Lyophilized composition of nimodipine

A composition and freeze-drying technology, which can be used in freeze-dried delivery, drug combination, cardiovascular system diseases, etc., and can solve problems such as unstable illumination of small water needles

Inactive Publication Date: 2003-06-18
KUNMING LONGJIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Studies have shown that the content of conventional small water needles containing nimodipine is placed under natural light for about 6 minutes, and its content drops by about 10%, indicating that small water needles are extremely unstable against light.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Embodiment 1: prepare the powder injection containing phospholipid

[0018] Take 2 mg of nimodipine, 10 mg of phospholipid and 2 mg of cholesterol, add 5 ml of absolute ethanol, stir until completely dissolved, dry under reduced pressure on a rotary evaporator, remove the solvent, add 5 ml of phosphate buffer, stir until uniform, and use ultrasonic oscillation , filter, add mannitol 100mg, put in a sterile vial, freeze-dry in a freeze dryer, and seal. That is, light yellow-light yellow nimodipine powder injection is obtained.

Embodiment 2

[0019] Embodiment 2: Preparation of powder injection containing cyclodextrin

[0020] Take 2mg of nimodipine, stir with 2ml of absolute ethanol until completely dissolved, take another 20mg of 2-hydroxypropyl-β-cyclodextrin, add 7ml of water to dissolve, add the nimodipine solution to 2-hydroxypropyl In the solution of base-β-cyclodextrin, a uniform cyclodextrin inclusion compound was prepared. Dry under reduced pressure on a rotary evaporator to evaporate ethanol. Under the condition of stirring, add 300 mg of mannitol, filter the solution with a sterilized vertical melting funnel in advance, put the filtrate in a sterile vial, freeze-dry it in a freeze dryer, and seal it. That is, light yellow-light yellow nimodipine powder injection is obtained.

[0021] It was confirmed by X-ray diffraction method that the pharmaceutical composition prepared in Example 2 was in the form of clathrate.

Embodiment 3

[0022] Embodiment 3: prepare the powder injection containing surfactant

[0023] Take 2 mg of nimodipine, 0.15 g of Tween-80, 0.2 g of polyethylene glycol-400, 20 mg of polyoxyethylene castor oil and 0.3 g of mannitol, add 5 ml of water, and stir until completely dissolved. Filter with a 0.22 μm microporous membrane, put it in a sterile vial to obtain a slightly yellow clear solution, put it in a freeze dryer for freeze-drying, and seal it. That is, light yellow-light yellow nimodipine powder injection is obtained.

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PUM

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Abstract

A freeze dried nimodipine composition in the form of injection contains nimodipine, phosphatide, cyclodextrin, and its derivative or surfactant. Its advantages are high solubility, high stability and high safety.

Description

technical field [0001] The invention relates to a pharmaceutical composition containing water-insoluble nimodipine, in particular to a freeze-dried pharmaceutical composition containing nimodipine and a preparation method thereof. Background technique [0002] Nimodipine (molecular formula is C 21 h 26 N 2 o 2 , with a molecular weight of 418.45) is a 1,4-dihydropyridine calcium channel antagonist, which can selectively act on cerebral blood vessels, has the effect of dilating cerebral arteries and increasing cerebral blood flow, and is mainly used for the treatment of ischemic cerebrovascular diseases , Prevention and treatment of cerebral vasospasm, sudden deafness, high blood pressure and migraine after subarachnoid hemorrhage. [0003] At present, there are many dosage forms of nimodipine on the market at home and abroad, wherein oral dosage forms include ordinary tablets, sustained-release tablets, capsules, and soft capsules; injections inc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K9/19A61K31/4422A61P9/10
Inventor 徐新盛文艳秋
Owner KUNMING LONGJIN PHARMA
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