Composition containing nimodipine, preparation method and application thereof

A technology of nimodipine and a composition is applied in the field of nimodipine-containing composition and preparation thereof, which can solve the problems of high drug safety risk, large toxic and side effects, poor stability and the like, and achieves simplified process flow and high drug loading capacity. , good stability

Active Publication Date: 2014-04-09
李宏 +1
View PDF2 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The defect of the prior art is that the existing nimodipine injection has

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Composition containing nimodipine, preparation method and application thereof
  • Composition containing nimodipine, preparation method and application thereof
  • Composition containing nimodipine, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0041] The embodiment of the present invention provides a preparation method of a composition containing nimodipine, comprising:

[0042] Take water for injection, adjust the pH of the water for injection to be 8-12, and form an aqueous phase;

[0043] Take the surfactant and add it to the water phase, under nitrogen protection, under the condition of water temperature of 50-70°C, shear the surfactant until it is uniformly dispersed;

[0044] Adding nimodipine into the above-mentioned solution containing surfactant, shearing to obtain a suspension;

[0045] Homogenize the suspension at 40°C to 65°C to obtain a nanosuspension with a particle size of less than 200nm (nanometer);

[0046] The nanosuspension was sterilized by circulating steam under the conditions of 121° C. and F0≧12.

[0047] In the preparation method of the composition containing nimodipine, there is no need to adopt airflow pulverization or precipitation with organic solvent and remove the organic solvent, onl...

Embodiment 1

[0056] Take 1000L of water for injection, and adjust the pH of the water for injection to 8-12 with 2% sodium hydroxide solution to form an aqueous phase;

[0057] Weigh the amount of surfactant (egg yolk lecithin) shown in Table 1, the content of which is the mass concentration, add it to the water phase, under the protection of nitrogen, cut the surfactant until it is evenly dispersed, and control the water temperature at 50-70 °C;

[0058] The nimodipine (content is mass concentration) of the amount shown in Table 1 is added in the above-mentioned solution containing surfactant, and sheared to form a suspension;

[0059] Homogenize the suspension in the way of gradient boosting: first carry out 300-500bar (bar) low-pressure circulation treatment, and then perform 900-1100bar high-pressure circulation treatment to prepare a nano-suspension with a particle size of less than 200nm. The homogenization temperature Controlled at 40~65℃;

[0060] The nanosuspension is sterilized ...

Embodiment 2～15

[0063] Each component and content etc. of preparation composition of embodiment 2~15 are as shown in table 1, and embodiment 2~15 except nimodipine content, surfactant content and aqueous phase pH and embodiment 1 are different, all the other and implementation Example 1 is the same.

[0064] Table 1 The components used in Examples 1 to 15 and the test result table

[0065]

[0066]

[0067] It can be seen from Table 1 that when egg yolk lecithin is used as a surfactant, and the content is 0.2% to 3%, especially at 0.2% to 1%, the particle size of the prepared nimodipine nanosuspension injection is small and uniform , the pH value of the final product is 6.5~8.5, especially when the pH value is 7.5~8.5, the absolute value of Zata potential is greater than 25mV, even for embodiment 12, Zata potential is greater than 30mV, illustrates that the nimodipine nano-mixture prepared by the present invention Suspension injections are more stable.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

PropertyMeasurementUnit
Particle sizeaaaaaaaaaa
Login to view more

Abstract

The invention relates to the technical field of calcium antagonist medicines, and discloses a composition containing nimodipine, a preparation method and application thereof. The composition containing nimodipine comprises the following components in mass concentration: 0.02-1 percent of nimodipine, and 0.2-3 percent of surfactant, wherein the pH value of the composition containing nimodipine is in a range of 6.5-8.5. Stimulating ethanol is not adopted in the composition containing nimodipine, so that the dosing risk of the composition containing nimodipine can be reduced, and the stability of the composition containing nimodipine can be improved.

Description

technical field [0001] The invention relates to the technical field of calcium antagonist drugs, in particular to a composition containing nimodipine and its preparation method and application. Background technique [0002] Nimodipine, also known as Nimotop, is the second-generation pyridine calcium antagonist. Produced by multiple manufacturers. Because nimodipine has high lipophilicity, easily penetrates the blood-brain barrier, selectively dilates cerebral blood vessels, and significantly reverses the spasm of the basilar artery and anterior spinal artery. The treatment of lesions, that is, for ischemic cerebrovascular disease, treatment of mild or moderate hypertension, prevention and treatment of cerebral vasospasm after subarachnoid hemorrhage, sudden deafness and migraine, etc., is the first choice for cerebrovascular treatment at present Drugs, especially for senile dementia have high clinical application value. [0003] Nimodipine preparations commonly used in cl...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
IPC IPC(8): A61K31/4422A61K9/10A61K47/24A61P9/10A61P9/12A61P27/16A61P25/06A61P25/28
Inventor 高山李宏岳昌林钟己未高洁
Owner 李宏
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap