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
CN101524329AActive Publication Date: 2009-09-09INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI +1
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
Publication Date
2009-09-09

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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.
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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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