JPS627169B2 - - Google Patents

Description

[Detailed description of the invention]

The present invention relates to activated charcoal taken to detoxify by removing harmful substances within the digestive system. More specifically, when taking activated charcoal to remove and detoxify harmful substances that exist or are generated in the digestive system such as the stomach and intestines, the spherical shape does not show the constipation side effect that has traditionally been a problem. Concerning activated charcoal antidote. Activated charcoal has long been known to be effective in treating people with intestinal disorders, and is used for many purposes. i.e. dysentery, cholera,
Typhoid fever, bacterial infections such as food poisoning, indigestion,
It has been reported that taking activated charcoal has a therapeutic effect on intestinal tension, chronic gastritis, epilepsy, dizziness, yellowing disease, anthrax, etc. Furthermore, when ingesting drugs, poisonous substances, etc., activated charcoal can be taken as an emergency to achieve a detoxifying effect.
Activated charcoal is also effective in removing harmful substances in the digestive system that are produced due to abnormalities of consciousness associated with various other diseases. These effects are due to the fact that toxins, abnormal substances, and other triggers in the digestive system are adsorbed by activated carbon, and activated carbon itself is completely non-toxic to living organisms, retaining harmful substances and expelling them from the body. It is believed that this is because the Conventionally, powdered activated carbon has been used for all of these purposes, and even if this is mixed with water or taken as an appropriate tablet, it is unlocked in the body and becomes a powder.
Demonstrates the above-mentioned adsorption power. However, on the other hand, it exhibited constipation as a side effect, which was a major drawback. Constipation is not only extremely painful for the patient, but also requires mechanical removal as the patient does not have sufficient excretion power, as constipation is often used to treat various illnesses. Life-threatening cases may also occur. In view of this situation, as a result of various studies to solve the above-mentioned drawbacks, it was discovered that a specific spherical activated carbon can maintain its detoxification effect while at the same time not exhibiting constipation side effects, and the present invention has been achieved. i.e. diameter
0.05~2mm, surface area 500~ ^2000m2 /g, pore radius
Pore volume 0.05~1.0cc/in the range of 100~75000Å
g spherical activated carbon antidote. As mentioned above, the spherical activated carbon exhibiting the effects of the present invention has a particle size of 0.05 to 2 mm in diameter, preferably
It is 0.2~1.0mm. If it is less than 0.05 mm, even if it has a detoxifying effect, it is not effective enough to eliminate constipation side effects.
If it is 2 mm or more, it is not only difficult to administer, but also the desired detoxifying effect will not occur quickly. The shape is one important factor in obtaining the effects of the present invention, and it is necessary that the shape is substantially spherical. Surface area and pore volume are also important factors for the activated carbon of the present invention to simultaneously exhibit sufficient detoxification and removal of constipation side effects. That is, if the surface area and pore volume are too small, the adsorption force will be weak and a practically sufficient detoxification effect will not be obtained, and if they are too large, even if there is a detoxification effect, it will be accompanied by constipation. . Moreover, at the same time, the strength decreases, the shape collapses during or after administration, and powdering occurs, which is also considered to be a cause of constipation side effects. In this way, the surface area was measured using a commercially available surface area measuring device, and its range was 500-2000 m ² /g;
Preferably it is 700 to 1500 m ² /g. The pore volume was measured with a commercially available mercury intrusion porosimeter and ranged from 0.05 to 1.0 in the region of pore radius 100 to 75000 Å.
cc/g, preferably 0.1 to 0.8 cc/g. Raw materials used to produce activated carbon with such characteristics include sawdust, coal, coconut shells, pithus,
Any known raw materials such as organic synthetic polymers may be used.
