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(11) Patent Number: KE 109
(45) Date of grant: 31/07/2000
(12) PATENT
(51) IPC (7): A61K35/78; A0IN65/00
(21) Application Number: KE/P/1993/00085   
(84) WO No:
(22) Filling Date: 30/04/1993
(31) Priority Number:
(32) Priority Date:
(33) Priority Country:
(73) Proprietor(s): (1) Dr. FRANCESCO Gerli, P.O Box 62642, Nairobi; (2) Dr DANIELE CIOPPI, P.O Box 62642, Nairobi.
(72) Inventor(s): Dr. FRANCESCO Garli, P.O Box 62642, Nairobi; Dr DANIELE CIOPPI, P.O Box 62642, Nairobi
(74) Agent: Hamilton Harrison & Mathews Advocates P.O Box 30333 Nairobi
(54) Title: Use of Tharchonanthus camphratus, L
(57) Abstract
Use of Tharchonanthus camphoratus parts and its derivatives in insect-repelling, anti-irritating, soothing, anti-oedema, decongesting formulations and compositions.
Cited Documents
WO 94/09631; Database WPI, week 6800, London: Demon Publications Ltd., AN 66-33730F, ZA 67(14243; Database WPI, Week 9736, London: Derwnet publications LTd. AN 97-385852, CN 1110562 A 25 October 1995.
 
USE OF THARCHONANTHUS CAMPHORATUS, L.
This invention is referred to the uses of the Tharchonanthus Camphoratus, L.; utilization of its leaves, roots and branches either fresh, dried, soaked, extracted or in form of essential oil.
The Tharchonanthus Camphoratus, L. is a shrub rearing in the wild in different African regions especially in the Rift Valley of Kenya uplands areas.
The shrub, mostly unknown by botanists, has different name6 such as Wild cotton, Sage wood, Wildesalie, Kamferhout, Kamferbos, Sieriehout, Valbos, Veld-valbos, Vaiobos, Santo Mofahlana, Rologe Thalaping mohathla, well known in the local Kiswahili dialect with the name of "Lsleshua", and in the abissianian language "Ebok" and so on, or simply with the botanic name of Tharchonanthus Camphoratus, L,
The Tharchonanthus Camphoratus, L. is a shrub reaching 2-4m. height; belonging to the compositae family; it has regular branches with velutinous white greenish oval or lanceolate shaped leaves ranging from 4 to 13 cm length having a strong camphorated aromatic smell, hence its Linnaeana denbmination.
This plant, with its wool-like, spike shaped flower heads is mentioned only in "The Medicinal and Poisonous Plants of Southern Africa" by John Mitchell Watt and Maria Gerdina Breyer-Brandwijk - Edimburgh, 1932 and Paolo Rovesti's communication, presented at the XXIX International Congress of Industrial Chemistry in Paris in December 1956, "Ecological influences in the composition of the essential oils".
Different applications and uses of this plant are reported in the literature. Some of them are listed here below:
-    It is used for woodcarving by Masai (Brown).
-    Usambara in Tanzania are reported to use it for its wood (Bugles).
A medicinal and antiseptic infusion for cattle is reported to be prepared by Ethiopians making the plant leaves ferment in urine (Schimper).
Dragerdoff reports the same therapeutic effect as the ones of Salvia Officinalis, L.
It has been found, and this is the subject of this invention, that some parts of the plants, in particular its leaves, fresh or dried, and their    derivatives,    have    some    mosquito    repelling,",    anti-oedema,
decongestant,anti-irritating and soothing properties that might be profitably used for therapeutic applications both for humans and animals.
The derivatives of this invention concern the Tharchonanthus Camphoratus, L. extracts obtained through an extraction as mentioned, for example, in the Italian Pharmacopeia.
Some examples of these preparations are: mosquito-fumigants, fumigants, vaporizing solutions platen, sprays, sticks, lotions, creams and gels.
One of the main goals of this incaution is the application of the essential oil. According to the present invention, the application of this plant and of their derivatives concerns not only its action with the mosquitoes but also the treatment of irritations and inflammations caused by insect bites.
In fact, the efficiency of the Tharchonanthus Camphoratus, L. derivatives has been also found during some irritations and inflammatory conditions on skin as, for example, eczema, acne, reddening, swelling and on genital and mouth mucosa.
The Tharchonanthus Camphoratus, L. essential oil obtained through a distillation in steam flow, has been characterized using a GC/MS analysis. In this way 44 components were identified. Among these, the following main ones have been found:
- Alpha Pinene    15.40%
- Camphene    4.35%
- Beta Pinene    3.50%
(1) The term "Mosquito Repellent" is used here for easy reference. It seems, in fact, that the plant fragrance works as a "decoy". From experiments carried out in Kenya with this plant it has been shown that Tharchonanthus Camphoratus, L. in one of the most attractive plants for mosquitoes for their day rest, The mosquitoes, infect, rest during day time under its leaves in great number, Moreover, it has been noted that the presence of mosquitoes in neighboring plants is very minimal and, in some cases, nihil. Humans and animals getting close to the plants during day time, are attacked by mosquitoes with particular virulence, mostly if the leaves are somehow stirred.
Using the essential oil extracted from the leaves, a cream has been prepared.
Smearing such a cream in the skin exposed to mosquitoes bite, it has been found that the Insects, possibly confused by the smell, do not recognize the human body as such. It seems that the mosquitoes "See" the body as if it were the friendly plant. Even when some mosquitoes by chance set on the skin smeared with the cream, they don't normally bite. Further experiments and observations showed that in the evening the mosquitoes leave the plant in search of food.
It seems that when it is dark the smell of the leaves "Push" the mosquitoes away.

 -Delta - 2 - Carene    4.30%
-Alpha Phellandrene    1.60%
-Limonene    3.00%
-Gamma Terpinene    2.05%
-Terpinolene    1.35%
-1,8 Cinoelene    12.10%
-Fenchol                                             14.40%
-1-Terpinen-4-ol                                2.30%
-Alpha Terpineol    4.50%
-Fenchone    0.85%
-Bergamatene    4.50%
-Delta Cadinene    1.40%
-Alpha Curcumene    1.70%
Basing on a test of primary skin irritation on human, it appears that the Tharchonanthus oil, smeared as it is on 20 volunteers' healthy skin in occlusive conditions, gave a medium irritation index of 0.4 after 15 minutes and of 0.35 24 hours after the sample removal.
Basing on the above mentioned parameter, the product is then classified as non-irritating.
The essential oil showed also some surprising therapeutic and anti-oedema properties, and for this reason another object of the present invention is the topical pharmaceutical compositions containing from 0.01 to 10 % of Tharchonanthus Camphorates, L. essential oil used as an_ active ingredient, alone or combined with other active materials. The compositions can be made according to conventional methods as reported, for example, in the "Remington's Pharmaceuticals Sciences Handbook". Mack Pub. H.Y.U.S.A.
Some examples of pharmaceuticals topical compositions are: Solutions, suspentions, emulsions, creams, toothpastes in gel form, sprays, prolonged release compositions such as transdermdc plasters, and soaps. One of the preferred embodiments of this invention is the preparation of "Mosquitoes Repellent" formulations containing from 0.01 to _10% of’’
This observations has been confirmed with experiments carried out during the night in a small room with openings on the outside in presence of a strong smell of Tharchonanthus oil. As long as the light is kept on, the mosquitoes present in the room are resting with very few of them flying for a short while. Once the light is switched off, a very strong buzz can be heard of mosquitoes flying and whoever present in the room is viciously stung.
Leaving the room empty (i.e., with neither humans nor animals present), after about half an hour, all the mosquitoes leave the room - possibly to chase for food - and, if a human comes and stays for a long period of time, no bites whatsoever are reported to happen because the mosquitoes are simply absent.
The Therchonantue Camphorates products are therefore working as a decoy for mosquitoes: i.e. mosquitoes feel the human body as being a plant. Therefore, the terminologies "mosquitoes repelling" and "mosquito repellent" are here used for easy reference only.
 
