MXPA99009657A - Process for the obtaining of the formulation of a new product insecticide, bactericide, fungicide and antimicotico atóxi - Google Patents

Abstract

The extract of the plant Chenopodium graveolens Will (epazote de zorrillo) is a new medicine of origin that acts as an insecticide, bactericide, fungicide and antifungal for combatiracaros, one of them is in the pediculosis disease presented in mammals, formulated as shampoo. This is effective for the total elimination of Pediculus humanus variety capitis and Phithirus pubis in humans, treated during a period of seven days maximum, having a successful effect from the first daily application for five minutes, without presenting any side effects or toxic during treatment, or subsequent to it, which constitutes an innovation in relation to existing products for this purpose. The formulation was obtained based on a pharmaceutical process for a new drug in shampoo (shampoo) presentation, ensuring the null toxicity in mammals The formulation contains the active ingredient, quantified according to the pharmacopoeial method, finding a dose ten thousand times less than the dose lethal for the active substance of this plant Chenopodium graveolens Will (epazote de zorrillo). This represents a high margin of safety in the handling of the product, applied topically in mammals. In the tests carried out on fifty-six people parasitized by the aforementioned insects (mites), an efficacy of 100% was presented, in no case were there any symptoms corresponding to adverse effects (at the level of the central nervous system), or any going again. In addition to the shampoo (shampoo) has other formulations based on the pharmacopoeia of the United Mexican States such as: cream, ointment, liquid soap or paste, talc gel lotion and atomizer, among others, all of them topically. For its industrialization this formulation is of high quality, safety and low cost

Description

PROCESS FOR THE OBTAINING OF THE FORMULATION OF A NEW PRODUCT INSECTICIDA.BACTERICIDA.FUNGICIDA AND ANTIMICOTICO ATÓXICOS. TECHNICAL FIELD. BIOTECHNOLOGY BACKGROUND. In Mexico, as well as in many countries regardless of the level of development, pediculosis is recognized as a public health problem that affects not only humans but also animals, both in domestic and breeding bs. This problem has been addressed with the production of mainly chlorinated synthetic compounds, which, although used as an effective treatment, also represent a high cost, as well as an environmental risk, due to their toxicity, and damage to health. For years the most common treatment for this problem has been the use of lotion and shampoo containing lindane.EI lindane is a potent pesticide that permanently damages the central nervous system; demonstrated and widely documented The products containing this active principle are absorbed by human and animal skin, thus increasing its toxic potential. Lindane is insoluble in water, neurotoxic and is more active than DDT; High toxicity in plants, animals and humans, causing irreversible damage to health, including: seizures, epileptic seizures, mental retardation and cancer among others In addition, its toxicity and high manufacturing cost is not viable for mass treatments in the population. At present, these pediculicides are not biodegradable, accumulating in the environment, and in the individuals that use them, which suffer effects in the short and medium term, depending on the time of treatment.

Currently the existing formulations have a content of 1 gram of lindane for each 100 mL of content, in the different laboratories example of them: Laboratory: AUSTRAL. Argentina industry. Therapeutic Action: Pediculicide and Escabiocide. Uses: scalp and skin. Laboratory: LABINCA. HEXA DEFITAL LABINCA. Composition for every 100 mL. Contains 1 gram of Hndano. Therapeutic Action: Ectoparasiticide. Contradictions: In case of skin intolerance or allergic reaction, stop treatment. Laboratory: CLIKC NOW! Uses: Treatment in scabies (Sarcoptesscabiel) and pediculicide. Content: lindane Laboratory: BUTYL GAMMA-SCAB Composition: In each 100 mL contains: 1 gram of lindane. Therapeutic treatment and pediculicide. Laboratory: REEDCU, INC. ROAD Product: KWELL, E.U. Laboratories of Mexico, S.A. of C.V. Product: Herklin As well as other laboratories that use lindane.

