Preparation of elaioplast and lipid compound preparation of nucleoside-phosphate compound

A technology of lipid complex and nucleoside phosphonic acid, which is applied in liposome delivery, medical preparations containing active ingredients, digestive system, etc. It can solve the problems of increased toxicity, large dosage, and low bioavailability , to improve the encapsulation rate, prolong the shelf life and improve the stability

Inactive Publication Date: 2007-10-31
SHANGHAI JIAOTONG UNIV
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  • Abstract
  • Description
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Problems solved by technology

However, the bioavailability of some of these compounds is low, especially the uptake rate of the lesion cells is low, but the metabolism is rapid, the dosage is large, and the toxicity is correspondingly large; can't complete treatment
The application of liposome and lipoplex technology to nucleoside phosphonic acid compounds has not yet been patented or reported in the literature

Method used

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  • Preparation of elaioplast and lipid compound preparation of nucleoside-phosphate compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] The chloroform solution that will contain 164mg dioleoylphosphatidylcholine (DOPC) and 54mg cholesterol is added in eggplant-shaped bottle, water bath, rotary evaporation removes chloroform, after making it film-forming, continue vacuumizing 1 hour to remove residual chloroform, to Add 10ml of HEPES solution (pH=7) into the eggplant-shaped bottle, shake it, let it stand at room temperature for 2 hours, add hydrochloric acid solution to adjust the outer water phase to pH=4, add 10mg of tenofovir (PMPA), shake well, and keep warm for 2 hours. Forms a homogeneous opalescent liposome suspension.

[0030] The encapsulation efficiency of the nucleoside phosphonic acid compound in this example is 23%.

Embodiment 2

[0032] Add a chloroform solution containing 277mg distearoylphosphatidylcholine (DSPC), 52mg distearoylphosphatidylethanolamine (DSPE) and 108mg cholesterol to an eggplant-shaped bottle, and remove the chloroform by rotary evaporation in a water bath to form a film Afterwards, continue vacuuming for 1 hour to remove residual chloroform, add 10ml of HEPES solution (pH=7) to the eggplant-shaped bottle, shake, leave at room temperature for 2h, add hydrochloric acid solution to adjust the external water phase to pH=4, add 10mg of tenoxine Forovir, shake well and keep warm for 2 hours to form a uniform milky white liposome suspension.

[0033] In this example, the encapsulation efficiency of the nucleoside phosphonic acid compound is 35%.

Embodiment 3

[0035] A chloroform solution containing 652 mg of dipalmitoylphosphatidylcholine (DPPC), 337 mg of 1-palmitoyl-2-oleoyl-sn-glycerol-3-phosphatidylcholine (POPC) and 344 mg of cholesterol was added to an eggplant-shaped bottle, Water bath, rotary evaporation to remove chloroform, make it into a film, continue vacuuming for 1 hour to remove residual chloroform, add HEPES solution (pH=7) 10ml into eggplant-shaped bottle, shake, leave at room temperature for 2h, add hydrochloric acid solution to adjust Add 10 mg of adefovir (PMEA) to the aqueous phase until pH = 3, shake well, and keep warm for 2 hours to form a uniform milky white liposome suspension.

[0036] The encapsulation efficiency of nucleoside phosphonic acid compounds in this example was 54%.

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Abstract

A liposome of nucleoside phosphate compound and its lipoid compound are proportionally prepared from nucleoside phosphate compound and lipoid by pH gradient method or Ca-ion gradient method or electric coating method. Its advantages are high encapsulation rate, high stability, and long storage time.

Description

technical field [0001] The present invention relates to a method for preparing a drug preparation, especially a method for preparing a liposome or liposome preparation of nucleoside phosphonic acid compounds. Background technique [0002] Viral infection is a serious threat to human health, and effective drug treatment is urgently needed. Taking hepatitis B as an example, there are more than 100 million hepatitis B virus carriers in my country, of which about 30 million are chronic hepatitis B patients. Among the current treatment drugs, α-interferon has a long course of treatment and is expensive, and only 30 ~50% response rate, lamivudine is a nucleoside analogue, which blocks virus reproduction by inhibiting reverse transcriptase and DNA polymerase, the effect is obvious, but it has certain side effects, and it is easy to trigger viral DNA polymerase Mutations lead to drug resistance, and the rebound after drug withdrawal is even more serious. Nucleoside phosphonic acid c...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/7052A61K9/127A61P31/12A61P31/14A61P1/16
Inventor 徐宇虹张健存章丽辉陈剑
Owner SHANGHAI JIAOTONG UNIV
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