JPS627169B2 - - Google Patents
Info
- Publication number
- JPS627169B2 JPS627169B2 JP52156546A JP15654677A JPS627169B2 JP S627169 B2 JPS627169 B2 JP S627169B2 JP 52156546 A JP52156546 A JP 52156546A JP 15654677 A JP15654677 A JP 15654677A JP S627169 B2 JPS627169 B2 JP S627169B2
- Authority
- JP
- Japan
- Prior art keywords
- activated carbon
- spherical
- constipation
- charcoal
- day
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired
Links
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 79
- 230000000694 effects Effects 0.000 claims description 22
- 206010010774 Constipation Diseases 0.000 claims description 20
- 239000011148 porous material Substances 0.000 claims description 8
- 239000000729 antidote Substances 0.000 claims description 3
- 239000003610 charcoal Substances 0.000 description 11
- 239000000126 substance Substances 0.000 description 8
- 238000000034 method Methods 0.000 description 7
- 239000000523 sample Substances 0.000 description 7
- 238000001784 detoxification Methods 0.000 description 5
- UFWIBTONFRDIAS-UHFFFAOYSA-N Naphthalene Chemical compound C1=CC=CC2=CC=CC=C21 UFWIBTONFRDIAS-UHFFFAOYSA-N 0.000 description 4
- 230000013872 defecation Effects 0.000 description 4
- 210000002249 digestive system Anatomy 0.000 description 4
- 229940079593 drug Drugs 0.000 description 4
- 239000003814 drug Substances 0.000 description 4
- 235000012054 meals Nutrition 0.000 description 4
- 239000002245 particle Substances 0.000 description 4
- 239000002994 raw material Substances 0.000 description 4
- 238000001179 sorption measurement Methods 0.000 description 4
- 208000024891 symptom Diseases 0.000 description 4
- 238000012360 testing method Methods 0.000 description 4
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- 206010000496 acne Diseases 0.000 description 3
- 230000037396 body weight Effects 0.000 description 3
- 201000010099 disease Diseases 0.000 description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
- 230000000968 intestinal effect Effects 0.000 description 3
- 238000004519 manufacturing process Methods 0.000 description 3
- 230000036407 pain Effects 0.000 description 3
- 239000012798 spherical particle Substances 0.000 description 3
- 206010012735 Diarrhoea Diseases 0.000 description 2
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical compound C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- 241000699670 Mus sp. Species 0.000 description 2
- 230000002159 abnormal effect Effects 0.000 description 2
- 230000005856 abnormality Effects 0.000 description 2
- 230000004913 activation Effects 0.000 description 2
- 231100000215 acute (single dose) toxicity testing Toxicity 0.000 description 2
