Title of Invention

"A HERBAL FORMULATION FOR TOOTHACHE AND RELATED DISORDERS AND A PROCESS FOR PREPARATION THEREOF"

Abstract This invention relates to a process for the preparation of a herbal formulation for the treatment of toothache and related dental disorders comprises of the following steps air drying in shade of the cleaned fresh plant parts of 8 to 15% w/v of Zanthoxylum armatum (fruit pericarp), 4.25 to 10.25% w/v of Spilanthes acmella (flowers), 1 to 4% w/v of Potentilla fulgans (Roots) and 1.5 to 4.5% w/v of Hedychium spicatum (rhizomes) followed by four phased oven drying schedule and then cooling the plant material in a desiccator, over anhydrous calcium chloride and then powdering the dried ingredient, extracting the active ingredients from the powdered herbs obtained in step (a) in ethanol by refluxing for 1 to 1.5 hours at 65 to 70°C and then filtering, extracting the volatile fraction of fresh fruits of 10 to 20% w/v of Zanthoxylum armatum and 1 to 5% w/v aerial parts of Ocimum Kilimandscharicum separately by hydro-distillation for 4-5 hours and separating the camphor from volatile fraction Ocimum Kilimandscharicum, preparing the toothache herbal formulation by mixing of alcoholic extract prepared in step (b) with 10 to 20% w/v of volatile oil fraction of Zanthoxylum armatum, essential oil and 1.5 to 4.5% w/v of camphor fractions of Ocimum Kilimandscharicum prepared in step (c).
Full Text FIELD OF INVNETION
This invention relates to a process for the preparation of a herbal formulation for the treatment of toothache and related dental disorders.
PRIOR ART
The toothache is a pain in a tooth or teeth caused by the inflammation of the nerve in dental pulp. Decay forms a dental cavity which extends into the pulp and causes excruciating toothache. The infection occurs in the tooth which gradually spreads through roots of the tooth into the jaws and gums causing an abscess. Symptoms include pain in a certain tooth or over several teeth, starting from mild to intermittent pain, it becomes worst with hot and cold foods, drinks, air and by the pressure of biting. If a booth is extracted and a large cavity is formed in which the food gets packed, it causes more pain by increased pressure.
A number of formulations are known in the art. These formulations are herbal as well as synthetic in origin. These formulations are available mostly in the form of tablets and capsules except Touch 85 Go' and 'Clove oil' which are liquid.
Some of the synthetic (allopathic) anti-inflammatory or analgesic formulations known in the art are Brufen, Ibugesic S.R., Ibuprofen NEPC, Wingesic Plus, Diclowin Plus, Voveran-50, Dolonex D.T., Diclonac S.R., Novaflam Plus, Chlorizok, Nimegesic, Dexovon, Parvon Forte and Parvon Spas. These formulations have a number of draw backs/ limitations.
The main draw back of above formulations is that they are mostly synthetic products which have side effects in vital body organs.
Another disadvantage of these synthetic medicines known in the art is that the formulations are not broad spectrum but are specific in their action and therefore need
an expert advise for diagnosis of the type of infection and pain in the teeth for prescription of medicine.
Still another disadvantage of these allopathic medicines known in the art is that they have a temporary analgesic effect, which evades pain for short duration and one has to take the medicine repeatedly, which leads to the ingestion and accumulation of ■' large quantity of unwanted chemicals.
I
Yet another disadvantage of allopathic medicines known in the art is that they are either in the form of oral tablets or capsules and thus take ,-.more time in relieving the '
pain..
Further disadvantage of the allopathic drugs known in the art is that most of them contain antipyretic salts which are not always required/useful for the patients. Besides this most of these drugs are costly and beyond the reach of poor people.
The herbal products known in the art are "Clove oil LP", "Touch and Go", Septilin tablets and Detonsy tablets.
The disadvantage of "Touch and Go" herbal product used for topical application available in the art is that it contains solvent ether, spirit and chlorofomi, which are harmful.
The disadvantage of herbal product Clove oil is that it has a burning sensation on gums and is quite costly also.
The disadvantage of the other herbal products viz. Septilin and Detonsy is that they are available in tablet form and thus take a longer time in relieving the pain.
A known process published in patent No. US 6264926 uses Zanthoxylum armatum and Spilanthes calva in the formulation of a natural herbal tooth powder/tooth paste for use as a preventive measure of toothache.
The disadvantage of this herbal formulation is that it is in the form of a toothpaste / powder which, can not be used at the time of incidence of acute pain.
Another published patent No. CN 1299675 utilizes a number of herbs including Zanthoxyium and insect material (Black bee) for the preparation of a gargle for treating toothache.
The main disaavantage of the ,above fonnulation is that it utilizes insect .material (black bee) which a large population may not accept to put in mouth for gargling. '
Another disadvantage of the formulation is that the black bee is difficult to obtain.
