Bicyclo-ethanol submicron emulsion and preparation method thereof

A technology of bicyclol and submicron emulsion, which is applied in the field of medicine, can solve the problems of local irritation and allergic adverse reactions, poor physical and chemical stability, induced superhemolysis, etc., and achieve the improvement of blood drug concentration and liver drug distribution concentration , good stability, low toxicity and side effects

Active Publication Date: 2009-09-09
INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Various methods can improve the solubility of bicyclic alcohol, but crystallization and chemical degradation are prone to occur during the storage process, and the physical and chemical stability are poor
In addition, after a large amount of surfactants and organic solvents are applied to the human body, they may cause hyperhemolysis, local irritation and allergic adverse reactions.

Method used

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  • Bicyclo-ethanol submicron emulsion and preparation method thereof
  • Bicyclo-ethanol submicron emulsion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] [Prescription composition] based on 1000ml

[0047] Substance

[0048] [Preparation method] Take glycerin and water for injection, heat to 40-60℃, add refined lecithin and poloxamer, put it in a tissue masher, stir at high speed to form a uniform water phase, keep it warm; take bicyclic alcohol and α vitamin E and oleic acid are added to soybean oil and heated to 40-60°C to prepare the oil phase. Under stirring conditions, the water phase is slowly added to the oil phase, and the tissue masher is stirred at high speed to form uniform colostrum. The colostrum is quickly transferred to a high-pressure homogenizer to homogenize, the particle size is controlled below 500nm, and all the emulsions are collected to obtain.

Embodiment 2

[0050] [Prescription composition] based on 1000ml

[0051] Substance

[0052] [Preparation method] Take glycerin and water for injection, heat to 40-60℃, add poloxamer, stir to make the water phase, keep it warm; take bicyclic alcohol, α vitamin E, refined lecithin and oleic acid, and add to Heat the soybean oil to 40-60°C, place it in a tissue masher, and stir at high speed to form a uniform oil phase. Under stirring conditions, the water phase is slowly added to the oil phase, and the tissue masher is stirred at high speed to form uniform colostrum. The colostrum is quickly transferred to a high-pressure homogenizer to homogenize, the particle size is controlled below 500nm, and all the emulsions are collected to obtain.

Embodiment 3

[0054] [Prescription composition] based on 1000ml

[0055] Substance

[0056] [Preparation method]: Add mannitol instead of glycerin to the water phase, and the other steps are the same as in Example 1.

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Abstract

The invention discloses a bicyclo-ethanol submicron emulsion and a preparation method thereof. the preparation method comprises the steps of dissolving bicyclo-ethanol and emulsifying agent in an oil phase, adding an assistant for emulsifying agent, a stabilizing agent, other additive and a water phase, adopting a cutting dispersing and high-pressure homogeneous emulsification process to prepare an oil-in-water(O / W) submicron emulsion with the average grain diameter below 500 nm and drug loading dosage between 0.01mg / ml and 5mg / ml. The bicyclo-ethanol submicron emulsion is injected through vein and used for treating medium and serious hepatitis. The prepared submicron emulsion does not contain solubilizer such as Tween-80 or organic solvent, can be mixed with glucose injection, physiological saline or distilled water according to random proportion, and can not easily generate insoluble particulates when stored, used or matched with other components, thereby having high security and good stability. The invention also relates to various preparations of the bicyclo-ethanol submicron emulsion.

Description

Technical field [0001] The invention relates to a bicyclic alcohol submicroemulsion and a preparation method thereof, and belongs to the technical field of medicine. Background technique [0002] Bicyclol is an innovative anti-chronic hepatitis drug with independent intellectual property rights developed by the Institute of Materia Medica, Chinese Academy of Medical Sciences. Bicyclol bulk medicine and its tablets were launched in 2002 for the treatment of chronic viral hepatitis, which can significantly improve liver function and reduce transaminase , At the same time, it has a certain antiviral effect, it is not easy to rebound after stopping the drug, and the safety is good. Because bicyclol is a poorly soluble drug, the oral bioavailability of ordinary tablets is less than 9%, and the clinical application varies significantly between individuals and the efficacy is unstable. For moderate to severe patients, oral bicyclol preparations cannot achieve satisfactory therapeutic ef...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/36A61P1/16
Inventor 刘玉玲夏学军王洪亮李琳汪仁芸金笃佳
Owner INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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