JPS6254282B2 - - Google Patents

Description

[Detailed description of the invention]

The present invention provides a herbicidal composition containing an emetic that can save lives by rapidly and reliably vomiting the herbicidal active ingredient compound, which is a toxic substance contained in the herbicide, when the herbicide is orally ingested. 1,1'-dimethyl-4,4'-bipyridylium salt-containing herbicide composition. In recent years, opportunities to handle toxic chemical substances have increased in factories, farms, homes, etc., and accidents in which these substances are accidentally or intentionally swallowed have become more common. Medical treatments for people who have ingested toxic substances include administration of antidotes, gastric lavage, hemodialysis, and expulsion from the body through vomiting, and the optimal treatment is taken depending on each case. However, the rapid diversification of toxic pest control agents and the relative delay in the development of antidotes,
Due to the spread of pest control agents such as herbicides in daily life and the expansion of knowledge about toxic substances, there is a need to improve first aid methods especially for suicide victims, and forced vomiting to expel toxic substances from the body has become necessary. It has come to be regarded as important. Conventionally, there are examples in which emetics are mixed with toxic substances in advance so that even if a suicidal person ingests a toxic substance, it is immediately expelled from the body through vomiting, such as in Swiss Patent No. 348003 and French Patent No. 2067846. It can be seen in the specification of the No. Further, JP-A-52-128222 and JP-A-53-101538 disclose toxic chemical compositions containing novel emetics. However, the emetics disclosed in the above-mentioned specifications and publications and the conventionally known emetics are not necessarily suitable for practical use for various reasons. That is, apomorphine, which has been conventionally often used for medical purposes, cannot be used for the above purpose because it is easily oxidized in the air.
Ipecaquanin syrup has an emetic effect, but it is dangerous because it requires a near-lethal dose to ensure the expulsion of the poisonous substance that has been ingested orally. Furthermore, although copper sulfate also has emetic properties, it is harmful to the human body even when ingested in amounts below the emetic threshold, and it is not desirable for such metal salts to be dispersed in the natural environment. The newly synthesized triazolo[1,5-a]pyrimidine derivative is an excellent emetic, but it is a central nervous system stimulant, and does not cause reflex vomiting immediately after oral ingestion, but is absorbed through the gastrointestinal tract. It has the disadvantage of being insufficiently effective against highly toxic substances. In other words, if there is no significant difference in the relative absorption rates of the emetics and toxic substances in the stomach and intestines, a considerable amount of the toxic substances will be absorbed into the stomach wall and the intestines before being excreted from the body through vomiting. It is taken into the bloodstream through the intestinal wall, significantly reducing the effectiveness of first aid. However, the present inventors recently conducted an acute toxicity test using beagle dogs on a 24% aqueous solution of 1,1'-dimethyl-4,4'-bipyridylium dichloride (paraquat), which is widely used as a herbicide.
It has been found that the survival rate is significantly increased by administering tripolyphosphate and/or pyrophosphate as an emetic, which takes a short time from oral ingestion to vomiting (hereinafter referred to as the incubation period). This led to the completion of the present invention. Currently, bipyridylium quaternary salts such as those mentioned above are supplied in large quantities on the market due to their strong herbicidal properties.
Since the toxicity of the drug was revealed, the number of people committing suicide using it has increased rapidly, and since no effective treatment has yet been found, it is extremely difficult for people to ingest more than a lethal dose of the drug and after a certain period of time has passed. It has a high mortality rate and has become a social problem. Orally ingested bipyridylium quaternary salt is absorbed relatively quickly mainly in the small intestine and taken into the blood, turning lung cells into fibrous forms and causing the death of living organisms. Bipyridylium quaternary salts taken orally are said to reach their maximum concentration in the blood in about 2 hours, and once bipyridylium quaternary salts are taken into the blood, it is impossible to remove them from the blood. It is said that When such toxic substances are ingested, the most effective medical treatment is to immediately induce vomiting to expel the toxic substances from the body. An emetic agent effective to achieve the above objectives must have the following properties: (1) The substance itself has low toxicity and is harmless to humans even if it is not excreted from the body through vomiting. (2) It is stable in the air and can withstand long-term storage. (3) Toxic substances. (4) Does not destroy the natural environment. (5) Can be supplied at low cost. The present inventors believe that tripolyphosphate and pyrophosphate are It was found that it has extremely good suitability for all of the requirements. Therefore, according to the present invention, 1 containing at least one of tripolyphosphate and pyrophosphate as an emetic and 1,1'-dimethyl-4,4'-bipyridylium salt as a herbicide active ingredient. , 1'-dimethyl-4,4'-bipyridylium salt is provided. The tripolyphosphate and pyrophosphate used in the present invention can be used in any salt form, but alkali metal salts such as sodium and potassium are preferred. The 1,1'-dimethyl-4,4'-bipyridylium salt used as the herbicide active ingredient in the composition of the present invention includes 1,1'-dimethyl-4,4'-bipyridylium dichloride (paraquat); There are corresponding dihalide salts such as dibromide salt. In addition to the above-mentioned emetic ingredients tripolyphosphate and/or pyrophosphate and the herbicide active ingredient, the composition of the present invention includes water, an organic solvent, a solvent or filler such as mineral powder, a surfactant, It may also contain inorganic salts such as common salt or other physiologically active substances. The composition of the present invention containing