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Floating microgranules

A technology of floating particles and alkaline agent, applied in the direction of anti-inflammatory agents, microcapsules, non-central analgesics, etc., can solve the problems of affecting the floating effect, increasing the weight and volume of tablets, etc., to ensure the effect of long-term diffusion

Active Publication Date: 2015-03-11
DEBREGEAS & ASSOCIES PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0017] The systems described above necessitate the use of an acid / base pair with effervescent ability, which further increases tablet weight and bulk, thus ultimately compromising the desired flotation effect

Method used

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  • Floating microgranules
  • Floating microgranules
  • Floating microgranules

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0117] Embodiment 1: Floating granules based on furosemide

[0118]

[0119] Above-mentioned granule obtains by following operation steps:

[0120] First, an assembly step of pulverizing furosemide flexibility components onto a neutral carrier was carried out, while intermittent atomization of ethanol solution of povidone binder was carried out.

[0121] Then, add alkali agent (calcium carbonate and sodium bicarbonate) and paraffin compound on the granule prepared before Form the first coat.

[0122] Finally, with plasticizer (dibutyl sebacate) and coating agent An aqueous suspension of EC30D (aqueous ethylcellulose dispersion) treated the granules to form the second coating.

Embodiment 2

[0123] Example 2: Nifedipine-based floating granules

[0124]

[0125] Above-mentioned granule obtains by following operation steps:

[0126] First, an aqueous suspension comprising active ingredient (MOR 920) and binder (HPMC) is prepared.

[0127] Next, this suspension is atomized onto a carrier consisting of sodium bicarbonate (alkaline agent), followed by drying of the granules in a fluidized air bed.

[0128] Thereafter, with plasticizer (triethyl citrate), talcum powder, coating agent An aqueous suspension of FS30D and colorant was used to LP coat the previously obtained granules.

Embodiment 3

[0129] Example 3: Metformin-based floating granules

[0130]

[0131] Above-mentioned granule obtains by following operation steps:

[0132] First, assembly was performed by pulverizing the furosemide flexibility component onto a mannitol vehicle (Mannitol 400DC, Roquette (Roquette)) while intermittently atomizing an ethanol solution of the binder (Shellac-GLDB).

[0133] The granules are then dried in a fluidized air bed.

[0134] Thereafter, by precipitating alkaline agent (sodium bicarbonate), atomizing containing ethyl cellulose and Ethanol suspension of E100 coating agent, and application ATO5 (glyceryl palmitostearate) (Gattefosse) was used to coat the previously obtained granules.

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Abstract

The present invention relates to a floating granule comprising a solid core, on which an active ingredient is supported and also comprising a compound which is capable of generating a gas discharge which is constituted by an alkaline agent, characterized in that it does not comprise an acid agent which is capable of generating a gas discharge.

Description

technical field [0001] The invention relates to a floating microparticle and a preparation process thereof. Background technique [0002] Of all the routes of administration, the oral route is the best and therefore the most commonly used route in the therapeutic field. [0003] In this regard, the physiology of the digestive system has been extensively studied with the aim of optimally regulating the absorption and excretion phenomena of drug pharmacokinetics. [0004] Therefore, the digestive system has been simulated and studied according to different parameters (food transport, pH, surface area, presence of receptors or specific transport substances). Active ingredients in medicines are absorbed with extreme precision in the digestive tract according to their intrinsic physicochemical properties. [0005] In this way, depending on the desired effect, there are different oral forms: slow-release, delayed-release, bioadhesive, which allow the duration and location of the...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K47/38A61K47/36A61K47/34A61K47/32A61K47/26A61K47/02A61K45/00
CPCA61K9/5078A61K31/00A61K31/635A61K9/5026A61K9/0065A61K31/4422A61K31/155A61P29/00A61P3/00A61P7/00A61P7/10A61P9/00A61P9/12A61P3/10
Inventor 克里斯托弗·勒邦帕斯卡·祖普利
Owner DEBREGEAS & ASSOCIES PHARMA