EPAZOTE DE ZORRILLO. Chenopodium graveolens Willd HISTORY. In data for the Mexican medical matter of the late nineteenth century, the epazote of skunk Chenopodium graveolens WHtd is mentioned, as digestive, in emmenagogue, antihelmitic and taken in teiform infusion, as sudorific and diuretic. Finally Maximino Martinez relates that he is "Antiparasitic, antitussive, for side pain due to cold, frightful and eupéptico cause". The origins of the Mexican Herbalist go back to pre-Hispanic times, having as a testimony the codes and murals of Tepantitla, where the paintings of autochthonous medicinal species were recorded. In the 16th century, when the indigenous herbalist medical knowledge was collected and written, the works of this period are highlighted by the information Herbolaria Nativa in the Florentine Codex written by Fray Bemardino de Sahagún, dedicating the book XI to the theme of "Medicinal Herbs" , the work of Martín de la Cruz translated into Latin by Juan Badiano called, "Libellus de Medicinalibus Indorúm Herbis" that makes up the first herbal of Mexican medicinal flora and finally the work "Natural History of New Spain" by naturopathic doctor Francisco Hernández. This last work contains information on 3076 plants, some of them the sarsaparilla, the root of Jalapa and the root of Michoacán. From the conquest begins to bring Spanish medicinal species how: chamomile, basil and mint, were some of them. Just as the settlers of New Spain begin to relate to each other forming mestizos, so the herbalist experiences this process of mestizaje of union between medical knowledge - autochthonous and European doctors. The study of Mexican herbalism in the light of clinical research is observed, to a large extent, in the seventeenth century and experimental pharmacological research from the nineteenth century to date. It is important to point out that the current Mexican Herbalist is a hybrid, on the one hand the native plants and foreign plants are used and on the other hand we see the mestizo herbalism together with patent medicines or religious magical rites.

Currently the study of medicinal plants in Mexico, conducted at the IMSS, has allowed to have statistical data on the presence and distribution of such resources depending on the disease or symptoms for which they are used. The analysis of the results has allowed to establish "Basic Pictures" of medicinal plants of greater demand according to Traditional Medicine, and to know the diseases most frequently treated with these plants. Taken from the illustrative poster of the IMSS.