these emetic ingredients and herbicide active ingredients (toxic substances) is provided on the market in various forms depending on its usage. An aqueous solution is the most readily available form for those attempting suicide; however, since the emetic component is water-soluble, it is particularly effective as an aqueous solution. A notable example of this is the aqueous paraquat solution mentioned above. In addition, the composition of the present invention in the form of a tablet is also suitable for taking, but since tripolyphosphate and pyrophosphate can be easily powdered in a dry state, they should not be mixed into tablets. is also easy. Although it is easy to mix the powder of the emetic component into the composition of the present invention in powder form, when mixing it into an organic solution in which it will not be dissolved, it is preferable to make it into a fine powder and suspend it in the liquid. In general, the mixing ratio of toxic substances and emetic agents is such that when a poisoned person ingests a lethal amount or more of a toxic substance, it is rapidly and reliably expelled from the body through vomiting, and the amount of toxic substance retained in the body is reduced. It is necessary to ensure that the dose is below lethal. Both the lethal dose LD ₅₀ and the emetic threshold dose ED ₅₀ vary greatly depending on individual differences such as age, gender, and health status, and may
It is difficult to ensure 100% lifesaving. Here, the lethal dose is defined as
This is the amount that will cause 50% death, and the vomiting threshold amount is the amount that will cause vomiting in 50% of living organisms who ingest this amount. The mixed composition of the toxic substance and the emetic is designed to contain equivalent amounts of the lethal dose of the toxic substance and the vomiting threshold amount of the emetic, that is, the mixing ratio is such that vomiting occurs exactly when the lethal dose is ingested. When ingesting the above-mentioned composition containing an emetic in a certain amount, one must be prepared for a considerably high mortality rate depending on individual differences. Therefore, it is clear that it is necessary to contain at least the above-mentioned equivalents of tripolyphosphate and pyrophosphate, and preferably at least twice the equivalent, and if circumstances permit, 3 to 10 times the equivalent to further improve the composition. Can cause vomiting reliably and rapidly. When the herbicide composition according to the present invention is ingested, the amount of vomiting is on average about 75% of the ingested amount, and a corresponding amount of the ingested toxic bipyridylium salt is excreted from the body. Furthermore, when a person who intends to commit suicide takes the composition of the present invention in the form of an aqueous solution, the person ingests an average volume of about 50 ml of the liquid, and rarely ingests more than 300 ml. Therefore, in order for the toxic bipyridylium salt that is not excreted from the body and remains in the body even through vomiting to be less than a lethal dose, the concentration of the toxic bipyridylium salt must be determined by adjusting the content of the bipyridylium salt in 12 ml of the composition. must be kept below a lethal dose. For example, in the case of the herbicide paraquat, the lethal dose of 1,1'-dimethyl-4,4'-bipyridylium salt, which is a toxic substance, is said to be about 4 g for an adult, so the concentration in the composition of the present invention is about 33% by weight or less. It is preferable to For example, since the emetic threshold amount of sodium tripolyphosphate is about 1500 mg, it is desirable that the concentration of sodium tripolyphosphate in the paraquat composition be at least 3% by weight, more preferably 6% by weight or more. Further, since the emesis threshold amount of potassium pyrophosphate is about 900 mg, it is desirable that the concentration of potassium pyrophosphate in the composition is at least 1.8% by weight, more preferably 3.6% by weight or more. Furthermore, in the case of paraquat aqueous solution, 1,
Since 1'-dimethyl-4,4'-bipyridylium salt decomposes in alkalinity, it is necessary to adjust the pH to 7 or less by adding acid. Even if the composition according to the present invention is ingested by mistake or for the purpose of suicide or homicide, most of the ingested toxic substances will be excreted from the body through vomiting after an extremely short incubation period, so the ingestor will not be able to survive. less likely to lose. Furthermore, tripolyphosphate and pyrophosphate have extremely low toxicity, and even if they are ingested below the vomiting threshold amount, or if they are not completely excreted from the body through vomiting, there is no risk of harm to the health of the person ingesting them. do not have. Furthermore, tripolyphosphate and pyrophosphate are stable chemical substances, and even if they are left in the air in the presence of many toxic substances, they undergo almost no chemical changes. Furthermore, when sprayed in the natural environment together with pesticides, tripolyphosphate and pyrophosphate have extremely low toxicity to living organisms.
Since it is easily metabolized, there is little risk of destroying the environment. Next, the effectiveness of the composition of the present invention will be explained using examples. Example 1 (Liquid) 5 g of potassium pyrophosphate (TKPP) as an emetic was dissolved in 50 g of water, and then dissolved in a 6N aqueous hydrochloric acid solution.
Adjust the pH to 7 and add 1,1'-dimethyl- to this solution.
Add 24 g of 4,4'-bipyridylium dichloride (paraquat) and further add 10 g of Tween 20 (surfactant). Finally, water was added appropriately to make the total weight 100 g. This formulation example is effective as an emetic herbicide composition. Example 2 (Emetic effect test) The following test was conducted to confirm the emetic effect of the emetic herbicide composition according to the present invention. That is, 1,1'-dimethyl-4,4'- containing potassium pyrophosphate (TKPP) and sodium tripolyphosphate (STP) according to Example 1.
An aqueous solution of bipyridylium dichloride (paraquat) and an aqueous paraquat solution containing no emetic were prepared and administered to test animals (beagle dogs) through gastric catheterization to determine the presence or absence of vomiting, the time until the onset of vomiting, and the following. Survival was confirmed after a week. The test results are shown in Table 1.

