SU621148A1 - Substance exhibiting anticoagulating activity - Google Patents
Substance exhibiting anticoagulating activity Download PDFInfo
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- SU621148A1 SU621148A1 SU731979785A SU1979785A SU621148A1 SU 621148 A1 SU621148 A1 SU 621148A1 SU 731979785 A SU731979785 A SU 731979785A SU 1979785 A SU1979785 A SU 1979785A SU 621148 A1 SU621148 A1 SU 621148A1
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- substance exhibiting
- anticoagulating activity
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Description
1one
Изобретение относитс к области син-i теза биологически активных .химических соединений, а именно созданию новых препаратов, предотвращающих свертывание крови, которые можно использовать в медицине.The invention relates to the field of syn-thesis of biologically active chemical compounds, namely the creation of new drugs that prevent blood clotting, which can be used in medicine.
Известен антикоагул нт крови пр мого действи - гепарин Known anticoagulant of blood of direct action - heparin
Цель изобретени - расширение арсенала веществ, обладающих антвкоагулйнтной активностью.The purpose of the invention is to expand the arsenal of substances with anti-coagulant activity.
Вещество, обладающее антикоагул нтной активностью представл ет собой оксисульфонокислое производное окисленного полиакролеина формулыThe substance with anticoagulant activity is an oxysulfonate derivative of an oxidized polyacrolein of the formula
3636
1 г окисленного полиакролеина заливают 50 мл 1О%-ного водного раствора бО. Через 2О ч удал ют избыток 502 нагреванием до температуры 50°С. Довод т рН раствора до 7 с помощью 1н. МаОН.1 g of oxidized polyacrolein is poured over 50 ml of a 1O% aqueous solution of bo. After 2 hours, the excess 502 is removed by heating to a temperature of 50 ° C. Adjust the pH of the solution to 7 with 1N. Maon.
Предлагаемое вещество обладает пр мым антикоагул нтным действием на кровь.The proposed substance has a direct anticoagulant effect on the blood.
Количественно антикоагуп нтна активность оценена титром стабилизации и проведено определение активности биологическим методом по способности вещества задерживать свертывание цитратной бараньей плазмы, вызываемое хлоридом кальций, путем сопоставлени активности испытуемого раствора антикоагул нта с активностью- стандартного препарата гепарина. Титр стабилизации вещества 1:2000, специфическа активность в единицах действи составл ет 27,6ЕДAnti-coagulant activity was quantified by a stabilization titer, and biological activity was measured by the ability of a substance to delay the coagulation of citrate mutton plasma, caused by calcium chloride, by comparing the activity of the test anticoagulant solution with that of a standard heparin preparation. The titer of stabilization of the substance is 1: 2000, the specific activity in units of action is 27.6 EDU.
Токсичность изучена на белых беспородных мышах при внутрибрюшинном введении. Летательна доза дл S0% животных ( ЬДдр) образцов препарата с активностью 27,6 ЕД составила 87О мг/кг.Toxicity was studied in white outbred mice after intraperitoneal administration. The flying dose for S0% animals (LDPE) of drug samples with an activity of 27.6 U was 87 O mg / kg.
С целью проверки антнкоагул нтного действи вещества проведены исследовани в услови х-in Vi-tv o in vivoВнутривенное введение сопровождаетс замедлением времени рекальиификации плазмы крови. Отмечено антитромбоппастиновое и антитромбиновое действие.In order to check the antinocoagulatory effect of the substance, studies have been performed under in-Vi-tv o conditions in vivo. Internal administration is accompanied by a slower recalification of blood plasma. Marked antithrombopastinovoy and antithrombin action.
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Лнтикоагул нтное действие вещества нейтрализуетс протамин-сульфатом. С фибриногеном синтетический антикоагу нт образует растворимый комплекс.The coagulant effect of the substance is neutralized by protamine sulfate. With fibrinogen, the synthetic anticoagus nt forms a soluble complex.
Двухкратное увеличение времени рекальцификации при инкубации плазмы крови -fh v-itro у вещества достигаетс при дозе 60 /мм. Внутривенное введение препарата сопровождаетс резким замедлением времени свертывани крови сразу после окончани инъекции. Дл увеличени времени свертывани до 2О мин требуетс 5 мг/кг вещества.A twofold increase in recalcification time during the incubation of blood plasma -fh v-itro in a substance is achieved at a dose of 60 / mm. Intravenous administration of the drug is accompanied by a sharp slowdown of the blood coagulation time immediately after the end of the injection. To increase the clotting time to 2 minutes, 5 mg / kg of the substance is required.
Продолжительность действи препарата составл ет 12 ч (при дозе 15мг/кг).The duration of the drug is 12 hours (at a dose of 15 mg / kg).
Длительное внутривенное введение препарата (7 дней по 5 мг/кг) приводит к повыщению антитромбиновой активности стенок аорты. Увеличиваетс также антитромбинова активность ткани сердца .Prolonged intravenous administration of the drug (7 days at 5 mg / kg) leads to an increase in the antithrombin activity of the aorta walls. The antithrombin activity of the heart tissue also increases.
Препарат нетоксичен - дозы 75О мг/кг животные перенос т хорошо.The drug is non-toxic - animals are well tolerated at a dose of 75O mg / kg.
Вещество достаточно эффективно, оказывает пр мое действие на крови, устойчиво в кислых средах и при хранении.The substance is quite effective, has a direct effect on the blood, is stable in acidic environments and during storage.
Получают из дешевого сырь .Receive from cheap raw materials.
Claims (1)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SU731979785A SU621148A1 (en) | 1973-12-21 | 1973-12-21 | Substance exhibiting anticoagulating activity |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SU731979785A SU621148A1 (en) | 1973-12-21 | 1973-12-21 | Substance exhibiting anticoagulating activity |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SU621148A1 true SU621148A1 (en) | 1980-01-05 |
Family
ID=20570586
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SU731979785A SU621148A1 (en) | 1973-12-21 | 1973-12-21 | Substance exhibiting anticoagulating activity |
Country Status (1)
| Country | Link |
|---|---|
| SU (1) | SU621148A1 (en) |
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1973
- 1973-12-21 SU SU731979785A patent/SU621148A1/en active
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