Search

CN-122005688-A - Chinese herbal compound preparation for enhancing transdermal absorption and antibacterial activity and preparation and application thereof

CN122005688ACN 122005688 ACN122005688 ACN 122005688ACN-122005688-A

Abstract

The invention belongs to the technical field of medicines, and in particular relates to a traditional Chinese medicine compound preparation for enhancing transdermal absorption and antibacterial activity, and preparation and application thereof. The preparation is prepared by adding functional auxiliary materials based on classical formulas of herba patriniae, radix clematidis and ephedra to improve the performance, and specifically comprises, by mass, 20 parts of herba patriniae, 15 parts of radix clematidis, 15 parts of ephedra, 0.1-0.5 part of transdermal enhancer, 3-10 parts of nano liposome carrier and 0.2-0.8 part of natural antibacterial synergist, wherein the transdermal enhancer comprises menthol, laurocapram and D-limonene, and the nano liposome carrier comprises soybean lecithin, cholesterol and polyethylene glycol. The invention can flexibly adapt to a plurality of dosage forms such as lotion, gel, cream, spray and the like through the synergistic effect of the nano liposome carrier, the composite transdermal enhancer and the natural antibacterial synergist, obviously promote the transdermal absorption of active ingredients, widen the antibacterial spectrum and strengthen the inhibition effect on drug-resistant strains.

Inventors

  • HUANG RUOGAN
  • HUANG ZIXUAN
  • WEI NA
  • LIANG CUILING
  • HUANG DEYUAN
  • QIN CUIPING
  • GUAN SHIYUAN
  • ZHANG KAI
  • HUANG TIANYAN
  • Zhong Linjing
  • WU RUNBIN
  • LIU WEIYAN
  • ZHOU CHUN
  • LI YUHUAN
  • WEI YUHANG

Assignees

  • 广西白云山盈康药业有限公司

Dates

Publication Date
20260512
Application Date
20260313

Claims (18)

