Alda-1 solution as well as preparation method and application thereof

A solution and solvent technology, used in the field of medicine, can solve the problems of low solubility of Alda-1 and the inability of the dissolution method to be used in clinical applications.

Pending Publication Date: 2020-05-15
SHANDONG UNIV QILU HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Therefore, the object of the present invention is to solve the problem that Alda-1 solubility is low and existing dissolving method can't be used clinically, a kind of Alda-1 solution and its preparation method and application thereof are provided, and this sol...

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  • Alda-1 solution as well as preparation method and application thereof
  • Alda-1 solution as well as preparation method and application thereof
  • Alda-1 solution as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] The preparation of embodiment 1 Alda-1 injection

[0052] Solvents: ethanol, polyethylene glycol 400, normal saline

[0053] Accurately weigh 20mg of Alda-1, add it to a clean 5ml ep tube, add ethanol to the ep tube, and use ultrasonic vibration for 3 minutes; add peg400 and normal saline, mix well, and sterilize to get ready. Wherein, the consumption situation of solvent is shown in Table 1.

[0054] Table 1 Solvent consumption situation

[0055] solvent ethanol polyethylene glycol 400 normal saline Preparation Example 1 1mL 600μL 400μL Preparation example 2 1mL 600μL 800μL Preparation example 3 1mL 1mL 400μL Preparation Example 4 1mL 1mL 800μL Preparation Example 5 1mL 1mL 600μL

[0056] The injections prepared in Preparation Examples 1-5 are all colorless transparent liquids, and their pH is in the range of 5-6.8. The injections prepared in Preparation Examples 1-5 above are stored at room...

experiment example 1

[0060] Experimental example 1, Alda-1 injection blood vessel stimulation test

[0061] Experimental method: Get 3 healthy rabbits, inject Alda-1 injection stock solution (taken from Preparation Example 1) (stock solution group), Alda-1 injection stock solution (preparation example 1 ) normal saline 1:1 dilution (1:1 dilution group), 0.9% sodium chloride injection (NS group), the injection volume is 1mL / kg, each adopts its own control, and the right ear margin is administered iv, etc. Volume 0.9% sodium chloride injection, 1 time / d, continuous administration for 3 days. 48 hours after the last administration, observe with the naked eye whether there is redness, swelling, hyperemia and other irritations at the injection site, and then kill the animal, and take three 1cm blood vessels and surrounding tissues continuously from the ear vein injection point to the centripetal direction, and add 4% neutral formaldehyde solution Fixed, routinely dehydrated, embedded in paraffin, ...

experiment example 2

[0070] Experimental Example 2, Alda-1 Injection Hemolytic Test

[0071] Experimental method: take 1 healthy rabbit, take about 20mL of blood from the heart, place it in a triangular flask containing glass beads and shake it for 5 minutes to remove fibrin and make it into defibrinated blood. Transfer the defibrillated blood into a centrifuge tube, add normal saline and shake gently, then centrifuge at 1500r / min for 15min, discard the supernatant, add normal saline to mix and centrifuge, repeat 2-3 times, until the supernatant does not appear red, The obtained erythrocytes were diluted with physiological saline according to their volume to form a 2% suspension for later use. Take a clean centrifuge tube and add different volumes of Alda-1 injection stock solution (preparation example 1) in sequence, i.e. the injection group, 2 tubes for each concentration in parallel, and set a negative control (normal saline) and a positive control (purified water) at the same time. After al...

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Abstract

The invention provides an Alda-1 solution as well as a preparation method and application thereof. According to the solution, Alda-1 is adopted as an active component, ethanol, polyethylene glycol 400and normal saline are adopted as solvents, and the problems that Alda-1 is poor in solubility and cannot be clinically used can be solved. The Alda-1 solution provided by the invention can be used asan injection for intravenous injection, heart functions can be well improved, in addition, the stability is good, the security is high, no hemolysis can be caused, and in addition, the solution has no conspicuous irritation to blood vessels in intravenous injection with dilution of the normal saline in a ratio of 1:1.

Description

technical field [0001] The invention relates to the field of medicine, in particular to Alda-1 solution and its preparation method and application. Background technique [0002] The information disclosed in this background section is only intended to increase the understanding of the general background of the present invention, and is not necessarily taken as an acknowledgment or any form of suggestion that the information constitutes the prior art already known to those skilled in the art. [0003] Aldehyde dehydrogenase 2 (ALDH2) gene is located on chromosome 12q24, including 13 exons and 12 introns, consisting of 43,437 base pairs, and can encode 517 amino acids. ALDH2 is located in mitochondria and contains three A tetrameric enzyme with a structural domain that metabolizes various endogenous and exogenous aldehydes; it is mainly distributed in tissues such as liver, heart, and brain. The wild-type ALDH2 gene is denoted as ALDH2*1, and the gene with a single base mutati...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/357A61K47/10A61P9/04A61P9/10
CPCA61K9/0019A61K9/08A61K31/357A61K47/10A61P9/04A61P9/10
Inventor 陈玉国翟光喜徐峰王甲莉郑博元付曼菲
Owner SHANDONG UNIV QILU HOSPITAL
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