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5α-androsta-3β, 5,6β-triol injection and preparation method thereof

The technology of a triol injection and androstatriol, which is applied in the field of medicine, can solve problems such as kidney side effects, and achieve the effects of improving solubility and increasing surface area.

Active Publication Date: 2017-05-10
GUANGZHOU CELLPROTEK PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, androstatriol solubilized by some of these substituted β-cyclodextrins has undesired side effects on the kidneys, especially mild to severe vacuolation of renal tubular epithelial cells in the renal cortex.

Method used

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  • 5α-androsta-3β, 5,6β-triol injection and preparation method thereof
  • 5α-androsta-3β, 5,6β-triol injection and preparation method thereof
  • 5α-androsta-3β, 5,6β-triol injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Weigh about 50mg of soybean lecithin, put it in a 50ml round bottom flask, add about 150mg of sodium deoxycholate, and add 7.5ml of ethanol solution (to make the bile salt concentration about 20mg / ml), and ultrasonically make it completely dissolved to form a blank micellar solution. Accurately weigh 20 mg of androstatriol, place it in a round bottom flask, and ultrasonically disperse it evenly. Then use a rotary evaporator to remove ethanol until there is no alcohol smell, make it form a transparent film, disperse it with 2ml of water for injection, and filter through a 0.22 μm microporous membrane to obtain androstatriol mixed micellar injection. The particle size measured by NANO ZS-90 laser particle size analyzer (Malvern, UK) is about 10-20nm.

Embodiment 2

[0031] Weigh about 66mg of egg yolk lecithin, put it in a 50ml round bottom flask, add about 133mg of sodium hyocholate, and add 7.0ml of methanol solution (to make the bile salt concentration about 20mg / ml), and ultrasonically make it completely dissolved to form a blank micellar solution. Accurately weigh 20 mg of androstatriol, place it in a round bottom flask, and ultrasonically disperse it evenly. Then use a rotary evaporator to remove ethanol until there is no alcohol smell, make it form a transparent film, disperse it with 2ml of water for injection, and filter through a 0.22 μm microporous membrane to obtain androstatriol mixed micellar injection.

Embodiment 3

[0033] Weigh about 66mg of soybean lecithin, put it in a 50ml round bottom flask, add about 133mg of sodium glycocholate, and add 7.0ml of chloroform:methanol 1:1 solution (make the bile salt concentration about 20mg / ml) , and ultrasonically dissolve it completely to form a blank micellar solution. Accurately weigh 20 mg of androstatriol, place it in a round bottom flask, and ultrasonically disperse it evenly. Then use a rotary evaporator to remove ethanol until there is no alcohol smell, make it form a transparent film, disperse it with 2ml of water for injection, and filter through a 0.22 μm microporous membrane to obtain androstatriol mixed micellar injection.

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Abstract

A 5alpha-androstane-3beta,5,6beta-triol injection and a preparing method thereof are provided. The injection comprises an injection solvent, 5alpha-androstane-3beta,5,6beta-triol, phospholipid and cholate, wherein the weight ratio of the 5alpha-androstane-3beta,5,6beta-triol, the phospholipid and the cholate is 1:1-15:1.5-45, and the phospholipid and the cholte form mixed micelle in the injection. The mixed micelle largely increases solubility of the 5alpha-androstane-3beta,5,6beta-triol. The mixed micelle injection is clear and transparent, and is a clear liquid having a color ranging from no color to faint yellow. The particle size of the injection is 10-100 nm.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a 5α-androsta-3β,5,6β-triol injection and a preparation method thereof. Background technique [0002] 5α-androsta-3β,5,6β-triol (hereinafter referred to as androstatriol) is a newly discovered neuroprotective agent, and its structural formula is: [0003] . [0004] Due to the low solubility of androstatriol in water, although commonly used non-aqueous solvents and their mixed solvents can improve its solubility, they all have greater irritation, and there is a phenomenon of precipitation after dilution with water, thereby affecting the preparation. Efficacy and safety limit the clinical application of androstatriol. [0005] Studies have shown that some substituted β-cyclodextrins can play a good role in solubilization, which provides an alternative solution for improving the solubility of androstatriol. However, androstatriol solubilized by some of these substituted β-cyc...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K9/107A61K31/568A61K47/24A61K47/28A61P27/02
Inventor 林穗珍胡海燕蔡婕石海涛王亚娜银巍邱朋新黄奕俊
Owner GUANGZHOU CELLPROTEK PHARMA