Tharchonanthus Camphoratus, L. essential oil as active ingredient, alone or with other similar components having the same activity.
The Tharchonanthus Camphoratus, L. essential oil, put in different topical formulations with "Mosquito Repelling' effect, can be used in quantities ranging from 0.03% to 7%, preferably from 0.05% to 3%.
In insect repelling formulations, where the shrub is used in its natural state, the quantity must be from 5% up to 95%. In this case it is advisable to use the plant during its balsamic period and immediately after being picked up; this, unfortunately, sets a limit to the Tharchonanthus use at its natural state, while no limit is fixed for its essential oil.
The Tharchonanthus Camphoratus, L. essential oil, put in different topical compositions having anti-oedema, decongestant, anti-irritating and soothing activity, can be used in quantities ranging from 0.01% to 5% and, preferably, from 0.03% to 0.5%.
The activity of its essential oil, being part of this invention has been tested in more than one pharmacological and clinical test.
The following example further illustrate the invention. For brevity sake, the essential oil is called E.O.
1.  “Mosquitoes Repellent"
1.1 A spray lotion containing 0.3% Tharchonanthus Camphoratus, L. essential oil was smeared on 10 volunteer’s skin in places with as extremely high mosquito’s concentration. It has been shown that none of them had bites on the skin (Example 1.1)
1.2 A Tharchonanthus Camphoratus, L. essential oil alcoholic lotion, containing 0.2% of Tharchonanthus essential oil was used in a diffusor with absorbent tampon and put in a dimly airly room of about 60mc infested with the boothersome insects. Once the diffusor worked, the insects disappeared within half an hour (Example 1.2)
3. Anti-oedema, decongestant, anti-irritating and soothing activity.
2.1 An application of 0.21 Tharchonanthus Camphorates, L. essential
oil gel was put on female genitals with itching problems. That brought an immediate relief (Example 2.1h       curative forces of fundal infection.

2.2 A gel containing 0.05% Tharchonanthus Camphoratus, L. essential oil was used against bags under one's eyes. A rapid and surprising recovery took place (Example 2.2).
2.3 A gel on 0.3% Tharchonanthus Camphoratus, L. essential oil basis was used on a right ear as remedy for a swelling due to mosquitoes, or some other unidentified insect bite. The problems was immediately solved. The same result was obtained after an application on different skin areas on 10 persons with various bites (Example 2.3)
2.4    A gel with 0.05% Tharchonanthus Camphoratus, L. essential oil content, was used on 10 persons suffering from frequent erythema generally treated with a cortisone cream. It was found that all subject recovered rapidly and both the painful and itching sensations disappeared (Example 2.4).
2.5 An alcoholic solution containing 0.1% Tharchonanthus Camphoratus, L. essential oil was put, by means of a tampon, on pimply skin full with acne on 10 patients in all of the above mentioned situations, the problem was totally solved. The same preparation was put on recent pimples that disappeared 24 hours later (Example 2.5).
 2.6    A gel with 0.1% Tharchonanthus Camphoratus, L. essential oil was used on 5 subjects' face and neck skin and on the armpits and legs suffering from irritation deriving from shaving and depilation treatments all the subjects declared a relief and freshness sensation (Example 2.6).
2.7 A fluid emulsion containing 0.1% Tharchonanthus Camphoratus, L. essential oil, was smeared on genital and anal areas on 2 aged people and on 3 new borne, suffering from itching conditions due to napkins use, All the cases were solved rapidly (Example 2.7).
2.8 A fluid emulsion containing 0.1% Tharchonanthus Camphoratus, L. essential oil, was smeared on bedsores on 3 patients. The recovery was rapid, the oedema and the irritation improved (Example 2.8).
2.9 A gel containing 0.05% Tharchonanthus Camphoratus, L. essential oil, was spread on 7 subjects with itching problems on the anal area due to emmorrhoids and rhagades. They recovered rapidly declaring a freshness and relief sensation (Example 2.9).
2.10 A mouthwash with 20% infusion, worked at cold state, obtained from Tharchonanthus Camphoratus, L. grinded fresh leaves, was used on 5 patients having irritated gums. In these cases a constant and periodic application brought a relief with a consequent decongestion of gums together with a freshness sensation and a good smelling breath (Example 2.10).
2.11 A toothpaste with 0.2% Tharchonanthus Camphoratus, L. essential oil, was used in 5 cases suffering from slightly irritated gums. A constant and periodic use of the formulation was of help in the guns decongestion. A freshness sensation and a good smelling breath was also noticed (Example 2.11).
2.12 An alcoholic gel containing 1% Tharchonanthus Camphoratus, L. essential oil, was used on legs suffering from phlebitis. A constant and periodic use was of help to solve the problem (Example 2.12)
 