- 238000011047 acute toxicity test Methods 0.000 description 2
- 239000007864 aqueous solution Substances 0.000 description 2
- 230000000052 comparative effect Effects 0.000 description 2
- 238000007796 conventional method Methods 0.000 description 2
- 230000003247 decreasing effect Effects 0.000 description 2
- 230000001747 exhibiting effect Effects 0.000 description 2
- 210000000936 intestine Anatomy 0.000 description 2
- JCQLYHFGKNRPGE-FCVZTGTOSA-N lactulose Chemical compound OC[C@H]1O[C@](O)(CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H](O)[C@@H](CO)O1 JCQLYHFGKNRPGE-FCVZTGTOSA-N 0.000 description 2
- 229960000511 lactulose Drugs 0.000 description 2
- PFCRQPBOOFTZGQ-UHFFFAOYSA-N lactulose keto form Natural products OCC(=O)C(O)C(C(O)CO)OC1OC(CO)C(O)C(O)C1O PFCRQPBOOFTZGQ-UHFFFAOYSA-N 0.000 description 2
- LQNUZADURLCDLV-UHFFFAOYSA-N nitrobenzene Chemical compound [O-][N+](=O)C1=CC=CC=C1 LQNUZADURLCDLV-UHFFFAOYSA-N 0.000 description 2
- 238000003756 stirring Methods 0.000 description 2
- 210000002784 stomach Anatomy 0.000 description 2
- 238000012546 transfer Methods 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- QHGUCRYDKWKLMG-QMMMGPOBSA-N (R)-octopamine Chemical compound NC[C@H](O)C1=CC=C(O)C=C1 QHGUCRYDKWKLMG-QMMMGPOBSA-N 0.000 description 1
- 206010002091 Anaesthesia Diseases 0.000 description 1
- 241000193738 Bacillus anthracis Species 0.000 description 1
- 208000035143 Bacterial infection Diseases 0.000 description 1
- 206010008631 Cholera Diseases 0.000 description 1
- 235000013162 Cocos nucifera Nutrition 0.000 description 1
- 244000060011 Cocos nucifera Species 0.000 description 1
- 206010010071 Coma Diseases 0.000 description 1
- 208000022540 Consciousness disease Diseases 0.000 description 1
- IMROMDMJAWUWLK-UHFFFAOYSA-N Ethenol Chemical compound OC=C IMROMDMJAWUWLK-UHFFFAOYSA-N 0.000 description 1
- 206010016952 Food poisoning Diseases 0.000 description 1
- 208000019331 Foodborne disease Diseases 0.000 description 1
- 208000007882 Gastritis Diseases 0.000 description 1
- QHGUCRYDKWKLMG-MRVPVSSYSA-N Octopamine Natural products NC[C@@H](O)C1=CC=C(O)C=C1 QHGUCRYDKWKLMG-MRVPVSSYSA-N 0.000 description 1
- 239000004372 Polyvinyl alcohol Substances 0.000 description 1
- 241000700157 Rattus norvegicus Species 0.000 description 1
- 206010070863 Toxicity to various agents Diseases 0.000 description 1
- 208000037386 Typhoid Diseases 0.000 description 1
- 229940082079 activated charcoal / magnesium hydroxide Drugs 0.000 description 1
- 231100000354 acute hepatitis Toxicity 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 150000001413 amino acids Chemical class 0.000 description 1
- 230000037005 anaesthesia Effects 0.000 description 1
