Title of Invention	STABLE DERMATOLOGICAL COMPOSITION CONTAINING ALLANTOIN,UREA AND DIMETHICONE AND PROCESS FOR PREPARATION THEREOF
Abstract	A stable synergistic dermatological composition comprising pharmaceutical^ active ingredients allantoin, urea, dimethicone and a buffer system along with pharmaceutically acceptable excipients. 2. The stable synergistic dermatological composition as claimed in claim 1, wherein said composition is in the cream dosage form. 3. The stable synergistic dermatological composition as claimed in claim 1, wherein said buffer system comprises glacial acetic acid- sodium acetate buffer. 4. The stable synergistic dermatological composition as claimed in claims 1 and 3, wherein said buffer system is used in concentration of 1.5% to 3 % by weight of cream, preferably 2.35 % by weight of cream. 5. The stable synergistic dermatological composition as claimed in claims 1 to 4, wherein pH of said composition is in the range of 5.0 to 7.5. 6. The stable synergistic dermatological composition as claimed in claim 1, wherein said pharmaceutically acceptable excipient is water washable cream base selected from group comprising Cetomagrogol 1000, Cetostearyl Alcohol, Hard Paraffin and Liquid Paraffin Light. 7. The stable synergistic dermatological composition as claimed in claim 1, wherein said pharmaceutically acceptable excipients are selected from group comprising humectants, emollients, emulsion stabilizers, preservatives, fragrance and other suitable additives. 8. The stable synergistic dermatological composition as claimed in claim 7, wherein said humectants are selected from group comprising Glycerin, Propylene glycol, etc. 9. The stable synergistic dermatological composition as claimed in claims 7 and 8, wherein said humectants are in the range of 5% to 20% by weight of the cream, more preferably 5-10% by weight. 10. The stable synergistic dermatological composition as claimed in claim 7, wherein said preservatives are selected from Methyl Paraben, Propyl Paraben, sodium benzoate and Potassium sorbate.

Title of Invention

STABLE DERMATOLOGICAL COMPOSITION CONTAINING ALLANTOIN,UREA AND DIMETHICONE AND PROCESS FOR PREPARATION THEREOF

Abstract

A stable synergistic dermatological composition comprising pharmaceutical^ active ingredients allantoin, urea, dimethicone and a buffer system along with pharmaceutically acceptable excipients. 2. The stable synergistic dermatological composition as claimed in claim 1, wherein said composition is in the cream dosage form. 3. The stable synergistic dermatological composition as claimed in claim 1, wherein said buffer system comprises glacial acetic acid- sodium acetate buffer. 4. The stable synergistic dermatological composition as claimed in claims 1 and 3, wherein said buffer system is used in concentration of 1.5% to 3 % by weight of cream, preferably 2.35 % by weight of cream. 5. The stable synergistic dermatological composition as claimed in claims 1 to 4, wherein pH of said composition is in the range of 5.0 to 7.5. 6. The stable synergistic dermatological composition as claimed in claim 1, wherein said pharmaceutically acceptable excipient is water washable cream base selected from group comprising Cetomagrogol 1000, Cetostearyl Alcohol, Hard Paraffin and Liquid Paraffin Light. 7. The stable synergistic dermatological composition as claimed in claim 1, wherein said pharmaceutically acceptable excipients are selected from group comprising humectants, emollients, emulsion stabilizers, preservatives, fragrance and other suitable additives. 8. The stable synergistic dermatological composition as claimed in claim 7, wherein said humectants are selected from group comprising Glycerin, Propylene glycol, etc. 9. The stable synergistic dermatological composition as claimed in claims 7 and 8, wherein said humectants are in the range of 5% to 20% by weight of the cream, more preferably 5-10% by weight. 10. The stable synergistic dermatological composition as claimed in claim 7, wherein said preservatives are selected from Methyl Paraben, Propyl Paraben, sodium benzoate and Potassium sorbate.

