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Praziquantel long-circulating nanoparticle injection and preparation method thereof

A technology for praziquantel and injection, which is applied in pharmaceutical formulations, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc. It can solve the problems of large particle size and strong irritation of injections, so as to achieve the effect of solving large dosage, preventing and treating schistosomiasis infection and improving curative effect.

Inactive Publication Date: 2013-11-06
CHANGSHA MEDICAL UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, in the dosage form of praziquantel, the oral dose of praziquantel tablet is large, and the drug effect is low; the injection is highly irritating, and the drug effect time is short; Large particle size, prone to residual organic solvents

Method used

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  • Praziquantel long-circulating nanoparticle injection and preparation method thereof
  • Praziquantel long-circulating nanoparticle injection and preparation method thereof
  • Praziquantel long-circulating nanoparticle injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] (1) Weigh 10 parts of poloxamer, 15 parts of soybean lecithin, 1 part of sodium stearate, 5 parts of DSPE-PEG2000, and 500 parts of water in a 50ml centrifuge tube. spare;

[0048] (2) Weigh 1.5 parts of each raw material praziquantel, 7.5 parts of glyceryl behenate, 7.5 parts of glyceryl monostearate, and 7.5 parts of butyl acetate in a 50ml centrifuge tube, dissolve in a 70°C water bath, and use it as the oil phase for later use;

[0049] (3) Inject the water phase into the oil phase, shear at 70°C and 8000rpm for 10 minutes, sonicate the probe for 10 minutes, and cool to room temperature with magnetic stirring to obtain praziquantel long-circulation nanoparticle injection, which contains 10% by mass Phosphatidylethanolamine-Polyethylene Glycol 2000.

Embodiment 2

[0051] (1) Weigh 10 parts of poloxamer, 15 parts of soybean lecithin, 1 part of sodium stearate, 2.5 parts of DSPE-PEG2000, and 500 parts of water in a 50ml centrifuge tube, ultrasonically dissolve the probe, and keep warm in a 70°C water bath. Standby as the aqueous phase;

[0052] (2) Weigh 1.5 parts of each raw material praziquantel, 7.5 parts of glyceryl behenate, 7.5 parts of glyceryl monostearate, and 7.5 parts of butyl acetate in a 50ml centrifuge tube, dissolve in a 70°C water bath, and use it as the oil phase for later use;

[0053] (3) Inject the water phase into the oil phase, shear at 70°C and 8000rpm for 10 minutes, sonicate the probe for 10 minutes, and cool to room temperature with magnetic stirring to obtain praziquantel long-circulation nanoparticle injection, which contains 5% by mass Phosphatidylethanolamine-Polyethylene Glycol 2000.

Embodiment 3

[0055] (1) Weigh 10 parts of poloxamer, 15 parts of soybean lecithin, 1 part of sodium stearate, 1.25 parts of DSPE-PEG2000, and 500 parts of water in a 50ml centrifuge tube, ultrasonically dissolve the probe, and keep warm in a 70°C water bath. Standby as the aqueous phase;

[0056] (2) Weigh 1.5 parts of each raw material praziquantel, 7.5 parts of glyceryl behenate, 7.5 parts of glyceryl monostearate, and 7.5 parts of butyl acetate in a 50ml centrifuge tube, dissolve in a 70°C water bath, and use it as the oil phase for later use;

[0057] (3) Inject the water phase into the oil phase, shear at 70°C and 8000rpm for 10 minutes, sonicate the probe for 10 minutes, and cool to room temperature with magnetic stirring to obtain praziquantel long-circulation nanoparticle injection, which contains 2.5% by mass Phosphatidylethanolamine-Polyethylene Glycol 2000.

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Abstract

The invention relates to a novel praziquantel drug and provides a praziquantel long-circulating nanoparticle injection. The praziquantel long-circulating nanoparticle injection contains a long-circulating modification material such as distearoyl phosphatidyl ethanolamine-polyethylene glycol 2000 (DSPE-PED2000). The preparation method comprises the following steps of 1, weighing poloxamer, soyabean lecithin, sodium stearate, DSPE-PED2000 and water, putting the materials into a centrifuge tube, and carrying out ultrasonic dissolution to obtain a solution as a water phase, 2, weighing praziquantel, glyceryl behenate, glyceryl monostearate and butyl acetate, putting the materials into a centrifuge tube, and carrying out water-bath dissolution to obtain a solution as an oil phase, 3, pouring the water phase into the oil phase, and carrying out ultrasonic and magnetic stirring cooling to a room temperature. The praziquantel long-circulating nanoparticle injection can be prepared simply and has a small particle size and an entrapment rate higher than an entrapment rate of liposome, can be stored stably, has small irritation and a long plasma concentration keeping period, can prevent and treat bilharziasis infection, can improve a whole body plasma concentration of the drug and curative effects, and is not accumulated at a specific target organ thereby having treatment effects on various bilharziasis of multiple organs.

Description

technical field [0001] The invention mainly relates to a pharmaceutical preparation for clinical application, in particular to a broad-spectrum antiparasitic drug—praziquantel long-circulation nanoparticle injection and a preparation method thereof. Background technique [0002] Praziquantel (PZQ) is the drug of choice for the treatment of schistosomiasis, and is currently the only drug that is effective against the five types of schistosomiasis that infect the human body. It has the advantages of broad anti-insect spectrum, high curative effect, low toxicity and short course of treatment. High concentration of PZQ acts on Schistosoma japonicum to make Ca 2+ Influx, causing parasite contracture, inhibiting parasite glucose metabolism, promoting parasite glycogen decomposition, and obviously inhibiting parasite RNA synthesis, ATPase, and cortical alkaline phosphatase. [0003] Praziquantel is a heterocyclic pyrazine isoquinoline derivative with a relative molecular mass of ...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/4985A61K47/34A61P33/12
CPCY02A50/30
Inventor 马宁邹永华丁劲松王建芬肖志勇李云贵
Owner CHANGSHA MEDICAL UNIV
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