- 238000010171 animal model Methods 0.000 description 1
- 239000007900 aqueous suspension Substances 0.000 description 1
- 208000022362 bacterial infectious disease Diseases 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 238000007664 blowing Methods 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 239000005539 carbonized material Substances 0.000 description 1
- 210000002318 cardia Anatomy 0.000 description 1
- 208000023652 chronic gastritis Diseases 0.000 description 1
- 239000003245 coal Substances 0.000 description 1
- 230000002301 combined effect Effects 0.000 description 1
- 239000010779 crude oil Substances 0.000 description 1
- 238000000354 decomposition reaction Methods 0.000 description 1
- 230000007423 decrease Effects 0.000 description 1
- 230000006866 deterioration Effects 0.000 description 1
- 208000002173 dizziness Diseases 0.000 description 1
- 239000003651 drinking water Substances 0.000 description 1
- 235000020188 drinking water Nutrition 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 208000001848 dysentery Diseases 0.000 description 1
- 201000006549 dyspepsia Diseases 0.000 description 1
- 206010015037 epilepsy Diseases 0.000 description 1
- -1 etc. Substances 0.000 description 1
- 238000002146 exchange transfusion Methods 0.000 description 1
- 230000029142 excretion Effects 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 230000001815 facial effect Effects 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 238000000227 grinding Methods 0.000 description 1
- 230000002650 habitual effect Effects 0.000 description 1
- 208000006454 hepatitis Diseases 0.000 description 1
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 description 1
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 description 1
- 208000028774 intestinal disease Diseases 0.000 description 1
- 239000002085 irritant Substances 0.000 description 1
- 231100000021 irritant Toxicity 0.000 description 1
- 208000019423 liver disease Diseases 0.000 description 1
- VTHJTEIRLNZDEV-UHFFFAOYSA-L magnesium dihydroxide Chemical compound [OH-].[OH-].[Mg+2] VTHJTEIRLNZDEV-UHFFFAOYSA-L 0.000 description 1
- 229910001862 magnesium hydroxide Inorganic materials 0.000 description 1
- 239000000347 magnesium hydroxide Substances 0.000 description 1
- 229940105082 medicinal charcoal Drugs 0.000 description 1
- QSHDDOUJBYECFT-UHFFFAOYSA-N mercury Chemical compound [Hg] QSHDDOUJBYECFT-UHFFFAOYSA-N 0.000 description 1
- 229910052753 mercury Inorganic materials 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 231100000252 nontoxic Toxicity 0.000 description 1
- 230000003000 nontoxic effect Effects 0.000 description 1
- 229960001576 octopamine Drugs 0.000 description 1