Full Text	FORM 2 THE PATENT ACT 1970 (39 of 1970) & The Patents Rules, 2003 COMPLETE SPECIFICATION (See section 10 and rule 13) 1. TITLE OF THE INVENTION: "Stable dermatological composition containing allantoin, urea and dimethicone and process for preparation thereof." 2. APPLICANT: (a) NAME: INDOCO REMEDIES LIMITED, (b) NATIONALITY: Indian Company incorporated under the Indian Companies ACT, 1956 (c) ADDRESS: Indoco House, 166, C. S. T. Road, Santacruz (East), Mumbai - 400 098. Maharashtra, India 3. PREAMBLE TO THE DESCRIPTION The following specification particularly describes the invention and the manner in which it is to be performed. Field of invention: The present invention relates to a stable synergistic dermatological composition comprising the active ingredients Allantoin, Urea and Dimethicone, along with other pharmaceutically acceptable excipients for the treatment of diabetic foot and dry skin. Further the present invention relates to a process for the preparation of the stable synergistic dermatological composition. Background of invention: Dry skin is often caused due to a decrease in the moisture content of the skin, especially following anhydrosis. The affected skin usually becomes hyperkeratotic. Allantoin is a commonly used ingredient in cosmetic preparation, particularly in skin dreams where it exerts a skin protective action. It is a valuable cell proliferating dealing agent which stimulates healthy tissue formation. Allantoin acts as a Keratolytic and an astringent agent. Due to its keratolytic action it removes the dead keratin that causes scaliness of the skin. It thus makes the skin smooth. By precipitating the proteins on the superficial surface of the skin, it protects and strengthens the skin. Urea is known for its keratolytic properties, ability to soften dry skin and help diminish crusted tissue. Urea is thus added to cosmetic and drug compositions with the object of preventing skin chapping and retaining moisture. But it decomposes into ammonia and carbon dioxide during the storage, thus increasing the pH of the composition and generating an unacceptable ammonia odor. Dimethicone (also known as Simethicone) is a water-repellant. By covering the skin it prevents further loss of moisture from the skin. It also acts as a topical barrier that protects the skin. US patent 6,281,236 describes a skin cream composition containing Allantoin and an emulsifier. The composition has improved stability resulting from adjustment of pH to a range of 4.5 to 5.8. US patent 6,329,413 describes an Allantoin containing skin cream comprising at least one anionic or nonionic emulsifier that is substantially hydrophilic and is soluble in water. The pH of this composition is in the range of 5 to 6.5. US patent 6,461,624 describes a skin protective composition comprising Dimethicone as a suitable skin protectant. DE19647100 describes a urea salve comprising urea, propylene glycol, medium length chain triglycerides, glycerin monostearate, Vaseline, cetyl alcohol, panthenol, vitamin E acetate, dimethicone and distilled water. Various prior arts are available which aim to solve the problem related to urea decomposition as follows: US patent 6,355,259 describes a skin cream comprising Urea and buffer system comprising disodium hydrogenphosphate and citric acid or a buffer comprising Potassium dihydrogenphosphate, or both, the composition further comprising Allantoin. Japanese patent application Laid-open No 109487/1977 discloses the addition of Allantoin in an amount of 1% wt or more for the amount of Urea to suppress the odor of ammonia. Japanese application Laid open No 48441/1976 discloses a method of adding a buffer to urea to adjust the pH to 6-9 and further adding ammonium salt, allantoin, allantoin derivative or Uric acid. Japanese application Laid open No30509/1986 describes a method of stabilization of adding a basic amino acid to urea. Japanese application Laid open No 81567/1992 describes a method of stabilization of urea by adding taurine. Japanese patent publication No 56002/1992 describes a method of stabilization of urea by adding neutral amino acid, acidic amino acid or alkaline salt of an acidic amino acid. Japanese patent publication No 31541/1993 describes a method of adding Lecitin to stabilize Urea. The Literature mentions various compositions containing Urea and Allantoin, however there is no report on chemical stability of AUantoin in presence of urea. In alkaline pH of 7.0 - 8.0, it is observed that AUantoin degrades drastically in presence of Urea in a cream base. Nevertheless, there is a need for a stable composition comprising AUantoin, Urea and Dimethicone for the treatment of diabetic foot and dry skin. The above mentioned active ingredients with synergistic effect offer a comprehensive solution required for tackling the problem of diabetic foot and dry skin. Thus the active ingredients in combination synergistically act and help in the management of diabetic foot and dry skin. Objectives: The main object of the present invention is to provide a stable synergistic dermatological composition comprising active ingredients AUantoin, Urea and Dimethicone, along with pharmaceutically acceptable excipients for the