2.13 An alcoholic gel containing 0.8% Tharchonanthus Camphoratus, L. essential oil was spread on same hematomaa 3 subjects. In both cases, a constant and periodic use was of help to improve the edema problem (Example 2.13).
Example 1.1
Mosquito- Repellent Spray lotion
Peg 40 Hydrogenated Castor Oil                           12.00%
Glycerine                                                                3.00%
Tharchonanthus Camphoratus, L. E.O.    0.30%
Preservatives (antibacterial/antimould)    q.s.
Demineralized water    q.s.    to 100.0%
Example 1.2
Mosquito–Repellent Alcoholic Solution for Environmental Purposes
Methlated alcohol type A            42.00%
Tharchonanthus Camphoratus, L. E.O.            0.20%
Sorbitan monoleate 20 (DE)            13.00%
Demineralized water    q.s.    to    100.0%
Example 2.1
 Anti - irritating soothing gel  
Carboxyvinyl polymer (Carbomer 940)            0.76%
Glycerine            3.00%
Sorbitan 20 (OE) monolaurate            0.20%
Tharchonanthus Camphoratus, L. E.O.             0.10%
Preservatives (antibacterial/antimould)    q.s.   0.10%
Thriethanolamine            0.50%
Demineralized water                               q.s. to 100.0%
Example 2.2
Anti - oedema gel           
Carboxyvinyl polymer (Carbomer 940)            0.76%
Glycerine                                                           3.00%

Sorbitan 20 (OE) monolaurate            0.40%
Tharchonanthus Camphoratus, L. E.O.
Preservatives (antibacterial/antimoud   q. s.        0.05%
Thriethanolamine            0.50%
Demineralized water                              q.s.    to    100.0%

Example 2.3    
Anti-edema gal
           Carboxyvinyl Polymer (Carboner 940)         0.50%
Glycerine            3.00%
Sorbitan 20 (0E) monolaurate            1.20%
Tharchonanthus Camphoratus, L.E.O.
Preservatives (antibacterial/antimould)    q.s.        0.30%
Triethanolamine            0.60%
Demineralized water    q.s.    to 100.0%
Example 2.4      
Anti-irritating, Soothing gel
Garboxyvinyl polymer (Carbomer 940)                        0.76%
Glycerine                                                                        3.00%
Sorbitan 20 COE) monolaurate                                      0.20%
Tharchonanthus Camphoratus, L. E.O.                          0.05%
Preservatives (antobacterial/antinould)                  g.s   
Thriethanolamine                                                          0.50%
Demineralized water                                          q.s. to 100.D%
Example 2.5       
Alcoholic solution for pimply skins    

Alcohol type G    50.00%
Glycerine    2.00%
Sorbitan 20 (OE) monolaurate    0.10%
Tharchonanthus canphoratus, L. E.O.    0.10%
Lavender E.O.    0.50%
Demineralizated water                                      q.s. to 100.0%
 
Example 2.6
Anti-irritating gel pre/after shave/ depletion
Carboxyvinyl polymer (carbomer 940)            0.70%
Glycerine            3.00%
Sorbitan 20 (E.O.) manolaurate            0.20%
Tharchonanthus Camphoratus, L. E.O.                         0.10%
Preservatives (antibacterial/antimould)    q.s
Triethanolamine            0.30%
Demineralizated water    q.s.    to    100.0%
Example 2.7    
Anti-irritating fluid emission
       Carboxyvinyl polymer (Carbomer 940)            0.40%
Glycerine            7.00%
Tharchonanthus Camphoratus, L.    E.O.            0.10%
Triethanolamine            0.25%
Acethylated Lanoline            1.00%
Dinethylated Lanoline            1.00%
Nyristil lactate            2.00%
Decyle cleats                                                               2.00%
Preservatives (antibacterial/antimould)    q.s.        2.00%
Dimineralizated water                                   q.s. to100.0%
Example 2.8    
Anti-irritating gel pre/after shave/ depletion
Carboxyvinyl polymer (Carbomer 940)            0.30%
Glycerine            7.00%
Tharchonanthus Camphoratus, L,    E.O.            0.10%
Allantoine            1.00%
Tocopheryl acetate            1.80%
Triethanolamine            0.40%
Acethilated lanoline                                                   1.00%
Dimethylpolysiloxane                                                3.00%
Myristil lactate            1.00%
Decyl oleate                                                               1.00%
Preservatives (antibacterial/antimould)    q.s.      
Demineralized water                                     q.s.    to100.0%