- 231100000614 poison Toxicity 0.000 description 1
- 230000007096 poisonous effect Effects 0.000 description 1
- 229920002451 polyvinyl alcohol Polymers 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 238000013094 purity test Methods 0.000 description 1
- 210000000664 rectum Anatomy 0.000 description 1
- 238000007873 sieving Methods 0.000 description 1
- 229910001220 stainless steel Inorganic materials 0.000 description 1
- 239000010935 stainless steel Substances 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- 239000000375 suspending agent Substances 0.000 description 1
- 229920001059 synthetic polymer Polymers 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 231100000765 toxin Toxicity 0.000 description 1
- 239000003053 toxin Substances 0.000 description 1
- 108700012359 toxins Proteins 0.000 description 1
- 201000008297 typhoid fever Diseases 0.000 description 1
- 238000009423 ventilation Methods 0.000 description 1
- 210000001835 viscera Anatomy 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
- 238000004383 yellowing Methods 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
- A61K33/44—Elemental carbon, e.g. charcoal, carbon black
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P39/00—General protective or antinoxious agents
- A61P39/02—Antidotes
Description
本発明は消化器系内の有害物質を除去すること
によつて解毒するために服用する活性炭に関す
る。更に詳しくは、胃、腸等の消化器系内に存在
する、又は生成する有害物質を活性炭の服用によ
つて除去して解毒するに際して、従来から問題と
されていた便秘性副作用を示さない球形活性炭解
毒剤に関する。
活性炭は、これを服用することにより腸疾患者
の治療に効果的であることが古くから知られ、多
くの目的に用いられている。即ち赤痢、コレラ、
腸チフス、食中毒等の細菌性感染症、消化不良、
腸の張り、慢性胃炎、又てんかん、めまい、萎黄
病、炭疽病等に対して、活性炭を服用することに
より治療効果のあることが報告されている。更に
薬物、毒物等の摂取に際しても救急的に活性炭を
服用することにより、解毒効果が得られている。
その他各種の疾患に伴なう代識異常により生成す
る消化器系内の有害物質の除去にも活性炭の服用
は有効である。これ等の効果は、消化器系内の毒
素、異常代識物又はこれ等の誘因物質が活性炭に
より吸着され、活性炭自体は生体に対して全く毒
性がなく、有害物を保持して体外に排出されるた
めと考えられている。
従来、この用途には全て粉末活性炭が用いら
れ、これを水に混ぜて服用するか、適当な錠剤と
して服用しても体内で解錠され粉末状となつて、
上記吸着力を発現する。しかし、一方では副作用
として便秘現象を示し、これが大きな欠点であつ
た。特に各種疾患に際して服用するものであるか
ら、体力が消耗している場合が多くこの時の便秘
は患者にとつて著しい苦痛であるのみならず、充
分な***力がなく機械的に除去しなければ生命に
関る場合も生じ得る。
この様な状況に鑑み、前記欠点を解決すべく各
種検討の結果、特定の球形活性炭では解毒作用は
維持しつつ同時に便秘性副作用は示さないことを
見出し、本発明に到達したものである。即ち直径
0.05〜２mm、表面積500〜2000m2／ｇ、細孔半径
100〜75000Åの範囲での細孔容積0.05〜1.0c.c.／
ｇの球形活性炭解毒剤である。
本発明の効果を示す球形活性炭としては、上述
の如く粒径は直径として0.05〜２mm、好ましくは
0.2〜1.0mmである。0.05mm以下では解毒作用はあ
つても便秘性副作用の除去に充分効果的でなく、
２mm以上になると、服用し難いだけでなく、目的
とする解毒効果も迅速に発現しない。
形状は本発明の効果を得る上でのひとつの重要
な因子であり、実質的に球形であることが必要で
ある。
表面積及び細孔容積も本発明の活性炭において
充分な解毒作用と便秘性副作用の除去という効果
を同時に発現させる上で重要な要因となる。即
ち、表面積、細孔容積が小さすぎると、吸着力が
弱くなり実用上充分な解毒効果は得られず、又こ
れ等が大きすぎると解毒作用はあつても便秘現象
を伴なうことになる。又、同時に強度が低下し
て、服用時又は服用後に形状が崩れ、粉化を伴な
うことも便秘性副作用を生じる原因と考えられ
る。
この様にして表面積は市販の表面積測定装置を
用いて測定され、その範囲は500〜2000m2／ｇ、
好ましくは700〜1500m2／ｇである。細孔容積は
市販の水銀圧入ポロシメーターで測定され、その
範囲は細孔半径100〜75000Åの領域で0.05〜1.0
