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Nimoldipine new nano liposome, its precursor freeze dryed matter and its preparing method

A technology of nimodipine nanometer and nimodipine, which is applied in freeze-drying delivery, drug combination, pharmaceutical formulation and other directions, can solve the problems of large particle size of liposomes and poor stability of lipid nanoparticles, and achieve high quality stable effect

Inactive Publication Date: 2004-12-15
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

But also there is certain defect in its formula, the prepared lipid nanoparticle stability according to the technical scheme it provides is not good, and the liposome particle size prepared by its method is also too large

Method used

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  • Nimoldipine new nano liposome, its precursor freeze dryed matter and its preparing method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0083] Preparation of Nimodipine Nanoliposomes:

[0084] Nimodipine 10mg

[0085] Hydrogenated egg yolk phospholipids 150mg

[0086] Cholesterol 20mg

[0087] poloxamer188 200mg

[0088] Sodium deoxycholate 10mg

[0089] Weigh the prescribed amount of nimodipine, hydrogenated egg yolk phospholipids, cholesterol, poloxamer188, sodium deoxycholate, etc., and dissolve them in 3ml of absolute ethanol to obtain a lipid solution, transfer it to a 1000ml eggplant-shaped bottle, and keep the temperature at 60°C In a water bath, use a rotary thin film evaporator to remove ethanol and form a uniform lipid film on the bottle wall. Measure 10ml of water and medium, pour it into an eggplant-shaped bottle, shake it gently, keep a constant temperature of 60°C, elute the lipid film and disperse it in the hydration medium to dissolve, and then obtain a liposome suspension, put it in a water bath for ultrasound Ultrasound to a translucent colloidal solution (keep in a 60°C water bath), and...

Embodiment 2

[0091] Preparation of Nimodipine Novel Nano-Liposome Precursor Lyophilizate

[0092] Prescription is the same as embodiment 1

[0093] Preparation process: After obtaining the liposome suspension with Example 1, place it in a refrigerator at -20°C for 12 hours, then freeze-dry to remove the solvent, and obtain the lyophilized product of nimodipine nano-liposome precursor. Nitrogen filled and sealed, protected from light.

Embodiment 3

[0095] Preparation of Nimodipine Nanoliposome Precursor Lyophilizate

[0096] prescription:

[0097] Nimodipine 10mg

[0098] Egg yolk phospholipids 250mg

[0099] Cholesterol 30mg

[0100] poloxamer188 100mg

[0101] Polyoxyethylene castor oil 50mg

[0102] Sodium deoxycholate 15mg

[0103] Mannitol 500mg

[0104] Leucine 150mg

[0105] Preparation process: with embodiment 1,2. The encapsulation efficiency of the obtained nimodipine nano liposome is 89.1%, and the average particle diameter is 20.3nm.

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Abstract

The present invention relates to pharmaceutical, and is especially new nano Nimoldipine liposome, its freeze dried precursor and preparation process. The nano Nimoldipine liposome consists of Nimoldipine, phosphatide, cholesterol, surfactant and antioxidant. The Nimoldipine liposome has stable quality, small average size and stable wrapping rate as high as 80%.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a novel nanoliposome of nimodipine, its precursor freeze-dried product and a preparation method thereof. Background technique [0002] Ischemic encephalopathy, such as stroke and subarachnoid hemorrhage, is a common and frequently-occurring clinical disease with a wide population distribution. Together with cardiovascular disease, it is also known as one of the three major killers (cardiovascular and cerebrovascular diseases, tumors and diabetes) that endanger human health. number one killer. Nimodipine (Nimodipine) is the first-line drug for the treatment of the above-mentioned diseases. It is a 1,4-dihydropyridine calcium ion antagonist that has been widely used clinically. It has shown the effect of dilating cerebral arteries and increasing cerebral blood flow in both animals and humans. It has a therapeutic effect on various cerebrovascular dysfunctions. At presen...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/12A61K9/19A61K31/4422A61P9/12
Inventor 朱家壁郑莹
Owner CHINA PHARM UNIV
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