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Gynostemma pentaphylla saponin long-circulating liposome preparation and preparation method thereof

A gypenoside and liposome technology, which is applied in liposome delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc., can solve the problems of no gypenoside long-circulation liposome reports, and achieve steric stabilization The effect of long circulation in the body, reducing the probability of cardiovascular and cerebrovascular diseases, and enhancing the stability

Inactive Publication Date: 2014-05-28
YANCHENG TEACHERS UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, there is no relevant report about gypenoside long-circulating liposomes

Method used

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  • Gynostemma pentaphylla saponin long-circulating liposome preparation and preparation method thereof
  • Gynostemma pentaphylla saponin long-circulating liposome preparation and preparation method thereof
  • Gynostemma pentaphylla saponin long-circulating liposome preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment l

[0038] prescription Dosage Distearoylphosphatidylethanolamine (DSPE) 200mg Compound of formula I 100mg Ether 3mL Gypenoside 20mg Phosphate buffer (pH=7.0) 15mL

[0039] craft

[0040] (1) selection of raw materials: get phosphate buffer saline and gypenoside by above-mentioned prescription, gypenoside is dissolved in phosphate buffer saline, for subsequent use;

[0041] (2) preparation of gypenoside liposome: get distearoylphosphatidylethanolamine, formula I compound and ether by above-mentioned prescription, mix homogeneously, then rotary evaporation makes it become uniform lipid film and covers the bottom in the pear-shaped bottle, Add gypenoside-containing phosphate buffer solution to the bottle, add glass beads, rotate and shake at 60°C for 30 minutes, and place it for 2 hours to fully hydrate.

Embodiment 2

[0043] prescription Dosage Gypenoside 20mg Lecithin 200mg Compound of formula I 50mg ethanol 10mL Phosphate buffer (pH=6.8) 10mL

[0044] craft

[0045] (1) Preparation of oil phase: get gypenoside, lecithin, formula I compound, ethanol according to the above prescription, mix well, as oil phase;

[0046] (2) Preparation of the water phase: take phosphate buffer as the water phase according to the above prescription;

[0047] (3) Preparation of liposomes: under constant temperature stirring, inject the oil phase into the water phase at a temperature of 45°C at a constant speed with a needle, stir at constant temperature for 2 hours to remove ethanol, and obtain the liposome.

Embodiment 3

[0049] prescription Dosage Gypenoside 200mg Phosphatidylserine 200mg Compound of formula I 50mg Dichloromethane 50mL Phosphate buffer (pH=8.0) 40mL

[0050] craft

[0051] (1) Take phosphatidylserine according to the above prescription: compound of formula I: dichloromethane=200mg: 50mg: 50mL to prepare the oil phase, place the oil phase in a round-bottomed flask, and rotate to evaporate the dichloromethane;

[0052] (2) 200mg gypenoside was dissolved in 20mL phosphate buffer (pH=8.0) as the water phase;

[0053] (3) Add 20 mL of phosphate buffer solution (pH=8.0) containing 200 mg of gypenoside to the oil phase, and in an ice bath, sonicate the probe for 10 minutes to form a uniform emulsion;

[0054] (4) Rotary evaporation to remove the organic phase, after forming a colloidal state, continue to add 20 mL of phosphate buffer, continue to evaporate under reduced pressure for 0.5 h, and ultrasonically probe for 10 min to obtai...

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Abstract

The invention provides a gynostemma pentaphylla saponin long-circulating liposome preparation and a preparation method thereof. The invention discloses a method for preparing gynostemma pentaphylla saponin long-circulating liposome after modification of beta-sitosterol by polyethylene glycol. Compared with common phosphatide polyethylene glycol modified long-circulating liposome, the gynostemma pentaphylla saponin long-circulating liposome prepared in the invention has the following advantages: material synthesis cost is greatly reduced, separation is easier, yield is substantially increased, and cost for the long-circulating liposome is substantially reduced. The novel long-circulating liposome has the characteristics of easy and wide availability of raw materials, a cheap price, good stability, capacity of substantially prolonging detention time of gynostemma pentaphylla saponin in a human body, realizing passive targeting of gynostemma pentaphylla saponin to tumor cells and improving tumor treatment effects and an excellent antihyperlipidemic effect.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a method for producing gypenoside long-circulation liposomes, more specifically, the invention relates to gypenoside long-circulation liposomes and pharmaceutical preparations containing gypenoside long-circulation liposomes. Background technique [0002] Liposome is a new dosage form of targeted drug delivery system, which is a closed vesicle with a water phase in the interior composed of a lipid bilayer. As an intelligent drug delivery carrier, liposome has remarkable advantages such as targeting, biocompatibility, improving drug stability and reducing toxic and side effects, so it has attracted more and more attention. Although ordinary liposomes can improve the curative effect of drugs, they are quickly swallowed by the reticuloendothelial system after entering the body, and are mainly targeted at organs of the reticuloendothelial system such as liver, spleen, and b...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/424A61K9/127A61K9/00A61K47/34A61P35/00A61P3/06C08G65/48
Inventor 喻樊
Owner YANCHENG TEACHERS UNIV
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