Process for granulating particles

A granulation and granulation technology, which is applied in pharmaceutical formulation, powder suspension granulation, drug combination, etc., can solve problems such as confusion, narrow injection area, and uncontrolled exposure

Inactive Publication Date: 2007-11-21
MERCK & CO INC +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This is because the sparged zone is narrower than the full solid bed in conventional methods
Furthermore, the exposure of solid particles in the spray zone is uncontrolled and chaotic in the conventional method compared to the orderly recirculation method in the Wurster granulation process

Method used

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  • Process for granulating particles
  • Process for granulating particles
  • Process for granulating particles

Examples

Experimental program
Comparison scheme
Effect test

preparation Embodiment 1

[0062] Coated etoricoxib microspheres

[0063] Coated etoricoxib microspheres were prepared by the methods described in U.S. No. 5,683,720, issued November 4, 1997, and U.S. No. 5,849,223, issued December 15, 1998, both of which are hereby incorporated by reference in their entirety This article. The composition of coated etoricoxib microspheres comprises:

[0064] (1) about 19% wt / wt etoricoxib, about 46% wt / wt distilled monoglyceride 03-VF and about 12% wt / wt ground Gelucire 50 / 13 (mixed before flash liquefaction process) ;and

[0065] (2) About 9% wt / wt Eudragit(R) NE30D, about 2% wt / wt Methocel and about 12% wt / wt microtalc 1538 (coating).

Embodiment l

[0067] Granulation of beads containing API cores with powder excipient (etoricoxib pediatric formulation)

[0068] Batches of 1.5 kg of etoricoxib oral granules were obtained by granulation in a Glatt GPCG3GPCG3 fluidized bed column fitted with a Wurster insert. Get the pre-mixture of the etoricoxib taste-masking microspheres (237 microns in volume mean diameter) and 742.5 g of mannitol (Pearlitol SD200) (137 microns in volume mean diameter) that comprise 585g and pack into the column and fluidize, take 8 A solution of % w / w hydroxypropyl cellulose (Klucel LF), 2.5% w / w artificial cherry flavor and 1% w / w aspartame was sprayed from below onto the separate part of the Wurster column. The inlet flow rate is varied during granulation to ensure proper particle flow pattern throughout the granulation process. The final product had a volume mean diameter of 799 microns as determined by laser diffraction. Scanning electron microscopy of the initial premix and final particles demons...

Embodiment 2

[0070] Granulation of excipient beads with powder excipients (granulation of pharmaceutical ingredients with different physical properties)

[0071] 1.5 kg and 10 kg of granules containing 39% sugar spheres (top grade) and 49.5% mannitol (Pearlitol SD200) were obtained in Glatt GPCG3GPCG3 and GPCG15GPCG15 fluidized bed columns, respectively. The fluidized bed was fitted with a Wurster insert and charged and fluidized with a premix containing 40-60 mesh sugar spheres and mannitol (Pearlitol SD200) (137 microns in volume mean diameter) while taking 8% w / w hydroxyl A solution of propylcellulose (Klucel LF), 2.5% w / w artificial cherry flavor and 1% w / w aspartame was sprayed from below onto the divided part of the Wurster column. The inlet flow rate is varied during granulation to ensure proper particle flow pattern throughout the granulation process. The final product of this batch had a volume average diameter of 750 to 800 microns as determined by laser diffraction. Scanning e...

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Abstract

The invention encompasses a process for granulating particles that produces homogeneous, free flowing, attrition resistant, uniform sized granules. When utilized with active pharmaceutical ingredients, such granules can be further processed into controlled released or taste-masked pharmaceutical formulations. Particularly, the process can be utilized to make an oral granule formulation of etoricoxib for treating pain and inflammation in patients that cannot swallow a tablet, such as young children and the elderly.

Description

Background of the invention [0001] Wurster unit operations are typically used in the pharmaceutical industry to apply a coating to a substrate. The Wurster unit consists of two concentric cylinders on a distribution plate, an insert and an annulus. The solid to be coated is loaded into the ring. After gas flow is initiated, the solids on the annulus pass through the partition gap and are transported by air into the insert. The coating solution is sprayed through nozzles onto the distribution plate, coating the solids flowing in the insert. The solids lose momentum in the ejection zone and fall onto the annulus where they travel down the annulus and back into the insert. The deposited coating dries mainly in the insert and spray zones. Continue this recirculation until the desired coat weight is achieved. [0002] The present invention relates to a Wurster granulation process, which is a process for granulating pharmaceutical ingredients by operating a Wurster unit above t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/22A61K9/26A61K9/50B05D7/00
CPCA61K9/1652A61K9/2081B01J2/16A61K9/5026A61P29/00
Inventor J·S·侯H·迪蒙C·曼奇内利S·D·谢卢卡
Owner MERCK & CO INC
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