treatment of diabetic foot and dry Scaly Skin of various etiologies. Another object of the present invention is to provide stable synergistic dermatological composition by using Glacial acetic acid- Sodium acetate buffer system. Yet another objective of the present invention is to provide a stable humectant, emollient, healing and protective composition for treatment of diabetic foot and dry skin in a cream dosage form. Yet another objective of the present invention is to provide a process for preparing the stable synergistic dermatological composition. Summary of the invention: The present invention relates to a stable synergistic dermatological composition comprising pharmaceutically active ingredients allantoin, urea, dimethicone and a buffer system, along with pharmaceutically acceptable excipients. The composition is in the cream dosage form. The buffer system comprises glacial acetic acid- sodium acetate buffer and is used in concentration of 1.5% to 3 % by weight of cream, preferably 2.35 % by weight of cream. The pH of the stable synergistic dermatological composition is in the range of 5.0 to 7.5. The pharmaceutically acceptable excipient is water washable cream base selected from group comprising Cetomagrogo11000, Cetostearyl Alcohol, Hard Paraffin, Liquid Paraffin Light and the like. The pharmaceutically acceptable excipients are selected from group comprising humectants, emollients, emulsion stabilizers, preservatives, fragrance and other suitable additives. The humectants are selected from group comprising Glycerin, Propylene glycol, etc. The humectants are in the range of 5% to 20% by weight of the cream, more preferably 5-10% by weight. The preservatives are selected from Methyl Paraben, Propyl Paraben, Sodium benzoate, Potassium sorbate, and the like. The preservatives are in the range of 0.1% to 0.2% by weight of the cream, more preferably 0.15% by weight of the cream. The composition may be in forms such as a liquid dosage form, a milky white lotion, a gel and the like. A process for the preparation of the stable compositions comprises adding Allontoin and Urea to the aqueous phase containing emollients, humectants and buffer system in purified water; preparing fatty phase consisting of group comprising Cetomagrogol 1000, Cetostearyl Alcohol, Hard Paraffin, Liquid Paraffin Light and preservatives; emulsifying the aqueous phase and fatty phase; adding Dimethicone to the emulsified system and adding other ingredients like fragrance. Detailed description: The present invention discloses a stable synergistic dermatological composition comprising allantoin, urea and dimethicone, along with pharmaceutically acceptable excipients in a water washable cream base for treatment of diabetic foot and dry skin. The stable synergistic dermatological composition is stabilized with sodium acetate-glacial acetic acid buffer system to maintain the pH of the composition in the range of 5.0-7.5, in order to maintain the stability of Allantoin and Urea, which have pH dependant stability. The buffer system is used in the range of 1.5-3.0%, preferably 2.35 % by weight of the cream. In the present invention, Allantoin is used as a healing agent, Urea is used as a moisturizer and Dimethicone is used as a skin protectant. The stable synergistic dermatological composition comprises pharmaceutically acceptable excipients selected from humectants, emollients, emulsion stabilizers, preservatives, fragrance and other suitable additives known to a person skilled in the art. The water washable cream base is selected from group comprising Cetomagrogol 1000, Cetostearyl Alcohol, Hard Paraffin, Liquid Paraffin Light and other suitable materials known to a person skilled in the art. They are used in the range of 1 -10% by weight individually and 10 - 40% by weight in total. Humectants are selected from group comprising Glycerin, Propylene glycol and other humectants known to a person skilled in the art. They are used in the range of 5% to 20% by weight of the cream, more preferably 5-10% by weight. The preservatives used are selected from the group comprising Methyl Paraben, Propyl Paraben, Sodium benzoate, Potassium sorbate or any other suitable preservatives known to a person skilled in the art. They are used in the range of 0.1% to 0.2% by weight of the cream, preferably 0.15% by weight of the cream. The fragrance is used in concentration 0.05% to 0.5%. The stable synergistic dermatological composition can be made into various other forms, such as a liquid preparation, a milky white lotion, a gel preparation and the like. Various additives can be added according to the dosage form. A process for the preparation of the stable synergistic dermatological composition comprises adding Allontoin and urea to the aqueous phase containing emollients, humectants and buffer system in purified water, preparing fatty phase consisting of group comprising Cetomagrogol 1000, Cetostearyl Alcohol, Hard Paraffin, Liquid Paraffin Light to preservatives; emulsifying the aqueous phase and fatty phase; adding Dimethicone to the emulsified system and adding ingredients like fragrance. In the present invention, physical as well as chemical stability of Allantoin, Urea and