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Percutaneous-absorption palonosetron patch and preparation method thereof

A technology of palonosetron and absorption enhancer, applied in the field of medicine

Active Publication Date: 2014-10-01
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the prior art, there is no relevant report on the patch of this type of palonosetron

Method used

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  • Percutaneous-absorption palonosetron patch and preparation method thereof
  • Percutaneous-absorption palonosetron patch and preparation method thereof
  • Percutaneous-absorption palonosetron patch and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0027] 0.5 g of palonosetron hydrochloride was dissolved in 20 ml of distilled water, and an aqueous solution of sodium hydroxide was added dropwise until no white turbidity occurred. Extract with 120ml of ethyl acetate for 5 times, combine the extracts, add an appropriate amount of anhydrous sodium sulfate for dehydration, and then dry by rotary evaporation to obtain palonosetron free base.

Embodiment 2

[0029]Disperse 0.121g of palonosetron hydrochloride (equivalent to 0.108g free base) into 2.55g of the polyacrylate pressure-sensitive adhesive DT-2287 of American National Starch Co. Dry at 60°C for 15 minutes, then cover with a backing material including PVC or non-woven fabric, and die-cut to make a patch with a thickness of 30 μm.

Embodiment 3

[0031] Palonosetron free base 0.108g obtained by ethyl acetate extraction was dispersed in 2.55g polyacrylate pressure-sensitive adhesive DT-2287 of National Starch Company of the United States, fully mixed, evenly coated on the release layer, and after 60 After drying at ℃ for 15 min, it was covered with a backing material including PVC or non-woven fabric, and punched to make a patch with a thickness of 30 μm.

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Abstract

The invention belongs to the technical field of medicines and relates to a percutaneous-absorption palonosetron patch and a preparation method thereof. The patch is composed of a backing layer, a medicine-carrying pressure-sensitive adhesive layer and an anti-sticking layer; the medicine-carrying pressure-sensitive adhesive layer comprises a beta-cyclodextrin inclusion compound of palonosetron free alkali, a pressure-sensitive adhesive and a percutaneous absorption enhancer, wherein the beta-cyclodextrin inclusion compound of the palonosetron free alkali accounts for 4.78%-20.09% of the total weight, preferably 9%-19%, the pressure-sensitive adhesive accounts for 68.80%-95.22% of the total weight and the percutaneous absorption enhancer accounts for 0-11.11wt% of the total weight. In the beta-cyclodextrin inclusion compound of the palonosetron free alkali, the ratio of the palonosetron free alkali to the beta-cyclodextrin inclusion compound is 1: (1-3). The percutaneous-absorption palonosetron patch is provided with the beta-cyclodextrin inclusion compound of the palonosetron free alkali, and therefore, compared with a patch with non-inclusion medicine, the slow release of the medicine within 7 days is realized.

Description

Technical field: [0001] The invention belongs to the technical field of medicine, and relates to a palonosetron percutaneous absorption patch and a preparation method thereof. Background technique: [0002] In the past 30 years, the incidence of cancer in the world has been increasing at an average annual rate of 3% to 5%. Cancer may surpass cardiovascular and cerebrovascular diseases to become the number one threat to human life. According to statistics, 70% to 80% of cancer patients receiving chemotherapy and radiotherapy will experience nausea and vomiting (chemotherapy-induced nausea and vomiting, CINV). Nausea and vomiting will cause dehydration, electrolyte imbalance, aspiration pneumonia, aggravation of the patient's condition, weakness, depression, intolerable vomiting, fear or even refusal of radiotherapy and chemotherapy, and will also increase the psychological and economic burden of family members and increase the workload of nursing . Therefore, it is imminent...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K9/70A61K31/473A61P1/08A61K47/69
Inventor 方亮惠美权鹏
Owner SHENYANG PHARMA UNIVERSITY
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