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Application of ionic type cyclodextrin derivative in preparation of medicine preparation for iontophoresis transdermal administration

A pharmaceutical preparation and iontophoresis technology, which is applied in drug delivery, non-active ingredients of polymer compounds, pharmaceutical formulations, etc., can solve the problems of limited transdermal penetration of drugs, and achieve increased transdermal penetration rate, enhanced electric field response, The effect of increasing solubility

Inactive Publication Date: 2010-12-01
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, when the cyclodextrin inclusion compound is directly used for transdermal administration, the improvement of the transdermal penetration effect of the drug is limited.
However, there are no relevant reports on the promotion of drug iontophoresis by ionic cyclodextrins in the literature at home and abroad.

Method used

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  • Application of ionic type cyclodextrin derivative in preparation of medicine preparation for iontophoresis transdermal administration
  • Application of ionic type cyclodextrin derivative in preparation of medicine preparation for iontophoresis transdermal administration
  • Application of ionic type cyclodextrin derivative in preparation of medicine preparation for iontophoresis transdermal administration

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Promotion of Hydrocortisone (HS) Iontophoresis by 5% Sulfobutyl-β-cyclodextrin (SBE-CD)

[0031] 1 g of excess hydrocortisone was placed in 100 ml of SBE-CD phosphate buffered solution (PBS) with a mass percent concentration of SBE-CD of 5%, and magnetically stirred to form a HS-SBE-CD clathrate solution.

[0032] Another 1 g of hydrocortisone was placed in 100 ml of phosphate buffered solution (PBS), and magnetically stirred evenly to form a control solution.

[0033] Take the skin of the rat body from which the subcutaneous tissue has been removed, and fix it between the supply pool and the receiving pool of the horizontal transdermal two-chamber iontophoresis diffusion cell, exhaust the air bubbles, and keep the circulating water at (32±0.5)°C. Place the above-mentioned HS-SBE-CD clathrate solution or control solution in the supply tank, use PBS as the receiving solution in the receiving tank, add a stirrer to stir at a speed of 500r / min, the electrodes are all Pt, the...

Embodiment 2

[0039] Promotion of Hydrocortisone (HS) Iontophoresis by 10% Sulfobutyl-β-cyclodextrin (SBE-CD)

[0040] 2 g of excess hydrocortisone was placed in 100 ml of SBE-CD phosphate buffer solution (PBS) with a concentration of 10% by mass of SBE-CD, and magnetically stirred to form a HS-SBE-CD clathrate solution.

[0041] Another 2 g of hydrocortisone was placed in 100 ml of phosphate buffered solution (PBS), and magnetically stirred evenly to form a control solution.

[0042] Take the skin of the rat body from which the subcutaneous tissue has been removed, and fix it between the supply pool and the receiving pool of the horizontal transdermal two-chamber iontophoresis diffusion cell, exhaust the air bubbles, and keep the circulating water at (32±0.5)°C. Place the above-mentioned HS-SBE-CD clathrate solution or control solution in the supply tank, use PBS as the receiving solution in the receiving tank, add a stirrer to stir at a speed of 500r / min, the electrodes are all Pt, the ne...

Embodiment 3

[0048] The promotion of iontophoresis of estradiol (ES) by sulfobutyl-β-cyclodextrin (SBE-CD)

[0049] 1.5 g of excess estradiol was placed in 10 ml of SBE-CD phosphate buffer solution (PBS) with a concentration of 5% by mass of SBE-CD, and magnetically stirred to form an ES-SBE-CD clathrate solution.

[0050] Take the skin of the rat body from which the subcutaneous tissue has been removed, and fix it between the supply pool and the receiving pool of the horizontal transdermal two-chamber iontophoresis diffusion cell, exhaust the air bubbles, and keep the circulating water at (32±0.5)°C. Place the above-mentioned ES-SBE-CD clathrate solution in the supply tank, use PBS as the receiving solution in the receiving tank, add a stirrer to stir at a speed of 500r / min, the electrodes are all Pt, the negative electrode is introduced, and the current intensity is 0.4mA / 0.79 cm 2 , for iontophoresis. Take 1ml of receiving solution at 1h, 2h, 3h, 4h, 6h, 8h, 10h and 12h respectively, ...

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Abstract

The invention discloses the application of ionic type cyclodextrin derivative in preparation of medicine preparation for iontophoresis transdermal administration. The ionic type cyclodextrin derivative comprises one or two of cationic cyclodextrin derivative and anionic cyclodextrin derivative; the medicine is selected from one or more of molecular type medicine, charged medicine with the dissolubility less than 1mg / ml, faintly acid charged medicine with the dissociation constant p Ka larger than 4, or alkalescent charged medicine with the dissociation constant p Ka less than 4. The ionic type cyclodextrin derivative applied to the iontophoresis transdermal administration improves the transdermal penetration rate of the molecular type medicinem and the charged medicine with low dissolubility or degree of dissociation.

Description

technical field [0001] The invention relates to the application field of cyclodextrin derivatives, in particular to the application of an ionic cyclodextrin derivative in the preparation of pharmaceutical preparations for iontophoresis transdermal administration. Background technique [0002] After more than 30 years of rapid development since the 1970s, modern transdermal drug delivery technology has researched and developed more than 30 transdermal patches (TTS) through the combination of many technologies including physics, chemistry and biology. product. The rapid development of transdermal drug delivery technology is due to the unique advantages of transdermal drug delivery, such as transdermal drug delivery can avoid the first-pass effect of the liver and degradation of drugs in the gastrointestinal tract; drugs can be released at the required rate, maintain Constant effective blood drug concentration, avoiding the peak and valley phenomenon of blood drug concentratio...

Claims

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Application Information

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IPC IPC(8): A61K47/40A61K9/08A61K9/10A61K9/06A61K9/00
Inventor 梁文权胡英许东航梁漪
Owner ZHEJIANG UNIV
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