Berberine-carried carboxymethyl Beta-cyclodextrin functional montmorillonite drug releasing system

A technology of carboxymethyl cyclodextrin and cyclodextrin, applied in the field of plant active ingredient berberine, can solve the problems of affecting the release and absorption of active ingredient berberine, easy aggregation and precipitation of montmorillonite particles, etc. The effect of improving utilization, drug loading and drug release

Inactive Publication Date: 2017-08-11
CHONGQING MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the process of studying the montmorillonite-loaded berberine drug delivery system, the inventors found that the montmorillonite particles in the drug-loaded system tend to aggregate and precipitate, thus affecting the release and absorption of the active ingredient berberine

Method used

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  • Berberine-carried carboxymethyl Beta-cyclodextrin functional montmorillonite drug releasing system
  • Berberine-carried carboxymethyl Beta-cyclodextrin functional montmorillonite drug releasing system
  • Berberine-carried carboxymethyl Beta-cyclodextrin functional montmorillonite drug releasing system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Example 1 Preparation of carboxymethyl β-cyclodextrin functionalized montmorillonite material

[0048] Preparation of Carboxymethylcyclodextrin (CMCD)

[0049] Weigh 9.3g of sodium hydroxide into a round bottom flask, add 37mL of deionized water and place in an ice-water bath and stir until completely dissolved. Add 10g of β-cyclodextrin and stir to dissolve. Prepare 27mL of 16.3% monochloroacetic acid aqueous solution and set aside. Place the above-mentioned round-bottomed flask in a constant temperature water bath at 60°C, slowly add an aqueous solution of chloroacetic acid (completely added within 20 minutes) dropwise, and after reacting for 5 hours, pour the reaction solution into a large beaker, and drop while stirring after cooling. Add concentrated hydrochloric acid until the pH test paper detects that it is neutral. Add a large amount of anhydrous methanol to the beaker, stir rapidly, and a white precipitate can be seen. Suction filtration, collect the white...

Embodiment 2

[0062] Embodiment 2 The establishment of berberine hydrochloride ultraviolet spectrophotometry content determination method

[0063] Determination of Ultraviolet Absorption Wavelength of Berberine Hydrochloride (BBH)

[0064] Accurately weigh 18 mg of berberine hydrochloride standard product dried at 105°C to constant weight, dissolve it completely with ultrapure water, and then set the volume in a 25 mL volumetric flask to obtain a berberine hydrochloride stock solution. Precisely draw 1 mL of berberine hydrochloride stock solution into a 25 mL volumetric flask to make up to volume, and finally prepare a berberine hydrochloride solution with a concentration of 29 μg / mL. The absorbance was measured by scanning in the range of 200-600 nm with a UV-Vis spectrophotometer. The results showed that berberine hydrochloride had maximum absorption at three wavelengths of 228, 263, and 345nm. In order to avoid the possible interference of impurities near the low wavelength of 200nm, th...

Embodiment 3

[0073] Example 3 CMCD-APTES-MMT Supramolecular Network Material Drug Loading Performance Examination Experiment

[0074] Calculate the drug loading rate of CMCD-APTES-MMT according to the following formula:

[0075]

[0076] Effect of drug loading time on drug loading rate

[0077] Weigh 50mg of berberine hydrochloride into a round bottom flask, add 100mL of ultrapure water and heat to dissolve, weigh 100mg of CMCD-APTES-MMT and evenly disperse in the above drug solution, keep stirring, and at the selected time point: 0.5, 1, 2 , 3, 4, 5, and 6 hours, precisely draw the suspension, centrifuge at 12,000 rpm for 5 minutes, collect the supernatant, and filter the supernatant with a 0.45 μm microporous membrane to remove suspended particles. The content of free berberine hydrochloride in the supernatant was determined by ultraviolet spectrophotometry at a wavelength of 345nm. All samples were tested in triplicate in parallel. Depend on Figure 5 It can be seen that the drug...

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Abstract

The invention provides a carboxymethyl Beta-cyclodextrin functional montmorillonite supramolecular network material. According to the infrared spectroscopy generated by the material, absorption peaks are displayed at positions of 3421cm<-1>, 2934cm<-1>, 1637cm<-1>, 1414cm<-1>, 1159cm<-1>, 1087cm<-1>, 1039cm<-1>, 745cm<-1>, 613cm<-1>, and 587cm<-1>. The drug releasing system is prepared by using a CMCD-APTES-MMT supramolecular network as a carrier of berberine hydrochloride, the dispersing property and solubility of berberine hydrochloride in the water are obviously increased, and the bioavailability of berberine hydrochloride is effectively improved; compared with a drug carrier system taking montmorillonite as a carrier, the drug loading capacity is obviously improved, the local release amount is greatly improved, and the material has stronger antibacterial effect. The drug releasing system prepared by taking the CMCD-APTES-MMT supramolecular network as the carrier of berberine hydrochloride has very strong germ capturing ability; meanwhile, the CMCD-APTES-MMT supramolecular network also can envelope the germ thallus, so that the contact between the berberine hydrochloride loaded therein and germ is enhanced, and the antimicrobial property of berberine hydrochloride is improved.

Description

technical field [0001] The invention relates to a plant active ingredient berberine, in particular to a carboxymethyl beta-cyclodextrin functionalized montmorillonite drug delivery system loaded with berberine. Background technique [0002] Infection caused by bacteria is one of the important factors that endanger human health. Globally, 15% of children under the age of 5 who died of illness were caused by diarrhea caused by bacterial infection, ranking second in the mortality rate after pneumonia (18%). For nearly a century, antibiotics have been widely used in the prevention and treatment of clinical bacterial infections. However, about 5-25% of patients with bacterial infections treated with antibiotics will have side effects such as diarrhea and inflammation. In addition, the overuse of antibiotics has made the problem of bacterial resistance increasingly serious, and has also caused a significant reduction in the efficacy of antibiotics. The existing antibacterial dru...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K47/40A61K47/02A61K31/4375A61P31/04
CPCA61K47/02A61K31/4375A61K47/40
Inventor 于明安王施韦
Owner CHONGQING MEDICAL UNIVERSITY
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