Fenticonazole nitrate vaginal suppository composition

Abstract

The invention discloses a fenticonazole nitrate vaginal suppository composition. By utilizing the high-efficiency antibacterial activity of the fenticonazole nitrate and adopting local vaginal administration, the antibacterial activity is greatly improved, and the toxic or side effect due to oral administration is remarkably reduced. The fenticonazole nitrate vaginal suppository composition is used for locally treating double infection caused by vulvovaginal candidiasis and gram positive bacteria. The invention also relates to a fenticonazole nitrate vaginal suppository composition and a preparation method thereof.

Description

technical field

[0001] The invention relates to a vaginal suppository composition of fenticonazole nitrate and a preparation method thereof. Background technique

[0002] Fenticonazole nitrate, its chemical name is: 1-[2-(2,4-dichlorophenyl)-2-[[4-(phenylthio)phenyl]methoxy]ethyl]-1H - imidazole nitrate.

[0003] Its structural formula is as follows:

[0004]

[0005] Molecular formula: C 24 h 20 C 12 N 2 oS·HNO 3

[0006] Molecular weight: 518.41

[0007] Fenticonazole nitrate is an imidazole derivative with antibacterial activity. Topical treatment of candidal vulvovaginal disease and double infection caused by Gram-positive bacteria such as: cervicitis, vaginitis, abnormal leucorrhea, etc. Fenticonazole nitrate was developed by the Italian Recordati pharmaceutical company and is listed in Italy, Argentina, Austria, Brazil, France, Germany, the United Kingdom, and Switzerland. The listed dosage forms include cream, solution, aerosol and vaginal soft capsule. ...

Examples

Embodiment 1

[0024] The prescription consists of:

[0025] (a) Fenticonazole Nitrate 200mg / capsule

[0026] (b) Semi-synthetic fatty acid glyceride (type 36) 2300mg / capsule

[0027] Taking the preparation of 1000 fenticonazole nitrate vaginal suppositories as an example, the specific preparation method is to grind and pulverize fenticonazole nitrate with a rotary mill or an air jet ultra-fine grinder. The particle size of the drug particles is not greater than 30 μm. Heat and melt the semi-synthetic fatty acid glyceride (type 36) in the preparation tank to 50°C ± 5°C, maintain the temperature of the melting matrix at 50°C ± 5°C, add the prescribed amount of fenticonazole nitrate into the above preparation tank , mix it well and homogenize to obtain a homogeneous dispersion. Maintaining mixing and maintaining the temperature at 45°C ± 5°C, the drug dispersion is formed into suppositories using an automatic form / fill / seal suppository machine.

Embodiment 2

[0029] The prescription consists of:

[0030] (a) Fenticonazole Nitrate 200mg / capsule

[0031] (b) Semi-synthetic fatty acid glyceride (type 38) 2300mg / capsule

[0032] Taking the preparation of 1000 fenticonazole nitrate vaginal suppositories as an example, the specific preparation method is to grind and pulverize fenticonazole nitrate with a rotary mill or an air jet ultra-fine grinder. The particle size of the drug particles is not greater than 30 μm. Heat and melt the semi-synthetic fatty acid glyceride (type 38) to 50°C±5°C in the preparation tank, and melt the base

[0033] The temperature of the substance was maintained at 50°C ± 5°C, and the prescribed amount of fenticonazole nitrate was added into the above preparation tank, mixed and homogenized to obtain a uniform dispersion. Maintaining mixing and maintaining the temperature at 45°C ± 5°C, the drug dispersion is formed into suppositories using an automatic form / fill / seal suppository machine.

Embodiment 3

[0035] The prescription consists of:

[0036] (a) Fenticonazole Nitrate 200mg / capsule

[0037] (b) Semi-synthetic fatty acid glyceride (type 36) 1800mg / capsule

[0038] Taking the preparation of 1000 fenticonazole nitrate vaginal suppositories as an example, the specific preparation method is to grind and pulverize fenticonazole nitrate with a rotary mill or an air jet ultra-fine grinder. The particle size of the drug particles is not greater than 30 μm. Heat and melt the semi-synthetic fatty acid glyceride (type 36) in the preparation tank to 50°C ± 5°C, maintain the temperature of the melting matrix at 50°C ± 5°C, add the prescribed amount of fenticonazole nitrate into the above preparation tank , mix it well and homogenize to obtain a homogeneous dispersion. Maintaining mixing and maintaining the temperature at 45°C ± 5°C, the drug dispersion is formed into suppositories using an automatic form / fill / seal suppository machine.

technical field

[0001] The invention relates to a vaginal suppository composition of fenticonazole nitrate and a preparation method thereof. Background technique

[0002] Fenticonazole nitrate, its chemical name is: 1-[2-(2,4-dichlorophenyl)-2-[[4-(phenylthio)phenyl]methoxy]ethyl]-1H - imidazole nitrate.