c.c.／ｇ、好ましくは0.1〜0.8c.c.／ｇである。
この様な特性を有する活性炭の製造に用いる原
料としては、オガ屑、石炭、ヤシ殻、ピツチ類、
有機合成高分子等の公知の原料の何れでもよい。
又これ等の原料を用いて、所期の球形活性炭を製
造する方法としては、粉末原料をピツチ等のバイ
ンダーで小粒球形に造粒し、次いで不活性雰囲気
中で800〜1000℃に加熱焼成して炭化し、次い
で、水蒸気雰囲気中で900〜1000℃で賦活する方
法、或は特公昭50−18879等に示されている方法
により、ピツチ類を熔融状態で小粒球形とし、次
いで酸化により不融性とした後、不活性雰囲気中
で800〜1000℃で加熱焼成して炭化し、次いで水
蒸気雰囲気中で900〜1000℃で賦活する方法等の
公知の方法を用いることができる。特に後者の方
法では真球性の高い、高強度の表面の滑らかな球
形活性炭が得られるので、本発明の活性炭の製造
方法として好適である。
何れの場合においても服用するものであるか
ら、安全上充分な純度のものでなければならない
のは勿論であつて例えば、日本薬局法第九改正、
“薬用炭”の項に示されている純度試験に適合す
るものでなければならない。
服用方法は、通常の活性炭と同様の公知の方法
でよい。飲料水に本球形活性炭を懸濁させて服用
するのが最も簡単であるが、本球形活性炭を医薬
上許容される担体及び／又は補助剤と組成物とし
て服用しても良い。即ち常法に従い適当な形の錠
剤として服用してもよい。但し、この場合は勿論
本発明の球形活性炭としての効果を示す様、体内
で元の活性炭粒子に解錠される必要がある。又常
法に従い通常の円筒形カプセルに包含させて服用
してもよい。
服用量は、疾患の程度、緊急解毒の必要性等に
よつても異なるが通常１回0.5〜10ｇ、１日３回
適度である。又、緊急を要する場合は勿論この限
りでない。
この様な特定の球形活性炭が解毒作用を維持し
つつも便秘性副作用の除去に著しい効果を示すこ
とは全く予期し得なかつたことで、未だその原因
は明らかでないが、従来の粉末炭では腸の刺激物
質も吸着し、腸運動を弱めると同時に便による混
合され便の凝集力を増して便秘をきたすのに対
し、球形炭では表面が滑らかな球体であるため、
便の凝集力上昇効果をもたらさないと同時に、腸
の刺激物質の吸着が少なく、又、球形炭が腸に適
度な刺激を与える等の複合効果により便秘をきた
さないとも推定される。
以下、実施例によつて本発明の効果を説明する
が、何等本発明の範囲を限定するものではない。
実施例 １
（活性炭の製造）
原油の高温分解により得られたピツチ（軟化点
190℃、ニトロベンゼン不溶分30％、Ｈ／Ｃ元素
比0.6）750部、ナフタレン250部を撹拌機付ステ
ンレス製オートクレーブに仕込み、170℃で混合
溶解し、これに「ゴーセノールGH−17」（日本合
成社製ポリビニルアルコール系懸濁剤）0.5％水
溶液3000部を加えて140℃で30分間激しく撹拌し
た後、撹拌下に室温まで冷却し、粒径0.1〜２mm
の真球状の球形粒子を得た。大部分の水を別し
た後、粒子重量の５倍量のメタノールに浸漬、振
盪してナフタレンを抽出除去した後通風乾燥し、
次いで、小型ロータリー・キルン中で空気を送入
しながら25℃／Hrで300℃まで昇温して不融性の
球形粒子を得た。次いで空気送入を停止し、代り
に水蒸気を送入しながら900℃まで昇温すること
によつて炭化し、更にこの温度に保つことによつ
て賦活を進めて、粒径0.07〜1.8mmの真球性の高
い球形活性炭を得た。900℃での賦活時間を変
え、又得られた活性炭を篩別することにより次の
表に示す球形活性炭試料を得た。
尚、吸着能については肝疾患者の代識異常で体
内に生成する有害物質として推定されているイン
ドール、オクトパミン等のアミン性物質、異常蓄
積するアミノ酸類についても調べた。
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.
【表】
〔急性毒性試験〕
第１表に示した試料について、マウスを用いた
急性毒性試験を実施した。結果は以下に示す通り
であり、多量に投与しても極めて安全性の高いも
のであることを確認した。
実験動物として、市販ICR−JCL系雌マウス
（体重22±１ｇ）を用い、第１表の試料−１、及
び３は球形のまま、又試料−２は細かく破砕し
て、胃ゾンデを用いて強制経口投与した。１週間
後の生死の判定により、Litchfield−Wilcoxon法
からLD50を求めた。結果を第２表に示す。１週
間後、解剖したが、外観的及び内臓観察において
も特記すべき異常所見を認めず又特記すべき中毒
症状も認められなかつた。[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.
【表】
実施例 ２
（動物実験）
体重130〜140ｇのウイスター（Wister）系雌
ラツトを用い、ペントパルビタール−Naを20
mg／Kg体重になるように水溶液として経口投与し
た。次いで直ちに第１表に示した試料及び薬用粉
末炭を水懸濁液として200mg／Kg体重になるよう
に経口投与した。同時に活性炭を投与しない比較
試験を実施した。検体は、各活性炭試料投与群及
び非投与群毎に10匹ずつ使用した。次いで血中の
ペントバルビタール−Naの最大濃度の平均値を
求め比較試験群での濃度に対する割合を除去率と
して算出した結果は第３表の通りであり、何れの
活性炭試料投与群においても、顕著な解毒作用が
観察された。[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.
【表】
次いで、活性炭の投与から90分後にこれ等の検
体群を痲酔死させ消化管を摘出して活性炭の腸内
移送の程度を比較した。即ち、噴門から直腸末端
までの全長に対する活性炭到達部までの移送距離
の割合を移送率として判定した。結果は第４表に
示す様に、粉末炭に対して第１表に示す本発明の
活性炭試料を用いた検体群では、その移送率が明
確に大きく、粉末炭でみられる便秘作用の少ない
ことが示された。[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.
