JPH02255616A - Drug for hepatic disease - Google Patents
Drug for hepatic diseaseInfo
- Publication number
- JPH02255616A JPH02255616A JP7629889A JP7629889A JPH02255616A JP H02255616 A JPH02255616 A JP H02255616A JP 7629889 A JP7629889 A JP 7629889A JP 7629889 A JP7629889 A JP 7629889A JP H02255616 A JPH02255616 A JP H02255616A
- Authority
- JP
- Japan
- Prior art keywords
- drug
- administration
- tablet
- hepatic disease
- formula
- 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.)
- Pending
Links
- 239000003814 drug Substances 0.000 title claims abstract description 16
- 229940079593 drug Drugs 0.000 title claims abstract description 16
- 208000019423 liver disease Diseases 0.000 title claims abstract description 8
- 239000000126 substance Substances 0.000 claims description 2
- 150000001875 compounds Chemical class 0.000 abstract description 12
- UIOFUWFRIANQPC-JKIFEVAISA-N Floxacillin Chemical compound N([C@@H]1C(N2[C@H](C(C)(C)S[C@@H]21)C(O)=O)=O)C(=O)C1=C(C)ON=C1C1=C(F)C=CC=C1Cl UIOFUWFRIANQPC-JKIFEVAISA-N 0.000 abstract description 7
- 238000000034 method Methods 0.000 abstract description 7
- LUSZGTFNYDARNI-UHFFFAOYSA-N Sesamol Natural products OC1=CC=C2OCOC2=C1 LUSZGTFNYDARNI-UHFFFAOYSA-N 0.000 abstract description 6
- 230000000694 effects Effects 0.000 abstract description 3
- 239000008187 granular material Substances 0.000 abstract description 3
- -1 troche Substances 0.000 abstract description 3
- 239000002775 capsule Substances 0.000 abstract description 2
- 238000002347 injection Methods 0.000 abstract description 2
- 239000007924 injection Substances 0.000 abstract description 2
- 239000000843 powder Substances 0.000 abstract description 2
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000001747 exhibiting effect Effects 0.000 abstract 1
- 229940126701 oral medication Drugs 0.000 abstract 1
- 239000002245 particle Substances 0.000 abstract 1
- 239000006187 pill Substances 0.000 abstract 1
- 230000003449 preventive effect Effects 0.000 abstract 1
- 239000002994 raw material Substances 0.000 abstract 1
- 239000000829 suppository Substances 0.000 abstract 1
- 239000003826 tablet Substances 0.000 abstract 1
- VZGDMQKNWNREIO-UHFFFAOYSA-N tetrachloromethane Chemical compound ClC(Cl)(Cl)Cl VZGDMQKNWNREIO-UHFFFAOYSA-N 0.000 description 14
- 241000700159 Rattus Species 0.000 description 7
- 239000004480 active ingredient Substances 0.000 description 5
- 238000002474 experimental method Methods 0.000 description 4
- 206010067125 Liver injury Diseases 0.000 description 3
- 229920002472 Starch Polymers 0.000 description 3
- 239000000654 additive Substances 0.000 description 3
- 210000004369 blood Anatomy 0.000 description 3
- 239000008280 blood Substances 0.000 description 3
- 239000002552 dosage form Substances 0.000 description 3
- 231100000234 hepatic damage Toxicity 0.000 description 3
- 230000008818 liver damage Effects 0.000 description 3
- 210000002966 serum Anatomy 0.000 description 3
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 2
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- 238000010171 animal model Methods 0.000 description 2
- 238000010241 blood sampling Methods 0.000 description 2
- OSGAYBCDTDRGGQ-UHFFFAOYSA-L calcium sulfate Chemical compound [Ca+2].[O-]S([O-])(=O)=O OSGAYBCDTDRGGQ-UHFFFAOYSA-L 0.000 description 2
- 238000007912 intraperitoneal administration Methods 0.000 description 2
- 210000004185 liver Anatomy 0.000 description 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 238000005259 measurement Methods 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 238000007911 parenteral administration Methods 0.000 description 2