Biology of the Epazote de Zorrillo. Chenopodium graveolens Willd. It is an herb that reaches up to one meter in height, with a wounded stem; leaves oblong, petiolate, acuminate, I auco - greenish, up to nine cm long, leaves longer than hanchas. The flowers in numerous clusters, are divided, rigid peduncles; very small flowers, open chalice, with the stamens included; two short and filiform styles; seeds globose, fragrant, numerous fruits brown or black; It blooms from June to November and the plant is found throughout the year. USED PARTS: The whole plant. ODOR: Penetrating, and very persistent although it is dry. DISTRIBUTION: Wide throughout the country. Originally from Mexico, it lives in warm, semi-warm, semi-dry, temperate and dry climates, between 20 and 2900 meters above sea level. ETHNOBOTANY AND ANTHROPOLOGY. The main use attributed to this plant is for stomach pain. It is used in temascal baths after giving birth, to remove the cramps; or colics; in any of these cases there is a cooking of epazote. Another use that is often mentioned is for diarrhea, in addition to being useful for various digestive disorders and is also used as a deparasitizer against (Ascaris, onchocerciasis, amoeba and solitary), for dysentery, indigestion and bile, empacho and vomit , in cases of pain and cold in the stomach or after a courage where stomach pain is caused. It is also recommended in respiratory diseases such as cough and pneumonia, cold or flu, chest pain, back pain and chills. I have also reported its use for "fright", "fright", cramps and stomach pain, when it is ruled, accelerates labor, cleans the womb and solves some breastfeeding problems. As for its preparation, in some conditions it is used alone and in others accompanied by various plants, either in cooking or infusion. THERAPEUTIC ACTION. Epazote de zorrillo Chenopodium graveolens Willd. Used in the same way it favors the expulsion of intestinal worms and even tapeworms, and duodenal hookworm. Because of its irritant action should not be used for many days in a row, this disrupts the intestinal functions causing colic and diarrhea, its use is not recommended when there are liver diseases because it congests the gland, and the kidneys also, decreasing the urine secretion, that is why dangerous its use in these conditions. By its action on the ovaries and the womb should never be used during pregnancy, it can cause abortion, and neither in women who breastfeed, it decreases the milk secretion, and also the active ingredient passes into the milk causing indigestion in the child; when the lethal dose is exceeded. CHEMISTRY. The chemistry of the skunk epazote Chenopodium graveolens Willd has been little studied and in fact there is only one work done by Mexican researchers. It describes the presence, in the aerial parts, of the sesquiterpene cryptomerdiol, its alpha-acetoxylated derivative and the hydroxy-elemol; the flavonoids crisina, pinocembrina and pinostrobina; the steroids daucosterol, stigmaterol and the stigmas-2-in 3 beta-ol and the monoterpene acetate of geraniol. TOXICITY. The epazote is part of one of the genres most used by the population, with both food and medicinal purposes. Among the genus Chenopodium graveolens Willd, it is the best known from the chemical point of view since its use as a dspaiásitante has produced abundant scientific information. Thus, Chenopoduim graveolens Willd, has been determined ascaridol composed of corroborated antihelminthic properties, which has cited the development of essences based on this product. Its inclusion in the picture of toxic plants is due to the symptomatology observed by ascaridol overdose. Currently more than 1000 species, 250 genera and 80 plant families are cited With ability to release hydrocyanic acid (ianofórícas), when their tissues are donated for different reasons. The production of hydrocyanic acid is attributed to the presence in the plant of some of the 21 cyanogenic glycosides of hygroxinrtrils (cyanohydrins). However, the original glycoside has been identified in just over 100 species and, among which, the Chinopodium ssp. ACTIVE PRINCIPLES From the skunk epazote plant (Chenopodium graveolens WHId). This is obtained by steam distillation of the aerial parts, fresh, collected in the period of fructification of the epazote of the Family quenopodiaceas. CAUTION: The chenopodium oil may explode if heated. MAIN COMPOUND: Greater than or equal to 65 percent ascaridol. DESCRIPTION: Oily liquid whose color varies from pale yellow to yellow Orange and unpleasant smell. SOLUBILITY IN ALCOHOL: A part of the epazote essential oil dissolves in 8 parts of 70 percent alcohol. ROTATION SPECIFIES: MGA 0771. From 4 degrees to 8 degrees. REFRACTION INDEX: MGA 0741. Determined at 20 ° C is 1,474 to 1,479. DENSITY: MGA 0251. From 0.950 to 0.980.

HEAVY METALS: MGA 0561. Not more than 40 ppm. PHARMACOPEA ISOLATED COMPOUNDS. The presence of alkaloids, steroids, riterpenoids, saponins and flavonoids has been studied in this plant Chenopodium graveolens Willd.

DESCRIPTION. It is a product of vegetable origin, that both in its process and in its formulation for human, veterinary, agricultural and domestic use, low-cost technology is used, according to the needs of Mexico for its industrialization, and toxic solvents are not required. , guaranteeing a product of stability, security and efficiency; The product meets the requirements of the SECRETARIAT OF COMMERCE AND INDUSTRIAL PROMOTION, as well as the MEXICAN STANDARDS, for its Shampoo Formulation. It contains an active ingredient identified as ASCARIDOL, which is found in the foliage of the Chenopodium graveóles Will. This active ingredient has a broad biological activity documented mainly as: insecticide, bactericide, fungicide and non-toxic antifungal; however, its effectiveness as pediculicide, scabiosis (Sarcoprtesscabiel), herpes Zoster (zone), and other skin problems has not been demonstrated so far. Since it had not been formulated to be applied on both the scalp and the human body, to allow a total insecticidal action without an irritant or collateral effect on the skin of the affected people. This product is an innovation compared to any other product when valued in the human species. It has been proven to be 100% effective, without causing irritation, or skin lesions, or any adverse reaction, all this I have documented to ensure its use. Contrary to the previous technique based on lindane, we used 1 gram of the lindane-based principle, which is carcinogenic, neurotoxic and non-biodegradable. The proposed formulation contains .2% of the active ingredient ASCARIDOL. It is a thousand times smaller than the lethal dose allowed for this substance. Not presenting effects. Secondary, short, medium and long term, which could damage the health of the user.

