JPS6213325B2 - - Google Patents
Info
- Publication number
- JPS6213325B2 JPS6213325B2 JP53030618A JP3061878A JPS6213325B2 JP S6213325 B2 JPS6213325 B2 JP S6213325B2 JP 53030618 A JP53030618 A JP 53030618A JP 3061878 A JP3061878 A JP 3061878A JP S6213325 B2 JPS6213325 B2 JP S6213325B2
- Authority
- JP
- Japan
- Prior art keywords
- pantethine
- platelet aggregation
- administered
- blood
- aggregation ability
- 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
- DJWYOLJPSHDSAL-ROUUACIJSA-N pantethine Chemical compound OCC(C)(C)[C@@H](O)C(=O)NCCC(=O)NCCSSCCNC(=O)CCNC(=O)[C@H](O)C(C)(C)CO DJWYOLJPSHDSAL-ROUUACIJSA-N 0.000 claims description 14
- 229920002472 Starch Polymers 0.000 claims description 2
- 229920002678 cellulose Polymers 0.000 claims description 2
- 239000001913 cellulose Substances 0.000 claims description 2
- 239000003795 chemical substances by application Substances 0.000 claims description 2
- 239000008107 starch Substances 0.000 claims description 2
- 235000019698 starch Nutrition 0.000 claims description 2
- 230000002471 thromboprophylactic effect Effects 0.000 claims description 2
- 239000003146 anticoagulant agent Substances 0.000 claims 2
- 229960004676 antithrombotic agent Drugs 0.000 claims 2
- 239000007864 aqueous solution Substances 0.000 claims 1
- RMAQACBXLXPBSY-UHFFFAOYSA-N silicic acid Chemical compound O[Si](O)(O)O RMAQACBXLXPBSY-UHFFFAOYSA-N 0.000 claims 1
- 235000012239 silicon dioxide Nutrition 0.000 claims 1
- DJWYOLJPSHDSAL-UHFFFAOYSA-N Pantethine Natural products OCC(C)(C)C(O)C(=O)NCCC(=O)NCCSSCCNC(=O)CCNC(=O)C(O)C(C)(C)CO DJWYOLJPSHDSAL-UHFFFAOYSA-N 0.000 description 10
- 229960000903 pantethine Drugs 0.000 description 10
- 235000008975 pantethine Nutrition 0.000 description 10
- 239000011581 pantethine Substances 0.000 description 10
- 208000010110 spontaneous platelet aggregation Diseases 0.000 description 7
- 208000007536 Thrombosis Diseases 0.000 description 4
- 238000004220 aggregation Methods 0.000 description 3
- 230000002776 aggregation Effects 0.000 description 3
- 210000004369 blood Anatomy 0.000 description 3
- 239000008280 blood Substances 0.000 description 3
- 208000031226 Hyperlipidaemia Diseases 0.000 description 2
- 208000029078 coronary artery disease Diseases 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 239000002552 dosage form Substances 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 208000031225 myocardial ischemia Diseases 0.000 description 2
- 210000004623 platelet-rich plasma Anatomy 0.000 description 2
- 208000014644 Brain disease Diseases 0.000 description 1
- RGJOEKWQDUBAIZ-IBOSZNHHSA-N CoASH Chemical compound O[C@@H]1[C@H](OP(O)(O)=O)[C@@H](COP(O)(=O)OP(O)(=O)OCC(C)(C)[C@@H](O)C(=O)NCCC(=O)NCCS)O[C@H]1N1C2=NC=NC(N)=C2N=C1 RGJOEKWQDUBAIZ-IBOSZNHHSA-N 0.000 description 1
- 241000699670 Mus sp. Species 0.000 description 1
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 1
- 238000002835 absorbance Methods 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 230000007059 acute toxicity Effects 0.000 description 1
- 231100000403 acute toxicity Toxicity 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- RGJOEKWQDUBAIZ-UHFFFAOYSA-N coenzime A Natural products OC1C(OP(O)(O)=O)C(COP(O)(=O)OP(O)(=O)OCC(C)(C)C(O)C(=O)NCCC(=O)NCCS)OC1N1C2=NC=NC(N)=C2N=C1 RGJOEKWQDUBAIZ-UHFFFAOYSA-N 0.000 description 1
- 239000005516 coenzyme A Substances 0.000 description 1
- 229940093530 coenzyme a Drugs 0.000 description 1
- KDTSHFARGAKYJN-UHFFFAOYSA-N dephosphocoenzyme A Natural products OC1C(O)C(COP(O)(=O)OP(O)(=O)OCC(C)(C)C(O)C(=O)NCCC(=O)NCCS)OC1N1C2=NC=NC(N)=C2N=C1 KDTSHFARGAKYJN-UHFFFAOYSA-N 0.000 description 1
- 239000006185 dispersion Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 208000019622 heart disease Diseases 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 239000002243 precursor Substances 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 230000029058 respiratory gaseous exchange Effects 0.000 description 1
Landscapes
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Description
本発明は血栓予防剤に関するものであり、パン
テチンを（Ｄ−パンテチンを意味する。以下同
じ。）を有効成分として含有することを特徴とす
るものである。
血栓は心疾患や脳疾患を引き起すため恐れられ
ており、その予防法の確立が望まれている。血栓
の原因については種々の説があるが血小板の凝集
もその一つであるといわれている。
本発明者は、コエンザイムＡの前駆物質である
パンテチンの血小板凝集への影響について研究を
続けていたが、このものが血小板の凝集を顕著に
抑制することを見出し、血栓形成の予防に有用な
本発明を完成した。
すなわち、種々の疾患を有する患者にパンテチ
ンを投与し、その血液を採取して血小板凝集能を
測定して効果を確めた。次にその例を示す。
血小板の凝集能は、採血後クエン酸ソーダを加
え170Gで５分遠沈した静脈血、PRP（platelet
rich plasma）について吸光度法（山崎、呼吸と
循環、23巻、９号、791〜798頁）により測定し
た。
以上の試験に基づいて、種々の疾患を有する患
