A pharmaceutical composition for treating cerebral apoplexy and acute cerebral infarction

A composition and technology for cerebral apoplexy, applied in the field of biomedicine, can solve the problems of short half-life, undetectable Apelin prototype drug, hindering the development of Apelin clinical therapeutic drugs, etc., and achieve the effect of alleviating neurological dysfunction and reducing the volume of cerebral infarction

Active Publication Date: 2022-03-25
温州医科大学慈溪生物医药研究院 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the half-life of Apelin in the body is extremely short. It has been reported in the literature that the prototype drug of Apelin cannot be detected in the body after 5 minutes of intravenous injection of Apelin solution (Hypertension 2016, 68: 365-377)
The defect of short half-life has seriously hindered the development of Apelin clinical therapeutic drugs

Method used

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  • A pharmaceutical composition for treating cerebral apoplexy and acute cerebral infarction
  • A pharmaceutical composition for treating cerebral apoplexy and acute cerebral infarction
  • A pharmaceutical composition for treating cerebral apoplexy and acute cerebral infarction

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1: The solid-phase synthesis of 2-(4-chlorophenyl)-2,2-difluoroacetic acid-QRPRLSHKGPMPF

[0023] (1) Weigh 1mmol of 2-cl-Trt resin in a solid-phase synthesizer, add 15mL of anhydrous dichloromethane (hereinafter referred to as DCM), place on a shaker and shake for 5min to fully swell the 2-Cl-Trt resin ;

[0024] (2) DCM is removed from the solid-phase synthesizer equipped with 2-Cl-Trt resin with ear washing ball;

[0025] (3) Dissolve 0.75 mmol of Fmoc-Phe in 10 mL of anhydrous DCM, add 0.75 mmol of DIPEA, then transfer to the above-mentioned solid-phase synthesizer, add 0.75 mmol of DIPEA, and react at room temperature for 1 h;

[0026] (4) Sealing: Remove the reaction solution in the solid-phase synthesizer with ear wash balls, then wash with 10 mL of anhydrous DCM for 1 min each time, and wash 5 times in total, and add the prepared volume ratio of anhydrous DCM: DIPEA: methanol =17:1:2 solution 20mL, react at room temperature for 10min;

[0027] (5) ...

Embodiment 2

[0032] Embodiment 2: Experiment of the biological half-life of the target active peptide in rats

[0033] (1) Experimental animal information

[0034] SPF grade SD rats, 16 males, weighing 190g to 210g, were provided by the Experimental Animal Center of Wenzhou Medical University.

[0035] (2) Dosing regimen and plasma sample collection and processing

[0036] Intravenous administration, the dosage was 10mg / kg, the rats were randomly divided into positive control [Pyr1]-Apelin-13 solution group, experimental group 2-(4-chlorophenyl)-2,2-di Fluoroacetic acid-QRPRLSHKGPMPF solution group, a total of 2 groups (n=8), fixed rats, administered through the tail vein. At different time points after administration, 0.2 mL of whole blood was collected through the jugular vein cannula and placed in a 1.5 mL LEDTA-2K anticoagulant centrifuge tube. ) to seal the tube for smooth collection at the next time point. The blood sample was centrifuged at 4000g for 5 minutes at 4°C, the plasma...

Embodiment 3

[0042] Example 3: The treatment of 2-(4-chlorophenyl)-2,2-difluoroacetic acid-QRPRLSHKGMPPF for cerebral apoplexy and cerebral infarction

[0043] 3.1 Experimental materials

[0044] Experimental Animals and Breeding

[0045] 2-3 months old, male C57BL / 6J mice, 24-28g, provided by Experimental Animal Center of Wenzhou Medical University. Raising conditions: the room temperature is between 22-24° C., the humidity is between 40-70%, the lighting time is 12 hours alternately between light and dark, and free to drink and eat.

[0046] 3.2 Modeling of tMCAo mice: Mice were fasted for 8-10 hours before surgery and had free access to water. Mice were anesthetized by intraperitoneal injection of chloral hydrate (350 mg / kg). According to the Longa method, the right middle cerebral artery occlusion (middle cerebral artery occlusion) in the monofilament lumen was prepared with 6-0 silica gel-coated nylon monofilament suture (Doccol Corp). , MCAO) model. After 60 minutes of ischemia, ...

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Abstract

The invention relates to a pharmaceutical composition for treating cerebral apoplexy and acute cerebral infarction, which uses active peptide Apelin as an active ingredient, and the structure of the active peptide Apelin is 2-(4-chlorophenyl)-2,2- Difluoroacetic acid‑QRPRLSHKGPMPF. The pharmaceutical composition of the present invention has bidirectional therapeutic effects on ischemic stroke, can relieve ischemic stroke neurological dysfunction, and reduce cerebral infarction volume.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to a pharmaceutical composition for treating cerebral apoplexy and acute cerebral infarction. Background technique [0002] Cerebral stroke is a group of diseases with cerebral ischemia and hemorrhagic injury symptoms as the main clinical manifestations, also known as stroke or cerebrovascular accident, with a very high mortality rate and disability rate, mainly divided into hemorrhagic stroke ( Cerebral hemorrhage or subarachnoid hemorrhage) and ischemic stroke (cerebral infarction, cerebral thrombosis), with cerebral infarction being the most common. Cerebral stroke is one of the most important fatal diseases in the world, with acute onset and high mortality rate. [0003] Cerebral stroke or cerebral apoplexy is a disease characterized by loss of local neurological function caused by disturbance of blood circulation in the brain. The incidence of ischemic stroke ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K38/10A61P9/10A61P25/00
CPCA61K38/10A61P9/10A61P25/00
Inventor 肖健张宏宇龚方华孔晓霞
Owner 温州医科大学慈溪生物医药研究院
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