- 230000001681 protective effect Effects 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 235000019698 starch Nutrition 0.000 description 2
- 238000007920 subcutaneous administration Methods 0.000 description 2
- 239000003981 vehicle Substances 0.000 description 2
- XGNXYCFREOZBOL-UHFFFAOYSA-N 1,3-benzodioxol-5-amine Chemical compound NC1=CC=C2OCOC2=C1 XGNXYCFREOZBOL-UHFFFAOYSA-N 0.000 description 1
- IXPNQXFRVYWDDI-UHFFFAOYSA-N 1-methyl-2,4-dioxo-1,3-diazinane-5-carboximidamide Chemical compound CN1CC(C(N)=N)C(=O)NC1=O IXPNQXFRVYWDDI-UHFFFAOYSA-N 0.000 description 1
- 244000215068 Acacia senegal Species 0.000 description 1
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 1
- 206010002091 Anaesthesia Diseases 0.000 description 1
- 241000416162 Astragalus gummifer Species 0.000 description 1
- 229920002261 Corn starch Polymers 0.000 description 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 1
- 229920001353 Dextrin Polymers 0.000 description 1
- 239000004375 Dextrin Substances 0.000 description 1
- 239000001856 Ethyl cellulose Substances 0.000 description 1
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 description 1
- 108010010803 Gelatin Proteins 0.000 description 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- 229920000084 Gum arabic Polymers 0.000 description 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 1
- 229930195725 Mannitol Natural products 0.000 description 1
- 239000004372 Polyvinyl alcohol Substances 0.000 description 1
- 240000004808 Saccharomyces cerevisiae Species 0.000 description 1
- ZZMNWJVJUKMZJY-AFHBHXEDSA-N Sesamolin Chemical compound C1=C2OCOC2=CC([C@H]2OC[C@H]3[C@@H]2CO[C@@H]3OC2=CC=C3OCOC3=C2)=C1 ZZMNWJVJUKMZJY-AFHBHXEDSA-N 0.000 description 1
- ZZMNWJVJUKMZJY-UHFFFAOYSA-N Sesamolin Natural products C1=C2OCOC2=CC(C2OCC3C2COC3OC2=CC=C3OCOC3=C2)=C1 ZZMNWJVJUKMZJY-UHFFFAOYSA-N 0.000 description 1
- 238000000692 Student's t-test Methods 0.000 description 1
- 229920001615 Tragacanth Polymers 0.000 description 1
- 229920004482 WACKER® Polymers 0.000 description 1
- 230000003187 abdominal effect Effects 0.000 description 1
- 235000010489 acacia gum Nutrition 0.000 description 1
- 239000000205 acacia gum Substances 0.000 description 1
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 1
- 125000000217 alkyl group Chemical group 0.000 description 1
- 230000037005 anaesthesia Effects 0.000 description 1
- 230000000844 anti-bacterial effect Effects 0.000 description 1
- 230000003078 antioxidant effect Effects 0.000 description 1
- 125000003118 aryl group Chemical group 0.000 description 1
- 230000001580 bacterial effect Effects 0.000 description 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 229910000019 calcium carbonate Inorganic materials 0.000 description 1
- 229920003123 carboxymethyl cellulose sodium Polymers 0.000 description 1
- 229940063834 carboxymethylcellulose sodium Drugs 0.000 description 1
- 239000001913 cellulose Substances 0.000 description 1
- 229920002678 cellulose Polymers 0.000 description 1
- 239000003153 chemical reaction reagent Substances 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 239000008120 corn starch Substances 0.000 description 1
- 238000012937 correction Methods 0.000 description 1
- 235000019425 dextrin Nutrition 0.000 description 1
- 239000007884 disintegrant Substances 0.000 description 1
- 239000003651 drinking water Substances 0.000 description 1
- 235000020188 drinking water Nutrition 0.000 description 1
- 238000007908 dry granulation Methods 0.000 description 1
- 235000019325 ethyl cellulose Nutrition 0.000 description 1