者についてパンテチンを投与し、その効果を確か
めた。次にその例を示す。
例
パンテチン５倍散を３〜５ｇ／日（３回に分
服）（パンテチンとして600〜1000mg／日）虚血性
心疾患（IHD）、冠動脈硬化症（CS）及び高脂血
症（HL）の患者に８週間経口投与し、投与前及
び投与後２週、４週、６週及び８週に採血し血小
板凝集能を測定した。凝集能の５分値（％）及び
最大凝集値（％）を次表に示すが、これからも分
るようにパンテチンは血小板の凝集能を抑制して
いることが認められる。
The present invention relates to a thromboprophylactic agent, which is characterized by containing pantethine (meaning D-pantethine, hereinafter the same) as an active ingredient. Blood clots are feared because they cause heart disease and brain disease, and there is a desire to establish methods for their prevention. There are various theories regarding the causes of blood clots, and platelet aggregation is said to be one of them. The present inventor has continued to research the effects of pantethine, a precursor of coenzyme A, on platelet aggregation, and has discovered that pantethine significantly inhibits platelet aggregation, and has published a book useful for preventing thrombus formation. Completed the invention. That is, pantethine was administered to patients with various diseases, their blood was collected, and their platelet aggregation ability was measured to confirm its effectiveness. An example is shown below. Platelet aggregation ability was measured using venous blood, PRP (platelet
rich plasma) was measured by the absorbance method (Yamazaki, Respiration and Circulation, Vol. 23, No. 9, pp. 791-798). Based on the above studies, pantethine was administered to patients with various diseases and its effects were confirmed. An example is shown below. Example Pantethine 5-dispersion 3-5g/day (3 doses) (600-1000mg/day as pantethine) for ischemic heart disease (IHD), coronary arteriosclerosis (CS), and hyperlipidemia (HL). The drug was orally administered to patients for 8 weeks, and blood was collected before administration and at 2, 4, 6, and 8 weeks after administration to measure platelet aggregation ability. The 5-minute value (%) and maximum aggregation value (%) of the aggregation ability are shown in the following table, and as can be seen from the table, it is recognized that pantethine suppresses the aggregation ability of platelets.
【表】【table】
【表】
以上述べたように、パンテチンは血小板凝集能
を抑制し、血栓の予防に有用であり、投与量とし
ては１日600〜1000mgを経口投与するのが適当で
ある。剤型としては通常は結晶セルロース、軽質
無水ケイ酸、デン粉等で散剤としたものが便利で
あるが、錠剤、その他の剤型も適宜用いてもよ
い。また、注射剤として静脈投与も可能である。
パンテチンの急性毒性はマウス経口投与におけ
るLD50として10ｇ／Kg以上であり、かなりの大
量投与においても安全度は高いと思われる。[Table] As mentioned above, pantethine suppresses platelet aggregation ability and is useful for preventing thrombosis, and the appropriate dosage is 600 to 1000 mg per day. As for the dosage form, it is usually convenient to use a powder made of crystalline cellulose, light silicic anhydride, starch, etc., but tablets and other dosage forms may also be used as appropriate. It can also be administered intravenously as an injection. The acute toxicity of pantethine is LD 50 of 10 g/Kg or more when administered orally to mice, and it is considered to be highly safe even when administered in large doses.
Claims (1)
及び軽質無水ケイ酸からなる特許請求の範囲第１
項の血栓予防剤。 ３ Ｄ−パンテチン水溶液である特許請求の範囲
第１項の血栓予防剤。[Scope of Claims] 1. Thromboprophylactic agent containing D-pantethine. 2 Claim 1 consisting of D-pantethine, starch, crystalline cellulose, and light anhydrous silicic acid
Antithrombotic agent. 3. The antithrombotic agent according to claim 1, which is an aqueous solution of D-pantethine.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP3061878A JPS54126737A (en) | 1978-03-17 | 1978-03-17 | Antithrombotic agent |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP3061878A JPS54126737A (en) | 1978-03-17 | 1978-03-17 | Antithrombotic agent |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS54126737A JPS54126737A (en) | 1979-10-02 |
| JPS6213325B2 true JPS6213325B2 (en) | 1987-03-25 |
Family
ID=12308846
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP3061878A Granted JPS54126737A (en) | 1978-03-17 | 1978-03-17 | Antithrombotic agent |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS54126737A (en) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE472321T1 (en) * | 2002-09-30 | 2010-07-15 | Daiichi Seiyaku Co | PARTICLE PRODUCT CONTAINING PANTETHINE |
| JP5080011B2 (en) * | 2005-02-28 | 2012-11-21 | 第一三共ヘルスケア株式会社 | Composition for increasing glutathione peroxidase activity |
-
1978
- 1978-03-17 JP JP3061878A patent/JPS54126737A/en active Granted
Also Published As
| Publication number | Publication date |
|---|---|
| JPS54126737A (en) | 1979-10-02 |
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