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WO2009010986A1 - Topical cream compositions of sertaconazole nitrate - Google Patents

Topical cream compositions of sertaconazole nitrate Download PDF

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Publication number
WO2009010986A1
WO2009010986A1 PCT/IN2007/000507 IN2007000507W WO2009010986A1 WO 2009010986 A1 WO2009010986 A1 WO 2009010986A1 IN 2007000507 W IN2007000507 W IN 2007000507W WO 2009010986 A1 WO2009010986 A1 WO 2009010986A1
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WO
WIPO (PCT)
Prior art keywords
sertaconazole
topical cream
cream composition
pharmaceutically acceptable
acceptable salts
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/IN2007/000507
Other languages
French (fr)
Inventor
Ulhas Rameshchandra Dhuppad
Vasant Sitaram Khachane
Nitin Babulal Bhamre
Girish Omkar
Santosh Dhulappa Patil
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Glenmark Pharmaceuticals Ltd
Original Assignee
Glenmark Pharmaceuticals Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Glenmark Pharmaceuticals Ltd filed Critical Glenmark Pharmaceuticals Ltd
Publication of WO2009010986A1 publication Critical patent/WO2009010986A1/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • A61K9/107Emulsions ; Emulsion preconcentrates; Micelles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41781,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0014Skin, i.e. galenical aspects of topical compositions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters

Definitions

  • the present invention relates generally to improved topical pharmaceutical formulations, their uses and methods of manufacturing. Specifically, the present invention relates to improved topical cream formulations of Sertaconazole or its pharmaceutically acceptable salts there of.
  • Sertaconazole nitrate contains one asymmetric carbon atom and exists as a racemic mixture of equal amounts of R and S enantiomers.
  • Sertaconazole nitrate is designated chemically as ( ⁇ )-l-[2,4-dichloro- ⁇ -[(7- chlorobenzo[ ⁇ ]thien- 3 -yl)methoxy]phenethyl] imidazole nitrate. It has a molecular weight of 500.8.
  • the molecular formula is C20H15C13N2OS ⁇ HN03 and the structural formula is as follows:
  • Sertaconazole nitrate is a white or almost white powder. It is practically insoluble in water, soluble in methanol, sparingly soluble in alcohol and methylene chloride.
  • Sertaconazole is an antifungal agent belongs to the imidazole class of antifungals. While the exact mechanism of action of this class of antifungals is not known, it is believed that they act primarily by inhibiting the cytochrome P450-dependent synthesis of ergosterol. Ergosterol is a key component of the cell membrane of fungi, and lack of this component leads to fungal cell injury primarily by leakage of key constituents in the cytoplasm from the cell.
  • Sertaconazole nitrate cream is used for the topical treatment of interdigital tinea pedis in immunocompetent patients 12 years of age and older, caused by Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum.
  • Sertaconazole nitrate cream 2% is marketed under the trade name ERTACZOTM, and contains sertaconazole nitrate in a white cream base of ethylene glycol and polyethylene glycol palmitostearate, glyceryl isostearate, light mineral oil, methylparaben, polyoxyethylened saturated glycerides and glycolized saturated glycerides, sorbic acid and purified water.
  • US Patent No. 5,135,943 ( ⁇ 943 patent) assigned to Ferrer is directed to Sertaconazole and salts there of and exemplifies dermal cream composition in example 1 ,
  • the cream formulation as prepared by following example 1 has been found to give sticky/waxy feeling after application and also is highly viscous in nature.
  • inventors of the present invention have been able to develop topical cream formulation with improved feel and consistency by using reduced amount of waxes and by addition of Glyceryl monostearate.
  • one of the objectives of the present invention is to provide topical cream composition of Sertaconazole or its pharmaceutically acceptable salts there of with improved feel and consistency.
  • Another objective of the present invention is to provide the process for preparing topical cream composition of Sertaconazole or its pharmaceutically acceptable salts there of.
  • Another objective of the present invention is to provide topical cream composition of
  • one of the objectives of the present invention is to provide the topical cream composition of Sertaconazole or its pharmaceutically acceptable salts there of with improved feel and consistency having reduced wax content in the range of 1-5%.
  • one of the objectives of the present invention is to provide the topical cream composition of Sertaconazole or its pharmaceutically acceptable salts there of with improved feel and consistency having emulsifier such as glyceryl monostearate.
  • composition of Sertaconazole or its pharmaceutically acceptable salts there of is indicated for the topical treatment of interdigital tinea pedis in immunocompetent patients caused by Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum.
  • the present invention relates generally to improved topical pharmaceutical formulations, their uses and methods of manufacturing. Specifically, the present invention relates to improved topical cream formulations of Sertaconazole or its pharmaceutically acceptable salts there of.
  • Creams are semisolid dosage forms containing one or more drug substances dissolved or dispersed in a suitable base, possessing relatively fluid consistency formulated as either water-in-oil or oil-in- water emulsions.
  • Consistency i.e., thickness or firmness
  • Consistency is the most important characteristic among the many physical properties of a semi-solid substances and it is a measure of thickness or firmness.
  • This invention is concerned with novel compositions for use as carriers for therapeutic compounds.
  • it is concerned with so-called "creams" used as vehicle for topical application of active therapeutic agents, , such as antibiotics.
