WO2007129136A1

WO2007129136A1 - Antimalarial properties of extracts of elaeis guineensis (oil palm) leaves

Info

Publication number: WO2007129136A1
Application number: PCT/IB2006/001693
Authority: WO
Inventors: Achidi Valentin Agon; Célestin Kinnoudo
Original assignee: Achidi Valentin Agon; Kinnoudo Celestin
Priority date: 2006-05-08
Filing date: 2006-05-08
Publication date: 2007-11-15

Abstract

The leaves of ELAEIS GUINEENSIS, a tropical African plant, French name oil palm, family Arecaceae in the large family of Palmae, harvested at an altitude of less than 300 meters, decocted for 45 minutes at 1000C give an antimalarial substance after dehydration (the extract of 100 kilograms of leaves gives 3077 grams, moisture level less than 10%). Any pharmaceutical industry can transform this extract into a drug (syrup, gel capsule, oral ampule, etc.). This substance taken orally at 1 g per 10 kg of body weight destroys Plasmodium, causal agent of malaria. The dosage frequency is at least four times the first day of treatment and at least 3 times the following days. The thick drop and the parasitic density constitute the medical exams for evaluation and confirmation of the efficacy of this extract.

Description

TITLE OF THE INVENTION

ANTIPALUDE PROPERTIES OF ELAEIS GUINEENSIS LEAF EXTRACTS (PALM OIL)

TECHNICAL FIELD: PHARMACY

We have discovered a plant whose extraction of the leaves by decoction at 100 ⁰ C is used to manufacture an antimalarial drug of immediate effectiveness as monotherapy on all types of plasmodium causative agent of malaria. The treatment offered by this medication is to destroy in a period of time plasmodiums in both the liver and blood in general. The natural origin of this active substance makes it a medication that eludes the possibility of developing resistance from all types of plasmodium.

The technique that we propose is a decoction at 100 ⁰ C which has been used for a long time in pharmacopoeia: the leaves are bathed in boiling water for 45 minutes and left for 5 hours.

PRIOR ART

In general, if a pharmaceutical industry is aware of the therapeutic virtues of a plant, the methods and techniques used for the extraction of the active ingredient or active substance vary according to the objectives. For example, by distillation it is possible to extract essential oils from a plant, it is possible to use water or alcohol to extract active ingredients according to whether the latter is soluble in water or in alcohol. In the context of the present invention, the process begins with the decoction and goes through dehydration to obtain an active substance convertible into a drug for human use.

SUMMARY OF THE INVENTION

We will expose the knowledge of the plant resource until obtaining the active ingredient convertible into medicine.

1-THE PLANT

1- 1-Scientific Name: Elaeis Guineensis

1- 2- Name in French: Palm oil

1- 3-Botanical family: arecaceae, of the large Palmaceae family, 1-4-Botanical source: tropical plant distributed in all coastal regions and mainly in West Africa.

1-5-Chemotype: 0 to 300 meters altitude in tropical region (Altitude at which the plant is very rich in this therapeutic and nontoxic property according to our research sites in West Africa within a radius of 250 kilometers from the side.)

1-6-Maturity: The young plant as an adult is useful at any time.

1- 7 - Useful part of the plant: The aerial part of the plant (the foliage) except the bare limbo. 1-8-Description of the plant: The oil palm has a very characteristic morphology: a single trunk, called stipe, without branches, surmounted by a pinnacle of pinnate leaves. The flowers are arranged in axillary clusters and an extensive mass of intertwined roots grows from the base of the trunk. The latter, like that of other monocots, does not show secondary growth and its diameter does not increase with the age of the tree, as in dicotyledons. The oil palm, native to western Africa but widely cultivated, gives a vegetable oil used in cooking and in the manufacture of margarine and soap.

1- 10-Large-scale Reproducibility: This plant is easily reproducible on a large scale from a nursery.