It has been found that some plants are sources of insecticides, for example, the insecticide called Piretrum that is extracted from the chrysanthemum plant, and that is very effective, but too expensive to be used on a large scale. Among the most common synthetic pesticides are chlorinated hydrocarbons, including DDT, dieldrin, aldrin, heptachlor, chlordane, endrin and lindane. Among other classes of common pesticides are carbonates (for example, servin) and types of organophosphorus (such as parathion). DDT was the first of the widely used synthetic pesticides, at first it was used in an unregulated form for agricultural control, public health and domestic pests. After many years of use, it was observed that DDT killed insects indiscriminately and was toxic to fish, birds, pets and humans; In addition, it was discovered that many pests developed resistance to DDT, making it more difficult to control such insects. On the other hand, some of the insects that survive have acquired immunity through a deviation or genetic mutation, these insects transmit immunity to the next generation and so on. Chlorinated hydrocarbons are resistant to degradation and hydrolyzed slowly, for this reason they have been called persistent or "hard" pesticides. And carbonate, organophosphorus, or phosphorus - organic pesticides are rapidly degraded in the environment and are known as mild or light pesticides, but they are much more toxic to humans and, therefore, pose a greater danger to humans. who applies them The commercial name of DDT is dichloro-diphenyl-trichloro-ethane, technically it is a cream-colored flake. In an indiscriminate way, lindane is also used as an insecticide in bean, peas, tomato and other vegetable crops; dairy cattle, cattle, domestic use and in the treatment of seeds, causing serious problems to a greater degree than DDT. With the use of these insecticides can not continue for many years, in Mexico as in other countries the authorities have been expressing concern, and scientific processes are studied, within biology, chemistry, biotechnology and other areas dedicated to This study, seeking to solve this and other problems with methods that do not harm human health, animals, plants and the environment. HUMAN PEDICULOSIS. ETIOLOGY: Anopluros or sucking lice are small external parasites, apters that feed by sucking blood. Its main differences with biting lice (MALOFAGOS) consist of having sucking mouthparts and that the head is narrower than the torx. All anopluros are parasites of mammals. The man louse belongs to the family pediculidae, this family includes the only lice that attack the man, the louse crab or louse of the pubis and the lice of the head and body. The latter are considered to be varieties of the same species. Pediculus human variety capitis Head louse is gray in color, but tends to resemble the color of the breastplate of the host. On average, the male is 2-2.5 mm long and the female is 3-3.5 mm long. In comparison with the louse of pubes Ptherius pubis the louse of the head is more elongated and narrow; The head is smaller and narrower than the thorax and abdomen without lateral lobes, also the legs are all the same size, shape and finer nails. In these lice, the antennas have five segments. The life cycle of the head louse is similar to that of the Malophagus. The eggs are attached to the hair of the host, the female is able to lay 50 to 50 eggs and even some authors indicate that they can oviposit up to 300 eggs. The eggs hatch for about a week, and the nymphs develop quickly, there are three molts and in about one month the total life cycle from egg to adult is usually covered. The life cycle of the head lice (Pediculus humanus variety capitises), and those of the body (Phthir? S pubis), are similar, they are differentiated mainly by their habits. The head louse is usually located on it and its eggs are attached to the hair. The eggs to hatch take about one week and the life cycle from egg to adult takes about one month. The lice are fed at frequent intervals and taking food lasts a few minutes, they do it by introducing the jaw and sucking through the mouth, holding their nails kind of stinger, characteristic of these insects are their three pairs of legs, the debris that originate They are usually composed of hemoglobin with a large amount of nutrients. Sucking lice are parasites of mammals. The order contains several parasites of domestic animals and two of its species attack man; Sucking lice are very irritating pests and some important disease vectors. Lice transmit exanthematous typhus (Rickettsia prowazeki), trench fever (R. Quintana), as well as recurrent fever (Borelia recurrentis). Recurrent fever is the term generally applied to recurrent fevers caused by spirochetes transmitted by lice and ticks. INJURIES The infestation of lice produces pruritus in which later frequent scratching produces secondary infections, so that the lesions are aggravated and adenopathies often appear in the affected region. In advanced cases, there is a strong inflammatory reaction and scabs; they originate bulky cases, which require hospitalization. As a result, there are pigmented and marked spots on the skin, and sometimes alopecia. As a result of secondary infections such as interaction with spirochetes, which is characterized by recurrent febrile seizures lasting three to six days, followed by an afebrile period of similar duration, the maximum temperature is 40.6 ° C (105.1 ° F). With companions of myalgia, headache, arthralgia, abdominal pain and sensory disorders. The resolution of each febrile episode can be followed after a few hours of the reaction of Jarisch - Herxheimer, even without previous use of antibiotics. In such a way that the diagnosis with the first symptoms may not be very precise, causing other disorders in the individual. TRANSFER. The louse (Pediculus humanus variety capáis), is transmitted from person to person mainly, also through the promiscuous use of combs, brushes, caps and clothes in which they adhere very easily. EPIDEMIOLOGY In the tropics, they are practically not found; It is very important to point out that sweat, in a certain way, is a repellent for lice, it is much more common infestations in temperate zones, all over the world these insects are found as they usually seek to stay in clean places. TREATMENT AND CONTROL. Formerly the control for these insects to a certain extent, used the shaving of the hair, the application of oil or insecticides that were quite toxic for the host. At present in the treatment is used tiabentasol ointment (Eprofíí ointment), which is applied daily after bathing, for a week.

