Nimodipine freeze-dried solid lipid nanoparticle and preparation method thereof

A technology of solid lipid nanometer and nimodide, applied in the field of medicine, can solve the problems of large particle size, large particle size of liposomes, unfavorable brain targeting, etc., and achieve the effects of improving compliance, good state and increasing solubility

Active Publication Date: 2013-08-21
西安远大科创医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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

Method used

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  • Nimodipine freeze-dried solid lipid nanoparticle and preparation method thereof
  • Nimodipine freeze-dried solid lipid nanoparticle and preparation method thereof
  • Nimodipine freeze-dried solid lipid nanoparticle and preparation method thereof

Examples

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Embodiment 1

[0037] The nimodipine freeze-dried solid lipid nanoparticles of the present embodiment are made by mixing the solid lipid nanoparticles solution with a lyoprotectant and then freeze-drying; 100mL of the solid lipid nanoparticles solution is made from the following raw materials: Nimodipine Modipine 20mg, phospholipid 2g, cholesterol sodium sulfate 0.1g, propylene glycol block polyether 0.2g, and the balance is phosphate buffer solution; the freeze-drying protectant is mannitol and trehalose, and the consumption of mannitol is 100mL The solid lipid nanoparticle solution uses 10g mannitol, and the consumption of trehalose is that every 100mL solid lipid nanoparticle solution uses 20g trehalose; the phospholipid is injection grade egg yolk lecithin PL-100M; the propylene glycol block polyether is Propylene glycol block polyether F-68.

[0038] The preparation method of the nimodipine freeze-dried solid lipid nanoparticles of the present embodiment comprises the following steps: ...

Embodiment 2

[0045] This example is the same as Example 1, except that the lyoprotectant is one or more than three of sucrose, glucose, trehalose, maltose and mannitol, or is sucrose, glucose, maltose and Two kinds of mannitol, or a mixture of sucrose, glucose and maltose and trehalose.

Embodiment 3

[0047] The nimodipine freeze-dried solid lipid nanoparticles of the present embodiment are made by mixing the solid lipid nanoparticles solution with a lyoprotectant and then freeze-drying; 100mL of the solid lipid nanoparticles solution is made from the following raw materials: Nimodipine Modipine 10mg, phospholipid 1g, cholesterol sodium sulfate 0.05g, propylene glycol block polyether 0.1g, and the balance is phosphate buffer solution; the freeze-drying protectant is mannitol and trehalose, and the consumption of mannitol is 100mL The solid lipid nanoparticle solution uses 10g mannitol, and the consumption of trehalose is that every 100mL solid lipid nanoparticle solution uses 20g trehalose; the phospholipid is injection grade egg yolk lecithin PL-100M; the propylene glycol block polyether is Propylene glycol block polyether F-68.

[0048] The preparation method of the nimodipine freeze-dried solid lipid nanoparticles of the present embodiment comprises the following steps: ...

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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...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K9/127A61K31/4422A61P9/10A61P25/00A61P25/06
Inventor 唐星关婷婷张宇何海冰王亚轩
Owner 西安远大科创医药科技有限公司
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