  • a pharmaceutical composition further comprising of stiffening agents, emulsifiers, emollients, preservatives, buffers, vehicles and mixtures there of.
  • Stiffening agents used according to the present invention include fatty alcohols or esters such as stearyl alcohol, cetyl alcohol, myristyl alcohol, cetyl stearyl alcohol, glycerin monostearate and mixtures there of and are used in the range from 5-10%.
  • Emulsifiers according to the present invention include polyoxyethylene glycol monocetyl ethers, such as the material sold under the trade name cetomacrogol 1000, and polyoxyethlene sorbitan monostearates, such as the material sold under the trade name Polysorbate 60, or polyoxyethylene sorbitan monoleates, as sold under the trade name Tween 80,- sorbitol monostearate (Span 60), glyceryl monostearate and mixtures there of and are used in the range from 4-10%.
  • Emollients include 2-Octyldodecanol, "mineral oil” and mixtures there of and are used in the range from 5-10%.
  • the term “mineral oil” as used herein includes any that is suitable for use in a topical pharmaceutical composition and includes mineral oil USP, light mineral oil NF, liquid paraffin BP and light liquid paraffin BP.
  • composition of this invention may also include minor amounts of conventional additives such as viscosity modifiers, for example xanthan gum, and preservatives, such as phenoxyethanol or benzyl alcohol and mixtures thereof and are used in the range from 1-3%, aqueous phase consisting primarily of water constitutes about 72- 75 %. Also, it may be necessary to incorporate buffering agents to maintain a suitable pH.
  • viscosity modifiers for example xanthan gum
  • preservatives such as phenoxyethanol or benzyl alcohol and mixtures thereof and are used in the range from 1-3%
  • aqueous phase consisting primarily of water constitutes about 72- 75 %.
  • buffering agents may be necessary to incorporate buffering agents to maintain a suitable pH.
  • the percentages mentioned in the present composition are based on the total weight of the composition which typically also contains from 1 to 3% by weight of a therapeutic agent, such as Sertaconazole nitrate.
  • composition of Sertaconazole nitrate cream according to the present invention is indicated for the topical treatment of interdigital tinea pedis in immunocompetent patients caused by Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum.
  • Sertaconazole or its pharmaceutically acceptable salts there of refers to various salt forms preferably including Sertaconazole nitrate.
  • the cream base may be prepared by conventional techniques well known to those skilled in the art. Generally, a suitable process comprises admixing the various ingredients of the cream in appropriate relative amounts in any order that is convenient and thereafter, if necessary adjusting the pH to the final desired value. For example, the components of the base may be mixed together at an elevated temperature of 65-75 0 C until an emulsion has formed, and therapeutic agent may be added after cooling the emulsified cream base, or during mixing, if it is stable to the temperatures employed.
  • preparation of Sertaconazole nitrate cream composition involves the following steps: i) heating oil phase excipients and water separately, ii) heated oil phase excipients and water were mixed together and homogenized for about 5-30 minutes, and followed by iii) addition of preservatives and Sertaconazole nitrate and stirring is continued
  • Viscosity 0.70 to 0.90 poise (observed: 0.80 poise)
  • Table 1 compares Sertaconazole cream composition as disclosed in Example 1 of US5135943 with Sertaconazole cream composition of the present invention.
  • Sertaconazole cream composition as disclosed in prior art was prepared (as disclosed in Example 1 of US5135943) by inventors of the present invention to compare consistency of the cream with the cream of present invention.
  • Inventors of the present invention could find improved feel and consistency of the cream obtained as per the present invention in comparison to cream obtained by prior art.
  • Sertaconazole nitrate cream contains Sertaconazole nitrate in a white cream base of ethylene glycol and polyethylene glycol palmitostearate, glyceryl isostearate, light mineral oil, methylparaben, polyoxyethylened saturated glycerides and glycolized saturated glycerides, sorbic acid and purified water, having viscosity of 1.3 poise.
  • Emulsif ⁇ cation and Homogenization Oil phase and aqueous phase were added at 70°C to 72 0 C and homogenized for 10 minutes, and cooled 4.
  • Viscosity 0.60 to 0.80 poise (observed: 0.70 poise)