  1. 1. The three-ingredient traditional Chinese medicine compound preparation for enhancing transdermal absorption and antibacterial activity is characterized by comprising the following raw materials, by mass, 20 parts of herba patriniae, 15 parts of radix clematidis, 15 parts of ephedra, 0.1-0.5 part of transdermal enhancer, 3-10 parts of nano liposome carrier and 0.2-0.8 part of natural antibacterial enhancer.
  2. 2. The three-ingredient traditional Chinese medicine compound preparation for enhancing transdermal absorption and antibacterial activity according to claim 1 is characterized by comprising the following raw materials, by mass, 20 parts of herba patriniae, 15 parts of radix clematidis, 15 parts of ephedra, 0.3 part of transdermal enhancer, 10 parts of nano liposome carrier and 0.8 part of natural antibacterial synergist.
  3. 3. The three-ingredient compound traditional Chinese medicine preparation for enhancing transdermal absorption and antibacterial activity according to claim 1 or 2, wherein the transdermal enhancer comprises menthol, laurocapram and D-limonene.
  4. 4. The three-ingredient compound Chinese medicinal preparation for enhancing transdermal absorption and antibacterial activity according to claim 3, wherein the transdermal enhancer consists of menthol, laurocapram and D-limonene according to a mass ratio of 12-15:3-5:1-2.
  5. 5. The three-ingredient traditional Chinese medicine compound preparation for enhancing transdermal absorption and antibacterial activity according to claim 4, wherein the transdermal enhancer consists of menthol, laurocapram and D-limonene according to a mass ratio of 13:4:1.
  6. 6. The three-ingredient traditional Chinese medicine compound preparation for enhancing transdermal absorption and antibacterial activity according to claim 1 or 2, wherein the nano liposome carrier comprises soybean lecithin, cholesterol and polyethylene glycol.
  7. 7. The three-ingredient traditional Chinese medicine compound preparation for enhancing transdermal absorption and antibacterial activity according to claim 6, wherein the nano liposome carrier consists of soybean lecithin, cholesterol and polyethylene glycol according to a mass ratio of 5-9:1-3:0.2-0.6.
  8. 8. The three-ingredient traditional Chinese medicine compound preparation for enhancing transdermal absorption and antibacterial activity according to claim 7, wherein the nano liposome carrier consists of soybean lecithin, cholesterol and polyethylene glycol according to a mass ratio of 8:2:0.5.
  9. 9. The three-ingredient compound traditional Chinese medicine preparation for enhancing transdermal absorption and antibacterial activity according to claim 6, wherein the molecular weight of the polyethylene glycol is 400-600.
  10. 10. The three traditional Chinese medicine compound preparation for enhancing transdermal absorption and antibacterial activity according to claim 1 or 2, wherein the natural antibacterial synergist is a combination of two or three of tea tree essential oil, eugenol and thymol.
  11. 11. The three-ingredient traditional Chinese medicine compound preparation for enhancing transdermal absorption and antibacterial activity according to claim 10, wherein the natural antibacterial synergist is composed of tea tree essential oil, eugenol and thymol according to a mass ratio of 3:1:1.
  12. 12. The three traditional Chinese medicine compound preparation for enhancing transdermal absorption and antibacterial activity according to claim 1, wherein the 24-hour accumulated transdermal quantity of ephedrine in the preparation is more than or equal to 50 mug/cm < 2 >, and the MIC value of ephedrine is less than or equal to 16 mug/mL for methicillin-resistant staphylococcus aureus.
  13. 13. The three-ingredient combination of any one of claims 1-12, wherein the formulation of the combination comprises a lotion, gel, cream or spray.
  14. 14. The method for preparing the three-ingredient compound Chinese medicinal preparation for enhancing transdermal absorption and antibacterial activity according to any one of claims 1 to 13, comprising the following steps: S1, crushing and sieving herba patriniae to obtain herba patriniae powder, adding water into the herba patriniae powder, wherein the adding amount of water is 7-10 times of the mass of the herba patriniae powder, adding complex enzyme, carrying out enzymolysis, inactivating enzyme, adding an ethanol aqueous solution, carrying out reflux extraction, centrifuging to obtain supernatant and filter residues, adding the ethanol aqueous solution into the filter residues, carrying out reflux extraction, centrifuging to obtain filtrate, and combining the supernatant and the filtrate to obtain a herba patriniae extract; S2, crushing radix clematidis, sieving to obtain radix clematidis powder, adding an ethanol water solution into the radix clematidis powder, wherein the addition amount of the ethanol water solution is 6-9 times of the mass of the radix clematidis powder, carrying out reflux extraction, centrifuging to obtain supernatant and filter residues, adding the ethanol water solution into the filter residues, carrying out reflux extraction, centrifuging to obtain filtrate, and mixing the supernatant and the filtrate to obtain radix clematidis extract; S3, pulverizing and sieving ephedra to obtain ephedra powder, adding water into the ephedra powder for decoction, wherein the adding amount of the water is 10-15 times of the mass of the ephedra powder, filtering to obtain filtrate and filter residue, adding an ethanol water solution into the filter residue, carrying out reflux extraction, filtering to obtain filtrate, and combining the two filtrates to obtain ephedra extract; s4, mixing the herba patriniae extract obtained in the step S1, the radix clematidis extract obtained in the step S2 and the ephedra extract obtained in the step S3, and concentrating to obtain extractum; S5, adding a solvent into the nano liposome carrier, adding the extract obtained in the step S4, adding a buffer solution, and homogenizing to obtain a drug-loaded liposome; s6, mixing the drug-loaded liposome obtained in the step S5 with a transdermal enhancer and a natural antibacterial synergist to prepare the traditional Chinese medicine compound preparation for enhancing transdermal absorption and antibacterial activity.
  15. 15. The preparation method of claim 14, wherein in the step S1, the complex enzyme consists of pectase and beta-glucosidase according to a mass ratio of 4-7:1, wherein the addition amount of the complex enzyme is 2-5% of the mass of the patrinia powder, the enzymolysis temperature is 35-45 ℃, the enzymolysis time is 2-4 hours, the volume fraction of the ethanol aqueous solution is 75-85%, the reflux extraction temperature is 60-70 ℃, and the time is 1-1.5 hours.
  16. 16. The preparation method according to claim 14, wherein the ethanol aqueous solution in step S2 has a volume fraction of 65-75%, the reflux extraction temperature is 70-80 ℃ and the time is 1-2 hours, the water-added decoction in step S3 has a time of 40-60 minutes, the ethanol aqueous solution has a volume fraction of 55-65%, and the reflux extraction temperature is 75-85 ℃ and the time is 50-80 minutes.
  17. 17. The method according to claim 14, wherein the solvent is absolute ethanol in step S5, the homogenization condition is 800bar high pressure homogenization 3 times, and the preparation is sterilized by 0.22 μm filter in step S6.
  18. 18. The use of a three-ingredient combination according to any one of claims 1-13 for enhancing transdermal absorption and antibacterial activity in the manufacture of a medicament for treating itch of skin, eczema, dermatitis or gynecological inflammation.

