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Brain-targeting nimodipine nano-suspension and preparation method thereof

A nimodipine nano- and nano-suspension technology, which is applied in the field of medicine, can solve the problems of short biological half-life of drugs, serious liver first-pass effect, and low solubility of nimodipine, and achieve uniform particle size, good application prospects, and improved The effect of the therapeutic effect

Inactive Publication Date: 2016-05-25
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] Aiming at the problems of low nimodipine solubility, poor bioavailability, short biological half-life of the drug, frequent administration, and serious liver first-pass effect, the present invention designs a stable nimodipine nano-mixed Suspension, using poloxamer and Tween to deliver drugs to the brain to achieve targeted drug delivery

Method used

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  • Brain-targeting nimodipine nano-suspension and preparation method thereof
  • Brain-targeting nimodipine nano-suspension and preparation method thereof
  • Brain-targeting nimodipine nano-suspension and preparation method thereof

Examples

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Effect test

Embodiment 1

[0030] Preparation of brain-targeted nimodipine nanosuspension: Accurately weigh 60 mg of nimodipine, dissolve it in 2 mL of ethanol, and magnetically stir until completely dissolved to obtain solution A. Accurately weigh 100 mg of Poloxamer 188 and 60 mg of Tween 80 and dissolve them in 50 mL of water, and magnetically stir until completely dissolved to obtain solution B. Under the condition of ultrasonication in an ice bath, slowly inject solution A into solution B with a syringe, and ultrasonicate at 400W for 10 minutes. Ethanol was removed by rotary evaporation at 45°C, and the resulting crude nanosuspension was placed in a high-pressure homogenizer at 0°C, under the homogenization condition of 500 bar for 4 times and then 900 bar for 15 times to obtain the brain-targeted Ni Modipine nanosuspension. The measured particle size was 204.2nm, the polydispersity coefficient was 0.24, and the Zeta potential was -23.9mV.

Embodiment 2

[0032] This example is basically the same as Example 1, except that the dosage of nimodipine is 30 mg. The particle size of the nanosuspension was determined to be 336.8nm, the polydispersity coefficient was 0.24, and the Zeta potential was -25.0mV.

Embodiment 3

[0034] This example is basically the same as Example 1, except that the homogenization condition is 4 times at 500 bar and then 15 times at 700 bar. The particle size of the nanosuspension was determined to be 229.2nm, the polydispersity coefficient was 0.26, and the Zeta potential was -22.6mV.

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Abstract

The invention discloses a brain-targeting nimodipine nano-suspension and a preparation method thereof. According to the preparation method, nimodipine serving as a model drug is subjected to ultrasonic supersonic coprecipitation and high pressure homogenization by using poloxamer 188 and tween 80 as stabilizing agents to prepare the brain-targeting nimodipine nano-suspension. The nano-suspension has a grain size of 200-230nm, a polydispersity index of 0.24+ / -0.056 and Zeta electric potential of (-23.8+ / -1.05)mV. The nano-suspension can be used for achieving the effect of brain-targeting administration by utilizing poloxamer and tween as the stabilizing agents.

Description

technical field [0001] The invention relates to a brain-targeted nimodipine nanosuspension and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Nimodipine is a second-generation 1,4-dihydropyridine calcium antagonist, which was synthesized by Bayer in Germany in the 1980s. Molecular formula is C 21 h 26 N 2 o 7 , the molecular weight is 418.45. The drug is extremely insoluble in water and very fat soluble. Its pharmacological effect is that nimodipine can effectively regulate the level of intracellular calcium ions, and can inhibit the influx of extracellular calcium ions in the case of cerebral ischemia (ie, calcium ion overload), so that cells can maintain normal physiological functions. Experimental studies in vivo have shown that nimodipine can selectively act on cerebral blood vessels, significantly expand cerebral blood vessels, improve reperfusion after cerebral ischemia, and prevent post-ischemic vasospas...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K47/10A61K47/26A61K31/4422A61P9/10A61P25/00A61P27/16A61P25/06A61P25/28
CPCA61K9/10A61K31/4422A61K47/10A61K47/26
Inventor 王柏刘蒙蒙
Owner CHINA PHARM UNIV
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