Nimodipine freeze-dried solid lipid nanoparticle and preparation method thereof

Abstract

The invention discloses a nimodipine freeze-dried solid lipid nanoparticle, which is prepared by mixing and freeze-drying a solid lipid nanoparticle solution and a freeze-drying protection agent. 20g-40g of the freeze-drying protection agent is added into every 100 mL of the solid lipid nanoparticle solution. Every 100 mL of the solid lipid nanoparticle solution is prepared from of the following raw materials by weight: 2-20mg of nimodipine, 0.5-4g of phospholipid, 0-0.2g of cholesterol sodium sulfate salt, 0.02-0.4g of propylene glycol block polyether and the balance of a phosphate bufferingsolution; and the freeze-drying protection agent is one or more of cane sugar, glucose, trehalose, maltose and mannitol. According to the nimodipine freeze-dried solid lipid nanoparticle, the medicament loading efficiency can be up to 0.2 mg / mL, the state is good after re-dissolving, the physicochemical property is accordant with an intravenous injection requirement, and the adaptability of a patient can be improved; and the nimodipine freeze-dried solid lipid nanoparticle has the characteristics of high efficiency, low toxicity, stability, and the like, and is suitable for being applied clinically.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a nimodipine freeze-dried solid lipid nanoparticle and a preparation method thereof. Background technique [0002] Nimodipine (Nimodipine, NMD) is the second-generation dihydropyridine calcium ion antagonist, which was synthesized by German Bayer in the 1980s. Its structural formula is as follows: [0003] [0004] Nimodipine can selectively act on calcium channels, specifically reversibly bind to related receptors, regulate the calcium ion concentration in vascular smooth muscle, cause smooth muscle relaxation, reverse vasospasm, and improve blood supply. Because nimodipine is a fat-soluble drug, it can pass through the blood-brain barrier, so it can protect brain cells and improve their tolerance to hypoxia. It is commonly used clinically for ischemic cerebrovascular disease, cerebral vasospasm caused by subarachnoid hemorrhage, stroke and migraine, and can als...

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Problems solved by technology

[0007] The liposome prepared by the disclosed nimodipine nano-liposome preparation technology of CN1418626A has good safety, biocompatibility and transmembrane property, but its stability is not very good, and the liposome prepared by this method The particle size of the plastid is also too large

CN1554340A provides a nimodipine nano liposome with good brain targeting and its precursor freeze-dried composition, its average particle diameter is below 100nm, but it does not give the particle size after reconstitution of the freeze-dried composition. Diameter change and stability data

CN1903173A discloses a kind of its preparation method of nimodipine nanoparticle, its drug load and stability are acceptable, but particle diameter is bigger, and the average particle diameter after reconstitution is below 0.3 μ m, and larger particle diameter will not Good for brain targeting but bad for intravenous administration

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