Description

Chinese herbal compound preparation for enhancing transdermal absorption and antibacterial activity and preparation and application thereof Technical Field The invention belongs to the technical field of medicines, and in particular relates to a traditional Chinese medicine compound preparation for enhancing transdermal absorption and antibacterial activity, and preparation and application thereof. Background Skin itch, eczema, dermatitis, various dermatitis and mucous membrane related diseases are clinically common multiple diseases, and the diseases often have the characteristics of long disease course, easy repeated attack, difficult radical treatment and the like, often accompany symptoms such as itch, red swelling, exudation, erosion or local discomfort, not only seriously influence the daily life, work and sleep quality of patients, but also cause great burden on physiological and psychological health of the patients. The external preparation of the traditional Chinese medicine has unique position and wide application in the treatment of skin and mucous membrane diseases due to the advantages of direct effect, high local concentration, better safety, small toxic and side effects of the whole body and the like. At present, various external traditional Chinese medicine compositions are disclosed in the prior art, and the external traditional Chinese medicine compositions improve local symptoms through the effects of clearing heat and detoxicating, dispelling wind and removing dampness, killing parasites and relieving itching, resisting bacteria and resisting inflammation and the like, so that a certain choice and reference are provided for clinical prevention and treatment of related diseases. The Chinese patent application CN100372550C discloses a traditional Chinese medicine preparation for treating skin itch and gynecological inflammation and a preparation method, the preparation takes patrinia as a principal drug, takes radix clematidis and ephedra as adjuvant drugs, has the functions of clearing heat and detoxicating, dispelling wind and eliminating dampness, killing parasites and relieving itching, relieving the pathogenic factors and enabling the pathogenic factors accumulated between the skin to permeate outside the skin, has wide application, is used for treating gynecological vaginal inflammation, vulvar itch, measles, skin itch, eczema, skin itch caused by pesticide allergy, skin allergy, rhinitis, scabies, chilblain and the like, and is a safe and reliable ideal traditional Chinese medicine external preparation for treating the diseases. Although the preparation has a certain curative effect, the preparation has the following problems in practical application that (1) the transdermal efficiency is low, the effective components (such as oleanolic acid, ephedrine and anemonin) in the traditional water decoction extract have large molecular polarity and poor fat solubility, are difficult to penetrate the stratum corneum of the skin, so that the local medicine concentration is insufficient, the preparation has slow effect, (2) the stability is insufficient, microorganisms are easy to breed in water extract, preservative (such as sodium benzoate) is needed, skin irritation can be caused after long-term use, and (3) the antibacterial spectrum is limited, although the preparation has an inhibitory effect on staphylococcus aureus, candida albicans and the like, the effect on drug-resistant strains (such as methicillin-resistant staphylococcus aureus (MRSA) and fluconazole-resistant candida) is poor, and (4) the preparation is single, namely only a lotion is provided, and the requirements of different indications (such as eczema exudation, chilblain and dry crack) on the preparation (gel, cream and spray) can not be met. Chinese patent application CN114748556A discloses a gynecological external antibacterial effervescent tablet, which also takes herba Patriniae, radix Clematidis and herba Ephedrae as raw materials, improves the use convenience through an effervescent tablet form, but the patent focuses on formulation improvement, does not relate to transdermal absorption enhancement, and does not disclose the synergistic effect of drug-resistant bacteria. Chinese patent CN103278582B relates to the detection method of the above preparation, and does not relate to formulation or drug efficacy improvement. In summary, although the existing three traditional Chinese medicine external preparations have basic treatment efficacy, in practical application, the problems of low transdermal efficiency, insufficient preparation stability, limited antibacterial spectrum, single dosage form and the like exist, and the requirements of clinical high-efficiency treatment, safe use and multi-scene adaptation are difficult to meet. Therefore, development of an upgraded three-ingredient external traditional Chinese medicine preparation which can remarkably improve the transdermal absorption efficiency of active ingredie