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Granisetron and/or hydrochloride patch thereof

A hydrochloride patch, the technology of hydrochloride, applied in the field of medicine, to achieve the effects of preventing and treating nausea and vomiting, high transdermal penetration rate, high and long-term continuous administration

Active Publication Date: 2013-04-17
DALIAN UNIV OF TECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] However, the technical effect of the prior art needs to be improved, and people expect to obtain a granisetron and / or its hydrochloride patch with a better technical effect

Method used

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  • Granisetron and/or hydrochloride patch thereof
  • Granisetron and/or hydrochloride patch thereof
  • Granisetron and/or hydrochloride patch thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] According to the formula (percentage by weight) shown in Table 1, granisetron is first dissolved in the solvent, then the acrylate pressure-sensitive adhesive is added, mixed and stirred evenly to prepare the drug-loaded pressure-sensitive adhesive, and then the usual pressure-sensitive adhesive paste technology is used. Apply the prepared drug-loaded matrix solution to a certain thickness on the plastic film treated with silicone resin, and cover it with a surface film that has not been treated with silicone resin after drying to make a matrix type with a thickness of 0.05 mm. Pressure-sensitive adhesive transdermal preparations.

[0042] Table 1

[0043] SMD number granisetron Pressure Sensitive Adhesive Type Pressure Sensitive Adhesive 1-1 4％ 87-2100 to 100% 1-2 4％ 87-2852 to 100% 1-3 4％ 87-2979 to 100% 1-4 4％ 87-2074 to 100% 1-5 4％ 87-2196 to 100% 1-6 4％ 87-2677 to 100%

Embodiment 2

[0045] Table 2

[0046] SMD number granisetron Organic acid (molar ratio to drug) Pressure sensitive adhesive (durotak) 1-1 4％ - to 100% (2677) 1-2 4％ Acetic acid 0.77% (1:1) to 100% (2677) 1-3 4％ Caprylic acid 1.85% (1:1) to 100% (2677) 1-4 4％ Fumaric acid 1.48% (5:1) to 100% (2677) 1-5 4％ Sorbic acid 1.44% (1:1) to 100% (2677) 1-6 4％ Oleic acid 3.61% (1:1) to 100% (2677) 1-7 6％ Stearic acid 2.61% (3:1) to 100% (2196) 1-8 8％ Arachidic Acid 4% (2:1) to 100% (2852) 1-9 4％ Oleic acid 1.81% and sorbic acid

[0047] (the above table includes saturated fatty acids with carbon atoms of 2, 8, 10, 18, and 20 and unsaturated fatty acids with carbon atoms of 4, 6, and 16) according to the formula (weight percentage) shown in Table 2. Dissolve agar and organic acid in co-solvent, then add acrylate pressure-sensitive adhesive, mix and stir evenly to prepare drug-loaded pressure-sensitive adhesive, ...

Embodiment 3

[0049] According to the formula (percentage by weight) shown in Table 3, granisetron and substances other than the pressure-sensitive adhesive durotak87-2677 were first dissolved in the solvent, then the acrylate pressure-sensitive adhesive was added, mixed, and stirred evenly to prepare the drug-loaded pressure-sensitive adhesive. Then use the usual pressure-sensitive adhesive paste technology to apply the prepared drug-loaded matrix solution to a certain thickness on the plastic film treated with silicone resin, and cover it with a surface film that has not been treated with silicone resin after drying , to make a matrix-type pressure-sensitive adhesive transdermal preparation with a thickness of 0.15 mm.

[0050] table 3

[0051]

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Abstract

The invention relates to a Granisetron and / or a hydrochloride patch thereof, which comprises a lining layer, a medicine carrying pressure sensitive adhesive layer containing the Granisetron or / and the hydrochloride thereof, and an anti-sticking layer, wherein the medicine carrying pressure sensitive adhesive layer is characterized in that pressure sensitive adhesive contains carboxylic groups; the content of the Granisetron or / and the hydrochloride thereof in percentage by weight is 1%-12%; the medicine carrying pressure sensitive adhesive layer contains metal ions capable of enabling the pressure sensitive adhesive to generate cross linking, and the content of the metal ions in the medicine carrying pressure sensitive adhesive layer in percentage by weight is 0.05%-2%; and the medicine carrying pressure sensitive adhesive layer contains organic acids with 2-18 carbon atoms, and the molar ratio of the adding amount of the organic acids to the adding amount of the Granisetron or / and the hydrochloride thereof is (1-5):1. The patch of the invention can obviously increase the percutaneous infiltration capacity of the Granisetron and improve the solvent resistant and ageing resistant action of the substrate, can be applied to preventing and treating the symptoms of nausea, emesis and the like caused by radiotherapy, chemotherapy and operations, and has great foreseeable economic value and social value.

Description

technical field [0001] The present invention relates to the technical field of medicine, and in particular provides a 5-HT 3 A transdermal delivery system for receptor antagonist granisetron and / or its hydrochloride, specifically granisetron and / or its hydrochloride patch. Background technique [0002] Side effects such as nausea and vomiting accompanying cancer radiotherapy and chemotherapy are difficult to control and avoid. Vomiting not only makes patients feel unpleasant, but also may cause severe dehydration and malnutrition, bringing great pain to patients. [0003] Chemotherapy, radiotherapy, surgery and other factors can cause enterochromaffin cells to release 5-HT, and 5-HT can activate 5-HT in the central or vagus nerve 3 receptors that trigger the gag reflex. 5-HT 3 Receptor antagonists can block the gag reflex induced by 5-HT through both peripheral and central mechanisms. Therefore 5-HT 3 Receptor antagonists can be used as antiemetic drugs, such as granis...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/70A61K31/439A61P1/08A61P35/00
Inventor 田昕汪晴李细海孙玉明
Owner DALIAN UNIV OF TECH
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