Febrifugine liposome and preparation method thereof

A technology of hibiscus and liposomes, which is applied in the direction of liposome delivery, anti-infective drugs, and drug combinations, etc. It can solve the problems of low bioavailability, affecting the effect of drug administration, and short administration time, and achieves improved physical and chemical properties. properties, improved atomization effect, uniform distribution effect

Inactive Publication Date: 2017-05-31
HENAN SOAR VETERINARY PHARMA +1
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] Stenosine is a fat-soluble substance, which has poor dissolution in the body and low bioavailability, resulting in short administration time and small area, which affects the administration effect

Method used

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  • Febrifugine liposome and preparation method thereof

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Embodiment 1

[0020] A preparation method of changshanine liposome:

[0021] (1) Dissolve changshanine and liposome encapsulating material in supercritical CO 2 / Obtain a supercritical solution in anhydrous ethanol mixed solvent;

[0022] (2) Dissolve the surfactant as a stabilizer in a pH=7, 0.01mol / L phosphate buffer to obtain a stabilizer solution;

[0023] (3) The supercritical solution is sprayed into the stabilizer solution at a spray speed of 60ml / sec under the set expansion pressure of 30MPa and the expansion temperature of 350K, and the solution is dispersed and precipitated to obtain the changshanine liposome mixture Suspension

[0024] Wherein, the liposome encapsulating material is tricaprylin; the mass ratio of ashenine to liposome encapsulating material is 1:10; supercritical CO 2 / In anhydrous ethanol mixed solvent, anhydrous ethanol and CO 2 The volume ratio is 1:10; the surfactant is Tween 80, and the concentration of the stabilizer solution is 10% by mass fraction.

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Abstract

The invention discloses a febrifugine liposome and a preparation method thereof. The preparation method comprises the following steps: dissolving febrifugine and a liposome encapsulating material in a supercritical CO2/ethanol mixed solvent to obtain a supercritical solution; dissolving a surfactant used as a stabilizer in a water phase medium to obtain a stabilizer solution; and spraying the supercritical solution to the stabilizer solution under 20-30 MPa at 300-350 K, and carrying out dispersion and precipitate precipitation to obtain the febrifugine liposome, wherein the liposome encapsulating material is tricaprylin, and a mass ratio of febrifugine to the liposome encapsulating material is 1:10 to 1:20; a volume ratio of ethanol to CO2 in the supercritical CO2/ethanol mixed solvent is 1:6 to 1:10; the surfactant is tween80; the water phase medium is a phosphate buffer solution; and the concentration of the stabilizer solution is 1-10 wt%. The method for preparing the febrifugine liposome by adopting a supercritical CO2 fluid technology has the advantages of no toxic organic solvents and mild conditions, and allows the encapsulating rate to be higher than 80%.

Description

Technical field [0001] The invention belongs to the field of veterinary medicine, and specifically relates to a changshanine liposome and a preparation method thereof. Background technique [0002] Changshanine is a quinazolone alkaloid with the molecular formula C 16 H 19 N 3 O 3 , Is the active ingredient in Changshan, a traditional Chinese medicine for malaria. In 1949, Chinese chemist Zhao Chenggu and others obtained it from Chang Shangen. [0003] There are three kinds of changshanine: a, β and γ. β-Changshanine, also known as antipyretic alkali, is the main alkaloid in Changshan root; its melting point is 139~140℃; it is hardly soluble in water and ethanol, and easily soluble in chloroform, methanol or a mixture of chloroform and dilute ethanol. a-Changshanine is also called metapyretic alkali; its melting point is 129~130℃; its properties are similar to β-Changshanine, but its solubility is greater in chloroform or acetone. The melting point of γ-changshanine is 161℃. Ch...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/517A61K47/14A61K47/26A61P33/06
CPCA61K9/1272A61K31/517A61K47/26
Inventor 孙江宏刘素梅阮心洁高贵超
Owner HENAN SOAR VETERINARY PHARMA
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