The literature survey describes that raw fruits of Zanthoxyium armatum and flowers of Spilanthes acmella are used for cure of toothache.
The main disadvantage of using raw fruits & flowers is that the flowering/fruiting season of plants is of very short duration and hence can be used during that period only.
Another limitation of using raw fruit of Zanthoxyium armatuim and flowers of
Spilanthes acmella is that the plants grow at an altitude of 3000 to 5000 feet, so can be
used by local inhabitants only. I
Another known art in the literature describes that the roots of Potentilla fulgans are antiodontalgic.
The main limitation of using roots of Potentilla fulgans is that it does not provide quick relief in acute toothache.
Another known art in literature describes that rhizome of Hedychium spicatum is anti-inflammatory and antimicrobial.
The main limitation of this plant is that it is not found to be effective in relieving toothache.
OBECTS OF PRESENT INVENTION
The main object of the present invention is to provide a herbal formulation for treatment of toothache and related dental disorders and a process for preparation thereof.
. Another object of the present invention is to provide a herbal formulation .and a process for its preparation which Involves plurality of herbs.
Still anothter object of the present invention is to provide a herbal fomiulation and a process for Its preparation which Is based on locally available plant materials.
Yet another object of the present invention is to provide a herbal formulation which can be used for swelling, Infection of gums and hot and cold sensation of teeth.
Further object of the present invention is to provide a herbal fomiulation which does not have any side effects.
Still further object of the present Invention is to provide a herbal formulation which relieves pain within 2 to 10 minutes.
Yet further object of the present Invention Is to provide a process for preparation vhich Is simple and economical.DESCRIPTION OF INVENTION
According to this invention there is provided a process for the preparation of a herbal formulation for the treatment of toothache and related dental disorders comprises of the following steps:
(a) air drying in shade of the cleaned fresh plant parts of 8 to 15% w/v of Zanthoxylum armatum (fruit pericarp), 4.25 to 10.25% w/v of Spilanthes acmella (flowers), 1 to 4% w/v of Potentilla fulgans (Roots) and 1.5 to 4.5% w/v of Hedychium spicatum (rhizomes) followed by four phased oven drying schedule and then cooling the plant material in a desiccator, over anhydrous calcium chloride and then powdering the dried ingredient,
(b) extracting the active ingredients from the powdered herbs obtained in step (a) in ethanol by refluxing for 1 to 1.5 hours at 65 to 70°C and then filtering,
(c) extracting the volatile fraction of fresh fruits of 10 to 20% w/v of Zanthoxylum armatum and 1 to 5% w/v aerial parts of Ocimum Kilimandscharicum separately by hydro-distillation for 4-5 hours and separating the camphor from volatile fraction Ocimum Kilimandscharicum,
(d) preparing the toothache herbal formulation by mixing of alcoholic extract prepared in step (b) with 10 to 20% w/v of volatile oil fraction of Zanthoxylum armatum, essential oil and 1.5 to 4.5% w/v of camphor fractions of Ocimum Kilimandscharicum prepared in step (c).
DESCRIPTION OF PROCESS
According to the present invention the process for preparation of herbal formulation comprises of the steps of:
a) Drying of plaint material for non-volatile fraction
The fresh plant material of plants namely Zanthoxylum armatum (Fruit pericarp), Spilanthes acmella( Flowers), Potentilla fulgans (Roots) and Hedychium spicatum fRhizomes) are taken separately and washed with water to remove dust and other foreign particles adhered to it. They are then spread for drying in shade. When the surface adhered moisture is dried, then they are re-dried in an oven at different temperatures. Each of the plant material is subjected to four phase heating schedule comprising of heating at about 40°C for about two hours, then at about 60°C for about one hour followed by about 30 min. at about 70°C and for about 15 min. at about 90°C. After drying, each plant material is put in a separate desiccator for cooling, over anhydrous calcium chloride. The cooled material is finely grounded and sieved by 0.3 mm mesh sieve.
(b) Solvent extraction of active ingredients
The dried and powdered plant material of each plant is taken in 90% ethanol in proportion of 8 to 15% W/V preferably 10 to 12% W/V of Zanthoxylum armatum,(fruit pencarp powder), 4.25 to 10.25% W/V preferably 6.25 to 7.25% WA/ of Spifanfhes, acmeila, (flower powder), 1 to 4% preferably 2 to 3% W/V of Potentilla fulgans (root powder) and 1.5 to 4.5 % preferably 2.5 to 3.5% W/V of Hedychium spicatum in a -conical flask fitted with water reflux condenser. The flask along with the assembly Is placed over a hot plate controlled at 65-70° C and refluxed for 1 to 1.5 hrs. The extraction s then stopped and contents are filtered.
c) Extraction of volatile fraction of plants