In addition, as a method for producing the desired spherical activated carbon using these raw materials, the powdered raw materials are granulated into small spherical shapes with a binder such as pitch, and then heated and fired at 800 to 1000°C in an inert atmosphere. The pitch is carbonized in a molten state, and then activated at 900 to 1000°C in a steam atmosphere, or by the method shown in Japanese Patent Publication No. 50-18879, etc., to form small spherical particles in a molten state, and then oxidized to make them infusible. A known method can be used, such as a method in which the carbonized material is heated and calcined at 800 to 1000°C in an inert atmosphere to carbonize it, and then activated at 900 to 1000°C in a steam atmosphere. In particular, the latter method yields highly spherical, high-strength, smooth-surfaced spherical activated carbon, and is therefore suitable as the method for producing activated carbon of the present invention. Since the drug is to be taken in any case, it must of course be of sufficient purity for safety.
It must pass the purity test specified in the “Medicinal charcoal” section. The administration method may be the same known method as for ordinary activated charcoal. Although it is easiest to take the spherical activated carbon by suspending it in drinking water, the spherical activated carbon may also be taken as a composition with a pharmaceutically acceptable carrier and/or adjuvant. That is, it may be taken as an appropriately shaped tablet according to a conventional method. However, in this case, of course, the spherical activated carbon of the present invention must be unlocked into the original activated carbon particles within the body in order to exhibit its effectiveness. It may also be taken in a conventional cylindrical capsule according to a conventional method. The dosage varies depending on the severity of the disease, the need for emergency detoxification, etc., but is usually 0.5 to 10 g at a time, three times a day. Of course, this does not apply in cases of emergency. It was completely unexpected that such a specific spherical activated carbon would have a remarkable effect on eliminating constipation side effects while maintaining its detoxifying effect, and although the cause is still unknown, conventional powdered charcoal In contrast, spherical charcoal is a sphere with a smooth surface, which causes constipation.
It is also presumed that constipation does not occur due to the combined effects of not increasing the cohesive force of stool, adsorption of intestinal irritants to a small extent, and the spherical charcoal providing appropriate stimulation to the intestines. Hereinafter, the effects of the present invention will be explained with reference to Examples, but the scope of the present invention is not limited in any way. Example 1 (Production of activated carbon) Pitch obtained by high-temperature decomposition of crude oil (softening point
At 190℃, 750 parts of nitrobenzene insoluble matter (30% H/C element ratio 0.6) and 250 parts of naphthalene were placed in a stainless steel autoclave equipped with a stirrer, mixed and dissolved at 170℃, and "Gohsenol GH-17" (Nippon Gosei) was added to this. After adding 3,000 parts of a 0.5% aqueous solution (polyvinyl alcohol suspension agent) and vigorously stirring at 140°C for 30 minutes, cool to room temperature while stirring.
True spherical spherical particles were obtained. After separating most of the water, the particles were immersed in methanol in an amount 5 times the weight of the particles, shaken to extract and remove naphthalene, and then dried with ventilation.
Next, the temperature was raised to 300°C at 25°C/Hr while blowing air into a small rotary kiln to obtain infusible spherical particles. Next, the air supply is stopped, and the temperature is raised to 900°C while steam is supplied instead to carbonize, and the activation is continued by maintaining this temperature. Spherical activated carbon with high sphericity was obtained. By changing the activation time at 900°C and sieving the obtained activated carbon, spherical activated carbon samples shown in the following table were obtained. Regarding the adsorption capacity, we also investigated aminic substances such as indole and octopamine, which are presumed to be harmful substances produced in the body due to abnormalities in liver disease patients, and amino acids that accumulate abnormally.