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Dispersion Chemistry (AREA)
  • Dermatology (AREA)
  • Medicinal Preparation (AREA)

Abstract

The present invention relates to topical formulations containing sertaconazole or its pharmaceutically acceptable salts as active ingredient. As adjuvants the formulations contain at least one stiffening agent, namely a fatty alcohol and/or its esters, at least one emulsifier and at least one emollient.

Description

TOPICAL CREAM COMPOSITIONS OF SERT ACONAZOLE NITRATE
PRIORITY This application claims the benefit of Indian complete Application 1393/MUM/2007, filed on My 19, 2007, and entitled "TOPICAL CREAM COMPOSITIONS OF SERTACONAZOLE NITRATE", the contents of which are incorporated by reference herein.
BACKGROUND OF THE INVENTION
1. Technical Field
The present invention relates generally to improved topical pharmaceutical formulations, their uses and methods of manufacturing. Specifically, the present invention relates to improved topical cream formulations of Sertaconazole or its pharmaceutically acceptable salts there of.
2. Description of the Related Art
Sertaconazole nitrate contains one asymmetric carbon atom and exists as a racemic mixture of equal amounts of R and S enantiomers.
Sertaconazole nitrate is designated chemically as (±)-l-[2,4-dichloro-β-[(7- chlorobenzo[ό]thien- 3 -yl)methoxy]phenethyl] imidazole nitrate. It has a molecular weight of 500.8. The molecular formula is C20H15C13N2OS HN03 and the structural formula is as follows:
Figure imgf000003_0001
Sertaconazole nitrate is a white or almost white powder. It is practically insoluble in water, soluble in methanol, sparingly soluble in alcohol and methylene chloride.
Sertaconazole is an antifungal agent belongs to the imidazole class of antifungals. While the exact mechanism of action of this class of antifungals is not known, it is believed that they act primarily by inhibiting the cytochrome P450-dependent synthesis of ergosterol. Ergosterol is a key component of the cell membrane of fungi, and lack of this component leads to fungal cell injury primarily by leakage of key constituents in the cytoplasm from the cell.
Sertaconazole nitrate cream is used for the topical treatment of interdigital tinea pedis in immunocompetent patients 12 years of age and older, caused by Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum.
Sertaconazole nitrate cream 2%, is marketed under the trade name ERTACZO™, and contains sertaconazole nitrate in a white cream base of ethylene glycol and polyethylene glycol palmitostearate, glyceryl isostearate, light mineral oil, methylparaben, polyoxyethylened saturated glycerides and glycolized saturated glycerides, sorbic acid and purified water.
US Patent No. 5,135,943 (ς943 patent) assigned to Ferrer is directed to Sertaconazole and salts there of and exemplifies dermal cream composition in example 1 , The cream formulation as prepared by following example 1 has been found to give sticky/waxy feeling after application and also is highly viscous in nature.
However, inventors of the present invention have been able to develop topical cream formulation with improved feel and consistency by using reduced amount of waxes and by addition of Glyceryl monostearate.
OBJECTIVES OF THE INVENTION
Accordingly, one of the objectives of the present invention is to provide topical cream composition of Sertaconazole or its pharmaceutically acceptable salts there of with improved feel and consistency.
Another objective of the present invention is to provide the process for preparing topical cream composition of Sertaconazole or its pharmaceutically acceptable salts there of.
Another objective of the present invention is to provide topical cream composition of
Sertaconazole or its pharmaceutically acceptable salts there of in which the strength of Sertaconazole nitrate is lOmg /gm - 30mg/ gm.
Accordingly, one of the objectives of the present invention is to provide the topical cream composition of Sertaconazole or its pharmaceutically acceptable salts there of with improved feel and consistency having reduced wax content in the range of 1-5%.
Accordingly, one of the objectives of the present invention is to provide the topical cream composition of Sertaconazole or its pharmaceutically acceptable salts there of with improved feel and consistency having emulsifier such as glyceryl monostearate.
In another objective of the present invention, the composition of Sertaconazole or its pharmaceutically acceptable salts there of is indicated for the topical treatment of interdigital tinea pedis in immunocompetent patients caused by Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum.
SUMMARY OF THE INVENTION
The present invention relates generally to improved topical pharmaceutical formulations, their uses and methods of manufacturing. Specifically, the present invention relates to improved topical cream formulations of Sertaconazole or its pharmaceutically acceptable salts there of.
DETAILED DESCRIPTION OF THE INVENTION
Creams are semisolid dosage forms containing one or more drug substances dissolved or dispersed in a suitable base, possessing relatively fluid consistency formulated as either water-in-oil or oil-in- water emulsions.
Consistency (i.e., thickness or firmness) is the most important characteristic among the many physical properties of a semi-solid substances and it is a measure of thickness or firmness.
This invention is concerned with novel compositions for use as carriers for therapeutic compounds. In particular it is concerned with so-called "creams" used as vehicle for topical application of active therapeutic agents, , such as antibiotics.
According to the present invention there is provided a pharmaceutical composition further comprising of stiffening agents, emulsifiers, emollients, preservatives, buffers, vehicles and mixtures there of.