For volatile fraction, the essential oil, of plants, the fresh plant material namely fruits of Zanthoxylum annatum and aerial parts of Ocimum kilimandschan'cum are distilled separately by Clevenger apparatus through hydro-distillation for 4 to 5 hours. The oil of Ocimum kilimandscharicum when distilled, the camphor portion gets solidified, which is separated from the oil.
(d) Preparation of anti-toothache herbal solution
The ethanol extract as prepared above in step (b) is taken in a conical flask and essential oil of Zanthoxylum armatum in a ratio of l6-20%VN preferably 15-18%V/V, essential oil of Ocimum kilimandschan'cum in a ratio of 1-5%V/V preferably 2-3%V/V and camphor of Ocimum kilimandscharicum in a ratio of 1.5-4.5%W/V preferably 2.5-3.5%W/V are added. The flask is then shaken on a mechanical shaker for 10 to 15 minutes so that all the contents are thoroughly mixed and a homogeneous solution is obtained. This solution thus becomes ready for application in paining tooth/ teeth, with the help of a cotton swab.
This invention will now be illustrated with a working example, which is intended to be typical example to explain the technique of the present invention and is not intended to be taken restrictively to imply any limitation to the scope of the present invention;
WORKING EXAMPLE
'The fruits of Zanthoxylum armatum, flowers'of Spilanthes acmella ;root of Potentilla fulgans and rhizomes of Hedychium spicatum were collected, washed and then spread for drying in shade. When the surface adhered moisture dried up, they'were re-dried in an oven at different temperatures. Each of the plant jnaterial was subjected to four phase heatihg schedule comprising of heating at 40%C for two hours, at 60°C for one hour, 30 min. at 70 C and 15 min. at 90 C. After drying, each plant material was put in a separate desiccator for cooling over anhydrous calcium chloride. The cooled "material was finely grounded and sleved by 0.3 mm mesh sieve. 40 g finely powdered fruit pericarp of Zanthoxylum armatum, 25g dried flower powder of Spilanthes acmella, 8 g root powder of Potentilla fulgans and 10 g rhizome powder of Hedychium spicatum were taken in a 1000 ml conical flask containing 400 ml of 90% ethanol. The flask was fitted with a water reflux condenser and then placed over a hot plate controlled at 65-70°C. The contents of the flask at this temperature were refluxed for 1 to 1.5 hrs. There after the heating was stopped and contents were left for cooling. The extracted material was then filtered and the volume of futrate was made up to 400 ml by adding additional amount of 90% ethanol.
For volatile fraction of plants, the fresh plant material (fruits) of Zanthoxylum armatum and aerial parts of Ocimum kilimandschan'cum were distilled by Clevenger apparatus through hydro-distillation for 4 to 5 hours and essential oil of both the plants and camphor from Ocimum kilimandscharicum were collected separately.
To the above filtered extract in 90% ethanol, 60 ml of Zanthoxylum armatum essential oil, 8 ml of Ocimum kilimandschan'cum essential oil and 10 g of Ocimum kilimandscharicum camphor were added. The whole contents of the flask were then shaken with the help of a mechanical shaker and homogenized for 10 to 15 minutes. This homogenized solution thus became ready, as anti-toothache formulation.
TOXICOLOGICAL STUDIES
The toxicity studies of the formulation for toothache and related dental disorders was done at ITRC, Lucknow for acute dermal toxicity, sub acute (28 days) dermal toxicity test in female rats and mucous membrane imtation test in rabbit vagina, by standard
methodologies using SOP /GTX /001, SOP/ GTX / 002 and SOP/GTX / 007 as J
referenc'e standards.' '
(I) . Acute dermal toxicity In male and female rats
-The LDso (lethal dose 50) of product at limit test dose was found to be .>2000 ,mg/kg body weight in both male and female rats. At this limit test dose i.e. 2o6o"mg/kg ' body weight did not produce any sign of toxicity and mortality of animals up to 14 days of observation. Autopsy of experimentaf animal at the end of observation period did not indicate any gross pathological changes in their vital organs.
(II) Sub Acute (28 days) dermal toxicity in rats
Repeated dermal application of the product (1000mg/kg/day) did not show any signs of poisoning through out the period of exposure.
It
• Body weight of control and treated rats did not show any variation.
• Organ body weight ratio of various vital organs did not show any variation.
• The gross pathological studies did not show any significant changes.
CLINICAL TRIALS
The clinical trials of the product were carried out at Govt. District Hospital and Military Hospital, Pithoragarii. The total patients covered during 2000, 2001, 2002 and 2003 were 235 in District Hospital, Pithoragarh and 128 at Military Hospital, Pithoragarh. The results are given in table 1 and 2. The feed back information indicates that the Tiajority of patients got relief from pain within 2 to 10 minutes.
Table 1 Clinical trials of Anti-toothache Herbal Formulation (Conducted at Govt. District Hospital, Pithoragarh)
(Table Removed)
It is to be understood that the process of the presentinvention is susceptible to modifications, changes, adaptations by those skilled in the art. Such modifications, changes, adaptations are intended to be within the scope of the present invention which is further set forth under the following claims:













