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

Abstract

The invention discloses a benflumetol fat emulsion injection preparation which contains 0.03 to 35 wt% of benflumetol, 10.0 to 30.0 wt% of oil for injection, 0.6 to 30.0 wt% of an emulsifier, 0 to 10 wt% of a solubilizer, 0 to 5 wt% of a co-emulsifier, 2.25 to 7 wt% of an isotonic agent and 0.002 to 0.075 wt% of an anti-oxidant, with the balance being injection water. The invention also discloses a preparation method and pharmacodynamic and safety evaluation for the benflumetol fat emulsion injection preparation. The benflumetol fat emulsion provided by the invention has the characteristics of good biocompatibility, high physical stability, convenient preparation, good security, high drug loading capacity and the like, has a particle size of less than 200 mu m and is suitable for injection, e.g, intravenous injection and intramuscular injection. According to the invention, the characteristic that a soybean oil fat emulsion inhibits growth of plasmodium falciparum is utilized to enhance anti-malarial effects of drugs, to improve bioavailability of the drugs and to reduce toxic and side effects of the drugs; nutrients needed by the body of a patient with malaria can be provided, the activity of lymphocytes of the patient is improved, which assists the patient in resisting malaria and recovering.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to a fat emulsion injection, in particular to a benzefantrine fat emulsion injection and a preparation method thereof. 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 history after quinine. However, studies have shown that taking artemisinin preparations alone for a long time can easily cause pathogens to develop drug resistance, and combining artemisinin with ot...

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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