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Nimodipine lipid nanoparticle and preparation technology thereof

A nimodipine lipid and lipid nanoparticle technology, which is applied to medical preparations containing no active ingredients, medical preparations containing active ingredients, drug combinations, etc., can solve the problem of long hydration time, easy leakage of drugs, and reduced Production efficiency and other issues, to achieve the effect of avoiding organic solvent residues, uniform distribution of active ingredients, and avoiding direct contact

Active Publication Date: 2017-08-08
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Because nimodipine is a poorly soluble drug, the clinically used nimodipine injection (trade name Nimodi) all uses higher concentration of ethanol to increase the solubility of the drug to reach the medicinal concentration, thus leading to the clinical application of nimodipine injection. There are great limitations in use: firstly, a special three-way infusion set must be used for simultaneous infusion with glucose or normal saline; secondly, nimodipine injection must be infused slowly at a rate of 1-2 mg / h. Note, otherwise the patient cannot tolerate its side effects, that is, the infusion time required for 10 mg of medicine generally needs at least 5 hours; again, Nimodipine injection is prone to crystallization during the mixed infusion process with glucose or normal saline, resulting in medication safety. The long-term use of this preparation will cause severe irritation of the patient's blood vessels and increase the risk of venous inflammation
[0006] Although the liposome prepared by CN1418626A disclosed nimodipine nano-liposome preparation technology has better safety, biocompatibility and transmembrane property, its stability is not very good, and the medicine is easy to leak. The particle diameter of the liposome prepared by the method is also relatively large
The nimodipine solid lipid nanoparticles disclosed in CN102552156B have the advantages of high efficiency, low toxicity, stability, etc., but its drug content is low, resulting in increased dosage and administration times, and the preparation process of the product is complicated, which is not conducive to industrial production
The nimodipine lipid nanoparticle composition disclosed by CN100486577C has the advantages of long-acting, low toxicity, stability, etc., but only selects phospholipids as the carrier component, resulting in lower drug loading, and longer hydration time, which reduces production efficiency
A nimodipine nanoparticle disclosed in CN103494820A realizes the co-loading of multiple drugs, and improves the blood drug concentration of nimodipine to a certain extent, but the polymer material carrier is not easy to realize expanded production, and is prone to certain biological toxicity

Method used

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  • Nimodipine lipid nanoparticle and preparation technology thereof
  • Nimodipine lipid nanoparticle and preparation technology thereof
  • Nimodipine lipid nanoparticle and preparation technology thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0028] Prescription composition:

[0029]

[0030] Preparation Process:

[0031] (1) The mixed lipids of glyceryl distearate and propylene glycol dicaprate according to a certain mass ratio are melted in a water bath at 80° C. for subsequent use;

[0032] (2) Dissolve the prescribed amount of nimodipine in an appropriate amount of ethanol in a water bath at 80°C, then slowly add it to the melted mixed lipids, then heat and evaporate the solvent to form an oil phase, and set aside;

[0033] (3) Evenly disperse the prescribed amount of Tween 80 in an appropriate amount of pure water under the condition of a water bath at 80° C. to form a water phase for later use;

[0034] (4) adding the oil phase in step (2) to the water phase in step (3), while high-speed shearing for a period of time to form colostrum;

[0035] (5) The colostrum obtained in the step (4) is quickly added to a high-pressure homogenizer and circulated several times, and cooled to room temperature to obtain ...

Embodiment 2

[0038] Prescription composition:

[0039]

[0040] Preparation Process:

[0041] (1) place the glyceryl distearate of prescription quantity under 80 ℃ of water bath conditions and melt, standby;

[0042] (2) Dissolve the prescribed amount of nimodipine in an appropriate amount of ethanol in a water bath at 80°C, then slowly add it to the melted solid lipid, then heat and evaporate the solvent to form an oil phase, and set aside;

[0043] (3) Evenly disperse the prescribed amount of Tween 80 in an appropriate amount of pure water under the condition of a water bath at 80° C. to form a water phase for later use;

[0044] (4) adding the oil phase in step (2) to the water phase in step (3), while high-speed shearing for a period of time to form colostrum;

[0045] (5) Add the colostrum obtained in step (4) into a high-pressure homogenizer and circulate it several times, and cool to room temperature to obtain the nimodipine lipid nanoparticle colloidal dispersion.

[0046] The ...

Embodiment 3

[0048] Prescription composition:

[0049]

[0050] Preparation Process:

[0051] (1) The glyceryl monostearate and propylene glycol dicaprate mixed lipids of the prescribed amount are melted in a water bath at 80° C. according to a certain mass ratio, and set aside;

[0052] (2) Dissolve the prescribed amount of nimodipine in an appropriate amount of ethanol in a water bath at 80°C, then slowly add it to the melted mixed lipids, then heat and evaporate the solvent to form an oil phase, and set aside;

[0053] (3) Evenly disperse the prescribed amount of Tween 80 in an appropriate amount of pure water under the condition of a water bath at 80° C. to form a water phase for later use;

[0054] (4) adding the oil phase in step (2) to the water phase in step (3), while high-speed shearing for a period of time to form colostrum;

[0055] (5) Add the colostrum obtained in step (4) into a high-pressure homogenizer and circulate it several times, and cool to room temperature to ob...

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Abstract

The invention belongs to the field of pharmaceutical preparations and discloses a nimodipine lipid nanoparticle and a preparation technology thereof. The lipid nanoparticle is prepared by an emulsification-evaporation technique combined with a high pressure homogenization method, and a drug is encapsulated in a lipid carrier to form a stable and homogeneous colloidal solution. The prepared lipid nanoparticle is small in nanoparticle size, high in dispersity, good in stability, and capable of releasing the drug slowly and permanently and improving the in vivo absorption of the drug. The preparation technology is simple, low in cost, free from residual organic solvent, low in biological toxicity, and easy to realize industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and discloses a nimodipine lipid nanoparticle and a preparation process thereof. Background technique [0002] Nimodipine is a second-generation 1,4-dihydropyridine calcium ion antagonist, which is extremely insoluble in water and highly fat-soluble. Clinically, it is mainly used in the treatment of ischemic cerebrovascular disease, cerebral vasospasm caused by subarachnoid hemorrhage, sudden deafness, migraine and other diseases. In addition, there have been many research reports on the protective effect of nimodipine on the central nervous system. If it has the effect of promoting memory, it can be used to prevent and treat Alzheimer's disease (AD). [0003] Nimodipine is widely used clinically, but it is an insoluble drug with low solubility and strong hepatic first-pass effect so that its bioavailability is very low (only 2.7%-27.9%), and its biological half-life (0.5-1.0 h) Short...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K9/52A61K31/4422A61K47/14A61P9/10A61P27/16A61P25/06A61P9/12
Inventor 周建平丁杨姜孟劳
Owner CHINA PHARM UNIV
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