[Table] From the above results, it is clear that the composition of the present invention has a remarkable life-saving effect, because the vomiting time is extremely short and the toxic bipyridylium salt is absorbed before it is absorbed. This is thought to be caused by causing vomiting. Example 3 (Herbicidal effect test) It was confirmed that the composition of the present invention, which has excellent emetic properties as shown in Example 2 above, is comparable in herbicidal effect to a composition that does not contain an emetic. Therefore, the following field tests were conducted. That is, each herbicide composition used in Example 2 was applied to one field where crabgrass was evenly growing.
The area was divided into 2 m ² plots and sprayed, and the test was conducted in triplicate. The test results were compared by cutting the weeds 10 days later and comparing the air-dried weight of the remaining grass. In addition, the expression of herbicidal effect and the results of visual observation after 5 days are also listed. The results are shown in Table 2. The results of visual observation were judged based on the following criteria. ×……Weed killing rate 90% or more compared to untreated area×～〓…… 〃 〃 89~75% 〓…… 〃 〃 74~50% +……Weed killing rate compared to untreated area 49~25% ±…… 〃 〃 24% or less−…… 〃 〃 0%

[Table] From the results below, it is clear that the composition of the present invention exhibits its effect without reducing the herbicidal activity of the herbicide active ingredient.

Claims (1)

[Scope of Claims] 1. Containing at least one of tripolyphosphate and pyrophosphate as an emetic and 1,1'-dimethyl-4,4'-bipyridylium salt as a herbicide active ingredient. 1′-dimethyl-4,
Herbicide composition containing 4′-bipyridylium salt. 2. The composition according to claim 1, wherein the tripolyphosphate and/or pyrophosphate is contained in a proportion greater than the equivalent of the emetic threshold amount of the tripolyphosphate and pyrophosphate and the lethal dose of the bipyridylium salt. . 3. The composition according to claim 1, wherein the tripolyphosphate and pyrophosphate are alkali metal salts of tripolyphosphate and pyrophosphate. 4. The composition containing the emetic agent contains 33% by weight or less of 1,1'-dimethyl-4,4'-bipyridylium salt;
The composition according to claim 1, which is an aqueous solution having a pH of 7 or less and containing 3% by weight or more of tripolyphosphate. 5. The composition containing the emetic agent contains 33% by weight or less of 1,1'-dimethyl-4,4'-bipyridylium salt;
The composition according to claim 1, which is an aqueous solution containing 1.8% by weight or more of pyrophosphate and having a pH of 7 or less.