【表】
実施例 ３
（臨床例）
習慣性の便秘と顔面の吹出物で悩んでいた24才
及び36才の女性に薬用粉末炭を１回３ｇ、１日３
回食間に服用させたところ３日目から吹出物は
やゝ減少したが、便秘は更にひどくなり排便時の
苦痛の増加を訴えた。そこで薬用粉末炭の服用を
停止し、次いで24才の女性には実施例１の第１表
に示す本発明の試料−１、36才の女性には試料−
３の球形活性炭を１回３ｇ、１日３回食間に服用
させた。何れの場合も４日目から吹出物は次第に
減少し１週間後には殆んど消失した。又、便秘症
状も著しく軽減され又、排便時の苦痛の消失とい
う報告を得た。
実施例 ４
（臨床例）
約１週間毎に便秘と下痢を繰返していた42才の
男性に薬用粉末炭を１回５ｇ、１日３回食間に服
用させたところ便秘時の排便の苦痛が増し、排便
の困難を訴えた。そこで、粉末炭の服用を停止
し、次いで実施例１、第１表に示す本発明の試料
−２の球形活性炭を１回５ｇ、１日３回食間に服
用させたところ、１週間後から正常な苦痛のない
排便がみられ、又、同時に下痢症状も殆んど消失
した。
実施例 ５
意識障害をきたしたノルモテストの結果は10％
以下、昏睡の急性肝炎症状の患者（59才）に対
し、鼻腔ゾンデにより１日当り第１表試料−２の
本発明の活性炭100ｇ、水酸化マグネシウム30
ｇ、ラクツロース60ｇを６回に分け、注入を開始
したところ、著名な悪化傾向もなく推移した。
翌日、4000mlの交換輸血を実施し、活性炭／水
酸化マグネシウム／ラクツロースの投与を続けた
ところ、３病日後には脳波上の改善を認め、次
後、１日当り活性炭50ｇ、水酸化マグネシウム30
ｇ、ラクチロース30ｇを６回に分け投与したが、
５病日には意識改善が著明となり、会話が可能と
なつた。次いで７病日にはノルモテスト32％と顕
著に改善した。尚活性炭投与による便秘症状は認
めず正常であつた。[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)
細孔半径100〜75000Åの範囲での細孔容積0.05〜
1.0c.c.／ｇの特性を有する、便秘性副作用のない
球形活性炭からなる経口解毒剤。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.
Priority Applications (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP15654677A JPS5489010A (en) | 1977-12-27 | 1977-12-27 | Spherical activated charcoal antidote |
| CA318,549A CA1112172A (en) | 1977-12-27 | 1978-12-22 | Antidote consisting of particles of activated carbon |
| GB7849806A GB2012257B (en) | 1977-12-27 | 1978-12-22 | Particles of activated carbon and their use in combatting gastrointrstinal illnesses |
| DE2855825A DE2855825C2 (en) | 1977-12-27 | 1978-12-22 | Use of activated carbon particles as an antidote |
| ES476321A ES476321A1 (en) | 1977-12-27 | 1978-12-26 | Activated carbon and its use in gastrointestinal disorders |
| FR7836293A FR2413092A1 (en) | 1977-12-27 | 1978-12-26 | PRODUCT BASED ON ACTIVATED CARBON PARTICLES AND ITS APPLICATION AS ANTIDOTE |
| NL7812550A NL7812550A (en) | 1977-12-27 | 1978-12-27 | ACTIVE CABBAGE AS AN AGAINST. |
| US06/759,933 US4761284A (en) | 1977-12-27 | 1985-07-29 | Antidote including activated carbon particles |
| US07/047,291 US4822765A (en) | 1977-12-27 | 1987-05-08 | Process for treating activated carbon with aqueous ammonia |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP15654677A JPS5489010A (en) | 1977-12-27 | 1977-12-27 | Spherical activated charcoal antidote |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS5489010A JPS5489010A (en) | 1979-07-14 |
| JPS627169B2 true JPS627169B2 (en) | 1987-02-16 |
Family
ID=15630152
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP15654677A Granted JPS5489010A (en) | 1977-12-27 | 1977-12-27 | Spherical activated charcoal antidote |
Country Status (7)
| Country | Link |
|---|---|
| JP (1) | JPS5489010A (en) |
| CA (1) | CA1112172A (en) |
| DE (1) | DE2855825C2 (en) |
