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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: 2014-09-03
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] Calculated in 1000ml

[0047] substance Proportion Feeding amount bicyclol Feed according to the drug loading amount of 0.1mg / ml 100mg Soybean oil 15% (ml / ml) 150ml Lecithin 1.5% (g / ml) 15g Poloxamer 188 3% (g / ml) 30g glycerin 2.5% (g / ml) 25g Oleic acid 0.6% (g / ml) 6g Alpha Tocopherol (Antioxidant) 0.05% (g / ml) 0.5g Water for Injection About 82% (ml / ml) 820ml

[0048] [Preparation method] Take glycerin and water for injection, heat it to 40-60°C, add refined lecithin and poloxamer, put it in a tissue masher, stir at high speed to form a uniform water phase, and keep it warm; take bicyclol and α-vitamin separately E and oleic acid are added to soybean oil and heated to 40-60°C to form an oil phase. Slowly add the water phase to the oil phase under the stirring condition, put it in a tissue masher and stir at a high speed to form uniform colostrum. The colostrum ...

Embodiment 2

[0050] [Prescription Composition] Calculated in 1000ml

[0051] substance Proportion Feeding amount bicyclol Feed according to the drug loading amount of 0.2mg / ml 200mg Soybean oil 20% (ml / ml) 200ml Lecithin 1.5% (g / ml) 15g Poloxamer 188 3% (g / ml) 30g glycerin 2.5% (g / ml) 25g Oleic acid 0.6% (g / ml) 6g Alpha Tocopherol (Antioxidant) 0.05% (g / ml) 0.5g Water for Injection About 77% (ml / ml) 770ml

[0052] [Preparation method] Take glycerin and water for injection, heat to 40-60°C, add poloxamer, stir evenly to make water phase, keep warm; take bicyclol, α vitamin E, refined lecithin and oleic acid, add to Soybean oil, heated to 40-60°C, placed in a tissue masher, stirred at high speed to form a uniform oil phase. Slowly add the water phase to the oil phase under the stirring condition, put it in a tissue masher and stir at a high speed to form uniform colostrum. The colostrum is quickly transferred...

Embodiment 3

[0054] [Prescription Composition] Calculated in 1000ml

[0055] substance Proportion Feeding amount bicyclol Feed according to the drug loading amount of 0.1mg / ml 100mg Soybean oil 20% (ml / ml) 200ml Lecithin 1.5% (g / ml) 15g Poloxamer 188 4% (g / ml) 40g Mannitol 6.0% (g / ml) 60g Oleic acid 0.6% (g / ml) 6g Alpha Tocopherol (Antioxidant) 0.05% (g / ml) 0.5g Water for Injection About 80% (ml / ml) 800ml

[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 submicron emulsion and a preparation method thereof, belonging 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 raw material and its tablets were launched in the market in 2002. It is used for the treatment of chronic viral hepatitis, which can significantly improve liver function and reduce transaminase , and has a certain antiviral effect at the same time, it is not easy to rebound after drug withdrawal, and the safety is good. Because bicyclol is an insoluble drug, the oral bioavailability of ordinary tablets is less than 9%, and there are significant individual differences in clinical application, and the curative effect is unstable. For moderate to severe patients, bicyclol oral preparations cannot...

Claims

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Application Information

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Patent Type & Authority Patents(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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