Preparation of artemether/benflumetol compound fat emulsion for injection and application of artemether/benflumetol compound fat emulsion in malaria treatment

Abstract

The invention discloses an artemether / benflumetol compound fat emulsion preparation which contains 0.01-1.5 percent by weight of artemether, 0.01-3.5 percent by weight of benflumetol, 10.0-30.0 percent by weight of injection oil, 0.6-30.0 percent by weight of emulsifier, 0-10 percent by weight of solubilizer, 00.01-5 percent by weight of co-emulsifier, 2.25-7 percent by weight of isoosmolar agent, 0.002-0.075 percent of antioxidant and the balance of injection water. The invention further discloses a preparation method as well as pharmacodynamics and safety elevation of the artemether / benflumetol compound fat emulsion preparation. The artemether / benflumetol compound fat emulsion preparation has the characteristics of good biocompatibility, high physical stability, good safety, high medicament-loading capacity and the like and is convenient to prepare. An in-vivo pharmacodynamic animal experiment proves that the artemether / benflumetol compound fat emulsion preparation has a remarkably killing role in plasmodium and can be used for effectively controlling the relapse of the plasmodium. Meanwhile, the artemether / benflumetol compound fat emulsion preparation can be used for providing nutritions required for the body of a patient suffering from malaria, improving the lymphocyte activity and assisting the patient in resisting malaria and getting recovery.

Description

technical field [0001] The invention relates to a fat emulsion injection, in particular to an artemether / lumefantrine compound fat emulsion injection. The route of administration is intravenous or intramuscular injection. It also relates to the preparation process, formula, application, pharmacodynamic research and safety evaluation of the artemether / lumefantrine compound fat emulsion injection. Background technique [0002] Artemisinin is an effective antimalarial monomer isolated and purified from Artemisia annua by Chinese scholars in the early 1970s. It is a new type of sesquiterpene lactone compound containing a peroxide bridge structure. The characteristics of no drug resistance and low toxicity are called "the greatest hope for the treatment of malaria" by the World Health Organization, and can be regarded as the greatest contribution of Chinese pharmaceutical workers to human society. Its discovery has become another important milestone in the world's antimalarial ...

AI Technical Summary

Problems solved by technology

These are all oral dosage forms, and cannot be used for emergency treatment of malaria in clinical use, and although they have improved the oral bioavailability of lumefantrine to varying degrees, but due to the fat dependence of lumefantrine (ie, lumefantrine The oral absorption of lumefantrine is affected by food, and the patient eats high-fat food when taking the drug, so as to have a higher drug absorption rate and a higher blood concentration to kill malaria parasites), so that lumefantrine needs to increase the dosage and frequency of oral administration To ensure the clinical efficacy of the drug

Therefore, the dose of benzefantrine in clinical use is as high as 1840mg, or even 2880mg. Such long-term high-dose use will accelerate the development of drug resistance, thereby greatly shortening the service life of benzefantrine and reducing the use effect

In addition, from the perspective of patients, high doses and frequent medication will undoubtedly increase the economic burden. In fact, high costs have become the main barrier to the treatment of malaria patients.

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