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Injection containing lipoid microsphere of etoposide and its prepn process

A technology of etoposide and lipid microspheres, which is applied in the field of medicine, can solve problems such as poor water solubility, interference with drug effects, and toxicity, and achieve the effects of reducing toxic side effects, reducing vascular irritation, and strong innovation

Inactive Publication Date: 2007-06-06
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Many clinical drugs have poor water solubility and must rely on organic solvents to play a role, and organic solvents not only have certain toxicity themselves, but may also interfere with the drug effect

Method used

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  • Injection containing lipoid microsphere of etoposide and its prepn process
  • Injection containing lipoid microsphere of etoposide and its prepn process
  • Injection containing lipoid microsphere of etoposide and its prepn process

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] The prescription preparation technology of embodiment 1 etoposide preparation

[0048] Prescription 1:

[0049] Safflower oil for injection 20g

[0050] Etoposide 0.2g

[0051] Lecithin 1.8g

[0052] Glycerin 2.5g

[0053] Add water for injection to 100ml

[0054] Preparation method 1:

[0055] (1) Mix the prescribed amount of glycerin with an appropriate amount of water for injection preheated to 40-100°C, transfer it to a tissue grinder, and stir for several minutes, 1-5 times, until the ingredients are dissolved to obtain an aqueous phase; at the same time Add lecithin to the prescribed amount of safflower oil and heat to dissolve at 40-100°C to obtain the oil phase; (2) Add the oil phase to the water phase, transfer it to a tissue grinder, stir for several minutes, 1-5 times, Until the oil phase is uniformly dispersed to obtain colostrum, adjust the pH value to 4-8; (3) Add etoposide drug powder to the colostrum, stir for 10 minutes, add water for injection pr...

Embodiment 2

[0096] Example 2 The investigation of the stability of etoposide lipid microspheres

[0097] According to the experimental method reported in the literature: the etoposide lipid microsphere sample was washed with redistilled water, buffer salt (Na 2 HPO 4 , 0.017M; KH 2 PO 4 , 0.0014M; NaCl, 0.1370M, pH7.4) and glycerol (2.21% w / w) were diluted, and the particle size, ζ-potential and drug encapsulation rate after dilution were measured 1h, 2h, 4h, 24h, and 48h. The etoposide lipid microspheres were stored at 4-8°C and 25°C for 6 months, and the particle size and encapsulation rate of the samples were measured at different time points. The test results showed that the particle size of the etoposide lipid microspheres was not affected by weight. Effect of distilled water, buffer saline (pH 7.4) and glycerol (2.21% w / w) dilution. After 48 h, the particle size in redistilled water and glycerol hardly changed, while in buffer salt (pH 7.4), the particle size increased by 50 nm....

Embodiment 3

[0098] Example 3 Irritation Test of Etoposide Lipid Microsphere Injection

[0099] (1) Vascular stimulation test

[0100] Two different dosage forms of etoposide injection were converted according to the clinical dosage (100mg / time) to obtain the experimental rabbit dose (5.2mg / kg) by body surface area conversion. Before the test, it was freshly prepared with sterile physiological saline injection according to the dosage of 2ml / kg. Six healthy New Zealand white rabbits with a body weight of 2.5-3.0 kg were selected, both male and female. After the injection site was disinfected with tincture of iodine and ethanol, 3 white rabbits were injected with etoposide water injection (Cs) in the ear vein of the right ear, and the left ear was injected with the same dose of sterile normal saline injection as a control; Rabbits were injected with etoposide lipid microsphere injection (Cz) in the ear vein of the right ear, and the same dose of sterile saline injection was injected into t...

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Abstract

The present invention belongs to the field of medicine technology, and is especially lipoid microsphere injection containing etoposide and its preparation process. The injection contains etoposide, fat soluble medium, water and surfactant; and consists of oil phase 5-30 wt%, etoposide 0.001-0.5 wt%, surfactant 0.5-5 wt%, osmotic regulator 0.5-5 wt%, and water for injection the rest. Etoposide is high pressure homogenized under the action of high speed airflow to form ultrasonic stirring, so as to be dissolved fast and permeated in molecular form into oil / water interface film. By means of medicine carrying interface film principle, the present invention raises the medicine carrying amount of insoluble etoposide and the stability while lowering the toxicity and blood vessel irritation. The preparation of the present invention has low toxicity, low irritation and high curative effect in clinical application.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a preparation process and formula of lipid microsphere injection (oil-in-water emulsion) containing etoposide. Background technique [0002] Cancer is one of the most difficult and common diseases of human beings. It is an extremely urgent and major issue in the world to conquer this stubborn fortress of cancer and benefit mankind. At present, the number of cancer patients is increasing year by year, and the mortality rate of cancer is constantly rising. According to statistics in recent years, about 800,000 people die of cancer every year, and an average of 1.5 people die of cancer every minute in the country. A large number of facts prove that the progress of cancer treatment is very little, and cancer is more and more serious threat to human life. Therefore, it is urgent to find new anti-cancer drugs, change their formulations to improve their anti-cancer efficac...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/7048A61P35/00
Inventor 唐星田玲玲张洪瑶
Owner SHENYANG PHARMA UNIVERSITY
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