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Esomeprazole magnesium pulse pellet capsule and preparation method thereof

A technology of esomeprazole magnesium and pulse pellets, which is applied in the field of medicine, can solve problems such as the inability to release gastric acid rhythmically and patients' nocturnal acid breakthrough, and achieve the effects of prolonging drug residence time, flexible behavior adjustment, and low side effects

Pending Publication Date: 2020-11-27
青岛吉达巴尔国际贸易有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the current formulation of esomeprazole magnesium pellets cannot target the rhythmic release of gastric acid, so that patients experience nocturnal acid breakthrough

Method used

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  • Esomeprazole magnesium pulse pellet capsule and preparation method thereof
  • Esomeprazole magnesium pulse pellet capsule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] (1) Preparation of esomeprazole magnesium-containing pill core:

[0038] prescription:

[0039] blank core 75.0 g Esomeprazole Magnesium 10.0 g (calculated as esomeprazole) microcrystalline cellulose 7.5 g sucrose 17.5 g magnesium carbonate 4.0 g Low-substituted hydroxypropyl cellulose 1.2 g 3% HPMC E5 aqueous solution 20mL

[0040]Esomeprazole magnesium, microcrystalline cellulose, sucrose, magnesium carbonate, and low-substituted hydroxypropyl cellulose in the prescribed amount are respectively passed through an 80-mesh sieve, and then added and mixed uniformly in equal amounts. Take the blank pellet core and put it in the centrifugal granulator, set the process parameters and run the machine, the parameters are the wheel speed 200rpm, the blast frequency 25 Hz, the spray pressure 0.16 Mpa, the spray speed 3.5 mL / min, set the gear The position of the plate makes the blank ball core move in the shape of hemp rope an...

Embodiment 2

[0057] (1) Preparation of esomeprazole magnesium-containing pill core:

[0058] prescription:

[0059] blank core 150.0 g Esomeprazole Magnesium 20.0 g (calculated as esomeprazole) microcrystalline cellulose 15.0 g sucrose 35.0 g magnesium carbonate 8.0 g Low-substituted hydroxypropyl cellulose 2.4 g 3% HPMC E5 aqueous solution 30mL

[0060] Esomeprazole magnesium, microcrystalline cellulose, sucrose, magnesium carbonate, and low-substituted hydroxypropyl cellulose in the prescribed amount are respectively passed through an 80-mesh sieve, and then added and mixed uniformly in equal amounts. Take the blank pellet core and put it in the centrifugal granulator, set the process parameters and run the machine, the parameters are the wheel speed 200rpm, the blast frequency 25 Hz, the spray pressure 0.16 Mpa, the spray speed 3.5 mL / min, set the gear The position of the plate makes the blank ball core move in the shape of hemp rope...

Embodiment 3

[0076] (1) Preparation of esomeprazole magnesium-containing pill core:

[0077] prescription:

[0078] blank core 300.0 g Esomeprazole Magnesium 40.0 g (calculated as esomeprazole) microcrystalline cellulose 30.0 g sucrose 70.0 g magnesium carbonate 16.0 g Low-substituted hydroxypropyl cellulose 4.8 g 3% HPMC E5 aqueous solution 50mL

[0079] Esomeprazole magnesium, microcrystalline cellulose, sucrose, magnesium carbonate, and low-substituted hydroxypropyl cellulose in the prescribed amount are respectively passed through an 80-mesh sieve, and then added and mixed uniformly in equal amounts. Take the blank pellet core and put it in the centrifugal granulator, set the process parameters and run the machine, the parameters are the wheel speed 200rpm, the blast frequency 30 Hz, the spray pressure 0.16 Mpa, the spray speed 3.5 mL / min, set the gear The position of the plate makes the blank ball core move in the shape of hemp rop...

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Abstract

The invention relates to an esomeprazole magnesium pulse pellet capsule and a preparation method thereof. The esomeprazole magnesium pulse pellet capsule is composed of an active pharmaceutical ingredient esomeprazole magnesium and other pharmaceutically acceptable auxiliary materials. The esomeprazole magnesium pulse pellet capsule is composed of two different pH-dependent enteric-coated pellets,wherein the enteric-coated pellet I is prepared by sequentially coating an esomeprazole magnesium drug-containing pellet core with an isolating layer I and an enteric-coated layer I; and the enteric-coated pellet II is prepared by sequentially coating an esomeprazole magnesium medicine-containing pellet core with an isolating layer II and an enteric-coated layer II. The invention has the following advantages: aiming at the rhythmicity of gastric acid secretion time, according to the principle of chronodynamics, the pellet for pulse release of drugs twice is designed, and the pellet is dosed once a day to maintain a good acid inhibition effect at night; the drug is sequentially released in the intestinal tract twice in a pulse manner, so that the drug retention time is prolonged, and the bioavailability is improved; the pulsatile preparation is prepared in a pellet form, the cost is low, the drug release behavior is flexible to adjust, and the blood concentration fluctuation is small.

Description

technical field [0001] The invention relates to an esomeprazole magnesium pulse capsule and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Esomeprazole magnesium trihydrate, English name: Esomeprazole magnesium trihydrate, chemical name: bis(5-methoxy-2-[(S)-[(4-methoxy-3,5-dimethyl -2-pyridyl)methyl]sulfinyl]-1H-benzimidazol-1-yl)magnesium salt trihydrate. Its physical and chemical properties are stable under weak alkaline conditions and easy to degrade in acidic environments. Molecular weight: 767.2, chemical structural formula: [0003] . [0004] Esomeprazole magnesium is the S-isomer of omeprazole, which can inhibit gastric acid secretion by specifically targeting gastric parietal cells and activating it into an active achiral sulfinamide, binding to H+ / K+-ATPase. It is suitable for symptom control and long-term treatment of gastroesophageal reflux venereal disease; combined with appropriate antimicrobial ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K9/48A61K47/38A61K47/32A61K31/4439A61P1/04
CPCA61K9/5042A61K9/5026A61K9/0002A61K31/4439A61P1/04
Inventor 黄桂华崔美兰许飞黄英豪王惠瑾贾情情张海涛王华轩
Owner 青岛吉达巴尔国际贸易有限公司
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