1- 11 -Toxicity: this medicinal plant is not toxic at all

2-HARVESTING AND STORAGE

The green leaves are good to be harvested. The yellows are to be discarded. The leaves should be stored for a maximum of 3 days. The storage is sheltered from the sun's rays on a dry ground, in a ventilated place and the thickness will not exceed 100 centimeters. Extraction can be done immediately after harvest, if possible.

3-EXTRACTION OF THE ACTIVE PRINCIPLE 3- 1 -METHODE: DECOCTION

3- 1-1-The weighing of the harvested leaves.

The total quantity to be extracted must be weighed and marked. This step is very important because the amount of the active substance depends on the total weight of the leaves decocted. During the weighing very large (more than two centimeters) and mostly bare limbs must be removed, otherwise they influence the total weight and distorts the total weight / quality ratio of the active ingredient.

3- 1- 2-Extraction itself

3- 1-2-1 -First phase: cooking The water must float the leaves and once the boiling is reached, it must last forty five (45) minutes, after this time the water is completed (because the loss of water due to evaporation) and the intensity of the heating must be maintained until a new boil after which the source of the heating must be cut and the leaves are left in the cooking water for 5 hours .

3- 1-2-1 -Second phase: leaf removal, rinsing and filtration

The leaves are removed, rinsed, the liquid from the rinsing is added to that of the extraction, and this liquid is used to make a new extraction and as many times as you want. We complete the water so that it floats on the leaves. The rinsing must be rigorously done to recover the maximum of the active substance. The liquid is filtered from the last extraction to dehydration.

3- 1-2-1 -Third phase: obtaining the active ingredient 3- 1-2-1-1-Method: dehydration

All the liquid obtained from the extraction obtained after filtration is subjected to heating for the purpose of complete dehydration, the aim is to obtain the active ingredient in its purest form. We do evaporate the liquid until you get a black PH substance located

95 between? and? and moisture content less than 10 percent (measured with a refractometer). Towards the end, the heating should be soft and controlled in such a way that the substance will not be charred. The substance solidifies without any special intervention after cooling if the dehydration is perfect.

100 Important clarification: 100 kilograms (100KG) of decocted leaves give 3077 grams of pure active substance or 1kg of pure extract is given by 32.5kg of leaves, and moisture content less than 10 per cent. This pure concentrate of the substance can be stored without further precautions and can be shipped anywhere in the world.

105 world without difficulty. If the moisture content is not respected the substance will mold and this affects the quality of the finished product.

In hot water this extract dissolves easily and can be exploited easily. NB: During dehydration the liquid tends to rise and

110 fill his container to overflow it. Monitoring is required to prevent this overflow which causes loss of molecules and decreases the amount of active ingredient that must be extracted from the total amount of leaves.

3-2-Important precision

115 The material used for decoction and dehydration must be stainless. 4 - THE TRANSFORMATION OF API-PALU IN FINISHED PRODUCT: MEDICINAL PRODUCT

Once the active ingredient in its pure form is obtained, any pharmaceutical industry can exploit it and turn it into a medicine in various forms: syrup, tablet, capsule, oral ampoule, etc.

5 - PHARMACOTHERAPEUTIC CLASS

5-1- MALARIA This antimalarial substance has an exceptional impact force on all types of plasmodium, causative agent of malaria, the effect is immediate if the daily dose is the size of the parasite density of the patient. It is an active ingredient that ranks among antimalarials and especially of natural origin.

5-1-1- CLINICAL STUDY: MEASURING ANTIPALUDEAN ACTIVITY OF LEAF EXTRACT OF ELAEIS GUINEENSIS, EXPERIMENTATION IN VIVO.

Taking before a meal: intestinal absorption is maximal and the number of plasmodium that disappears from the blood in less than three hours is at least 600 per cubic millimeter.

Taking after a meal: the absorption is minimal and the number of plasmodium that disappears from the blood in less than three hours is at most 300 per cubic millimeter.

The absorbed dose is the same in both cases: 5127 milligrams or 5.127 grams. The plasma life of the substance is approximately 2h 30.