Dimethicone of the stable synergistic dermatological composition has been studied. Other features of the invention will become apparent in the course of the following description of the exemplary embodiments which are given for illustration of the invention and are not intended to be limiting thereof. Example: Ingredients Qty in %w/w Allantoin 0.200 Activated Dimethicone 1.000 Urea 10.000 Propylene glycol 5.000 Glycerin 5.000 Liquid Paraffin, Light 8.000 Cetomagrogol 1000 3.000 Cetostearyl Alcohol 9.000 Hard Paraffin 3.000 Polyethylene Glycol 400 8.000 Methyl Paraben 0.100 Propyl Paraben 0.050 Acetic acid, Glacial 0.701 Sodium Acetate Anhydrous 1.680 Fragrance 0.050 Purified Water Qs 1) Cetomacrogol 1000, Cetostearyl alcohol, Hard paraffin, Liquid Paraffin Light were melted at 65°C - 75°C. 2) Methyl Paraben and Propyl Paraben were dissolved in it. 3) Allantoin was added under stirring to part of purified water heated to 50°C - 55°C. 4) Acetic Acid Glacial and Sodium Acetate anhydrous were dissolved under stirring to part of water. 5) Urea was dissolved in part of purified water. 6) Urea solution from step 5 was added to Allantoin solution from step 3. 7) Propylene Glycol, Glycerine and Polyethylene Glycol 400 were added to the aqueous phase from step 6. The aqueous phase was heated and maintained at 50°C - 55°C. 8) Oil phase from step 1 was added to aqueous phase from step 7 slowly under stirring to form primary emulsion 9) Activated Dimethicone was added to primary emulsion under stirring and cooled to 40 °C. 10) Fragrance was added to the above mass with continuous stirring and the mass was cooled to room temperature. Results Initial 6M 40°C/75% RH pH 5.66 7.36 Odor of Ammonia Nil Nil Assay Allantoin 105.23 101.35% Urea 98.17 100.94% Dimethicone 101.83 97.00% Claim: 1. A stable synergistic dermatological composition comprising pharmaceutical^ active ingredients allantoin, urea, dimethicone and a buffer system along with pharmaceutically acceptable excipients. 2. The stable synergistic dermatological composition as claimed in claim 1, wherein said composition is in the cream dosage form. 3. The stable synergistic dermatological composition as claimed in claim 1, wherein said buffer system comprises glacial acetic acid- sodium acetate buffer. 4. The stable synergistic dermatological composition as claimed in claims 1 and 3, wherein said buffer system is used in concentration of 1.5% to 3 % by weight of cream, preferably 2.35 % by weight of cream. 5. The stable synergistic dermatological composition as claimed in claims 1 to 4, wherein pH of said composition is in the range of 5.0 to 7.5. 6. The stable synergistic dermatological composition as claimed in claim 1, wherein said pharmaceutically acceptable excipient is water washable cream base selected from group comprising Cetomagrogol 1000, Cetostearyl Alcohol, Hard Paraffin and Liquid Paraffin Light. 7. The stable synergistic dermatological composition as claimed in claim 1, wherein said pharmaceutically acceptable excipients are selected from group comprising humectants, emollients, emulsion stabilizers, preservatives, fragrance and other suitable additives. 8. The stable synergistic dermatological composition as claimed in claim 7, wherein said humectants are selected from group comprising Glycerin, Propylene glycol, etc. 9. The stable synergistic dermatological composition as claimed in claims 7 and 8, wherein said humectants are in the range of 5% to 20% by weight of the cream, more preferably 5-10% by weight. 10. The stable synergistic dermatological composition as claimed in claim 7, wherein said preservatives are selected from Methyl Paraben, Propyl Paraben, sodium benzoate and Potassium sorbate. 11. The stable synergistic dermatological composition as claimed in claims 7 and 8, wherein said preservatives are in the range of 0.1% to 0.2% by weight of the cream, more preferably 0.15% by weight of the cream. 12. The stable synergistic dermatological composition as claimed in claim 1, wherein said composition may be in forms such as a liquid dosage form, a milky white lotion, a gel and the like. 13. A process for the preparation of the stable synergistic dermatological composition comprising the steps of a. adding Allantoin to purified water and heated to 50°C - 55°C; b. dissolving the buffers in purified water and adding the buffer solution to step (a); c. dissolving urea in purified water; d. adding urea solution from step (c) to allantoin solution of step (a); e. adding humectants to the aqueous phase of step (d) followed by heating and maintaining the aqueous phase at 50°C - 55°C; f. preparing a fatty phase by melting Cetomagrogol 1000, Cetostearyl Alcohol, hard paraffin and Liquid paraffin light at 65°C - 75°C followed by dissolving the preservatives in the said fatty phase; g. adding activated dimethicone to said emulsified system of step (f) and cooling at 40°c; and h. adding ingredients like fragrance to the mass of step (g) to obtain stable composition. 14. A stable synergistic dermatological composition and process thereof as substantially described herein with reference to foregoing example. Dated this 10th day of September 2007 Dr. Gopakumar G. Nair Agent for the Applicant

