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Medicament composition containing tirofiban and antithrombotic medicament active component

A technology for tirofiban and active ingredients, applied in the field of pharmaceutical compositions, can solve problems such as difficulty in oral administration, and achieve the effects of solving difficulty in oral administration, improving medication safety, and improving compliance

Inactive Publication Date: 2009-01-14
GRAND PHARM (CHINA) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it is relatively difficult to take oral medication for complications of coronary thrombosis during interventional surgery, especially for comatose or unconscious high-risk ACS patients, which is an urgent clinical problem to be solved

Method used

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  • Medicament composition containing tirofiban and antithrombotic medicament active component
  • Medicament composition containing tirofiban and antithrombotic medicament active component
  • Medicament composition containing tirofiban and antithrombotic medicament active component

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Drug compatibility and stability of embodiment 1 tirofiban and arginine aspirin injection

[0031] We combine tirofiban and arginine aspirin to prepare tirofiban-arginine aspirin injection, specification: 100ml / bottle, each bottle contains tirofiban hydrochloride 5.618mg (in the form of anhydrous tirofiban Class 5mg), arginine aspirin 393.3mg (equivalent to acetylsalicylic acid 200mg) and sodium chloride 0.9g.

[0032] prescription:

[0033] Tirofiban Hydrochloride 56.18mg

[0034] Lysine Aspirin 3.933g

[0035] Sodium chloride 9g

[0036] Water for injection to 1000ml

[0037]

[0038] A total of 10 bottles of injection were made

[0039] Preparation Process:

[0040] Weigh sodium chloride according to the prescription amount, add it to 100ml of water for injection, stir until completely dissolved; weigh 0.3% activated carbon in solution, stir well, heat and boil for 15 minutes, after cooling, filter out the activated carbon; a...

Embodiment 2

[0051] Embodiment 2 The injection of prescription of the present invention is to rat right carotid artery-vein bypass thrombosis experiment experimental drug:

[0052] normal saline

[0053] Lysine Aspirin

[0054] Tirofiban

[0055] Tirofiban-lysine aspirin injection (divided into large, medium and small dose groups)

[0056] Experimental animals: 60 Wistar rats, half male and half male, body weight 250±10g.

[0057] Rats were randomly divided into 6 groups, 10 in each group. Drug dosage is (A) blank control (0.9% sodium chloride solution), (B) lysine aspirin group (240.0mg·kg -1 ), (C) tirofiban group (8.0mg·kg -1 ), (D) tirofiban-lysine aspirin group (2.0 / 160.0mg·kg -1 ), (E) tirofiban-lysine aspirin group (4.0 / 240.0mg·kg -1 ), (F) tirofiban-lysine aspirin group (8.0 / 320.0mg·kg -1 ).

[0058] experimental method:

[0059] Animals in each group were administered intraperitoneally according to the above dose, and the blank group was given the same amount of normal s...

Embodiment 3

[0064] Example 3 Tirofiban-Arginine Aspirin Injection Measures Thrombosis Time in Rats

[0065] experimental method:

[0066] Rats were taken, and the administration was the same as before, once a day for 3 consecutive days, and 30 minutes after the last administration, chloral hydrate (350 mg·kg -1 ) anesthetized, fixed in the supine position, separated the right common carotid artery about 15mm, placed the stimulating electrode and temperature sensor probe of the in vivo thrombosis instrument on the artery, stimulated the blood vessel with 2mA current to damage the arterial endothelium, recorded the result of thrombus in the arterial lumen The time it takes to block blood flow is called the thrombosis time. The measurement results are shown in Table 4:

[0067] The impact of table 4 on the time of thrombus formation in rats (X±S, n=10)

[0068]

[0069] Compared with normal saline group, *P<0.05, **P<0.01

[0070] The results showed that both group E and group F conta...

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Abstract

The invention relates to a medicine composition, in particular to the medicine composition containing tirofian and active antithrombotic component. The active components are the tirofiban and aspirin. The medicine composition contains 1 to 50mg of the tirofiban and the aspirin with 20 to 800mg of effective dose. Compared with using the tirofiban or the aspirin separately, the blooding time of the invention is prolonged, so the occurrence rate of blooding and thrombus is reduced. In addition, the medicine composition solves a problem that the medicine is difficult to be taken orally for the part of high-risk ACS patients who can not take the medicine orally or have poor compliance. Therefore, the medicine composition is beneficial to improving the compliance of the patients and the safe use of the medicine, etc.

Description

technical field [0001] The invention relates to a pharmaceutical composition, in particular to a pharmaceutical composition containing tirofiban and active ingredients of antithrombotic drugs, wherein the active ingredients are tirofiban and aspirin. Background technique [0002] The incidence of coronary artery thrombosis and cerebral arterial thrombosis-based vascular embolism is currently on the rise, and seriously endangers people's health. Platelet-rich thrombus formation in coronary arteries plays an important role in the pathology of both acute coronary syndrome (ACS) and major complications after cardiac intervention (PCI). ACS represented by unstable angina pectoris (UAP) and myocardial infarction (MI) is the main cause of coronary artery disease morbidity and death. ACS has a common pathophysiological basis, that is, the rupture of coronary atherosclerotic plaque, the formation of thrombus, the partial or complete occlusion of coronary vessels, resulting in myocar...

Claims

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Application Information

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IPC IPC(8): A61K31/616A61K31/4465A61P7/02
Inventor 黄璐谢国范周建明朱毅赵蓉
Owner GRAND PHARM (CHINA) CO LTD
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