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Etoposide cubic liquid crystal as well as preparation method and application thereof

A technology of etoposide and cube, which is applied in the field of etoposide cubic liquid crystal and its preparation, can solve the problem of low incidence of vomiting and achieve the effects of short preparation time, short preparation process time and encapsulation efficiency measurement

Inactive Publication Date: 2017-10-10
GUANGDONG PHARMA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Intravenous versus oral formulations are less likely to vomit but may cause severe allergic reactions

Method used

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  • Etoposide cubic liquid crystal as well as preparation method and application thereof
  • Etoposide cubic liquid crystal as well as preparation method and application thereof
  • Etoposide cubic liquid crystal as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] An etoposide cubic liquid crystal, the average particle size of the etoposide cubic liquid crystal is 208nm, and the encapsulation rate of the etoposide cubic liquid crystal is 65%.

[0058] Preparation method: Weigh 0.1g of GMO, add 5mg of etoposide and 1ml of acetone into a 50ml Erlenmeyer flask to dissolve, and use an ultrasonic cleaner to sonicate for 15min, as phase A; accurately weigh 0.02g of F1270.02g, add 20ml of water, Heat in a water bath to fully dissolve, stir, and prepare a solution with a concentration of 0.1% F127 to form phase B. Phase A was slowly added dropwise to phase B, and stirred at room temperature for 1 h. Then ultrasonic treatment was performed at 300w for 5 minutes in a cell disruptor, once every 5 seconds (with an interval of 5 seconds), to obtain a cubic liquid crystal solution of etoposide.

[0059] The application of etoposide cubic liquid crystal is made into a hollow suppository; its preparation is specifically:

[0060] (1) Take an a...

Embodiment 2

[0064] An etoposide cubic liquid crystal, the average particle size of the etoposide cubic liquid crystal is 180nm, and the encapsulation rate of the etoposide cubic liquid crystal is 75%.

[0065] Preparation method: Weigh 0.08g of phytantriol, add 6mg of etoposide and 0.8ml of acetone into a 50ml Erlenmeyer flask to dissolve, and use an ultrasonic cleaner to sonicate for 13min, as phase A; accurately weigh 0.018g of lecithin , add 22ml of water, heat in a water bath to fully dissolve, stir, and prepare a solution with a concentration of 0.08% lecithin to form phase B. Phase A was slowly added dropwise to phase B, and stirred at room temperature for 1.2h. Then ultrasonic treatment was performed at 280w for 4 minutes in a cell disintegrator, once every 5 seconds (with an interval of 5 seconds), to obtain a cubic liquid crystal solution of etoposide.

[0066] The application of etoposide cubic liquid crystal is made into hollow suppository; its preparation is specifically the ...

Embodiment 3

[0068] An etoposide cubic liquid crystal, the average particle size of the etoposide cubic liquid crystal is 100nm, and the encapsulation rate of the etoposide cubic liquid crystal is 90%.

[0069] Preparation method: Weigh 0.12g of glycerol monolauryl ester, add 4mg of etoposide and 1.2ml of acetone into a 50ml Erlenmeyer flask to dissolve, and use an ultrasonic cleaner to sonicate for 17min, as phase A; accurately weigh Cremophor RH400. 022g, add 22ml of water, heat in a water bath to fully dissolve, stir, and prepare a solution with a concentration of 0.1% Cremophor RH40 to form a B phase. Phase A was slowly added dropwise to phase B, and stirred at room temperature for 0.8h. Then ultrasonic treatment was performed at 320w for 5 minutes in a cell disruptor, once every 5 seconds (with an interval of 5 seconds), to obtain a cubic liquid crystal solution of etoposide.

[0070] The application of etoposide cubic liquid crystal is made into hollow suppository; its preparation i...

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Abstract

The invention belongs to the technical field of medicines and in particular relates to an etoposide cubic liquid crystal as well as a preparation method and application thereof. The preparation method comprises the following steps: firstly selecting a lipid material / water system and a stabilizer for preparing the etoposide cubic liquid crystal, wherein the average particle size of the prepared etoposide cubic liquid crystal is 208nm, and the encapsulation efficiency is 60-65%; and secondly preparing the etoposide cubic liquid crystal into a hollow suppository by adopting a special pharmaceutical adjuvant combination, so that drug bioavailability and drug stability are improved, toxic and side effects are reduced, and targeted drug delivery is realized; and a preparation process is simple, instruments are available, and the preparation time is short.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to an etoposide cubic liquid crystal and a preparation method and application thereof. Background technique [0002] Etoposide (etoposide), also known as etoposide, etoposide, chemical name is 9-(4,6-O-ethylidene-β-D-glucopyranoside)-4'-nor The epipodophyllotoxin, VP-16 for short, is derived from the plant component podophyllotoxin through multi-step chemical synthesis. Etoposide is white or off-white crystalline powder, odorless, hygroscopic; insoluble in water and ether, soluble in ethanol, easily soluble in methanol and chloroform. The solubility in water is 58.7ug / ml, the pKa value is 9.5, and the aqueous solution is most stable when the pH value is 4-5. [0003] [0004] Etoposide has a significant effect on lung cancer, leukemia, testicular cancer, Ewing's tumor, gestational blastoma, Kaposi's tumor, Hodgkin's disease, neuroblastoma and children's striated m...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K9/02A61K31/7048A61P35/00A61P35/02
CPCA61K9/0031A61K9/025A61K9/1274A61K31/7048A61K47/10A61K47/14
Inventor 卫世杰霍务贞
Owner GUANGDONG PHARMA UNIV
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