Stiffening agents used according to the present invention include fatty alcohols or esters such as stearyl alcohol, cetyl alcohol, myristyl alcohol, cetyl stearyl alcohol, glycerin monostearate and mixtures there of and are used in the range from 5-10%.
Emulsifiers according to the present invention include polyoxyethylene glycol monocetyl ethers, such as the material sold under the trade name cetomacrogol 1000, and polyoxyethlene sorbitan monostearates, such as the material sold under the trade name Polysorbate 60, or polyoxyethylene sorbitan monoleates, as sold under the trade name Tween 80,- sorbitol monostearate (Span 60), glyceryl monostearate and mixtures there of and are used in the range from 4-10%. Emollients include 2-Octyldodecanol, "mineral oil" and mixtures there of and are used in the range from 5-10%. The term "mineral oil" as used herein includes any that is suitable for use in a topical pharmaceutical composition and includes mineral oil USP, light mineral oil NF, liquid paraffin BP and light liquid paraffin BP.
The composition of this invention may also include minor amounts of conventional additives such as viscosity modifiers, for example xanthan gum, and preservatives, such as phenoxyethanol or benzyl alcohol and mixtures thereof and are used in the range from 1-3%, aqueous phase consisting primarily of water constitutes about 72- 75 %. Also, it may be necessary to incorporate buffering agents to maintain a suitable pH.
The percentages mentioned in the present composition are based on the total weight of the composition which typically also contains from 1 to 3% by weight of a therapeutic agent, such as Sertaconazole nitrate.
It has been found that addition of glyceryl monostearate along with other emulsifϊers /surfactants is an essential component of the invention to make a cream having better feel on application and provide the required consistency.
Composition of Sertaconazole nitrate cream according to the present invention is indicated for the topical treatment of interdigital tinea pedis in immunocompetent patients caused by Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum.
According to the present invention, Sertaconazole or its pharmaceutically acceptable salts there of refers to various salt forms preferably including Sertaconazole nitrate.
Instrument for measuring consistency is Brookfield CAP Viscometer, Model: CAP 2000+. The cream base may be prepared by conventional techniques well known to those skilled in the art. Generally, a suitable process comprises admixing the various ingredients of the cream in appropriate relative amounts in any order that is convenient and thereafter, if necessary adjusting the pH to the final desired value. For example, the components of the base may be mixed together at an elevated temperature of 65-75 0C until an emulsion has formed, and therapeutic agent may be added after cooling the emulsified cream base, or during mixing, if it is stable to the temperatures employed.
More preferably, preparation of Sertaconazole nitrate cream composition involves the following steps: i) heating oil phase excipients and water separately, ii) heated oil phase excipients and water were mixed together and homogenized for about 5-30 minutes, and followed by iii) addition of preservatives and Sertaconazole nitrate and stirring is continued
& cooled up to room temperature.
Viscosity Details of Prior art as well as present formulation:
Instrument : Brookfield CAP Viscometer
Model : CAP 2000+
Prior Art
RPM : 900
Run time : 30 seconds
Temperature : 25°C
Spindle No. : 1
Viscosity : 0.70 to 0.90 poise (observed: 0.80 poise)
Present invention
RPM : 900
Run time : 30 seconds
Temperature : 25°C
Spindle No. : 1
Viscosity : 0.60 to 0.80 poise (observed: 0.70 poise) Tablel
Figure imgf000009_0001
Table 1 compares Sertaconazole cream composition as disclosed in Example 1 of US5135943 with Sertaconazole cream composition of the present invention. Sertaconazole cream composition as disclosed in prior art was prepared (as disclosed in Example 1 of US5135943) by inventors of the present invention to compare consistency of the cream with the cream of present invention. Inventors of the present invention could find improved feel and consistency of the cream obtained as per the present invention in comparison to cream obtained by prior art. Marketed Sertaconazole nitrate cream (ERTACZO™), contains Sertaconazole nitrate in a white cream base of ethylene glycol and polyethylene glycol palmitostearate, glyceryl isostearate, light mineral oil, methylparaben, polyoxyethylened saturated glycerides and glycolized saturated glycerides, sorbic acid and purified water, having viscosity of 1.3 poise.
The invention is further exemplified with following examples and is not intended to limit the scope of the inventions. It is obvious to those skilled in the art to find out the composition for other dosage forms and substitute the equivalent excipients as described in this specification or with the one known to the industry.
Example 1
Figure imgf000010_0001
Brief Manufacturing Process
1. Oil Phase
All oil Phase excipients were heated up to 70°C to 72°C
2. Aqueous Phase
Water is heated up to 7O0C to 72°C
3. Emulsifϊcation and Homogenization Oil phase and aqueous phase were added at 70°C to 720C and homogenized for 10 minutes, and cooled 4. Benzyl Alcohol Phase
Benzyl alcohol is added to the base obtained from step 3, at 650C to 680C 5. Sertaconazole Nitrate Phase
Dispersed drug in mixture of purified water and polysorbate 60 and then added to the base of steρ(3) at 400C or below 400C 6. Stirring is continued & cooled up to room temperature. Physical Parameters:
Description : white semisolid cream pH at 250C : 2 to 4 (observed: 3.18)
Viscosity : 0.60 to 0.80 poise (observed: 0.70 poise)

