WO2002089826A1

WO2002089826A1 - Method of preparing garlic ointment and garlic ointment composition for topical use in skin infections

Info

Publication number: WO2002089826A1
Application number: PCT/IN2001/000098
Authority: WO
Inventors: Sanjay Suri; J. Singh; Ulhas Dhuppad; A. K. Bhatham
Original assignee: Morepen Laboratories Ltd.
Priority date: 2001-05-04
Filing date: 2001-05-04
Publication date: 2002-11-14

Abstract

Garlic Ointment of the present invention is an effective antibacterial and antifungal ointment for tropical use in skin infections. The object of this ointment is to utilize all constituents of garlic to achieve maximum benefit. Allin and Allicin are stablized in the ointment. The preparation comprises of freeze dried garlic powder together with a pharmaceutically acceptable carrier therefore. The composition may be applied topically in treatment of general skin infections.

Description

TITLE: METHOD OF PREPARING GARLIC OI TMENT AND bARi. it; U IN I MKN Γ C MPOS I T I ON FOR TOP I CAL USE

IN SI- IN INFECTIONS. Technical Field:

the invention relates to 'Method of preparing Garlic Ointment and Garlic-Ointment composition' for exte l use on fr->cted kin.

PRIOR ART/FIELD OF INVENTION:

tablet. Oils, I'voiic loriris are already available and traditionally being used as chest plaster, chest rub, compress cold/hot decoction, foot poultice, douche and as nose drops.

^"the present preparation describes the method of preparation of ointment of Garlic. Garlic has been exploited for ts medicinal proper ies Finte centuries by people and physicians throughout the world. Garl c contains atleast 400 compounds which are unique to it. Of these 400 compounds, atleast Z<Δ compounds AΠ.^ Inown to have <Fome or the other medicinal properties.

Most of the garlic compounds havmq medicinal properties derived from the breakdown of a compound known as Allicin, Allicin s an active medicinal compound. The compounds present n garlic have one or more than one of the following activities. These can be used as an antibiotic, detoxifying agent, as an antioxidant and fol^¬ lowermq of blond sugar and cholesterol levels. It can b also be- used for liver protection. These . the functions of the compounds which arr? identified and had been exploited. There

presently, many unidentified compounds whose functions has not been exploited. Therefore, t s advisable to use garlic: as a whole,

.1 rather thctn using i s active components selectively, to derive maximum benefits from the medicinal properties of the ga 1 IC .

Uses of garlic as medicine are quite wide, more than, what are known to the human beings. Garlic has been .15 found to be a broad spectrum antibiotic and is effective n lillinq variety of gram positive and gram negative bacteria. It does posses a good anti fungal and antiparasi ti proper t .

Allicin, one of the mam active ingredient of qarlir is 20 not a stable mol cule. it tends to degrade n the presence of water , acid and base. Henc the conditions in which allicin s stable <3κr <s limited. Garlic powder n the present inven ion is freeze dried to preserve its allicin content. Also there AΓG different varieties of ?^r garlic being cultivated, which contains different allicin content. An object of the present invention s to provide a new type of preparation of ga lic which is useful or external use on the skin. Another object of the present invention s to provide a stable ointment preparation of garlic, which provide stability to allicin. Still further object of the invention te to provide a process for preparing a preparation as set forth above. These and other objects of the invention will be apparent from the following description.

A topically adm ini str able composition of the invention will preferably be in the form of an ointment. In a further aspect the composition of the present invention w ll be m the form of a hydrophobic ointment. When the preparation is applied on the sk n, it comes in contact with water available on the surface of the skin in the f rm of perspiration and gets emulsified after rubbing with fingers. in the presence of water, allicin from the garlic is being released and alnn is also being converted nto allicin. Suitable hydrophobic ointments A Γ those which are formed from white or yellow soft paraffin with liquid paraffin. The preparation of the present invention can be prepared by dispersing freeze dried garlic powder in the light liguid paraffin with continuous stirring to get homogenous mixture of garlic powder and l ght liquid paraffin, and admixing the dispersion of ciarlic powder n liquid paraffin m a mixture of microcrystal 1 me wax and white sof paraffin at temperature between 40 o i o 45 C. A mi ture of micror ry t al I ine wax and white soft, paraffin is prepared by heating the mixture in hot o water bath to 6ø~ 65 C, and stirring continuously to ge a homoqenous mixture. A suitable perfume may be added to give pleasant smell to the preparation, after o cooling down the above preparation to about 30 C.

According to the invention, the method of preparing garlic ointment for topical use comprises of the ollowing steps :-

( dispersing the free∑od dried garlic powder in the light liquid paraffin w th mecrhanical stirrer to get homogenous mixture of garlic powder and light liquid paraffin in the ratio of 1:5 to :10 (w/w 7. ) . Preferred ra io is 1.5: 10.

(n) mix micro ryst al 1 me wax in white.* soft paraffin in the ratio of 2:70 to 10:90 (w/w "/.). By heating the mixture in hot water bath and contmously stirring to get a homogenous mixture of microcryε tai 1 ine way, and o white soft paraffin at temperature ranges of 60-65 C, preferred ratio is 5:83.4 (w/w 7. ).

(in) cooling the mixture prepared in step (it) to c 40 C and adding the mixture of garlic powder and 1 Liquid paraffin prepared under step (i) above and stirring continuously to qet homogenous mixture, at a temperature o of 40-45 C.

o (iv) cooling down the preparation of step (in) to 30 C and adding suitable prefume to give pleasant smell using a mecrhanical stirrer.

