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

Dexlansoprazole sustained release capsule and preparation method thereof

A technology of lansoprazole late and dexlansoprazole, which is applied in the field of dexlansoprazole delayed-release capsules and its preparation, can solve the problem that the stability is susceptible to light, heavy metal ions, oxidizing and reducing components, etc. Influence of various factors, reduction of drug onset speed and bioavailability, changes in the chemical structure of dexlansoprazole, etc., to achieve the effects of high predictability of drug efficacy, improvement of bioavailability, and enhanced solubility

Active Publication Date: 2012-07-25
乐普药业科技有限公司
View PDF2 Cites 12 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Dexlansoprazole belongs to the prazole class of PPIs antiulcer drugs. There is a chemical structure of sulfinylbenzimidazole in the structure of dexlansoprazole, and its stability is easily affected by light, heavy metal ions, oxidizing and reducing components, etc. The impact of these factors, especially in acidic conditions, the chemical structure of dexlansoprazole can undergo destructive changes, discoloration and polymerization, so dexlansoprazole is unstable in acidic diluents, and it is made into oral After preparation, drug absorption needs to go through the process of drug disintegration and release, and the gastric acid in the stomach leads to the destruction and decomposition of dexlansoprazole, which reduces the speed of drug onset and bioavailability. How to make dexlansoprazole capsules mainly in the intestinal tract Environmental release is the key

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
  • Dexlansoprazole sustained release capsule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Dexlansoprazole delayed-release capsules, two kinds of micropills are installed in the capsule, the mass ratio of the first kind of micropills to the second kind of micropills (based on dexlansoprazole) is 1:3;

[0043] The first micropill is successively a blank core, a drug-containing layer, an isolation layer and an enteric coating layer from the inside to the outside, and the mass parts of the blank core are 800 parts, and the composition and mass parts of the drug-containing layer are dexlansoprazole: 300 copies,

[0044] Sodium hydroxide: 16 parts,

[0045] Tween 80: 5 servings,

[0046] Sodium carboxymethyl starch: 50 parts,

[0047] Colloidal silica: 20 parts,

[0048] Hypromellose: 200 parts,

[0049] The composition and mass parts of the isolation layer are hypromellose: 50 parts,

[0050] Tween 80: 6 servings,

[0051] Titanium dioxide: 6 parts,

[0052] Macrogol 8000: 10 parts,

[0053] The composition and mass parts of the casing layer are methacryl...

Embodiment 2

[0062] Dexlansoprazole delayed-release capsules, two kinds of micropills are installed in the capsule, the mass ratio of the first kind of micropills to the second kind of micropills (based on dexlansoprazole) is 1:3;

[0063] The first micropill is successively a blank core, a drug-containing layer, an isolation layer and an enteric coating layer from the inside to the outside, and the mass parts of the blank core are 800 parts, and the composition and mass parts of the drug-containing layer are dexlansoprazole: 300 copies,

[0064] Magnesium hydroxide: 5 parts,

[0065] Poloxamer: 1 part,

[0066] Microcrystalline cellulose: 200 parts,

[0067] Magnesium stearate: 5 parts,

[0068] Polyvinylpyrrolidone: 50 parts,

[0069] The composition and mass parts of isolation layer are polyvinylpyrrolidone: 30 parts,

[0070] Poloxamer: 3 parts,

[0071] Titanium dioxide: 3 parts,

[0072] Micronized silica gel: 5 parts,

[0073]The composition and mass parts of the casing laye...

Embodiment 3

[0082] Dexlansoprazole delayed-release capsules, two kinds of micropills are installed in the capsule, the mass ratio of the first kind of micropills to the second kind of micropills (based on dexlansoprazole) is 1:4;

[0083] The first micropill is successively a blank core, a drug-containing layer, an isolation layer and an enteric coating layer from the inside to the outside, and the mass parts of the blank core are 800 parts, and the composition and mass parts of the drug-containing layer are dexlansoprazole: 300 copies,

[0084] Sodium carbonate: 20 parts,

[0085] Tween 80: 3 servings,

[0086] Low-substituted hydroxypropyl cellulose: 100 parts,

[0087] Talcum powder: 30 parts,

[0088] Dextrin: 300 parts,

[0089] The composition and mass parts of isolation layer are dextrin: 60 parts,

[0090] Tween 80: 10 servings,

[0091] Titanium dioxide: 8 parts,

[0092] Talc powder: 8 parts,

[0093] The composition and mass parts of the casing layer are methacrylic aci...

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

No PUM Login to View More

Abstract

The invention belongs to the technical field of pharmaceutical preparation, and particularly relates to a dexlansoprazole sustained release capsule and a preparation method thereof. Two kinds of pellets are arranged in the capsule, and the weight ratio of dexlansoprazole contained in the first kind of pellets and the second kind of pellets is 1:3-4. The dexlansoprazole sustained release capsule disclosed by the invention can avoid the destruction of the dexlansoprazole in gastric acid, and is released in the intestinal tract in a fixed position so as to achieve the purposes of taking effect rapidly and improving bioavailability.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to a delayed-release capsule of dexlansoprazole and a preparation method thereof. Background technique [0002] The molecular formula of dexlansoprazole is: [0003] [0004] Chemical name: (+)-2-[(R)-[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl]sulfinyl] -1H-benzimidazole. [0005] Dexlansoprazole is a newly developed proton pump inhibitor anti-ulcer drug. Its oral preparation is developed by Takeda Pharmaceutical Company in Japan. Its trade name is Kapilax. It can continuously inhibit gastric acid secretion, so it can improve GERD symptoms. The effect is significant and tolerated In January 2009, it was approved by the US FDA for the "heartburn" symptoms and erosive esophagitis caused by non-erosive GERD, as well as for the maintenance treatment of erosive esophagitis. [0006] Dexlansoprazole belongs to the prazole class of PPIs antiulcer drugs....

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 Applications(China)
IPC IPC(8): A61K9/64A61K9/62A61K9/58A61K31/4439A61P1/04
Inventor 张克军王庆鹏马可鸿杨永霞魏巧
Owner 乐普药业科技有限公司
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