Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

A kind of nimodipine solid dispersion and tablet preparation method thereof

A nimodipine solid and solid dispersion technology, which is applied in the field of medicine, can solve problems such as recrystallization and crystallization, and achieve the effects of accelerated dissolution, low hygroscopicity, and improved bioavailability

Active Publication Date: 2021-04-06
LIAOCHENG UNIV
View PDF4 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The preparation of amorphous SD is an effective technical means to improve the solubility of poorly soluble drugs, but the high energy state of SD leads to the risk of recrystallization during storage, in vitro dissolution and in vivo absorption.
Tang Xing and others used the hot-melt extrusion technology to prepare nimodipine solid dispersions, tablets, etc. with copovidone VA64 (Kollidon VA64) as auxiliary materials, and acrylic resin EPO Kollidon VA64 is used as an auxiliary material to prepare solid dispersions and comparative studies on tablets; Hyo-JungLee et al. used PVPk30 as a carrier to prepare nimodipine solid dispersions and sustained-release tablets by solvent method, and the dissolution rate in vitro increased; but the solid dispersions prepared above After the dissolution of the body or tablet, there will be crystallization

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
  • A kind of nimodipine solid dispersion and tablet preparation method thereof
  • A kind of nimodipine solid dispersion and tablet preparation method thereof
  • A kind of nimodipine solid dispersion and tablet preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1 Differential scanning calorimetry analysis: Weigh 4mg of the sample and place it in an aluminum pan, using alumina as a reference, heat up in a nitrogen flow in the range of 25°C to 150°C at a rate of 10°C / min scanning.

[0036] Such as figure 1 As shown, it can be seen that the melting point of the nimodipine bulk drug (NM) is 125°C-127°C, and the bulk drug is transformed from a crystalline state to an amorphous state after being prepared into a solid dispersion (SD).

Embodiment 2

[0038](1) Prepare 5000 mL of phosphate buffer solution of pH 6.8;

[0039] (2) Prepare nimodipine solution: take by weighing 300 mg of nimodipine crude drug into a 10 mL measuring bottle, add absolute ethanol to dissolve and settle to the mark;

[0040] (3) Weigh PVP K30 70.2g, PVP K25 71.1g, HPMCAS-HF 70.3g, HPMCAS-HF120.9g, HPMCAS-HF 271.5g into a beaker, add 200mL of pH6.8 phosphate buffer solution, ultrasonically It dissolves, moves in the dissolution cup, adds the phosphate buffer solution of remaining 700mL pH6.8, adjusts the speed of dissolution apparatus to be 75rpm, and temperature is 37 ℃, respectively gets 1mL above-mentioned nimodipine solution of preparation in each dissolution cup, Samples were taken at different time points to detect the content of nimodipine.

[0041] The experimental results are shown in Table 1:

[0042] Table 1

[0043]

[0044] Such as figure 2 And the above results show that HPMCAS-HF has a better crystallization inhibitory effect ...

Embodiment 3

[0045] Example 3 Accurately weigh 30.0 mg of nimodipine bulk drug onto weighing paper, place it in a blast drying oven heated to 130°C for 30 minutes, take it out and put it at room temperature to obtain amorphous nimodipine bulk drug , taking nimodipine crystalline API (API), amorphous API (amorphous API), 30% NM-HPMCASHF physical mixture (PM), solid dispersion (SD) for in vitro dissolution experiments.

[0046] Such as image 3 As shown, it can be seen that the dissolution rate of nimodipine and HPMCASHF auxiliary materials through the solid dispersion (SD) prepared by hot-melt extrusion technology is the highest.

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
glass transition temperatureaaaaaaaaaa
melting pointaaaaaaaaaa
Login to View More

Abstract

The invention discloses a nimodipine solid dispersion and a preparation method thereof. The solid dispersion is prepared from nimodipine as an active ingredient and an enteric polymer carrier. The solid dispersion is prepared by hot-melt extrusion technology, and nimodipine exists in the solid dispersion in an amorphous state. The enteric polymer carrier can not only greatly improve the dissolution rate of nimodipine, but also has a good effect of inhibiting crystallization, which solves the problem of recrystallization after dissolution of nimodipine, thereby improving bioavailability and reducing adverse reactions.

Description

[0001] Technical field: the invention belongs to the technical field of medicine, in particular to a nimodipine solid dispersion and a method for preparing a tablet thereof. Background technique: [0002] Nimodipine, the English name is Nimodipine, the chemical name is 1-methylethyl-2-methoxyethyl, 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl) -3,5-pyridinedicarboxylate, the structural formula is as follows: [0003] [0004] The pharmacological property of nimodipine is to effectively regulate the level of intracellular calcium to maintain normal physiological functions. The effect on cerebrovascular is particularly prominent, and can be combined with specific receptors of the central nervous system. It is mostly used clinically to effectively prevent and treat cerebral vasospasm, sudden deafness, and migraine caused by subarachnoid hemorrhage. Selective dilation of cerebral blood vessels at an appropriate dose hardly affects peripheral blood vessels, but increasing the dose...

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
Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K31/4422A61K47/38A61K9/20A61P9/12A61P9/10A61P27/16A61P25/06A61P9/00
CPCA61K9/146A61K9/2054A61K31/4422
Inventor 韩军张勤秀赵燕娜王正平刘敏
Owner LIAOCHENG UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com