5-1-2- DOSAGE AND PRECAUTION

The dosage depends on the parasite density, however the recommended minimum dose is 1 gram per dose per 10 kg of

145 body weight. The frequency is 4 times at least the first day and 3 times at least the following days. Preferably the intake should be before meals for better and faster intestinal absorption.

This substance is consumed without inconvenience by the pregnant or nursing woman and any child.

NB: In an area where the population is permanently exposed to mosquito bites, it is advisable to take at least one daily dose once a week for prevention. However, any access to malaria must be attacked immediately.

5-1-3- ADVERSE EFFECTS

155 No effects are reported on the sample of 5000 malarial patients.

5-1 -4-DURATION OF TREATMENT

This duration depends on the size of the parasitaemia, a parasite density less than 1500 plasmodiums / mm3 is canceled in a maximum of 160 days if the recommended minimum dose is respected. δ

5-1-5- DEVELOPMENT OF RESISTANCE OF PLASMODIUMS IS POSSIBLE?

Plasmodiums can not develop resistance against this active ingredient. This substance is one hundred percent natural

165 (not synthesized in the laboratory) permanently maintains its therapeutic property against plasmodiums. The natural origin of its chemical composition gives it this power, it is not a molecule which is directed against the parasites, but a set of molecules acting in harmony for this effectiveness on the

170 plasmodiums. Admittedly this composition varies in time and according to the seasons but remains effective on the different types of plasmodium.

5-1-6- MEDICAL EXAMINATIONS YES CONFIRM ANTIMALARIAL EFFECTIVENESS OF THIS SUBSTANCE.

5-1-6- 1- THE THICK DROP

It is the microscopic examination of a drop of blood which makes it possible to detect the presence of plasmodia in the blood.

5-1-6- 2- THE PARASITIC DENSITY

This is the medical examination that consists of evaluating the number of plasmodium per cubic millimeter of blood. It is the rapid procedure that makes it possible to determine the effectiveness and the force of striking of any antimalarial. This analysis can be repeated at any time of the treatment to ensure the progressive or total disappearance of plasmodiums.

Claims

1- The use of the leaf extract of the medicinal plant of the scientific name Elaeis Guineensis for the manufacture of a medicament for the treatment of malaria, the causative agent of which is plasmodium.

2- The medical evidence of the efficacy of this antimalarial is demonstrated by the gradual or even complete cancellation of the parasite density and the negativity of the thick drop.

3- The use of the medicinal plant of scientific name Elaeis Guineensis, name in French oil palm, according to claims 1 and 2 in the form of an extract of the leaves of said plant.

4. The use of the plant Elaeis Guineensis according to claim 3 wherein said extract of the leaves of said plant is obtained by the manufacturing procedure comprising at least: a- A decoction step of the aerial part of the medicinal plant Elaeis Guineensis, which decoction step comprises: 00 - A first boiling phase boiling preferably for 45 minutes,

A phase of adding a volume of water evaporated during the first cooking phase,

- A second baking phase until boiling and 05 - A rest phase without heating preferentially for 5 hours; b- A step of separation of the aerial part of the medicinal plant Elaeis Guineensis from the liquid resulting from the decoction step, which separation step comprises:

210 - Removal of the aerial part of the medicinal plant

Elaeis Guineensis of the liquid from the decoction step;

- A complete rinse of the aerial part of the Elaeis Guineensis plant with water so as to obtain a liquid which will be used for a new decoction or which will be filtered and subjected to

215 dehydration. c- A step of dehydration of said filtered liquid, which dehydration step comprises evaporation under heating of said filtered liquid so as to obtain said extract of Elaeis Guineensis, said evaporation under heating being maintained until the

220 color of said extract of Elaeis Guineensis is black and the moisture content of said extract of Elaeis Guineensis is less than 10%

5- Use of the medicinal plant of Elaeis Guineensis according to one of the preceding claims, wherein said medicament is in the form of syrup, tablet, capsule or drinkable ampoule ...

6. The use of the medicinal plant Elaeis Guineensis according to one of the preceding claims, in which said medicinal product must be taken at a rate of one gram per ten kilograms of body weight and this at least four times on the first day and three times on the first day. less the following days.