Powders or soaps with DDT are also used; These powders contain 10 percent insecticide. Likewise, the use of petrolatum for hair containing 2 percent DDT or 0.2 percent gamexane has been recommended. For the cleanliness of the clothes it is suggested to be boiled in a solution of DDT to the 5 percent of course, this clothes should be well washed after the treatment. Of the most novel and that is for sale to combat the louse (Pediculus humanus variety capitis), are lotions and shampoos based on lindane; These products have much more demand for the ease of their uses, they offer exterminate insects. These are sold in pharmacies, shopping centers, small businesses, are acquired are very easy and do not need a prescription. Unfortunately the risks that have affect health because, among other things, they produce certain injuries among them: nervous disorders, dermatitis, seizures, epileptic attacks, permanent mental retardation and cancer. This serious problem is faced by many countries and they have not been able to solve it in a less dangerous way, and other countries are already facing the problem, in such a way that they find clinical cases especially in infants who for the moment have no solution. Recently in the year (1997-1999) in the United States of North America was formed an Institution called Association of Pediculosis National (NPA), dedicated to provide all possible information on the damage caused by lindane.

The (NPA), wants the government of that country to make some decisions regarding products that contain lindane and that are of human use, considering that these are quite toxic. This association makes this problem public through the Internet, summarizing that every day they receive no less than 50 calls to request as much information as possible, after having applied the product containing lindane and some serious consequence was obtained. Service is also provided to all the public that requests it and provide information before it is too late. This information is based on documented cases of people who have already had an injury, as reported by the president of the National Pediculosis Association (NPA), Deborah Altschuler, which makes this service available through this means. This association also informs that the prescribing physician will be the one that indicates the dose, how to use it, and the patient will remain under continuous surveillance until the end of his treatment. The NPA (Association of the National Pediculosis), asked the FDA (Federal Food and Drug Administration (FDA), the latter is the one that regulates the use of lindane as a medicine, to be studied and report more about the use of this pesticide since recently, reports are received where there are children under the age of ten who have convulsions due to the use of lindane-containing products, specifying that there are a hundred cases in which they do not receive any kind of attention or advice. of the ZEILLO EPAZOTE (Chenopodium graveolens Willd), in the Herbarium of the MEXICAN INSTITUTE OF SOCIAL SECURITY Tests of toxicity of the product, as well as safety rank in accordance with the valuation of the active principle in the (Chenopodium graveolens Willd), in the UNIVERSIDAD AUTÓNOMA METROPOLITANA DE XOCHIMILCO As well as the identification of the insect and classification, in the AUTONOMOUS UNIVERSITY OF CHAPINGO.

