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Method for preparing etoposide nanometer suspension freeze-drying preparation

A freeze-dried preparation, the technology of Poside Nanometer, which is applied in the field of medicine, can solve the problems of serious sensitization reaction, high can only reach 0.5%, toxic and side effects in clinical application, etc.

Inactive Publication Date: 2011-08-10
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The Chinese patent with the application number 200610169149.8 describes a lipid microsphere injection containing etoposide and its preparation method, which is essentially an oil-in-water fat emulsion. Even so, the highest drug loading can only reach 0.5%, which leads to the amount of other excipients far greater than the amount of the main drug, and a certain amount of Tween-80, Span-80, etc. Surfactants have been reported in a large number of literatures. Tween and Span surfactants have strong hemolytic properties, severe sensitization reactions, and can extract toxic substances in plastic syringes / infusion sets, which will inevitably cause potential problems in clinical applications. sexual side effects

Method used

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  • Method for preparing etoposide nanometer suspension freeze-drying preparation
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  • Method for preparing etoposide nanometer suspension freeze-drying preparation

Examples

Experimental program
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Effect test

Embodiment 1

[0031] 10 mg of etoposide was dissolved in 1.0 ml of methylene chloride, and added to 5 ml of a 2% (W / V) aqueous solution of human serum albumin, and the mixture was sheared at high speed (9000 rpm) for 3 min to form colostrum, which was then Transfer to the ultrasonic treatment tank, ultrasonic (600W) 5min, the obtained suspension was evaporated under reduced pressure at 40°C for 15-20min to remove dichloromethane, and the etoposide nanosuspension was obtained, and its particle size range was 150 ~300nm.

[0032] The above-prepared suspension was divided into vials, pre-frozen in a low-temperature refrigerator (-80°C) for 24 hours, and then transferred to a freeze dryer (-40°C, 0.5mbar) for 48 hours to obtain etoposide nanomixtures. Suspension freeze-dried formulations.

Embodiment 2

[0034] Dissolve 90 mg of etoposide in 3.0 ml of chloroform, and add it to 30 ml of a 1% (W / V) aqueous solution of human serum albumin. The mixture is sheared at high speed (12000 rpm) for 5 min, and then transferred to a high-pressure milk In the homogenizer, 1500bar was circulated for 20 times, and the obtained suspension was evaporated at 40°C under reduced pressure for 15-20 minutes to remove chloroform. The obtained suspension was translucent and the particle diameter was 160-220nm.

[0035] The above-prepared suspension was divided into vials, pre-frozen in a low-temperature refrigerator (-80°C) for 24 hours, and then transferred to a freeze dryer (-40°C, 0.5mbar) for 48 hours to obtain etoposide nanomixtures. Suspension freeze-dried formulations.

Embodiment 3

[0037] Dissolve 200 mg of etoposide in a mixed solution of 3.0 ml of chloroform and 0.4 ml of absolute ethanol, add to 100 ml of bovine serum albumin aqueous solution with a concentration of 3% (W / V), shear (9000 rpm) for 2 min, and transfer rapidly Put it in a high-pressure milk homogenizer, circulate 15 times at 1300 bar, remove the organic solvent quickly from the obtained suspension under reduced pressure at 35°C, and obtain etoposide albumin nanosuspension, the particle size range of which is 300-450nm .

[0038]The above-prepared suspension was divided into vials, pre-frozen in a low-temperature refrigerator (-80°C) for 24 hours, and then transferred to a freeze dryer (-40°C, 0.5mbar) for 48 hours to obtain etoposide nanomixtures. Suspension freeze-dried formulations. After adding physiological saline, it can quickly return to the state before freeze-drying, and the particle size of the particles does not change.

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Abstract

The invention relates to a method for preparing an etoposide nanometer suspension freeze-drying preparation, and belongs to the technical field of medicines. An etoposide nanometer suspension of which the grain diameter is less than 200 nanometers is prepared by a high-pressure homogenization technology, and the suspension is filtered, sterilized and freeze-dried to form solid powder. By the preparation method, a large amount of cosolvent and surfactant which are used in the conventional etoposide injection can be prevented, so that the incidence rate of toxic and side reactions is reduced, and the stability of the preparation is improved; and albumin used in the preparation method can be used as a cryoprotectant, so other auxiliary materials are prevented from being added. The preparation method is easy to operate, mild in conditions and high in controllability and suitable for industrial production; and the prepared etoposide nanometer suspension freeze-drying preparation has the advantages of high safety and stability, low toxic and side effect and the like.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a preparation method of a new formulation of etoposide etoposide nano-suspension freeze-dried preparation. Background technique [0002] Etoposide, the Chinese alias is etoposide, etoposide, epipodophyllotoxin glucopyranose; the English name is Etoposide, Etopl, Vepeside, often abbreviated as VP-16, VP16-213, EPEG; it is a ghost Active ingredients of lignans isolated from Podophyllin. VP-16 is a cell cycle-specific antitumor drug that activates certain endonucleases in vivo, or acts on DNA through its metabolites, and its non-glycoside homologue 4-desmethyl epipodophyllotoxin can inhibit microregulatory assembly . This product is mainly for small cell lung cancer, the effective rate is increased from 40% to 85%, and the complete remission rate is 14% to 34%. It is also effective for acute leukemia, malignant lymphoma, testicular tumor, bladder cancer, prostate cancer, gastric...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/7048A61K47/42A61P35/00A61P35/02
Inventor 黄桂华张志岳张栋苗蕾
Owner SHANDONG UNIV
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