| ES (1) | ES476321A1 (en) |
| FR (1) | FR2413092A1 (en) |
| GB (1) | GB2012257B (en) |
| NL (1) | NL7812550A (en) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4761284A (en) * | 1977-12-27 | 1988-08-02 | Kureha Kagaku Kogy Kabushiki Kaisha | Antidote including activated carbon particles |
| JPS565313A (en) * | 1979-06-26 | 1981-01-20 | Kureha Chem Ind Co Ltd | Detoxificating spherical active carbon and preparing the same |
| JPS5673542A (en) * | 1979-11-22 | 1981-06-18 | Kureha Chem Ind Co Ltd | Adsorbent |
| JPS5731864A (en) * | 1980-08-04 | 1982-02-20 | Teijin Ltd | Oral activated carbon microcapsule |
| DE3819000A1 (en) * | 1988-06-03 | 1989-12-14 | Hasso Von Bluecher | Bag of a teabag type for eliminating pollutants |
| IT1273678B (en) * | 1993-08-12 | 1997-07-09 | Bluecher Hasso Von | ACTIVATED CARBON PRODUCTION PROCESS |
| NL1000078C2 (en) * | 1994-04-19 | 1996-04-22 | Bluecher Hasso Von | Odor filter for vacuum cleaners. |
| SE515506C2 (en) * | 1994-06-17 | 2001-08-20 | Mhb Filtration Gmbh & Co Kg | Odor filter for ventilation outlet hoods |
| SE509743C2 (en) * | 1994-06-17 | 1999-03-01 | Bluecher Hasso Von | Adsorptionsfilterskikt |
| FR2745981B1 (en) * | 1996-03-15 | 1998-06-05 | ADSORBENT AGENT REDUCING OR ELIMINATING SIDE EFFECTS LINKED TO THE ABSORPTION OF SWEETENERS | |
| JPH1129485A (en) * | 1997-07-10 | 1999-02-02 | Kureha Chem Ind Co Ltd | Antiobestic medicine |
| JP3522708B2 (en) * | 2001-04-11 | 2004-04-26 | 呉羽化学工業株式会社 | Adsorbent for oral administration |
| RU2306941C2 (en) * | 2002-11-01 | 2007-09-27 | Куреха Корпорейшн | Adsorbent for peroral administration |
| US7651974B2 (en) | 2002-11-01 | 2010-01-26 | Kureha Chemical Industry Co., Ltd. | Adsorbent for oral administration |
| KR101135260B1 (en) | 2003-10-22 | 2012-04-12 | 가부시키가이샤 쿠레하 | Adsorbent for oral administration, and agent for treating or preventing renal or liver disease |
| US20070231394A1 (en) * | 2004-02-06 | 2007-10-04 | Sumie Goto | Agent for Removing Circulatory Dysfunction Factor |
| TWI370012B (en) | 2004-04-02 | 2012-08-11 | Kureha Corp | Adsorbent for oral administration, and agent for treating or preventing renal or liver disease |
| TWI370013B (en) | 2004-04-02 | 2012-08-11 | Kureha Corp | Adsorbent for oral administration, and agent for treating or preventing renal or liver disease |
| EP1757362A4 (en) * | 2004-05-31 | 2007-08-22 | Teikoku Medix Co Ltd | Adsorbent and process for producing the same |
| US8247072B2 (en) | 2006-02-14 | 2012-08-21 | Eastman Chemical Company | Resol beads, methods of making them and methods of using them |
| EP2120861A2 (en) * | 2006-11-27 | 2009-11-25 | De Novo Inc. | Decontaminant edible product, methods of production and uses thereof |