I CLAIM:
1. A process for the preparation of a herbal formulation for the treatment of toothache and related dental disorders comprises of the following steps:
(a) air drying in shade of the cleaned fresh plant parts of 8 to 15% w/v of Zanthoxylum armatum (fruit pericarp), 4.25 to 10.25% w/v of Spilanthes acmella (flowers), 1 to 4% w/v of Potentilla fulgans (Roots) and 1.5 to 4.5% w/v of Hedychium spicatum (rhizomes) followed by four phased oven drying schedule and then cooling the plant material in a desiccator, over anhydrous calcium chloride and then powdering the dried ingredient,
(b) extracting the active ingredients from the powdered herbs obtained in step (a) in ethanol by refluxing for 1 to 1.5 hours at 65 to 70°C and then filtering,
(c) extracting the volatile fraction of fresh fruits of 10 to 20% w/v of Zanthoxylum armatum and 1 to 5% w/v aerial parts of Ocimum Kilimandscharicum separately by hydro-distillation for 4-5 hours and separating the camphor from volatile fraction Ocimum Kilimandscharicum,
(d) preparing the toothache herbal formulation by mixing of alcoholic extract prepared in step (p) with 10 to 20% w/v of volatile oil fraction of Zanthoxylum armatum, essential oil and 1.5 to 4.5% w/v of camphor fractions of Ocimum Kilimandscharicum prepared in step (c).
2. A process as claimed in claim 1 wherein said four phased oven drying schedule comprises at a temperature of about 40°C for about two hours, at about 60°C for about one hour, at about 70°C for about 30 minutes and at about 90°C for about 15 min.
3. A process as claimed in claim 1 wherein fruit pericarp powder of Zanthoxylum armatum is taken in range of preferably 10 to 12% w/v in 90% ethanol.
4. A process as claimed in claim 1 wherein flower powder of spilanthes acmella is taken in range of preferably 6.25 to 7.25% w/v in 90% ethanol.
5. A process as claimed in claim 1 wherein root powder of potentilla fulgans is taken in range of preferably 2 to 3% w/v in 90% ethanol.
6. A process as claimed in claim 1 wherein rhizome powder of hedychium spicatum is taken in range of preferably 2.5 to 3.5% w/v in 90% ethanol.
7. A process as claimed in claim 1 wherein volatile fraction of zanthoxylum armatum is taken in range of preferably 15 to 18% v/v.
8. A process as claimed in claim 1 wherein volatile oil fraction of ocimum kilimandscharicum is taken in range of preferably 2 to 3% v/v.
9. A process as claimed in claim 1 wherein camphor of ocimum
kilimandscharicum is taken in range of preferably 2.5 to 3.5% w/v.
10. A process for the preparation of a herbal formulation for the
treatment of toothache and related dental disorders substantially
as described and illustrated in the examples herein.

