Compound composition based on clotrimazole for gynecology department

Abstract

The invention relates to a composition based on clotrimazole. The composition comprises the clotrimazole and timosaponin B2 used as active ingredients, and at least one ingredient used as a vagina drug delivery preparation, wherein the mass ratio of the clotrimazole and the timosaponin B2 in the composition is (2 to 4) to 1. The composition is prepared into a gel or a cream, the content of the clotrimazole in the composition is 1 percent to 3 percent by weight, and the pH value of the composition is 4 to 5.

Description

Technical field:

[0001] The invention provides a gynecological composition, especially a compound antifungal gynecological medicine containing clotrimazole. Background technique:

[0002] Clotrimazole (CAS: 23593-75-1) is a broad-spectrum azole antifungal drug, and its vaginal preparations, such as clotrimazole suppositories and creams, are widely used in the treatment of gynecological diseases such as fungal vaginitis. However, due to its wide application, fungal vaginitis pathogens such as Candida albicans have developed strong resistance to clotrimazole. Timosaponin B2 (CAS: 136656-07-0) is a saponin compound extracted from the Chinese medicinal material Anemarrhena. According to prior art reports, it has various pharmacological activities such as anti-tumor and anti-depression. In the previous study, we It is found that clotrimazole and timosaponin B2 formulated according to a certain ratio can improve the bacteriostatic effect on artificially induced clotrimazole-resis...

Examples

Embodiment 1

[0012] Pharmacological Example 1, Preparation of drug-resistant strains

[0013] Preparation

[0014] 1) Candida albicans (Candida albicans) (Code: ATCC10231) was used as the standard strain, and the standard strain of Candida albicans was continuously transplanted twice on Sabouraud agar (SDA) medium (cultivation temperature 35°C), and cultivated for 24 hours Finally, select 5 bacterial colonies with a diameter greater than 1 cm and shake them in 5 mL sterile normal saline for 15 seconds to make a bacterial suspension. 5×10 5 CFU / mL.

[0015] 2) Detect the minimum inhibitory concentration (MIC) of clotrimazole against Candida albicans, according to the CLSIM38-2 protocol, the quality control strain is Candida parapsilosis (ATCC 22019); the MIC result of the standard strain of Candida albicans is negative Compared with the control group, the minimum concentration that can significantly inhibit the growth of fungi (about 80%) is the minimum inhibitory concentration

[0016]...

preparation Embodiment

[0040] In the preparation examples, the preparation is made into a gel, and the content specification of clotrimazole in all gels is unified as 50mg / 5g

[0041] Example 1

[0042] Clotrimazole 1g, Timosaponin B2 0.25g

[0043] Carbomer 941 1g, glycerol 10g Tween 80 1g

[0044] Ethylparaben 0.1g Purified water added to 100g

[0045] Preparation method

[0046] 1) Carbomer is soaked overnight with an appropriate amount of purified water, fully stirred until it is completely swollen into a uniform gel-like polymer, then added ethylparaben and the main ingredient and mixed evenly to obtain a mixed solution 1)

[0047] 2) Mix glycerol and Tween 80 and add the mixed solution 1) Stir well, add an appropriate amount of purified water to 80g, adjust the pH to 4-4.5 with triethanolamine, make up the remaining water and stir well to obtain a transparent gel .

Embodiment 2

[0049] Clotrimazole 1g, Timosaponin B2 0.5g

[0050] Carbomer 941 1g, glycerol 10g Tween 80 1g

[0051] Ethylparaben 0.1g Purified water added to 100g

[0052] Preparation method

[0053] 1) Carbomer is soaked overnight with an appropriate amount of purified water, fully stirred until it is completely swollen into a uniform gel-like polymer, then added ethylparaben and the main ingredient and mixed evenly to obtain a mixed solution 1)

[0054] 2) Mix glycerol and Tween 80 and add the mixed solution 1) Stir well, add an appropriate amount of purified water to 80g, adjust the pH to 4-4.5 with triethanolamine, make up the remaining water and stir well to obtain a transparent gel .

Technical field:

[0001] The invention provides a gynecological composition, especially a compound antifungal gynecological medicine containing clotrimazole. Background technique:

[0002] Clotrimazole (CAS: 23593-75-1) is a broad-spectrum azole antifungal drug, and its vaginal preparations, such as clotrimazole suppositories and creams, are widely used in the treatment of gynecological diseases such as fungal vaginitis. However, due to its wide application, fungal vaginitis pathogens such as Candida albicans have developed strong resistance to clotrimazole. Timosaponin B2 (CAS: 136656-07-0) is a saponin compound extracted from the Chinese medicinal material Anemarrhena. According to prior art reports, it has various pharmacological activities such as anti-tumor and anti-depression. In the previous study, we It is found that clotrimazole and timosaponin B2 formulated according to a certain ratio can improve the bacteriostatic effect on artificially induced clotrimazole-resis...

Examples

Embodiment 1

[0012] Pharmacological Example 1, Preparation of drug-resistant strains

[0013] Preparation

[0014] 1) Candida albicans (Candida albicans) (Code: ATCC10231) was used as the standard strain, and the standard strain of Candida albicans was continuously transplanted twice on Sabouraud agar (SDA) medium (cultivation temperature 35°C), and cultivated for 24 hours Finally, select 5 bacterial colonies with a diameter greater than 1 cm and shake them in 5 mL sterile normal saline for 15 seconds to make a bacterial suspension. 5×10 5 CFU / mL.

[0015] 2) Detect the minimum inhibitory concentration (MIC) of clotrimazole against Candida albicans, according to the CLSIM38-2 protocol, the quality control strain is Candida parapsilosis (ATCC 22019); the MIC result of the standard strain of Candida albicans is negative Compared with the control group, the minimum concentration that can significantly inhibit the growth of fungi (about 80%) is the minimum inhibitory concentration

[0016]...

preparation Embodiment

[0040] In the preparation examples, the preparation is made into a gel, and the content specification of clotrimazole in all gels is unified as 50mg / 5g

[0041] Example 1

[0042] Clotrimazole 1g, Timosaponin B2 0.25g

[0043] Carbomer 941 1g, glycerol 10g Tween 80 1g

[0044] Ethylparaben 0.1g Purified water added to 100g

[0045] Preparation method

[0046] 1) Carbomer is soaked overnight with an appropriate amount of purified water, fully stirred until it is completely swollen into a uniform gel-like polymer, then added ethylparaben and the main ingredient and mixed evenly to obtain a mixed solution 1)

[0047] 2) Mix glycerol and Tween 80 and add the mixed solution 1) Stir well, add an appropriate amount of purified water to 80g, adjust the pH to 4-4.5 with triethanolamine, make up the remaining water and stir well to obtain a transparent gel .

Embodiment 2

[0049] Clotrimazole 1g, Timosaponin B2 0.5g

[0050] Carbomer 941 1g, glycerol 10g Tween 80 1g

[0051] Ethylparaben 0.1g Purified water added to 100g

[0052] Preparation method

[0053] 1) Carbomer is soaked overnight with an appropriate amount of purified water, fully stirred until it is completely swollen into a uniform gel-like polymer, then added ethylparaben and the main ingredient and mixed evenly to obtain a mixed solution 1)

[0054] 2) Mix glycerol and Tween 80 and add the mixed solution 1) Stir well, add an appropriate amount of purified water to 80g, adjust the pH to 4-4.5 with triethanolamine, make up the remaining water and stir well to obtain a transparent gel .

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