Full Text

FORM 2
THE PATENT ACT 1970
(39 of 1970)
&
The Patents Rules, 2003
COMPLETE SPECIFICATION
(See section 10 and rule 13)

1. TITLE OF THE INVENTION:
"Stable dermatological composition containing allantoin, urea and dimethicone and process for preparation thereof."
2. APPLICANT:
(a) NAME: INDOCO REMEDIES LIMITED,
(b) NATIONALITY: Indian Company incorporated under the Indian Companies
ACT, 1956
(c) ADDRESS: Indoco House, 166, C. S. T. Road, Santacruz (East), Mumbai -
400 098. Maharashtra, India
3. PREAMBLE TO THE DESCRIPTION
The following specification particularly describes the invention and the manner in which it is to be performed.

Field of invention:
The present invention relates to a stable synergistic dermatological composition comprising the active ingredients Allantoin, Urea and Dimethicone, along with other pharmaceutically acceptable excipients for the treatment of diabetic foot and dry skin. Further the present invention relates to a process for the preparation of the stable synergistic dermatological composition.
Background of invention:
Dry skin is often caused due to a decrease in the moisture content of the skin, especially following anhydrosis. The affected skin usually becomes hyperkeratotic.
Allantoin is a commonly used ingredient in cosmetic preparation, particularly in skin dreams where it exerts a skin protective action. It is a valuable cell proliferating dealing agent which stimulates healthy tissue formation. Allantoin acts as a Keratolytic and an astringent agent. Due to its keratolytic action it removes the dead keratin that causes scaliness of the skin. It thus makes the skin smooth. By precipitating the proteins on the superficial surface of the skin, it protects and strengthens the skin.
Urea is known for its keratolytic properties, ability to soften dry skin and help diminish crusted tissue. Urea is thus added to cosmetic and drug compositions with the object of preventing skin chapping and retaining moisture. But it decomposes into ammonia and carbon dioxide during the storage, thus increasing the pH of the composition and generating an unacceptable ammonia odor.
Dimethicone (also known as Simethicone) is a water-repellant. By covering the skin it prevents further loss of moisture from the skin. It also acts as a topical barrier that protects the skin.
US patent 6,281,236 describes a skin cream composition containing Allantoin and an emulsifier. The composition has improved stability resulting from adjustment of pH to a range of 4.5 to 5.8.

US patent 6,329,413 describes an Allantoin containing skin cream comprising at least one anionic or nonionic emulsifier that is substantially hydrophilic and is soluble in water. The pH of this composition is in the range of 5 to 6.5.
US patent 6,461,624 describes a skin protective composition comprising Dimethicone as a suitable skin protectant.
DE19647100 describes a urea salve comprising urea, propylene glycol, medium length chain triglycerides, glycerin monostearate, Vaseline, cetyl alcohol, panthenol, vitamin E acetate, dimethicone and distilled water.
Various prior arts are available which aim to solve the problem related to urea decomposition as follows:
US patent 6,355,259 describes a skin cream comprising Urea and buffer system comprising disodium hydrogenphosphate and citric acid or a buffer comprising Potassium dihydrogenphosphate, or both, the composition further comprising Allantoin.
Japanese patent application Laid-open No 109487/1977 discloses the addition of Allantoin in an amount of 1% wt or more for the amount of Urea to suppress the odor of ammonia.
Japanese application Laid open No 48441/1976 discloses a method of adding a buffer to urea to adjust the pH to 6-9 and further adding ammonium salt, allantoin, allantoin derivative or Uric acid.
Japanese application Laid open No30509/1986 describes a method of stabilization of adding a basic amino acid to urea.
Japanese application Laid open No 81567/1992 describes a method of stabilization of urea by adding taurine.

