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Dextrorotation lansoprazole diphasic spansule preparation and preparing method thereof

A dual- and sustained-release technology for dexlansoprazole, which is applied in pharmaceutical formulations, drug delivery, and the digestive system, and can solve the problems of low process feasibility, instability of dexlansoprazole in acid, and unstable release rate And other issues

Inactive Publication Date: 2015-09-30
HEFEI HUAFANG PHARMA SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This patent adopts the general enteric-coated pellet technology, which has certain disadvantages: 1. D-lansoprazole is slightly soluble in water and soluble in ethanol. It is easy to form a thick colloid when it is made into a solution, and the process is feasible. Low
2. Dexlansoprazole itself is unstable and is very sensitive to heat and humidity. If the fluidized bed bottom spraying process is adopted, the main drug needs to be prepared in an aqueous solution and stirred on a fluidized bed to put on sugar pills. The process cycle is longer. It has low stability in the aqueous solution under stirring for a long time
[0008] Dexlansoprazole itself is unstable in case of acid, and if it is made into a common preparation and released in the stomach, it is easily destroyed by acid
However, the general enteric coating layer is generally acidic, so it is necessary to coat a layer of isolation layer before coating the functional coating, and the release rate of ordinary enteric coated tablets in the gastrointestinal tract is unstable and the bioavailability is low.

Method used

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  • Dextrorotation lansoprazole diphasic spansule preparation and preparing method thereof
  • Dextrorotation lansoprazole diphasic spansule preparation and preparing method thereof
  • Dextrorotation lansoprazole diphasic spansule preparation and preparing method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] Embodiment 1: Formulation 1

[0067]

[0068]

[0069] Preparation method:

[0070] 1. According to formula 1, mix dexlansoprazole with sucrose and starch and ball mill it at a speed of 20 rpm for 3 hours, and pass through a 200-mesh sieve to obtain the main drug mixed powder;

[0071] 2. Mix the ball-milled main drug mixed powder with low-substituted hydroxypropyl cellulose and magnesium carbonate according to formula 1 to obtain the drug mixed powder;

[0072] 3. Prepare the adhesive solution according to formula 1 and set aside;

[0073] 4. Using a centrifugal granulator, the speed of feeding the powder and the speed of the binder solution are 2:1, while inhaling the mixed powder of the drug and spraying the binder solution on the side to apply the drug to the blank pellet core, and then drying and sieving to increase the weight 340%, get the pill core;

[0074] 5. Prepare the isolation layer solution according to formula 1, use the fluidized bed bottom spra...

Embodiment 2

[0078] Embodiment 2: Recipe 2

[0079]

[0080]

[0081] Preparation method:

[0082] 1. Mix dexlansoprazole with sucrose and microcrystalline cellulose according to formula 2 and ball mill it at a speed of 30 rpm for 4 hours, and pass through a 200-mesh sieve to obtain the main drug mixed powder;

[0083] 2. Mix the ball-milled main drug mixed powder with low-substituted hydroxypropyl cellulose and sodium bicarbonate evenly according to formula 2 to obtain the drug mixed powder;

[0084] 3. Prepare the adhesive solution according to formula 2, and set aside;

[0085] 4. Use a centrifugal granulator to apply medicine to the blank pill core at a rate of 2:1 between the powder feeding speed and the binder solution feeding speed, dry and sieve, and increase the weight by 320%, and the pill core is obtained;

[0086] 5. Prepare the isolation layer solution according to formula 2, use the fluidized bed bottom spray method to coat the isolation layer on the upper pill core, ...

Embodiment 3

[0090] Embodiment 3: formula 3

[0091]

[0092]

[0093] Preparation method:

[0094] 1. According to formula 3, mix dexlansoprazole with lactose and microcrystalline cellulose and ball mill for 5 hours at a speed of 40 rpm, and pass through a 200-mesh sieve to obtain the main drug mixed powder;

[0095] 2. Mix the ball-milled main drug mixed powder with low-substituted hydroxypropyl cellulose and sodium bicarbonate evenly according to formula 3 to obtain the drug mixed powder;

[0096] 3. Prepare the adhesive solution according to formula 3 and set aside;

[0097] 4. Use a centrifugal granulator to apply medicine to the blank pellet core at a rate of 2:1 between the powder feed rate and the binder solution feed rate, dry and sieve, increase the weight by 250%, and get the pill core;

[0098] 5. Prepare the isolation layer solution according to formula 3, use the fluidized bed bottom spray method to coat the isolation layer on the upper pill core, dry and sieve to obt...

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Abstract

The invention belongs to the pharmacy field, and particularly relates to a dextrorotation lansoprazole diphasic spansule preparation and a preparing method thereof. According to the method, drug applying is carried out through the ball grinding technology and a centrifugal granulator, and the dextrorotation lansoprazole diphasic spansule preparation has good stability and a high releasing rate.

Description

technical field [0001] The invention belongs to the field of pharmacy. Specifically, the present invention relates to a biphasic sustained-release capsule preparation of dexlansoprazole and a preparation method thereof. Background technique [0002] The molecular formula of dexlansoprazole is C 16 h 14 f 3 N 3 o 2 S, the chemical name is: (+)-2-[(R)-[3-methyl-4-(2,2,2-trifluoroethoxy)-2pyridyl]methyl]-1H-benzene And imidazole. [0003] Dexlansoprazole is easily soluble in methanol, insoluble in water, and soluble in other organic solvents such as ethanol. It is very unstable under hot and humid conditions, and it is very easy to react and change color when encountering acid. [0004] The proton pump (proton pump) is a hydrogen ion ATPase (H+-K+-ATPase), which can convert H in gastric parietal cells + pumped out to the gastric cavity, while extracellular K + pumped into the gastric parietal cells. Therefore, the proton pump is the common and final link in the abnorm...

Claims

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Application Information

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IPC IPC(8): A61K9/52A61K31/4439A61P1/04
Inventor 吴宗好周小兴孙立云何勇陈玉洁李春妮
Owner HEFEI HUAFANG PHARMA SCI & TECH
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