- 229920001249 ethyl cellulose Polymers 0.000 description 1
- 229960004667 ethyl cellulose Drugs 0.000 description 1
- 239000003205 fragrance Substances 0.000 description 1
- 239000000499 gel Substances 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 229940014259 gelatin Drugs 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 238000005469 granulation Methods 0.000 description 1
- 230000003179 granulation Effects 0.000 description 1
- 229910052739 hydrogen Inorganic materials 0.000 description 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 1
- 230000007062 hydrolysis Effects 0.000 description 1
- 238000006460 hydrolysis reaction Methods 0.000 description 1
- 230000003301 hydrolyzing effect Effects 0.000 description 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 235000019359 magnesium stearate Nutrition 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 238000000691 measurement method Methods 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 235000010981 methylcellulose Nutrition 0.000 description 1
- 229960002900 methylcellulose Drugs 0.000 description 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
- 239000004006 olive oil Substances 0.000 description 1
- 235000008390 olive oil Nutrition 0.000 description 1
- 239000006186 oral dosage form Substances 0.000 description 1
- 239000006201 parenteral dosage form Substances 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 1
- 229920000053 polysorbate 80 Polymers 0.000 description 1
- 229920002451 polyvinyl alcohol Polymers 0.000 description 1
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 description 1
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 description 1
- 239000001253 polyvinylpolypyrrolidone Substances 0.000 description 1
- 229920001592 potato starch Polymers 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 235000010413 sodium alginate Nutrition 0.000 description 1
- 239000000661 sodium alginate Substances 0.000 description 1
- 229940005550 sodium alginate Drugs 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 229920002554 vinyl polymer Polymers 0.000 description 1
- 238000005550 wet granulation Methods 0.000 description 1
- 229940100445 wheat starch Drugs 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
Abstract
Description
【発明の詳細な説明】 [産業上の利用分野] 本発明は、肝臓疾患用剤に関する。[Detailed description of the invention] [Industrial application field] TECHNICAL FIELD The present invention relates to a drug for liver diseases.
[従来の技術]
従来、ヒトの肝臓疾患を治療及び予防する薬剤として、
種々のものが考えだされてきている。しかし、これら従
来の薬剤には、副作用の強いもの(式中、R+及びRo
は、−緒になって一〇CH20−を表し、R5はH,O
H,NHz、 CQCHs、 CH”CH−CH3又は
CHz−CH=CJを表す)
よりなる肝臓疾患用剤に関する。[Prior Art] Conventionally, as a drug for treating and preventing liver diseases in humans,
Various things have been devised. However, these conventional drugs have strong side effects (in the formula, R+ and Ro
- together represent 10CH20-, and R5 is H, O
H, NHz, CQCHs, CH"represents CH-CH3 or CHz-CH=CJ).
セサモールのメチレンジオキシ基のメチレンにおける2
個の水素原子をアルキル基で置換した化合物、セサモー
ルの芳香環にヒドロキシメチル基を導入した化合物につ
いては、抗菌性を有することが知られており(「防菌防
黴J13巻、2号、51〜55ページ、11号、495
〜499ページ、1985年)、またセサモールには抗
酸化作用があることが知られているが、肝臓の疾患に有
用であることについては未だ知られていない。2 in methylene of methylenedioxy group of sesamol
Compounds in which hydrogen atoms have been replaced with alkyl groups, and compounds in which hydroxymethyl groups have been introduced into the aromatic ring of sesamol are known to have antibacterial properties ("Bacterial and Mildew Prevention J Vol. 13, No. 2, 51 ~page 55, issue 11, 495
499, 1985), and sesamol is known to have an antioxidant effect, but it is not yet known that it is useful for liver diseases.
