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

Sustained release capsule of sodium dexlansoprazole and preparation method thereof

A technology of dexlansoprazole sodium and lansoprazole sodium, which is applied to the sustained-release capsule of dexlansoprazole sodium and its preparation field, can solve the problem of low stability of preparation products and poor stability of dexlansoprazole , temperature and humidity sensitivity, etc.

Active Publication Date: 2017-05-17
NANJING HERON PHARM CO LTD +1
View PDF3 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] In view of the deficiencies in the prior art, the existing dexlansoprazole has poor stability, is sensitive to temperature and humidity, and is difficult to operate in the preparation process, the production cost is high, and the preparation product stability is not high. Due to the defects of the hot-melt extrusion process, such as obvious drug degradation in the hot-melt process, the invention provides a new crystal form A of dexlansoprazole sodium dimethylacetamide solvate and a preparation method thereof. Form A has better physical and chemical properties, suitable melting point, and strong stability. It is very convenient to be made into various pharmaceutical dosage forms, and is also convenient to be processed by hot-melt extrusion technology.

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
  • Sustained release capsule of sodium dexlansoprazole and preparation method thereof
  • Sustained release capsule of sodium dexlansoprazole and preparation method thereof
  • Sustained release capsule of sodium dexlansoprazole and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0083] Example 1 Preparation of the new crystal form A of dexlansoprazole sodium dimethylacetamide of the present invention

[0084] The present invention provides a new crystal form A of dexlansoprazole sodium dimethylacetamide solvate. Each mole of the new crystal form A contains 1 mole of dimethylacetamide solvent molecules, and the structural formula is as follows:

[0085] .

[0086] The new crystal form A of dexlansoprazole sodium of the present invention has characteristic diffraction patterns at diffraction angles 2θ of 5.9, 7.6, 12.2, 12.7, 16.6, 18.4, 20.5, 25.8, 26.8, and 31.4 degrees. Peak, where the error range of the 2θ value is ±0.2, the spectrum is attached to the manual figure 1 Shown.

[0087] The new crystal form A of dexlansoprazole sodium according to the present invention has a DSC chart with an endothermic characteristic peak at 132.4±1°C and an exothermic characteristic peak at 204.6±1°C. The chart is attached to the specification. figure 2 Shown.

[0088] The...

Embodiment 2

[0091] Example 2 Preparation of comparative crystal form 1

[0092] Refer to Example5 on page 15 of the specification in PCT patent WO2012095859A1 for preparation. 25g of dexlansoprazole was dissolved in 250mL of absolute ethanol, 32.5g of sodium isooctanoate was added, the reaction was stirred for 30min, the solvent was removed under reduced pressure, 250mL of n-heptane was added to the residue, stirred at room temperature for 3h, filtered and dried to obtain a comparison The crystal form 1 is about 18.5g.

Embodiment 3

[0093] Example 3 Preparation of comparative crystal form 2

[0094] Refer to Example 8 on page 16 of the specification in PCT patent WO2012095859A1 for preparation.

[0095] 10g of dextrolanoprazole was dissolved in a mixed solvent of 100mL of absolute ethanol and 5mL of water, cooled to -5°C, added 2.2g of sodium hydroxide, stirred at -5°C for 30min, and then added 80mL of n-heptane to the reaction solution. Stirring was continued for 30 minutes, and the solid was collected and dried to obtain about 6 g of comparative crystal form 2.

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
Diameteraaaaaaaaaa
Master granularityaaaaaaaaaa
Login to View More

Abstract

The invention belongs to the technical field of drug preparation, and particularly relates to a sustained release capsule of sodium dexlansoprazole prepared by hot melting extruding technique. The raw material drug for preparing the capsule is new crystal form A of dexlansoprazole, the PXRD atlas has diffraction absorbing peaks at the diffraction angles 2 theta of 5.9, 7.6, 12.2, 12.7, 16.6, 18.4, 20.5, 25.8, 26.8, and 31.4. The sustained release capsule comprises enteric-soluble immediate-release pellet A and enteric-soluble sustained-release pellet B; the content ratio of main drug of two pellets is about 1: 3 according to content of dexlansoprazole, and the two pellets are coated with enteric-soluble coatings with different pH value response, and thus the double control releases of two drug releases are reached, the sustained release capsule shell of sodium dexlansoprazole avoids damage of dexlansoprazole by gastric acid, and positions and releases it in a intestinal tract, so as to reach the purpose of rapidly taking effect and improving the bioavailability. The preparation technique of the capsule avoids the use of ethanol solvent coating, stops ethanol residue in a finished product; the preparation technique is advanced, the operation is simple, safe and free from pollution; therefore, the capsule is applicable to the major industrial production.

Description

Technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and specifically relates to a sustained-release capsule of dexlansoprazole sodium and a preparation method thereof. Background technique [0002] Dexlansoprazole (Dexlansoprazole, R-(+)-Lansoprazole), the chemical name is (R)-(+)-2-([3-methyl-4-(2,2,2-trifluoroethoxy (Yl)pyridin-2-yl]methylsulfinyl)-1H-benzimidazole, its structural formula is as follows, [0003] . [0004] Dexlansoprazole is a new drug for the treatment of esophagitis developed by Japan's Takeda Pharmaceutical Company. It was approved for marketing by the US FDA on January 30, 2009. The drug is a single enantiomer of the proton pump inhibitor lansoprazole. It is used to treat heartburn and various degrees of erosive esophagitis associated with non-erosive gastroesophageal reflux disease. It is more effective than lansoprazole. Bioavailability and fewer side effects. [0005] Dexlansoprazole belongs to the PPIs ant...

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): A61K31/4439A61K9/52A61K9/32A61K9/30A61K47/02A61K47/18A61K47/32A61P1/04
CPCA61K9/0002A61K9/2009A61K9/282A61K9/2853A61K9/4866A61K31/4439
Inventor 包玉胜闵涛徐丽袁尚陆晔枫叶海周桂梅刘飞
Owner NANJING HERON PHARM CO LTD
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