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5 alpha- androstane-3 beta, 5,6 beta-triol injection and preparation method thereof

A technology of triol injections and injections, applied in the field of medicine, to achieve the effects of good stability of the liquid medicine, simple preparation process, and non-irritating liquid medicine

Active Publication Date: 2013-10-02
GUANGZHOU CELLPROTEK PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, studies have shown that cyclodextrin and its hydrophilic derivatives do not have an ideal solubilization effect on all poorly soluble drugs, and not all solubilization systems have good stability

Method used

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  • 5 alpha- androstane-3 beta, 5,6 beta-triol injection and preparation method thereof
  • 5 alpha- androstane-3 beta, 5,6 beta-triol injection and preparation method thereof
  • 5 alpha- androstane-3 beta, 5,6 beta-triol injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] Example 1: In this example, 200 tubes of androstatriol injection (specification 5ml: 40mg) were prepared.

[0015] Androstatriol 8g

[0016] Sulfobutyl-β-cyclodextrin 100 g

[0017] Make up to 1000 ml with water for injection

[0018] Preparation process: Take sulfobutyl-β-cyclodextrin, dissolve it in fresh water for injection with a prescription volume of 70%, add androstatriol, ultrasonicate at 60°C for 5-10 minutes to dissolve completely, and add an appropriate amount of pH Regulators adjust the injection solution to neutrality. Add water for injection to a sufficient amount, then add 0.05% activated carbon and stir for 15 minutes, let cool, and filter through a 0.22 μm microporous membrane. The filtrate is potted into 5 ml injection solution and sterilized at 121°C for 15 minutes.

Embodiment 2

[0019] Example 2: In this example, 200 androstatriol injections (specification 5ml: 90mg) were prepared

[0020] Androstatriol 18 g

[0021] Sulfobutyl-β-cyclodextrin 400 g

[0022] Add water for injection to 2000 ml

[0023] Preparation process: Take sulfobutyl-β-cyclodextrin, dissolve it in fresh water for injection with 70% of the prescription amount, stir in a water bath at 80°C for 15-30 minutes to completely dissolve, and add an appropriate amount of pH regulator to adjust the injection to neutral. sex. Add water for injection to a sufficient amount, then add 0.1% activated carbon and keep warm at 60°C for 15 minutes, let cool, and filter through a 0.22 μm microporous membrane. The filtrate was encapsulated to obtain 5 ml injection. Sterilize at 121°C for 15 minutes.

Embodiment 3

[0024] Example 3: In this example, 200 androstatriol injections (specification 5ml: 140mg) were prepared

[0025] Androstatriol 28 g

[0026] Sulfobutyl-β-cyclodextrin 300 g

[0027] Make up to 1000 ml with water for injection

[0028] Preparation process: Take sulfobutyl-β-cyclodextrin, dissolve it in fresh water for injection with 70% of the prescription volume, add androstatriol, ultrasonicate for 5-10 minutes to completely dissolve, and add an appropriate amount of pH regulator to make the injection Neutral. Add water for injection to a sufficient amount, then add 0.1% activated carbon and stir for 15 minutes, let cool, and filter through a 0.22 μm microporous membrane. The filtrate was potted to obtain 5ml injection. Sterilize at 115°C for 30 minutes.

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Abstract

The invention provides a 5 alpha- androstane-3 beta, 5, 6 beta-triol injection and a preparation method thereof. The injection comprises 5 alpha- androstane-3 beta, 5, 6 beta-triol, solvent for injection, and soluble excipient, which contains sulfobutyl-beta-cyclodextrin. In the 5 alpha- androstane-3 beta, 5, 6 beta-triol injection, sulfobutyl-beta-cyclodextrin is taken as a solubilizer, not only solubility of androstane triol is improved, and problems of instable clarity and irritation of androstane triol are solved, but also isoosmotic adjusting agent does not need to be added in to the injection or in application, and hemolysis phenomenon does not appear. Furthermore, the applicant discovers that solubilization effect of sulfobutyl-beta-cyclodextrin to androstane triol is better than that of hydroxypropyl-beta-cyclodextrin, is larger than 30 mg / ml, and no crystal precipitates after being diluted with water.

Description

technical field [0001] The invention relates to the field of medical technology, in particular to a 5α-androsta-3β,5,6β-triol injection (including liquid injection and solid 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. However, due to the low solubility of androstatriol in water, although commonly used non-aqueous solvents and mixed solvents thereof can improve its solubility, they all have greater irritation, and there is a phenomenon of precipitation after dilution with water, thereby affecting the preparation. The efficacy and safety of androstatriol limit the clinical application of androstatriol. [0003] Cyclodextrin has a cylindrical space structure, the inner cavity is hydrophobic, and the two ends are hydrophilic. Its special structure can embed insoluble drugs or groups into its molecular cavity in the form of non-covalent...

Claims

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Application Information

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IPC IPC(8): A61K47/40A61K31/565A61K9/19A61K9/08A61P25/00
Inventor 胡海燕蔡婕王亚龙王亚娜林穗珍石海涛
Owner GUANGZHOU CELLPROTEK PHARMA