| JP5984352B2 (en) * | 2010-10-12 | 2016-09-06 | フタムラ化学株式会社 | Method for producing pharmaceutical adsorbent for oral administration |
| JP5985027B2 (en) * | 2010-10-12 | 2016-09-06 | フタムラ化学株式会社 | Method for producing pharmaceutical adsorbent for oral administration |
| JP6456830B2 (en) * | 2012-09-21 | 2019-01-23 | フェリング ベスローテン フェンノートシャップ | Pharmaceutical composition |
| WO2014154677A1 (en) | 2013-03-25 | 2014-10-02 | Ferring Bv | Composition for the treatment of disease |
| KR101924201B1 (en) * | 2014-02-07 | 2018-12-03 | 대원제약주식회사 | Medicinal adsorbent for oral administration with increased strength |
Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS4983690A (en) * | 1972-12-20 | 1974-08-12 | ||
| JPS49126591A (en) * | 1973-04-10 | 1974-12-04 | ||
| JPS5018879A (en) * | 1973-06-20 | 1975-02-27 | ||
| JPS5051996A (en) * | 1973-09-11 | 1975-05-09 | ||
| JPS51148291A (en) * | 1975-06-13 | 1976-12-20 | Teijin Ltd | Artificial organ |
| JPS51151693A (en) * | 1975-06-23 | 1976-12-27 | Eisai Co Ltd | Coated bead-like activated carbon for blood purification |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5018879B2 (en) * | 1971-08-27 | 1975-07-02 | ||
| DE2410372C2 (en) * | 1974-03-05 | 1982-03-04 | Kureha Kagaku Kogyo K.K., Tokyo | Process for reactivating spent practically spherical activated carbon of small size |
-
1977
- 1977-12-27 JP JP15654677A patent/JPS5489010A/en active Granted
-
1978
- 1978-12-22 DE DE2855825A patent/DE2855825C2/en not_active Expired
- 1978-12-22 GB GB7849806A patent/GB2012257B/en not_active Expired
- 1978-12-22 CA CA318,549A patent/CA1112172A/en not_active Expired
- 1978-12-26 ES ES476321A patent/ES476321A1/en not_active Expired
- 1978-12-26 FR FR7836293A patent/FR2413092A1/en active Granted
- 1978-12-27 NL NL7812550A patent/NL7812550A/en active Search and Examination
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS4983690A (en) * | 1972-12-20 | 1974-08-12 | ||
| JPS49126591A (en) * | 1973-04-10 | 1974-12-04 | ||
| JPS5018879A (en) * | 1973-06-20 | 1975-02-27 | ||
| JPS5051996A (en) * | 1973-09-11 | 1975-05-09 | ||
| JPS51148291A (en) * | 1975-06-13 | 1976-12-20 | Teijin Ltd | Artificial organ |
| JPS51151693A (en) * | 1975-06-23 | 1976-12-27 | Eisai Co Ltd | Coated bead-like activated carbon for blood purification |
Also Published As
| Publication number | Publication date |
|---|---|
| GB2012257A (en) | 1979-07-25 |
| FR2413092B1 (en) | 1982-11-19 |
| ES476321A1 (en) | 1979-06-16 |
| DE2855825C2 (en) | 1984-03-01 |
| FR2413092A1 (en) | 1979-07-27 |
| GB2012257B (en) | 1983-03-30 |
| DE2855825A1 (en) | 1979-06-28 |
| NL7812550A (en) | 1979-06-29 |
| JPS5489010A (en) | 1979-07-14 |
| CA1112172A (en) | 1981-11-10 |
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