder (MeOH). mp: 260-265°C (dec.).

[0018] TLC examination: white fluorescence under 365nm ultraviolet light.

[0019] EI-MS m / z: 284 (M+), 242, 174.

[0020] UV (MeOH) nm: 205, 276, 446.

[0021] 1 H NMR (DMSO-d 6 )δ: 7.81 (1H, d, J = 8.5Hz), 6.57 (1H, dd, J = 8.5, 2.0Hz), 6.36 (1H, d, J = 2.0Hz), 6.33 (1H, s), 7.11 ( 1H, s), 4.01 (1H, d, J = 11.5 Hz), 4.47 (1H, d, J = 11.5 Hz), 2.85 (2H, s).

[0022] 13 C NMR (DMSO-d 6 )δ: 39.7 (C-7), 72.9 (C-6), 74.2 (C-6a), 102.8 (C-4), 104.1 (C-11), 110.8 (C-1a), 110.8, (C- 2), 117.5(C-8), 126.0(C-11a), 130.5(C-1), 151.5(C-12), 152.3(C-10), 157.7(C-4a), 158.9(C-7a ), 162.2(C-3), 179.3(C-9).

[0023] 1. ...

experiment example 2

[0045] Experimental Example 2 Preparation of Brazilian Hematoxylin-Hydroxypropyl-β-Cyclodextrin Inclusion Compound

[0046] 1. Determination of inclusion stability constant

[0047] Five concentrations of HP-β-CD aqueous solutions of 1%, 5%, 10%, 15%, and 20% were prepared, and excess brazilian hematoxylin was added respectively, and ultrasonication was performed for 10 minutes. Shake at a constant temperature of 25°C, 37°C, and 50°C for 24 hours, respectively, to make it reach the dissolution equilibrium, and let it stand still. The supernatant was taken, and the concentration of brazilian hematoxylin was determined by HPLC. The concentration of brazilian hematoxylin (mmol / L) was plotted against the concentration of HP-β-CD (mmol / L), and the equilibrium phase solubility diagram was drawn. Perform linear regression on the straight line in the equilibrium phase solubility diagram, and calculate the apparent stability constant Kc under various temperature conditions according ...

experiment example 3

[0062] Experimental Example 3 Verification of Brazilian Hematoxylin-Hydroxypropyl Inclusion Complex

[0063] 1. NMR method

[0064] Brazilian hematoxylin was deuterated dimethyl sulfoxide (DMSO) as solvent, HP-β-CD and clathrate were deuterium water (D 2 O) as a solvent 1 H-NMR analysis. according to 1 H-NMR results, H in the cavity of HP-β-CD 3 The chemical shift shifted from 4.026ppm downfield to 4.064ppm, a shift of 0.038ppm, while the H in the cavity 5 And the chemical shifts of the other hydrogens, including the solvent peak, all moved downfield by 0.035ppm. According to the above 1H-NMR experimental results, it is judged that brazilian hematoxylin has entered into the cavity of HP-β-CD, and it is compatible with H 3 Linked, indicating that the drug has formed an inclusion complex with HP-β-CD.

[0065] 2. Infrared spectroscopy

[0066] The infrared spectra of brazilian hematoxylin, HP-β-CD, physical mixture of brazilian hematoxylin and HP-β-CD and clathrate were ...

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 freeze-dried powder injection for injecting brazilein and a preparation method thereof, belonging to the technical field of medicines. The freeze-dried powder injection for injecting brazilein, which is provided by the invention, contains brazilein and hydroxypropyl-beta-cyclodextrin, and the weight ratio of the brazilein to the hydroxypropyl-beta-cyclodextrin is 1:150-300. The preparation method of the freeze-dried powder injection comprises the following steps: firstly, dissolving the hydroxypropyl-beta-cyclodextrin into the distilled water; adding the brazilein into the hydroxypropyl-beta-cyclodextrin solution the PH value of which is 6.0-7.5; stirring and carrying out inclusion for 1-3h at 30-50 DEG C; filtering by a microporous filtering film; adding activated carbon for filtering; then, adding the water for injection into the filtered solution to the full dose; respectively packaging in antibiotic bottles; and freeze-drying to obtain finished products. The invention has the advantage that the defects that the brazilein has poor water solubility, and the concentration of the saturated water solution of the brazilein can not meet the requirements of the injection are solved. The invention has the characteristics of good redissolution property, good stability, high safety and the like, and is convenient in storage and transportation.

Description

Technical field: [0001] The invention provides a Brazilian hematoxylin injection freeze-dried powder injection and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Sappan is the dry heartwood of Caesalpinia sappan L., a leguminous plant. It is mainly used for promoting blood circulation and removing blood stasis, reducing swelling and relieving pain. According to existing reports, sumac has anti-atherosclerosis, inhibition of inducible nitrogen oxide synthase, and anti-convulsant effects. At the same time, sumac also has anti-complement activity, antioxidant activity and antibacterial activity. Brazilian hematoxylin (Brazilein) is the main chemical component in hematoxylin. Animal experiments have proved that Brazilian hematoxylin can be used to treat diseases caused by elevated blood pressure in the body, such as various types of hypertension, atherosclerosis, coronary heart disease, cerebral thrombosis and cerebral...

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
IPC IPC(8): A61K9/19A61K31/352A61K47/48A61P9/10A61P9/12A61K47/69
Inventor 杜力军朱春燕雷帆安琳娜邢东明王玉刚胡珺李伯男柴玉爽詹宏磊
Owner TSINGHUA UNIV
Features
  • R&D
  • Intellectual Property
  • Life Sciences
  • Materials
  • Tech Scout
Why Patsnap Eureka
  • Unparalleled Data Quality
  • Higher Quality Content
  • 60% Fewer Hallucinations
Social media
Patsnap Eureka Blog
Learn More

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

© 2025 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com