Clevidipine butyrate liquid liposome preparation

Abstract

The invention discloses a clevidipine butyrate liposome preparation and a preparation method thereof. The preparation includes 0.05wt%(wt%)-0.1%(wt%) of clevidipine butyrate, 40%(wt%) -70%(wt%) of phosphatidylcholine, 10%(wt%)-40%(wt%) of phosphatidyl glycerol, 10%(wt%)-30%(wt%) of sterol, and 0.55%(wt%)-3.3%(wt%) of stabilizer. The stabilizer contains a component A and a component B, wherein the component A is selected from one or more of oleic acid, sodium oleate, linoleic acid and sodium linoleate; and the component B is selected from one or more of vitamin E, coenzyme Q10, propyl gallate and ascorbyl palmitate. The liposome prepared by the method is in the form of liquid, and can be stored for a long time, therefore not only the potential safety hazard due to use of middle-chain and long-chain triglyceride in the traditional clevidipine butyrate emulsion is thoroughly solved, but also the freeze-drying operation in the traditional liposome preparation is omitted and the production cost is reduced; moreover, the liposome preparation is convenient for clinical application, overcomes the defect of uneven quality of redissolved freeze-drying liposome preparation and is beneficial to increase of the compliance and the medication safety of a patient.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a clevidipine butyrate liposome preparation, in particular to a clevidipine butyrate liquid liposome preparation containing a stabilizer and a preparation method thereof. Background technique [0002] Clevidipine butyrate (clevidipine butyrate) is a new generation of ultra-short-acting dihydropyridine calcium channel blocker, which is the first new intravenous antihypertensive drug approved by the FDA in the past ten years. The drug was developed by AstraZeneca as a short-term control drug for perioperative hypertension. In 2002, The Medicines Company obtained product authorization from AstraZeneca, and it was launched in the United States on August 1, 2008. The chemical structure of clevidipine butyrate is similar to that of felodipine, and it is easily metabolized by esterases in blood and tissues, and hydrolyzed into inactive metabolites, so its activity in the body...

AI Technical Summary

Problems solved by technology

On the one hand, this method completely solves the potential safety hazard caused by the use of medium and long-chain triglycerides in previous clevidipine butyrate emulsions; on the other hand, it solves the stability problem of liquid liposomes during long-term storage , save the freeze-drying step, greatly reducing the time cost and economic cost of liposome development, the present invention is realized through the following technical solutions:

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