Arteannuin transdermal patch substrate, preparation method and arteannuin transdermal patch thereof

Abstract

The invention relates to arteannuin transdermal patch matrix, a preparation method and arteannuin transdermal patch thereof. The matrix of the patch contains acrylic acid pressure-sensitive adhesive, transdermal accelerating agent and arteannuin medicament. The pressure-sensitive adhesive, the transdermal accelerating agent and the medicament are blended, and then coated and dried to prepare the transdermal patch with viscosity. The patch can make the medicament released stably and prolong half-life; and through transdermal experiments in vitro and in vivo, permeating amount of arteannuin for full skin of nude mice can reach more than 500 mu g / cm<2> in 24 hours. Transdermal experiments on mouse show that the patch is applied once, and concentration of blood medicament is stable after 96 hours and kept at 100ng / ml. Pharmacodynamical experiments on the nude mice show that after the nude mice are affected by plasmodium, the backs of the nude mice are applied by the patch, the patch is replaced every day in four days continuously, and then the suppression ratio is 15.44 percent after 1 day of patch application and 96.51 percent after 4 days.

Description

technical field [0001] The invention relates to an artemisinin transdermal patch matrix, which contains a penetration enhancer and a pressure-sensitive adhesive, and a preparation method for the transdermal patch matrix, which contains the matrix and the drug artemisinin patch. Background technique [0002] Malaria is a widespread epidemic that seriously endangers people's health. It ranks first among the four major epidemics. At present, 40% of the world's people live in malaria-endemic areas. More than 90% of malaria patients in Africa, Southeast Asia, and South America are infected with Plasmodium falciparum, which is seriously harmful. If the disease is not treated for 2-3 days, it will turn into dangerous malaria and cerebral malaria, which can easily lead to death. Malaria kills one million children in Africa every year. Quinine, chloroquine, aldipine, etc. used to be effective in the past. Since the 1960s, drug resistance has developed, that is, it has lost its due ...

AI Technical Summary

Problems solved by technology

Mefloquine, a new antimalarial drug developed in the United States in the 1970s and 1980s, had already exposed signs of drug resistance. By the end of the 20th century, it had lost its superiority due to resistance problems.

[0010] 1. It is insoluble in water and cannot be made into a dosage form suitable for injection or intravenous drip to rescue critically ill patients. It can only be made into tablets orally. Once the patient is unconscious, it cannot be taken orally, and it is difficult for children to take it when they have high fever or vomiting. Dosage not guaranteed

[0011] 2. The re-ignition rate within one month is relatively high, up to 11%

[0012] The above problems are because although artemisinin is absorbed quickly, it is also decomposed and destroyed quickly, and the half-life is short. The Institute of Chinese Materia Medica, China Academy of Traditional Chinese Medicine first reported that the blood concentration of artemisinin reached its peak in 1 hour after oral administration, and 50% was excreted in 4 hours. (T1 / 2), it can be seen that the effective concentration in the blood cannot be maintained for a long time

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