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Preparation method and application of podophyllotoxin transdermal drug delivery preparation

A podophyllotoxin and transdermal drug delivery technology, applied in antiviral agents, pharmaceutical formulations, skin diseases, etc., to achieve good clinical application value, convenient use, and easy to meet the preparation conditions

Active Publication Date: 2016-04-27
SOUTH CHINA AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Regarding the podophyllotoxin transdermal drug delivery preparation of the present invention, there is no report

Method used

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  • Preparation method and application of podophyllotoxin transdermal drug delivery preparation
  • Preparation method and application of podophyllotoxin transdermal drug delivery preparation
  • Preparation method and application of podophyllotoxin transdermal drug delivery preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1: Preparation and Characterization of PPT-CNTs-COOH

[0035] Precisely weigh 5 mg of podophyllotoxin raw material drug and ultrasonically dissolve it in 10 mL of absolute ethanol for later use; accurately weigh 50 mg of multi-walled carboxylated carbon nanotubes (CNTs-COOH) and place it in a ball mill jar; add podophyllotoxin in absolute ethanol three times Solution, 580rpm·min under the protection of liquid nitrogen 1 Ball mill three times, 6 minutes each time; collect the ball-milled mixture in a stoppered Erlenmeyer flask (protected from light), and let it stand for 12 hours; filter the unadsorbed medicinal solution with a 0.45 μm organic filter membrane, and put the filter cake into a petri dish After evaporating absolute ethanol, add 10mL of purified water, place in a centrifuge tube and centrifuge for 1h (12000rpm·min 1); purify the centrifuged supernatant through a Sephadex column, use water as the eluent, and freeze-dry the eluent to obtain the PPT-CNT...

Embodiment 2

[0039] Embodiment 2: Determination of PPT-CNTs-COOH content

[0040] Chromatographic conditions: Column: EcosilC 18 column; mobile phase (water-methanol: 40-60); flow rate (1mL min -1 ); detection wavelength (292nm); column temperature (room temperature); injection volume (10μL).

[0041] Preparation of reference substance solution: Accurately weigh 1.2mg of PPT reference substance in a 25mL measuring bottle, dissolve in methanol and dilute to the mark to prepare 44.88μg·mL -1 The reference substance solution was obtained by passing through a 0.45 μm microporous membrane.

[0042] Linearity and range: Precisely pipette 2mL, 4mL, 6mL, 8mL, 10mL to 10mL of the reference substance solution into a 10mL measuring bottle, prepare a series of standard solution, and inject 10μL to measure the peak area. Carry out linear regression with the quality of the drug injected as the abscissa and the peak area as the ordinate, and the linear equation is: y=620.39x-811.20, the correlation co...

Embodiment 3

[0045] Example 3: Three batches of samples prepared by expanded production of PPT-CNTs-COOH and their content determination results

[0046] Precisely weigh 50g of podophyllotoxin raw material drug and ultrasonically dissolve it in 1000mL of absolute ethanol for later use; accurately weigh 500mg of multi-walled carboxylated carbon nanotubes (CNTs-COOH) and place it in a ball mill jar; add podophyllotoxin in absolute ethanol solution, 580rpm·min under liquid nitrogen protection 1 Ball mill three times, 6 minutes each time; collect the ball-milled mixture in a stoppered Erlenmeyer flask (protected from light), and let it stand for 12 hours; filter the unadsorbed medicinal solution with a 0.45 μm organic filter membrane, and put the filter cake into a tray , after evaporating the ethanol to dryness, put it in a beaker, add 1000mL of purified water, stir and dissolve, put it in a centrifuge tube and centrifuge for 1h (12000rpm·min 1 ); purify the centrifuged supernatant through a...

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Abstract

The invention relates to a preparation method of a podophyllotoxin transdermal drug delivery preparation; the water solubility and the stability of podophyllotoxin can be effectively improved, and skin irritation can be relieved; according to the prescription of the prepared preparation, each 100g of the prescription consists of the following ingredients by mass: 0.1-10g of carboxylic carbon nanotube loaded podophyllotoxin, 1-5g of carbomer, 5-15g of glycerol, 3-6g of azone, 0.1-0.5g of triethanolamine and 80-85g of pure water. The transdermal drug delivery preparation disclosed by the invention has the advantages that the carboxylic carbon nanotube, which is loaded with the podophyllotoxin, is prepared into a gel, and compared with a podophyllotoxin gel, the stability of the podophyllotoxin is enhanced, a skin penetration rate is relatively low and an amount retained in skin is increased, so that the curative effect on condyloma acuminate is enhanced, adverse reactions such as the skin irritation and the like are reduced, and toxic and side reactions in a whole body are reduced. The transdermal drug delivery preparation disclosed by the invention is simple in preparation process, controllable in quality, good in stability and suitable for mass production; therefore, a novel dosage form is provided for clinical administration.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a preparation method of podophyllotoxin transdermal administration preparation and its application in external administration for treating condyloma acuminatum. Background technique [0002] Podophyllotoxin (PPT) is a plant of the family Berberidaceae, the genus Taoerqi, the plants of the genus Podophyllum, the star anise lotus, the hexagonal lotus, the Yunnan star anise lotus, the Tibetan star anise lotus, and the lotus leaf of the genus Nanshan lotus, etc. The lignan components extracted from the roots and rhizomes of plants have significant anti-tumor, anti-virus, and anti-immune effects. Podophyllum is widely distributed in the world, mainly in Gansu, Qinghai, Tibet, Sichuan, Taiwan and other places in my country. The extract is also used in anthelmintic insecticides, laxatives, etc. (Liu Jie, 2011). [0003] The molecular formula of podophyllotoxin is C 22 h 22 ...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K31/365A61P17/12A61P31/20
Inventor 邓亚利蔡鑫剑姚淑娴
Owner SOUTH CHINA AGRI UNIV
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