Fine granules containing acid-labile medicine and preparation thereof

A fine particle, acid-unstable technology, applied in the direction of pill delivery, emulsion delivery, liquid delivery, etc., can solve the problems of damage, destruction of enteric coating layer, rough feeling, etc.

Active Publication Date: 2006-09-06
SHANGHAI ALLIST PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, when the drug-containing granules are made into tablets (such as orally disintegrating tablets, dispersible tablets), the tableting process may destroy the enteric coating layer, resulting in a greatly reduced acid resistance
During the course of taking the medicine, sensitive

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Example 1: Preparation of omeprazole outer-coated enteric-coated granules

[0058] 1. Preparation of Drug-Containing Layer Granules

[0059] Add 600 g of Microcrystalline Cellulose Celphere CP-102 (particle size: 100-200 μm, Asahi Kasei, Japan) into the hopper of the fluidized bed (WBF-2 multifunctional fluidized bed granulation and coating machine, Chongqing Yingge). The inlet air temperature and outlet air temperature were controlled at 50°C and 31°C respectively, and the drug-containing layer coating liquid was sprayed and coated by bottom spraying process. After coating, dry for 10 minutes.

[0060] Coating liquid composition:

[0061] Omeprazole (micronized) 600g

[0062] Heavy Magnesium Carbonate 300g

[0063] HPMC (Pharmacoat 606) 300g

[0064] Distilled water 6000g

[0065] 2. Preparation of drug-containing granules with barrier layer

[0066] The drug-containing layer granules are wrapped with an isolation layer, the inlet air temperature and outlet air ...

Embodiment 2

[0104] Example 2: Preparation of pantoprazole outer-coated enteric-coated granules

[0105] 1. Preparation of drug-containing layer particles

[0106] Add 600 g of Microcrystalline Cellulose Celphere CP-102 (particle size: 100-200 μm, Asahi Kasei, Japan) into the hopper of the fluidized bed (WBF-2 multifunctional fluidized bed granulation and coating machine, Chongqing Yingge). The inlet air temperature and outlet air temperature were controlled at 50°C and 31°C respectively, and the drug-containing layer coating liquid was sprayed and coated by bottom spraying process. After coating, dry for 10 minutes.

[0107] Coating liquid composition:

[0108] Pantoprazole (micronized) 600g

[0109]Heavy Magnesium Carbonate 300g

[0110] HPMC (Pharmacoat 606) 300g

[0111] Distilled water 6000g

[0112] 2. Preparation of drug-containing granules with isolation layer

[0113] The drug-containing layer granules are wrapped with an isolation layer, the inlet air temperature and outle...

Embodiment 3

[0142] Example 3: Preparation of duloxetine outer-coated enteric-coated granules

[0143] 1. Preparation of drug-containing layer particles

[0144] Add 600 g of Microcrystalline Cellulose Celphere CP-102 (particle size: 100-200 μm, Asahi Kasei, Japan) into the hopper of the fluidized bed (WBF~2 multi-functional fluidized bed granulation and coating machine, Chongqing Yingge). The inlet air temperature and outlet air temperature were controlled at 50°C and 31°C respectively, and the drug-containing layer coating liquid was sprayed and coated by bottom spraying process. After coating, dry for 10 minutes.

[0145] Coating liquid composition:

[0146] Duloxetine 600g

[0147] HPMC (Pharmacoat 603) 300g

[0148] Distilled water 6000g

[0149] 2. Preparation of drug-containing granules with isolation layer

[0150] The drug-containing layer granules are wrapped with an isolation layer, the inlet air temperature and outlet air temperature are controlled at 50°C and 30°C respec...

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PUM

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Abstract

By coating one or more lagging covers outside the casing foil of acid-unstable drug, this invention obtains a fine acid-resistant micro-fine grain, whose mean particle diameter is 450ª–m or less. After undergoing oral pH environment and stomach acid environment, its acid-resistivity does not fall markedly, and also it has good mechanical-resistance. This invention also supplies agents of this casing foil grain, such as troche, dispersing agent and mixing agent. Material choosing of lagging cover brings marked effect to acid-resistant of micro-fine grain. The outer lagging cover can isolate the casing foil with dispersion medium or oral saliva environment, so as to avoid the casing foil dissolve in dispersion medium or oral. Coating one or more lagging covers outside the casing foil can also increase active mechanical-resistivity of constituent micro-fine grain, and it is more suitable in routine agents.

Description

technical field [0001] The present invention relates to a pharmaceutical form and describes a micronized particle containing an acid-labile active ingredient, in particular an acid-labile proton pump inhibitor, and a formulation thereof. Background technique [0002] Acid labile active ingredients such as erythromycin, duloxetine, benzimidazole proton pump inhibitors (H + / K + -ATPase inhibitors) are easily degraded in acidic and neutral media, but are stable in mixtures with basic compounds. With regard to the stability of such active substances, it is evident that they must be protected against contact with the acidic gastric juices. Proton pump inhibitors, especially the pyridin-2-ylmethylsulfinyl-1H-benzimidazole class of proton pump inhibitors, are very important for the treatment of conditions caused by increased gastric acid secretion. Examples of marketed active ingredients of this type are omeprazole, pantoprazole, lansoprazole and rabeprazole. The aforementione...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K9/20A61K9/10
Inventor 郭建辉杜志永李素华
Owner SHANGHAI ALLIST PHARM CO LTD
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