Nimodipine lipid nano particle compositions, and its prepn. method

A nimodipine lipid and nanoparticle technology, applied in the field of medicine, can solve the problems of reducing the application scope of the drug, difficult to redissolve, inconvenient operation, etc., and achieves the benefits of transportation, storage and clinical application, increased cerebral blood flow, and reduced work. amount of effect

Inactive Publication Date: 2003-05-21
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the poor water solubility of nimodipine, the commercially available nimodipine injection contains about 30% organic solvent, and the organic solvent is not beneficial to the body. Dipine is precipitated, treatment is interrupted, and the drug is scrapped. In order to avoid the precipitation of nimodipine during the infusion process, the technology used by Bayer Company in Germany is to use accessories such as three-way valves and infusion pumps when administering drugs. This obviously has high

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0005] Embodiment 1: the preparation of nimodipine lipid nanoparticles

[0006] prescription:

[0007] Nimodipine 0.1g

[0008] Soy Lecithin 1g

[0009] Poloxamer 1g

[0010] Proper amount of ethanol

[0011] Appropriate amount of water for injection

[0012] Make 1000ml

[0013] Preparation process: Weigh the prescribed amount of soybean lecithin, Poloxamer and nimodipine, put them in a beaker, add an appropriate amount of ethanol to dissolve, shake off the ethanol, add water for injection, and hydrate for 1 to 2 hours to obtain nimodipine lipid Granular solution, then high-speed stirring under nitrogen flow or ultrasonic treatment or pressurized extrusion, filtered with 0.2um microporous membrane, and added water for injection to a total of 1000ml. The obtained liquid was potted and sterilized under the protection of nitrogen to obtain nimodipine lipid nanoparticles. The obtained nanoparticles were subjected to particle size measurement, and th...

Embodiment 2

[0014] Embodiment 2: the preparation of nimodipine lipid nanoparticles

[0015] prescription:

[0016] Nimodipine 0.1g

[0017] Soy Lecithin 10g

[0018] Proper amount of ethanol

[0019] Appropriate amount of water for injection

[0020] Make 1000ml

[0021] Preparation process: same as above, the average particle size is 205nm.

Embodiment 3

[0022] Embodiment 3: the preparation of nimodipine lipid nanoparticles

[0023] prescription:

[0024] Nimodipine 0.1g

[0025] Hydrogenated Soy Lecithin 5g

[0026] Poloxamer 1g

[0027] Dextrose for injection 50

[0028] Proper amount of ethanol

[0029] Appropriate amount of water for injection

[0030] Make 1000ml

[0031] Preparation process: Weigh the hydrogenated soybean lecithin, Poloxamer and nimodipine in the prescribed amount, put them in a beaker, add an appropriate amount of ethanol to dissolve them, shake off the ethanol, and set aside; take another glucose for injection, dissolve it with water for injection, add In the above-mentioned nimodipine lipid mixture, hydrate for 0.5 to 1 hour to obtain a nimodipine lipid particle solution, then process it with a high-pressure homogenizer under nitrogen flow for 10 minutes, filter with a 0.2um microporous membrane, and add water for injection to Total 1000ml. The obtained liquid was pott...

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Abstract

The present invention relates to a nimodipine lipid nano granular composition and its preparation method. It can be made into injection, its composition includes 0.002-0.2% of nimodipine, 0.02-10% ofphospholipid and 0-2% of Poloxamer. Its preparation method includes the following steps: dissolving the above-mentioned materials in ethyl alcohol, adding injection water, making hydration for 1-2 hr. to obtain nimodipine lipid granular solution, high-pressure homogenizing for 10 min. under the condition of nitrogen gas flow, filtering with 0.2 micrometer micropore filtering membrane, adding injection water, filling, sealing, sterilizing so as to obtain the invented product.

Description

Technical field: [0001] The invention relates to the technical field of medicine, in particular to a nimodipine lipid nanoparticle composition and a preparation method thereof. Background technique: [0002] Nimodipine is a calcium channel blocker, which can dilate blood vessels and prevent cerebral ischemic damage. It is an ideal drug for patients with cerebrovascular diseases. No obvious adverse reactions (Li Zhaoren Nimodipine New Drug and Clinical 1987, 6(2): 12-124). It has the following characteristics: (1) Selective expansion of cerebral blood vessels: (2) Increase cerebral blood flow without 'blood stealing' phenomenon: (3) Increase cerebral blood circulation without increasing cerebral metabolism: (4) Anti-platelet aggregation. It is clinically used to treat subarachnoid hemorrhage, migraine, stroke, cerebrovascular insufficiency, sudden deafness, vestibular nystagmus, etc. In view of the above-mentioned characteristics, there are many dosage forms of nimodipine d...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/4422A61P9/10
Inventor 邓意辉吴琼王绍宁
Owner SHENYANG PHARMA UNIVERSITY
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