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Why was norcantharidin made into a new dosage form?

Dec 27, 2019

The moth is a dried body of the Coleoptera aurantidae, the southern giant spotted pheasant or the small yellow-and-black spotted moth, Cantharidin is the main effective component of cantharidium anticancer. Norcantharidin is a derivative derived from the artificial removal of the two methyl groups of cantharidin, which is a new type of low-toxic anticancer drug. Compared with cantharidin, it significantly reduces the stimulating effect on the urinary system and enhances the anti-cancer effect. At the same time, it can increase the number of white blood cells and regulate immunity without bone marrow inhibitory effect. As a result, more and more attention has been paid. At present, NCTD and its sodium salts are mainly used in the clinical treatment of various cancers such as liver cancer, esophageal cancer, gastric cancer and cardia cancer, especially ideal drugs for treating primary liver cancer.

The anticancer mechanism of norcantharidin is relatively clear, and it has become a research hotspot for many pharmaceutical workers. According to reports in the literature, norcantharidin is mainly used in the treatment of liver cancer clinically, and there have been cases of treatment of esophageal cancer, hepatitis B, and genital warts.

Norcantharidin

This article will review the current research status of norcantharidin in pharmaceutical dosage forms. At present, norcantharidin is mainly used clinically in tablets and injections. Although norcantharidin significantly reduced the toxicity of cantharidin, it was not eliminated, so its maximum dosage was severely restricted. In order to make norcantharidin better exert its clinical effect, norcantharidin can be prepared into a new dosage form, utilizing the targeted properties of the new dosage form, fully exerting the antitumor activity of norcantharidin and reducing its toxic and side effects.

Norcantharidin 99%

1. Oral preparations.

The application of ultrafine pulverization technology and drip pill preparation technology to make norcantharidin drop pills and norcantharidin soft capsules with accurate contents, high bioavailability and good stability overcome the long dissolution and dissolution of tablets. And low dissolution rate, large amount of auxiliary materials, etc.

Because of its simple production process and low cost, it has a good prospect.

2. Slow release agent.

Animal tests confirmed that NCTD-poloxamer 407 sustained-release preparation

It can reduce the toxicity and improve the curative effect by delaying the release rate of NCTD and increasing the time of direct interaction with tumor cells.

3. Microemulsion.

The study found that under the same dosage conditions, the NCTD microemulsion can maintain a higher concentration in the body for a longer period of time, and the targeting indexes in the liver and kidney are 0.43 and 0.12, respectively, indicating that the norcantharidin microemulsion is less Acantharidin injection enhances the drug's liver targeting, reduces kidney distribution, and prolongs the circulation time of the drug in mice to a certain extent.