Nimodipime nanometer suspension freeze-dried composition, its preparing method and use

A nimodipine nano-suspension technology, which is applied in the direction of freeze-drying delivery, drug combination, cardiovascular system diseases, etc., can solve the problems of toxic and side effects, difficulty in accurate dosage, and less dissolution, so as to facilitate transportation and storage, Avoid irritation and reduce toxic and side effects

Inactive Publication Date: 2007-10-03
SHANGHAI INST OF PHARMA IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because nimodipine has very little solubility in water (about 1.4ug/ml at 37 degrees), its solid preparations are less dissolved in the gastrointestinal tract, and there is a strong hepatic first-pass effect in addition, resulting in bioavailability after oral administration. Low degree, requiring multiple doses
[0004] Yet, contain the organic solvent of about 30% in the nimodipine injection of clinical use, cause the stimulation of administration and toxic side effect (such as pain, vasculitis etc.)
At the same time, in clinical application, dilution is often required, and the concentration of organic solvents is reduced, resulting in the precipitati

Method used

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  • Nimodipime nanometer suspension freeze-dried composition, its preparing method and use

Examples

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Example Embodiment

[0020] Example 1: Preparation of nimodipine nano-suspension by combining direct dispersion method and high-pressure homogenization method

[0021] Weigh 250mg sodium deoxycholic acid, 500mg poloxamer 188, add 50ml of water, magnetic stirring to make it completely dissolved, then add 500mg nimodipine crushed by airflow, magnetic stirring for 10min; high shear stirring for 1min; The suspension was homogenized under high pressure, and the conditions were 150 bar cycle 2 times, 500 bar cycle 2 times, and 1500 bar cycle 15 times. Finally, a milky white suspension was obtained with a measured particle size of 200 nm.

Example Embodiment

[0022] Example 2: Preparation of nimodipine nano-suspension by combining micro-precipitation method and high-pressure homogenization method

[0023] Add 500mg of poloxamer 188 to 48ml of water, magnetically stir to dissolve it completely; place 1ml of propylene glycol in a 50℃ water bath, and then add 250mg of soy lecithin and 100mg of nimodipine, and use a syringe to dissolve this solution. Add dropwise to 48ml of aqueous solution, magnetically stir for 20min; the initial suspension is homogenized at high pressure under the conditions of 150 bar cycle 2 times, 700 bar cycle 10 times, and finally a milky white suspension with a measured particle size of 350 nm.

Example Embodiment

[0024] Example 3: Preparation of nimodipine nano-suspension by combining direct dispersion method and ultrasonic method

[0025] Pipette 25ml of 1% Tween 80 solution into 25ml water, then add 500mg poloxamer 188, magnetically stir to make it evenly mixed, then add nimodipine 125mg, magnetically stir for 10min; high shear stirring for 1min; mix the initial The suspension is subjected to probe ultrasound, and the condition is ultrasound for 15 minutes at an intensity of 70Khz. In order to prevent excessive heat generation, it can be stopped every 5 minutes. The milky white suspension was finally obtained, and the measured particle size was 520nm.

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Abstract

A freeze-dried nano-suspension of nimodipine for intravenous injection with low stimulation and high curative effect and stability contains nimodipine, surfactant and scaffolding agent. Its preparing process and application are also disclosed.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a nimodipine nanosuspension freeze-dried composition, a preparation method and application thereof. Background technique [0002] Nimodipine (molecular formula is C 21 h 26 N 2 o 2 , with a molecular weight of 418.45) belongs to 1,4-dihydropyridine calcium channel antagonists, which can selectively act on cerebral blood vessels, dilate cerebral arteries, increase cerebral blood flow without increasing brain metabolism, and also have anti-platelet aggregation effects . Clinically, it is mainly used for the treatment of cerebral vasospasm, sudden deafness, high blood pressure and migraine after arachnoid hemorrhage. [0003] At present, there are many formulations of nimodipine on the market at home and abroad, mainly including oral agents (such as ordinary tablets, sustained-release tablets, capsules, soft capsules) and injections (small water injections and large i...

Claims

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Application Information

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IPC IPC(8): A61K31/4422A61K9/19A61P9/00
Inventor 陆伟根熊若兰
Owner SHANGHAI INST OF PHARMA IND
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