Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Injection dosage form, preparation method and purpose of clopidogrel and salt thereof

A technology of clopidogrel and injection, applied in the direction of non-active ingredient medical preparations, medical preparations containing active ingredients, pharmaceutical formulations, etc., can solve the irreversible anti-platelet aggregation effect, insufficient threshold of active metabolite formation, tablet Slow onset and other issues, to achieve the effect of rapid anti-platelet aggregation, rapid anti-platelet, and high clinical safety

Inactive Publication Date: 2020-08-25
FANTAI INST OF CHEM MEDICINES NANJING
View PDF5 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are the following problems in the use of clopidogrel: 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 the emergency PCI of acute myocardial infarction; The aggregation is irreversible, and the recovery time of platelet function is longer (5-7 days), which may affect other therapeutic effects of patients. For patients undergoing coronary artery bypass grafting (CABG), the drug should be discontinued for at least 5-7 days
Although MDCO-157 can improve the stability of clopidogrel against hydrolytic degradation, thermal degradation and photodegradation, the threshold for the generation of active metabolites after injection administration is insufficient, and the effect of inhibiting platelets cannot be fully inhibited until the dose is increased to 300 mg, and it is not good Responses were significantly greater than oral formulations
The low solubility of clopidogrel in water at neutral pH makes it very difficult to develop bioavailable and physically stable injectable products

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Injection dosage form, preparation method and purpose of clopidogrel and salt thereof
  • Injection dosage form, preparation method and purpose of clopidogrel and salt thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] (1) Synthesis and characterization of mPEG-PDLLA

[0029] 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

[0033] Synthesis of mPEG-PDLLA micellar nanosystems encapsulating clopidogrel and its salts: Precisely weigh 20 mg of clopidogrel and its salts and 140 mg of mPEG-PDLLA in a vial, ultrasonically dissolve them with an appropriate amount of methanol, and transfer them to an eggplant-shaped bottle , 40°C rotary evaporation until the solvent evaporates and the film is completely formed, then add 2 mL of up water to hydrate, and pass through a 0.22 μm filter membrane to obtain the micellar injection of clopidogrel and its salt.

[0034] The experimental steps and conditions for the synthesis and characterization of mPEG-PDLLA are the same as in Example 1.

Embodiment 3

[0036] Synthesis of mPEG-PDLLA micellar nanosystems loaded with clopidogrel and its salts: Precisely weigh 20 mg of clopidogrel and 200 mg of mPEG-PDLLA into a vial, dissolve them in an appropriate amount of methanol ultrasonically, transfer them to an eggplant-shaped bottle, and keep at 40°C Rotary evaporate until the solvent is evaporated and the film is completely formed, then add 4 mL of up water for hydration, and pass through a 0.22 μm filter membrane to obtain a micellar injection of clopidogrel and its salt.

[0037] The experimental steps and conditions for the synthesis and characterization of mPEG-PDLLA are the same as in Example 1.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
particle sizeaaaaaaaaaa
Login to View More

Abstract

The invention discloses an injection dosage form, preparation method and purpose of clopidogrel and salt thereof. According to the injection of the clopidogrel and salt thereof, the clopidogrel and the salt thereof are used as active components, an amphipathic block copolymer is used as a medicine carrier, wherein the amphipathic block copolymer is selected from a diblock copolymer and a triblockcopolymer, a hydrophilic region of the amphipathic block copolymer is selected from polyethylene glycol, mono-methyl polyethylene glycol, polyvidone, chitosan and polymethacrylic acid, and a hydrophobic region of the amphipathic block copolymer is selected from polyoxypropylene, polystyrene, polyaminoacid, polyester and biodegradation type high molecular materials. The injection dosage form of theclopidogrel and the salt thereof disclosed by the invention is good in stability, can quickly produce high-concentration active metabolism products, and can be applied to preparation of medicines fortreating platelet aggregation relevant diseases and medicines having pharmacodynamics effects on the 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 and a salt thereof. 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 su...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K47/34A61K31/4365A61P9/10A61P7/02C08G63/78C08G63/664
CPCA61K9/0019A61K9/08A61K31/4365A61K47/34A61P7/02A61P9/10C08G63/664C08G63/78
Inventor 涂家生孙春萌吴建梅唐宝强孙平平
Owner FANTAI INST OF CHEM MEDICINES NANJING
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com