[0003] Its structural formula is as follows:

[0004]

[0005] Molecular formula: C 24 h 20 C 12 N 2 oS·HNO 3

[0006] Molecular weight: 518.41

[0007] Fenticonazole nitrate is an imidazole derivative with antibacterial activity. Topical treatment of candidal vulvovaginal disease and double infection caused by Gram-positive bacteria such as: cervicitis, vaginitis, abnormal leucorrhea, etc. Fenticonazole nitrate was developed by the Italian Recordati pharmaceutical company and is listed in Italy, Argentina, Austria, Brazil, France, Germany, the United Kingdom, and Switzerland. The listed dosage forms include cream, solution, aerosol and vaginal soft capsule. ...

Examples

Embodiment 1

[0024] The prescription consists of:

[0025] (a) Fenticonazole Nitrate 200mg / capsule

[0026] (b) Semi-synthetic fatty acid glyceride (type 36) 2300mg / capsule

[0027] Taking the preparation of 1000 fenticonazole nitrate vaginal suppositories as an example, the specific preparation method is to grind and pulverize fenticonazole nitrate with a rotary mill or an air jet ultra-fine grinder. The particle size of the drug particles is not greater than 30 μm. Heat and melt the semi-synthetic fatty acid glyceride (type 36) in the preparation tank to 50°C ± 5°C, maintain the temperature of the melting matrix at 50°C ± 5°C, add the prescribed amount of fenticonazole nitrate into the above preparation tank , mix it well and homogenize to obtain a homogeneous dispersion. Maintaining mixing and maintaining the temperature at 45°C ± 5°C, the drug dispersion is formed into suppositories using an automatic form / fill / seal suppository machine.

Embodiment 2

[0029] The prescription consists of:

[0030] (a) Fenticonazole Nitrate 200mg / capsule

[0031] (b) Semi-synthetic fatty acid glyceride (type 38) 2300mg / capsule

[0032] Taking the preparation of 1000 fenticonazole nitrate vaginal suppositories as an example, the specific preparation method is to grind and pulverize fenticonazole nitrate with a rotary mill or an air jet ultra-fine grinder. The particle size of the drug particles is not greater than 30 μm. Heat and melt the semi-synthetic fatty acid glyceride (type 38) to 50°C±5°C in the preparation tank, and melt the base

[0033] The temperature of the substance was maintained at 50°C ± 5°C, and the prescribed amount of fenticonazole nitrate was added into the above preparation tank, mixed and homogenized to obtain a uniform dispersion. Maintaining mixing and maintaining the temperature at 45°C ± 5°C, the drug dispersion is formed into suppositories using an automatic form / fill / seal suppository machine.

Embodiment 3

[0035] The prescription consists of:

[0036] (a) Fenticonazole Nitrate 200mg / capsule

[0037] (b) Semi-synthetic fatty acid glyceride (type 36) 1800mg / capsule

[0038] Taking the preparation of 1000 fenticonazole nitrate vaginal suppositories as an example, the specific preparation method is to grind and pulverize fenticonazole nitrate with a rotary mill or an air jet ultra-fine grinder. The particle size of the drug particles is not greater than 30 μm. Heat and melt the semi-synthetic fatty acid glyceride (type 36) in the preparation tank to 50°C ± 5°C, maintain the temperature of the melting matrix at 50°C ± 5°C, add the prescribed amount of fenticonazole nitrate into the above preparation tank , mix it well and homogenize to obtain a homogeneous dispersion. Maintaining mixing and maintaining the temperature at 45°C ± 5°C, the drug dispersion is formed into suppositories using an automatic form / fill / seal suppository machine.

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