[Table] [Acute toxicity test] An acute toxicity test using mice was conducted on the samples shown in Table 1. The results are shown below, and it was confirmed that the drug is extremely safe even when administered in large doses. Commercially available ICR-JCL female mice (body weight 22±1 g) were used as experimental animals. Samples 1 and 3 in Table 1 were kept spherical, and sample 2 was finely crushed and crushed using a stomach probe. Administered orally by force. LD ₅₀ was determined by the Litchfield-Wilcoxon method based on the determination of life and death one week later. The results are shown in Table 2. One week later, the animal was dissected, but no notable abnormal findings were found in the external appearance or internal organ observation, nor were any notable toxic symptoms observed.

[Table] Example 2 (Animal experiment) Using female Wistar rats weighing 130 to 140 g, 20% pentoparbital-Na was used.
It was orally administered as an aqueous solution at mg/Kg body weight. Immediately thereafter, the samples shown in Table 1 and medicated powdered charcoal were orally administered as a water suspension at a dose of 200 mg/Kg body weight. At the same time, a comparative test was conducted in which activated charcoal was not administered. Ten specimens were used for each activated carbon sample administration group and non-administration group. Next, the average value of the maximum concentration of pentobarbital-Na in the blood was calculated and the removal rate was calculated as a percentage of the concentration in the comparative test group.The results are shown in Table 3. A detoxifying effect was observed.

[Table] Next, 90 minutes after the administration of activated charcoal, these sample groups were killed by anesthesia, the gastrointestinal tract was removed, and the degree of intestinal transport of activated charcoal was compared. That is, the ratio of the transfer distance to the activated carbon reaching part to the total length from the cardia to the end of the rectum was determined as the transfer rate. The results are shown in Table 4. Compared to powdered charcoal, in the sample group using the activated carbon samples of the present invention shown in Table 1, the transport rate was clearly higher, indicating that the constipation effect seen with powdered charcoal was less. It has been shown.

[Table] Example 3 (Clinical case) 24- and 36-year-old women who were suffering from habitual constipation and facial pimples were given 3 g of medicated powdered charcoal at a time, 3 times a day.
When he took the drug between meals, his pimples slightly decreased from the third day onward, but his constipation became even worse and he complained of increased pain during defecation. Therefore, we stopped taking the medicated powdered charcoal, and then the 24-year-old woman received Sample-1 of the present invention shown in Table 1 of Example 1, and the 36-year-old woman received Sample-1 of the present invention shown in Table 1 of Example 1.
The subjects were given 3 g of spherical activated carbon in No. 3 at a time, three times a day between meals. In all cases, the pimples gradually decreased from the fourth day and almost disappeared after one week. It was also reported that constipation symptoms were significantly reduced and pain during defecation disappeared. Example 4 (Clinical case) A 42-year-old man who had repeated bouts of constipation and diarrhea about every week was given 5 g of medicated powdered charcoal three times a day between meals, and the pain of defecation during constipation increased. , complained of difficulty defecating. Therefore, we stopped taking the powdered charcoal and then took 5 g of spherical activated carbon of Sample 2 of the present invention shown in Example 1 and Table 1, three times a day between meals. Painless defecation was observed, and at the same time, most of the diarrhea symptoms disappeared. Example 5 The result of the Normo test that caused consciousness disorder was 10%.
Hereinafter, a patient (59 years old) with acute hepatitis symptoms who was in a coma was given 100 g of activated carbon of the present invention of Table 1 Sample-2 and 30 g of magnesium hydroxide per day using a nasal probe.
When we started injecting 60 g of lactulose in 6 doses, there was no noticeable deterioration trend. The next day, an exchange transfusion of 4,000 ml was performed and administration of activated charcoal/magnesium hydroxide/lactulose was continued, and an improvement in electroencephalogram was observed after 3 days of illness.
g, 30 g of lactylose was administered in 6 doses,
On the 5th hospital day, the patient's consciousness improved markedly and he was able to have a conversation. Then, on the 7th day of illness, the Normo test showed a marked improvement of 32%. There were no symptoms of constipation due to the administration of activated charcoal, and the condition was normal.

Claims (1)

[Claims] 1 Diameter 0.05~2.0mm, surface area 500~ ^2000m2 /g,
Pore volume 0.05~ in the pore radius range 100~75000Å
Oral antidote consisting of spherical activated carbon with the property of 1.0cc/g and no constipation side effects.