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Aureobasidin A and nystatin composition and composite ointment, gel and spray thereof

A composite gel and nystatin technology, which is applied in the field of medicine, can solve problems affecting the treatment effect of patients, drug resistance, and recurrent disease

Pending Publication Date: 2020-12-18
珠海中科先进技术研究院有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the first-line drug for the clinical treatment of oral candidiasis is the antifungal antibiotic nystatin, and other antifungal drugs such as fluconazole, miconazole, and itraconazole are also used as adjuvant therapy, but long-term use of the above broad-spectrum antifungal agents Fungal drugs can produce drug resistance, leading to recurrent disease and affecting the treatment effect of patients
[0004] For oral candidiasis, there are Nystatin Tablets (Zhenyuan) and Nystatin Tablets (Lukang) currently on the market, but since both contain only one active ingredient, drug resistance still exists
[0005] In addition, because the complexity of the oral environment is higher than that of other internal environments in the human body, the texture of the drug has a great influence on its effective antibacterial degree in actual drug use
The medicines in the prior art have a single texture and are difficult to smear or the degree of bacteriostasis is greatly reduced after smearing

Method used

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  • Aureobasidin A and nystatin composition and composite ointment, gel and spray thereof
  • Aureobasidin A and nystatin composition and composite ointment, gel and spray thereof
  • Aureobasidin A and nystatin composition and composite ointment, gel and spray thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0027] The preparation method of above-mentioned composite ointment comprises the steps:

[0028] S1. Put Aureobasicin A and Nystatin in a mixing tank, add polyoxyethylene (40) stearate and ethyl formate and mix and stir for 5 minutes at 40° C. to obtain an active ingredient solution;

[0029] S2. Put white vaseline, liquid paraffin, and glycerin in a mixing tank, heat and stir at 78° C. until all melted, and obtain a matrix solution;

[0030] S3. Cool the active ingredient solutions and matrix solutions obtained in the step S1 and the step S2 to 50° C. and mix them uniformly to obtain the composite ointment containing aureus A and nystatin.

[0031] Preferably, the medicine is a gel, and the composite gel is composed of the following raw materials, and the quality of each raw material in every 1000ml of the composite gel is respectively: 15g aureobasicin A and nystatin composition, 230g porol Sham, 20g chitosan, 20g hyaluronic acid, 0~25g carboxypropyl-β-cyclodextrin, 0~25g ...

Embodiment 1

[0047] The minimum inhibitory concentration (MIC) of the composition of aureobasicin A and nystatin against Candida albicans was determined.

[0048] Experimental method: inoculate Candida albicans suspension in broth medium, culture overnight at 37°C, correct the bacterial solution to make it equivalent to 0.5 McFarland turbidimetric standard, and then dilute it with broth medium at 1:200 for later use .

[0049] Prepare 11 test tubes, take one test tube to prepare 2ml of Pulebamycin A broth medium solution with a working concentration of 50μg / ml, take 1ml and add it to the test tube containing 1ml broth medium, mix well, suck out 1ml and add to the second In the three tubes, after the 11th tube by analogy, aspirate 1ml and discard it. The final content of A. , 0.049 μg / ml.

[0050] The nystatin broth medium solution with a working concentration of 50 μg / ml was configured and prepared according to the above method, and the gradient dilution was performed in the same way.

...

Embodiment 2

[0061] Various formulations of composite ointments of aureobasicin A and nystatin were prepared and the antibacterial activity of the composite ointments against Candida albicans was tested.

[0062] Composite ointments containing aureus A and nystatin compositions with different components were prepared according to the formulations in Table 2, and were divided into groups A1 to A9 according to different formulations, and the components not contained were indicated by "\". .

[0063] According to the method of the present invention, prepare the compound ointment containing pullobasicin A and nystatin composition of above-mentioned A1~A9 group formula, and carry out bacteriostasis test to above-mentioned each group compound ointment respectively, each group compound ointment in different time The diameter of inhibition is shown in Table 3.

[0064] Table 2 A1~A9 group compound ointment formula containing aureobasicin A and nystatin composition

[0065]

[0066] Table 3 An...

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PUM

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Abstract

The invention relates to an aureobasidin A and nystatin composition as well as composite ointment, gel and spray thereof. In the composition, the mass ratio of aureobasidin A to nystatin is (1.29-4):1; The composition is used for treating oral candidiasis. A medicine containing the composition solves the problem of drug resistance caused by single antibiotic medication. Besides, the invention also provides composite ointment, composite gel and composite spray containing the composition. Animal experiments prove that the finished product medicaments containing three textures have obviously higher treatment effects on oral candidiasis than commercially available medicaments containing single components.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a composition of aureus A and nystatin and its composite ointment, gel and spray. Background technique [0002] Aureobasidin A (AbA), also known as Aureobasidin A, is a cyclic lipopeptide antifungal antibiotic derived from Aureobasidium pullulans, which can effectively inhibit Saccharomyces cerevisiae, Candida albicans, Cryptococcus and other fungi activity. The mechanism of action of Pulebamycin A is to inhibit the activity of inositol phosphatidyl ceramide synthetase on which fungal growth depends, hinder the synthesis of ceramide to inositol phosphatidyl ceramide, rupture the fungal cell membrane, and kill the fungus. Foreign literature has shown that aureobasidin A has antibacterial activity against Candida albicans (Munusamy K., Vadivelu J.&Tay ST.A study on Candida biofilm growth characteristics and its susceptibility to aureobasidinA.2016; 1130-1406), with certain drug ...

Claims

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Application Information

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IPC IPC(8): A61K38/12A61K31/7048A61K9/06A61K9/12A61P1/02A61P31/10
CPCA61K38/12A61K31/7048A61K9/06A61K9/12A61K9/006A61K47/44A61K47/40A61P1/02A61P31/10A61K2300/00
Inventor 徐畅谢桦函卢申姣陈婉玲高飞姜长安
Owner 珠海中科先进技术研究院有限公司