Japanese patent publication No 56002/1992 describes a method of stabilization of urea by adding neutral amino acid, acidic amino acid or alkaline salt of an acidic amino acid.
Japanese patent publication No 31541/1993 describes a method of adding Lecitin to stabilize Urea.
The Literature mentions various compositions containing Urea and Allantoin, however there is no report on chemical stability of AUantoin in presence of urea. In alkaline pH of 7.0 - 8.0, it is observed that AUantoin degrades drastically in presence of Urea in a cream base.
Nevertheless, there is a need for a stable composition comprising AUantoin, Urea and Dimethicone for the treatment of diabetic foot and dry skin.
The above mentioned active ingredients with synergistic effect offer a comprehensive solution required for tackling the problem of diabetic foot and dry skin.
Thus the active ingredients in combination synergistically act and help in the management of diabetic foot and dry skin.
Objectives:
The main object of the present invention is to provide a stable synergistic dermatological composition comprising active ingredients AUantoin, Urea and Dimethicone, along with pharmaceutically acceptable excipients for the treatment of diabetic foot and dry Scaly Skin of various etiologies.
Another object of the present invention is to provide stable synergistic dermatological composition by using Glacial acetic acid- Sodium acetate buffer system.
Yet another objective of the present invention is to provide a stable humectant, emollient, healing and protective composition for treatment of diabetic foot and dry skin in a cream dosage form.

Yet another objective of the present invention is to provide a process for preparing the stable synergistic dermatological composition.
Summary of the invention:
The present invention relates to a stable synergistic dermatological composition comprising pharmaceutically active ingredients allantoin, urea, dimethicone and a buffer system, along with pharmaceutically acceptable excipients.
The composition is in the cream dosage form.
The buffer system comprises glacial acetic acid- sodium acetate buffer and is used in concentration of 1.5% to 3 % by weight of cream, preferably 2.35 % by weight of cream.
The pH of the stable synergistic dermatological composition is in the range of 5.0 to
7.5. The pharmaceutically acceptable excipient is water washable cream base selected
from group comprising Cetomagrogo11000, Cetostearyl Alcohol, Hard Paraffin,
Liquid Paraffin Light and the like.
The pharmaceutically acceptable excipients are selected from group comprising humectants, emollients, emulsion stabilizers, preservatives, fragrance and other suitable additives.
The humectants are selected from group comprising Glycerin, Propylene glycol, etc.
The humectants are in the range of 5% to 20% by weight of the cream, more
preferably 5-10% by weight.
The preservatives are selected from Methyl Paraben, Propyl Paraben, Sodium benzoate, Potassium sorbate, and the like. The preservatives are in the range of 0.1% to 0.2% by weight of the cream, more preferably 0.15% by weight of the cream.

The composition may be in forms such as a liquid dosage form, a milky white lotion, a gel and the like. A process for the preparation of the stable compositions comprises adding Allontoin and Urea to the aqueous phase containing emollients, humectants and buffer system in purified water; preparing fatty phase consisting of group comprising Cetomagrogol 1000, Cetostearyl Alcohol, Hard Paraffin, Liquid Paraffin Light and preservatives; emulsifying the aqueous phase and fatty phase; adding Dimethicone to the emulsified system and adding other ingredients like fragrance.
Detailed description:
The present invention discloses a stable synergistic dermatological composition comprising allantoin, urea and dimethicone, along with pharmaceutically acceptable excipients in a water washable cream base for treatment of diabetic foot and dry skin.
The stable synergistic dermatological composition is stabilized with sodium acetate-glacial acetic acid buffer system to maintain the pH of the composition in the range of 5.0-7.5, in order to maintain the stability of Allantoin and Urea, which have pH dependant stability.
The buffer system is used in the range of 1.5-3.0%, preferably 2.35 % by weight of the cream.
In the present invention, Allantoin is used as a healing agent, Urea is used as a moisturizer and Dimethicone is used as a skin protectant.
The stable synergistic dermatological composition comprises pharmaceutically acceptable excipients selected from humectants, emollients, emulsion stabilizers, preservatives, fragrance and other suitable additives known to a person skilled in the art.
The water washable cream base is selected from group comprising Cetomagrogol 1000, Cetostearyl Alcohol, Hard Paraffin, Liquid Paraffin Light and other suitable materials known to a person skilled in the art. They are used in the range of 1 -10% by weight individually and 10 - 40% by weight in total.

