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Nimodipine liposome for nasal delivery and preparation method thereof

A technology for nimodipine lipid and intranasal administration, applied in the field of pharmaceutical preparations, can solve problems such as limited improvement of drug absorption, and achieve the effects of avoiding or reducing irritant toxicity, low irritation, and improving therapeutic effect

Active Publication Date: 2015-06-17
TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, the gel preparation itself has a limited effect on improving drug absorption.

Method used

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  • Nimodipine liposome for nasal delivery and preparation method thereof
  • Nimodipine liposome for nasal delivery and preparation method thereof
  • Nimodipine liposome for nasal delivery and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] 1. Prescription:

[0034] Nimodipine-β-cyclodextrin inclusion compound 0.025g (the mass ratio of nimodipine to β-cyclodextrin is 1:3)

[0035]

[0036]

[0037] Second, the preparation method:

[0038] 1. Preparation of nimodipine-β-cyclodextrin inclusion compound by saturated aqueous solution method

[0039] Weigh 0.1g of nimodipine and 0.3g of β-cyclodextrin respectively, dissolve nimodipine in an appropriate amount of absolute ethanol (1ml) at 50°C, add β-cyclodextrin into distilled water to make a saturated aqueous solution; The solution was slowly added dropwise to a saturated aqueous solution of β-cyclodextrin, stirred in a water bath at 50°C for 3 hours; stored at 4°C overnight, filtered with suction, washed with water, washed with an appropriate amount of absolute ethanol to remove residual nimodipine, and dried at 40°C for 1 hour , that is, nimodipine-β-cyclodextrin inclusion compound (NM-β-CD).

[0040] 2. Preparation of nimodipine inclusion complex f...

Embodiment 2

[0043] 1. Prescription

[0044] Nimodipine-β-cyclodextrin inclusion compound 0.025g (the mass ratio of nimodipine to β-cyclodextrin is 1:10)

[0045]

[0046] Second, the preparation method:

[0047] 1. Preparation of nimodipine-β-cyclodextrin inclusion compound by saturated aqueous solution method

[0048] Weigh 0.1g of nimodipine and 1.0g of β-cyclodextrin respectively, dissolve nimodipine in an appropriate amount of absolute ethanol (1ml) at 40°C, add β-cyclodextrin into distilled water to make a saturated aqueous solution; The solution was slowly added dropwise to the saturated aqueous solution of β-cyclodextrin, stirred in a water bath at 40°C for 1 hour; stored at 4°C overnight, filtered with suction, washed with water, washed with an appropriate amount of absolute ethanol to remove residual nimodipine, and dried at 40°C for 1 hour , that is, nimodipine-β-cyclodextrin inclusion compound (NM-β-CD).

[0049] 2. Preparation of nimodipine inclusion complex flexible nan...

Embodiment 3

[0052] 1. Prescription:

[0053] Nimodipine-β-cyclodextrin inclusion compound 0.025g (the mass ratio of nimodipine to β-cyclodextrin is 1:1)

[0054]

[0055] Second, the preparation method:

[0056] 1. Preparation of nimodipine-β-cyclodextrin inclusion compound by saturated aqueous solution method

[0057] Weigh 0.1g of nimodipine and 0.1g of β-cyclodextrin respectively, dissolve nimodipine in an appropriate amount of absolute ethanol (1ml) at 65°C, add β-cyclodextrin into distilled water to make a saturated aqueous solution; The solution was slowly added dropwise to a saturated aqueous solution of β-cyclodextrin, stirred in a water bath at 65°C for 5 hours; stored at 4°C overnight, filtered with suction, washed with water, washed with an appropriate amount of absolute ethanol to remove residual nimodipine, and dried at 40°C for 1 hour , that is, nimodipine-β-cyclodextrin inclusion compound (NM-β-CD).

[0058] 2. Preparation of nimodipine inclusion complex flexible nano...

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Abstract

The invention discloses a nimodipine liposome for nasal delivery and a preparation method thereof, which belong to the field of pharmaceutic preparations. The nimodipine liposome for nasal delivery contains nimodipine and pharmaceutical effective auxiliary materials, wherein the concentration of the nimodipine is 2-9% w / v. The nimodipine liposome disclosed by the invention has the advantages that a nimodipine cyclodextrin inclusion compound flexible nano liposome is prepared according to the invention, so that the stability of the flexible nano liposome can be effectively improved, the direct exposure of nimodipine to nasal mucosa can be reduced, the toxic and side effects of drugs can be reduced, and the safety of nasal delivery can be improved; and the nimodipine liposome is absorbed rapidly, so that the nimodipine liposome can significantly improve the bioavailability of drugs, thereby facilitating the quick and full play of the pharmacologic action of nimodipine.

Description

technical field [0001] The invention relates to a nimodipine liposome for nasal administration and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] Nimodipine (Nimodipine, NM) is a dihydropyridine calcium ion antagonist with strong selective expansion of cerebrovascular effect. It has a good therapeutic effect on diseases such as stroke, sudden deafness, and brain dysfunction caused by chronic cerebrovascular disease. However, due to the poor water solubility of NM and the serious first-pass effect, the bioavailability of oral preparations such as tablets and capsules is low, and the average bioavailability is only 5-20%. In order to maintain the curative effect, patients need large doses and frequent medication. This not only increases the toxic and side effects of the drug, but also the concentration of nimodipine transported into the brain after oral administration is easily affected by changes in physiolo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/4422A61K47/48A61K47/44A61P25/06A61P9/10A61P27/16A61P25/00
Inventor 王亚静高秀梅张伟玲皮佳鑫胡利民王小莹孟亚飞
Owner TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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