DESCRIPTION. I. PROCESS OF OBTAINING 1. -Selection. The foliage of (Chenopodium graveolens Willd); obtained in a flask, it is washed twice by water, the water is removed, dried, and fragmented for later use. 2.- Disinfected. The plant (5 grams) is weighed for each liter of distilled water to make shampoo and disinfected for a period of no more than 10 minutes. It is rinsed with distilled water and placed in the container where it will drain to later use. 3.- Extraction. In a glass container put a volume of water at boiling temperature for 5 minutes, the plant is incorporated and left at boiling temperature for 10 minutes completely covered. It is cooled to room temperature. 4.- It is filtered twice first with a large pore filter, second with a totally small pore. The container containing the filtrate is covered immediately to avoid contamination. It can be refrigerated for 24 hrs, being completely covered.

II.- FORMULATION OF THE SHAMPOO It is prepared in the following way for (1 liter), obtaining approximately a total of 1200 mL of shampoo, using distilled water. 1.-DIETANOLAMIDE OF COCONUT FATTY ACIDS, is prepared at 2% in 1 liter of water at a temperature of 100 ° C is incorporated, slowly until its total integration, being at a temperature of 80 ° C minimum, LAURIL is added % SODIUM SULFATE ETHER with continuous stirring, incorporated COCOAMIDA PROPIL BETAÍNA, to 6% without stopping to shake, and before the temperature decreases more than 5 ° C. 2.-In another glass container is incorporated, DIESTERATO POLIETILENGLICOL, to 0.3% in 100 mL of distilled water of 60 ° C to 80 ° C, without exceeding this range until it dissolves, it is followed immediately to the extraction of Chenopodium graveolens willd. 3.-Heat 100 mL of distilled water in another container. At a temperature of 60 ° C to 80 ° C, PROPYLPARABEN is added to 0.5%, once dissolved, homogenized the formulation with continuous stirring. 4.- Finally, the chamomile fragrance for 0.2% shampoo is added.

The final point is marked by the slow decrease in foam presented by the integration process, thus concluding the formulation.

Claims (3)

CLAIMS. Claim of my property contained in the following: CLAIMS. 1. Process for obtaining a new insecticidal, bactericidal, fungicidal and non-toxic antifungal product of the new formulation comprising the following stages: Selection: The foliage of (Chenopodium graveolens Willd); obtained in fresh water is washed twice, the water is removed, dried, and fragmented for later use. Disinfected: The plant (5 grams) is weighed for each liter of distilled water to prepare shampoo, disinfected with NaCl for a period of no more than 10 minutes.
1. Rinse with distilled water and place in a container to drain. 2. Process for obtaining a new insecticidal, bactericidal, fugicidal, non-toxic antomichotic product, which comprises: Extraction, which is carried out in a container, a predetermined volume of water is set at boiling temperature for 5 minutes; Incorporate the plant and leave it at boiling temperature for 10 minutes covering the container. It is cooled to room temperature. 1.This process for the new formulation characterizing, the high temperature for its complete integration. Temperatures, of 100 ° C. This temperature was incorporated DIETANOLAMIDE OF COCONUT FATTY ACIDS, decreasing to 80 ° C minimum, LAURYL ETHER SULFATE
2. SODIO, with continuous agitations. The following incorporation COCOAMIDA PROPIL BETAÍNA, at not less than a temperature d 5 ° C. Temperatures of 60 ° C to 80 ° C without exceeding this range correspond to DIESTERATE POLYETHYLENGLYCOL and PROPYLPARABEN. Using these temperatures in that order the complete integration of the substance of Chenopudium graveolens willd, known as ASCARIDOL, is achieved.
3. 3. All this process allows a transformation into: cream, ointment, liquid soap, paste soap, laundry soap, lotion, gel, talc and atomizer among others, all of them topically, both in humans, veterinary and agricultural .