Humectants are selected from group comprising Glycerin, Propylene glycol and other humectants known to a person skilled in the art. They are used in the range of 5% to 20% by weight of the cream, more preferably 5-10% by weight.
The preservatives used are selected from the group comprising Methyl Paraben, Propyl Paraben, Sodium benzoate, Potassium sorbate or any other suitable preservatives known to a person skilled in the art. They are used in the range of 0.1% to 0.2% by weight of the cream, preferably 0.15% by weight of the cream.
The fragrance is used in concentration 0.05% to 0.5%.
The stable synergistic dermatological composition can be made into various other forms, such as a liquid preparation, a milky white lotion, a gel preparation and the like. Various additives can be added according to the dosage form.
A process for the preparation of the stable synergistic dermatological composition comprises adding Allontoin and urea to the aqueous phase containing emollients, humectants and buffer system in purified water, preparing fatty phase consisting of group comprising Cetomagrogol 1000, Cetostearyl Alcohol, Hard Paraffin, Liquid Paraffin Light to preservatives; emulsifying the aqueous phase and fatty phase; adding Dimethicone to the emulsified system and adding ingredients like fragrance.
In the present invention, physical as well as chemical stability of Allantoin, Urea and Dimethicone of the stable synergistic dermatological composition has been studied.
Other features of the invention will become apparent in the course of the following description of the exemplary embodiments which are given for illustration of the invention and are not intended to be limiting thereof.
Example:

Ingredients Qty in %w/w
Allantoin 0.200

Activated Dimethicone 1.000
Urea 10.000
Propylene glycol 5.000
Glycerin 5.000
Liquid Paraffin, Light 8.000
Cetomagrogol 1000 3.000
Cetostearyl Alcohol 9.000
Hard Paraffin 3.000
Polyethylene Glycol 400 8.000
Methyl Paraben 0.100
Propyl Paraben 0.050
Acetic acid, Glacial 0.701
Sodium Acetate Anhydrous 1.680
Fragrance 0.050
Purified Water Qs
1) Cetomacrogol 1000, Cetostearyl alcohol, Hard paraffin, Liquid Paraffin Light were melted at 65°C - 75°C.
2) Methyl Paraben and Propyl Paraben were dissolved in it.
3) Allantoin was added under stirring to part of purified water heated to 50°C - 55°C.

4) Acetic Acid Glacial and Sodium Acetate anhydrous were dissolved under stirring to part of water.
5) Urea was dissolved in part of purified water.
6) Urea solution from step 5 was added to Allantoin solution from step 3.
7) Propylene Glycol, Glycerine and Polyethylene Glycol 400 were added to the
aqueous phase from step 6. The aqueous phase was heated and maintained at 50°C -
55°C.
8) Oil phase from step 1 was added to aqueous phase from step 7 slowly under stirring to form primary emulsion
9) Activated Dimethicone was added to primary emulsion under stirring and cooled to 40 °C.
10) Fragrance was added to the above mass with continuous stirring and the mass was
cooled to room temperature.

Results

Initial 6M 40°C/75% RH
pH 5.66 7.36
Odor of Ammonia Nil Nil
Assay
Allantoin 105.23 101.35%
Urea 98.17 100.94%
Dimethicone 101.83 97.00%

Claim:
1. A stable synergistic dermatological composition comprising pharmaceutical^ active ingredients allantoin, urea, dimethicone and a buffer system along with pharmaceutically acceptable excipients.
2. The stable synergistic dermatological composition as claimed in claim 1, wherein said composition is in the cream dosage form.
3. The stable synergistic dermatological composition as claimed in claim 1, wherein said buffer system comprises glacial acetic acid- sodium acetate buffer.
4. The stable synergistic dermatological composition as claimed in claims 1 and 3, wherein said buffer system is used in concentration of 1.5% to 3 % by weight of cream, preferably 2.35 % by weight of cream.
5. The stable synergistic dermatological composition as claimed in claims 1 to 4, wherein pH of said composition is in the range of 5.0 to 7.5.
6. The stable synergistic dermatological composition as claimed in claim 1, wherein said pharmaceutically acceptable excipient is water washable cream base selected from group comprising Cetomagrogol 1000, Cetostearyl Alcohol, Hard Paraffin and Liquid Paraffin Light.
7. The stable synergistic dermatological composition as claimed in claim 1, wherein said pharmaceutically acceptable excipients are selected from group comprising humectants, emollients, emulsion stabilizers, preservatives, fragrance and other suitable additives.
8. The stable synergistic dermatological composition as claimed in claim 7, wherein said humectants are selected from group comprising Glycerin, Propylene glycol, etc.
9. The stable synergistic dermatological composition as claimed in claims 7 and 8, wherein said humectants are in the range of 5% to 20% by weight of the cream, more preferably 5-10% by weight.
10. The stable synergistic dermatological composition as claimed in claim 7, wherein said preservatives are selected from Methyl Paraben, Propyl Paraben, sodium benzoate and Potassium sorbate.

