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Palonosetron transdermal patch and preparation method thereof

A patch and agar base technology, applied in the field of medicine, can solve problems such as poor compliance, unfavorable use by patients, inconvenient administration of injections, etc., and achieve the effect of simple production process and low production cost

Active Publication Date: 2019-06-14
GUANGDONG HONGSHANHU PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the commercially available preparations of this drug are mainly injections and capsules, but the administration of injections is inconvenient, the compliance is poor, and multiple injections can easily lead to phlebitis. Oral capsules are not conducive to drug administration in the treatment of vomiting and are not conducive to those who have difficulty swallowing patient use

Method used

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  • Palonosetron transdermal patch and preparation method thereof
  • Palonosetron transdermal patch and preparation method thereof
  • Palonosetron transdermal patch and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Dissolve 0.1g (5% w / w) palonosetron base in 5.278g polyacrylate pressure-sensitive adhesive, add 0.002g vitamin E, add 2ml ethyl acetate and mix well, let stand at room temperature for 1h to degas, transfer Coating on the anti-adhesive layer, drying the solvent, and compounding the upper backing layer to form a palonosetron transdermal patch.

Embodiment 2

[0049]Dissolve 0.1g of palonosetron base in 4.722g of polyacrylate pressure-sensitive adhesive, add 0.2g of IPM and 0.002g of vitamin E, add 2ml of ethyl acetate and mix well, let it stand at room temperature for 1h to degas, transfer coating on On the anti-adhesive layer, the solvent is dried in the drying process, and the upper backing layer is compounded to form a palonosetron transdermal patch.

Embodiment 3

[0051] Swell 0.2g E100 with ethyl acetate, add 4.167g polyacrylic acid pressure-sensitive adhesive to form a uniform pressure-sensitive adhesive matrix, dissolve 0.1g palonosetron base in the matrix, add 0.2g IPM and 0.002g VE , add 2ml of ethyl acetate and mix well, let it stand at room temperature for 1h to degas, transfer and coat on the anti-adhesive layer, dry the solvent during the process, and compound the upper backing layer to form a palonosetron transdermal patch.

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Abstract

The invention discloses a palonosetron transdermal patch and a preparation method thereof. The palonosetron transdermal patch is composed of a backing layer, a medicine carrying pressure-sensitive adhesive layer and an anti-bonding layer. The medicine carrying pressure-sensitive adhesive layer comprises palonosetron, polyacrylate resin, a polyacrylate pressure-sensitive adhesive, a chemical penetration enhancer and an antioxidant, the palonosetron accounts for 1% to 5% of the total weight of the medicine carrying pressure-sensitive adhesive layer, the medicine content of the patch ranges from0.5 mg to 20.0 mg, preferably 0.5 mg to 2.0 mg, and the area of the patch is smaller than or equal to 10 cm<2>. According to the palonosetron transdermal patch, the polyacrylate resin is added, the medicine percutaneous penetration rate is increased, the content of unknown impurities is reduced, and the patch meets the dosing requirement of 5-7 days after being dosed for 3 days.

Description

Technical field: [0001] The invention belongs to the technical field of medicine, and in particular relates to a palonosetron transdermal patch and a preparation method thereof. Background technique: [0002] Cancer chemotherapy kills cancer cells and also causes toxicity to normal cells, which causes unbearable pain for patients after chemotherapy. Chemotherapy-induced nausea and vomiting (CINV) remains a major side effect, and despite a plethora of novel antiemetics, delayed effects are often observed. [0003] Palonosetron is a second-generation highly selective and high-affinity 5-HT3 receptor antagonist, which has a longer half-life compared with the first-generation 5-HT3 receptor antagonist, and is approved by the US FDA for use in Prevention and treatment of delayed nausea and vomiting induced by chemotherapy. At present, the commercially available preparations of this drug are mainly injections and capsules, but the administration of injections is inconvenient, th...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K47/32A61K31/473A61P1/08
Inventor 王高华汪晴徐春霞方燕秋李晓晖
Owner GUANGDONG HONGSHANHU PHARM CO LTD
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