 
 Example 2.9
Anti-irritating soothing gel
Carboxyvinyl polymer (Carbomer 940)                   0.86%
Glycerine                                                                   3.00%
Sorbitan 20 (OE) monolaurate                                   0.20%
Tharchonanthus Camphoratus, L. E.O
Preservatives (antibacterial/antimould    q.s.       
Triethanolamlne            0.5%
Demineralized water                                         q.s. to100.0%
Example 2.10     
Idroalcoholic mouthwash            
Alcohol type E           20.00%
Glycerine            4.00%
Glycyrrhizicate            0.10%
Tharchonanthus Camphoratus, L.    Infusion
cold obtained stirring slowly grinned
Fresh leaves for 7 days in demin water            20.00%
Demineralized water                                 q.s. to 100.0%

Example 2.11     
Gum Toothpaste           
Potassium sorbate            0.20%
Glycerine            21.00%
Sorbitan 20 (0E) monolaurate            0.80%
Tharchonanthus Camphoratus, L, E.O.            0.20%
Carboxyvinyl cellulose medium density            1.50%
Dicalcium phosphate di-hydrate            50.00%
Sorbitol 70%            11.00%
Sodium laurilether sulfate            2.00%
Acesulfame Hoechst (sweetener)0.20%
Preservatives (antibacterial/antimould)    q.s.       
Demineralized water                                   q.s. to100.0%


 Example 2.12           
Antiedema alchoholic gel
Carboxyvinyl polymer (Carbomer 940)            0.05%
Alcoholic type D            30.00%
Glycerine            5.00%
Peg 40 Hydrogenated Castor Oil            4.00%
Tharchonanthus Camphoratus, L. E.O.             1.00%
Preservatives (antibacterial/antimould)    q.s.       
Trietbanolamine            0.30%
Demineralixated water                               q.s. to100.0%
Example 2.13  
Carboxyinyl polymer (Carbomer 940)            0.5%
Alcohol type D            30.0%
Glycerine            5.0%
Peg 40 Hydrogenerated Castor Oil            4.5%
Tharchonanthus Camphoratus, L. E.O.0.8%
Preservatives (attibacterial/antimould)    q.s.       
Triethanolamine            0.8%
Demineralizated water                          q.s. to 100.0%

Example of Mosquito fumigants           
A convenient quantity of dried leaves, belonging to a plant picked up by no more than 30 days, was grinned small.
30% of it was mixed up with arabic gum (10%), pit-coal (50%) potassium nitrate (10%, worked in water, spiral shaped and dried in a heater at 35 C deg for 24 hrs.
The same examples can be formulated with extracts and soaked in the proper concentration.
 
 CLAIMS
l. Use of Tharchonanthus Camphoratus, L. parts and its derivatives in insect-repelling, anti-irritating, soothing, anti-oedema, decongesting formulations and compositions.
2. Use of Tharchonanthus Camphoratus, L. extracts in insect-repelling, anti-irritating, soothing, antioedema, decongesting formulations.
3. Use of Tharchonanthus Camphoratus, L. essential oil in insect repelling, anti-irritating, soothing, anti-oedema, decongesting formulations and compositions.
4. Topical pharmaceutical compositions containing Tharchonanthus Camphoratus, L. as active ingredient.
5. Topical pharmaceutical compositions containing Tharchonanthus Camphoratus, L. as active ingredient in concentrations ranging from 0.05% and 10%.
6. Use of Tharchonanthus Camphoratus, L. parts, and its derivatives, in insect-repelling and insecticide formulations.
7. Use of Tharchonanthus Camphoratus, L. extracts in insect-repelling and insecticide activity.
8. Use of Tharchonanthus Camphoratus, L. essential oil in insect-repelling and insecticide formulations.
9. Insect-repelling and insecticide formulations containing from 5% to 95% of the parts according to claim 6.
10. Insect-repelling and insecticide formulations containing from 5% to 95% of the extracts according to claim 7.
11. Insect-repelling and insecticide formulations containing from 5% to 95% of essential oil according to claim 8.
 
ABSTRACT
USE OF THE THARCHONANTHUS CAPHORATUS, L.
Use of Tharchonanthus Camphoratus, L. parts and its derivatives in insect-repelling, anti-irritating, soothing, anti-oedema, decongesting formulations and compositions.

 

 

 

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