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Injection dosage form of clopidogrel, and preparation method and application thereof

A clopidogrel and injection technology, applied in the field of clopidogrel injection formulation, preparation and use, can solve the problems of lack, slow onset of tablet effect, increased bleeding risk, etc., and achieve the effects of increasing solubility and improving stability

Pending Publication Date: 2020-04-24
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, clopidogrel still has the following problems: ①The tablet has a slow onset of action, and the anti-platelet aggregation effect will not be produced until about 6 hours after taking it, which is the main defect of clopidogrel when it is used in emergency PCI for acute myocardial infarction; Irreversible, and the recovery time of platelet function is longer (5-7 days), which may affect other treatment effects of patients. For patients undergoing coronary artery bypass grafting (CABG), the drug should be stopped for at least 5-7 days
Therefore, the absence of a loading dose of clopidogrel does not increase bleeding risk if cardiac surgery is decided

Method used

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  • Injection dosage form of clopidogrel, and preparation method and application thereof
  • Injection dosage form of clopidogrel, and preparation method and application thereof
  • Injection dosage form of clopidogrel, and preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0034] (1) Synthesis and characterization of mPEG-PLA

[0035] Take 10g of mPEG 2000 and lactide each, place them in a 250mL two-neck bottle, and slowly raise the temperature to 135°C, and cool down to 110°C after mPEG2000 and lactide are completely melted. Add 20% (v / v) toluene solution of stannous octoate (the addition of stannous octoate is 0.25% of the total weight of the reactant) as a catalyst, after magnetic stirring and mixing, vacuum remove toluene and residual moisture until the reaction solution has no bubbles generated, heated to 140°C, and reacted for 6h under the protection of nitrogen. After the reaction was completed, after cooling to room temperature, an appropriate amount of dichloromethane was added to the reactant to dissolve, precipitated with low-temperature anhydrous ether, and filtered under reduced pressure to obtain a white filter cake. The purification was repeated 3 times, and the obtained product was vacuum-dried at room temperature for 24 hours. ...

Embodiment 2

[0039] Synthesis of clopidogrel-encapsulated mPEG-PLA micellar nanosystem: Precisely weigh 40mg of clopidogrel and 100mg of mPEG-PLA into a vial, dissolve them ultrasonically with an appropriate amount of methanol, transfer them to an eggplant-shaped bottle, and spin evaporate to the solvent at 40°C. Volatilize and completely form a film, then add 5 mL of up water to hydrate, and pass through a 0.22 μm filter membrane to obtain a clopidogrel micellar solution.

[0040] The experimental steps and conditions for the synthesis and characterization of mPEG-PLA are the same as in Example 1.

Embodiment 3

[0042] Synthesis of clopidogrel-encapsulated mPEG-PLA micellar nanosystem: Precisely weigh 60mg of clopidogrel and 100mg of mPEG-PLA into a vial, dissolve them ultrasonically with an appropriate amount of methanol, transfer them to an eggplant-shaped bottle, and spin evaporate to the solvent at 40°C Volatilize and completely form a film, then add 5 mL of up water to hydrate, and pass through a 0.22 μm filter membrane to obtain a clopidogrel micellar solution.

[0043] The experimental steps and conditions for the synthesis and characterization of mPEG-PLA are the same as in Example 1.

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Abstract

The invention discloses an injection dosage form of clopidogrel, and a preparation method and an application thereof. The injection dosage form of clopidogrel adopts a micelle nano-system as a medicine loading system. The micelle nano-system is prepared from an mPEG-PLA block copolymer and clopidogrel a through a thin film dispersion method. The clopidogrel injection form can realize the advantages of high solubility, quick release, quick drug effect and the like, and can be applied to the preparation of drugs for treating platelet aggregation related diseases and drugs for treating diseases with pharmacological effects on clopidogrel.

Description

technical field [0001] The invention relates to a pharmaceutical dosage form, a preparation method and an application, in particular to an injection dosage form, a preparation method and an application of clopidogrel. Background technique [0002] Acute coronary syndrome (ACS) is a common serious cardiovascular disease, a group of clinical syndromes based on the rupture or erosion of coronary atherosclerotic plaque, followed by the formation of complete or incomplete occlusive thrombus. Including unstable angina (UA), acute ST-segment elevation myocardial infarction (STEMI) and acute non-ST-segment elevation myocardial infarction (NSTEMI). When the coronary blood flow cannot meet the needs of myocardial metabolism, it will cause acute and temporary ischemia and hypoxia of the myocardium, resulting in angina pectoris. Coronary atherosclerosis can cause narrowing of the lumen of one or more vessels and insufficient myocardial blood supply. Once the blood supply is sharply red...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/4365A61K47/34A61P9/10A61P9/00
CPCA61K9/0019A61K9/1075A61K31/4365A61K47/34A61P9/00A61P9/10
Inventor 涂家生孙春萌孙平平
Owner CHINA PHARM UNIV
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