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A long-acting transdermal patch containing granisetron

A transdermal patch, long-acting technology, applied in the field of medicine, can solve the problems of skin damage, irritation of the back skin, adverse skin reactions, etc., and achieve the effect of good adhesion and less skin irritation

Active Publication Date: 2016-04-27
BEIJING CAS MICRONEEDLE TECH LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, experiments have shown that the use of simple acrylic pressure-sensitive adhesives containing functional groups such as carboxyl groups or hydroxyl groups are all irritating to the skin on the back of New Zealand white rabbits, especially the addition of various chemical penetration enhancers in the prescription have different degrees of skin irritation. damage
And if the prescription contains excess sodium hydroxide, it can also cause adverse reactions to the patient's skin

Method used

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  • A long-acting transdermal patch containing granisetron
  • A long-acting transdermal patch containing granisetron
  • A long-acting transdermal patch containing granisetron

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] According to the data in Table 1, weigh 20g 387-2510(A) with 20g pressure sensitive adhesive 87-2677(B), add it to a round bottom flask, stir in a water bath at 40°C, wait for it to mix evenly to form a mixed pressure-sensitive adhesive, and transfer it to a vial for later use. Weigh 10g of the mixed pressure-sensitive adhesive and add it to a round-bottomed flask containing 10ml of ethyl acetate, stir at room temperature to mix, then add 0.21g of free granisetron base, and stir in a water bath at 30°C until the granisetron base After dissolving, stir evenly and transfer it to the anti-adhesive layer for coating, then dry it in a blast oven at 70°C for 20-120 minutes, press it with a lining film, and cut it into a suitable size.

Embodiment 2

[0039] According to the data in Table 1, weigh 10g 387-2510(A) with 20g pressure sensitive adhesive 87-2677(B), add it to a round bottom flask, stir in a water bath at 50°C, wait for it to mix evenly to form a mixed pressure-sensitive adhesive, and transfer it to a vial for later use. Weigh 10g of mixed pressure-sensitive adhesive and add it to a round-bottomed flask containing 10ml of ethyl acetate, stir at room temperature to mix, then add 0.3g of free granisetron base, and stir in a water bath at 45°C until the granisetron base After dissolving, stir evenly and transfer it to the anti-adhesive layer for coating, then dry it in a blast oven at 70°C for 20-120 minutes, press it with a lining film, and cut it into a suitable size.

Embodiment 6-8

[0041] Using the method of Example 1, according to the weight percentages of the substances given in Table 1, the patches of Examples 3-8 were prepared.

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PUM

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Abstract

The invention discloses a long-acting transdermal patch containing granisetron. The transdermal patch comprises a lining membrane, a pressure-sensitive adhesive skeleton medicine-storing layer and an antisticking layer. The pressure-sensitive adhesive skeleton medicine-storing layer comprises mixed pressure-sensitive adhesives and the granisetron, wherein the mixed pressure-sensitive adhesives comprise a hydroxy-containing acrylate pressure-sensitive adhesive and a carboxyl-containing acrylate pressure-sensitive adhesive in a weight ratio of 1:5-2:1. The long-acting transdermal patch adopts the mixed pressure-sensitive adhesives as a skeleton is provided. The granisetron can exist in the pressure-sensitive adhesive skeleton stably in a dissolved state, does not crystallize or precipitate, and can be stably released on skin because of unique infiltration promoting effects of the transdermal patch. The transdermal patch is advantaged by low skin irritation.

Description

technical field [0001] The invention belongs to the technical field of medicine, and particularly provides a long-acting transdermal patch of granisetron, a 5-HT3 receptor antagonist, and a preparation method thereof. Background technique [0002] Nausea and vomiting caused by chemotherapy and radiotherapy is one of the most common and most influential adverse reactions in cancer treatment. Nausea and vomiting caused by chemotherapy and radiotherapy can be divided into acute, delayed, and anticipatory processes, which generally last for several days, which greatly affects the quality of life of patients and their confidence in treatment. [0003] Granisetron is a potent and highly selective serotonin (5-HT3) receptor antagonist in the central and peripheral nervous systems, which can effectively inhibit the nausea and vomiting induced by chemotherapy and radiotherapy. Currently, granisetron is clinically available in two forms: oral administration and intravenous administra...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K31/439A61K47/34A61P1/08A61K47/32
CPCA61K9/0002A61K9/0014A61K9/7069A61K31/439
Inventor 高云华杨国忠
Owner BEIJING CAS MICRONEEDLE TECH LTD
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