Camptothecinum derivative emulsion agent and preparation thereof

Abstract

The invention provides an emulsion of camptothecin derivative which comprises the components by weight: 0.01 to 0.1 percent of 10-methyl-9 nitryl camptothecin, 5 to 20 percent of oil for injection, 1-4 percent of emulsifier, 1-4 percent of co-emulsifier, 0 to 60 percent of solubilizer, 2 to 3 percent of glycerin of isotonizing agent and Vitamin E and the rest is water for injection; the sum of the percentages of all components is 100 percent. The emulsifier and a co-surfactant are dissolved in the oil for injection, heated and added with the solubilizer and 10-methyl-9 nitryl camptothecin to be dissolved, ant then added with the glycerin of isotonizing agent and the water for injection and made into primary emulsion by means of high speed homogenization or ultrasound, then further made into the emulsion by means of high pressure homogenization or micro jet. The prepared emulsion of the invention has uniform particle diameter and high content of drug and the appearance of the emulsion is a milky white or blue opalescence homogeneous system; meanwhile, compared with other preparation methods, the micro jet technique is adopted by the invention to prepare the emulsion, so as to ensure less loss of drug and better stability of the emulsion. The emulsion of camptothecin derivative of the invention has reasonable design and easy operation, which is suitable for practical use.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a novel anticancer compound (10-methyl-9-nitrocamptothecin, abbreviated as MONCPT) emulsion and a preparation method thereof. technical background [0002] More than 6 million people die of malignant tumors in the world every year, and about 1.7 million people die of cancer every year in my country, and the incidence rate is increasing year by year. Countries all over the world invest considerable manpower and material resources in the research of anticancer drugs every year. With the deepening of the research on the tumor mechanism, new targets of anti-tumor drugs are also emerging, among which the research on DNA topoisomerase I (TOPI) inhibitors is developing extremely rapidly. DNA topoisomerase I is located in the nucleus matrix. It is a monomeric enzyme protein containing 765 amino acids and a molecular weight of 100KD. It is located on chromosome 20. TOPI cuts one...

AI Technical Summary

Problems solved by technology

In the 1970s, camptothecin entered clinical research in the form of water-soluble sodium salt with its ring-opening structure. As a result, side effects such as severe bone marrow suppression, vomiting, diarrhea, and severe bleeding occurred, and the activity of the ring-opening form was greatly reduced, making clinical research difficult. continue

However, preliminary studies have shown that the drug is unstable, easily degraded when exposed to light, and has extremely poor solubility in water. The previous animal experiments were administered intramuscularly with its oil suspension. Therefore, how to make it into a dosage form suitable for clinical use , which is of great significance for the clinical prevention and treatment of tumors, as well as the research and development of camptothecin drugs in the future

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