Claims

We claim: 1. Topical cream composition of Sertaconazole or its pharmaceutically acceptable salts there of with improved feel and consistency.
2. Process for preparing topical cream composition of Sertaconazole or its pharmaceutically acceptable salts there of comprising the following steps: i) heated oil phase excipients and water separately, ii) oil phase excipients and water were mixed together and homogenized for about
5-30 minutes, and iii) preservatives and Sertaconazole nitrate are added to the mixture of step (ii) and cooled up to room temperature. 3. Topical cream composition according to claim 1, in which the strength of
Sertaconazole nitrate is lOmg /gm - 30mg/ gm. 4. Topical cream composition according to claim 1, in which Sertaconazole or its pharmaceutically acceptable salts there of with improved feel and consistency having reduced wax content in the range of 1-5%. 5. Topical cream composition according to claim 1, in which Sertaconazole or its pharmaceutically acceptable salts there of with improved feel and consistency having glyceryl monostearate.
6. Topical cream composition of Sertaconazole according to any of the preceding claims further comprises stiffening agents, emulsifiers, emollients, preservatives, buffers, vehicles and mixtures there of.
7. Topical cream composition of Sertaconazole or its pharmaceutically acceptable salts there of with improved feel and consistency comprises stiffening agents selected from fatty alcohols or esters such as stearyl alcohol, cetyl alcohol, myristyl alcohol, cetyl stearyl alcohol and glycerin monostearate and mixtures there of; emulsifiers selected from polyoxyethylene glycol monocetyl ethers, and polyoxyethlene sorbitan monostearates, or polyoxyethylene sorbitan monoleates, sorbitol monostearate, glyceryl monostearate and mixtures there of; and emollients include 2- octyldodecanol, "mineral oil" and mixtures there of. Topical cream composition of Sertaconazole or its pharmaceutically acceptable salts there of is indicated for the topical treatment of interdigital tinea pedis in immunocompetent patients caused by Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum.
PCT/IN2007/000507 2007-07-19 2007-10-25 Topical cream compositions of sertaconazole nitrate Ceased WO2009010986A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN1393/MUM/2007 2007-07-19
IN1393MU2007 2007-07-19

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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102440947A (en) * 2011-11-15 2012-05-09 海南海神同洲制药有限公司 Sertaconazole nitrate cream and preparation method thereof
CN112691075A (en) * 2020-12-31 2021-04-23 海南海神同洲制药有限公司 Sertaconazole nitrate cream and preparation method thereof
CN113520993A (en) * 2021-07-30 2021-10-22 海南海神同洲制药有限公司 Preparation method of low-viscosity sertaconazole nitrate cream and product prepared by same

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003032948A2 (en) * 2001-10-16 2003-04-24 Mcneil-Ppc, Inc. Compositions and methods for delivering antibacterial, antifungal and antiviral ointments to the oral, nasal or vaginal cavity
WO2004054576A1 (en) * 2002-12-18 2004-07-01 Ferrer Internacional, S.A. Pharmaceutical compositions of sertaconazole for vaginal use
WO2005087195A2 (en) * 2004-03-18 2005-09-22 Panacea Biotec Ltd. Novel compositions for topical delivery
WO2006071912A2 (en) * 2004-12-27 2006-07-06 Johnson & Johnson Consumer Companies, Inc. A method for treating or preventing pruritic and neurogenic skin disorders by applying sertaconazole

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003032948A2 (en) * 2001-10-16 2003-04-24 Mcneil-Ppc, Inc. Compositions and methods for delivering antibacterial, antifungal and antiviral ointments to the oral, nasal or vaginal cavity
WO2004054576A1 (en) * 2002-12-18 2004-07-01 Ferrer Internacional, S.A. Pharmaceutical compositions of sertaconazole for vaginal use
WO2005087195A2 (en) * 2004-03-18 2005-09-22 Panacea Biotec Ltd. Novel compositions for topical delivery
WO2006071912A2 (en) * 2004-12-27 2006-07-06 Johnson & Johnson Consumer Companies, Inc. A method for treating or preventing pruritic and neurogenic skin disorders by applying sertaconazole

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102440947A (en) * 2011-11-15 2012-05-09 海南海神同洲制药有限公司 Sertaconazole nitrate cream and preparation method thereof
CN112691075A (en) * 2020-12-31 2021-04-23 海南海神同洲制药有限公司 Sertaconazole nitrate cream and preparation method thereof
CN112691075B (en) * 2020-12-31 2023-06-20 海南海神同洲制药有限公司 Sertaconazole nitrate emulsifiable paste and preparation method thereof
CN113520993A (en) * 2021-07-30 2021-10-22 海南海神同洲制药有限公司 Preparation method of low-viscosity sertaconazole nitrate cream and product prepared by same
CN113520993B (en) * 2021-07-30 2022-07-29 海南海神同洲制药有限公司 Preparation method of low-viscosity sertaconazole nitrate cream and product prepared by same

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