Documents:

260-DEL-2004-Abstract (25-01-2010).pdf

260-del-2004-Abstract-(01-04-2010).pdf

260-del-2004-abstract.pdf

260-DEL-2004-Claims (25-01-2010).pdf

260-del-2004-Claims-(01-04-2010).pdf

260-del-2004-claims.pdf

260-DEL-2004-Correspondence-Others (25-01-2010).pdf

260-del-2004-correspondence-others.pdf

260-del-2004-correspondence-po.pdf

260-DEL-2004-Description (Complete) (25-01-2010).pdf

260-del-2004-Description (Complete)-(01-04-2010).pdf

260-del-2004-description (complete).pdf

260-del-2004-Form-1-(01-04-2010).pdf

260-del-2004-form-1.pdf

260-del-2004-Form-2-(01-04-2010).pdf

260-del-2004-form-2.pdf

260-DEL-2004-Form-3 (25-01-2010).pdf

260-DEL-2004-GPA (25-01-2010).pdf


Patent Number 240652
Indian Patent Application Number 260/DEL/2004
PG Journal Number 22/2010
Publication Date 28-May-2010
Grant Date 21-May-2010
Date of Filing 23-Feb-2004
Name of Patentee THE DIRECTOR GENERAL(DRDO)
Applicant Address DEFENCE RESEARCH & DEVELOPMENT ORGANISATION MINISTRY OF DEFENCE, GOVT OF INDIA, WEST BLOCK-VIII, WING-1, SECTOR-1, RK PURAM, NEW DELHI-110 066, INDIA.
Inventors:
# Inventor's Name Inventor's Address
1 HEMANT KUMAR PANDEY GOVT. OF INDIA, MINISTRY OF DEFENCE DEFENCE RESEARCH AND DEVELOPMENT ORGANIZATION DEFENCE AGRICULTURAL RESEARCH LABORATORY, PITHORAGARH-262 501 (UTTARANCHAL), INDIA.
2 PURAN SINGH RAWAT GOVT. OF INDIA, MINISTRY OF DEFENCE DEFENCE RESEARCH AND DEVELOPMENT ORGANIZATION DEFENCE AGRICULTURAL RESEARCH LABORATORY, PITHORAGARH-262 501 (UTTARANCHAL), INDIA.
3 NARENDRA KUMAR GOVT. OF INDIA, MINISTRY OF DEFENCE DEFENCE RESEARCH AND DEVELOPMENT ORGANIZATION DEFENCE AGRICULTURAL RESEARCH LABORATORY, PITHORAGARH-262 501 (UTTARANCHAL), INDIA.
4 GAURI SHANKER VERMA GOVT. OF INDIA, MINISTRY OF DEFENCE DEFENCE RESEARCH AND DEVELOPMENT ORGANIZATION DEFENCE AGRICULTURAL RESEARCH LABORATORY, PITHORAGARH-262 501 (UTTARANCHAL), INDIA.
PCT International Classification Number A61K 35/78
PCT International Application Number N/A
PCT International Filing date
PCT Conventions:
# PCT Application Number Date of Convention Priority Country
1 NA