Fat emulsion injection containing nimodipine and preparation method thereof

Abstract

The invention discloses a fat emulsion injection containing nimodipine and a preparation method thereof. The fat emulsion injection containing the nimodipine is prepared from nimodipine, injection oil, injection phospholipid, injection polyethylene glycol hydroxy stearate, an isoosmotic adjusting agent, a pH regulator and injection water. The preparation method comprises the following steps: mixing the nimodipine, the injection oil, the injection phospholipid with the injection polyethylene glycol hydroxy stearate, and agitating to clear and transparent as an oil phase; evenly mixing the isoosmotic adjusting agent with the injection water as a water phase; mixing the oil phase with the water phase; processing emulsion particles into the stated particle size range by adopting a two-step homogenization method; bulking and sterilizing after adjusting the pH value. The injection phospholipid and the polyethylene glycol hydroxy stearate are adopted as a mixed emulsifier, and the prepared fat emulsion injection containing the nimodipine can endure high-pressure moist heat sterilization, and does not need an expensive sterile manufacturing process, so that the production cost is greatly reduced, and industrial production is facilitated.

Description

technical field [0001] The invention relates to a fat emulsion injection of nimodipine and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Nimoldipine is a dihydropyridine calcium antagonist that selectively interacts with L-type Ca 2＋ Channel binding, high fat solubility, easy to pass through the blood-brain barrier, larger volume distribution and stronger receptor binding force in the brain than other blockers, its brain protection mechanism mainly includes: (1) direct Acts on neurons, blocks Ca 2＋ channel, reducing Ca 2＋ Influx, inhibition of intracellular Ca 2＋ Overload reduces secondary damage and cerebral edema; (2) Acts on vascular smooth muscle and inhibits depolarization of cerebral ischemic cells ＋ efflux, relieve Ca 2＋ Influx induces smooth muscle cell contraction and vasospasm, thereby improving cerebral circulation. Nimodipine, as a calcium antagonist with strong selective expansion of cerebral bloo...

AI Technical Summary

Problems solved by technology

However, because nimodipine is a poorly soluble drug, the clinically used nimodipine injection (trade name Nimodi) all uses higher concentration of ethanol to increase the solubility of the drug to reach the medicinal concentration, thus resulting in nimodipine injection There are great limitations in clinical use: first, a special three-way infusion set must be used for infusion with glucose or normal saline; second, nimodipine injection must be administered slowly at a rate of 1-2 mg / h. Otherwise, the patient cannot tolerate its side effects, that is, the infusion time required for 10mg of the drug generally needs at least 5 hours; again, Nimodipine injection is prone to crystallization during infusion with glucose or normal saline, resulting in The drug safety is reduced and long-term use of this preparation will cause serious irritation to the patient's blood vessels and increase the risk of venous inflammation

However, this type of ingredient has a strong hemolytic effect, and there is a greater risk when used for intravenous injection, and its dosage must be strictly regulated

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