11. The stable synergistic dermatological composition as claimed in claims 7 and 8, wherein said preservatives are in the range of 0.1% to 0.2% by weight of the cream, more preferably 0.15% by weight of the cream.
12. The stable synergistic dermatological composition as claimed in claim 1, wherein said composition may be in forms such as a liquid dosage form, a milky white lotion, a gel and the like.
13. A process for the preparation of the stable synergistic dermatological composition comprising the steps of
a. adding Allantoin to purified water and heated to 50°C - 55°C;
b. dissolving the buffers in purified water and adding the buffer solution to
step (a);
c. dissolving urea in purified water;
d. adding urea solution from step (c) to allantoin solution of step (a);
e. adding humectants to the aqueous phase of step (d) followed by heating
and maintaining the aqueous phase at 50°C - 55°C;
f. preparing a fatty phase by melting Cetomagrogol 1000, Cetostearyl
Alcohol, hard paraffin and Liquid paraffin light at 65°C - 75°C followed
by dissolving the preservatives in the said fatty phase;
g. adding activated dimethicone to said emulsified system of step (f) and
cooling at 40°c; and
h. adding ingredients like fragrance to the mass of step (g) to obtain stable composition.
14. A stable synergistic dermatological composition and process thereof as
substantially described herein with reference to foregoing example.
Dated this 10th day of September 2007
Dr. Gopakumar G. Nair Agent for the Applicant

Documents:

19-mum-2004-cancelled pages(10-9-2007).pdf

19-mum-2004-claims(granted)-(10-9-2007).doc

19-mum-2004-claims(granted)-(10-9-2007).pdf

19-mum-2004-correspondence(10-9-2007).pdf

19-mum-2004-correspondence(ipo)-(26-9-2008).pdf

19-mum-2004-form 1(8-1-2004).pdf

19-mum-2004-form 18(22-6-2006).pdf

19-mum-2004-form 2(granted)-(10-9-2007).doc

19-mum-2004-form 2(granted)-(10-9-2007).pdf

19-mum-2004-form 26(8-1-2004).pdf

19-mum-2004-form 3(8-1-2004).pdf

19-mum-2004-form 5(7-1-2005).pdf

« Previous Patent

Next Patent »

Patent Number

224363

Indian Patent Application Number

19/MUM/2004

PG Journal Number

02/2009

Publication Date

09-Jan-2009

Grant Date

13-Oct-2008

Date of Filing

08-Jan-2004

Name of Patentee

M/S. INDOCO REMEDIES LIMITED

Applicant Address

INDOCO HOUSE, 166 C.S.T. ROAD, SANTACRUZ (EAST), MUMBAI - 400 098

Inventors:

#	Inventor's Name	Inventor's Address
1	KARE SURESH GOVIND	6TH FLOOR REGENCY AVENUE, NORTH AVENUE ROAD, SANTACRUZ(WEST), MUMBAI-400 054
2	NAIDU RAVI PEDDI	903 -MANISHA TOWER, NAVGHAR 60 FEET ROAD, NEAR TATA COLONY, MULUND (HAST), MUMBAI - 400 081
3	PANANDIKAR ADITI MILIND	DURGA NIVAS, NEHRU ROAD, VILE PARLE (EAST), MUMBAI -400 057 MAHARASHTRA, INDIA
4	RANADE SUNITA Y	B - 504, AYATRI DARSHAN, THAKUR COMPLEX, KANDIVLI (EAST), MUMBAI-400 101

PCT International Classification Number

A61K 31/415

PCT International Application Number

N/A

PCT International Filing date

PCT Conventions:

#	PCT Application Number	Date of Convention	Priority Country
1			NA