Phospholipids compound of bicyclo-ethanol and preparation method thereof

A technology of bicyclic alcohol phospholipids and cycloalcohol phospholipids, which is applied in the field of medicine, can solve the problems of slow dissolution rate, low bioavailability, poor water solubility of bicyclic alcohols, etc., and achieve improved bioabsorption, improved bioabsorption, and improved hydrophilicity and lipophilicity Effect

Active Publication Date: 2014-01-15
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

Due to the poor water solubility of bicyclol, the dissolution rate of ordinary tablets in vitro is relatively slow. When distilled water is used as the dissolution medium, only 60% to 70% can be dissolved within two hours. There are more significant individual differences, which is not conducive to the exertion of its curative effect

Method used

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  • Phospholipids compound of bicyclo-ethanol and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1: Drug-loaded phospholipid complex (bicyclic alcohol: phospholipid material=1:6.100 weight ratio)

[0028] Take 0.60g of bicyclic alcohol, 3.66g of soybean lecithin, add 40ml of tetrahydrofuran, compound at 40°C for 1 hour, remove the tetrahydrofuran by rotary evaporation, and dry in vacuum for more than 12 hours (20-30°C) to obtain the drug-loaded phospholipid complex, which is sealed and packaged , stored in the refrigerator.

Embodiment 2

[0029] Example 2: Drug-loaded phospholipid complex (bicyclic alcohol: phospholipid material=1:6.033 weight ratio)

[0030] Take 0.60g of bicyclic alcohol and 3.62g of soybean lecithin, add 40ml of acetone preheated to 40°C, compound at 40°C for 1 hour, remove the solvent by rotary evaporation, and dry in vacuum for more than 12 hours (20-30°C), and the drug-loaded product is obtained Phospholipid complex, airtightly packaged, stored in the refrigerator.

Embodiment 3

[0031] Example 3: Drug-loaded phospholipid complex (bicyclic alcohol: phospholipid material=1:6.075 weight ratio)

[0032] Take 0.40g of bicyclic alcohol, 2.43g of soybean lecithin, add 60ml of acetone preheated to 40°C, compound at 40°C for 2 hours, remove the solvent by rotary evaporation, and dry in vacuum for more than 12 hours (20-30°C) to obtain the loaded drug Phospholipid complex, airtightly packaged, stored in the refrigerator.

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PUM

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Abstract

The invention discloses a phospholipids compound of bicyclo-ethanol and a preparation method thereof, in particular relates to a phospholipids compound of bicyclo-ethanol, a preparation method of the phospholipids compound of bicyclo-ethanol and a preparation containing the phospholipids compound of bicyclo-ethanol. The phospholipids compound of bicyclo-ethanol comprises bicyclo-ethanol and phospholipids material with the weight proportion of 1 to 2-12. The phospholipids compound can be selectively added with antioxidative stabilizer and / or srobent. In the invention, bicyclo-ethanol is prepared into the phospholipids compound so that the water-dispersible property and the lipotropy of the bicyclo-ethanol are both improved. Compared with the raw material medicine of the bicyclo-ethanol, the phospholipids compound of bicyclo-ethanol can remarkably improve the blood concentration after being orally taken, and has higher biological validity when used for clinic treatment for chronic hepatitis.

Description

technical field [0001] The invention relates to a bicyclic alcohol phospholipid complex, the phospholipid complex is composed of bicyclic alcohol and phospholipid materials, and the weight ratio is 1:2-12; the phospholipid complex can also selectively add antioxidant stabilizers and / or adsorbents . The invention also relates to a preparation method of the bicyclic alcohol phospholipid complex and a preparation containing the bicyclic alcohol phospholipid complex, 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 has poor water-solubility and fat-solubility, and its bioavailability after oral administration is low, with significant individual differences. [0003] Bicyclol is a new anti-hepatitis drug developed by the Institute of Medicine, Chinese Academy of ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/36A61K47/24A61P1/16
Inventor 刘玉玲李燕李琳夏学军王洪亮陈晖扈金萍
Owner INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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