本発明に使用される式(1)の化合物は、セサモール(
R3=OH)又はその誘導体であって、よく知られた化
合物である0例えば、セサモールは、セサモリンを塩酸
により加水分解するか、4−アミノ−1,2−メチレン
ジオキシベンゼンをジアゾ化し、次いで加水分解するこ
となどにより得ることができる。The compound of formula (1) used in the present invention is sesamol (
R3=OH) or a derivative thereof, which is a well-known compound 0. For example, sesamol is prepared by hydrolyzing sesamolin with hydrochloric acid or diazotizing 4-amino-1,2-methylenedioxybenzene, and then It can be obtained by hydrolysis etc.
本発明の薬剤は、投与に当たって、経口でも又は非経口
でも用いることが出来る。経口用の剤型としては、例え
ば粉末、顆粒、細粒、錠剤、トローチ剤、カプセル剤、
大割などの従来用いられてい剤型が挙げられる。非経口
の剤型としては、例えば注射剤、座刑などのこれまた従
来用いられている剤型が挙げられる。これら剤型の製造
に当たっては、従来行なわれている方法が用いられる。The drug of the present invention can be administered orally or parenterally. Examples of oral dosage forms include powders, granules, fine granules, tablets, troches, capsules,
Examples include conventionally used dosage forms such as Owari. Examples of parenteral dosage forms include conventionally used dosage forms, such as injections and seated tablets. In manufacturing these dosage forms, conventional methods are used.
例えば、錠剤の製造では、式(1)の化合物に従来添加
物として用いられているものを加えて十分に混合する。For example, in the production of tablets, conventionally used additives are added to the compound of formula (1) and mixed thoroughly.
添加剤としては、例えば賦形剤例えばとうもろこし澱粉
、小麦澱粉、馬鈴薯澱粉、ラクトース、ぶどう糖、マニ
トール、炭酸カルシウム、硫酸カルシウムなど:結合剤
例えば澱粉類、デキストリン、アラビアゴム、トラガン
トゴム、アルギン酸ナトリウム、ゼラチン、メチルセル
ロース、エチルセルロース、ポリビニルとロリドン、ポ
リビニルアルコールなど:崩壊剤例えば澱粉類、ポリビ
ニルポリピロリドン、結晶セルロースなど:滑沢剤例え
ばステアリン酸マグネシウム、タルクなど:着色剤、香
料などが挙げられる。得られた混合物を、湿式又は乾式
で顆粒とするか又はすることなく打錠機にかけて打錠し
錠剤とする。錠剤中の有効成分の量は、任意でよい。Examples of additives include excipients such as corn starch, wheat starch, potato starch, lactose, glucose, mannitol, calcium carbonate, calcium sulfate, etc.; binders such as starches, dextrin, gum arabic, gum tragacanth, sodium alginate, gelatin, Methyl cellulose, ethyl cellulose, polyvinyl and lolidone, polyvinyl alcohol, etc.; Disintegrants, such as starches, polyvinyl polypyrrolidone, crystalline cellulose, etc.; Lubricants, such as magnesium stearate, talc, etc.; Coloring agents, fragrances, etc. The resulting mixture is made into tablets by wet or dry granulation, or by using a tablet machine without granulation. The amount of active ingredient in the tablet may be arbitrary.
また例えば、非経口投与としては、式(1)の化合物及
び滅菌媒体を含む、化合物は、媒体及び濃度に応じて懸
独又は溶解される。そして非経口投与として、例えば腹
腔内、皮下の投与が挙げ・られる。Also, for example, for parenteral administration, the compound may be suspended or dissolved, depending on the vehicle and concentration, including a compound of formula (1) and a sterile vehicle. Examples of parenteral administration include intraperitoneal and subcutaneous administration.
本発明薬剤の投与に当たっては、症状に応じ、成人では
1日1〜数回、1日当たり合計量で有効成分を50〜5
000■好ましくはioo〜50omg用いる。When administering the drug of the present invention, for adults, the total amount of the active ingredient should be 50-50% per day, once to several times a day, depending on the symptoms.
000■ioo~50omg is preferably used.