DESCRIPTION OF PREFERRED EMBODI ENTS:

The garlic ointment is based on the properties of garlic, and ither constituents of the ointment only as a diluents. Freeze dried garlic powder acts as an antibateπal and antifungal agent. White soft paraffin, a purified mixture of semisol id saturated hydrocarbon, qιve= its emollient property to the preparation and acts as a carrier. Microcrystal 1 me wax is used as a stiffening agent, thereby increasing the consistency of ointment. Light liguid paraffin, a purified mixture of liquid saturated hydrocarbon , gives its emollient property to the preparation and act as a carrier for dispersion oi drug.

F-ol lowing table shows the percentage weight of the constituents of garlic; ointment which have been obtained experimentally and for maximum benefits. Ex am l 1 .

Ingredient- Range 'referred ( V. /w ) (V. w/w)

Fr ez d ied g r 11 Powder 1 - 7 1 . 50 Whi e soft paraffin 70 - ^■ 90 S3 . 40 c roc r y t a 111ne wax 1 5.0ø Light liquid paraffin 5 - • lø 10 .00 Pe fume 0 . 05 - 0. 15 0. 1 0 ,. >. — . ._____._-_ — __

St AMII 1TY TESTING OF I HE FORMULATION

Formulation as described in example I was tested under accelerated conditions for the stability of allic m the composition. Composition A is the formulation disclosed in the invention and composition B is oil in water emulsion ointment composition.

T ble 1 Ingredient? A B

Freeze dried Garlic powder- 1.5 ^■/. 1.5 7. Wh te soft paraffin 8:3.5 V. 1 .0 V. Light liquid paraffin 10.0 7. 6.0 "/. Microcrystal 1 me wax 5.0 7. Cetostearyi alcohol / .2 /. Cetomacrogoi .1.8 "/. Gl ycerol 5.0 V. Purified Water q.s. to 100 7. Each composition was prepared as follows:

Composition A is prepared by dispersing freeze dried garlic powder in the light liquid paraffin with continuous stirring to get homogenous mixture of garlic powder and light liquid paraffin, and admixing the dispersion of garlic powder in liquid paraffin in a mixture of microcrystal 1 ine wax and white soft paraffin o at temperature between 40 to 45 C. A mixture of microcrystal 1 ine wax and white soft paraffin is prepared o by heatmq the mixture-? in hot water bath to 60-65 C, and stirring cot uously to get a homoςienous mixture.

Composition B is prepared by dispersing freeze dried garlic powder in giyceroi to form a smooth homogeneous suspension and this is then added to the stirred water in the mixing vessel. C tostearyl alcohol and paraffin o are melted together and heated to /0 C. The molten mixture is added to the aqueous component with stirring.

Stirring is gradually reduced as the mixture cools and thict- ens . fable - 2 o

Allic content on ageing at 25 C

Time in mon hs A B

0 0.0195 7. Θ.01S6 7. .1 0.0.192 7. 0.01/3 7.

2 0.0192 7. 0.0161 7.

3 0.0190 7. 0.0154 V. t> ,0189 7.

From the stability data, it is evident that composition of the present invention (A) s superior to composition B, which is, a aqueous base preparation.

While the present invention has been described above with respect to several preferred embodiments thereof, it should of course¹ be understood that it should not be limited only to them but various changes or modific tion may be made in any acceptable manner without departing from the spirit and scope of invention as defined by the appended claims.

Claims

WF CLA I M :

1- A method of preparing ointment for topical use comprising the steps of:~

(i) dispersing the freezed dried garlic powder in the light liquid paraffin with mechanical stirrer to get homogenous mixture of garln powder and 1 lgtit liquid paraffin m the ratio of 1:5 to /slø (w/w %). Preferred

(n ) mix mi rocrystal line wax white soft paraffin in the ratio of 2:70 to 10:90 (w/w V. \ . By hea mq the mixture in hot water bath and c ontmously stirring to get a homogenous mixture of microcrystal 1 me wax and o white soft paraffin at temperature ranqes of 60-65 C, preferred ratio is 5:83.4 iw/w 7. ) .

(in) cooling the mixture prepared in s,tep (n) to o 40 C and adding the mixture of garlic powder and liquid paraffin prepared under step (l) above and stirring continuously to get homogenous mixture, at a temperature o of 40-45 .

o (iv) cooling down the preparation of step (in) to 30 C and adding suitable prefume to give pleasant sm ll using a mechanical stirrer.

2. A method of preparing an ointment as claimed in claim 1 wherein the ratio (w/w 7.) of dried garlic powder to light liquid paraffin is .1:5 to : .10 preferably 1.5:10.

3. A method of preparing an ointment as claimed in claim I wherein the ratio (w/w 7. ) of microcryst l 1 e wax to white soft paraifin is 2.70 to 10.90 preferably 5:8 .4.

4. A method of preparing an ointment as claimed in claim 1 wherein step (in) is carried out at temperature of 40 C.

5. A method of preparing an ointment as claimed in earlier claims wherein any suitable perfume is added at o a t mpe ature of 30 C and stirring cont nuously.

6. The qarlic ointment composition for topical use substantial ly as herein described with reference to the fors id examples.

7. A method of prep rinci ointment i or topical use substantially as herein described with reference to the? examples described herein.