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CN-122005634-A - Compound antibacterial gel of herba Pileae Scriptae, and preparation method and application thereof

CN122005634ACN 122005634 ACN122005634 ACN 122005634ACN-122005634-A

Abstract

The invention discloses a compound antibacterial gel of herba sarcandrae, a preparation method and application thereof, and belongs to the technical field of oral pharmaceutical preparations, wherein the gel comprises, by weight, 2-8 parts of 90% ethanol eluate of herba sarcandrae, 0.5-2 parts of eugenol, 0.3-1 part of gallic acid, 1-2 parts of carbomer 940, pH (potential of hydrogen) regulated by triethanolamine to 6.5-7.0, 15-25 parts of glycerol and the balance of purified water, the 90% ethanol eluate of herba sarcandrae is rich in dihydrochalcone compounds, has remarkable inhibitory activity on porphyromonas gingivalis and fusobacterium nucleatum, has a synergistic antibacterial effect by three-component compounding, does not obviously inhibit streptococcus mutans, and realizes the selective action on periodontal pathogenic bacteria.

Inventors

  • CHEN JIANZHOU
  • LIU HUI
  • CHEN XIN
  • SHI HUI
  • LI ZEXI
  • YANG ANPING

Assignees

  • 贵州盛世泰合医药科技有限公司
  • 佛山大学

Dates

Publication Date
20260512
Application Date
20260413

Claims (10)

  1. 1. The compound antibacterial gel is characterized by comprising, by weight, 2-8 parts of an extract of herba sarcandrae, 0.5-2 parts of eugenol, 0.3-1 part of gallic acid, 1-2 parts of carbomer 940, a pH regulator, adjusting the pH of the gel to 6.5-7.0, 15-25 parts of glycerol and purified water, wherein the extract of herba sarcandrae is obtained by extracting a herba sarcandrae medicinal material with 90% ethanol, extracting the extract with dichloromethane, and eluting a dichloromethane layer concentrate with 90% ethanol by silica gel column chromatography.
  2. 2. The compound antibacterial gel of herba sarcandrae is characterized in that the preparation of the 90% ethanol eluate of herba sarcandrae comprises the steps of crushing dry herba sarcandrae medicinal materials, extracting with 8-12 times of 90% ethanol under reflux for 2-3 times, 1-2 hours each time, combining extract solutions, concentrating under reduced pressure to obtain an extract, dispersing the extract with water, sequentially extracting with petroleum ether and dichloromethane, collecting dichloromethane extract, subjecting the dichloromethane extract to silica gel column chromatography, sequentially eluting with petroleum ether-ethyl acetate gradient, eluting with 90% ethanol, collecting 90% ethanol eluate fraction, concentrating under reduced pressure, and drying.
  3. 3. The compound antibacterial gel of herba sarcandrae according to claim 1, wherein the eugenol is used in an amount of 0.8-1.5 parts.
  4. 4. The compound antibacterial gel of herba sarcandrae according to claim 1, wherein the dosage of gallic acid is 0.5-0.8 part.
  5. 5. The compound antibacterial gel of herba sarcandrae, according to claim 1, wherein the amount of the 90% ethanol eluate of herba sarcandrae is 4-6 parts.
  6. 6. The preparation method of the compound antibacterial nine-herb tea gel according to any one of claims 1-5 is characterized by comprising the steps of (1) preparing a gel matrix, dispersing carbomer 940 in purified water, standing and swelling for 8-16 hours at room temperature to obtain a uniform and transparent gel matrix, (2) preparing an active component solution, namely dissolving 90% ethanol eluate of nine-herb tea, eugenol and gallic acid in glycerol, stirring until the active component solution is completely dissolved, and (3) mixing, namely slowly adding the active component solution into the gel matrix under the condition of continuous stirring, dropwise adding triethanolamine to adjust the pH value to 6.5-7.0 after stirring uniformly, continuing stirring until a gel system is uniform and transparent, and (4) degassing and filling, namely degassing the gel under the vacuum condition for 10-20 min, and filling.
  7. 7. The method according to claim 6, wherein in the step (1), the feeding ratio of carbomer 940 to purified water is 1:40 to 1:60, and the swelling temperature is 20 ℃ to 30 ℃.
  8. 8. The method according to claim 6, wherein in the step (3), the stirring speed is 200-500 r/min, and the stirring time is 20-40 min.
  9. 9. The method according to claim 6, wherein in the step (4), the step of pasteurizing at 60 ℃ for 30 minutes is further included after the deaeration.
  10. 10. The use of an kappaphycus alvarezii compound antibacterial gel according to any one of claims 1 to 5 in the preparation of a periodontal pocket topical formulation.