本発明に用いられる化合物は、以下の実施例の実験にお
いて毒性は全く認められない。The compounds used in the present invention were not found to be toxic at all in the experiments of the following examples.
本発明の薬剤は、下記の実験結果から分かるように、ラ
ットの四塩化炭素による肝障害に対して防護作用を有し
、肝疾患に対して有効である。As can be seen from the experimental results below, the drug of the present invention has a protective effect against liver damage caused by carbon tetrachloride in rats, and is effective against liver diseases.
[実施例コ 次に、実施例を示す。[Example code] Next, examples will be shown.
実施例 1
成 −」にQ
弧工こlLと活 性 成 分
50カルボキシメチルセルロ
ースナトリウム、
140ラ り ト − ス
40活性
成分と添加物とをそれぞれ5錠分ずつ秤取し、それらを
均一に混合した。混合物から1錠分を秤取し、打錠機に
より200 kg/cdの圧力で直接打錠して、錠剤を
得た0錠剤は、活性成分を1錠当たり50mg含有した
。Example 1 Q
Arc Works and Active Ingredients
50 carboxymethylcellulose sodium,
140 liters
Five tablets each of the 40 active ingredients and additives were weighed out and mixed uniformly. One tablet was weighed out from the mixture and directly compressed using a tablet press at a pressure of 200 kg/cd to obtain a tablet.Tablet 0 contained 50 mg of the active ingredient per tablet.
[効果コ 本発明の薬剤の肝実買障害防護効果を示す。[Effect Co. 1 shows the protective effect of the drug of the present invention on liver disease.
実験動物
Wistar系雄性ラット(生後7週令、体重180〜
200g、埼玉実験動物供給所)を1群3〜4匹として
用いた。飼料(オリエンタル酵母製)は、自由摂取させ
たが、CCl4投与24時間前と採血24時間前の計4
8時間は絶食させ、飲料水は採血時まで自由摂取させた
。Experimental animal Wistar male rat (7 weeks old, weight 180~
200 g, Saitama Experimental Animal Supply Center) were used, with 3 to 4 animals per group. Feed (manufactured by Oriental Yeast) was given ad libitum, but 4 hours in total, 24 hours before CCl4 administration and 24 hours before blood collection.
The animals were fasted for 8 hours and had free access to drinking water until blood sampling.
CCl4肝障害ラットの作成
CCL (和光純薬、特級)の投与量が0.3d/kg
になるように、20%オリーブ油(日本薬局方)溶液と
して、24時間絶食させたラットの腹腔内に投与して作
成した。Creation of CCl4 liver-damaged rats The dose of CCL (Wako Pure Chemical, special grade) was 0.3 d/kg.
It was prepared by intraperitoneally administering it as a 20% olive oil (Japanese Pharmacopoeia) solution to rats that had been fasted for 24 hours.
試料の投与方法
試料は、5%Tween 80で懸独させ、0.4NN
aOHを加えpH7に補正し、投与液量がO14〜1t
xl/200gになるように調製して、CC1,処理前
に投与した。Sample administration method Samples were suspended in 5% Tween 80 and 0.4NN
Add aOH to correct the pH to 7, and adjust the volume of the administered solution to 014~1t.
xl/200g and administered before CC1 treatment.
採血及び測定法
CC1,投与24時間後に、ラットをエーテル麻酔下で
開腹し、腹部下行大静脈から採血した。得られた血液は
、遠心分離(3000rpm、 10分)して、血清を
分取した。血清成分の測定は、GOTとGPTはKar
men法で、LDHはWacker法で、LAPはNa
gel法で、T−BIL及びD−OILはJendra
ssik法により、それぞれ測定用試薬(デンカ生研)
を用い、生化学自動分析装置(TBA−380、東芝メ
ディカル)で測定した。Blood Sampling and Measurement Method CC1. Twenty-four hours after administration, the rats were laparotomyd under ether anesthesia, and blood was collected from the abdominal descending vena cava. The obtained blood was centrifuged (3000 rpm, 10 minutes) to separate serum. For measurement of serum components, GOT and GPT are
Men method, LDH is Wacker method, LAP is Na
By gel method, T-BIL and D-OIL are Jendra
Using the ssik method, each measurement reagent (Denka Seiken)
It was measured using an automatic biochemical analyzer (TBA-380, Toshiba Medical).
