Granisetron and dexamethasone compound percutaneous controlled release patch and preparation method thereof

A technology of dexamethasone and compound recipe, applied in the field of pharmaceutical preparations, can solve the problems of unstable penetration, large difference in oil-water partition coefficient, etc.

Inactive Publication Date: 2013-07-31
NANJING UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The invention discloses a compound transdermal controlled-release patch of granisetron and dexamethasone. By selecting a suitable transdermal penetration enhancer, it overcomes the large difference in oil-water partition coefficient between granisetron and dexamethasone, which leads to unstable penetration At the same time, two drugs with different physical and chemical properties, granisetron and dexamethasone, have a higher penetration and maintain a higher blood concentration for a longer period of time

Method used

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  • Granisetron and dexamethasone compound percutaneous controlled release patch and preparation method thereof
  • Granisetron and dexamethasone compound percutaneous controlled release patch and preparation method thereof
  • Granisetron and dexamethasone compound percutaneous controlled release patch and preparation method thereof

Examples

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Effect test

Embodiment 1

[0038] Prepare granisetron-dexamethasone compound transdermal controlled-release patch, which is composed of a backing layer, a pressure-sensitive adhesive skeleton-type drug-containing reservoir layer and a protective film. The preparation method is as follows:

[0039] (1) Accurately weigh 0.18g of granisetron, 0.48g of dexamethasone, 0.15g of succinic acid, add 6ml of ethanol and stir until dissolved, slowly add 1g of dibutyl sebacate and 0.16g of azone and stir until the solution becomes clear. Add 1.8g Eudragit E100, and continue to stir until the transparent gel-like drug-containing pressure-sensitive adhesive reservoir viscose;

[0040] (2) Heat the above-mentioned drug-containing pressure-sensitive adhesive reservoir viscose until the ethanol volatilizes to obtain a drug-containing glue with a suitable consistency, degas it by ultrasonic, and apply it on a certain area of ​​CoTran by salivating process TM Put it on the 9720 polyethylene backing film, put it in an oven ...

Embodiment 2

[0055] Prepare granisetron-dexamethasone compound transdermal controlled-release patch, which is composed of a backing layer, a pressure-sensitive adhesive skeleton-type drug-containing reservoir layer and a protective film. The preparation method is as follows:

[0056] (1) Accurately weigh 0.18g granisetron, 0.48g dexamethasone, 0.15g succinic acid, add 6ml ethanol and stir until dissolved, slowly add 1g polyethylene glycol 400 and 0.16g azone and stir until the solution is clear, then add 1.8g Eudragit E100, continue to stir until transparent gel-like medicated pressure-sensitive adhesive reservoir viscose;

[0057] (2) Heat the above-mentioned drug-containing pressure-sensitive adhesive reservoir viscose until the ethanol volatilizes to obtain a drug-containing glue with a suitable consistency, degas it by ultrasonic, and apply it on a certain area of ​​CoTran by salivating process TM Put it on the 9720 polyethylene backing film, put it in an oven at 60°C to cure for 40 mi...

Embodiment 3

[0059] Prepare granisetron-dexamethasone compound transdermal controlled-release patch, which is composed of a backing layer, a pressure-sensitive adhesive skeleton type drug-containing reservoir layer and a protective film. The preparation method is as follows:

[0060] (1) Accurately weigh 0.18g granisetron, 0.48g dexamethasone, 0.16g citric acid, add 6ml ethanol and stir until dissolved, slowly add 1g dibutyl sebacate and 0.16g azone and stir until the solution is clear, then add 1.8g of Eudragit E100, continue to stir until the viscose of the drug-containing pressure-sensitive adhesive reservoir is transparent; Ultrasonic degassing, CoTran coated on a certain area by salivation process TM Put it on the 9720 polyethylene backing film, put it in an oven at 60°C to cure for 40 minutes, and laminate it with inert siliconized release paper after cooling.

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Abstract

The invention relates to the field of pharmaceutic preparations and in particular relates to a granisetron and dexamethasone compound percutaneous controlled release patch and a preparation method thereof. The granisetron and dexamethasone compound percutaneous controlled release patch is characterized by being composed of a lining layer, a pressure-sensitive adhesive skeleton pattern medicine-containing storage layer and a protective film, wherein the pressure-sensitive adhesive skeleton pattern medicine-containing storage layer contains granisetron, dexamethasone, a transdermal penetration enhancer, a cross-linking agent, a plasticizer and pressure-sensitive adhesive, the transdermal penetration enhancer is azone preferably, and the content of azone is 2-5wt% based on the total weight of the pressure-sensitive adhesive skeleton pattern medicine-containing storage layer. The granisetron and dexamethasone compound percutaneous controlled release patch overcomes the defect that osmolality is unstable as difference between oil-water partition coefficients of granisetron and dexamethasone is large, and two medicines, namely granisetron and dexamethasone with different physical and chemical properties, have high osmolality and also maintain high blood concentration in a long time.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a compound transdermal controlled-release patch for treating nausea and vomiting caused by chemotherapy, radiotherapy or postoperative treatment and a preparation method thereof. Background technique [0002] The chemical name of granisetron is 1-methyl-N-(9-methyl-9-azabicyclo[3,3,1]nonan-3-yl)-1H-indole-3- Formamide, the molecular formula is C 18 h 24 N 4 O, white crystalline powder, granisetron is a potent and highly selective 5-HT 3 Receptor antagonist, its anti-emetic mechanism is highly selective blocking of abdominal vagus nerve terminal neurons, as well as 5-HT on the chemoemetic receptor area of ​​the fourth ventricle and intestinal mucosal enterochromaffin cells 3 receptor. Granisetron and Modulation of 5-HT on Vomiting Tissue 3 Receptor binding sites have high affinity and high selectivity. [0003] The chemical name of Dexamethasone is 16α-methyl-11β,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/573A61K9/70A61K47/22A61P1/08A61K31/439
Inventor 任丽莉陈国广翟川
Owner NANJING UNIV OF TECH
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