Description

Compound antibacterial gel of herba Pileae Scriptae, and preparation method and application thereof Technical Field The invention belongs to the technical field of oral pharmaceutical preparations, and particularly relates to a compound antibacterial gel of sarcandra glabra, a preparation method and application thereof. Background Periodontitis is a chronic infectious disease caused by periodontal pathogens, the major pathogens of which include Porphyromonas gingivalis (Porphyromonas gingivalis) and Fusobacterium nucleatum (Fusobacterium nucleatum). Porphyromonas gingivalis is one of the most critical pathogenic bacteria for periodontitis, and produces gingival proteases and lipopolysaccharides that destroy periodontal tissue and activate the host inflammatory response. Fusobacterium nucleatum plays a core bridge role in the formation process of periodontal biomembrane and connects early-stage field bacteria with late-stage pathogenic bacteria. At present, nitroimidazole antibiotics such as metronidazole, tinidazole and the like and beta-lactam antibiotics such as amoxicillin and the like are mainly used for clinically treating periodontitis. However, long-term use of antibiotics is likely to cause the generation of drug-resistant strains, and systemic administration has problems such as gastrointestinal adverse reactions. Chinese patent CN101978961B discloses a composition for treating gingivitis or periodontitis, which mainly consists of amoxicillin, metronidazole, trimethoprim and vitamin B6, belonging to a multiple antibiotic combination regimen. The scheme has the defects of high antibiotic drug resistance risk, obvious gastrointestinal side effect and the like, and dose form optimization is not carried out aiming at the periodontal pocket local administration. Chinese patent CN116492369B discloses a traditional Chinese medicine polysaccharide composition with anti-inflammatory and hemostatic functions, the active ingredients of which are the combination of sarcandra glabra polysaccharide and elsholtzia polysaccharide prepared from ginger, and the composition is mainly applied to oral care products such as toothpaste and the like. The technical proposal utilizes the anti-inflammatory activity of plant polysaccharide, but not the direct antibacterial effect of small molecular compound, and the toothpaste formulation is difficult to realize effective medicine retention in periodontal pocket. Herba Pileae Scriptae (SARCANDRA GLABRA) is plant of genus herba Pileae Scriptae of family Chloranthaceae, also called herba Pileae Scriptae, and has been widely used for treating stomatitis. Modern pharmacological studies show that the herba sarcandrae contains rich flavonoids, terpenes and organic acid compounds, wherein the dihydrochalcone compounds have remarkable antibacterial activity. However, no report of compounding the herba Pileae Scriptae dihydrochalcone enriched fraction with eugenol and gallic acid to obtain periodontal pocket topical gel is known in the prior art. Therefore, the development of natural product-based topical gel formulations that target dental Zhou Ya oxygen pathogenic bacteria would be of great clinical value for reducing antibiotic use and reducing risk of drug resistance. Disclosure of Invention Aiming at the defects existing in the prior art, the invention aims to provide a compound antibacterial gel of sarcandra glabra and a preparation method thereof. The gel takes the 90% ethanol eluate of the herba sarcandrae as the main medicine, and is compounded with eugenol and gallic acid, and carbomer 940 is adopted as the gel matrix, so that the gel preparation suitable for the local administration of periodontal pockets is formed. The gel has remarkable inhibitory activity on the main pathogenic bacteria of periodontitis, namely Porphyromonas gingivalis and Fusobacterium nucleatum, has synergistic antibacterial effect among three active components, has no obvious inhibitory effect on normal symbiotic bacteria streptococcus mutans of the oral cavity, and realizes the selective inhibition on periodontal pathogenic bacteria. In order to achieve the aim, the technical scheme is that the compound antibacterial gel comprises, by weight, 2-8 parts of a herba sarcandrae-tea 90% ethanol eluate, 0.5-2 parts of eugenol, 0.3-1 part of gallic acid, 1-2 parts of carbomer 940, pH adjustment of triethanolamine to 6.5-7.0, 15-25 parts of glycerol and 100 parts of purified water. In a second aspect, the invention provides a method for preparing the gel, which comprises the steps of gel matrix preparation, active component solution preparation, mixing and blending, and degassing and filling. Compared with the prior art, the preparation method has the advantages that 90% ethanol eluent of sarcandra glabra is used as a main medicine, the fraction is rich in dihydrochalcone compounds, the minimum inhibitory concentration of Wu Fange statin on Porphyromonas gingivalis is 16 mu mol/L, the minimum inhibitory conc