肝障害防護 力の表示
肝障害防護効力は、無処置の正常群、CCl4投与群及
び薬物+CCt、CCl4投与群れの血清成分の測定値
の平均を次の式に代入し、算出した。Display of liver damage protection efficacy The liver damage protection efficacy was calculated by substituting the average of the measured values of serum components of the untreated normal group, the CCl4 administration group, and the drug+CCt and CCl4 administration groups into the following formula.
CCl4投与醪−正ll
5tudent’s t−テストにより、各測定値の効
力の有意性を判定した。 +:p<0.05.++:p
<0.01実験 1
セサモールを投与量を変えて、ラット(n・4)に、C
C1,(0,3艷/kg、 i、p、)処理30分前に
腹腔内に投与した。The significance of the efficacy of each measured value was determined by CCl4 administration moromi-correction 5 student's t-test. +: p<0.05. ++:p
<0.01 Experiment 1 C
C1, (0.3 g/kg, i, p,) was administered intraperitoneally 30 minutes before treatment.
結果を、第1表に示す、肝臓の状態は、投与量1 nm
ol/kgでやや良好であり、投与量0.5及び0 、
25 n+mol/kgで良好テアツタ。The results are shown in Table 1.
ol/kg, slightly better at dosages of 0.5 and 0,
25 n+mol/kg with good tearing.
第1表
0.5
0.25
a、12
0.06
95.8+中
91.5”
91.4”
82.4”
0.7
92.2”
88.7”
87.9”
55.1”
17.9
97.1”
95.5”
81.5”
47.4
−48.1
102.2+中
80.4”
60J”
30.4
=4.3
100.9”
96.4”
87.4”
58.6÷
18.4
87.3”
80.3”
71、P”
58.5”
32.1
実験 2
セサモールを投与量を変えて、ラット(n=4又は3)
に、CC1a (0、3+d / kg%i、p、)処
理前、表に示す時間をおいて腹腔内に投与した。Table 1 0.5 0.25 a, 12 0.06 95.8 + medium 91.5” 91.4” 82.4” 0.7 92.2” 88.7” 87.9” 55.1” 17.9 97.1"95.5"81.5" 47.4 -48.1 102.2 + Medium 80.4"60J" 30.4 = 4.3 100.9"96.4" 87.4 " 58.6 ÷ 18.4 87.3"80.3" 71, P"58.5" 32.1 Experiment 2 Rats (n = 4 or 3) with different doses of sesamol
CC1a (0,3+d/kg%i,p,) was administered intraperitoneally at the time shown in the table before treatment.
結果を第2表に示す、肝臓の状態は、腹腔的投与では、
投与量0.250o1/kgで30分前でやや良好、皮
下投与では投与量l及び0 、 5 *mol/kgで
30分前でやや良好、経口投与では投与量0 、 5
mmol/ kgで60分前でやや良好であった。The results are shown in Table 2. The liver condition was determined by intraperitoneal administration.
Slightly good after 30 minutes at dose 0.250o1/kg, slightly good after 30 minutes before subcutaneous administration at doses 1 and 0,5*mol/kg, and slightly good after 30 minutes before oral administration at doses 0, 5
It was slightly better at mmol/kg before 60 minutes.
実験 3
表に示す化合物を投与量を変えて、ラット(n:4)に
、CCl4(0,3艷/kg、 i、p、)処理30分
前に皮下に投与した。結果を第3表に示す。Experiment 3 The compounds shown in the table were subcutaneously administered to rats (n: 4) at different doses 30 minutes before treatment with CCl4 (0.3 rods/kg, i, p). The results are shown in Table 3.
