Controlled release solid preparation

A technology of solid preparation and controlled release, which is applied in the direction of pill delivery, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., and can solve problems such as difficult pharmacological effects

Inactive Publication Date: 2009-03-18
TAKEDA PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it is difficult for these preparations to maintain the pharmacological effects over a long period of time

Method used

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  • Controlled release solid preparation
  • Controlled release solid preparation
  • Controlled release solid preparation

Examples

Experimental program
Comparison scheme
Effect test

preparation example 1

[0172] Preparation of Immediate Release Partial Granular Powders

[0173] Lansoprazole (hereinafter referred to as Compound A; 10 g), calcium carbonate (166.67 g) and D-mannitol (155.8 g) were loaded in a fluidized bed granulator, and hydroxypropyl cellulose ( 13.87 g) The mixture was granulated while spraying an aqueous solution in purified water (231.11 g), and then the granules were dried to obtain a granulated powder (340 g) for the immediate-release portion.

preparation example 2

[0175] Preparation of granular powders containing antacids

[0176] Magnesium hydroxide (96.67g), magnesium oxide (133.33g), D-mannitol (121.87g) and crospovidone (10.68g) were loaded in a fluidized bed granulator, and hydroxypropyl The mixture was granulated while cellulose (13.42 g) was sprayed in an aqueous solution in purified water (223.67 g), and then the granules were dried to obtain an antacid-containing granulated powder (370 g).

preparation example 3

[0178] Preparation of core particles

[0179] Core granules serving as the core of the sustained-release portion were prepared as follows. Hydroxypropylcellulose (HPC-SL, 50g) was dissolved in purified water (640g), and low-substituted hydroxypropylcellulose (L-HPC-32W, 25g) and magnesium carbonate (50g) were added to the solution and dispersed in it. Compound A (150 g) was uniformly dispersed in the resulting dispersion to obtain a coating solution. Lactose·crystalline cellulose particles (Nonpareil 105, 100 g) were coated with the compound A-containing coating solution (610 g) using a rotary fluidized bed coater (SPIR-A-FLOW, manufactured by Freund Industry Co., Ltd). . The coating conditions are: inlet air temperature: about 60°C, spray air pressure: about 1kgf / cm 2, exhaust pressure gauge: 100, BED pressure: about 250mmHg, rotor speed: about 300rpm, spray rate: about 6g / min, and spray gun position: lower side. After the coating operation was completed, the obtained fi...

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Abstract

Disclosed is a controlled release solid preparation which is excellent in stability of an active ingredient, can exert a pharmacological effect steadily and rapidly after administration and can retain the pharmacological effect for a prolonged period of time. The controlled release solid preparation comprises a combination of a rapid release part and a controlled release part, wherein the rapid release part comprises an antacid (1), a compound unstable under acidic conditions (2) and a basic substance and the controlled release part comprises a coating film comprising a compound unstable under acidic conditions (3) and a basic substance and capable of being dissolved at a pH value equal to or higher than 6.5.

Description

technical field [0001] The invention relates to a solid preparation. More specifically, the present invention relates to a controlled-release solid preparation, which has excellent stability of active ingredients, can exhibit pharmacological effects stably and rapidly after administration, and can exhibit sustained pharmacological effects over a long period of time. Background technique [0002] Since proton pump inhibitors (hereinafter sometimes referred to as PPIs) such as benzimidazole compounds (eg, lansoprazole, omeprazole, rabeprazole, pantoprazole, ilaprazole, etc.) have gastric acid Secretion-inhibiting action, gastric mucosa-protecting action, etc., they have been widely used as peptic ulcer therapeutic agents. [0003] However, these compounds have poor stability and are unstable to humidity, temperature, light, acid, and the like. These compounds are especially unstable to acids and become extremely unstable when the pH of their aqueous solutions or suspensions ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/26A61K9/14A61K31/4439A61K47/02A61K47/32A61K47/38A61P1/04A61P43/00
CPCA61K9/5078A61K9/5084A61K9/1652A61K9/2081A61K31/4439A61K9/1611A61K9/2077A61K9/1623A61K9/5026A61P1/04A61P1/18A61P25/34A61P3/10A61P43/00A61K9/20A61K47/32
Inventor 坂东博人仓泽卓
Owner TAKEDA PHARMA CO LTD
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