轟
第2表
0.25
b、4hr
b、乃r
b、30Isin
b、301Lin
b、30ILin
b、30ILin
b、60odn
b260社n
−13,4
21,0
84,2”
89.5”
11.9
35.2”
118.7”
73.4”
0.9
9.6
69、O”
84.8”
0.7
19.2
80.3”
70.0中“
−n、2
1.2
611.0”
97.4”
−n、9
16.8
95.8”
78.1”
−5,7
0,0
34,3中
83.3中十
−2,9
22,9
go、o”
45.7+“
−16,7
18,3
41,7
69,6”
5.0
18.3
88.7”
713.7”
2゜
C113
H
Cl1=C11−COO1!
0.5
各表の項目において、Aは投与量、Bは投与方法、Cは
投与前の時間、Dは肝臓の状態を示すことにする。Todoroki 2nd table 0.25 b, 4hr b, no r b, 30Isin b, 301Lin b, 30ILin b, 30ILin b, 60odn b260 company n -13,4 21,0 84,2"89.5" 11.9 35.2"118.7"73.4" 0.9 9.6 69, O"84.8" 0.7 19.2 80.3" 70.0 " -n, 2 1.2 611. 0"97.4" -n, 9 16.8 95.8"78.1" -5,7 0,0 34,3 out of 83.3 out of 10 -2,9 22,9 go, o" 45. 7+" -16,7 18,3 41,7 69,6" 5.0 18.3 88.7"713.7" 2°C113H Cl1=C11-COO1! 0.5 In the items in each table, A indicates the dose, B indicates the administration method, C indicates the time before administration, and D indicates the liver condition.
第3表から分かるように、本発明の化合物(即ちNo、
1.5.8,13.14及びllでは良好又はやや良
好な結果を得ることができるが、これら化合物と構造が
極めて似ている他の化合物では、満足できる結果を得る
ことが出来ない、このことから、本発明の薬剤が優れて
いることは容易に理解できる。As can be seen from Table 3, the compounds of the present invention (i.e. No.
Good or somewhat good results can be obtained with 1.5.8, 13.14 and ll, but satisfactory results cannot be obtained with other compounds whose structures are extremely similar to these compounds. Therefore, it can be easily understood that the drug of the present invention is superior.
Claims (1)
2O−を表し、R_3はH、OH、NH_2、COCH
_3、CH=CH−CH_3又はCH_2−CH=CH
_2を表す) よりなる肝臓疾患用剤。[Claims] Formula (1) ▲There are mathematical formulas, chemical formulas, tables, etc.▼(1) (In the formula, R_1 and R_2 together represent -OCH_
2O-, R_3 is H, OH, NH_2, COCH
_3, CH=CH-CH_3 or CH_2-CH=CH
_2) A drug for liver diseases.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP7629889A JPH02255616A (en) | 1989-03-27 | 1989-03-27 | Drug for hepatic disease |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP7629889A JPH02255616A (en) | 1989-03-27 | 1989-03-27 | Drug for hepatic disease |
Publications (1)
Publication Number | Publication Date |
---|---|
JPH02255616A true JPH02255616A (en) | 1990-10-16 |
Family
ID=13601459
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP7629889A Pending JPH02255616A (en) | 1989-03-27 | 1989-03-27 | Drug for hepatic disease |
Country Status (1)
Country | Link |
---|---|
JP (1) | JPH02255616A (en) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0818196A1 (en) * | 1989-07-21 | 1998-01-14 | Suntory Limited | Food or drink containing dioxabicyclo (3.3.0) octane compounds |
-
1989
- 1989-03-27 JP JP7629889A patent/JPH02255616A/en active Pending
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0818196A1 (en) * | 1989-07-21 | 1998-01-14 | Suntory Limited | Food or drink containing dioxabicyclo (3.3.0) octane compounds |
EP0826369A1 (en) * | 1989-07-21 | 1998-03-04 | Suntory Limited | Therapeutic use of dioxabicyclo (3.3.0)octane compounds |
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